Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID) that is used to treat pain, fever, and inflammation. It is typically prescribed for conditions such as rheumatoid arthritis, osteoarthritis, and gout. The drug was first synthesized in 1963 by scientists at Merck & Co., and it was approved for medical use in 1965. Indomethacin works by blocking the production of prostaglandins, which are chemicals in the body that contribute to pain and inflammation. The drug has been shown to be effective in reducing pain and inflammation, but it can also cause side effects such as stomach ulcers, heartburn, and gastrointestinal bleeding. Due to its efficacy in reducing inflammation and pain, indomethacin is studied extensively for its potential therapeutic benefits in various other conditions, including Alzheimer's disease, cancer, and cardiovascular disease.'
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
ID Source | ID |
---|---|
PubMed CID | 3715 |
CHEMBL ID | 6 |
CHEBI ID | 49662 |
SCHEMBL ID | 9300 |
MeSH ID | M0011240 |
Synonym |
---|
nsc77541 |
nsc-77541 |
BIDD:GT0132 |
AC-532 |
S00108 |
MLS001074194 |
HMS3268A14 |
AB00052022-20 |
AB00052022-21 |
BRD-K57222227-001-06-1 |
gtpl1909 |
KBIO1_000271 |
DIVK1C_000271 |
NCI60_041708 |
[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indol-3-yl]acetic acid |
EU-0100692 |
indomethacin, >=99% (tlc) |
indometacin (jp17/inn) |
aconip (tn) |
indocin (tn) |
D00141 |
indomethacin (usp) |
SPECTRUM_000919 |
LOPAC0_000692 |
BSPBIO_002176 |
PRESTWICK_597 |
BIO2_000405 |
lopac-i-7378 |
NCGC00015562-02 |
tocris-1708 |
cas-53-86-1 |
NCGC00024135-02 |
NCGC00015562-01 |
BIO2_000885 |
BSPBIO_000144 |
BPBIO1_000160 |
PRESTWICK3_000272 |
NCGC00024135-11 |
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indole-3-acetic acid |
metindol |
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indole-3-acetic acid & map-30 |
tannex |
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-indol-3-yl]acetic acid |
imbrilon |
indomethacin & map-30 |
SPECTRUM5_000868 |
PRESTWICK2_000272 |
BSPBIO_001149 |
indacin |
artrinovo |
mikametan |
sadoreum |
vonum |
metartril |
catlep |
indomo |
indo-tablinen |
inacid |
indo-spray |
bonidon |
indocid (pharmaceutical) |
1h-indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl- (9ci) |
durametacin |
metacen |
lausit |
artrivia |
inteban sp |
flexin continus |
indocin |
indmethacine |
indomed |
dolcidium |
1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid |
1-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indoleacetic acid |
indocid |
1h-indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl- |
inflazon |
arthrexin |
indole-3-acetic acid, 1-(p-chlorobenzoyl)-5-methoxy-2-methyl- |
indoptic |
indole-3-acetic acid, 1-(p-chlorobenzoyl)-5-methoxy-2-methyl- (8ci) |
ccris 3502 |
indomee |
rheumacin la |
usan |
indoptol |
confortid |
dolcidium pl |
infrocin |
IMN , |
hicin |
chrono-indocid |
idomethine |
indorektal |
artracin |
1-(p-chlorobenzoyl)-2-methoxy-3-methyl-1h-indole-3-acetic acid |
hsdb 3101 |
mobilan |
1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid |
indolar sr |
indo-phlogont |
chibro-amuno |
amuno |
methazine |
indameth |
mezolin |
alpha-(1-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indolyl)acetic acid |
indomecol |
elmetacin |
dolovin |
indomethazine |
indo-rectolmin |
indomethacinum |
indometacine |
1-(p-chlorobenzoyl)-2-methyl-5-methoxyindole-3-acetic acid |
reumacide |
indoxen |
bonidon gel |
NCGC00024135-04 |
UPCMLD-DP023:001 |
BIM-0050670.0001 |
AB00052022 |
brn 0497341 |
indometacina [inn-spanish] |
n-p-chlorbenzoyl-5-methoxy-2-methylindole-3-acetic acid |
indometicina [spanish] |
indometacyna [polish] |
(1-p-chlorobenzoyl-5-methoxy-2-methylindol-3-yl)acetic acid |
1-p-cloro-benzoil-5-metoxi-2-metilindol-3-acido acetico [spanish] |
einecs 200-186-5 |
indocin sr |
1-(p-chlorbenzoyl)-5-methoxy-2-methylindol-3-essigsaeure [german] |
indometacinum [inn-latin] |
indomet 140 |
indo-lemmon |
indometacine [inn-french] |
indomethacine |
nci-c56144 |
kwas 1-(p-chlorobenzoilo)-2-metylo-5-metoksy-3-indolilooctowy [polish] |
53-86-1 |
indometacin |
indomethacin |
C01926 |
indomethacin, meets usp testing specifications |
{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1h-indol-3-yl}acetic acid |
DB00328 |
1Z9H |
UPCMLD-DP023 |
IDI1_002160 |
OPREA1_686105 |
NCGC00024135-06 |
NCGC00024135-07 |
NCGC00024135-08 |
smr000058195 |
MLS000069402 , |
KBIO2_003967 |
KBIO3_001396 |
KBIOSS_001399 |
KBIO3_000897 |
KBIO2_001399 |
KBIO2_003057 |
KBIOSS_000489 |
KBIOGR_000395 |
KBIO3_000898 |
KBIO2_005625 |
MOLMAP_000032 |
KBIO2_000489 |
KBIO2_006535 |
KBIOGR_000489 |
SPECTRUM4_000018 |
SPBIO_000979 |
PRESTWICK1_000272 |
NINDS_000271 |
SPECTRUM2_000970 |
SPECTRUM3_000468 |
PRESTWICK0_000272 |
SPBIO_002363 |
SPECTRUM1500350 |
IDI1_000271 |
NCGC00024135-09 |
NCGC00015562-03 |
NCGC00024135-05 |
chembl6 , |
bdbm17638 |
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1h-indol-3-yl}acetic acid |
aconip |
indometacinum |
indometacina |
CHEBI:49662 , |
NCGC00015562-08 |
HMS2091N09 |
HMS2089N19 |
I 7378 , |
HMS1990I11 |
I0655 |
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetic acid |
NCGC00015562-19 |
L000959 |
nsc-757061 |
AKOS000592893 |
HMS1792I11 |
HMS500N13 |
HMS1362I11 |
inchi=1/c19h16clno4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9h,10h2,1-2h3,(h,22,23) |
cgigdmfjxjatdk-uhfffaoysa- |
HMS1920F21 |
HMS1568H06 |
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid |
NCGC00024135-13 |
NCGC00024135-12 |
NCGC00024135-14 |
NCGC00024135-10 |
NCGC00024135-15 |
HMS2095H06 |
HMS3262K05 |
1-(p-chlorobenzoyl)-5-methoxy-2-methyl-indole-3-acetic acid |
NCGC00259340-01 |
tox21_300266 |
dtxsid9020740 , |
dtxcid50740 |
NCGC00254075-01 |
tox21_113109 |
tox21_201791 |
nsc757061 |
pharmakon1600-01500350 |
STL257874 |
chrono-indicid |
bonidin |
indomod |
indomethine |
indomethancin |
miametan |
indocin-sr |
indochron e-r |
HMS2231J10 |
CCG-40186 |
NCGC00015562-10 |
NCGC00015562-21 |
NCGC00015562-13 |
NCGC00015562-15 |
NCGC00015562-07 |
NCGC00015562-17 |
NCGC00015562-22 |
NCGC00015562-11 |
NCGC00015562-20 |
NCGC00015562-04 |
NCGC00015562-16 |
NCGC00015562-14 |
NCGC00015562-05 |
NCGC00015562-06 |
NCGC00015562-12 |
NCGC00015562-18 |
NCGC00015562-09 |
nsc 757061 |
indometacyna |
ec 200-186-5 |
flam |
indometicina |
1-p-cloro-benzoil-5-metoxi-2-metilindol-3-acido acetico |
indomethacin [usan:usp] |
tivorbex |
5-22-05-00239 (beilstein handbook reference) |
1-(p-chlorbenzoyl)-5-methoxy-2-methylindol-3-essigsaeure |
xxe1cet956 , |
kwas 1-(p-chlorobenzoilo)-2-metylo-5-metoksy-3-indolilooctowy |
unii-xxe1cet956 |
indometacin [inn] |
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methylindol-3-yl}acetic acid |
FT-0603227 |
NCGC00015562-24 |
LP00692 |
indomethacin [usan] |
indomethacin [hsdb] |
indometacin [who-dd] |
indometacin [who-ip] |
indometacinum [who-ip latin] |
indomethacin [orange book] |
indomethacin [mi] |
acemetacin impurity b [ep impurity] |
indometacin [ep monograph] |
indomethacin [usp-rs] |
indometacin [mart.] |
indomethacin [usp monograph] |
indomethacin [vandf] |
(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indol-3-yl)acetic acid |
indometacin [jan] |
4KYK |
S1723 |
HMS3374F07 |
BP-30207 |
HY-14397 |
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2methylindol-3-yl}acetic acid |
2-{1-((4-chlorophenyl)carbonyl)-5-methoxy-2-methylindol-3-yl}acetic acid |
1-(4-chloro-benzoyl)-5-methoxy-2-methyl-3-indolyl-acetic acid |
2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indol-3-yl)acetic acid |
1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indol acetic acid |
1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetic acid |
1-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indolylacetic acid |
1-(4-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid |
1-p-chlorobenzoyl-2-methyl-5-methoxyindol-3-acetic acid |
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2 methylindol-3-yl}acetic acid |
SCHEMBL9300 |
tox21_113109_1 |
NCGC00015562-25 |
KS-5255 |
NCGC00261377-01 |
tox21_500692 |
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indol-3-yl]acetic acid |
inteban |
1-(p-chlorobenzoyl)-5-methoxy-2-methylindol-3-acetic acid |
innamit |
n-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indolylacetic acid |
indocollyre |
1-(4-chlorobenzoyl)-2-methyl-5-methoxyindole-3-acetic acid |
1-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indole-acetic acid |
.alpha.-(1-(p-chlorobenzoyl)-2-methyl-5-methoxy-3-indolyl)acetic acid |
indonol |
[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1h-indol-3-yl]acetic acid # |
MLS006011845 |
indomethacin, antibiotic for culture media use only |
Q-201239 |
HB4422 |
1-(4-chlorobenzoyl)-5-methoxy-2-met hyl-1h-indole |
HMS3649K17 |
HMS3403I11 |
HMS3430L03 |
OPERA_ID_56 |
AB00052022_24 |
AB00052022_23 |
mfcd00057095 |
indomethacin, united states pharmacopeia (usp) reference standard |
indomethacin, >=99.0% (tlc) |
indomethacin, european pharmacopoeia (ep) reference standard |
HMS3655O04 |
AT13679 |
indomethacin, pharmaceutical secondary standard; certified reference material |
indometacin 1.0 mg/ml in acetonitrile |
SR-01000000014-4 |
SR-01000000014-2 |
sr-01000000014 |
SR-01000000014-6 |
SR-01000000014-10 |
SBI-0050670.P004 |
HMS3712H06 |
Z56784896 |
SW196768-5 |
BCP18951 |
indomethacin - cas 53-86-1 |
indomethacin (indocid, indocin) |
HMS3678N11 |
indomethacin,(s) |
SR-01000000014-16 |
HMS3414N13 |
Q409231 |
BRD-K57222227-001-18-6 |
BRD-K57222227-001-27-7 |
SDCCGSBI-0050670.P005 |
NCGC00015562-40 |
HMS3884E08 |
HMS3747K21 |
indomethacin-d4(chlorobenzoyl-d4) |
EN300-16807 |
indomethacine impurity mixture |
BI166166 |
indometacina (inn-spanish) |
indometacine (inn-french) |
indomethacin extended-release |
acemetacin impurity b (ep impurity) |
indometacin (mart.) |
indomethaciner |
s01bc01 |
indometacin (ep monograph) |
m02aa23 |
indomethacin (usp monograph) |
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1-h-indole-3-acetic acid |
c01eb03 |
indometacinum (inn-latin) |
indomethacin (usp-rs) |
(1-((4-chlorophenyl)carbonyl)-5-methoxy-2-methyl-1h-indol-3-yl)acetic acid |
chrono-indocid 75 |
indomethacin (usan:usp) |
indomethacin er |
n-p-chlorobenzoyl-5-methoxy-2-methylindole-3-acetic acid |
indren |
m01ab01 |
indometacinum (latin) |
Indomethacin is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase inhibitor. It is frequently used as a research tool to study the process of adipocyte differentiation. IndomethAcin is an important medication in the headache medicine toolbox.
Indomethacin has a moderately short half-life, usually requiring dosing twice a day or three times a day. It has a protective effect on the incidence of intraventricular hemorrhage (IVH) but reduces the blood flow to the kidneys and the brain.
Indomethacin has been proven to be more effective than other tocolytic agents in terms of delaying birth but is often prescribed with caution because of its potential association with adverse neonatal outcomes. The drug is associated with renal, gastrointestinal, and cerebral side effects.
Indomethacin was found to activate PKR in an interferon- and dsRNA-independent manner, causing rapid phosphorylation of eukaryotic initiation factor-2 α-subunit (eIF2α) The indomethAcin-induced increase of macroscopic and microscopic scores of intestinal inflammation were unchanged after pretreatment with L-NIL.
Indomethacin pretreatment of primary and GP8 cells turned vasorelaxation into contraction while N(omega)-nitro-L-arginine pretreatment decreased the vasore laxation induced by primary. Co-treatment partially prevented blood pressure elevation, restored restored blood pressure.
Excerpt | Reference | Relevance |
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"Indomethacin treated Panc-1 cells were analyzed with Raman spectroscopy, quantitative polymerase chain reaction and immunofluorescence techniques after the induction of EMT with TGF-β." | ( Indomethacin prevents TGF-β-induced epithelial-to-mesenchymal transition in pancreatic cancer cells; evidence by Raman spectroscopy. Çamdal, A; Ciftci, Z; Inal, A; Onses, MS; Sahin, F; Sakir, M; Sezer, G; Sezer, Z, 2022) | 2.89 |
"Indomethacin treatment after AIE restored molecular endpoints to control levels and rescued AIE-induced reversal learning deficits in the Morris water maze in both sexes." | ( Indomethacin restores loss of hippocampal neurogenesis and cholinergic innervation and reduces innate immune expression and reversal learning deficits in adult male and female rats following adolescent ethanol exposure. Crews, F; Elchert, N; Fisher, R; Macht, V; Vetreno, R, 2023) | 3.07 |
"The indomethacin treatment increased the level of p53 in the leukemic cells, implying that COX inhibition might reduce progression of ALL by attenuating protective paracrine PGE2 signaling from bone marrow stroma to leukemic cells." | ( Targeting cyclooxygenase by indomethacin decelerates progression of acute lymphoblastic leukemia in a xenograft model. Bhagwat, S; Blomhoff, HK; Burman, MM; Duthil, E; Ford, A; Gilljam, KM; Naderi, EH; Richartz, N; Ruud, E; Skah, S, 2019) | 1.29 |
"Indomethacin treatment for patent ductus arteriosus (PDA) is associated with acute kidney injury (AKI). " | ( Role of dopamine and selective dopamine receptor agonists on mouse ductus arteriosus tone and responsiveness. Berger, CD; Boatwright, N; Crockett, SL; Harris, M; Reese, J; Segar, JL; Shelton, EL; Su, RL; Yarboro, MT, 2020) | 2 |
"Indomethacin treatment success was defined as: (i) where PDA closed or became haemodynamically insignificant (hisPDA) after treatment and (ii) only including neonates where PDA had complete closure after treatment." | ( Association between changes in urine output and successful indomethacin treatment for patent ductus arteriosus in preterm neonates. Dey, A; Jain, A; Louis, D, 2021) | 1.59 |
"Indomethacin treatment revealed histopathological changes and ulcer scoring and ulcer index were markedly increased." | ( Possible protective effect of TNF-α inhibition and triad NO/cGMP/VEGF activation on gastric ulcer in rats. Abd Al Haleem, EN; Arafa, HMM; Ibrahim, FAM; Zaytoon, SAB, 2021) | 1.34 |
"Indomethacin is the best treatment both for HC and PH. " | ( Therapeutical approaches to paroxysmal hemicrania, hemicrania continua and short lasting unilateral neuralgiform headache attacks: a critical appraisal. Baraldi, C; Cainazzo, MM; Guerzoni, S; Pellesi, L; Pini, LA, 2017) | 1.9 |
"Indomethacin treatment enhanced water maze performance." | ( Nonsteroidal anti-inflammatory drug, indomethacin improves spatial memory and NMDA receptor function in aged animals. Foster, TC; Kumar, A; Ormerod, BK; Rani, A; Scheinert, RB, 2018) | 1.48 |
"Indomethacin-treated, antibiotic-exposed mice infected with C." | ( Indomethacin increases severity of Clostridium difficile infection in mouse model. Aronoff, DM; Bergin, IL; Castro-Córdova, P; Gil, F; Kirk, LA; Muñoz-Miralles, J; Paredes-Sabja, D; Trindade, BC, 2018) | 2.64 |
"Indomethacin treatment inhibits proliferation (at concentrations from 25 to 400 µmol/l) and induces apoptosis (at concentrations from 100 to 400 µmol/l) of human retinoblastoma cell line Y79 in a dose-dependent manner. " | ( Antiproliferative and apoptotic effects of indomethacin on human retinoblastoma cell line Y79 and the involvement of β-catenin, nuclear factor-κB and Akt signaling pathways. Chen, H; Li, W; Ren, Y; Wu, Y; Yang, S; Zhang, Y; Zheng, Q; Zhu, Y, 2014) | 2.11 |
"Indomethacin treatment induced intestinal ulcers that gradually healed after treatment. " | ( Dipeptidyl peptidase IV inhibition prevents the formation and promotes the healing of indomethacin-induced intestinal ulcers in rats. Akiba, Y; Engel, E; Guth, PH; Higashiyama, M; Higuchi, K; Inoue, T; Kaji, I; Kaunitz, JD; Rudenkyy, S, 2014) | 2.07 |
"Indomethacin-treated rats showed increased gastric acidity, acid concentration and ulcer index as compared to control rats. " | ( The impact of dehydroepiandrosterone on indomethacin-induced gastric lesions in rats. Alessa, R; Alkhateeb, M; Bayoumy, NM; Bin-Jaliah, I; Eleawa, S; Sakr, HF, 2014) | 2.11 |
"Indomethacin treatment and castration weaken immune responses and clinical state of infected rats, while testosterone and estradiol have a beneficial effect." | ( The effect of indomethacin, myeloperoxidase, and certain steroid hormones on bactericidal activity: an ex vivo and in vivo experimental study. Békési, G; Dinya, E; Ghidán, Á; Magyar, T; Marczell, I; Nagy, K; Rácz, K; Stark, J; Székács, B; Szombath, D; Tulassay, Z; Vajdovich, P; Várbíró, S; Varga, Z, 2014) | 1.48 |
"In indomethacin-treated rats, Wnt4 was down-regulated, suggesting effect on tissue integrity and steroid genesis." | ( Altered gene expression profile in ovarian follicle in rats treated with indomethacin and RU486. Kanki, M; Matsumoto, M; Nakatsuji, S; Nakayama, H; Noto, T; Oishi, Y; Tsubota, K, 2015) | 1.16 |
"Indomethacin pretreatment is used as a potential chemopreventive agent in cancers for it could assist in anti-tumor functions of other agents and exert anti-tumor effect." | ( Long-term use of indomethacin leads to poor prognoses through promoting the expression of PD-1 and PD-L2 via TRIF/NF-κB pathway and JAK/STAT3 pathway to inhibit TNF-α and IFN-γ in hepatocellular carcinoma. Miao, C; Sun, Z; Wang, Y; Xu, P, 2015) | 1.48 |
"Indomethacin treatment dose-dependently decreased the protein level of pBCR/ABL and total BCR/ABL without affecting bcr-abl mRNA expressions." | ( [Effect of indomethacin on BCR/ABL-Wnt/β-catenin pathway in K562 cells]. Feng, W; Hu, J; Huang, Z; Li, H; Liu, X; Liu, Z, 2015) | 1.53 |
"The indomethacin treatment of EAT-bearing mice inhibited the tumor growth and PGE2 synthesis from the 10th day." | ( Modulation of Cytokines Production by Indomethacin Acute Dose during the Evolution of Ehrlich Ascites Tumor in Mice. Fecchio, D; Gentile, LB; Massoco, Cde O; Queiroz-Hazarbassanov, N, 2015) | 1.17 |
"Indomethacin treatment prior to PTZ-induced seizures downregulated the mRNA expression of il1b, cox2b, and c-fos." | ( Indomethacin treatment prior to pentylenetetrazole-induced seizures downregulates the expression of il1b and cox2 and decreases seizure-like behavior in zebrafish larvae. Barbalho, PG; Lopes-Cendes, I; Maurer-Morelli, CV, 2016) | 2.6 |
"Indomethacin treatment reduced microglia activation and the number of ED1+ cells in both 8 and 14 days post injury as compared with controls." | ( Indomethacin treatment reduces microglia activation and increases numbers of neuroblasts in the subventricular zone and ischaemic striatum after focal ischaemia. Barbosa, MS; Cardoso, MM; DA Silva, MC; Ferreira, EM; Freire, MA; Gomes-Leal, W; Lima, RR; Lopes, RS; Sampaio, AO; Souza, CC, 2016) | 2.6 |
"Indomethacin-treated rats showed significant decrease in testicular weight, sperm count, sperm motility, serum gonadotropins and testosterone concentrations. " | ( Sub-chronic indomethacin treatment and its effect on the male reproductive system of albino rats: possible protective role of black tea extract. Bagoji, IB; Das, KK; Hadimani, GA; Yendigeri, SM, 2017) | 2.28 |
"Indomethacin treatment lasted for 2 years and 6 months." | ( Three-year follow-up of a girl with chronic paroxysmal hemicrania. Peet, A; Talvik, I; Talvik, T, 2009) | 1.07 |
"Indomethacin treatment had either no effect or a slightly inhibitory effect on [3H]-thymidine incorporation on all surfaces." | ( Arachidonic acid and prostaglandin E2 influence human osteoblast (MG63) response to titanium surface roughness. Campbell, CM; Chuang, HH; Dean, DD; Gruwell, SF; Schmitz, JP; Sylvia, VL; Tindall, JW; Zhong, W, 2008) | 1.07 |
"Indomethacin treatment decreased glutathione content and glutathione-conjugates in K562/ADR cells." | ( Indomethacin overcomes doxorubicin resistance by decreasing intracellular content of glutathione and its conjugates with decreasing expression of gamma-glutamylcysteine synthetase via promoter activity in doxorubicin-resistant leukemia cells. Asano, T; Fukunaga, Y; Tsutsuda-Asano, A, 2009) | 2.52 |
"Indomethacin treatment was associated with the disruption of mitochondrial transmembrane potential, release of cytochrome c, down-regulation of Bcl-2 and Mcl-1, upregulation of Bax, and elevation of caspases activity." | ( Indomethacin causes renal epithelial cell injury involving Mcl-1 down-regulation. Chen, CJ; Cheng, CL; Hung, YY; Li, JR; Ou, YC; Raung, SL; Yang, CR, 2009) | 2.52 |
"In indomethacin-treated animals, esomeprazole was more effective than famotidine or the antioxidant melatonin in promoting ulcer healing. " | ( Characterization of mechanisms underlying the effects of esomeprazole on the impairment of gastric ulcer healing with addition of NSAID treatment. Antonioli, L; Blandizzi, C; Colucci, R; Del Tacca, M; Fornai, M; Ghisu, N; Tuccori, M, 2009) | 0.97 |
"Indomethacin treatment was followed by severe injury to the gastric mucosa, decrease in proliferative activity of the epithelium, and stimulation of free-radical processes in gastric tissues." | ( Gastroprotective effect of dalargin in gastropathy due to treatment with nonsteroid antiinflammatory drugs. Fleishman, MY; Lebed'ko, OA; Sazonova, EN; Timoshin, SS; Zhivotova, EY, 2009) | 1.07 |
"Indomethacin is the best treatment, although HC could respond to other NSAIDs, such as the selective COX-2 inhibitors." | ( Misdiagnosis of hemicrania continua. Gonçalves, AL; Peres, MF; Valença, MM, 2009) | 1.07 |
"Indomethacin treatment for patent ductus arteriosus may have a protective role in the development of severe ROP." | ( Retinopathy of prematurity in very low birth weight infants and the potential protective role of indomethacin. Ben Simon, GJ; Goldman, RD; Kwint, J; Schwarcz, M; Spierer, A; Zhurkovsky, A, ) | 1.07 |
"Indomethacin treatment significantly decreased cotton pellet implantation induced white blood cell count elevation and immune cells infiltration in epididymal white adipose tissue." | ( Indomethacin activates peroxisome proliferator-activated receptor γ to improve insulin resistance in cotton pellet granuloma model. Chen, W; Cheng, JT; Cheng, KC; Shen, KH; Wu, HT; Yeh, CH, 2010) | 2.52 |
"Indomethacin treatment for 50 days caused a significant but reversible decrease in prostate weight, epididymal sperm reserves and sperm motility score compared with control rats (p < 0.05). " | ( Effect of chronic treatment with a cyclooxygenase inhibitor on reproductive parameters in male rat. Anwar, N; Khan, KM; Saeed, SA; Sarfraz, N, ) | 1.57 |
"Indomethacin treatment markedly enhanced inducible nitric oxide synthase and chemokine mRNA expression in the small intestine, but these responses were all significantly attenuated by either domperidone or metoclopramide." | ( Dopamine D₂-receptor antagonists ameliorate indomethacin-induced small intestinal ulceration in mice by activating α7 nicotinic acetylcholine receptors. Amagase, K; Hashimura, H; Iimori, M; Kato, S; Kawahara, R; Takeuchi, K; Yamanaka, N; Yasuda, M, 2011) | 1.35 |
"Indomethacin in treated sediments induced an increase in C." | ( Effects of indomethacin and propranolol on Chironomus riparius and Physella (Costatella) acuta. Kukkonen, JV; López-Doval, JC; Muñoz, I; Rodrigo, P, 2012) | 1.49 |
"In indomethacin-treated aortic rings, maximal ACH relaxations of 91.3±4.0%, decreased to 54.5±3.0% by the NO synthase inhibitor, nitro-l-arginine (LNA), to 49.8±3% by the guanylate cyclase (GC) inhibitor, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, to 63.7±4.9% by the lipoxygenase (LO) inhibitor, nordihydroguaiaretic acid (NDGA) and were completely inhibited by the combination of LNA and NDGA." | ( Endothelial nitric oxide and 15-lipoxygenase-1 metabolites independently mediate relaxation of the rabbit aorta. Aggarwal, NT; Campbell, WB; Gauthier, KM, ) | 0.65 |
"Indomethacin-treated fractures had similar length density and surface density of vasculature as the controls at 3 days after injury." | ( Anti-inflammatory treatment increases angiogenesis during early fracture healing. Lu, C; Mao, J; Marcucio, RS; Miclau, T; Wang, X; Xing, Z, 2012) | 1.1 |
"In indomethacin-treated rats, most newly formed corpora lutea showed abnormal follicle rupture at the basolateral sides." | ( Prostaglandin E(1) inhibits abnormal follicle rupture and restores ovulation in indomethacin-treated rats. Bellido, C; Gaytán, F; Morales, C; Sánchez-Criado, JE; Tarradas, E, 2002) | 1.06 |
"(II) Indomethacin pretreatment. During early infusion the dDAVP-induced reductions in the urinary flow rate and 6KPGF excretion were enhanced in both conditions." | ( Low-dose desmopressin infusion: renal action in healthy women in moderate salt retention and depletion, and interactions with prostanoids. Agnoli, GC; Borgatti, R; Cacciari, M; Lenzi, P; Marinelli, M; Stipo, L, 2002) | 0.77 |
"Indomethacin pretreatment did not affect the enzyme expressions, whereas dexamethasone administration significantly inhibited the meconium-induced COX-2 and NOS-2 up-regulation." | ( Meconium aspiration stimulates cyclooxygenase-2 and nitric oxide synthase-2 expression in rat lungs. Kääpä, P; Kytölä, J; Uotila, P, 2003) | 1.04 |
"Indomethacin treatment inhibited IgG1 and IgG2 production, and PGE2 restored both immunoglobulins in PWM-stimulated cultures. " | ( Prostaglandin E2-mediated regulation of immunoglobulin G2 via interferon gamma. Barbour, SE; Best, AM; Schenkein, HA; Tanaka, S; Tew, JG, 2003) | 1.76 |
"Indomethacin treatment increased renal brush border membrane vesicle NaPi-2 protein abundance in Hyp mice to levels comparable to that of C57/B6 mice, but had no effect in C57/B6 mice." | ( Correction of proximal tubule phosphate transport defect in Hyp mice in vivo and in vitro with indomethacin. Baum, M; Dwarakanath, V; Loleh, S; Quigley, R; Saini, N; Seikaly, M, 2003) | 1.26 |
"Indomethacin treatment was successful in 52 infants (93%)." | ( High efficacy and minor renal effects of indomethacin treatment during individualized fluid intake in premature infants with patent ductus arteriosus. Barth, H; Leonhardt, A; Seyberth, HW; Strehl, R, 2004) | 1.31 |
"Indomethacin treatment abolished these effects." | ( Prostanoids contribute to the oxygen-dependent regulation of vascular tone of human umbilical vein. Mildenberger, E; Siegel, G; Versmold, HT, 2004) | 1.04 |
"Indomethacin pretreatment abolished the changes in residual flux seen in FRL rats." | ( Phenotypic differences in cholinergic responses of distal colonic epithelium. Hernandez, J; Prior, T; Rangachari, PK; Tougas, G, 2004) | 1.04 |
"Indomethacin treatment increased TNF-alpha/chemokine mRNA expression from 30 min and induced macroscopic erosions after 4 h." | ( Monocyte chemotactic protein-1 regulates leukocyte recruitment during gastric ulcer recurrence induced by tumor necrosis factor-alpha. Arakawa, T; Fujiwara, Y; Hamaguchi, M; Higuchi, K; Matsumoto, T; Shiba, M; Tominaga, K; Watanabe, T, 2004) | 1.04 |
"In indomethacin- and L-NA-treated arteries, acetylcholine induced a smooth muscle hyperpolarization, which was blocked by SKF 525A (3 +/- 1 mV vs." | ( Acetylcholine-induced relaxation and hyperpolarization in small bovine adrenal cortical arteries: role of cytochrome P450 metabolites. Campbell, WB; Gauthier, KM; Zhang, DX, 2004) | 0.84 |
"Indomethacin treatment induced a better renal function (serum urea) when compared to control animals at 24, 48 and 72 h (219+/-54.5 vs." | ( Cyclooxygenase 1 and/or 2 blockade ameliorates the renal tissue damage triggered by ischemia and reperfusion injury. Câmara, NO; Cenedeze, MA; Feitoza, CQ; Gonçalves, GM; Pacheco-Silva, A; Pinheiro, HS; Santos, OF, 2005) | 1.05 |
"In indomethacin and rofecoxib-treated gerbils, the following results were obtained in H pylori-infected group vs H pylori-eradicated group respectively: hyperplasia area of the stomach (mm2): 82.4+/-9.2 vs 13.9+/-3.5 (P<0.05), 30.5+/-5.1 vs 1.3+/-0.6 (P<0.05); erosion and ulcer area (mm2): 14.4+/-4.9 vs 0.86+/-0.5 (P<0.05), 1.3+/-0.6 vs 0.4+/-0.3 (P<0.05); score of gastritis: 7.0+/-0.0 vs 3.6+/-0.5 (P<0.05), 7.0+/-0.0 vs 2.7+/-0.5 (P<0.05); MPO activity (micromol H2O2/min/g tissue): 104.7+/-9.2 vs 9.0+/-2.3 (P<0.05), 133.5+/-15.0 vs 2.9+/-0.7 (P<0.05); PGE2 synthesis (pg/mg wet weight/min): 299.2+/-81.5 vs 102.8+/-26.2 (P<0.05), 321.4+/-30.3 vs 11.9+/-4.8 (P<0.05)." | ( Eradication of Helicobacter pylori significantly reduced gastric damage in nonsteroidal anti-inflammatory drug-treated Mongolian gerbils. Chang, CC; Chen, SH; Fang, CL; Hsieh, CR; Lien, GS; Lou, HY; Pan, S, 2005) | 0.95 |
"Indomethacin treatment, which inhibited PGE2 production in both strains, suppressed the protection in Tg5 mice, supporting the idea that IL-9 controls blm-induced lung injury through a prostaglandin-dependent mechanism." | ( IL-9 protects against bleomycin-induced lung injury: involvement of prostaglandins. Arras, M; Brombacher, F; Delos, M; Heilier, JF; Huaux, F; Lison, D; Louahed, J; Renauld, JC, 2005) | 1.05 |
"Indomethacin treatment dose-dependently reduced survivin protein levels and caused severe injury of gastric mucosa and RGM-1 cells. " | ( Survivin: a novel target for indomethacin-induced gastric injury. Abdelkarim, B; Akahoshi, T; Chiou, SK; Jones, MK; Tanigawa, T; Tarnawski, AS, 2005) | 2.06 |
"Indomethacin-treated mice developed weight loss and melena." | ( Effects of esomeprazole magnesium on nonsteroidal anti-inflammatory drug gastropathy. Darrabie, M; Koch, TR; Opara, EC; Petro, A, 2005) | 1.05 |
"Indomethacin treatment decreased IL-11 secretion, which was largely restored by cotreatment with PGE(2) or RLX." | ( Relaxin and prostaglandin E(2) regulate interleukin 11 during human endometrial stromal cell decidualization. Baca, M; Dimitriadis, E; Fairlie, WD; McCoubrie, JE; Salamonsen, LA; Stoikos, C, 2005) | 1.05 |
"Indomethacin treatment caused a significant decrease in urinary ET-1 and AVP excretion (UET-1/Ucr 0.14+/-0.01 vs." | ( Urinary ET-1, AVP and sodium in premature infants treated with indomethacin and ibuprofen for patent ductus arteriosus. Faggian, D; Favaro, F; Lago, P; Plebani, M; Trevisanuto, D; Vedovato, S; Zanardo, V, 2005) | 1.29 |
"Indomethacin treatment decreased MTP but increased both cellular lipid peroxidation and cellular apoptosis via caspase 3 and 9 activation." | ( Rebamipide significantly inhibits indomethacin-induced mitochondrial damage, lipid peroxidation, and apoptosis in gastric epithelial RGM-1 cells. Matsui, H; Matsuzaki, Y; Muramatsu, M; Nagano, Y; Nakahara, A; Nakamura, Y; Shibahara, T; Shimokawa, O; Tanaka, N; Yanaka, A, 2005) | 1.33 |
"Indomethacin pretreatment did not modify the spasmogen responses of the explant." | ( Organ-cultured airway explants: a new model of airway hyperresponsiveness. Brayden, J; Morin, C; Proteau, S; Rousseau, E, 2005) | 1.05 |
"Indomethacin treatment caused a significant decrease in urinary ADH excretion (21.8 +/- 20.8 vs. " | ( Effects of ibuprofen and indomethacin on urinary antidiuretic hormone excretion in preterm infants treated for patent ductus arteriosus. Chiozza, L; Faggian, D; Lago, P; Piva, D; Vedovato, S; Zanardo, V, ) | 1.88 |
"Indomethacin treatment increased 5(6)-carboxyfluorescein diacetate (CFDA) efflux, as well as decreased accumulation in K562/ADR cells." | ( Indomethacin overcomes doxorubicin resistance with inhibiting multi-drug resistance protein 1 (MRP1). Asano, T; Fukunaga, Y; Matsunaga, S; Tsutsuda-Asano, A, 2006) | 2.5 |
"Indomethacin treatment significantly decreased WT survivin and survivin-DeltaEx3 (30.5+/-10.4% and 20.3+/-6.7%, respectively) but not survivin-2b mRNA in RKO cells." | ( Roles of survivin isoforms in the chemopreventive actions of NSAIDS on colon cancer cells. Chiou, SK; Huang, R; Mandayam, S; Tarnawski, AS, 2007) | 1.06 |
"Indomethacin treatment partially restored T cell proliferation and lowered IL-5 production to wild-type levels." | ( Francisella tularensis-infected macrophages release prostaglandin E2 that blocks T cell proliferation and promotes a Th2-like response. Drake, JR; Frelinger, JA; Hensley, LL; Jania, LA; Kawula, TH; Wilson, JE; Woolard, MD, 2007) | 1.06 |
"Indomethacin treatment was associated with increased expression of glucose-regulated protein 78 (GRP78) and C/EBP homologus protein (CHOP) and activation of ATF-6, characteristics of endoplasmic reticulum stress." | ( Indomethacin induces apoptosis in 786-O renal cell carcinoma cells by activating mitogen-activated protein kinases and AKT. Chen, CJ; Cheng, CL; Hung, YY; Ou, YC; Raung, SL; Yang, CR, 2007) | 2.5 |
"Indomethacin treatment significantly reduced the invasion of MDA-MB-435 cells independent of the culture and perfusion conditions examined." | ( Anti-inflammatory agent indomethacin reduces invasion and alters metabolism in a human breast cancer cell line. Ackerstaff, E; Artemov, D; Bhujwalla, ZM; Gimi, B, 2007) | 1.37 |
"Indomethacin treatment (2 microg/g/d) for 7 days resulted in disruption of epithelial barrier integrity, but it caused neither a systemic inflammatory response nor a mucosal inflammatory response in the colon or cecum. " | ( Epithelial barrier disruption allows nondisease-causing bacteria to initiate and sustain IBD in the IL-10 gene-deficient mouse. Churchill, TA; Dmytrash, AL; Doyle, J; Fedorak, RN; Macfarlane, SM; Sydora, BC; Walker, JW, 2007) | 1.78 |
"Indomethacin treatments also increased ATP hydrolysis." | ( Indomethacin stimulates activity and expression of ecto-5'-nucleotidase/CD73 in glioma cell lines. Battastini, AM; Bavaresco, L; Bernardi, A; Delgado-Cañedo, A; Jacques-Silva, MC; Lenz, G; Wink, MR, 2007) | 2.5 |
"Indomethacin-treated RGM-1 cells were investigated by conventional cytotoxicity assay, fluorometry of diphenyl-1-pyrenylphosphine (DPPP) to detect lipid peroxidation, and FP. " | ( Cellular membrane fluidity measurement by fluorescence polarization in indomethacin-induced gastric cellular injury in vitro. Hyodo, I; Kaneko, T; Matsui, H; Nakahara, A; Shimokawa, O, 2007) | 2.02 |
"Indomethacin treatment attenuated the dilation in paired (-33 +/- 5%) but not unpaired (-6 +/- 4%) arterioles." | ( Functional vasodilation in the rat spinotrapezius muscle: role of nitric oxide, prostanoids and epoxyeicosatrienoic acids. Hester, RL; Naik, JS; Xiang, L, 2008) | 1.07 |
"In indomethacin-treated rats at 6-24 hours, inflammation was evident as was redistribution of CD103+DC from LP to Peyer's patches." | ( Intestinal epithelial barrier dysfunction and dendritic cell redistribution during early stages of inflammation in the rat: role for TLR-2 and -4 blockage. Jury, J; Perdue, MH; Porras, M; Silva, MA; Vergara, P, 2008) | 0.86 |
"Nine indomethacin-treated babies (29%) versus twelve ibuprofen babies (38%) underwent repeated therapy (p = 0.656)." | ( Ibuprofen versus continuous indomethacin in premature neonates with patent ductus arteriosus: is the difference in the mode of administration? Bromiker, R; Hammerman, C; Jacobson, S; Kaplan, M; Nir, A; Schimmel, MS; Shchors, I, 2008) | 1.1 |
"Indomethacin treatment did not have a measurable effect on any of the other components of the glucagon transducer system." | ( Modulation of hepatic protein kinase activity by indomethacin. Banach, WJ; Ganguli, S; Harris, PS; Sinha, MK; Sterman, B, 1984) | 1.24 |
"Indomethacin-treated cultures exhibited lower creatine kinase levels, though no change in the ratio of the three isoenzymes was observed." | ( Prostaglandins and cyclic AMP stimulate creatine kinase synthesis but not fusion in cultured embryonic chick muscle cells. Pette, D; Schützle, UB; Wakelam, MJ, 1984) | 0.99 |
"In indomethacin-treated dogs, dibutyryl cyclic AMP also produced significant and reversible increases in renin secretion rate and renal blood flow but had no effect on Na+ excretion." | ( Mechanism of effect of dibutyryl cyclic adenosine 3',5'-monophosphate on canine renal renin release. Bondar, N; Cadnapaphornchai, P; McDonald, FD; Taher, S, 1984) | 0.78 |
"Indomethacin pretreatment (10 mg kg-1 i.v.) attenuated the decrease in blood pressure following endotoxin injection." | ( Effect of indomethacin on the blood pressure and plasma catecholamine responses to acute endotoxaemia. Dimicco, JA; Feuerstein, G; Kopin, IJ; Ramu, A, 1981) | 1.39 |
"Indomethacin pretreated animals regained the righting response at a higher blood ethanol concentration than did saline pretreated animals." | ( Antagonism of alcohol hypnosis by blockade of prostaglandin synthesis and activity: genotype and time course effects. Collins, AC; Elmer, GI; George, FR; Howerton, TC, 1983) | 0.99 |
"In indomethacin-treated (5 mg/kg, i.v.) dogs, K-351 decreased renal blood flow and caused smaller decrease in systemic blood pressure and larger suppression of renin secretion rate than in non-treated dogs." | ( Effects of K-351 on hemodynamics and renin release in anesthetized dogs. Hisa, H; Kamijo, T; Satoh, S; Suzuki, M, 1984) | 0.78 |
"In indomethacin-treated dogs the residual relaxation of the bovine coronary artery induced by intravenous angiotensin II was not further reduced by treating the tissues with hyoscine, mepyramine, cimetidine, and methysergide." | ( Angiotensin-induced release of a prostacyclin-like substance from the lungs. Dusting, GJ, ) | 0.65 |
"In indomethacin-treated rabbits, however, ceruloplasmin at the same high doses failed to induce angiogenesis." | ( Role of prostaglandin E1 and copper in angiogenesis. Gullino, PM; Jones, J; Ziche, M, 1982) | 0.78 |
"In indomethacin-treated rats there was a reduction in the cardiac response to epinephrine in vivo as indicated by a shift to the right of the epinephrine dose-heart rate response curve." | ( Effect of indomethacin on cardiac beta-adrenergic receptors. Feuerstein, G; Kopin, IJ; Torda, T, 1980) | 1.18 |
"Indomethacin post-treatment significantly elevated aortic pressure, cardiac output, and left ventricular isometric tension elevated aortic pressure, cardiac output, and left ventricular isometric tension rise (LVP dp/dt max) following endotoxin administration in the dog." | ( The effect of indomethacin and adrenergic receptor blocking agents on rats and canine responses to endotoxin. Fujita, T; Goto, F; Otani, E; Yamamuro, M, 1980) | 1.34 |
"5 Indomethacin treatment reversed the isoprenaline desensitization induced by chronic treatment (0.4 mumol isoprenaline) but was ineffective in animals that received the higher doses of isoprenaline in vivo." | ( Tolerance of guinea-pig airway muscle preparations to relaxant agonists induced by chronic exposure to isoprenaline in vivo. Brink, C, 1981) | 0.82 |
"Indomethacin treatment (1 microgram/ml) of the RA auto-MLR led to increased production of supernatant inhibitory activity (8% +/- 4 without, 57% +/- 4 with indomethacin), but had no significant effect on the inhibition of EBV-induced B cell proliferation by normal auto-MLR supernatants." | ( Analysis of the defects responsible for the impaired regulation of EBV-induced B cell proliferation by rheumatoid arthritis lymphocytes. II. Role of monocytes and the increased sensitivity of rheumatoid arthritis lymphocytes to prostaglandin E. Bluestein, HG; Epstein, LB; Hasler, F; Zvaifler, NJ, 1983) | 0.99 |
"Indomethacin treatment decreased human luteinizing hormone (hLH) binding in rat testis in a time-dependent fashion." | ( Indomethacin decreases both luteinizing hormone binding and fluidity of testicular microsomal membranes in rat. Dave, JR; Witorsch, RJ, 1983) | 2.43 |
"Indomethacin treatment promoted clearance of the Salmonella and a 50-90% increase in macrophages recovered from the peritoneal cavity in both primary and secondary infected animals." | ( Immunoregulation by macrophages. III. Prostaglandin E suppresses lymphocyte activation but not macrophage effector function during Salmonella enteritidis infection. Cahill, J; Hopper, KE, 1984) | 0.99 |
"Indomethacin pretreatment caused an augmented blood pressure response after ANG II infusion, which returned to near control level after concomitant infusion of a subdepressor dose of PGI2." | ( Role of prostacyclin in blood pressure regulation and aldosterone production in conscious rabbits. Ikeda, M; Koshida, H; Miyamori, I; Morise, T; Takeda, R; Takeda, Y; Takimoto, H; Yasuhara, S, 1984) | 0.99 |
"Indomethacin treatment did not inhibit CyA-mediated accumulation of renin in the renal cortex." | ( Cyclosporin A and renal prostaglandin biosynthesis. Baxter, CR; Duggin, GG; Hall, BM; Horvath, JS; Tiller, DJ, 1984) | 0.99 |
"Indomethacin pretreatment prevented the initial phase of pulmonary hypertension, the increases in thromboxane and prostacyclin metabolites in lung lymph, and the febrile response to toxin infusion but did not modify the granulocytopenia or the increased pulmonary vascular permeability." | ( Effects of cyclooxygenase inhibition on the response to group B streptococcal toxin in sheep. Brigham, KL; Larsson, LE; Ogletree, ML; Rojas, J; Stahlman, MT, 1983) | 0.99 |
"Indomethacin pretreatment (14 microM, 30 min) potentiated the relaxation response in intact rings." | ( Endothelium-dependent relaxation of rabbit aorta. I. Relaxation stimulated by arachidonic acid. Peach, MJ; Singer, HA, 1983) | 0.99 |
"Indomethacin treatment induced a qualitatively similar shifting of the concentration-response curves of noradrenaline and angiotensin II in some vessels: the concentration-response curves remained unchanged for the aorta, were slightly shifted to the left of the pulmonary artery, were markedly shifted to the left for the coeliac artery, and were shifted to the right for the femoral artery." | ( The importance of endogenous prostaglandins other than prostacyclin, for the modulation of contractility of some rabbit blood vessels. Förstermann, U; Hertting, G; Neufang, B, 1984) | 0.99 |
"Indomethacin pretreatment markedly reduced the number of convulsion-resistant animals." | ( Anticonvulsive effects of endogenous prostaglandins formed in brain of spontaneously convulsing gerbils. Förstermann, U; Hertting, G; Seregi, A, 1984) | 0.99 |
"Indomethacin-pretreatment did not affect drug-induced relaxations of either normal or sensitized tracheal spirals." | ( Bronchodilator-mediated relaxation of normal and ovalbumin-sensitized guinea-pig airways: lack of correlation with lung adenylate cyclase activation. Burka, JF; Saad, MH, 1984) | 0.99 |
"Indomethacin pre-treatment reduced the levels estimated in both extracted and unextracted samples; the results indicating that the higher estimates obtained by direct assay were due to a combination of PG/TXB2 metabolites and non-specific interference." | ( Radioimmunoassay of prostaglandins and thromboxane B2 in extracted and unextracted urine and serum using an iodinated ligand. Barden, A; Beilin, LJ; Mahoney, DP; Vandongen, R, 1983) | 0.99 |
"Indomethacin pretreatment did not significantly change the pharmacokinetics of bumetanide, affecting neither the total amount of drug nor time course of drug delivered into the urine." | ( Determinants of bumetanide response in the dog: effect of indomethacin. Lau, HS; Smith, DE, 1983) | 1.23 |
"Indomethacin treatment (10 micrograms/gm body weight) of ovulatory brook trout significantly decreased plasma and ovarian PGF levels by 12 hours post-ovulation." | ( Ovarian and plasma PGE and PGF levels in naturally ovulating brook trout (Salvelinus fontinalis) and the effects of indomethacin on prostaglandin levels. Cetta, F; Goetz, FW, 1983) | 1.2 |
"Indomethacin (10 mg/kg) pretreatment blocked the decapitation rise in PGE and TXB2 levels and gave values similar to focused microwave irradiation." | ( In vivo regional levels of PGE and thromboxane in mouse brain: effect of decapitation, focused microwave fixation, and indomethacin. Anton, RF; Randall, CL; Wallis, C, 1983) | 1.2 |
"Indomethacin treatment to rats bearing dimethylhydrazine-induced colonic cancer resulted in increased mortality (p less than 0.01) and a greater incidence of metastases compared to untreated animals with the same stage of disease. " | ( Enhancement of colonic cancer by indomethacin treatment in dimethylhydrazine pretreated rats. Abate, S; Califano, G; Danzi, M; Ferulano, GP, 1984) | 1.99 |
"If indomethacin treatment was initiated prior to transplantation of the tumor or 2 weeks post-transplantation, and continued throughout the disease process, there was no effect on either the course of the disease or mortality." | ( Increased sensitivity to indomethacin of mice bearing the BCL1-leukemia. Hart, DA, 1984) | 1.08 |
"Indomethacin treatment of donor rabbits (10 mg/kg s.c.) given every 6 h during the day before transfer had no effect on subsequent implantation of the blastocysts." | ( Site of action of indomethacin on implantation in the rabbit. Harper, MJ; Snabes, MC, 1984) | 1.32 |
"Indomethacin pretreatment, 2 mg/kg, did not significantly reduce these responses." | ( Renal effects of indanone in dogs and rats: modification by a cyclooxygenase inhibition. Diz, DI; Kauker, ML, 1980) | 0.98 |
"In indomethacin treated dogs (5 mg/kg, i.v.) intrarenal infusion of A23187 significantly decreased RBF." | ( Effects of calcium ionophore, A23187, on prostaglandin E2 and renin release in dogs. Abe, Y; Imanishi, M; Miura, K; Okahara, T; Yamamoto, K, 1980) | 0.78 |
"Indomethacin treatment enhanced the PFC response to a chicken lysozyme-lipopolysaccharide conjugate, and did not greatly affect the PFC response to pneumococcal polysaccharide." | ( Effects of prostaglandin synthesis inhibition on the immune response. Benjamini, E; Schleimer, RP, 1981) | 0.98 |
"Indomethacin treatment suppressed many of the morphological changes normally occurring in the apex during preovulatory development." | ( An ultrastructural study of preovulatory apical development in mouse ovarian follicles: effects of indomethacin. Downs, SM; Longo, FJ, 1983) | 1.2 |
"Indomethacin treatment before LT infusion significantly altered the changes in GL by reducing the early (less than 1 min) response and potentiating the later (3-5 min) response, significantly reduced the fall in Cdyn." | ( Effects of indomethacin on the guinea-pig pulmonary response to intravenous leukotrienes C4 and D4. Austen, KF; Corey, EJ; Drazen, JM; Leitch, AG, 1983) | 1.38 |
"Indomethacin pretreatment (6 mg/kg i.v.) had no effect on leukotriene-induced coronary constriction." | ( Effects of FPL-55712 or indomethacin on leukotriene-induced coronary constriction in the intact pig heart. Boyd, LM; Ezra, D; Feuerstein, G; Goldstein, RE, 1983) | 1.29 |
"Indomethacin treatment significantly reduced prostaglandin E and F levels in the tumor tissue, but 5-fluorouracil did not." | ( Growth inhibition of transplantable murine colon adenocarcinoma 38 by indomethacin. Goto, A; Narisawa, T; Sano, M; Sato, M; Takahashi, T, 1983) | 1.22 |
"Indomethacin pretreatment significantly reduced the mortality rate independent of pretreatment time and produced an increase in the number of animals exhibiting a depressed behavioral response as measured by loss of the righting reflex." | ( Indomethacin significantly reduces mortality due to acute ethanol overexposure. Collins, AC; Elmer, GI; George, FR, 1982) | 2.43 |
"Indomethacin treatment of rats during early pregnancy caused a delay in implantation, a significant reduction in uterine weight, and a much reduced number or absence of implanted blastocysts in the uterus on Day 9." | ( Studies on the involvement of prostaglandins in implantation in the rat. Phillips, CA; Poyser, NL, 1981) | 0.98 |
"Indomethacin treatment (15 mg/kg) reduced bleeding volume and diminished the survival rate in haemorrhagically shocked rats. " | ( Prostaglandins E1 and E2 antagonize indomethacin-induced decrease in survival rate of haemorrhagically shocked rats. Hedqvist, P; Perbeck, L, 1980) | 1.98 |
"The indomethacin pretreatment considerably increased the diuretic and natriuretic effect of the volume expansion in the rabbit." | ( The effect of indomethacin on renal function. Kövér, G, 1980) | 1.1 |
"In indomethacin-treated subjects, the increment of alpha-amino-nitrogen was less marked and the increase in plasma glucagon was not observed." | ( Effect of indomethacin on the metabolic and hormonal response to a standardized breakfast in normal subjects. Delporte, JP; Guerten, D; Jaminet, F; Lefebvre, PJ; Luyckx, AS; Scheen, A, ) | 1.05 |
"Indomethacin pretreatment decreased basal PGE2 excretion (P less than 0.02) and baseline PRA as well as the increase in PRA after captopril (P less than 0.05)." | ( Acute haemodynamic and hormonal effects of captopril are diminished by indomethacin. Hirsch, F; Scherer, B; Weber, PC; Witzgall, H, 1982) | 1.22 |
"Indomethacin-treated animals had an increased saccular wall mass, decreased airspace mass, and a decreased capillary to saccular wall ratio (P less than 0.05)." | ( Effects of indomethacin on fetal rat lungs: a possible cause of persistent fetal circulation (PFC). Bloor, CM; Friedman, WF; Harker, LC; Kirkpatrick, SE, 1981) | 1.37 |
"Indomethacin treatment (24 mg X 4 daily) reduced the rectal PGE2 excretion from 2.2 to 0.3 microgram/day and caused a decrease in the rectal fluid loss of 850 ml/day associated with a similar reduction in rectal sodium excretion." | ( Prostaglandin E2-mediated secretory diarrhea in villous adenoma of rectum: effect of treatment with indomethacin. Bukhave, K; Lange, P; Rask-Madsen, J; Steven, K, 1981) | 1.2 |
"Indomethacin treatment resulted in more rapid healing of the esophageal inflammation and prevented or promptly corrected the esophagitis-associated LES hypotension." | ( Beneficial effect of indomethacin on acid-induced esophagitis in cats. Beck, BD; Brown, FC; Castell, DO; Eastwood, GL; Fletcher, JR, 1981) | 1.3 |
"Indomethacin treatment (3-8 daily doses of 100 mg) to patients resulted in an increased level of peripheral blood monocytes, as compared to the initial values measured in each individual subject before taking the drug. " | ( Effects of indomethacin treatment of human peripheral blood monocytes. Globerson, A; Klein, B; Razin, E, 1981) | 2.1 |
"Indomethacin treatment (0.5 microgram/ml) significantly reduced the occurrence of ovulation in gonadotropin-treated ovaries." | ( The effect of prostaglandin synthesis inhibition by indomethacin on ovulation and ovum maturation in the in vitro perfused rabbit ovary. Kobayashi, Y; Santulli, R; Wallach, EE; Wright, KH, 1981) | 1.23 |
"Indomethacin pretreatment decreased the cumulative 4-hour excretion of sodium caused by 1.0 mg bumetanide from 276 +/- 22.9 to 202 +/- 20.9 mEq (P less than 0.003)." | ( Interaction studies with bumetanide and furosemide. Effects of probenecid and of indomethacin on response to bumetanide in man. Brater, DC; Chennavasin, P; Fox, WR, ) | 1.08 |
"Indomethacin-treated animals showed no signs or only mild esophagitis posttreatment." | ( Radiation esophagitis in the opossum: radioprotection with indomethacin. Feldman, MS; Libshitz, HI; Mamel, JJ; Northway, MG; Osborne, BM; Szwarc, IA; West, JH, 1980) | 1.23 |
"Indomethacin treatment was effective in all the 68 patients." | ( Classification of threatened premature labor related to treatment with a prostaglandin inhibitor: indomethacin. Abramovici, H; Atad, J; David, A; Moise, J, 1980) | 1.2 |
"The indomethacin pretreated group responded similarly to the control group; there was no difference in the 5 hour course of Pa02 (p = .34), P(A-a)02 (p = .21) or QS/QT (p = .99)." | ( Failure of indomethacin to prevent or ameliorate oleic acid pulmonary edema in the dog. Blatnick, RA; Goitz, H; Johansen, RK; Pace, NL, 1980) | 1.13 |
"Indomethacin treatment of rats resulted in a significant increase of pineal monoamine oxidase (MAO) type A activity, whereas it depressed MAO type B and hydroxyindole-O-methyl transferase activities. " | ( Effect of indomethacin on monoamine metabolism and melatonin synthesis in rat pineal gland. Cardinali, DP; Ritta, MN, 1980) | 2.11 |
"Indomethacin treatment prevented this effect." | ( Induction of implantation in the rat by iproniazid. Pakrashi, A; Pal, AK, 1980) | 0.98 |
"1 Indomethacin treatment of postural hypotension in four patients with chronic autonomic failure increased their pressor supersensitivity to intravenous noradrenaline without causing fluid retention. " | ( The pressor actions of noradrenaline and angiotension II in chronic autonomic failure treated with indomethacin. Bannister, R; Davies, IB; Hensby, C; Sever, PS, 1980) | 1.2 |
"Indomethacin pretreatment (5 mg/kg orally) greatly induced the effect of chlorazanil on urinary prostaglandin E2-excretion." | ( Enhancement of urinary prostaglandin excretion by chlorazanil in rats. Effects of indomethacin. Arrigoni-Martelli, E; Eilertsen, E; Olsen, UB, 1980) | 1.21 |
"Indomethacin treatment enhanced vasoconstriction to LTC4 in the control group to a similar constriction to that observed in the hematoma group." | ( Hematoma-induced enhanced cerebral vasoconstrictions to leukotriene C4 and endothelin-1 in piglets: role of prostanoids. Leffler, CW; Shibata, M; Yakubu, MA, 1995) | 1.01 |
"In indomethacin-treated strips with intact endothelium, L-NOARG attenuated but did not abolish the relaxation." | ( Mechanism underlying substance P-induced relaxation in dog isolated superficial temporal arteries. Enokibori, M; Okamura, T; Toda, N, 1994) | 0.8 |
"Indomethacin treatment did not affect endothelium-dependent relaxation in the control solution but partially restored the response to ACh in elevated glucose." | ( Magnesium modulates endothelial dysfunction produced by elevated glucose incubation. Duhault, J; Félétou, M; Rasetti, C, 1994) | 1.01 |
"Indomethacin pretreatment (3 mg/kg) markedly attenuated the phosphaturic response to PTH in phosphate-deprived rats with a denervated kidney (delta FEPi, 3.2 +/- 1.3%, n = 7) but not in animals fed an LPD with innervated kidneys or in rats fed an NPD." | ( Interaction of the renal nerves and prostaglandins on the phosphaturic response to PTH in phosphate-deprived rats. Berndt, TJ; Khraibi, AA; Knox, FG, 1995) | 1.01 |
"Indomethacin treatment resulted in mucosal ulceration and granulocyte infiltration, and a corresponding inflammatory response in the mesentery, which was characterised by an increase in the number of adherent (eightfold) and emigrated (sixfold) leucocytes and a reduction (80%) in leucocyte rolling velocity." | ( Leucocyte-endothelial cell adhesion in a model of intestinal inflammation. Anderson, DC; Arndt, H; Granger, DN; Grisham, MB; Palitzsch, KD; Rusche, J, 1995) | 1.01 |
"Indomethacin treatment of the M phi also prevents M." | ( Plasminogen activator inhibitor type 2 prevents programmed cell death of human macrophages infected with Mycobacterium avium, serovar 4. Gan, H; Newman, GW; Remold, HG, 1995) | 1.01 |
"Indomethacin treatment led to distortion of hepatic cell arrangement as well as marked cellular infiltration and congestion." | ( Studies on the effect of acute doses of indomethacin (prostaglandins inhibitor) during induced liver failure. Abdel-Wahab, MM; Bayoumy, AS; Hassounah, OA, 1995) | 1.28 |
"In indomethacin-treated cells, PGs caused a four-fold increase in NAT activity." | ( Prostaglandins stimulate serotonin acetylation in chick pineal cells: involvement of cyclic AMP-dependent and calcium/calmodulin-dependent mechanisms. Collin, JP; Pontoire, C; Van Camp, G; Voisin, P, 1993) | 0.8 |
"Indomethacin treatment abolished the influence of the epithelium on ovalbumin-induced tracheal contraction." | ( Pharmacologic modulation of the influence of the epithelium on immunologic- and nonimmunologic-induced histamine release and contraction in guinea pig superfused tracheal strips. Buckner, CK; Conklin, R; Doran, O; Fishleder, RI; Graziano, FM; Will, JA, 1993) | 1.01 |
"The indomethacin-treated group showed significantly decreased levels of substance P." | ( Indomethacin reduces substance P levels in human ocular aqueous humor. Kaehler, C; Kieselbach, G; Saria, A; Troger, J, 1993) | 2.21 |
"Indomethacin pretreatment prevented the hypoxia-induced increase in membrane lipid peroxidation products but had no effect on the decrease in Na+,K(+)-ATPase activity." | ( Effect of cyclooxygenase inhibition on brain cell membrane lipid peroxidation during hypoxia in newborn piglets. Delivoria-Papadopoulos, M; McGowan, JC; McGowan, JE; Mishra, OP, 1994) | 1.01 |
"Indomethacin treatment significantly reduced the levels of TxB2 and 6-keto-PGF1 alpha to < 10% of those present in untreated or irradiated cells." | ( Effect of modifiers of arachidonic acid metabolism on radiation transformation and eicosanoid formation in C3H/10T1/2 cells. Billings, PC; Kennedy, AR; Maki, PA, 1994) | 1.01 |
"Indomethacin pretreatment did not accentuate this hypertensive effect of cyclosporin." | ( Acute haemodynamic and renal effects of cyclosporin and indomethacin in man. Clark, G; Lang, CC; Struthers, AD; Sturrock, ND, 1994) | 1.26 |
"In indomethacin-treated fetuses, in which the prostanoids had decreased and remained at approximately 20% normal, cooling initiated moderate nonshivering thermogenesis, and ventilation and cord occlusion caused no further changes." | ( Role of prostaglandin E2 and prostacyclin in nonshivering thermogenesis during simulated birth in utero. Power, GG; Takeuchi, M; Yoneyama, Y, 1994) | 0.8 |
"Indomethacin pretreatment of aortae from 20 week old SHRSP restored acetylcholine-induced EDR to a level comparable with that in age-matched WKY.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Enhancement of endothelium-dependent relaxation in the aorta from stroke-prone spontaneously hypertensive rats at developmental stages of hypertension. Hamano, M; Mashiko, S; Onda, T; Tomita, I; Tomita, T, 1994) | 1.01 |
"Indomethacin-treated patients suffered less pain and consumed less additional analgetics compared to the other patient groups." | ( Anti-inflammatory treatment may prolong survival in undernourished patients with metastatic solid tumors. Gelin, J; Gülich, M; Hyltander, A; Kärrefors, I; Körner, U; Lönnroth, C; Lundholm, K; Norli, B; Sandström, R; Svaninger, G, 1994) | 1.01 |
"Oral indomethacin treatment for tocolysis has no impact on PT and aPTT; however, profound acute changes in maternal bleeding time occur." | ( The effect of indomethacin tocolysis on maternal coagulation status. Barth, WH; Hankins, GD; Lunt, CC; Satin, AJ, 1994) | 1.16 |
"Indomethacin suppository treatment was effective in controlling rectal remnant polyps in the two patients with familial adenomatous polyposis. " | ( Regression of rectal polyps by indomethacin suppository in familial adenomatous polyposis. Report of two cases. Hirata, K; Itoh, H; Ohsato, K, 1994) | 2.02 |
"Indomethacin-treated animals had CSA values 244% those of untreated burn-infected animals (p = 0.016)." | ( Marrow granulocyte-macrophage progenitor cell response to burn injury as modified by endotoxin and indomethacin. Gamelli, RL; He, LK; Liu, H, 1994) | 1.23 |
"Indomethacin pretreatment (5 mg/kg, s.c.) significantly inhibited these changes seen after exposure to TC, except for PD reduction." | ( Capsaicin-sensitive sensory nerves in recovery of gastric mucosal integrity after damage by sodium taurocholate in rats. Narita, M; Ohuchi, T; Okabe, S; Takeuchi, K, 1993) | 1.01 |
"In indomethacin-pretreated animals, no neurons expressing fos-IR were found in nuclei associated with relay of nociception nor in nuclei contributing to inhibition of nociception." | ( Expression of c-fos-like protein in the rat brain after injection of interleukin-1-beta into the gingiva. Hamba, M; Hiraide, T; Muro, M; Ozawa, H, 1994) | 0.8 |
"Four indomethacin-treated and three saline solution-treated infants had parenchymal extension of the hemorrhage." | ( Low-dose indomethacin therapy and extension of intraventricular hemorrhage: a multicenter randomized trial. Allan, W; Ehrenkranz, RA; Katz, KH; Makuch, RW; Ment, LR; Oh, W; Phillip, AG; Schneider, KC; Taylor, KJ; Vohr, B, 1994) | 1.16 |
"Indomethacin treatment prevented both the maximum increment in glomerular filtration rate occurring in normal pregnancy between days 14 to 18 and the physiological near term decline in kallikrein excretion." | ( Chronic indomethacin administration and its relation with the renal kallikrein kinin system during rat pregnancy. Arrizurieta, EE; Martín, RS; Negri, AL; Oddo, EM; Santos, JC, 1993) | 1.44 |
"Indomethacin treatment did not affect the mastoparan contraction even though mastoparan has been shown to stimulate phospholipase A2 in other cell types." | ( Enhanced vascular reactivity to mastoparan, a G protein activator, in genetically hypertensive rats. Kanagy, NL; Webb, RC, 1994) | 1.01 |
"Indomethacin pretreatment did not abolish the Ang II-induced rise in the M value." | ( Angiotensin II enhances insulin sensitivity in healthy volunteers under euglycemic conditions. Arnold, U; Fliser, D; Hartung, R; Kohl, B; Ritz, E, 1993) | 1.01 |
"In indomethacin-treated cultures, % 45Ca release and the labeling of CDP were significantly reduced." | ( Systematic assessment of bone resorption, collagen synthesis, and calcification in chick embryonic calvaria in vitro: effects of prostaglandin E2. Nagai, M; Ota, M; Suzuki, Y, ) | 0.65 |
"In indomethacin-treated lungs, Pao was greater than Pa80, Pvo equaled Pv20 and Pv150, and Pdo was the same as Pa80, Pv20, and Pv150." | ( Micropipette and vascular occlusion pressures in isolated lungs of newborn lambs. Fike, CD; Gordon, JB; Kaplowitz, MR, 1993) | 0.8 |
"Indomethacin pretreatment prevented the furosemide-induced decrease in blood pressure in rats with ligation of the ureters." | ( Acute effects of furosemide on blood pressure in functionally anephric, volume-expanded rats. Bartoli, E; Palomba, D; Sechi, LA, 1993) | 1.01 |
"In indomethacin (Indo)-treated dogs (5 mg/kg) ACh produced a transient rise in RPF and UNaV, followed by a progressive decline in RPF and UNaV." | ( Role of muscarinic receptors in renal response to acetylcholine. Coleman, BR; Gill, JR; Keiser, H; Oriji, G; Peters, J; Yun, JC, 1993) | 0.8 |
"Indomethacin treatment of rats also inhibited PMNL migration into the inflamed joints, but unlike ebselen, indomethacin inhibited only ZAS induced dermal PMNL accumulation." | ( The effect of ebselen on polymorphonuclear leukocyte and lymphocyte migration to inflammatory reactions in rats. Gao, JX; Issekutz, AC, ) | 0.85 |
"Indomethacin pretreatment (5 mg/kg, subcutaneously) caused a significant decrease in basal gastric mucosal blood flow of portal-hypertensive rats but did not modify this parameter in sham-operated animals." | ( Involvement of nitric oxide and prostaglandins in gastric mucosal hyperemia of portal-hypertensive anesthetized rats. Bosch, J; Casadevall, M; Marroni, N; Panés, J; Piqué, JM; Whittle, BJ, 1993) | 1.01 |
"Indomethacin treatment was associated with a marked reduction in serum calcitriol concentration, as well as decreased prostaglandin E excretion." | ( Calcium kinetics in the hyperprostaglandin E syndrome. Abrams, SA; Bergstrom, W; Shoemaker, L; Vieira, N; Welch, TR; Yergey, AL, 1993) | 1.01 |
"In indomethacin treated rats, simultaneous administration of hydrotalcit did not affect the concentrations of indomethacin in serum or inflammatory exudates nor did it attenuate the inhibition of prostaglandin release into the exudates." | ( Role of eicosanoids, nitric oxide, and afferent neurons in antacid induced protection in the rat stomach. Korolkiewicz, R; Lambrecht, N; Liszkay, M; Peskar, BM; Trautmann, M, 1993) | 0.8 |
"Indomethacin treatment resulted in a normalization of the cellular imbalance at the end of the first postoperative week, but IL-2 synthesis remained significantly reduced during the entire observation period." | ( Alterations of cell-mediated immune response following cardiac surgery. Endres, S; Faist, E; Hültner, L; Lang, S; Markewitz, A; Reichart, B; Weinhold, C, 1993) | 1.01 |
"indomethacin pretreatment, on rat duodenal bicarbonate secretion was investigated." | ( Duodenal bicarbonate secretion induced by human epidermal growth factor in rats is partially mediated by prostaglandins. Chui, DH; Fesce, E; Ideo, G; Marotta, F; Rezakovic, I; Zhong, GG, 1993) | 1.01 |
"Indomethacin pretreatment almost completely abolished the responsiveness to sodium nitroprusside (NaNP) in cirrhotic rats, while not affecting controls." | ( Prostaglandins modulate the responsiveness of the gastric microcirculation of sodium nitroprusside in cirrhotic rats. Ferraz, P; Geraldo, J; Wallace, JL, 1996) | 1.02 |
"Indomethacin pretreatment inhibited the increase in plasma levels of 6-keto-PGF1 alpha produced by AT III." | ( Effects of antithrombin III (AT III) and Trp49-modified AT III on plasma level of 6-keto-PGF1 alpha in rats. Murakami, K; Okabe, H; Okajima, K; Takatsuki, K; Uchiba, M, 1995) | 1.01 |
"Indomethacin pre-treatment (12.5 mg, s.c.) eliminated the IOP response to administered anandamides and arachidonic acid." | ( Effects of topical anandamides on intraocular pressure in normotensive rabbits. Fich, M; Jarho, P; Järvinen, K; Järvinen, T; Mahadevan, V; Pate, DW; Urtti, A, 1996) | 1.02 |
"Indomethacin treatment (75 mg daily) seemed to have a complete or partial effect in most patients treated as such (n = 17)." | ( Idiopathic stabbing headache (jabs and jolts syndrome) al-Sabbah, H; de Isla, C; Espejo, J; Pareja, JA; Ruiz, J, 1996) | 1.02 |
"3. Indomethacin (1 microM) treatment abolished responses to 2 methylthio ATP, alpha,beta methylene ATP and UTP, while spasm to ATP was significantly inhibited." | ( P2-purinoceptors mediating spasm of the isolated uterus of the non-pregnant guinea-pig. Hollingsworth, M; Piper, AS, 1996) | 0.81 |
"Indomethacin treatment for 1 month increased systolic (+/- s.e.m.: 4.1 +/- 2.2 mm Hg; 95% confidence interval 0 to 8.3 mm Hg) and diastolic BP (2.7 +/- 1.1 mm Hg; 0.4 to 4.9 mm Hg) without altering cardiac output (P = 0.59), implying an increase in total peripheral resistance." | ( Potential mechanisms by which nonsteroidal anti-inflammatory drugs elevate blood pressure: the role of endothelin-1. Day, RO; Johnson, AG; Nguyen, TV; Owe-Young, R; Williamson, DJ, 1996) | 1.02 |
"Indomethacin pretreatment attenuated the responses to both stimuli as did phosphoramidon." | ( Mechanism of irritant-induced cough: studies with a kinin antagonist and a kallikrein inhibitor. Church, MK; Evans, DM; Featherstone, RL; Jones, DM; Olsson, H; Parry, JE; Szelke, M, 1996) | 1.02 |
"This indomethacin-treated normal platelet mimicked the CHS collagen-induced aggregation pattern." | ( Inhibition of collagen-induced platelet aggregation in Japanese black cattle with inherited platelet disorder, Chediak-Higashi syndrome. Goryo, M; Inanami, O; Kaketa, K; Kamata, R; Kobayashi, H; Okabe, S; Okada, K; Oshima, T; Saito, S; Sakaguchi, M; Sato, I; Shimizu, H; Shuto, F; Suzuki, T; Tachikawa, E; Tanaka, T; Uetsuki, J, 1996) | 0.75 |
"Indomethacin treatment dose-dependently prevented increases in paw volume and osteoclast number." | ( Effects of indomethacin administration on bone turnover and bone mass in adjuvant-induced arthritis in rats. Aota, S; Kikuchi, S; Miura, M; Nakamura, T; Okazaki, Y; Segawa, Y; Suzuki, K; Tanaka, Y, 1996) | 1.41 |
"The indomethacin-treated infants had a lower incidence of NEC and IVH." | ( Is surgical ligation of a patent ductus arteriosus the preferred initial approach for the neonate with extremely low birth weight? Garcia-Prats, JA; Jaksic, T; Pokorny, WJ; Robie, DK; Waltrip, T, 1996) | 0.77 |
"Indomethacin treatment at 3 mg/kg/day from day 18 to day 20 of gestation significantly decreased the activity of 15-PGDH in neonatal lungs." | ( Inhibitory effect of indomethacin on neonatal lung catabolism of prostaglandin E2: possible mechanism of the re-opening of the ductus arteriosus after indomethacin therapy. Akahori, F; Arishima, K; Ikeda, Y; Masaoka, T; Takizawa, T; Togashi, H; Yamamoto, M, 1996) | 1.33 |
"Indomethacin treatment significantly decreased bile acid-independent bile flow and biliary secretion of bile acid and cholesterol, while increasing biliary phospholipid output in vivo." | ( Bile secretion in rats with indomethacin-induced intestinal inflammation. Hayakawa, T; Hoshino, M; Inagaki, T; Kamiya, Y; Miyaji, M; Mizuno, K; Nakazawa, T; Ohhara, H; Takeuchi, T; Uchida, A; Yamada, H; Yamada, T, 1996) | 1.31 |
"Indomethacin pretreatment blunted the NE-induced augmentation in eicosanoid excretion and resulted in further increases in arterial pressure and in renal vascular resistance." | ( Eicosanoid modulation of the norepinephrine effect on blood pressure and renal hemodynamics in humans. Falardeau, P; Grose, JH; Isenring, P; Lebel, M, 1996) | 1.02 |
"Indomethacin treatment improved mean graft-adherent bacterial clearance by 54% at 7 days and 75% at 28 days compared with control (not significant)." | ( Prostaglandin E2 modulates monocyte MHC-II (Ia) suppression in biomaterial infection. Bergamini, TM; Brittian, KR; Henke, PK; Polk, HC, 1997) | 1.02 |
"In indomethacin-treated rats, NKA further increased motility but decreased indomethacin-stimulated bicarbonate secretion by 70%." | ( Neurokinin A increases duodenal mucosal permeability, bicarbonate secretion, and fluid output in the rat. Flemström, G; Hällgren, A; Hellgren, S; Hellström, PM; Lördal, M; Nylander, O, 1997) | 0.81 |
"Indomethacin treatment was provided by daily subcutaneous injections (1 microgram/g body weight)." | ( Tumor suppressive action of indomethacin is NK-cell-independent. Asea, A; Cvetkovska, E; Edström, S; Hellstrand, K, ) | 1.15 |
"Indomethacin treatment or removal of the venular endothelium will attenuate functional arteriolar vasodilation in the hamster cremaster muscle. " | ( Influence of venular prostaglandin release on arteriolar diameter during functional hyperemia. Boyd, D; Gardner, AL; Hester, RL; McKay, MK, 1998) | 1.74 |
"Indomethacin is the treatment of choice of benign cough headache, but has no effect in symptomatic cases, which respond to suboccipital craniectomy." | ( [Headaches due to cough, exertion and sexual intercourse]. Berciano, J; Oterino, A; Pascual, J, 1997) | 1.02 |
"Indomethacin treatment did not affect either of the two CPT activities of the mitochondria isolated from tumour tissue." | ( Carnitine palmitoyltransferase II activity is decreased in liver mitochondria of cachectic rats bearing the Walker 256 carcinosarcoma: effect of indomethacin treatment. Colquhoun, A; Curi, R; Seelaender, MC; Williams, JF; Zammitt, VA, 1998) | 1.22 |
"Indomethacin pretreatment inhibited increases in mRNA and protein for PGHS-2 after ischemia, while 7-NI had little effect on increases in PGHS-2 immunoreactivity." | ( Effects of anoxic stress on prostaglandin H synthase isoforms in piglet brain. Bari, F; Beasley, TC; Busija, DW; Dégì, R; Louis, TM; Thore, C; Thrikawala, N, 1998) | 1.02 |
"In indomethacin-pretreated pigs, ET-1 significantly increased Rrs and decreased Crs." | ( Prostanoids counterbalance the bronchoconstrictor activity of endothelin-1 in pigs. Albertini, M; Clement, MG; Dimori, M; Marzani, M, 1998) | 0.81 |
"Indomethacin pretreatment, although by itself nondamaging, was associated with elevated intracellular Ca2+ concentrations and an increased cellular permeability, an effect that was dependent on extracellular Ca2+." | ( Indomethacin increases susceptibility to injury in human gastric cells independent of PG synthesis inhibition. Deshpande, Y; Kokoska, ER; Miller, TA; Smith, GS; Wolff, AB, 1998) | 2.46 |
"Indomethacin treatment was successful in 27 infants." | ( Surgical ligation of patent ductus arteriosus in very low birth weight infants: is it safe? Atkinson, JB; Bustorff-Silva, JM; Fonkalsrud, EW; Perez, CA; Villasenor, E, 1998) | 1.02 |
"Oral indomethacin treatment did not reduce fluorescein staining on day 14." | ( Suppression of laser-induced choroidal neovascularization by oral tranilast in the rat. Akahane, S; Kitamura, T; Kitazawa, M; Kurokawa, T; Takehana, Y; Tsukahara, Y; Yoshimura, N, 1999) | 0.76 |
"Indomethacin pretreatment of primary and GP8 cells turned vasorelaxation into contraction while N(omega)-nitro-L-arginine pretreatment decreased the vasorelaxation induced by primary, but not by GP8 cells." | ( Vasoactive substances produced by cultured rat brain endothelial cells. Deli, MA; Gecse, A; Kis, B; Krizbai, IA; Mezei, Z; Papp, JG; Pataricza, J; Szabó, CA; Telegdy, G, 1999) | 1.02 |
"Indomethacin treatment increased the expression of both Cox-I and Cox-II in co-cultured SMC under high flow conditions." | ( Sustained pulsatile flow regulates endothelial nitric oxide synthase and cyclooxygenase expression in co-cultured vascular endothelial and smooth muscle cells. Cahill, PA; Cappadona, C; Hendrickson, RJ; Redmond, EM; Sitzmann, JV; Yankah, EN, 1999) | 1.02 |
"Indomethacin-treated infected mice had higher mortality compared to untreated infected animals." | ( Prostaglandins mediate suppression of lymphocyte proliferation and cytokine synthesis in acute Trypanosoma cruzi infection. Abrahamsohn, IA; Pinge-Filho, P; Tadokoro, CE, 1999) | 1.02 |
"Indomethacin treatment eliminated the postexercise increase in PGE2 concentration and completely reversed the suppression of total and per CD16(+)56(+) NKCA 2 h after exercise." | ( Indomethacin inhibits circulating PGE2 and reverses postexercise suppression of natural killer cell activity. Gannon, GA; Rhind, SG; Shek, PN; Shephard, RJ; Suzui, M, 1999) | 2.47 |
"Indomethacin treatment (5 mg/kg subcutaneously) completely abolished these responses." | ( Polysaccharide mannan components of Candida albicans and Saccharomyces cerevisiae cell wall produce fever by intracerebroventricular injection in rats. Akarsu, ES; Ataoğlu, H; Ataoğlu, O; Doğan, MD, 1999) | 1.02 |
"An indomethacin treatment strategy for PDA based on measurement of the ductal flow pattern is associated with a reduction in the total doses of indomethacin administered, and a reduced rate of complications, compared with a conventional protocol. " | ( Echocardiographic flow pattern of patent ductus arteriosus: a guide to indomethacin treatment in premature infants. Peng, CT; Su, BH; Tsai, CH, 1999) | 1.16 |
"Indomethacin co-treatment partially prevented blood pressure elevation, restored responsiveness to phenylephrine and improved sensitivity to acetylcholine." | ( Cyclooxygenase inhibition reduces blood pressure elevation and vascular reactivity dysfunction caused by inhibition of nitric oxide synthase in rats. da Cunha, V; Oliveira, PA; Poton, S; Pretti, SC; Rossoni, LV; Stefanon, I; Vassallo, DV, 2000) | 1.03 |
"The indomethacin treatment of the premedicated animals with the drug hardly affected either the malondialdehyde (MDA) or superoxide dismutase (SOD) level in gastric tissue while the ulcerative agent itself significantly enhanced both the levels." | ( The role of antioxidant activity of Phyllanthus emblica fruits on prevention from indomethacin induced gastric ulcer. Bandyopadhyay, SK; Pakrashi, A; Pakrashi, SC, 2000) | 1.01 |
"In indomethacin-pretreated vessels, subsequent deendothelisation by air bubbles enhanced the constrictor responses to NA." | ( Effect of indomethacin and deendothelisation on vascular responses in the renal artery. Kriska, M; Kristová, V; Kurtanský, A; Vojtko, R, 2000) | 1.22 |
"Indomethacin pretreatment increased both PAS- and AB-positive perfusate glycoprotein at baseline; subsequent acid superfusion decreased perfusate glycoproteins and gel thickness." | ( Dynamic regulation of mucus gel thickness in rat duodenum. Akiba, Y; Engel, E; Guth, PH; Kaunitz, JD; Nastaskin, I, 2000) | 1.03 |
"Indomethacin (2.5 microM) treatment of both the donor bronchi and the airway segment and removal of donor epithelium abolished the rightward shift in the acetylcholine-response curves." | ( An epithelial-derived factor inhibits contraction in canine perfused bronchial segments. Armour, CL; Black, JL; Johnson, PR; McParland, BE, 2000) | 1.03 |
"Indomethacin pretreatment significantly attenuated ozone-induced decreases in FVC and FEV(1) in Nm, but not in Asth." | ( Cyclooxygenase metabolites play a different role in ozone-induced pulmonary function decline in asthmatics compared to normals. Alexis, N; Corey, P; O'Byrne, P; Pengelly, D; Silverman, F; Tarlo, S; Urch, B, 2000) | 1.03 |
"Indomethacin (Indo) treatment of infected hamsters reduced abscess weight by 30% at 7 days post-infection presumably by inhibition of PGE2." | ( Liver function tests during amoebic liver abscess formation in indomethacin-treated hamsters. Mata-González, S; Ramos-Martínez, E; Sánchez-Ramírez, B; Talamás-Rohana, P; Valdez, A, 2001) | 1.27 |
"In indomethacin-treated rats, both the cytosolic Cu,Zn superoxide dismutase (Cu,Zn-SOD) and mitochondrial Mn-SOD activities were significantly diminished in gastric mucosa as well as the total SOD activity in testis." | ( The protective action of melatonin on indomethacin-induced gastric and testicular oxidative stress in rats. Amer, MA; El-Missiry, MA; Othman, AI, 2001) | 1.1 |
"Indomethacin treatment showed a tendency to delay ulcer healing." | ( [Pharmacological study on the pathological changes of the gastric mucosa in Helicobacter pylori-infected Mongolian gerbils]. Ebata, M; Keto, Y; Okabe, S, 2001) | 1.03 |
"Indomethacin treatment, by itself, did not alter plasma renin activity." | ( Baroreceptor and prostanoid control of fetal renal cortical blood flow and plasma renin activity. Lakhdir, FR; Tong, H; Wood, CE, 2001) | 1.03 |
"Indomethacin treatment was associated with a specific decrease in beta-catenin (but not gamma-catenin) expression." | ( Indomethacin induces differential expression of beta-catenin, gamma-catenin and T-cell factor target genes in human colorectal cancer cells. Albanese, C; D'Amico, M; Hawcroft, G; Hull, MA; Markham, AF; Pestell, RG, 2002) | 2.48 |
"In indomethacin-treated macrophages, nitric oxide production and leishmanicidal ability were partially restored by the addition of exogenous prostaglandin E2." | ( Nitric oxide production by Leishmania-infected macrophages and modulation by prostaglandin E2. Acquafredda, A; Brandonisio, O; Fumarola, L; Leogrande, D; Mitolo, V; Panaro, MA; Sisto, M, 2001) | 0.82 |
"Indomethacin treatment reversed all the measured parameters, although the reversal of mechanical allodynia was only partial." | ( Therapeutic administration of nitric oxide synthase inhibitors reverses hyperalgesia but not inflammation in a rat model of polyarthritis. Fuseler, J; Grisham, M; Roerig, SC; Tedesco, LS; Wolf, R, 2002) | 1.04 |
"The indomethacin treatment cost was $95,157 and that of the control groups was $99,955." | ( Cost-effectiveness of prophylactic indomethacin in very-low-birth-weight infants. Goldberg, RN; Moya, MP, 2002) | 1.07 |
"Indomethacin-treated animals showed less nest building than controls between 1 and 5 h after injection (P<0.05), during which time they were mostly inactive and lay down for longer than controls." | ( Indomethacin blocks pre-partum nest building behaviour in the pig (Sus scrofa): effects on plasma prostaglandin F metabolite, oxytocin, cortisol and progesterone. Burne, TH; Gilbert, CL; Goode, JA; Murfitt, PJ; Walton, SL, 2002) | 2.48 |
"The indomethacin-treated group showed the lowest PGE2 concentration, similar to that of the NS-398 and vehicle-alone treated groups, both without H." | ( Effects of selective cyclooxygenase-2 inhibitor and non-selective NSAIDs on Helicobacter pylori-induced gastritis in Mongolian gerbils. Bhang, CS; Chung, IS; Kim, JI; Kim, SS; Lee, HS; Lee, YS; Park, DH; Song, HJ; Sun, HS; Sung, YJ, 2002) | 0.8 |
"Indomethacin is the best treatment, although HC could respond to other nonsteroidal anti-inflammatory drugs, such as the selective cyclo-oxygenase-2 inhibitors." | ( Hemicrania continua: recent treatment strategies and diagnostic evaluation. Peres, MF, 2002) | 1.04 |
"Indomethacin pretreatment enhanced or slightly reduced the amplitude of contractions evoked by both H2O2 and hydroxyl radical on the intact and denuded preparations, respectively." | ( Effects of various reactive oxygen species on the guinea pig trachea and its epithelium. Bauer, V; Mátyás, S; Pucovský, V, 2002) | 1.04 |
"Indomethacin treatment showed a tendency to delay ulcer healing." | ( Influence of Helicobacter pylori infection on healing and relapse of acetic acid ulcers in Mongolian gerbils. Ebata, M; Keto, Y; Okabe, S; Tomita, K, 2002) | 1.04 |
"In indomethacin-treated rats (n = 6), DRIVE again significantly increased RIHP by 40% (Delta1.9 +/- 0.2 mmHg), but it did not increase La backflux (Delta-39.0 +/- 24.4 pg/min per mm) or significantly decrease proximal reabsorption (Delta1.2 +/- 2.3 nl/min)." | ( Indomethacin blocks enhanced paracellular backflux in proximal tubules. Berndt, TJ; Knox, FG; Ramsey, CR, 2002) | 2.27 |
"Indomethacin-treated eyes showed significantly less inflammatory response, and an insignificantly greater number of antibody-forming cells, than the controls." | ( Indomethacin and the corneal immune response. Belfort, R; Hall, JM; Okumoto, M; Smolin, G, 1976) | 2.42 |
"Indomethacin pretreatment had no effect on the ADH-induced redistribution (17 +/- 2 vs." | ( Redistribution of intrarenal blood flow following ADH administration: lack of inhibition by blockade of prostaglandin in cyclooxygenase. Frolich, JC; Gerber, JG; Nies, AS; Walker, LA, 1978) | 0.98 |
"Indomethacin treatment significantly potentiated the TSH response to synthetic TRH (20 ng." | ( Potentiation by indomethacin of TRH-induced TSH secretion in the rat. Kabayashi, I; Mori, M; Tonooka, N; Tsuyusaki, K, 1979) | 1.33 |
"Indomethacin treatment changed the blood pressure response to saralasin in such a way that the blood pressure was increased in one patient and was unchanged in the other." | ( Effect of Sar1-ala8-angiotensin II on blood pressure and renin in Bartter's syndrome, before and after treatment with prostaglandin synthetase inhibitors. Aurell, M; Hansson, L; Rudin, A; Westberg, G, 1979) | 0.98 |
"Indomethacin pretreatment prevented the first part of the febrile response and only a slight temperature rise occurred after a long latency." | ( Endotoxin fever in the newborn kitten. The role of prostaglandins and monoamines. Székely, M, 1979) | 0.98 |
"Indomethacin pretreatment also resulted in approximately a 10-fold decrease in thyroidal prostaglandin levels." | ( Regulation of thyroid ornithine ornithine decarboxylase (ODC) by thyrotropin. I. The rat. Akbar, M; Burke, G; Park, S; Richman, R; Yu, S, 1975) | 0.98 |
"Indomethacin and aspirin treatment of animals injected with PMSG also reduced the ovarian weight gain." | ( The effect of inhibition of prostaglandin synthesis on ovarian hypertrophy in the rat. Castracane, VD; Shaikh, AA; Tankenow, LF, 1975) | 0.98 |
"Indomethacin pretreatment of cyclase activation." | ( Pathogenesis of Salmonella-mediated intestinal fluid secretion. Activation of adenylate cyclase and inhibition by indomethacin. Charney, AN; Formal, SB; Giannella, RA; Gots, RE; Greenough, WB, 1975) | 1.19 |
"Indomethacin treatment, 1 h before LH, prevented the LH-induced increase in ovarian PGF levels, depressed PGF values considerably in saline-injected controls but produced no significant inhibition of ovarian cAMP and progesterone levels." | ( Effects of indomethacin and aminoglutethimide phosphate in vivo on luteinizing-hormone-induced alterations of cyclic adenosine monophosphate, prostaglandin F, and steroid levels in preovulatory rat ovaries. Armstrong, DT; Dorrington, JH; Robinson, J, 1976) | 1.37 |
"In indomethacin-treated animals, there was a striking reduction of secretion in CT loops (0.07 ml per cm per 4 hr, P less than 0.001)." | ( Effect of indomethacin on cholera-induced fluid movement, unidirectional sodium fluxes, and intestinal cAMP. Gotterer, GS; Hendrix, TR; Rajendra, GR; Turjman, NA; Wald, A, 1977) | 1.17 |
"1. Indomethacin treatment of renomedullary interstitial cells (RIC) causes a marked increase in number and size of their lipid droplets. " | ( Functional-morphological correlates of renomedullary interstitial cells. Brooks, B; Brown, P; Muirhead, EE; Pitcock, JA; Rightsel, WA, 1976) | 0.88 |
"Indomethacin pretreatment completely blocked the oil stimulated DCR as well as all prostaglandin increases following either stimulus." | ( Uterine prostaglandin levels following stimulation of the decidual cell reaction: effects of indomethacin and tranylcypromine. Baggett, B; Jonsson, HT; Ledford, BE; Rankin, JC, 1979) | 1.2 |
"Indomethacin-treated bovine iris-ciliary body microsomes (IBIM) have been studied for their ability to convert PG endoperoxides into either thromboxane-A2 (TxA2)-like or prostacyclin (PGI2)-like activity. " | ( Microsomal preparations of normal bovine iris-ciliary body generate prostacyclin-like but not thromboxane-A2-activity. Eakins, HM; Eakins, KE; Kulkarni, FS; Saber, WL, 1977) | 1.7 |
"Indomethacin pretreatment abolished the toxic AA effect." | ( Anti-aggregatory effect of prostacyclin (PGI2) in vivo. Bayer, BL; Blass, KE; Förster, W, 1979) | 0.98 |
"Only indomethacin treatment was successful in reversing the biochemical abnormalities and improving the growth pattern." | ( Successful indomethacin treatment of two paediatric patients with severe tubulopathies. A boy with an unusual hypercalciuria and a girl with cystinosis. Bétend, B; David, L; François, R; Hermier, M; Vincent, M, 1979) | 1.1 |
"Indomethacin pretreatment shortened the duration of PGE2-induced abortion in primigravid and multigravid groups of patients by about 4 and 2 hours respectively." | ( Indomethacin increases abortifacient effect of PGE2 in man. Basta, A; Dłuzniewska, M; Klimczyk, K; Małolepazy, A; Piotrowski, J; Spławinski, JA, 1979) | 2.42 |
"Indomethacin treatment raised the incidence of psychic complaints over those with ASA or placebo (P.05)." | ( Prostaglandin biosynthesis inhibitors and endometriosis. Kauppila, A; Puolakka, J; Ylikorkala, O, 1979) | 0.88 |
"Indomethacin treatment significantly (2P less than 0.019) inhibited haversian remodelling as estimated by fluorochrome labelling." | ( Indomethacin-induced inhibition of haversian remodelling in rabbits. Bang, G; Sudmann, E, 1979) | 2.42 |
"Indomethacin pretreatment caused a dose-related decrease in the plasma fibrinogen response 24 h after fracture: 1, 2, 10 or 20 mg/kg/day of drug reduced the response by approximately 3, 10, 13 and 23%." | ( The effect of indomethacin on the biochemical response to fracture stress in rats. Broom, J; Fleck, A; Gedeon, G; Rowe, DJ, 1979) | 1.34 |
"Indomethacin treatment (2.5 mg/kg i.v.) decreased renal blood flow (35%) and inhibited urine PG-excretion." | ( Kidney volume expansion and prostaglandin release by bradykinin. The effect of indomethacin pretreatment. Olsen, UB, 1978) | 1.21 |
"Indomethacin treatment precipitated gastric ulceration, which led to the formation of a gastro-colic fistula." | ( Gastro-colic fistula secondary to benign gastric ulceration. Taylor, R, 1978) | 0.98 |
"Indomethacin pretreatment inhibited the hemodynamic response to furosemide." | ( The influence of indomethacin on the pharmacokinetics, diuretic response and hemodynamics of furosemide in the dog. Branch, RA; Data, JL; Gerkens, J; Nies, AS; Rane, A; Wilkinson, GR, 1978) | 1.32 |
"Indomethacin treatment did not terminate pregnancy: the proportion of animals pregnant on Days 5, 7, 10 and 16 was not affected, although fetal mortality was slightly greater in these animals." | ( The importance of prostaglandin synthesis for the initiation of blastocyst implantation in the hamster. Evans, CA; Kennedy, TG, 1978) | 0.98 |
"Indomethacin treatment neutralized the differences between the different diet groups." | ( Influence of linoleic acid in the diet on arterial pressure of salt loaded rats. II. Effects on plasma catecholamine concentration, renin activity, and reactivity of isolated vessels. Davidova, F; Förster, W; Hoffmann, P; Orbetzova, V; Pönicke, K; Somova, L; Taube, C, 1978) | 0.98 |
"Indomethacin treatment caused no changes in the spontaneous motility, and this inhibitor of prostaglandins synthesis decreased the responses of epididymis to norepinephrine or acetylcholine." | ( Effects of prostaglandins and indomethacin on rat epididymal responses to norepinephrine and acetylcholine. Hib, J; Oscar, P, 1978) | 1.27 |
"Indomethacin treatments increased serum potassium concentration and urinary Na/K ratio, and improved the response of blood pressure to angiotensin II infusion, while it decreased plasma renin activity, plasma aldosterone and urinary kallikrein." | ( Quantitative and qualitative estimation of urinary kallikrein in a patient with Bartter's syndrome. Kumagai, A; Matsuda, Y; Mikami, K; Moriya, H; Nishikawa, T; Shirai, K; Tamura, Y; Watanabe, M; Yamada, K; Yamamoto, M, 1978) | 0.98 |
"The indomethacin pretreatment had no effect on pupil size of any group, but phenoxybenzamine (PBA) reduced the mydriatic effect, implying a direct or a predominant role of NE on iris muscle." | ( Effects of prostaglandins and norepinephrine on ocular pressure and pupil size in rabbits following bilateral cervical ganglionectomy. Cheek, WV; Waitzman, MB; Woods, WD, 1979) | 0.74 |
"Indomethacin pretreatment prevented an alteration in ocular vascular permeability 1 1/2 hours after the injection of 100 mug per kilogram of endotoxin and significantly reduced the alteration 4 hours after endotoxin." | ( The effects of aspirin and indomethacin on the ocular response to circulating bacterial endotoxin in the rabbit. Howes, EL; McKay, DG, 1976) | 1.27 |
"Indomethacin treatment had no effect on the serum TSH or prolactin response to 100 mug TRH or the serum T3 and T4 levels." | ( The effect of aspirin and indomethacin on the TRH response in man. Burrow, GN; Donabedian, RK; Frantz, AG; Ramey, JN; Spaulding, SW; Speroff, L, 1976) | 1.28 |
"Indomethacin pretreatment resulted in 60% reduction of PRA following furosemide, and three of these subjects now fell into the low renin category." | ( Suppression of plasma renin activity by indomethacin in man. Dormois, JC; Frölich, BL; Frölich, JC; Hollifield, JW; Michelakis, AM; Oates, JA; Seyberth, H, 1976) | 1.24 |
"Indomethacin treatment was without effect, and the mean aortic pressure of all rabbits varied generally between 65 and 80 mm." | ( Indomethacin and blood pressure control. Brooks, B; Brosius, WL; Muirhead, EE, 1976) | 2.42 |
"Indomethacin pretreatment abolished the biosynthesis of PGD2." | ( Biosynthesis of prostaglandin D2. 1. Formation of prostaglandin D2 by human platelets. Knapp, HR; Oates, JA; Oelz, O; Oelz, R; Sweetman, BJ, 1977) | 0.98 |
"Indomethacin treatment before lens extraction and vitrectomy-lensectomy reduces postoperative inflammation as measured by protein determination of the ocular fluid." | ( Indomethacin inhibition of prostaglandin-mediated inflammation following intraocular surgery. Huang, K; Janevicius, R; McGetrick, J; Peyman, GA, 1977) | 3.14 |
"In indomethacin-treated ECV-expanded rats an increase in relative inner cortical perfusion was observed." | ( Effects of prostaglandin inhibition on intrarenal hemodynamics in acutely saline-loaded rats. Düsing, R; Kramer, HJ; Melder, B, 1977) | 0.77 |
"Indomethacin treatment lowered both serum calcium and the plasma level of 15-keto-13,14-dihydro-PGE2." | ( Prostaglandin-mediated hypercalcemia in the VX2 carcinoma-bearing rabbit. Hubbard, WC; Oates, JA; Oelz, O; Seyberth, HW; Sweetman, BJ; Watson, JT, 1977) | 0.98 |
"Indomethacin treatment had no effect on plasma kininogen levels in healthy volunteers." | ( A novel relationship between plasma kininogen and rheumatoid. Brooks, PM; Dick, WC; Sharma, JN; Zeitlin, IJ, 1976) | 0.98 |
"Indomethacin pretreatment inhibits the increase of renal blood flow as well as the cortical blood redistribution." | ( Renal cortical blood redistribution after bumetanide related to heterogenicity of cortical prostaglandin metabolism in dogs. Ahnfelt-Ronne, I; Olsen, UB, 1976) | 0.98 |
"Indomethacin pretreatments of rabbits did not significantly alter the PMNs migration indicating that PGs synthetized in vivo was not involved in the migration." | ( Effects of prostaglandins on leukocyte migration. Izawa, Y; Masuda, K; Shibuya, E, 1976) | 0.98 |
"Indomethacin treatment did not inhibit or suppress spontaneous or oxytocin-induced contractions, which were of the same intensity in indomethacin-treated as in control rats." | ( The effect of indomethacin on uterine contractility and luteal regression in pregnant rats at term. Chantharaksri, U; Fuchs, AR; Smitasiri, Y, 1976) | 1.34 |
"5 Indomethacin treatment did not affect monoamine oxidase and catechol O-methyl-transferase activities in the different tissues." | ( Indomethacin-induced increase in noradrenaline turnover in some rat organs. Fredholm, BB; Hedqvist, P, 1975) | 2.26 |
"Indomethacin treatment at the time of implantation interfered with pregnancy and caused degeneration and resorption of embryos." | ( Effect of indomethacin on egg transport and pregnancy in the rabbit. El-Banna, AA; Sacher, B; Schilling, E, 1976) | 1.38 |
"Indomethacin treatment and/or handling stress induced by simply measuring rectal temperature was found to dramatically alter the direction of the conditioned NK cell response." | ( The direction of the conditioned natural killer cell response can be re-directed with indomethacin and/or handling. Ghanta, V; Hiramoto, N; Hiramoto, R; Hsueh, CM; Rogers, C, ) | 1.08 |
"Indomethacin treatment applied after the sixth annual follow up significantly reduced DLCO and Dm." | ( Biphasic lung diffusing capacity: detection of early asbestos induced changes in lung function. Boschi, S; Dujić, Z; Eterović, D; Sarić, M; Tocilj, J, 1992) | 1 |
"Indomethacin pretreatment caused an apparent dose-related increase in pressor responses in all animals." | ( Effects of endothelin upon blood pressure in normotensive rabbits and in perinephritis hypertension. Hamilton, CA; Huang, YT; Reid, JL, 1992) | 1 |
"Indomethacin treatment prior to induction of colitis reduced endogenous mucosal PGE2 levels and exacerbated macroscopic ulceration and net fluid absorption." | ( Indomethacin worsens and a leukotriene biosynthesis inhibitor accelerates mucosal healing in rat colitis. Empey, LR; Fedorak, RN; Walker, K, 1992) | 2.45 |
"Indomethacin treatment did not affect baseline SGaw or methacholine airway responsiveness." | ( Effect of indomethacin on leukotriene4-induced histamine hyperresponsiveness in asthmatic subjects. Christie, PE; Hawksworth, R; Lee, TH; Spur, BW, 1992) | 1.41 |
"Indomethacin pretreatment failed to prevent the permeability-enhancing action of SP." | ( Effect of substance P administration on vascular permeability in the rat dental pulp and submandibular gland. Fazekas, A; Györfi, A; Irmes, F; Rosivall, L, 1992) | 1 |
"With indomethacin treatment diurnal rectal fluid production dropped by about 50% and all prostanoids measured in urine and rectal fluid decreased below control values." | ( Secretory diarrhea in villous adenoma of rectum: effect of treatment with somatostatin and indomethacin. Hoekman, K; Keirse, MJ; Meinders, AE; Noort, WA; Smelt, AH, 1992) | 0.96 |
"Indomethacin treatment had no effect on control RBF, mean arterial pressure, or renal vascular resistance in the 40-wk-old SHR." | ( Effect of cyclooxygenase inhibition on renal blood flow autoregulation in SHR. Iversen, BM; Kvam, FI; Mørkrid, L; Ofstad, J; Sekse, I, 1992) | 1 |
"Indomethacin pretreatment induced a dose-dependent vasoconstriction by thiopental in endothelium-intact rings and decreased the vasodilation due to propofol.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Effects of propofol and thiopental in isolated rat aorta and pulmonary artery. Johns, RA; Lynch, C; Park, WK, 1992) | 1 |
"Indomethacin is a powerful treatment for polyhydramnios but its use requires close monitoring of the fetal heart." | ( Indomethacin for the treatment of polyhydramnios: a case of constriction of the ductus arteriosus. D'Orsogna, L; Mohen, D; Newnham, JP, 1992) | 2.45 |
"In indomethacin-treated bones, however, caffeine potentiated the stimulatory effect on 45Ca release induced by choleratoxin and forskolin." | ( Caffeine has the capacity to stimulate calcium release in organ culture of neonatal mouse calvaria. Lerner, UH; Mellström, D, 1992) | 0.8 |
"Indomethacin pretreatment significantly inhibited the effect of sucralfate, but not SOS, on the stimulation of phospholipid release." | ( Effect of sucralfate on components of mucosal barrier produced by cultured canine epithelial cells in vitro. Boland, CR; Kraus, ER; Scheiman, JM; Yoshimura, K, 1992) | 1 |
"Indomethacin pretreatment had no effect on baseline spirometry between the two study days; however, the baseline geometric mean PD20FEV1 fell from 145 +/- 2 cbu (+/- percent SD) after placebo pretreatment to 65 +/- 1 cbu (+/- percent SD) on the indomethacin day (p = 0.046)." | ( Indomethacin and methacholine tolerance in normal subjects. Role of prostaglandin synthesis in the attenuation of methacholine's effect during repeated inhalation challenges. Beckett, WS; Haber, AD, 1992) | 2.45 |
"Indomethacin treatment did not correct the increased response to noradrenaline in microvessel preparations." | ( Effect of indomethacin on the microvessel reactivity of two-kidney, one-clip hypertensive rats. Costa, SG; de Carvalho, MH; de Oliveira, MA; Fortes, ZB; Nigro, D; Scivoletto, R, ) | 1.26 |
"Indomethacin pretreatment restored the LVP effect on creatinine cl." | ( Effects of experimental potassium depletion on renal function and urinary prostanoid excretion in normal women during moderate anti-diuresis. Agnoli, GC; Borgatti, R; Cacciari, M; Ikonomu, E; Lenzi, P; Marinelli, M, 1992) | 1 |
"Indomethacin treated animals demonstrated significantly less polymorphonuclear leukocyte infiltration and decreased degeneration." | ( The effect of indomethacin on acute radiation induced gastrointestinal injury: a morphologic study. Halter, SA; Rose, PG; Su, CM, 1992) | 1.37 |
"Indomethacin pretreatment abolished most of these responses, suggesting that acute reactions following photodisruption largely depended on prostaglandin synthesis in iris tissue." | ( Prostaglandin E in rabbit aqueous humor after Nd-YAG laser photodisruption of iris and the effect of topical indomethacin pretreatment. Joo, CK; Kim, JH, 1992) | 1.22 |
"Indomethacin pretreatment blunted the hyperglycemia caused by GM-CSF injection; however, it did not inhibit the increased glucose utilization by immune-competent cells." | ( In vivo metabolic response of hepatic nonparenchymal cells and leukocytes to granulocyte-macrophage colony-stimulating factor. Bagby, GJ; Lang, CH; Nelson, S; Schuler, A; Spitzer, JJ; Spolarics, Z, 1992) | 1 |
"Indomethacin treatment reduced arteriolar dilation to bradykinin (BK, 1-100 ng), which was significantly inhibited by additional administration of L-NNA." | ( Regulation of arteriolar tone and responses via L-arginine pathway in skeletal muscle. Kaley, G; Koller, A; Messina, EJ; Rodenburg, JM; Wolin, MS, 1992) | 1 |
"Indomethacin treatment did not alter the outcome in these two infections, thus arguing against reduced prostaglandin synthesis as an explanation for the increase in resistance to infection." | ( Dietary fish-oil supplementation in experimental gram-negative infection and in cerebral malaria in mice. Blok, WL; Buurman, WA; Curfs, JH; Eling, WM; van der Meer, JW; Vogels, MT, 1992) | 1 |
"Indomethacin treatment partially attenuates the hypotensive effects of the basic amino acids." | ( Effect of N-substituted arginine compounds on blood pressure in anesthetized rats. Cathapermal, S; Farhat, M; Myers, A; Ramwell, PW; Thomas, G, 1992) | 1 |
"Indomethacin treatment of the patients reduced intoxication, did not affect leukocytic function, diminished plasma chemiluminescence." | ( [Functional activity of leukocytes and enzyme indicators in acute intestinal infections]. Malov, VA; Pak, SG; Popov, PIu; Roslyĭ, IM, 1992) | 1 |
"Indomethacin pretreatment (n = 11) to inhibit prostanoid production enhanced the magnitude of CSD-induced vasodilation from the pretreatment levels of 59 +/- 9% (from 82 +/- 5 to 130 +/- 8 microns for 1.7 min) to the post-treatment levels of 82 +/- 13% (from 78 +/- 5 to 142 +/- 12 microns for 1.8 min).(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Pial arteriolar constriction following cortical spreading depression is mediated by prostanoids. Busija, DW; Leffler, CW; Shibata, M, 1992) | 1 |
"4. Indomethacin pretreatment (5 mg/kg) significantly antagonized the hypothermia induced by GABA and muscimol." | ( Opioid and prostaglandin mechanisms involved in the effects of GABAergic drugs on body temperature. Miñano, FJ; Sancibrian, M; Serrano, JS, 1991) | 0.8 |
"In indomethacin (10 microM)-treated washed platelets superoxide dismutase (SOD; 60 U/ml) or ferricytochrome c (FCC; 70 microM) inhibited platelet aggregation by thrombin but not that by collagen or ADP." | ( Superoxide dismutase cooperates with prostacyclin to inhibit platelet aggregation: a comparative study in washed platelets and platelet rich plasma. de Nucci, G; Salvemini, D; Vane, JR, 1991) | 0.8 |
"Indomethacin pretreatment caused only slight attenuation of the peptide 6A-induced increase in femoral blood flow." | ( Fibrin(ogen) degradation product peptide 6A increases femoral artery blood flow in dogs. Andersson, R; Lawson, D; Mehta, J; Nichols, W; Saldeen, K; Saldeen, T, 1991) | 1 |
"Indomethacin treatment led to a dose-dependent inhibition in the receptor expression in the cells treated with TPA plus insulin more than that in the cells with FSH plus insulin, suggesting that the synergistic action was dependent upon cyclooxygenase and/or phospholipase A2 activity." | ( Tumor-promoting phorbol ester acts synergistically with insulin to induce lutropin receptor expression in rat granulosa cells. Hattori, M; Horiuchi, R; Takahashi, M, 1991) | 1 |
"Indomethacin pretreatment of veins did not influence the endothelin-induced contractions, suggesting that cyclo-oxygenase products are not involved in the response." | ( Endothelium-dependent relaxation and effects of prostacyclin, endothelin and platelet-activating factor in human hand veins and arteries. Arner, M; Högestätt, ED, 1991) | 1 |
"In indomethacin-pretreated hamsters, acetylcholine produced similar vasodilatation before and after exposure to cigarette smoke extract." | ( Cigarette smoke extract attenuates endothelium-dependent arteriolar dilatation in vivo. Mayhan, WG; Rennard, SI; Rubenstein, I; Yong, T, 1991) | 0.8 |
"Indomethacin pretreatment potentiated the nephrotoxic potential of NDPS and its two metabolites, while dazmegrel pretreatment attenuated NDPS nephrotoxicity without marked effects on NDHS or NDHSA nephropathy." | ( Effect of autacoid modulation on N-(3,5-dichlorophenyl)succinimide (NDPS) and NDPS metabolite nephrotoxicity. Anestis, DK; Brown, PI; Nicoll, DW; Rankin, GO; Teets, VJ; Valentovic, MA, 1991) | 1 |
"The indomethacin pretreatment also resulted in a potentiation of the natriuretic effect of clonidine at all infusion rates." | ( Potentiation of the natriuretic effect of clonidine following indomethacin in the rat. Blandford, DE; Smyth, DD, 1991) | 1 |
"This indomethacin treatment immediately reversed the hypotension, restored the organ perfusion, delayed the haemoconcentration and thrombocytopenia and prevented death." | ( Sequential release of tumour necrosis factor, platelet activating factor and eicosanoids during endotoxin shock in anaesthetized pigs: protective effects of indomethacin. Ben-Efraim, S; Bonta, IL; Heiligers, JP; Mózes, T; Saxena, PR; Tak, CJ; Zijlstra, FJ, 1991) | 0.93 |
"The indomethacin treated group required significantly less postoperative pain treatment than did the placebo group." | ( [Indomethacin enema in treatment of postoperative pain after knee arthrotomy. A double-blind controlled trial]. Hemmingsen, C; Poulsen, JA; Risbo, A, 1991) | 1.67 |
"When indomethacin-treated rat platelets were activated with the thromboxane A2 analogue U46619, the presence of a second agonist such as collagen." | ( Dietary fat modifies thromboxane A2-induced stimulation of rat platelets. Feijge, MA; Heemskerk, JW; Hornstra, G; Kester, A, 1991) | 0.74 |
"Indomethacin treatment was also found to reduce elevated prostaglandin E2 (PGE)2 levels in the skin of BP-treated mice, whereas PGE2 levels were not significantly raised in DMBA-treated mice." | ( Indomethacin inhibits the chemical carcinogen benzo(a)pyrene but not dimethylbenz(a)anthracene from altering Langerhans cell distribution and morphology. Andrews, FJ; Halliday, GM; Muller, HK; Narkowicz, CK, 1991) | 2.45 |
"In indomethacin-treated lungs (group 3) and indomethacin and U60257-treated lungs (group 4), total and segmental vascular resistance was not significantly different from untreated lungs (group 1)." | ( Segmental vascular resistance in isolated perfused rat lungs. Influence of vasomotor tone and cyclooxygenase and lipoxygenase inhibition. Anderson, J; Hillyard, R; Raj, JU, 1991) | 0.8 |
"Indomethacin treatment (5 mg/kg) of hypotensive piglets decreased blood flow to all brain regions within 20 min; this decrease in CBF resulted from increases in cerebral vascular resistance of 65 and 281% at 20 and 40 min after treatment, respectively." | ( Opioids and the prostanoid system in the control of cerebral blood flow in hypotensive piglets. Armstead, WM; Busija, DW; Leffler, CW; Mirro, R, 1991) | 1 |
"Indomethacin pretreatment reversed the increased prostanoid synthesis in mucosa exposed to 100% ethanol, with or without mild irritant pretreatment, and partially reversed the protective effect of 25% ethanol." | ( Adaptive cytoprotection against alcohol injury in the rat stomach is not due to increased prostanoid synthesis. Bartula, LL; Miller, TA; Myers, SI; Smith, GS, 1991) | 1 |
"Indomethacin treatment 20 min prior to LPS injection attenuated the hypotension (50 +/- 3 mmHg at 120 min, p less than 0.05) and the decrease of cardiac output (0.18 +/- 0.02 L/min/kg at 120 min, p less than 0.05)." | ( Indomethacin treatment in newborn canine endotoxic shock. Goto, M; Griffin, AJ, 1991) | 2.45 |
"Indomethacin pretreatment significantly attenuated increases in water and sodium content seen at 48 hours in gerbils undergoing repetitive ischemia (peak 80.02 +/- 0.45% and 300 +/- 39 meq/kg dry wt), but did not affect mortality." | ( Effect of indomethacin on edema following single and repetitive cerebral ischemia in the gerbil. Betz, AL; Deluga, KS; Plötz, FB, 1991) | 1.41 |
"Indomethacin treatment was accompanied by maternal side effects 20% of the time, significantly less commonly (P less than .001) than with nylidrin (83%)." | ( A randomized double-dummy comparison between indomethacin and nylidrin in threatened preterm labor. Eronen, M; Kurki, T; Lumme, R; Ylikorkala, O, 1991) | 1.26 |
"Indomethacin treatment did not correct the altered response to norepinephrine in mesenteric preparations studied in vivo in situ." | ( Indirect evidence for an endothelium-derived contracting factor released in arterioles of deoxycorticosterone acetate salt hypertensive rats. de Carvalho, MH; Fortes, ZB; Nigro, D; Scivoletto, R, 1990) | 1 |
"In indomethacin treated skins A23187 did not stimulate but on the contrary inhibited the basal SCC." | ( Role of Ca2+ and prostaglandin in regulation of active Na+ transport in frog skin. Bjerregaard, HF; Nielsen, R, 1990) | 0.79 |
"The indomethacin-treated group was more resistant to reinfection." | ( Prostaglandins in experimental syphilis: treponemes stimulate adherent spleen cells to secrete prostaglandin E2, and indomethacin upregulates immune functions. Fitzgerald, TJ; Rice, T; Tomai, MA; Trachte, GJ, 1991) | 0.97 |
"Indomethacin-treated tumor-bearing mice were also less anorectic than untreated tumor-bearing mice, and their nutritional state, particularly lean body mass, was significantly improved by indomethacin at doses (1 micrograms/g) that did not influence the food intake or body composition in non-tumor-bearing mice." | ( Effects of indomethacin, cytokines, and cyclosporin A on tumor growth and the subsequent development of cancer cachexia. Andersson, C; Gelin, J; Lundholm, K, 1991) | 1.39 |
"Indomethacin pretreatment resulted in the delay of neutrophil immigration into tissues without any change in the glucose response of different liver cells." | ( Metabolic response of isolated liver cells to in vivo phagocytic challenge. Bautista, AP; Spitzer, JJ; Spolarics, Z, 1991) | 1 |
"Indomethacin treatment also disrupted the normal birth process when it occurred, as all females receiving this compound exhibited parturition of only a portion (24-32%) of the total clutch." | ( Exogenous progesterone or indomethacin delays parturition in the viviparous lizard Sceloporus jarrovi. DeMarco, V; Guillette, LJ; Palmer, BD, 1991) | 1.3 |
"Indomethacin pretreatment raised inducible Ia antigen levels on macrophages of NM mice to those seen on cells from untreated high-affinity mice." | ( Induction of leukotriene production before antigen challenge enhances antibody affinity in genetically selected mice. Phillips, C, 1991) | 1 |
"Indomethacin pretreatment reversed these actions, whereas misoprostol administration produced the similar effects as 20% ethanol." | ( Endogenous prostaglandins: its role in gastric mucosal blood flow and ethanol ulceration in rats. Chen, BW; Cho, CH; Hui, WM; Lam, SK; Luk, CT, 1990) | 1 |
"Indomethacin treatment also inhibited PDT-induced vascular stasis and tumor destruction, suggesting that the release of thromboxane is linked to these events." | ( Role of thromboxane and prostacyclin release on photodynamic therapy-induced tumor destruction. Doak, KW; Fingar, VH; Wieman, TJ, 1990) | 1 |
"Indomethacin-treated rats had significantly lower lavage levels of PGE and TxA2 and significantly increased numbers of M." | ( Alterations in lung prostaglandin synthesis and release in murine respiratory mycoplasmosis. Chandler, DB; Reinhard, MK, 1990) | 1 |
"Indomethacin treatment prolonged survival and 40% of these tumour-bearers were 'complete responders'." | ( The effect of indomethacin on food and water intake, motor activity and survival in tumour-bearing rats. Gelin, J; Lundholm, K; Sandström, R, 1990) | 1.36 |
"Indomethacin treatment did not effect the suppression caused by Mac-1+ M phi, suggesting that proataglandin E2 was not involved." | ( Modulation of alloreactivity by Mac-1+, -2+, and -3+ macrophages from normal and tumor-bearing hosts: flow cytofluorometrically separated macrophages. Askew, D; Burger, CJ; Elgert, KD, 1990) | 1 |
"Indomethacin treatment altered the response to noradrenaline only in unrubbed aorta of hypertensive rats." | ( Indirect evidence for an endothelium-derived contracting factor release in aorta of deoxycorticosterone acetate-salt hypertensive rats. Carvalho, MH; Cordellini, S; Fortes, ZB; Nigro, D; Scivoletto, R, 1990) | 1 |
"Indomethacin treatment inhibited PG synthesis in all BDL groups but only decreased the inflammation score in the 6 and 24 hour BDL groups." | ( Common bile ligation in the rabbit: an appropriate model for investigating the relationship of endogenous gallbladder prostanoid synthesis with evolving acute inflammation. Bartula, LL; Haley-Russell, D; Myers, SI; Nabzdyk, W, 1990) | 1 |
"Indomethacin treatment abolished this difference and lowered coronary flow: exercise -3.81(3.75) ml.min-1.g-1; control 0.38(2.44) ml.min-1.g-1." | ( Indomethacin suppresses the coronary flow response to hypoxia in exercise trained and sedentary rats. Baur, TS; Brodowicz, GR; Lamb, DR, 1990) | 2.44 |
"Indomethacin pretreatment (5 mg/kg i.v.) did not change arteriolar responses to AEE, NBA, and BAEE." | ( Mono-L-arginine-containing compounds dilate piglet pial arterioles via an endothelium-derived relaxing factor-like substance. Busija, DW; Leffler, CW; Wagerle, LC, 1990) | 1 |
"Indomethacin pretreatment significantly enhanced arteriolar dilation during CSD (from 73 +/- 4 to 138 +/- 6 microns, 89%, n = 4).(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Cerebral hemodynamics during cortical spreading depression in rabbits. Busija, DW; Leffler, CW; Shibata, M, 1990) | 1 |
"Indomethacin pretreatment blocked synthesis of both PGF and PGE2 for 30 min following AVT treatment." | ( Arginine vasotocin-induced prostaglandin synthesis in vitro by the reproductive tract of the viviparous lizard Sceloporus jarrovi. Gross, TS; Guillette, LJ; Matter, JH; Palmer, BD, 1990) | 1 |
"Indomethacin treatment (5 mg/kg) of hypotensive piglets caused a significant decrease in blood flow to all brain regions within 20 min." | ( Vasopressin and prostanoid mechanisms in control of cerebral blood flow in hypotensive newborn pigs. Armstead, WM; Busija, DW; Leffler, CW; Mirro, R, 1990) | 1 |
"Indomethacin pre-treatment caused 2-fold greater increases in Ra and Rv with histamine and more prolonged changes." | ( Indomethacin enhances histamine-induced pulmonary hemodynamic changes. Ohgami, M; Ohtaka, H; Schellenberg, RR; Tsang, JY, 1990) | 2.44 |
"Indomethacin treatment at either the 1 or 2 mg/kg dose was found to depress the proliferative responses of T cells by 60 and 95%, respectively." | ( Changes in T and B lymphocyte proliferative responses in adjuvant-arthritic rats: antagonism by indomethacin. Bayer, BM; Benensohn, J; Seng, GF, 1990) | 1.22 |
"Indomethacin pretreatment blocked the rise in thromboxane in lung lymph and arterial plasma and substantially, although not entirely, blocked the rise in pulmonary arterial pressure." | ( Intravenous injection of propylene glycol causes pulmonary hypertension in sheep. Hales, CA; Quinn, DA; Robinson, D, 1990) | 1 |
"When indomethacin treatment blocked KC PGE2 production, IL-6 levels significantly increased." | ( Interleukin-6 production by endotoxin-stimulated Kupffer cells is regulated by prostaglandin E2. Callery, MP; Flye, MW; Kamei, T; Mangino, MJ, 1990) | 0.73 |
"Indomethacin pretreatment significantly attenuated the adaptive protective response, resulting in greater loss of H+ (-29 +/- 4 vs -18 +/- 3) and DNA efflux (190 +/- 35 vs 110 +/- 18, both p less than 0.05) after exposure to 5 mmol/L ATC." | ( Adaptive cytoprotection of gastric surface epithelial cells against injury by physiologic concentrations of bile acid. Deb, B; Dempsey, DT; Mercer, DW; Ritchie, WP; Sauter, A, 1990) | 1 |
"(3) Indomethacin treatment resulted in changes in mean arterial pressure (increase) and creatinine cl." | ( Effects of experimental potassium depletion on renal function and urinary prostanoid excretion in normal women during hypotonic polyuria. Agnoli, GC; Borgatti, R; Cacciari, M; Garutti, C; Ikonomu, E; Lenzi, P; Marinelli, M, 1990) | 0.76 |
"In indomethacin pretreated dogs, intracoronary PGE2 (30 ng kg-1 min-1) or PGI2 (60 ng kg-1 min-1) attenuated the positive inotropic effect produced by left cardiac sympathetic nerve stimulation or intracoronary injections of NE." | ( Inhibition by prostaglandins of adrenergic transmission in the left ventricular myocardium of anesthetized dogs. Lanier, SM; Malik, KU, ) | 0.65 |
"Indomethacin treatment inhibited the flare reactions induced by histamine and compound 48/80 to about 50%, whereas no influence was seen on the itch responses." | ( Separate effects of topical indomethacin on the itch response and on the flare reaction induced by histamine in human skin. Hägermark, O; Ståhle, M, 1985) | 1.28 |
"Indomethacin treatment (2 mg kg-1 day-1, ip, for 13 days) of rats which received gentamicin or tobramycin (40 mg kg-1 day-1, ip, for 10 days) caused a further fall in glomerular filtration rate (GFR) and renal blood flow and an impressive increase in renal resistance." | ( Role of the prostaglandin and kallikrein-kinin systems in aminoglycoside-induced acute renal failure. Ajzen, H; Boim, MA; Higa, EM; Ramos, OL; Schor, N, 1985) | 0.99 |
"Indomethacin pretreatment experiments suggest that activation of the arachidonic pathway accounts for approx." | ( Thrombin-induced calcium movements in platelet activation. Haynes, DH; Jy, W, 1987) | 0.99 |
"Indomethacin treatment may augment lung inflammation and fibrosis by increasing BAL elastase activity and fibronectin concentration." | ( Effects of dexamethasone and indomethacin on elastase, alpha 1-proteinase inhibitor, and fibronectin in bronchoalveolar lavage fluid from neonates. Gerdes, JS; Harris, MC; Polin, RA, 1988) | 1.29 |
"In indomethacin-pretreated preparations, cremasteric arteriolar dilator responses to acetylcholine, bradykinin, or ATP, but not to adenosine, histamine, or prostaglandin E2, were inhibited by hydroquinone (50 microM)." | ( Endothelium-associated vasodilators in rat skeletal muscle microcirculation. Kaley, G; Messina, EJ; Rodenburg, JM; Wolin, MS, 1989) | 0.79 |
"Indomethacin pretreatment produced a marked increase in residual volume." | ( Further studies on mechanisms regulating the voiding cycle of the rat urinary bladder. Conte, B; Furio, M; Giuliani, S; Maggi, CA; Meli, A; Santicioli, P, 1989) | 1 |
"Indomethacin pretreatment significantly enhanced (P less than 0.03) the mucosa's response to PGE1 compared to PGE1 alone." | ( Cyclooxygenase inhibition with indomethacin increases human duodenal mucosal response to prostaglandin E1. Ballesteros, MA; Hogan, DL; Isenberg, JI; Koss, MA, 1989) | 1.28 |
"Indomethacin pretreatment did not significantly alter any of these findings." | ( Microscopic correlates of adaptive cytoprotection in an ethanol injury model. Miller, TA; Schmidt, KL; Smith, GS, 1989) | 1 |
"3. Indomethacin pre-treatment abolished the AVP-induced increases in renal PGE2 synthesis and also the dose-related differences in ANF immunoreactivity." | ( Vasopressin-induced natriuresis in the conscious rat: role of blood pressure, renal prostaglandin synthesis and the peptide ANF. Lote, CJ; Thewles, A; Wood, JA, 1989) | 0.79 |
"The indomethacin-treated co-cultures, which manifest a normal IL 2 production but lack the IL 2 receptors, manifest an impaired DNA synthesis and contain a decreased number of T cell blasts." | ( Different mechanisms account for the suppression of interleukin 2 production and the suppression of interleukin 2 receptor expression in Trypanosoma brucei-infected mice. Darji, A; De Baetselier, P; Hamers, R; Remels, L; Sileghem, M, 1989) | 0.76 |
"Indomethacin pretreatment suppressed the delayed antigen induced asthmatic response." | ( Lung function and plasma levels of thromboxane B2, 6-ketoprostaglandin F1 alpha and beta-thromboglobulin in antigen-induced asthma before and after indomethacin pretreatment. Joubert, JR; Macfarlane, CM; Malan, L; Mouton, W; Shephard, EG, 1985) | 1.19 |
"Indomethacin pretreatment did not affect the captopril-induced increase in bradykinin, but it did completely eliminate the increase in the prostaglandins." | ( Peripheral hemodynamic effects of captopril in patients with congestive heart failure. Kawamura, K; Kubo, S; Kubota, J; Nishimura, H; Ueyama, M, 1989) | 1 |
"Indomethacin treatment was initiated as a 100 mg rectal suppository and maintained thereafter by 50 mg orally every 6 hours." | ( Twin with hydramnios: treating premature labor at source. Ash, KM; Harman, CR; Lange, IR; Manning, FA; Menticoglou, S, 1989) | 1 |
"Indomethacin pretreatment decreased adenosine hyperresponsiveness and shifted the dose-response curves of adenosine challenge to the right with a geometric mean PD20 of 1.28 mg (95% confidence limits, 0.64 to 2.56)." | ( Effect of indomethacin on adenosine-induced bronchoconstriction. Crimi, N; Maccarrone, C; Mistretta, A; Oliveri, R; Palermo, B; Palermo, F; Polosa, R, 1989) | 1.4 |
"Indomethacin pretreatment did not cause changes in responsiveness or sensitivity of lung parenchymal strips from normal or sensitized guinea-pigs to the agonists tested." | ( Modification by indomethacin of airway contractile responses in normal and sensitized guinea-pigs. Cortijo, J; Esplugues, J; Morcillo, EJ; Ortiz, JL; Pascual, R; Perpiñá, M; Sanz, C; Sarría, B, 1989) | 1.34 |
"Indomethacin treatment (0.3-10.0 mg/rat, s.c.) partially inhibited this 7-fold increase in ovarian blood volume." | ( Increase in ovarian blood volume during ovulation in the gonadotropin-primed immature rat. Espey, LL; Okamura, H; Tanaka, N, 1989) | 1 |
"Indomethacin treatment abolished the reduction of infarct size seen with defibrotide alone." | ( Defibrotide reduces infarct size in a rabbit model of experimental myocardial ischaemia and reperfusion. Thiemermann, C; Thomas, GR; Vane, JR, 1989) | 1 |
"Indomethacin pretreatment attenuated the increase in glomerular filtration rate following the protein meal, 105 +/- 6 ml/min/1.73 m2 pre-meal level to 118 +/- 4 ml/min/1.73 m2 post-meal, P greater than 0.1." | ( Protein-induced glomerular hyperfiltration: role of hormonal factors. Heeger, P; Hoeldtke, R; Kapoor, S; Krishna, GG; Miller, E; Newell, G; Polansky, M; Smith, R, 1988) | 1 |
"Indomethacin treatment inhibited the stimulatory effect of dbcAMP; butyrate had no effect on PGF2 alpha secretion." | ( Secretion of progesterone and prostaglandins by cells of bovine corpora lutea from three stages of the luteal phase. Mitchell, MD; Rodgers, RJ; Simpson, ER, 1988) | 1 |
"Indomethacin treatment, resulting in 90% inhibition of prostaglandin E2 synthesis, did not affect glucose- or peptone-stimulated acid output or modify the inhibitory action of somatostatin." | ( Somatostatin inhibits gastric acid secretion after gastric mucosal prostaglandin synthesis inhibition by indomethacin in man. Elashoff, JD; Kauffman, GL; Kovacs, T; Maxwell, V; Mogard, MH; Van Deventer, G; Walsh, JH; Yamada, T, 1985) | 1.2 |
"Indomethacin pretreatment (20 mg/kg, p.o.) markedly reduced PGE2 levels in the same region of the stomachs, and worsened stress-induced lesion formation." | ( Sulphasalazine and experimental stress ulcers. Cho, CH; Dai, S; Ogle, CW, 1985) | 0.99 |
"Indomethacin (Id) treatment of rabbits at the time of implantation resulted in a significant reduction in the number of viable embryos as well as significant reduction in plasma progesterone concentrations. " | ( Treatment with prostaglandins reduces the antifertility effect of indomethacin in rabbits. el-Banna, AA, 1986) | 1.95 |
"Indomethacin pretreatment reduced gastrin secretion at luminal pH 7." | ( Effect of indomethacin on bombesin-like immunoreactivity, somatostatin and gastrin secretion from rat stomach. Bender, H; Pfeffer, A; Schusdziarra, V, 1987) | 1.4 |
"Indomethacin treatment partially reversed the reduction in the amplitude but not the frequency of antral contractions." | ( Effect of inhibition of prostaglandin synthesis on epinephrine-induced gastroduodenal electromechanical changes in humans. Abell, TL; Hanson, RB; Kim, CH; Malagelada, JR, 1989) | 1 |
"Indomethacin treatment induced a significant reduction in urinary prostaglandin E2 excretion (73%) (2p less than 0.01), urinary albumin excretion rate diminished from 207 (63-253) to 87 (49-147) mg/24 h (2p less than 0.01), fractional clearance of albumin declined (70%) (2p less than 0.01)." | ( Elevated urinary prostaglandin excretion and the effect of indomethacin on renal function in incipient diabetic nephropathy. Hommel, E; Mathiesen, ER; Olsen, UB; Parving, HH, 1988) | 1.24 |
"Indomethacin treatment of animals challenged with Salmonella resulted in less fluid accumulation, in addition to lower concentrations of intestinal cAMP and prostaglandins, compared to that of similarly changed loops in normal animals." | ( Enterotoxin-induced fluid accumulation during experimental salmonellosis and cholera: involvement of prostaglandin synthesis by intestinal cells. Duebbert, IE; Peterson, JW, 1985) | 0.99 |
"When indomethacin treatment was associated to oPRL administration it was able to counteract the increase in binding capacity caused by oPRL, even at doses ineffective in reducing the binding in non oPRL-treated mice." | ( Drug-induced membrane modifications differentially affect prolactin and insulin binding in the mouse liver. Di Carlo, R; Ghè, C; Muccioli, G, 1985) | 0.72 |
"Indomethacin treatment elevated levels of peptido-LTs, reduced PGE2 levels and inhibited writhing." | ( Intraperitoneal injection of zymosan in mice induces pain, inflammation and the synthesis of peptidoleukotrienes and prostaglandin E2. Beaver, TH; Borgeat, P; Doherty, NS; Poubelle, P; Schrader, NL; Westrich, GL, 1985) | 0.99 |
"Indomethacin treatment inhibited the decreases in blood flow whereas the transient increases in flow became more pronounced." | ( Mechanisms of vascular actions of PAF. Piper, PJ; Stanton, AW; Stewart, AG, 1987) | 0.99 |
"Indomethacin-pretreatment prevented the increase in release of the measured cyclo-oxygenase metabolites without significantly altering the generation of either LTB4 or LTC4." | ( Platelet-activating factor-induced vasoconstriction in rat isolated, perfused hearts: contribution of cyclo-oxygenase and lipoxygenase arachidonic acid metabolites. Piper, PJ; Stewart, AG, 1986) | 0.99 |
"Indomethacin treatment may affect both fetal and neonatal renal function." | ( Prostaglandins and the developing kidney. Gleason, CA, 1987) | 0.99 |
"Indomethacin treatment was associated with an increased release of newly synthesized macromolecules by cartilage into the media (p less than 0.01)." | ( Effects of anti-inflammatory drugs on cartilage recovery from catabolin-induced degradation. Gorski, JP; Strathy, GM, 1987) | 0.99 |
"Indomethacin treatment (5 mg/kg ia) of piglets following hemorrhage caused a significant decrease in blood flow to all brain regions within 20 min." | ( Adrenergic and prostanoid mechanisms in control of cerebral blood flow in hypotensive newborn pigs. Armstead, WM; Beasley, DG; Busija, DW; Leffler, CW; Mirro, R, 1988) | 1 |
"In indomethacin-pretreated rats, Rioprostil, a synthetic prostaglandin E1 analogue, reversed this effect of topical ethanol." | ( Laparotomy stimulates an endogenous gastric mucosal protective mechanism in the rat. A microcirculatory and morphologic study of ethanol injury. Guth, PH; Yonei, Y, 1988) | 0.79 |
"Indomethacin pretreatment attenuated the antigen-induced increase in Qbr, thus suggesting that vasodilator cyclooxygenase products contribute to the vascular response." | ( Modification of bronchial blood flow during allergic airway responses. Abraham, WM; Codias, E; Long, WM; Martinez, H; Sprung, CL; Wanner, A; Yerger, LD, 1988) | 1 |
"Indomethacin pretreatment and systemic capsaicin desensitization each increased the micturition threshold without affecting the amplitude of micturition contraction." | ( Prostanoids modulate reflex micturition by acting through capsaicin-sensitive afferents. Conte, B; Furio, M; Giuliani, S; Gragnani, L; Maggi, CA; Meli, A; Meli, P; Santicioli, P, 1988) | 1 |
"Indomethacin treatment inhibited PGE excretion by 73% during the test meal but did not modify the protein-induced hyperfiltration." | ( Urinary prostaglandin E and kallikrein activity in glomerular hyperfiltration induced by a meat meal in man. Coello, J; Colina-Chourio, J; García, R; Herrera, J; Parra, G; Rodríguez-Iturbe, B; Sinaiko, A, 1988) | 1 |
"Indomethacin treatment increased rather than diminished the PLA2 stimulation." | ( Stimulation of luteinizing hormone-releasing hormone release from perifused hypothalamic fragments by phospholipase A2. Malacara, JM; Nava, LE, 1987) | 0.99 |
"3 Indomethacin pretreatment prevented the transient decrease in pulmonary removal of [3H]-PGE1 in response to endotoxin, prevented the haemodynamic effects and inhibited prostaglandin synthesis." | ( Effect of nafazatrom and indomethacin on pulmonary removal of prostaglandin E1 after endotoxin in rabbits. Gillis, CN; Havill, AM; Moalli, R, 1987) | 1.13 |
"Indomethacin pretreatment in five additional addicts also caused normalization of the impaired insulin responses to the intravenous glucose challenge and restored to normal the reduced glucose disappearance rate." | ( Sodium salicylate restores the impaired insulin response to glucose and improves glucose tolerance in heroin addicts. Ceriello, A; Consoli, G; Giugliano, D; Paolisso, G; Quatraro, A; Simeone, V; Stante, A; Torella, R, ) | 0.85 |
"Indomethacin pretreatment had no beneficial effect, whereas 30% and 40% of the animals survived for 36 h after treatment with Flunarizine and dazoxiben, respectively." | ( Raised plasma thromboxane B2 levels in experimental acute necrotizing pancreatitis in rats. The effects of flunarizine, dazoxiben, and indomethacin. Kort, WJ; Ouwendijk, RJ; van Ooijen, B; Vincent, JE; Westbroek, DL; Wilson, JH; Zijlstra, FJ, 1988) | 1.2 |
"Two indomethacin-treated infants and three infants given placebo had significant urinary output difficulties, requiring that the study medication be withheld." | ( Randomized low-dose indomethacin trial for prevention of intraventricular hemorrhage in very low birth weight neonates. Duncan, CC; Ehrenkranz, RA; Gettner, P; Kleinman, CS; Ment, LR; Scott, DT; Sherwonit, E; Taylor, KJ; Williams, J, 1988) | 1.08 |
"Indomethacin treatment significantly decreased (p less than 0.001) lysosomal enzyme activities in purified lysosomes, while an increase in the activities was observed in intestinal homogenates." | ( Towards the mechanism of protection against indomethacin induced gastro-intestinal ulceration by naloxone. Aulakh, BS; Chakravarti, RN; Dhaunsi, GS; Gupta, NM; Majumdar, S, 1988) | 1.26 |
"Indomethacin pretreatment exaggerated cefotaxime and desacetylcefotaxime accumulation in the obstructed kidney of the UUO model, indicating that this drug inhibits renal elimination of cefotaxime when urinary tract obstruction exists." | ( Serum and renal tissue concentrations of cefotaxime in urinary tract obstruction in rabbits. Tago, K; Ueno, A; Yabusaki, N, 1988) | 1 |
"Indomethacin pretreatment (10 mg/kg p.o.) did not interfere with this effect." | ( Protective action of SCH 12223 against experimentally induced gastric and intestinal lesions. Barnett, A; Brown, AD; Chiu, PJ; Gerhart, C; Siegel, M, 1988) | 1 |
"Indomethacin pretreatment resulted in attenuation, but not suppression of contractile activity." | ( Effects of prazosin and indomethacin on the alpha-adrenergic stimulation of rabbit myometrium. Barss, VA; Phillippe, M; Valles, L, 1988) | 1.3 |
"Indomethacin pretreatment (2 mg/kg) failed to significantly alter the vasodepressor and renal responses to furosemide in both hypertensive and normal rats." | ( Antihypertensive and bilateral renal responses to diuretics in 2-kidney, 1-clip Goldblatt hypertensive rats. Han, YF; Huang, WC; Tsai, LM; Wu, JN, 1987) | 0.99 |
"In indomethacin-pretreated animals, the coronary effects of PAF were significantly attenuated." | ( Biphasic effects of platelet-activating factor on coronary blood flow in anesthetized dog. Mehta, J; Nichols, WW; Wargovich, T, 1986) | 0.78 |
"Indomethacin treatment had no effect on serum gastrin levels but reduced mucosal prostaglandin E2." | ( Indomethacin and turnover of gastric mucosal cells in the rat. Baumgartner, A; Halter, F; Koelz, HR, 1986) | 2.44 |
"When indomethacin or ibuprofen-treated cells were compared to control cells in regards to motility, they were more active." | ( Modulation of tumor cell motility by prostaglandins and inhibitors of prostaglandin synthesis. Fligiel, SE; He, XM; Varani, J, 1986) | 0.73 |
"Indomethacin treatment of low-dose UVR-exposed animals (to inhibit prostaglandin synthesis in vivo) caused a retention in the capacity to respond normally to CH induction to haptens applied to the nonirradiated, but not to irradiated, dorsal skin surfaces." | ( Involvement of prostaglandins in the immune alterations caused by the exposure of mice to ultraviolet radiation. Burnham, DK; Chung, HT; Daynes, RA; Roberts, LK; Robertson, B, 1986) | 0.99 |
"Indomethacin pretreatment enhanced the capacity of PGD2 to potentiate cholinergic-induced contraction in normal but not in ovalbumin-sensitized guinea-pig." | ( Prostaglandin D2 (PGD2) potentiates cholinergic responsiveness in guinea-pig trachea. Berti, F; Brunelli, G; Daffonchio, L; Fabbri, L; Mapp, C; Omini, C, 1986) | 0.99 |
"Indomethacin treatment showed Prostaglandin E2 was not a direct in vitro factor in Ia antigen-mediated reduction of splenic M phi MLR stimulatory activity." | ( Variations in macrophage antigen phenotype: a correlation between Ia antigen reduction and immune dysfunction during tumor growth. Elgert, KD; Garner, RE; Malick, AP, 1986) | 0.99 |
"Indomethacin treatment induced a significant reduction in urinary prostaglandin E2 excretion (73%, p less than 0.01), glomerular filtration rate diminished from 120 +/- 18 to 106 +/- 17 ml/min/1.73 m2 (p less than 0.05), albuminuria declined from 148 to 69 micrograms/min (median and range) (p less than 0.05) and fractional clearance of albumin diminished 42% (p less than 0.05)." | ( Effects of indomethacin on kidney function in type 1 (insulin-dependent) diabetic patients with nephropathy. Arnold-Larsen, S; Edsberg, B; Hommel, E; Mathiesen, E; Olsen, UB; Parving, HH, 1987) | 1.38 |
"In indomethacin-treated hens increases in uterine EMG activity and plasma concentrations of PGF, PGE, and AVT were not observed at the expected time of oviposition, whereas a marked increase in plasma PGF and AVT occurred during spontaneous oviposition." | ( Interrelationship between arginine vasotocin, prostaglandin, and uterine contractility in the control of oviposition in the hen (Gallus domesticus). Koike, TI; Saito, N; Shimada, K, 1987) | 0.79 |
"Indomethacin treatment of piglets following hemorrhage inhibited the net cerebral production of 6-keto-PGF1 alpha and caused a decrease in blood flow (approximately equal to 40%) to all brain regions within 20 minutes." | ( Maintenance of cerebral circulation during hemorrhagic hypotension in newborn pigs: role of prostanoids. Beasley, DG; Busija, DW; Fletcher, AM; Leffler, CW, 1986) | 0.99 |
"Indomethacin treatment for 1 week monitored by drug level determinations was evaluated in 32 preterm infants with symptomatic patent ductus arteriosus (sPDA). " | ( Prolonged indomethacin treatment in preterm infants with symptomatic patent ductus arteriosus: efficacy, drug level monitoring, and patient selection. Isken, V; Kühl, PG; Leonhardt, A; Seyberth, HW, 1987) | 2.12 |
"Indomethacin co-treatment attenuated the reduction of ulcer formation of both pretreatments." | ( Evidence of "cross-stressor"-induced adaptive gastric cytoprotection. Glavin, GB; Hall, AM; Kiernan, KM; Lockhart, LK; Rockman, GE, 1987) | 0.99 |
"Indomethacin-treated suckling animals prevented from weaning did not develop intestinal lesions until they had access to solid food on day 23." | ( Indomethacin fails to induce ulceration in the gastrointestinal tract of newborn and suckling rats. Bedrick, AD; Holtzapple, PG, 1986) | 2.44 |
"Indomethacin treatment effectively controlled the increased prostaglandin excretion but corrected only partially the potassium and the calcium losses." | ( Familial Bartter's syndrome: report of a case with early manifestations and persistent hypercalciuria. Favre, L; Girardin, E; Paunier, L; Vallotton, MB, 1986) | 0.99 |
"Indomethacin pretreatment did not significantly augment the duodenal lesions induced by mepirizole or cysteamine, but did augment the gastric lesions induced by these compounds." | ( Augmentation of cysteamine and mepirizole-induced lesions in the rat duodenum and stomach by histamine or indomethacin. Kuwahara, Y; Okabe, S; Tanaka, H, 1986) | 1.21 |
"Indomethacin pretreatment also prevented radiation-induced emesis in two of seven dogs and in the remainder reduced the average number of episodes." | ( Radiation-induced emesis in the dog: effects of lesions and drugs. Briggs, DB; Carpenter, DO; Knox, AP; Strominger, NL, 1986) | 0.99 |
"Indomethacin treatment completely prevented the carcinogenic effect of methylazoxymethanol." | ( Antitumor effects of inhibitors of arachidonic acid cascade on experimentally induced intestinal tumors. Birkenfeld, S; Kohen, F; Krispin, M; Zakut, H; Zaltsman, YA; Zor, U, 1987) | 0.99 |
"Indomethacin pretreatment abolished the BK effect." | ( Bradykinin inhibits a slow spike afterhyperpolarization in visceral sensory neurons. Weinreich, D, 1986) | 0.99 |
"Indomethacin treatment lowered but did not eliminate mean levels of PGF2 alpha in the venous effluent from the largest preovulatory follicle at the first ovulation (36.0 +/- 9.9 ng/ml vs." | ( The effect of indomethacin on ovarian prostaglandin release in hens. Etches, RJ; Olson, DM; Shimada, K, 1986) | 1.35 |
"Indomethacin treatment by 6h30 after administration of an ovulatory LH dose significantly increased the occurrence of LUF at the expense of POCL." | ( Prostaglandins involvement in the formation of luteinized unruptured follicles in the cyclic female rat. Aron, C; Kauffmann, MT; Plas-Roser, S, 1985) | 0.99 |
"Indomethacin treatment in intact rats evoked increased blood flow as compared with the indomethacin control group." | ( Renal vasodilation after unilateral renal ablation. Hahne, B; Karlberg, L; Persson, AE, 1985) | 0.99 |
"Indomethacin treatment partially inhibited all of these responses." | ( Collagen stimulates [3H]inositol trisphosphate formation in indomethacin-treated human platelets. Lapetina, EG; McConnell, RT; Reep, B; Watson, SP, 1985) | 1.23 |
"When indomethacin treatment was discontinued in those patients receiving topical epinephrine, there was a further significant (P less than .05) reduction in intraocular pressure compared with the placebo-treated group." | ( Inhibition of the epinephrine-induced reduction of intraocular pressure by systemic indomethacin in humans. Camras, CB; Christensen, RE; Fazio, DT; Feldman, SG; Gardner, SK; Podos, SM, 1985) | 0.95 |
"Indomethacin treatment significantly suppressed the adrenal renin response to nephrectomy." | ( Effect of indomethacin on the adrenal renin response to nephrectomy in the rat. Atarashi, K; Baba, K; Franco-Saenz, R; Izumi, Y; Mulrow, PJ, 1985) | 1.39 |
"The indomethacin-treated group had significant decreases in serum prostaglandin values 30 hours after the initiation of therapy." | ( Randomized indomethacin trial for prevention of intraventricular hemorrhage in very low birth weight infants. Duncan, CC; Ehrenkranz, RA; Gettner, P; Kleinman, CS; Ment, LR; Pitt, BR; Scott, DT; Stewart, WB; Taylor, KJ, 1985) | 1.14 |
"Indomethacin pretreatment did not prevent the p.d." | ( Effect of castration on prostaglandin-mediated changes in membrane potential and prostaglandin synthesis in guinea-pig seminal vesicle tissue. Carbonaro, C; Gerritsen, ME; Levine, N; Tarlin, N, 1985) | 0.99 |
"Indomethacin pretreatment totally or partially inhibited the delayed asthmatic response in 10 of 11 subjects." | ( Non-steroid anti-inflammatory drugs in asthma: dangerous or useful therapy? Joubert, JR; Mouton, W; Shephard, E; Van Zyl, L; Viljoen, I, 1985) | 0.99 |
"Indomethacin treatment did not inhibit this effect." | ( Ozone-induced bronchial hyperreactivity in guinea pigs is abolished by BW 755C or FPL 55712 but not by indomethacin. Lee, HK; Murlas, C, 1985) | 1.21 |
"Indomethacin treatment inhibited renal cyclo-oxygenase with a 78% reduction in urinary prostaglandin E2 excretion and 89% suppression of plasma renin activity." | ( Differential effects of sulindac and indomethacin on blood pressure in treated essential hypertensive subjects. Banks, R; Beilin, LJ; Puddey, IB; Rouse, I; Vandongen, R, 1985) | 1.26 |
"Indomethacin pretreatment, which significantly decreased gastric mucosal prostaglandin E2 content, did not modify the inhibitory effects of 5-HT on histamine-induced acid secretion, nor did phentolamine or propranolol." | ( The inhibitory action of 5-hydroxytryptamine on gastric secretory function in rats. Cho, CH; Ogle, CW, 1986) | 0.99 |
"Indomethacin treatment did not prevent the formation of a peritoneal inflammatory exudate or peritoneal oil granulomatous tissue, although it had a mild inhibitory effect on the intensity of the cellular inflammation, particularly after extensive treatment of greater than 100 d." | ( Inhibition of plasmacytoma development in BALB/c mice by indomethacin. Anderson, AO; Nordan, RP; Potter, M; Wax, JS, 1985) | 1.24 |
"Indomethacin-treated rats with innervated kidneys responded to a similar increase in venous pressure with pronounced constriction; RVR increased by 50% (P less than 0.005)." | ( Rat renal hemodynamics during venous compression: roles of nerves and prostaglandins. Arendshorst, WJ; Corradi, A, 1985) | 0.99 |
"Indomethacin treatment was also shown to potentiate the action of estradiol." | ( Structural and functional studies of myometrial gap junctions. Cole, WC; Garfield, RE; MacKenzie, LW, 1985) | 0.99 |
"Indomethacin treatment reduced the potency of LTD4 and increased maximal contractile responses in most tissues." | ( Influences of gender and maturation on responses of guinea-pig airway tissues to LTD4. Douglas, JS; Duncan, PG, 1985) | 0.99 |
"Indomethacin pretreatment antagonized sodium benzoate-ulcer reducing properties indicating that this latter acts, at least in part, through stimulation of prostaglandins synthesis." | ( Influence of antioxidants and radical scavengers on ethanol-induced gastric ulcers in the rat. Evangelista, S; Meli, A, 1985) | 0.99 |
"Indomethacin pretreatment also greatly enhanced the capacity of naloxone to decrease temperature and suppress FR 30 behavior in morphine-treated rats." | ( Indomethacin facilitates acute tolerance to and dependence upon morphine as measured by changes in fixed-ratio behavior and rectal temperature in rats. Nielsen, JA; Sparber, SB, 1985) | 2.43 |
"Indomethacin pretreatment abolished the pressor response to vertebral infusion and reduced that to carotid infusion." | ( Role of prostaglandins and the areas postrema in the central pressor action of bradykinin. Scroop, GC; Wilkinson, DL, 1985) | 0.99 |
"Indomethacin treatment 3 to 4 times daily was continued postoperatively for up to 8 months." | ( [Treatment of cystoid macular edema after intracapsular cataract extraction and implantation of the Binkhorst 4-loop lens]. Gnad, HD; Paroussis, P; Skorpik, C, 1985) | 0.99 |
"Indomethacin pretreatment (5 mg/kg iv) prevented histamine tachyphylaxis, whereas atropine (4 mg iv) did not." | ( Tachyphylaxis to inhaled aerosolized histamine in anesthetized dogs. Martin, JG; Shore, S, 1985) | 0.99 |
"The indomethacin treatment did not change progesterone and oestradiol serum concentrations compared with animals injected with vehicle only." | ( Progesterone and oestradiol receptor concentration and translocation in uterine tissue of rabbits treated with indomethacin. Cao, ZD; Harper, MJ; Jones, MA, 1985) | 0.96 |
"Indomethacin treatment was also ineffective." | ( Pharmacological analysis of the vascular permeability response in the anaphylactic phase of allergic inflammation in rats. Hirasawa, N; Ohuchi, K; Tsurufuji, S; Watanabe, M, 1985) | 0.99 |
"Indomethacin-pretreated skin tolerated 4.3 times more UVB light and indomethacin-protected skin developed significantly less sunburn cells than untreated areas." | ( Photoprotective effect of topical indomethacin--an experimental study. Greiter, F; Gschnait, F; Schwarz, T, 1985) | 1.27 |
"Treatment with indomethacin and celecoxib reduced the Ca and P content, microhardness and mineral density in enamel." | ( Enamel biomineralization under the effects of indomethacin and celecoxib non-steroidal anti-inflammatory drugs. Almeida-Junior, LA; Arnez, MFM; de Carvalho, FK; de Queiroz, AM; Duarte, ACA; Faccioli, LH; Gonçalves, JL; Paula-Silva, FWG, 2022) | 1.32 |
"Pretreatment with indomethacin inhibited the diuresis induced by 4α-PDD." | ( Central Transient Receptor Potential Vanilloid 4 Contributes to Systemic Water Homeostasis through Urinary Excretion. Mori-Kawabe, M; Tsushima, H, 2019) | 0.84 |
"Treatment with Indomethacin had no pronounced effect on the immune system or bacterial burden." | ( A novel model to study neonatal Escherichia coli sepsis and the effect of treatment on the human immune system using humanized mice. Entleutner, K; Ernst, W; Fill Malfertheiner, S; Schlieckau, F; Schulz, D; Seelbach-Goebel, B, 2018) | 0.82 |
"Co-treatment of indomethacin inhibited AB1010-induced COX-2 expression leading to an additive effect in inhibition of cell viability and PGE" | ( Cyclooxygenase inhibitors potentiate receptor tyrosine kinase therapies in bladder cancer cells in vitro. Bourn, J; Cekanova, M, 2018) | 0.81 |
"Pretreatment with indomethacin or L-NAME did not affect NVKE-induced vasorelaxation." | ( Effects of Phikud Navakot extract on vascular reactivity in the isolated rat aorta. Nusuetrong, P; Sotanaphun, U; Tep-Areenan, P, 2012) | 0.7 |
"Pretreatment with indomethacin attenuated NGF-facilitated weight-bearing asymmetry and reversed OA-induced ipsilateral TrkA mRNA up-regulation." | ( Augmented pain behavioural responses to intra-articular injection of nerve growth factor in two animal models of osteoarthritis. Ashraf, S; Bennett, AJ; Burston, J; Chapman, V; Mapp, PI; Walsh, DA, 2014) | 0.73 |
"Treatment with indomethacin can potently suppress proliferation and induce apoptosis in the retinoblastoma Y79 cell line. " | ( Antiproliferative and apoptotic effects of indomethacin on human retinoblastoma cell line Y79 and the involvement of β-catenin, nuclear factor-κB and Akt signaling pathways. Chen, H; Li, W; Ren, Y; Wu, Y; Yang, S; Zhang, Y; Zheng, Q; Zhu, Y, 2014) | 1.02 |
"treatment with indomethacin plus glibenclamide." | ( The role of endothelium-derived hyperpolarizing factor and cyclooxygenase pathways in the inhibitory serotonergic response to the pressor effect elicited by sympathetic stimulation in chronic sarpogrelate treated rats. García, M; García-Pedraza, JÁ; Martín, ML; Morán, A; San Román, L, 2014) | 0.74 |
"Treatment with indomethacin significantly decreased COX-1 and COX-2 transcript expression." | ( Impact of indomethacin on neuroinflammation and hippocampal neurogenesis in aged mice. Boehme, M; Frahm, C; Guenther, M; Jaenisch, N; Liebmann, M; Stahr, A; Witte, OW, 2014) | 1.14 |
"Treatment with indomethacin caused macroscopic intestinal injury in mice; however, many dying cells were observed even in areas that macroscopically appeared to have no injury after treatment with indomethacin." | ( Indomethacin-induced generation of reactive oxygen species leads to epithelial cell injury before the formation of intestinal lesions in mice. Matsui, H; Sadakata, H; Tamura, M; Tomita, T, 2014) | 2.18 |
"Pretreatment with indomethacin and N-(G)-nitro-L-arginine methyl ester did not prevent gentamicin-induced DA relaxation." | ( Aminoglycoside-mediated relaxation of the ductus arteriosus in sepsis-associated PDA. Brown, N; Clark, RH; Cotton, RB; Ehinger, NJ; Goettel, JA; Paria, BC; Poole, SD; Reese, J; Rojas, MA; Shelton, EL; Slaughter, JC; Vucovich, MM; Wynn, JL, 2014) | 0.73 |
"Treatment with indomethacin, inhibited the rise in FDG-uptake observed with either LPS or PDT." | ( Deciphering PDT-induced inflammatory responses using real-time FDG-PET in a mouse tumour model. Cauchon, N; Hasséssian, HM; Lecomte, R; Turcotte, E; van Lier, JE, 2014) | 0.74 |
"Pretreatment with indomethacin, nimesulide, or dexamethasone blocked zymosan-induced behavioral changes in both the FST and OFT at 2 h post administration." | ( Prostaglandins mediate zymosan-induced sickness behavior in mice. Giusti-Paiva, A; Lima, JBM; Veloso, CC; Vilela, FC, 2017) | 0.78 |
"Pretreatment with indomethacin, which is an inhibitor of cyclooxygenase (COX), a prostaglandin synthase, had no effect on LPS-induced inhibition of crop emptying." | ( Lipopolysaccharide reduces food passage rate from the crop by a prostaglandin-independent mechanism in chickens. Cline, MA; Khan, MS; Makino, R; Ogino, M; Tachibana, T, 2017) | 0.78 |
"Treatment with indomethacin reduced IP response in the hyper-reactive model, and did not produce any change in diabetic model with hyper-reactive airways, indicating further disruption of the COX pathway." | ( Deterioration of epithelium mediated mechanisms in diabetic-antigen sensitized airways of guinea pigs. Bano, S; Kambadur, M; Mohammad, F; Swati, O, 2016) | 0.77 |
"Pretreatment with indomethacin (50 mg/kg, i.p., 1-3.5 h), a cyclooxygenase (COX)-inhibitor with a preferential selectivity for COX-1, which produced a significant elevation in brain KYNA levels, reversed the excitatory action of clozapine into an inhibitory response." | ( Clozapine interacts with the glycine site of the NMDA receptor: electrophysiological studies of dopamine neurons in the rat ventral tegmental area. Engberg, G; Erhardt, S; Linderholm, KR; Nilsson-Todd, LK; Schwieler, L, 2008) | 0.67 |
"Pretreatment with indomethacin at both concentrations did not result in a significant reduction in the maximum contraction compared with the control." | ( In vitro effects of the cyclooxygenase inhibitor indomethacin and of the phospholipase-C inhibitor U-73122 on carbachol-induced contractions of porcine detrusor muscle. Badawi, JK; Bross, S; Seja, T, 2008) | 0.92 |
"Treatment with indomethacin significantly changed the phosphometabolite fingerprint in this endothelial model, by, respectively, increasing (81%) and decreasing (42%) glycerophosphocholine (GPC) and phosphomonoesters (PM)." | ( 31P magnetic resonance spectroscopy of endothelial cells grown in three-dimensional matrigel constructs as an enabling platform technology: II. The effect of anti-inflammatory drugs on phosphometabolite levels. Lazarovici, P; Lecht, S; Lelkes, PI; Ringel, I; Sterin, M, ) | 0.47 |
"Treatment with indomethacin (10 and 100mg/kg) restored the weight bearing (measured as the ratio of the pressure exerted by the paws) and the print area ratios of LPS-inoculated mice similar to that observed in control mice." | ( Assessment of weight bearing changes and pharmacological antinociception in mice with LPS-induced monoarthritis using the Catwalk gait analysis system. Masocha, W; Parvathy, SS; Pavarthy, SS, 2009) | 0.69 |
"Pretreatment with indomethacin significantly accentuated the reduction in cardiac output produced by IL2." | ( Alteration in hemodynamic effects of interleukin 2 after treatment with indomethacin in anesthetized rats. Ford, CA; Tabrizchi, R, ) | 0.69 |
"Treatment with indomethacin, a COX inhibitor, induced a reduction on PGEx, as well as in fungus viability." | ( Paracoccidioides brasiliensis uses endogenous and exogenous arachidonic acid for PGE x production. Acorci-Valério, MJ; Biondo, GA; Bordon-Graciani, AP; Dias-Melicio, LA; Soares, AM, 2010) | 0.7 |
"The treatment with Indomethacin in the antenatal period can prevent severe nephrocalcinosis." | ( Antenatal Bartter syndrome: analysis of two cases with placental findings. Aksoy, F; Cetin, A; Dane, B; Dane, C; Yayla, M, 2010) | 0.68 |
"Treatment with indomethacin or piroxicam alone induced ulcer indices of 26 +/- 2.3 or 14 +/- 1.8, respectively." | ( Influence of cyclodextrin complexation with NSAIDs on NSAID/cold stress-induced gastric ulceration in rats. Ahmed, MO; Alanazi, FK; Alsarra, IA; Alsheikh, AM; Eltahir, KE; Neau, SH, 2010) | 0.7 |
"Pretreatment with indomethacin (10mg/kg; i.p.) or nimesulide (5mg/kg) blocked behavioural changes induced by LPS in the FTS, TST, open field and light-dark box test." | ( Prostaglandins mediate depressive-like behaviour induced by endotoxin in mice. Andrade, CA; de Paiva, VN; Fernandes, MM; Giusti-Paiva, A; Lima, SN; Soncini, R, 2010) | 0.68 |
"Rats treated with indomethacin revealed mucosal hemorrhagic lesions, increased microvascular permeability and inhibited prostaglandin E₂ and mucus content." | ( Coenzyme Q10: a novel gastroprotective effect via modulation of vascular permeability, prostaglandin E₂, nitric oxide and redox status in indomethacin-induced gastric ulcer model. El-Abhar, HS, 2010) | 0.89 |
"Treatment with indomethacin (1 mg/kg) or minocycline (50 mg/kg) had no effects on the weight bearing and print area ratios deficits of monoarthritic mice." | ( Enhancement of antinociception by coadministration of minocycline and a non-steroidal anti-inflammatory drug indomethacin in naïve mice and murine models of LPS-induced thermal hyperalgesia and monoarthritis. Abu-Ghefreh, AA; Masocha, W, 2010) | 0.91 |
"Treatment with indomethacin led to ductal closure and concomitant restoration of diastolic flow and resolution of symptoms." | ( Doppler manifestations of ductal steal: role in decision making. Carse, E; Sehgal, A; Tran, H, 2011) | 0.71 |
"When treated with indomethacin (AP + C + I), all the alterations in the exudate, tissue and serum shifted towards normalcy, except LPO in exudate and nitrite in tissue, while, hesperidin (AP + C + H) or naringin (AP + C + N) treatment normalized all the alterations." | ( Evaluation of antioxidative and anti-inflammatory potential of hesperidin and naringin on the rat air pouch model of inflammation. Jain, M; Parmar, HS, 2011) | 0.69 |
"Treatment with indomethacin increased intracellular concentration of [³H] eugenol and [³H] isoeugenol in moDCs." | ( Active transport of contact allergens in human monocyte-derived dendritic cells is mediated by multidrug resistance related proteins. Baron, JM; Czaja, K; Heise, R; Marquardt, Y; Merk, HF; Ott, H; Skazik, C, 2011) | 0.71 |
"Pretreatment with indomethacin (20 mg kg(-1)) decreased the background activities of both CFRs (from 0.48 ± 0.12 to 0.25 ± 0.08 impulses/s, n = 7, P < 0.05) and HTARs (from 0.54 ± 0.14 to 0.23 ± 0.08 impulses/s, n = 10, P < 0.01)." | ( Arachidonic acid products in airway nociceptor activation during acute lung injury. Guardiola, J; Li, H; Lin, S; Moldoveanu, B; Xu, L; Yu, J, 2011) | 0.69 |
"Pretreatment with indomethacin, a nonselective cyclooxygenase inhibitor, completely blocked the early rise in plasma corticosterone, but not at 2 h, whereas pretreatment with IL-6 antibodies had no effect on the early rise in corticosterone but attenuated corticosterone at 2 h." | ( Time-dependent mediators of HPA axis activation following live Escherichia coli. Camp, RM; Johnson, JD; Porterfield, VM; Zimomra, ZR, 2011) | 0.69 |
"Treatment with indomethacin (10 mg/kg) improved or restored the gait parameters of CFA inoculated mice i.e." | ( Gait analysis of C57BL/6 mice with complete Freund's adjuvant-induced arthritis using the CatWalk system. Masocha, W; Parvathy, SS, 2013) | 0.73 |
"Pretreatment with indomethacin completely inhibited CO- and hemin-induced fever." | ( Carbon monoxide as a novel central pyrogenic mediator. Jang, CG; Kim, JH; Lee, SJ; Lee, SY; Sohn, UD; Yang, SI, 2002) | 0.64 |
"Mice treated with indomethacin are responsive to treatment with exogenous IL-12 through at least the first 2 weeks of infection and, unlike control mice treated with IL-12, develop an enhanced Th1-type response associated with increased enhanced resistance to infection." | ( Combined treatment with interleukin-12 and indomethacin promotes increased resistance in BALB/c mice with established Leishmania major infections. Farrell, JP; Li, J; Padigel, UM; Scott, P, 2002) | 0.9 |
"Rats treated with indomethacin were injected with different doses (50, 250, or 500 micro g/rat) of PGE(1), PGE(2), PGF(2alpha), or vehicle (saline) at 1900 h in proestrus." | ( Prostaglandin E(1) inhibits abnormal follicle rupture and restores ovulation in indomethacin-treated rats. Bellido, C; Gaytán, F; Morales, C; Sánchez-Criado, JE; Tarradas, E, 2002) | 0.87 |
"Pretreatment with indomethacin (2 mg/kg i.p.), a non-selective cyclooxygenase inhibitor, significantly diminished the ACTH and corticosterone responses to carbachol (0.2 mg/kg i.p.) in control rats and moderately decreased these responses in stressed rats." | ( Effect of constitutive- and inducible-cyclooxygenase in the carbachol-induced pituitary-adrenocortical response during social stress. Bugajski, AJ; Bugajski, J; Gadek-Michalska, A, 2002) | 0.64 |
"Pretreatment with indomethacin or NS 398 completely blocked this long-term effect of IL-1beta, revealing a PGE(2)-dependent pathway." | ( Interleukin-1beta induces phosphodiesterase 4B2 expression in human myometrial cells through a prostaglandin E2- and cyclic adenosine 3',5'-monophosphate-dependent pathway. Dallot, E; Ferré, F; Leroy, MJ; Méhats, C; Oger, S, 2002) | 0.64 |
"Pre-treatment with indomethacin reduced the fever and adrenocortical activation induced by gp120 administration, but not its behavioral effects." | ( Intracerebral HIV-1 glycoprotein 120 produces sickness behavior and pituitary-adrenal activation in rats: role of prostaglandins. Barak, O; Ben-Hur, T; Goshen, I; Taylor, AN; Weidenfeld, J; Yirmiya, R, 2002) | 0.63 |
"Pretreatment with indomethacin was not effective." | ( Gut barrier permeability, reticuloendothelial system function and protease inhibitor levels following intestinal ischaemia and reperfusion--effects of pretreatment with N-acetyl-L-cysteine and indomethacin. Andersson, R; Deng, X; Lasson, A; Olanders, K; Sun, Z, 2002) | 0.83 |
"Pretreatment with indomethacin abolished the endothelium-dependent attenuation of lemakalim-induced relaxation caused by etomidate." | ( Inhibitory effects of etomidate and ketamine on adenosine triphosphate-sensitive potassium channel relaxation in canine pulmonary artery. Murray, PA; Sohn, JT, 2003) | 0.64 |
"Pretreatment with indomethacin, a cyclooxygenase inhibitor, blocked LPS and IL-1 induced neuronal activation in the PVN, but did not reduce the induction of IkappaBalpha in PVN endothelium." | ( Endothelial activation is an intermediate step for peripheral lipopolysaccharide induced activation of paraventricular nucleus. He, L; Lai, W; Quan, N, 2003) | 0.64 |
"Pretreatment with indomethacin (10 mg/kg), an inhibitor of prostaglandin synthesis, also did not affect NMU-induced acid inhibition." | ( Neuromedin U acts in the central nervous system to inhibit gastric acid secretion via CRH system. Date, Y; Kangawa, K; Mondal, MS; Murakami, N; Nakazato, M; Shimbara, T; Toshinai, K, 2003) | 0.64 |
"pretreatment with indomethacin (200 micro g/5 micro l, i.c.v.), an inhibitor of cyclo-oxygenase, showing that they are mediated by prostaglandin(s)." | ( Role of prostaglandin, endothelin and sympathetic nervous system on the L-NAME-induced pressor responses in spontaneously hypertensive rats. Kadekaro, M; Salas, N; Summy-Long, JY; Terrell, ML, 2003) | 0.64 |
"Treatment with indomethacin increased sleep efficiency (p<0.001) and paradoxical sleep time (p<0.001)." | ( Sleep alterations in an experimental orofacial pain model in rats. Andersen, ML; Schütz, TC; Tufik, S, 2003) | 0.66 |
"Pre-treatment with indomethacin, but not with l-NAME, prevented the relaxation induced by alpha-CGRP in pulmonary arteries suggesting that prostaglandins but not nitric oxide (NO) are involved in the intracellular signal transduction pathway." | ( Effects of alpha calcitonin gene-related peptide in human bronchial smooth muscle and pulmonary artery. Amadesi, S; Dinh, QT; Fischer, A; Geppetti, P; Groneberg, DA; Harrison, S; McGregor, GP; Springer, J; Trevisani, M, 2004) | 0.64 |
"Pretreatment with indomethacin, a cyclooxygenase inhibitor, further reduced the first increase and abolished the second increase." | ( Cholecystokinin and prostaglandins inhibit responses of vagal afferent activity to systemic administration of nicotine in anesthetized rats. Kurosawa, M; Taniguchi, T; Yoneda, M, 2004) | 0.65 |
"pretreatment with indomethacin. At the end of experiments, the rats were anesthetized, the stomach was exposed to measure gastric blood flow (GBF), to determine the area of gastric lesions and to take biopsy samples from the oxyntic mucosa for determination of transcripts of ghrelin, tumor necrosis alpha (TNF-alpha) and transforming growth factor alpha (TGFalpha) using RT-PCR and to assess the generation of PGE(2) by RIA." | ( Ghrelin-a new gastroprotective factor in gastric mucosa. Brzozowski, T; Drozdowicz, D; Hahn, EG; Harsch, I; Konturek, PC; Konturek, SJ; Kwiecien, S; Nikiforuk, A; Pajdo, R, 2004) | 0.65 |
"Pretreatment with indomethacin (0.5 microM) reduced the response to the two PGE2 concentrations by about 70 and 25%, respectively." | ( Effects of norepinephrine or prostaglandin E2 on extracellular acidification rate of MCG 101, or K1735-M2 tumor cells. Andersson, M; Delbro, DS; Haraldsson, B; Nylund, G, 2004) | 0.65 |
"Pretreatment with indomethacin or N(G) nitro-l-arginine methylester (l-NAME) reduced the mesenteric vasodilator response to hUII, and abolished the late tachycardia and hindquarters vasodilatation." | ( Bolus injection of human UII in conscious rats evokes a biphasic haemodynamic response. Bennett, T; Gardiner, SM; Kemp, PA; March, JE, 2004) | 0.65 |
"Pretreatment with indomethacin (10 microM) completely abolished the stimulatory effect of A23187 (10 microM) on 6-keto-prostaglandin F1alpha release." | ( The differential role of exogenous and endogenous prostacyclin in the control of renin release from dog renal cortical slices. Hayashi, M; Kurosawa, H; Satoh, H; Satoh, S; Yatsu, T, 2004) | 0.65 |
"Rats treated with indomethacin had significant higher plasma levels of TNF-alpha (indomethacin vs N/S: 22+/-5 vs 10+/-1 pg/mL, P<0.05) and lower plasma levels of 6-keto-PGF1alpha (P<0.001), but not total bilirubin or creatinine (P>0.05), as compared with rats treated with N/S." | ( Prostacyclin inhibition by indomethacin aggravates hepatic damage and encephalopathy in rats with thioacetamide-induced fulminant hepatic failure. Chan, CY; Chang, FY; Chen, YC; Chu, CJ; Hsiao, CC; Huang, HC; Lee, FY; Lee, SD; Wang, SS; Wang, TF, 2005) | 0.95 |
"Pretreatment with indomethacin (4 mg/kg, i.p.) inhibited the phenomenon at all the times analyzed." | ( A novel hot-plate test sensitive to hyperalgesic stimuli and non-opioid analgesics. Cordeiro, RS; Lavich, TR; Martins, MA; Silva, PM, 2005) | 0.65 |
"Pretreatment with indomethacin (2 mg/kg/day) or celecoxib (5 mg/kg/day) post surgery and up to 3 days thereafter did not prevent memory deficits caused by silicone collar implants." | ( Inhibitory avoidance memory retention in the elevated T-maze is impaired after perivascular manipulation of the common carotid arteries. Almeida, Sde S; de Aguiar Corrêa, FM; de Bortoli, VC; de Oliveira, AM; Zangrossi Júnior, H, 2005) | 0.65 |
"Pretreatment with indomethacin significantly attenuated the venom-induced responses and also blocked the paw oedema." | ( Intra-arterial injection of Mesobuthus tamulus venom elicits cardiorespiratory reflexes involving perivascular afferents. Deshpande, SB; Singh, SK, 2005) | 0.65 |
"Pretreatment with indomethacin (10 mg/kg sc) prevented the IL-1beta-induced increases in body temperature and the apparent increase in hypothalamic NE release, but only attenuated the IL-1beta-induced shivering and the increase in plasma ACTH." | ( Relationships among the behavioral, noradrenergic, and pituitary-adrenal responses to interleukin-1 and the effects of indomethacin. Dunn, AJ; Wieczorek, M, 2006) | 0.87 |
"Treatment with indomethacin, which prevents the formation of PGF2alpha, caused the PBR density in the uterus of pseudopregnant rats at day 53 PP to be twice as high as in pseudopregnant control rats." | ( The effects of prostaglandin F2alpha treatment on peripheral-type benzodiazepine receptors in the ovary and uterus during pseudopregnancy of rats. Bar-Ami, S; Bendel, N; Gavish, M; Leschiner, S; Levin, E; Veenman, L, 2006) | 0.67 |
"Treatment with indomethacine improves ductal closure and is associated with few reversible adverse effects." | ( Management of patent ductus arteriosus in preterm infants. Arsan, S; Atalay, S; Atasay, B; Ekici, F; Eyileten, Z; Günlemez, A; Naçar, N; Tutar, E; Uysalel, A, 2006) | 0.67 |
"Pretreatment with indomethacin or ketoprofen (non-selective COX inhibitors; 0.3 mg kg(-1) i.v.) inhibited acetic acid-evoked irritation (characterised by a decrease in bladder capacity in vehicle pretreated animals)." | ( Dual, but not selective, COX-1 and COX-2 inhibitors, attenuate acetic acid-evoked bladder irritation in the anaesthetised female cat. Edwards, RM; Evans, C; Hieble, JP; McCafferty, GP; Wibberley, A, 2006) | 0.66 |
"Pretreatment with indomethacin completely reversed both of the therapeutic effects of dalteparin, whereas pretreatment with NS-398, a selective inhibitor of cyclooxygenase-2, did not." | ( Dalteparin, a low molecular weight heparin, attenuates inflammatory responses and reduces ischemia-reperfusion-induced liver injury in rats. Harada, N; Okajima, K; Uchiba, M, 2006) | 0.66 |
"Treatment with indomethacin (2 mg/kg), rofecoxib, (10 mg/kg), or dexamethasone (2 mg/kg) significantly reduced the BaV- and BjV-induced oedema formation." | ( Role of cyclooxygenases in oedema-forming activity of bothropic venoms. Gutierrez, JM; Olivo, Rdo A; Teixeira, CF; Wallace, JL; Zamuner, SR, 2007) | 0.68 |
"Pretreatment with indomethacin or L-Nomega-nitroarginine methylester (L-NAME) abolished U-II-induced ear flushing." | ( Urotensin-II induces ear flushing in rats. Andrade-Gordon, P; Colburn, R; Damiano, BP; Haertlein, B; Minor, LK; Parry, TJ; Qi, JS; Schulingkamp, R; Stone, D, 2007) | 0.66 |
"Pretreatment with indomethacin reduced the protective effects of piperine, and L-NAME reduced the effects of capsaicin and omeprazole." | ( Effects of allyl isothiocyanate from horseradish on several experimental gastric lesions in rats. Matsuda, H; Nagatomo, A; Ochi, M; Yoshikawa, M, 2007) | 0.66 |
"Pretreatment with indomethacin, an inhibitor of cyclooxygenase, or addition of nordihydroguaiaretic acid, an inhibitor of lipoxygenase, had no effect on AA-induced changes in I(Ca,L)." | ( Inhibition of L-type Ca2+ channel current and negative inotropy induced by arachidonic acid in adult rat ventricular myocytes. Liu, SJ, 2007) | 0.66 |
"Treatment with indomethacin alone induced growth arrest, but not the death of AML-2/IDAC cells." | ( Alleviation of the drug-resistant phenotype in idarubicin and cytosine arabinoside double-resistant acute myeloid leukemia cells by indomethacin. Hwang, SY; Kim, HJ; Kim, SH; Kim, TS; Song, JH, 2008) | 0.89 |
"Treatment with indomethacin inhibited prostaglandin synthesis by the cultured cells and also elevated levels of P4 from Days 3 to 11 of culture." | ( Effects of prostaglandin F2 alpha on agonist-induced progesterone production in cultured bovine luteal cells. Condon, WA; Pate, JL, 1984) | 0.61 |
"Pretreatment with indomethacin and clidanac reduced the effect of these beta-blockers on the mean arterial blood pressure and had no effect on the heart rate." | ( [Influence of indomethacin and clidanac on the blood pressure lowering effect of beta-blockers]. Fujimura, H; Imai, H; Niwa, M; Nozaki, M; Tsurumi, K, 1983) | 0.95 |
"Pretreatment with indomethacin (0.1 mg/kg) or acetylsalicylic acid (1 mg/kg) selectively eliminated the decreases in compliance observed after diazoxide." | ( The effects of diazoxide on total lung resistance in the anesthetized paralyzed guinea-pig. Biggs, DF; Peterson, MA, 1980) | 0.58 |
"Pretreatment with indomethacin did not significantly reduce the very marked increases in these parameters produced by the combined prostaglandin E1-bradykinin infusions." | ( Pharmacological modification of the edema produced by combined infusions of prostaglandin E1 and bradykinin in canine forelimbs. Adamski, SW; Grega, GJ; Prasad, CM; Svensjö, E, 1982) | 0.59 |
"Treatment with indomethacin was stopped in one case (erythema and conjunctivitis)." | ( Double-blind parallel study of piroxicam versus indomethacin in the treatment of low back pain. Osterman, K; Videman, T, 1984) | 0.86 |
"Pretreatment with indomethacin prevented the increase in PGE2 content and the stimulation of adenyl cyclase induced by bisacodyl." | ( Effects of bisacodyl on cAMP and prostaglandin E2 contents, (Na + K) ATPase, adenyl cyclase, and phosphodiesterase activities of rat intestine. Karmeli, F; Okon, E; Rachmilewitz, D, 1980) | 0.58 |
"Pretreatment with indomethacin abolished the preventive effects of theophylline on anaphylactic shock, and the effect of theophylline on the cyclic AMP content." | ( Preventive effects of theophylline on anaphylactic shock in rats. Okabe, E, 1980) | 0.58 |
"Pretreatment with indomethacin alone did not increase the survival rates in endotoxin-administered rats." | ( The effect of indomethacin and adrenergic receptor blocking agents on rats and canine responses to endotoxin. Fujita, T; Goto, F; Otani, E; Yamamuro, M, 1980) | 0.95 |
"Pretreatment with indomethacin (4 mg/kg b.w., s.c./day x 2) prevented the increase in PGE2 content, the stimulation of adenylate cyclase activity and the inhibition of jejunal Na-K-ATPase activity induced by pentagastrin." | ( PGE2 mediates the effect of pentagastrin on intestinal adenylate cyclase and Na-K-ATPase activities. Karmeli, F; Rachmilewitz, D; Sharon, P, 1981) | 0.59 |
"Pretreatment with indomethacin significantly (P less than 0.01) inhibited PG production, but did not alter adrenal steroidogenesis." | ( Role of prostaglandins in adrenal steroidogenesis. Swartz, SL; Williams, GH, 1983) | 0.59 |
"Treatment with indomethacin, another PES inhibitor, also did not reduce the pulmonary BP metabolite:DNA adduct levels." | ( Effect of aspirin and indomethacin on the formation of benzo(a)pyrene-induced pulmonary adenomas and DNA adducts in A/HeJ mice. Adriaenssens, PI; Anderson, MW; Boorman, GA; Eling, TE; Sivarajah, K, 1983) | 0.92 |
"Pretreatment with indomethacin blunted the rise in PAC from 159.0 +/- 21.5 to 63.3 +/- 10.2 pg/ml upon standing with CEI, without a concurrent change in circulating 6-keto prostaglandin F1 alpha (from 57.7 +/- 9.5 to 56.0 +/- 11.1 pg/ml) in 4 patients." | ( Indomethacin blunts the orthostatic increase in plasma aldosterone in glomerulonephritis. Abe, H; Fujiwara, Y; Orita, Y; Sasaki, E; Takamitsu, Y, 1984) | 2.03 |
"Pretreatment with indomethacin, a prostaglandin synthesis inhibitor, did not modify the antihypertensive action of captopril." | ( Circulatory effects of renin-angiotensin system antagonists during halothane anaesthesia in hypertensive rats. Kataja, J; Kaukinen, S; Ylitalo, P, 1983) | 0.59 |
"Treatment with indomethacin, 10 mg/day for 5 days, partially reversed the increase in the urinary excretion of norepinephrine metabolites." | ( Endogenously synthesized prostaglandins stimulate sympathetic nervous system activity. Güllner, HG, 1983) | 0.61 |
"Pretreatment with indomethacin (2 mg/kg BW) prevented not only the change in feedback sensitivity at nephrectomy but also the rise in GFR." | ( Indomethacin inhibits renal functional adaptation to nephron loss. Erik, A; Hahne, B; Persson, G; Selén, G, 1984) | 2.03 |
"Treatment with indomethacin also improved the pressor responsiveness to angiotensin II and norepinephrine, but this occurred in association with a decrease in PRA, PAC and urinary excretion of PGE2 and PGF2 alpha." | ( Hypokalemia and prostaglandin overproduction in Bartter's syndrome. Amagasaki, Y; Kato, E; Konishi, K; Nakata, I; Ozawa, Y; Saruta, T; Senba, S, 1984) | 0.61 |
"Pretreatment with indomethacin prevented only the temperature response to lipid A." | ( Effect of bacterial endotoxin on body temperature, plasma zinc and plasma concentrations of the acute-phase protein serum amyloid p component in mice. Baltz, M; Gordon, AH; Poole, S; Stenning, BE, 1984) | 0.59 |
"Pretreatment with indomethacin significantly decreased urine TxB2 and 6-keto-PGF1 alpha in both irradiated and nonirradiated animals." | ( Thromboxane and prostacyclin synthesis following whole body irradiation in rats. Kot, PA; Ramwell, PW; Rose, JC; Schneidkraut, MJ, 1984) | 0.59 |
"Pretreatment with indomethacin did not inhibit the ability of 111In-labeled eosinophils to accumulate at the site of lymphokine injection in vivo." | ( Arachidonic acid metabolism in the murine eosinophil. III. Effect of nonsteroid anti-inflammatory drugs on lymphokine-directed eosinophil migration in vivo. Clanton, JA; Colley, DG; Rand, TH, 1983) | 0.59 |
"Pretreatment with indomethacin (1 mg/kg ip) abolished the protective effects of CMR against ethanol injury." | ( Gastric mucosal protection with chronic mild restraint: role of endogenous prostaglandins. Cohen, MM; Wallace, JL, 1984) | 0.59 |
"Pretreatment with indomethacin (8.5 microM), a cyclo-oxygenase inhibitor, reduced the resting tone of tracheal spirals, but did not significantly affect the tone of lung strips." | ( Bronchodilator-mediated relaxation of normal and ovalbumin-sensitized guinea-pig airways: lack of correlation with lung adenylate cyclase activation. Burka, JF; Saad, MH, 1984) | 0.59 |
"Pretreatment with indomethacin (3 mg/kg) or ibuprofen (10 mg/kg) inhibited the potentiation of pentobarbital sleeping time produced by arachidonic acid." | ( Sedation produced by prostaglandins is not a nonspecific fatty acid effect. Holingsworth, EB; Patrick, GA, 1984) | 0.59 |
"Pretreatment with indomethacin, a cyclooxygenase inhibitor, was followed by a significant decrease in the PGE level and a significant increase in the vasoconstrictor response to exogenous NA." | ( Effect of endogenous prostaglandin E on the vasoconstrictor response to noradrenaline. Michibayashi, T, 1984) | 0.59 |
"pretreatment with indomethacin, an inhibitor of cyclooxygenase, abolished the hypertensive effect of AA, but did not influence the hypertensive and hypotensive effect caused by PGE2 and PGI2, respectively." | ( [Pressor and depressor responses to intracerebroventricularly administered prostaglandins and arachidonic acid in anaesthetized rabbits]. Ohkubo, K; Otorii, T; Suzuki, K, 1984) | 0.59 |
"Pretreatment with indomethacin did not affect DHE response in central haemodynamic variables or in tissue blood flow in dogs; nor did it affect the reduced venous vessel area, increased blood flow in dogs; nor did it affect the reduced venous vessel area, increased venous blood flow velocity (measured ultrasonically), or reduced resting calf volume blood flow (measured by plethysmography), caused by DHE in humans." | ( The role of the prostanoid system in mediating the haemodynamic effects of dihydroergotamine. Bergqvist, D; Lindblad, B, 1984) | 0.59 |
"Treatment with indomethacin blocks prostaglandin synthesis and induces thermosensitivity." | ( Natural thermal resistance of human tumor cells and the role of prostaglandin. Hildebrand-Zanki, S; Kern, DH; Morton, DL; Roe, DJ; Storm, FK; Worth, GD, 1983) | 0.61 |
"Treatment with indomethacin to block the secondary aggregation and secretion pathways of platelets reduced the aggregatory and secretory responses of control platelets induced by epinephrine, ADP, and low concentrations of thrombin to those characteristic of platelets suspended in "Na+-free" medium." | ( Removal of extraplatelet Na+ eliminates indomethacin-sensitive secretion from human platelets stimulated by epinephrine, ADP, and thrombin. Connolly, TM; Limbird, LE, 1983) | 0.87 |
"Pretreatment with indomethacin, 30 mg/kg given intraperitoneally, significantly potentiates the decrements in Cdyn and GL elicited by aerosol LTC4 at 1 microgram/ml." | ( Indomethacin potentiates the pulmonary response to aerosol leukotriene C4 in the guinea pig. Austen, KF; Corey, EJ; Drazen, JM; Leitch, AG, 1983) | 2.03 |
"Pretreatment with indomethacin (50 mg/kg), verapamil (40 mg/kg) or nifedipine (4 mg/kg) failed to inhibit the lethal effect of 20 micrograms/kg PAF-acether." | ( Glucocorticoid protection against PAF-acether toxicity in mice. Myers, A; Ramey, E; Ramwell, P, 1983) | 0.59 |
"Pretreatment with indomethacin produced a marked drop in the incidence of IVH as well as significant alterations in the blood pressure responses to the hemorrhagic hypotension/volume reexpansion insult." | ( Beagle puppy model of intraventricular hemorrhage. Effect of indomethacin on local cerebral glucose utilization. Duncan, CC; Lambrecht, R; Ment, LR; Scott, DT; Stewart, WB, 1984) | 0.83 |
"Pretreatment with indomethacin 3 mg/kg i.p., dazoxiben 3 mg i.p." | ( Endotoxin, prostaglandins and renal fibrin deposition in obstructive jaundice. Fletcher, MS; Kakkar, VV; Westwick, J, 1982) | 0.59 |
"Pretreatment with indomethacin (75 mg/day) reversed the hypotensive effect of the analogue of angiotensin II and abolished the increase of plasma renin concentration." | ( Effect of indomethacin upon the renin--angiotensin system in patients with Bartter's syndrome. Vierhapper, H; Waldhäusl, W, 1980) | 0.99 |
"Pretreatment with indomethacin was introduced in order to evaluate the possible influence of fatty acid cyclo-oxygenase products on the pattern of CBF changes." | ( Cerebrovascular response during and following severe insulin-induced hypoglycemia: CO2-sensitivity, autoregulation, and influence of prostaglandin synthesis inhibition. Agardh, CD; Ingvar, M; Nilsson, B; Siesjö, BK, 1981) | 0.59 |
"Pretreatment with indomethacin or with ibuprofen significantly decreased the inhibitory effect of high extracellular calcium, ionophore, or carbachol on AVP-stimulated water flow in the toad bladder." | ( Interaction of calcium and cyclooxygenase inhibitors on transport by the turtle and toad bladders. Arruda, JA, 1982) | 0.59 |
"Pretreatment with indomethacin abolished the protection afforded by chronic mild restraint, suggesting a mechanism involving endogenous prostaglandin synthesis." | ( Chronic mild restraint protects the rat gastric mucosa from injury by ethanol or cold restraint. Cohen, MM; Track, NS; Wallace, JL, 1983) | 0.59 |
"Treatment with indomethacin for 6 or 7 days did not affect dopamine excretion in either Bartter's syndrome or in a group of normal control subjects." | ( Free dopamine excretion in disorders with increased prostaglandin synthesis. Güllner, HG, 1982) | 0.6 |
"Pretreatment with indomethacin (150 mg for 3 days) failed to modify the effect of arginine on the release of these hormones." | ( Unchanged arginine-induced stimulation of insulin, glucagon, growth hormone, and prolactin after pretreatment with indomethacin in normal man. Bratusch-Marrain, P; Vierhapper, H; Waldhäusl, W, 1980) | 0.79 |
"Pretreatment with indomethacin (15 mg/kg/day) reduced the capacity of the aorta to release PGI2-like material." | ( Release of prostaglandin I2-like activity from the rat aorta: effect of captopril, furosemide, and sodium. Patrick, DR; Sullivan, JM, 1981) | 0.59 |
"Treatment with indomethacin during DOCA-induced hypokalemia, polyuria, hypernatremia, and increased urinary PG, restored urinary PGs to control values, and corrected the polyuria and hypernatremia without a change in serum potassium." | ( The role of prostaglandins in diabetes insipidus produced by desoxycorticosterone in the dog. Bartter, FC; Düsing, R; Gill, JR; Güllner, HG, 1982) | 0.6 |
"Pretreatment with indomethacin (150 mg/day) decreased baseline plasma renin activity and reversed the hypotensive effect of the analogue of angiotensin II." | ( Independent roles of prostaglandins and the renin-angiotensin system in abnormal vascular reactivity in Bartter's syndrome. Ando, K; Fujita, T; Fukui, T; Nomura, M; Sato, Y; Yamashita, K, 1982) | 0.59 |
"Pretreatment with indomethacin (10 mg/kg X 3 p.o.), a PG synthesis inhibitor, inhibited the increasing effects of this drug on urinary volume and Na+ and Cl-excretions by 80 or approximately 90%." | ( [Pharmacological studies on azosemide [5-(4'-chloro-5'-sulfamoyl-2'-thenylamino)-phenyltetrazole], a new diuretic (1) Effects on diuresis, plasma renin activity and urinary prostaglandin E excretion in normal rats (author's transl)]. Ito, M; Komura, T; Suzuki, Y, 1982) | 0.59 |
"Pretreatment with indomethacin did not interfere with the response of blood pressure and pulse rate to orthostasis (10 minutes), a cold pressor test (2 minutes), and the intravenous (i.v.) administration of norepinephrine (NE) (50, 100, and 200 ng kg-1 min-1)." | ( Release and vasoactive actions of catecholamines during inhibition of prostaglandin synthesis in normal man. Grubeck-Loebenstein, B; Korn, A; Vierhapper, H; Waldhäusl, W, ) | 0.45 |
"(4) Treatment with indomethacin was undertaken in all patients and studied in detail in one patient." | ( Bartter's syndrome--observations on the pathophysiology. Astley, P; Bobinski, H; Goldby, FS; Mallick, NP; Solomon, LR, 1982) | 0.58 |
"Pretreatment with indomethacin significantly reduced albumin extravasation after the administration of adrenalin but not after bicuculline, i.e." | ( Indomethacin and cerebrovascular permeability to albumin in acute hypertension and cerebral embolism in the rat. Johansson, BB, 1981) | 2.03 |
"Pretreatment with indomethacin improved cortical reperfusion but did not influence cortical pO2 and electrocorticographic activity." | ( Recovery from global cerebral ischemia in rabbits: influence of indomethacin. Boulu, RG; Gueniau, C; Plotkine, M; Sofeir, M, 1981) | 0.82 |
"Treatment with indomethacin alone or indomethacin plus dexamethasone prolonged gestation and prevented an increase in PGF2 alpha-M and a decrease in progesterone." | ( Effect of indomethacin dexamethasone-induced parturition in swine. First, NL; Nara, BS, 1981) | 1 |
"Treatment with indomethacin enhanced the plateau phase of the spontaneously occurring gastric action potential and the amplitude of the phasic contraction." | ( Does endogenous prostaglandin affect gastric antral motility? Sanders, KM; Szurszewski, JH, 1981) | 0.6 |
"Treatment with indomethacin is an interesting alternative to surgical ligation in prematures with patent ductus arteriosus." | ( [Patent ductus arteriosus in premature newborns. Treatment with indomethacin (author's transl)]. Bianchetti, G; Marchal, F; Monin, P; Morselli, PL; Vert, P, ) | 0.71 |
"Pretreatment with indomethacin, hydrocortisone, ibuprofen and sodium salicylate caused a dose-dependent inhibition of histamine-induced fragility." | ( Effects of inflammatory agents on endothelial lysosomal fragility and their inhibition by anti-inflammatory drugs. Yoffe, JR, 1981) | 0.59 |
"Pretreatment with indomethacin abolished piretanide-induced dissociation of sodium and calcium excretions." | ( Piretanide and urinary excretion of ions in rat. Effect of indomethacin. Gauthier, C; Nguyen-Simonnet, H; Pellet, M, 1981) | 0.83 |
"Treatment with indomethacin on days 4-6 after BHT had no beneficial effect." | ( The effect of indomethacin, prednisolone and cis-4-hydroxyproline on pulmonary fibrosis produced by butylated hydroxytoluene and oxygen. Kehrer, JP; Witschi, H, 1981) | 0.96 |
"Pretreatment with indomethacin did abolish the pulmonary effects of a further intravenous dose of the drug." | ( Indomethacin-induced pulmonary vasoconstriction in the conscious newborn lamb. Coceani, F; Lock, JE; Olley, PM; Soldin, S, 1980) | 2.03 |
"Pretreatment with indomethacin or paracetamol (100 micrograms/rat into the fourth cerebral ventricle) antagonised the central hypotensive effect of clonidine (0.125-16.0 micrograms/rat into the fourth cerebral ventricle)." | ( Influence of analgesic antipyretics on the central cardiovascular effects of clonidine in rats. Karppanen, H; Sirén, AL, 1980) | 0.58 |
"Treatment with indomethacin, a potent inhibitor of prostaglandin synthesis, did not lower serum calcium concentrations with two different doses (1·6 mg/kg/day orally and 5 mg/kg/day i.m.); effective inhibition of prostaglandin synthesis was demonstrated by the suppression of PGE-M excretion rates below basal levels." | ( Prostaglandin E production and hypercalcaemia in rats bearing the Walker carcinosarcoma. Bonsch, G; Erlenmaier, T; Imbeck, H; Minne, HW; Mrongovius, R; Müller, H; Seyberth, HW; Strein, K, 1980) | 0.6 |
"Treatment with indomethacin in dosages from 25 mg three times daily to 50 mg four times daily resulted in complete clearing of all disease manifestations in six of ten patients within 17 days and partial improvement in three." | ( The therapeutic response of urticarial vasculitis to indomethacin. Dicken, CH; Millns, JL; Randle, HW; Solley, GO, 1980) | 0.85 |
"Pretreatment with indomethacin did not, however, block the pulmonary vasodilator effects of intravenous prostacyclin (PGI(2))." | ( Influence of prostaglandin synthesis inhibitors on pulmonary vasodilatory effects of hydralazine in dogs with hypoxic pulmonary vasoconstriction. Lazar, JD; Rubin, LJ, 1981) | 0.59 |
"Pretreatment with indomethacin (5 mg/kg IM, n = 7) also attenuated the bradykinin-potentiating activity of Ang-(1-7) in enalaprilat-treated rats." | ( Angiotensin-(1-7) potentiates the hypotensive effect of bradykinin in conscious rats. Khosla, MC; Lima, CV; Paula, RD; Santos, RA, 1995) | 0.61 |
"Pretreatment with indomethacin at a dose (5 mg/kg i.p.) which completely blocked the decrease in food-motivated behavior induced by LPS abrogated this effect." | ( A behaviorally active dose of lipopolysaccharide increases sensory neuropeptides levels in mouse spinal cord. Bret-Dibat, JL; Couraud, JY; Creminon, C; Dantzer, R; Kent, S, 1994) | 0.61 |
"Treatment with indomethacin prevented and prostaglandin E2 (PGE2), dibutyryl-cAMP, or forskolin mimicked reduction of basal ICAM-1 expression by RA, indicating that this effect of RA is mediated by PGE2 synthesis and subsequent cAMP elevation." | ( Retinoic acid inhibits basal and interferon-gamma-induced expression of intercellular adhesion molecule 1 in monocytic cells. Calzada-Wack, JC; Goretzki, M; Johnson, JP; Pietsch, A; Weber, C; Ziegler-Heitbrock, HW, 1995) | 0.63 |
"The treatment with indomethacin but not capsaicin decreased the ecabet-induced increase in PGE2 formation." | ( Roles of prostaglandins, nitric oxide and the capsaicin-sensitive sensory nerves in gastroprotection produced by ecabet sodium. Kinoshita, M; Kume, E; Tamaki, H, 1995) | 0.61 |
"Treatment with indomethacin, however, counteracted the elevated pulmonary artery pressure occurring in the early phase after thrombin infusion, but not that in the late phase." | ( Effect of indomethacin on thrombin-induced pulmonary edema in the rat. Ahn, CM; Saldeen, T; Sandler, H; Wegener, T, 1995) | 1.03 |
"Pretreatment with indomethacin (cyclooxygenase inhibitor) abolished the IL-1-induced, but not the CRH-induced, increase in hypothalamic and splenic NE turnover." | ( Roles of prostaglandins D2 and E2 in interleukin-1-induced activation of norepinephrine turnover in the brain and peripheral organs of rats. Asano, A; Kitamura, H; Kobayashi, M; Saito, M; Terao, A, 1995) | 0.61 |
"Pretreatment with indomethacin had no significant effect on tumour take or initial growth." | ( Influence of zymosan (a non-specific macrophage stimulator) and of indomethacin on liver tumours--an experimental study in rats. Daneryd, PL; Hafström, LR; Holmberg, SB; Karlberg, IH; Karlsson, LM; Lindnér, GO; Naredi, PL; Pettersson, A; Stenram, U, 1995) | 0.85 |
"Pretreatment with indomethacin (IND) did not alter the protective effects of honey or the NP-SH levels, but significantly reduced the protective effects of sucralfate." | ( Natural honey exerts its protective effects against ethanol-induced gastric lesions in rats by preventing depletion of glandular nonprotein sulfhydryls. Mobarok Ali, AT, ) | 0.45 |
"Pretreatment with indomethacin (5 mg.kg-1.day-1 for 3 days) did not blunt the diuresis that occurred with an exchange of 2 ml.100 gm-1 XLHb." | ( Renal and systemic-hemodynamic response to isovolemic exchange transfusion with hemoglobin cross-linked with bis (3,5-dibromosalicyl) fumarate or albumin. Bucci, E; Fronticelli, C; Lu, YS; Matheson-Urbaitis, B, 1995) | 0.61 |
"Pretreatment with indomethacin (30 microM) inhibited the [Ca2+]i increment by BK (10 microM), but not by the subsequent addition of PGE2 (0.5 micrograms/ml)." | ( Effect of bradykinin on intracellular signalling systems in a rat clonal dental pulp-cell line. Kawase, T; Orikasa, M; Suzuki, A, 1993) | 0.61 |
"Pretreatment with indomethacin resulted in the attenuation of the acute increase in cardiac output and decrease in systemic vascular resistance that occurred with captopril." | ( Peripheral haemodynamic effects of inhibition of prostaglandin synthesis in congestive heart failure and interactions with captopril. Davies, MK; Doran, J; Lote, CJ; Townend, JN, 1995) | 0.61 |
"Pretreatment with indomethacin had no influence on sensory irritation of any of the solvents." | ( Sensory irritation effects of n-propanol and ethylbenzene after pretreatment with capsaicin or indomethacin. Hansen, LF; Nielsen, GD, ) | 0.67 |
"Pretreatment with indomethacin (10 mg/kg ip) partially reversed the inhibitory effects of IL-1 beta on gastrin-stimulated fundic HDC activity and acid secretion." | ( Interleukin-1 beta inhibits gastric histamine secretion and synthesis in the rat. Fukui, H; Imamura, I; Kanayama, S; Kawabata, S; Kondo, S; Matsuzawa, Y; Miyazaki, Y; Shinomura, Y, 1994) | 0.61 |
"Pretreatment with indomethacin did not significantly alter the effects of guanylin and STa." | ( Segmental differences in the effects of guanylin and Escherichia coli heat-stable enterotoxin on Cl- secretion in human gut. Adermann, K; Forssmann, WG; Jähne, J; Kuhn, M; Rechkemmer, G, 1994) | 0.61 |
"Pretreatment with indomethacin significantly decreased the proportion of fetal death from 83% to < 25% in mice injected with 10 micrograms of LPS." | ( Bacterial lipopolysaccharide-mediated fetal death. Production of a newly recognized form of inducible cyclooxygenase (COX-2) in murine decidua in response to lipopolysaccharide. Branch, DW; Dudley, DJ; Edwin, SS; Mitchell, MD; Silver, RM; Simmons, DL; Trautman, MS, 1995) | 0.61 |
"Pretreatment with indomethacin, 10 mg/kg s.c." | ( Prevention by rutin of gastric lesions induced by ethanol in rats: role of endogenous prostaglandins. Marhuenda, E; Martín, MJ; Pérez Guerrero, C, 1994) | 0.61 |
"Treatment with indomethacin, a cyclooxygenase inhibitor, dilated the vessel to 115.2 +/- 7% (P < .05) but did not change the constricting effect of Nw-nitro-L-arginine." | ( Nitric oxide regulates cerebral arteriolar tone in rats. Dacey, RG; Dietrich, HH; Kimura, M, 1994) | 0.63 |
"Pretreatment with indomethacin, an inhibitor of prostaglandin synthesis, did not affect IL-1 beta production in the brain induced by 4 micrograms kg-1 LPS." | ( Interleukin-1 beta production in the rabbit brain during endotoxin-induced fever. Morimoto, A; Murakami, N; Nakamori, T; Watanabe, T; Yamaguchi, K, 1994) | 0.61 |
"Pretreatment with indomethacin (10 mg/kg, i.p.) 30 min before trauma significantly reduced the edema and microvascular permeability increase." | ( Prostaglandins modulate alterations of microvascular permeability, blood flow, edema and serotonin levels following spinal cord injury: an experimental study in the rat. Dey, PK; Nyberg, F; Olsson, Y; Sharma, HS, 1993) | 0.61 |
"Treatment with indomethacin alone or in combination with MK-886 resulted in the toxicity normally associated with NSAIDs, including gastrointestinal lesions." | ( Chronic leukotriene inhibition in the rat fails to modify the toxicological effects of a cyclooxygenase inhibitor. Anderson, CA; Ching, SV; Coleman, JB; Ford-Hutchinson, AW; Peter, CP; Tagari, P, ) | 0.47 |
"Pretreatment with indomethacin ameliorated the decrease in arterial oxygen tension from prebypass to postbypass values (477 +/- 50 mm Hg versus 339 +/- 57 mm Hg, respectively)." | ( Neutrophil-mediated acute lung injury after extracorporeal perfusion. Hurst, T; Johnson, D; Mayers, I; Murphy, F; Prasad, K; Saxena, A; Thomson, D; Wilson, T, 1994) | 0.61 |
"Pretreatment with indomethacin (IMC) did not abrogate significantly the protective effect of IL-1." | ( The effect of interleukin 1 alpha on acetaminophen-induced hepatotoxicity. Bilić, A; Bukovec, Z; Culo, F; Renić, M; Sabolović, D; Zupanović, Z, 1993) | 0.61 |
"Pretreatment with indomethacin suppressed the difference between diets." | ( Influence of dietary fat on duodenal resistance to acid. Guarner, F; Lugea, A; Malagelada, JR; Salas, A, 1993) | 0.61 |
"Pretreatment with indomethacin alone or in combination with furegrelate abolished the furosemide-induced CPAH increment." | ( Thromboxane synthase inhibition enhances furosemide-induced renal vasodilation. Badahman, AH; Kaushal, RD; Wilson, TW, 1993) | 0.61 |
"Pretreatment with indomethacin (5 mg/kg, i.v.) or with a thromboxane A2/prostaglandin endoperoxide receptor antagonist, ONO-3708 (0.5 and 1.0 mg/kg, i.v.) significantly attenuated the pressor responses." | ( Different modes of endothelin-1 action in pressor response in vivo and pulmonary parenchymal contraction in vitro in the guinea pig. Beppu, S; Matsuda, H; Miyatake, K; Ohmori, F, 1993) | 0.61 |
"Pretreatment with indomethacin (1 x 10(-6) M) as a cyclooxygenase inhibitor did not reduce the response to PDB, indicating that prostaglandin release is of minor importance in the PDB-induced increase in microvascular permeability." | ( Involvement of protein kinase C in the control of microvascular permeability to colloidal carbon. Northover, AM; Northover, BJ, 1993) | 0.61 |
"Pre-treatment with indomethacin or a combination of indomethacin and L-NAME caused vasoconstriction in many tissues and modified the responses to ET-1 in a variable way, suggesting that normally, ET-1 tends to release arachidonic acid metabolites and nitric oxide with great variations between different tissues." | ( Vascular effects of endothelin-1 in the cat; modification by indomethacin and L-NAME. Bill, A; Granstam, E; Wang, L, 1993) | 0.85 |
"Treatment with indomethacin during induced inflammation had no effect on the inflammatory reaction in terms of the microvascular hemodynamics measured in this study." | ( Effects of nonsteroidal anti-inflammatory drugs on microvascular dynamics. House, SD; Slater, C, 1993) | 0.63 |
"Pretreatment with indomethacin did not result in improved fetal survival." | ( A rabbit model for ascending infection in pregnancy: intervention with indomethacin and delayed ampicillin-sulbactam therapy. Gibbs, RS; Heddleston, L; McDuffie, RS, 1993) | 0.84 |
"Pretreatment with indomethacin (10 mg/kg body weight i.p." | ( Indomethacin, an inhibitor of prostaglandin synthesis attenuates alteration in spinal cord evoked potentials and edema formation after trauma to the spinal cord: an experimental study in the rat. Olsson, Y; Sharma, HS; Stålberg, E; Winkler, T, 1993) | 2.05 |
"Pretreatment with indomethacin did not attenuate the protective effect of unmodified or acidified hydrotalcit." | ( Role of eicosanoids, nitric oxide, and afferent neurons in antacid induced protection in the rat stomach. Korolkiewicz, R; Lambrecht, N; Liszkay, M; Peskar, BM; Trautmann, M, 1993) | 0.61 |
"Pretreatment with indomethacin (5 mg/kg i.p.), which suppressed the generation of PG by 85%, slightly enhanced the mucosal lesions induced by ethanol but failed to affect the fall in GBF induced by this irritant." | ( Role of nitric oxide and prostaglandins in gastroprotection induced by capsaicin and papaverine. Brzozowski, T; Drozdowicz, D; Konturek, SJ; Majka, J; Pytko-Polonczyk, J; Szlachcic, A, 1993) | 0.61 |
"Pretreatment with indomethacin also delayed ulcer healing and this was reversed by the coadministration of L-arginine." | ( Healing of chronic gastric ulcerations by L-arginine. Role of nitric oxide, prostaglandins, gastrin and polyamines. Brzozowski, T; Dembiński, A; Drozdowicz, D; Konturek, SJ; Stachura, J, 1995) | 0.61 |
"Co-treatment with indomethacin significantly reduced the proliferative response of KATO III cells to EGF." | ( Indomethacin interferes with epidermal growth factor binding and proliferative response of gastric KATO III cells. Arakawa, T; Fujiwara, Y; Halter, F; Schmassmann, A; Tarnawski, A, 1995) | 2.06 |
"Pretreatment with indomethacin attenuated metabolism of all products in the males but enhanced production of some compounds in vessels from the females." | ( Role of endothelium-derived metabolites of arachidonic acid in enhanced pulmonary artery contractions in female rabbits. Campbell, WB; Pfister, SL, 1996) | 0.62 |
"Pretreatment with indomethacin (5 mg/kg body wt IV) did not alter ramiprilat-induced increase in epicardial cross-sectional area, nor did it significantly influence coronary blood flow." | ( Coronary vasodilation induced by angiotensin-converting enzyme inhibition in vivo: differential contribution of nitric oxide and bradykinin in conductance and resistance arteries. Chatterjee, K; Chou, TM; Hutchison, SJ; Sudhir, K, 1996) | 0.62 |
"Pretreatment with indomethacin further increased the arterial levels of TNF alpha after portal infusion, but did not after them after i.p." | ( Release site of TNF alpha after intravenous and intraperitoneal injection of LPS from Escherichia coli in rats. Asari, Y; Katori, M; Majima, M; Ohwada, T; Sugimoto, K, 1996) | 0.62 |
"Pretreatment with indomethacin did not prevent the induction of CRF1 receptor transcription in the PVN of rats injected with a high dose of LPS." | ( Role of cyclo-oxygenase pathways in the stimulatory influence of immune challenge on the transcription of a specific CRF receptor subtype in the rat brain. Lacroix, S; Rivest, S, 1996) | 0.62 |
"Pretreatment with indomethacin did not alter the inhibitory effect of arachidonic acid on PAF production, indicating no involvement of cyclooxgenase products." | ( Inhibitory effect of arachidonic acid on platelet-activating factor production in rat neutrophils. Matsumoto, H; Naraba, H; Oh-ishi, S; Ueno, A, 1996) | 0.62 |
"Pretreatment with indomethacin only partially counteracted the protective activity of CuNSN against ethanol-induced damage." | ( A copper-complex reduced gastric damage caused by acetylsalicylic acid and ethanol. Franco, L; Velo, GP, 1996) | 0.62 |
"Pretreatment with indomethacin inhibited the second responses to PAF without affecting the first responses." | ( Involvement of nitric oxide and eicosanoids in platelet-activating factor-induced haemodynamic and haematological effects in dogs. Matsuzaki, T; Noguchi, K; Ojiri, Y; Sakanashi, M; Shiroma, N, 1996) | 0.62 |
"Pretreatment with indomethacin by either route strongly suppressed the corticosterone response to noradrenaline, but did not substantially affect the hormonal response to adrenaline." | ( Effect of indomethacin on the pituitary-adrenocortical response to adrenergic stimulation. Borycz, J; Bugajski, AJ; Bugajski, J; Gadek-Michalska, A; Głód, R, 1996) | 1.02 |
"pretreatment with indomethacin (50-500 micrograms/animal), while the same dose of indomethacin by the intravenous route was without effect." | ( Brain prostaglandins mediate the bombesin-induced increase in plasma levels of catecholamines. Okuma, Y; Osumi, Y; Yokotani, K, 1996) | 0.62 |
"Pretreatment with indomethacin enhanced PGF2 alpha-induced PtdEt accumulation." | ( Activation of phospholipase D by prostaglandin F2 alpha in rat luteal cells and effects of inhibitors of arachidonic acid metabolism. Endo, T; Goto, T; Ito, E; Kiya, T; Kudo, R; Sagae, S; Watanabe, H; Yamamoto, H, 1995) | 0.61 |
"Pretreatment with indomethacin (2.0 mg/kg body wt iv) completely abolished the effects of AP6A on urine flow and Na+ excretion." | ( Effects of diadenosine polyphosphates on renal function and blood pressure in anesthetized Wistar rats. Borucki, U; Enck, G; Hohage, H; Reinhardt, C; Schlatter, E; Schlüter, H; Zidek, W, 1996) | 0.62 |
"Rats treated with indomethacin and L-NAME before abdominal operation exhibited duodenal motility postoperatively and had higher DMAS than in controls." | ( Interaction between prostanoids, NO, and VIP in modulation of duodenal alkaline secretion and motility. Hällgren, A; Nylander, O; Sababi, M, 1996) | 0.62 |
"Pretreatment with indomethacin could significantly suppress the PGE2 and protein content of aqueous humor at both 1 and 24 hours after injection." | ( The effects of ETB receptor-selective agonist on IOP and blood-aqueous barrier in rabbit eyes: role of cyclooxygenase products. Haque, MS; Kitazawa, Y; Nakai, Y; Okada, K; Sugiyama, K; Taniguchi, T, 1995) | 0.61 |
"Treatment with indomethacin reduced only PGE2 and TXB2 in SF." | ( Low dose methotrexate decreases intraarticular prostaglandin and interleukin 1 levels in antigen induced arthritis in rabbits. Cossermelli, W; Laurindo, IM; Mello, SB; Novaes, GS, 1996) | 0.63 |
"Pretreatment with indomethacin (5 mg/kg i.v.) at 20 min and immediately before hypotension did not block this response (28 +/- 7% and 23 +/- 9% increase in diameter, respectively)." | ( The effects of treatment with indomethacin on the cerebral vasculature of newborn piglets before and during hemorrhagic hypotension. Hayden, JE; Leffler, CW, 1997) | 0.91 |
"Pretreatment with indomethacin (5 mg/kg) did not affect pial arteriolar dilation to hypoxia." | ( Cerebral arteriolar dilation to hypoxia: role of prostanoids. Leffler, CW; Parfenova, H, 1997) | 0.62 |
"Treatment with indomethacin enhanced this response equivalently in both sexes and thus did not affect the sex difference in the pressor action of vasopressin." | ( Sex differences in the cardiovascular and renal actions of vasopressin in conscious rats. Crofton, JT; Share, L; Wang, YX, 1997) | 0.64 |
"Treatment of indomethacin-treated piglets with iloprost (10(-12) M topically) restored dilation to 5,6-EET." | ( Newborn piglet cerebral microvascular responses to epoxyeicosatrienoic acids. Fedinec, AL; Leffler, CW, 1997) | 0.65 |
"Pretreatment with indomethacin (10 mg kg[-1], s.c.), a nonselective COX-1 and COX-2 inhibitor, attenuated the gastric hyperaemic response caused by TC without affecting p.d." | ( Cyclo-oxygenase isozymes in mucosal ulcergenic and functional responses following barrier disruption in rat stomachs. Hirata, T; Kato, S; Takeuchi, K; Ukawa, H; Yamakuni, H, 1997) | 0.62 |
"Pretreatment with indomethacin reduced RBF in the paws, but not in the periarticular tissue." | ( Changes in vascular porosity and joint blood flow during development of collagen induced arthritis in the rat. Modulation by indomethacin and L-NAME. Andersson, SE; Ekström, GM, 1997) | 0.83 |
"Pretreatment with indomethacin had no effect on tumor take or initial growth." | ( The influence of zymosan and indomethacin on liver and kidney tumor growth. An experimental study in rats. Blind, PJ; Hafström, LR; Holmberg, SB; Lindnér, PG; Naredi, PL; Ohman, MG, 1997) | 0.91 |
"Pretreatment with indomethacin did not affect the cardiovascular effect of GR138950 in conscious RALH rats." | ( Investigation of the inhibitory effect of N(G)-nitro-L-arginine methyl ester on the antihypertensive effect of the angiotensin AT1 receptor antagonist, GR138950. Anderson, IK; Drew, GM, 1997) | 0.62 |
"Pretreatment with indomethacin (cyclooxygenase inhibitor, 1 x 10[-5] M) had no effect on contractile responses to phenylephrine in rings from both groups of rats." | ( Enhanced endothelial nitric oxide activity contributes to the reduced responsiveness of vascular alpha1-adrenoceptors following aortic barodenervation. Abdel-Galil, AG; Daabees, TT; El-Gowelli, HM; El-Mas, MM, 1997) | 0.62 |
"Pretreatment with indomethacin only partially counteracted the protective activity of Cu(II)(L-Trp)(L-Phe)." | ( Prostaglandins and nitric oxide in copper-complex mediated protection against ethanol-induced gastric damage. Doria, D; Franco, L, 1997) | 0.62 |
"Pretreatment with indomethacin, isoproterenol, or nifedipine significantly reduced post-air-embolism lung water content to 85.8 +/- 0.5%, 84.1 +/- 0.4%, and 86.5 +/- 04%, respectively, and reduced the Kf increase to 17 +/- 8%, 1 +/- 9%, and 72 +/- 8%, respectively." | ( Pharmacologic modulation of pulmonary vascular permeability during air embolism. Huang, KL; Lin, YC, 1997) | 0.62 |
"Pretreatment with indomethacin did not influence the endotoxin-induced leukopenia observed at the 2nd h or the accompanying neutropenia and left shift." | ( Effects of indomethacin on lipopolysaccharide-induced plasma PGE2 concentrations and clinical pathological disorders in experimental endotoxemia. Andonova, M; Georgiev, P; Goundasheva, D; Ivanov, V, 1998) | 1.01 |
"Treatment with indomethacin did not diminish relaxin's effects on either cervical wet weight or cervical extensibility." | ( Evidence that relaxin's effects on growth and softening of the cervix are not mediated through prostaglandins in the rat. Cramer, JM; Jungheim, ES; Masferrer, JL; Sherwood, OD, 1998) | 0.64 |
"Pretreatment with indomethacin, which is a prostaglandin synthesis inhibitor and idoacetamide, which is a sulfhydryl blocker did not influence the inhibited ethanol lesion of WBS." | ( Prevention of ethanol-induced gastric lesions in rats by wu-bei-san. Lin, WC, 1998) | 0.62 |
"Pretreatment with indomethacin to suppress endogenous PG reversed completely the protective and hyperemic effects of SU-840 against ethanol and stress induced damage whereas L-NNA, a potent inhibitor of NO-synthase, failed to affect protection but completely abolished the hyperemia evoked by this agent." | ( SU-840, a novel synthetic flavonoid derivative of sophoradin, with potent gastroprotective and ulcer healing activity. Brzozowski, T; Drozdowicz, D; Konturek, SJ; Kwiecien, S; Muramatsu, M; Pajdo, R; Sliwowski, Z, 1998) | 0.62 |
"5. Treatment with indomethacin (5 mg kg-1, i.v.) in eight different cats did not alter the response of nine C fibre afferents to exogenous 5-HT (0.91 +/- 0." | ( Role of 5-HT3 receptors in activation of abdominal sympathetic C fibre afferents during ischaemia in cats. Fu, LW; Longhurst, JC, 1998) | 0.62 |
"Pretreatment with indomethacin diminished the inhibitory effect of IL-1 on CAT activity and collagen synthesis, suggesting partial mediation by prostaglandins." | ( Interleukin-1 represses COLIA1 promoter activity in calvarial bones of transgenic ColCAT mice in vitro and in vivo. Clark, S; Harrison, JR; Kelly, PL; Kleinert, LM; Kream, BE; Krebsbach, PH; Lichtler, AC; Rowe, DW; Woody, C, 1998) | 0.62 |
"Treatment with indomethacin did not affect NPY- and PYY3-36-induced alterations of systemic and renovascular hemodynamics but completely abolished NPY- and PYY3-36-induced diuresis and natriuresis." | ( Indomethacin inhibits the natriuretic effects of neuropeptide Y in anesthetized rats. Bischoff, A; Limmroth, V; Michel, MC, 1998) | 2.08 |
"Pretreatment with indomethacin (10 mg kg(-1) i.v.) had no significant effect on basal renal function, or on the Ang II-induced reduction in RVC (-25+/-7% vs -38+/-3% at Ang II 30 ng kg(-1) min(-1))." | ( Effects of prostaglandins and nitric oxide on the renal effects of angiotensin II in the anaesthetized rat. Clark, KL; Clayton, JS; Drew, GM; Johns, EJ, 1998) | 0.62 |
"Pretreatment with indomethacin partially blocked the enhancing effect of SP on protein leakage, while it did not block that of NKA." | ( Tachykinins as enhancers of prostaglandin E2-induced intraocular inflammation. Hamada, M; Shirasawa, E; Tsuji, F, 1998) | 0.62 |
"pretreatment with indomethacin at 5 mg/kg." | ( Protective role of melatonin and the pineal gland in modulating water immersion restraint stress ulcer in rats. Arakawa, Y; Asai, S; Ishikawa, K; Iwasaki, A; Kaneda, N; Kato, K; Komuro, S; Kuwayama, H; Matsuno, Y; Murai, I; Nakagawa, S, 1998) | 0.62 |
"Pretreatment with indomethacin completely blocked the effects induced by IL-1beta on hypothalamic HA." | ( Prostaglandin E2 mediates activation of hypothalamic histamine by interleukin-1beta in rats. Kang, M; Kurokawa, M; Ogawa, R; Sakata, T; Yoshimatsu, H, 1999) | 0.63 |
"Treatment with indomethacin but not with NG-nitro-L-arginine methyl ester completely inhibited the relaxation." | ( Endothelium-independent vascular relaxation mediating ETB receptor in rabbit mesenteric arteries. Hayasaki-Kajiwara, Y; Iwasaki, T; Nakajima, M; Naya, N; Ninomiya, M; Notoya, M; Shimamura, T, 1999) | 0.64 |
"Pretreatment with indomethacin, but not with NG-monomethyl-L-arginine, can attenuate the observed pressor response to BQ-788." | ( Elevation of blood pressure by genetic and pharmacological disruption of the ETB receptor in mice. Cao, WH; Dewit, D; Ju, KH; Kumada, M; Kuwaki, T; Ling, GY; Ohuchi, T; Onodera, M; Yanagisawa, M, 1999) | 0.63 |
"Treatment with indomethacin or NMLA stimulated lymphoproliferation on days 6 and 22 of infection; on day 14, when suppression of proliferation and NO production was maximal, combined inhibition of NO and PG production restored parasite Ag specific and Con A proliferative responses." | ( Prostaglandins mediate suppression of lymphocyte proliferation and cytokine synthesis in acute Trypanosoma cruzi infection. Abrahamsohn, IA; Pinge-Filho, P; Tadokoro, CE, 1999) | 0.64 |
"Pretreatment with indomethacin enhanced the relaxation response to acetylcholine in only SHRs at ages 16-20 and 55-60 weeks, thereby cancelling the difference in the relaxation response between WKY rats and SHRs." | ( Nitric oxide-dependent vasodilator mechanism is not impaired by hypertension but is diminished with aging in the rat aorta. Imaoka, Y; Kamada, T; Mio, Y; Okumura, K; Osanai, T; Satoh, K, 1999) | 0.63 |
"Pretreatment with indomethacin attenuated the increase in Kf after 65% triolein but not after 99% triolein." | ( Triolein-induced pulmonary embolization and increased microvascular permeability in isolated perfused rat lungs. Kuwagata, Y; Nakata, Y; Sugimoto, H; Tanaka, H; Yoshioka, T, 1999) | 0.63 |
"Pretreatment with indomethacin reduced the negative effect of TNF-alpha, while propranolol abolished the initial increase of contractility." | ( Role of nitric oxide and platelet-activating factor in cardiac alterations induced by tumor necrosis factor-alpha in the guinea-pig papillary muscle. Alloatti, G; Camussi, G; De Martino, A; Montrucchio, G; Penna, C, 1999) | 0.63 |
"Treatment with indomethacin before stress inhibited the increase in 6-keto-PGF1alpha levels and markedly reduced mucosal blood flow." | ( Gastric prostacyclin (PGI2) prevents stress-induced gastric mucosal injury in rats primarily by inhibiting leukocyte activation. Harada, N; Isobe, H; Liu, W; Murakami, K; Okajima, K, 1999) | 0.64 |
"5 Pretreatment with indomethacin completely abolished the induction of COX-2 in paw oedema but not in hyperalgesia." | ( Distribution and regulation of cyclooxygenase-2 in carrageenan-induced inflammation. Chan, CC; Cirino, M; Denis, D; Gordon, R; Metters, KM; Nantel, F; Northey, A, 1999) | 0.62 |
"Pretreatment with indomethacin or with N-ethylmaleimide did not affect the gastroprotective effect of TJ-43." | ( Gastroprotection by Liu-Jun-Zi-Tang (TJ-43): possible mediation of nitric oxide but not prostaglandins or sulfhydryls. Arakawa, T; Fujiwara, Y; Hayakawa, T; Higuchi, K; Kuroki, T; Tominaga, K; Watanabe, T, 1999) | 0.63 |
"Treatment with indomethacin was without significant effect on the early (1 h) response to IL-1beta; however, it led to complete and highly significant dose-dependent blockade of the late (48 h) response to IL-1beta as assessed in terms of PGS-2 transcripts, proteins and activity." | ( Non-steroidal anti-inflammatory drugs (NSAIDs) block the late, prostanoid-dependent/ceramide-independent component of ovarian IL-1 action: implications for the ovulatory process. Adashi, EY; Ando, M; Irahara, M; Kol, S; Sirois, J, 1999) | 0.64 |
"Treatment with indomethacin, a potent inhibitor of PG biosynthesis, inhibited UV-induced ear swelling, abrogated local immunosuppression, and decreased the amount of PGE2 in the ear skin of XPA-deficient mice." | ( Possible involvement of enhanced prostaglandin E2 production in the photosensitivity in xeroderma pigmentosum group A model mice. Eguchi, N; Horio, T; Inui, T; Kuwamoto, K; Miyauchi-Hashimoto, H; Tanaka, K; Urade, Y, 2000) | 0.65 |
"Treatment with indomethacin decreased the abundance of PKC-beta1 and increased that of PKC-beta2, eta, and epsilon, but did not alter the expression of PKC alpha, gamma, zeta, delta, iota, and micro. " | ( Overexpression of protein kinase C-beta1 isoenzyme suppresses indomethacin-induced apoptosis in gastric epithelial cells. Ching, CK; Eggo, MC; Lai, KC; Lam, SK; Slosberg, ED; Soh, JW; Weinstein, IB; Wong, BC; Yuen, ST; Zhu, GH, 2000) | 0.9 |
"A pretreatment with indomethacin (200 microg mouse(-1)) significantly reduced the RPA-induced but not the BK-induced increase in Evans blue extravasation." | ( Contribution of B(2) receptors for bradykinin in arthus reaction-induced plasma extravasation in wild-type or B(2) transgenic knockout mice. Bkaily, G; D'Orleans-Juste, P; de Brum-Fernandes, A; Samadfam, R; Sirois, P; Teixeira, C, 2000) | 0.62 |
"Pretreatment with indomethacin completely blocked oxygen-induced vasodilation." | ( Oxygen-induced vasodilation in pulmonary arterioles from fetal rats. Coppola, CP; Gosche, JR; Reyes-Mugica, M; Vukcevic, Z, 2000) | 0.63 |
"Pretreatment with indomethacin did not influence the cytoprotective effect of rabeprazole." | ( Cytoprotective effect of rabeprazole against ethanol-induced gastric mucosal damage: possible involvement of nitric oxide. Arakawa, T; Fujiwara, Y; Higuchi, K; Tominaga, K; Watanabe, T, 2000) | 0.63 |
"Treatment with indomethacin induced gastric lesions by tissue peroxidation, with mucosal fluorescence intensity increasing time-dependently." | ( Autofluorescence in indomethacin-induced gastric mucosal lesions in rats. Hirano, KI; Kondo, Y; Matsui, H; Murata, Y; Muto, H; Nakahara, A; Tanaka, N; Yanaka, A, 2000) | 0.97 |
"Treatment with indomethacin partially reversed the inhibition of migration, but not DNA synthesis by IL-1beta suggesting cyclooxygenase products play an inhibitory role in migration." | ( Blockade of smooth muscle cell migration and proliferation in baboon aortic explants by interleukin-1beta and tumor necrosis factor-alpha is nitric oxide-dependent and nitric oxide-independent. Clowes, AW; Kenagy, RD, ) | 0.47 |
"Treatment with indomethacin (10 microg/mL), an established inhibitor of prostaglandin biosynthesis, resulted in a significant (P <.05) decrease (79%) in the ability of IL-1 beta to up-regulate IL-6 transcripts." | ( Periovulatory and interleukin (IL)-1-dependent regulation of IL-6 in the immature rat ovary: a specific IL-1 receptor-mediated eicosanoid-dependent effect. Adashi, EY; Ando, M; Chung, KW, ) | 0.47 |
"Pre-treatment with indomethacin significantly reduced the protective effect of the extract against HCl/ethanol solution to 31%." | ( Effects of methanol, cyclohexane and methylene chloride extracts of Bidens pilosa on various gastric ulcer models in rats. Dimo, T; Dongo, E; Tan, PV, 2000) | 0.63 |
"Pretreatment with indomethacin (200 microg/5 microl; icv), an inhibitor of cyclo-oxygenase, significantly attenuated the ANG II-induced increase in oxytocin secretion only." | ( Central interactions between angiotensin II and PGD(2) in the regulation of vasopressin and oxytocin secretion in dehydrated rats. Bui, V; Kadekaro, M; Summy-Long, JY; Terrell, ML, 2001) | 0.63 |
"Pretreatment with indomethacin, a cyclooxygenase inhibitor, also inhibited the carrageenin-induced responses significantly in normal rats." | ( Evidence for bradykinin mediation of carrageenin-induced inflammatory pain: a study using kininogen-deficient Brown Norway Katholiek rats. Ikeda, Y; Naraba, H; Oh-ishi, S; Ueno, A, 2001) | 0.63 |
"Pretreatment with indomethacin 10 min before LPS injections enhanced BBB disruption, but not insulin transport." | ( Effect of LPS on the permeability of the blood-brain barrier to insulin. Banks, WA; Morley, JE; Niehoff, ML; Xaio, H, 2001) | 0.63 |
"Treatment with indomethacin 50 mg/day promptly relieved the pain which had affected her for the previous 9 years." | ( Hemicrania continua with onset at an early age. Fragoso, YD; Machado, PC, ) | 0.47 |
"Treatment with indomethacin, a potent inhibitor of PG biosynthesis, inhibited DMBA-induced inflammation and local immunosuppression." | ( Carcinogen-induced inflammation and immunosuppression are enhanced in xeroderma pigmentosum group A model mice associated with hyperproduction of prostaglandin E2. Horio, T; Kuwamoto, K; Miyauchi-Hashimoto, H; Tanaka, K; Urade, Y, 2001) | 0.65 |
"Pretreatment with indomethacin (5 mg/kg) abolished the NB(ONH) increase but not the IOP reduction in latanoprost-treated eyes in rabbits and monkeys." | ( Effects of topical latanoprost on optic nerve head circulation in rabbits, monkeys, and humans. Araie, M; Fukaya, Y; Ishii, K; Kanno, M; Nagahara, M; Tamaki, Y; Tomidokoro, A, 2001) | 0.63 |
"Treatment with indomethacin induced intracellular oxidant formation in colon cancer cells significantly increased the spermidine/spermine-acetyltrasferase activity (SSAT) and enhanced polyamine acetylation and efflux from colon cancer cells." | ( Nonsteroidal anti-inflammatory drugs stimulate spermidine/spermine acetyltransferase and deplete polyamine content in colon cancer cells. Dauletbaev, N; Milovic, V; Stein, J; Turchanowa, L, 2001) | 0.65 |
"Treatment with indomethacin, an inhibitor of prostaglandin (PG) synthesis, inhibited UV-induced inflammation and abrogated immunosuppression." | ( Photobiologic and photoimmunologic characteristics of XPA gene-deficient mice. Horiki, S; Horio, T; Kuwamoto, K; Miyauchi-Hashimoto, H; Okamoto, H; Tanaka, K, 2001) | 0.65 |
"Treatment with indomethacin induced a time-dependent increase of fluorescence intensity. " | ( Endoscopic fluorescence observation of gastric mucosa after indomethacin treatment in rats. Matsui, H; Murata, Y; Nakahara, A; Tanaka, N, 2002) | 0.91 |
"Pretreatment with indomethacin exacerbated coronary flow reduction observed with alpha1 stimulation in failing hearts only." | ( Altered coronary and cardiac adrenergic response in the failing hamster heart: role of cyclooxygenase derivatives. Brousseau, D; Desjardins, JF; Dumont, L; Jasmin, G, 2002) | 0.64 |
"Treatment with indomethacin (75-150 mg/day) raised the upright blood-pressure (B.P.) by an average of 20-30 mm Hg diastolic and allowed the four patients with I.O.H." | ( Treatment of idiopathic orthostatic hypotension (Shy-Drager syndrome) with indomethacin. Itskovitz, HD; Kochar, MS, 1978) | 0.83 |
"Treatment with indomethacin for 7 days resulted in significant decreases in basal plasma norepinephrine from 134 +/- 7 to 99 +/- 6 (SEM) pg/ml (P less than 0.01), a 26% decrease." | ( Effect of inhibition of prostaglandin synthesis on sympathetic nervous system function in man. Bartter, FC; Güllner, HG; Kafka, MS; Lake, CR, 1979) | 0.6 |
"Pretreatment with indomethacin inhibited the effect of caffeine." | ( Effect of prostaglandins on the increased corticosterone output induced by caffeine in the rat. Ceserani, R; Costa, G; De Pasquale, A; Trovato, A, 1979) | 0.58 |
"Treatment with indomethacin resulted in rapid defervescence, resolution of the pericardial effusion and the orogenital ulcerations, and disappearance of the cryoglobulinemia." | ( Behçet's syndrome. Report of a case associated with pericardial effusion and cryoglobulinemia treated with indomethacin. Kistner, ML; Scarlett, JA; Yang, LC, 1979) | 0.81 |
"3 Pretreatment was indomethacin diminished or abolished the actions of the three effective fatty acids but not those of prostaglandin E2." | ( Actions of prostaglandin precursors and other unsaturated fatty acids on conduction time and refractory period in the cat heart in situ. Bayer, BL; Förster, W, 1979) | 0.58 |
"Pretreatment with indomethacin (INDO) significantly increased the abortifacient effect of prostaglandin (PG) E2 when administered intravenously to abort pregnancies with fetal death in utero. " | ( Indomethacin increases abortifacient effect of PGE2 in man. Basta, A; Dłuzniewska, M; Klimczyk, K; Małolepazy, A; Piotrowski, J; Spławinski, JA, 1979) | 2.04 |
"Pretreatment with indomethacin resulted in increased and prolonged fourosemide plasma levels, increased area under the curve, decreased plasma clearance, decreased renal clearance, increased half-life, no change in volume of distribution, and decreased sodium excretion and urine volume." | ( Attenuation of furosemide's diuretic effect by indomethacin: pharmacokinetic evaluation. Benet, LZ; Brater, DC; Lin, ET; Smith, DE, 1979) | 0.84 |
"Treatment with indomethacin, hydrocortisone, dexamethasone, promethazine, metiazinic acid and (+)-catechin ameliorated the liver damage." | ( Protection of mice against endotoxin-induced liver damage by anti-inflammatory drugs. Allison, AC; Ferluga, J; Kaplun, A, 1979) | 0.6 |
"Treatment with indomethacin eliminated these headaches." | ( Chronic paroxysmal hemicrania: a disabling headache syndrome responding to indomethacin. Posner, JB; Price, RW, 1978) | 0.83 |
"Rats treated with indomethacin showed a marked decrease of proteinuria (tested by the 3% sulfosalicylic aicd method) and a clear ultrastructural picture of hyperplasia and hypertrophy of podocytes." | ( Indomethacin and lysine acetylsalicylate in rats with autologous nephrotoxic serum nephritis. Biochemical and morphological studies. Cioffi, A; Conte, F; Di Belgiojoso, GB; Donati, MB; Saruggia, M; Sessa, A, 1978) | 2.02 |
"Pre-treatment with indomethacin (2 mg/kg/i.p.) was effective in reducing oedema and protein extravasation for both doses of carrageenin." | ( Relationship between oedema and plasma exudation in rat paw carrageenin inflammation. Ferreira, SH; Zanin, MT, 1978) | 0.58 |
"Pretreatment with indomethacin did not block the intraocular pressure rise induced by A23187." | ( The effect of cation ionophores on intraocular pressure. Podos, SM, 1976) | 0.58 |
"Treatment with indomethacin, which decreased urinary prostaglandin E-like material by 69 per cent or more, did not affect blood pressure." | ( Bartter's syndrome: a disorder characterized by high urinary prostaglandins and a dependence of hyperreninemia on prostaglandin synthesis. Bartter, FC; Bowden, RE; Frölich, JC; Gill, JR; Keiser, HR; Oates, JA; Seyberth, HW; Taylor, AA, 1976) | 0.6 |
"Treatment with indomethacin, phenylbutazone, or flufenamic acid caused some inhibition of the traumatic deciduomal response in spayed rats treated with progesterone, while treatment with cortisone acetate and Compound 83161 did not." | ( Studies on the effects of pharmacologic doses of cortisone acetate and several nonsteroidal anti-inflammatory compounds on ovo-implantation, early pregnancy, and the deciduomal response in the rat. Bennett, DR; Cochrane, RL; Powell, JG; Rathmacher, RP; Shaar, CJ; Smalstig, EB, 1977) | 0.6 |
"Pretreatment with indomethacin markedly attenuated both the hemodynamic changes and the rise in plasma renin activity caused by endotoxin administration." | ( Prostaglandins and the renin-angiotensin system in canine endotoxemia. Feldhaus, RA; Isakson, PC; McKnight, RC; Needleman, P; Raz, A; Shofer, F, 1977) | 0.58 |
"Pretreatment by indomethacin reduced the antiarrhythmic effects of linoleic acid from 40 percent to 9 percent on ouabain-induced arrhythmias in cats." | ( Effects of arachidonic, linoleic, linolenic and oleic acid on experimental arrhythmias in cats, rabbits and guinea-pigs. Blass, KE; Forter, W; Mest, HJ, 1977) | 0.59 |
"Pretreatment with indomethacin abolished the release of PGE2 and PGA2-like substances but no arachidonic acid and reduced the reactive hyperemic response in magnitude and duration." | ( Prostaglandin-like substances in coronary venous blood following myocardial ischemia. Folts, JD; Kraemer, RJ; Phernetton, TM, 1976) | 0.58 |
"Pretreatment with indomethacin did not affect or slightly potentiated the cholecystokinetic effect of the three prostaglandins but abolished that of pentagastrin, suggesting that prostaglandins are possible mediators for the cholecystokinetic action of the gastrointestinal hormones." | ( Effect of prostaglandins E1, E2 and F2alpha and pentagrastin on the gall bladder pressure in dogs. McCloy, RE; Nakano, J, 1975) | 0.58 |
"Treatment with indomethacin significantly prolonged the length of gestation (P smaller than 0-01) compared iwth control, untreated animals." | ( The effects of dexamethasone and indomethacin on the outcome of pregnancy in the rabbit. Challis, JR; Davies, IJ; Ryan, KJ, 1975) | 0.88 |
"Treatments of indomethacin and/or PGF2alpha did not affect the duration of parturition." | ( Effects of indomethacin and prostaglandin F2alpha on parturition in the hamster. Chang, MC; Lau, IF; Saksena, SK, 1975) | 0.99 |
"Treatment with indomethacin elevated systemic arterial pressure and pulmonary vascular resistance in hypotensive newborn goats. " | ( Use of indomethacin to reverse neonatal hypotension. Cassin, S; Leffler, C; Tyler, T, 1976) | 1.06 |
"Dogs treated with indomethacin prior to SAO shock did not exhibit a significant increase in portal venous PGF2alpha." | ( Release of prostaglandin F2alpha during splanchnic artery occlusion shock. Bridenbaugh, GA; Flynn, JT; Lefer, AM, 1976) | 0.58 |
"Pretreatment with indomethacin (5 mg/kg i.p.), which suppressed the generation of PG by 85%, slightly enhanced the mucosal lesions induced by ethanol but failed to affect the fall in GBF induced by this irritant." | ( Studies on gastroprotection induced by capsaicin and papaverine. Brzozowski, T; Drozdowicz, D; Konturek, SJ; Majka, J, 1992) | 0.61 |
"Pretreatment with indomethacin also prevented the O3 effects, as reflected by the decreased protein and albumin flux in BAL and 99mTc-DTPA transport from trachea to blood." | ( Attenuation of ozone-induced airway permeability in rats by pretreatment with cyclophosphamide, FPL 55712, and indomethacin. Bhalla, DK; Daniels, DS; Luu, NT, 1992) | 0.82 |
"Treatment with indomethacin as well as removal of the endothelium was followed by contractions of umbilical arteries and a reduced formation of prostacyclin." | ( Any physiological role for prostacyclin in regulation of fetal vessel tone? Klockenbusch, W; Schrör, K; Strobach, H, 1992) | 0.62 |
"Pretreatment with indomethacin (10 mg/kg) reduced the secretory response to the enterotoxin by about 50%." | ( 5-HT receptor antagonists and heat-stable Escherichia coli enterotoxin-induced effects in the rat. Badhri, P; Beubler, E; Schirgi-Degen, A, 1992) | 0.61 |
"Pretreatment with indomethacin (5 mg/kg intraperitoneally), which reduced mucosal generation of PGE2 by 85%, decreased in part the protection by TGF and EGF against ethanol-induced damage and virtually abolished the protective action of these peptides against stress-induced injury.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Transforming growth factor alpha and epidermal growth factor in protection and healing of gastric mucosal injury. Brzozowski, T; Dembinski, A; Konturek, SJ; Majka, J; Slomiany, A; Slomiany, BL, 1992) | 0.61 |
"Pretreatment with indomethacin (5 mg/kg, subcutaneously) significantly attenuated the GMBF responses to 1 M NaCl and 0.2 N HCl and inhibited the increase of pH caused by 1 M NaCl." | ( Role of capsaicin-sensitive afferent neurons in mucosal blood flow response of rat stomach induced by mild irritants. Matsumoto, J; Okabe, S; Takeuchi, K; Ueshima, K, 1992) | 0.61 |
"Treatment with indomethacin could only abrogate the effects of nanogram doses of rIL-1 beta." | ( In-vivo administration of interleukin 1 both enhances and suppresses contact sensitivity in the mouse. Bäck, O; Linna, J, 1992) | 0.62 |
"Treatment with indomethacin had a dramatic effect on the CPH attacks but did not modify the course of the migraine." | ( Chronic paroxysmal hemicrania coexisting with migraine. Differential response to pharmacological treatment. Pareja, J, 1992) | 0.62 |
"Treatment with indomethacin inhibited the phasic component in the strips with endothelium, but did not influence the relaxation after endothelium denudation." | ( [Mechanisms of histamine-induced relaxation in isolated dog mesenteric arteries and veins]. Toda, N; Yamazaki, M, 1992) | 0.62 |
"Pretreatment with indomethacin also reversed, in part, the protective and hyperemic effects of sucralfate but the combination of both indomethacin and L-NNA completely abolished these effects." | ( Role of nitric oxide and prostaglandins in sucralfate-induced gastroprotection. Brzozowski, T; Czarnobilski, K; Konturek, SJ; Majka, J, 1992) | 0.61 |
"Treatment with indomethacin (2.8 microM) had no effect on arteries preequilibrated at low PO2 (21 +/- 1 mm Hg); however, the same treatment contracted (approximately 45% of the response to activating solution) arteries at either an intermediate (40 +/- 0.8 mm Hg) or high (70 +/- 0.9 mm Hg) PO2." | ( Isolated pulmonary resistance vessels from fetal lambs. Contractile behavior and responses to indomethacin and endothelin-1. Coceani, F; Wang, Y, 1992) | 0.84 |
"Pretreatment with indomethacin blocked the decrease in water intake by IL-1 beta, suggesting the involvement of production of prostaglandins." | ( Intraperitoneal administration of recombinant human interleukin-1 beta inhibits osmotic thirst in the rat. Kannan, H; Kawano, S; Osaka, T; Ueta, Y; Yamashita, H, 1992) | 0.61 |
"Pretreatment with indomethacin did not attenuate the neutrophil sequestration within the pulmonary parenchyma." | ( Acute lung injury following reperfusion after ischemia in the hind limbs of rats. Cashmer, B; Oldham, K; Punch, J; Rees, R; Smith, DJ; Wilkins, E, 1991) | 0.6 |
"Pretreatment with indomethacin abolished the facilitatory effect of Cap and enhanced its inhibitory effect, indicating that prostaglandins are involved in the action of Cap." | ( Dual effects of capsaicin on responses of the rabbit ear artery to field stimulation. Moritoki, H; Takase, H; Tanioka, A, 1990) | 0.6 |
"Pretreatment with indomethacin significantly mitigated the protective effect of stress against ethanol injury." | ( Gastric mucosal protection induced by restraint and water-immersion stress in rats. Ishihara, T; Ohno, T; Uramoto, H, 1990) | 0.6 |
"Treatment with indomethacin shifted the dose-response curves of angiotensin II- and arginine vasopressin-induced inositol trisphosphate production to the left." | ( Potentiation of inositol trisphosphate production by dexamethasone. Iwaita, Y; Kato, H; Nakazato, Y; Saruta, T; Sato, A; Suzuki, H, 1992) | 0.62 |
"Pretreatment with indomethacin, which inhibited prostaglandin E2 output by 60%, did not prevent protection by cysteamine; incubation with cysteamine decreased prostaglandin E2 production by cultured cells." | ( Cysteamine protects gastric epithelial cell monolayers against drug induced damage: evidence for direct cellular protection by sulphydryl compounds. Ivey, J; Raza, A; Razandi, M; Romano, M; Szabo, S, 1992) | 0.61 |
"Pretreatment with indomethacin prevented these effects of T3." | ( Evidence for direct non-genomic effects of triiodothyronine on bone rudiments in rats: stimulation of the inositol phosphate second messenger system. Lakatos, P; Stern, PH, 1991) | 0.6 |
"Treatment with indomethacin potentiated the contractile response of the arteries and reversed the relaxant response of veins to a contraction." | ( Comparison of responses to angiotensin II of dog mesenteric arteries and veins. Toda, N; Yamazaki, M, 1991) | 0.62 |
"Treatment with indomethacin spray appeared to be effective in 80% and well-tolerated in 93% of the patients studied." | ( Double-blind, randomized crossover study of the percutaneous efficacy and tolerability of a topical indomethacin spray versus placebo in the treatment of tendinitis. Famaey, JP; Ginsberg, F, ) | 0.69 |
"Pretreatment with indomethacin to suppress mucosal generation of prostaglandin or the removal of salivary glands to eliminate the endogenous source of epidermal growth factor failed to affect sucralfate-induced gastroprotection." | ( Role of acid milieu in the gastroprotective and ulcer-healing activity of sucralfate. Brzozowski, T; Drozdowicz, D; Garlicki, J; Konturek, SJ; Majka, J; Pytko-Polonczyk, J, 1991) | 0.6 |
"Pretreatment with indomethacin abolished the pressor response to NMA; however, systemic vasoconstriction and cardiac depression still occurred." | ( Cardiovascular actions of inhibitors of endothelium-derived relaxing factor (nitric oxide) formation/release in anesthetized dogs. Helgren, MC; Klabunde, RE; Ritger, RC, 1991) | 0.6 |
"Pretreatment with indomethacin did not reverse the protective effects of hyperoxia or the hypoxia-induced enhancement of bronchial reactivity." | ( Hyperoxia prevents hypoxia-induced bronchial hyperreactivity via a cyclooxygenase-independent mechanism. Ahmed, T; D'Brot, J, 1991) | 0.6 |
"Pretreatment with indomethacin (5 mg kg-1 i.v.) or meclofenamic acid (2 mg kg-1 i.v.) attenuated the mannitol-induced response but acetylsalycilic acid (10 mg kg-1 i.v.) was without effect." | ( Differential effects of cyclooxygenase inhibitors on the cardiovascular response to hyperosmotic mannitol. Barrachina, MD; Cortijo, J; Durá, JM; Martí-Cabrera, M; Morcillo, E; Ortiz, JL, 1991) | 0.6 |
"Treatment with indomethacin did not affect the initial rapid twitch-like contraction, but inhibited the augmented spontaneous motility." | ( Contraction and prostaglandin biosynthesis by myometrium from non-pregnant and pregnant rabbits in response to adenosine 5'-triphosphate. Suzuki, Y, 1991) | 0.62 |
"Pretreatment with indomethacin and d-naproxen completely inhibited ozone-induced increases in PGE recovered by BAL and the suppression of peritoneal macrophage phagocytic activity." | ( Ozone reduces murine alveolar and peritoneal macrophage phagocytosis: the role of prostanoids. Canning, BJ; Hmieleski, RR; Jakab, GJ; Spannhake, EW, 1991) | 0.6 |
"Pretreatment with indomethacin, to suppress mucosal generation of prostaglandins (PG), greatly augmented stress-induced gastric ulcerations and antagonized the protection exerted by both Solcoseryl and EGF." | ( Solcoseryl in prevention of stress-induced gastric lesions and healing of chronic ulcers. Bielański, W; Brzozowski, T; Drozdowicz, D; Konturek, SJ; Pytko-Polonczyk, J, 1991) | 0.6 |
"Pretreatment with indomethacin failed to affect the gastroprotective action of EGF and polyamines, suggesting that endogenous PGs may not play any major role in this protection." | ( Role of polyamines and prostaglandins in gastroprotective action of epidermal growth factor against ethanol injury. Brzozowski, T; Drozdowicz, D; Garlicki, J; Konturek, SJ; Majka, J, 1991) | 0.6 |
"Pretreatment with indomethacin, or BM 13505, a specific thromboxane A2 receptor blocker, ameliorated the development of metabolic acidosis in N-6 fatty acid-fed animals, demonstrating a role for prostanoids in the sequelae of endotoxemia." | ( Diets enriched with N-3 fatty acids ameliorate lactic acidosis by improving endotoxin-induced tissue hypoperfusion in guinea pigs. Bistrian, BR; Blackburn, GL; Flores, EA; Pomposelli, JJ; Zeisel, SH, 1991) | 0.6 |
"Treatment with indomethacin or diclofenac sodium (voltaren) completely inhibited the production and secretion of PGE2 but not the tumoricidal activity of activated macrophages measured either immediately after activation or 1 to 3 days thereafter." | ( Prostaglandin E2 does not inhibit tumoricidal activity of mouse macrophages against adherent tumor cells. Fidler, IJ; Utsugi, T, 1991) | 0.62 |
"Pretreatment with indomethacin decreased myocardial CK in the exercise-trained rats (indomethacin: 15.4 +/- 0.8 U.mg-1 protein; saline: 17.7 +/- 0.7 U.mg-1 protein; p less than 0.05), but not in the controls (indomethacin: 10.3 +/- 1.0 U.mg-1 protein; saline: 10.8 +/- 0.6 U.mg-1 protein; p greater than 0.05)." | ( Exercise training, indomethacin, and isoproterenol-induced myocardial necrosis in the rat. Brodowicz, GR; Lamb, DR, ) | 0.78 |
"Treatment with indomethacin, a cyclooxygenase inhibitor, significantly lowered FENa to 0.45 +/- 0.13, 0.77 +/- 0.21, and 1.19 +/- 0.59% at RPP of 91, 121, and 146 mmHg, respectively." | ( Renal interstitial hydrostatic pressure and PGE2 in pressure natriuresis. Berndt, TJ; Gonzalez-Campoy, JM; Knox, FG; Long, C; Roberts, D; Romero, JC, 1991) | 0.62 |
"Pretreatment with indomethacin (3 mg/kg body weight), however, completely blocked the interleukin-1-induced stimulation of insulin secretion." | ( Indomethacin reverses interleukin-1-induced hyperinsulinemia in conscious and freely moving rats. Kumei, Y; Namiki, M; Okumura, T; Takasugi, Y; Uehara, A, 1991) | 2.05 |
"Pretreatment with indomethacin significantly enhanced the affinity of antibodies produced 21 days after immunization with human serum albumin (HSA)." | ( Induction of leukotriene production before antigen challenge enhances antibody affinity in genetically selected mice. Phillips, C, 1991) | 0.6 |
"Pretreatment with indomethacin to decrease endogenous prostaglandin production resulted in more severe ethanol-induced duodenal injury in both groups; however, there were no longer statistically significant differences between the omeprazole and control groups." | ( Chronic omeprazole treatment increases duodenal susceptibility to ethanol injury in rats. Bezabah, S; Erickson, RA; Jonas, G; Lifrak, E; Tarnawski, AS, 1991) | 0.6 |
"Pretreatment with indomethacin abolishes postlavage pulmonary hypertension, preserves a slightly better lung function with higher arterial PO2, and prevents the postlavage peripheral neutropenia found in untreated animals." | ( Lung injury in a surfactant-deficient lung is modified by indomethacin. Bryan, AC; Burger, R; Fung, D, 1990) | 0.85 |
"Treatment with indomethacin slightly potentiated the contractions induced by PGF2 alpha in mesenteric arteries." | ( Regional differences in the prostanoid receptors mediating prostaglandin F2 alpha-induced contractions of cat isolated arteries. Nakajima, M; Ueda, M, 1990) | 0.62 |
"Pre-treatment with indomethacin completely prevented the effects of solcoseryl on mucosal PGE2, but not LTC4 levels, and significantly reduced its circulatory and metabolic actions on the stomach." | ( Contribution of prostanoids to gastric circulatory and metabolic actions of solcoseryl. Czarnobilski, K; Gustaw, P; Konturek, SJ; Pawlik, WW; Sendur, R, ) | 0.45 |
"Pretreatment with indomethacin which significantly reduced serum thromboxane and urinary thromboxane and 6-keto-PGF 1 alpha prevented the renin stimulating effect and the increase in GFR induced by ketanserin without changing the other actions of this drug." | ( [Humoral and hemodynamic (systemic and renal) effects of ketanserin in patients with essential hypertension: what is the role of prostaglandins?]. Lucarini, AR, ) | 0.45 |
"Treatment with indomethacin at a dose (5 mg kg-1, i.v.) that reduced urinary prostaglandin E2 (PGE2) excretion by at least 70% did not alter these responses." | ( Effect of cyclo-oxygenase blockade on the renal actions of vasopressin and SK&F 105494 in the rhesus monkey. Albrightson-Winslow, CR; Brooks, DP; Caldwell, NC; Kinter, LB; Koster, PF, 1990) | 0.62 |
"Pretreatment with indomethacin, 5 mg/kg sc one hour before aluminium phosphate, slightly but significantly (p less than 0.05) reduced the cytoprotective effect of aluminium phosphate." | ( Prevention by aluminium phosphate of gastric lesions induced by ethanol in the rat: role of endogenous prostaglandins and sulfhydryls. Duchateau, A; Garbe, E; Thiefin, G; Varin-Bischoff, S; Zeitoun, P, 1990) | 0.6 |
"Pretreatment with indomethacin (2 mg/kg) ameliorated PAF-induced alterations in renal hemodynamics and glomerular permselectivity in the final collection period." | ( Thromboxane mediates the renal hemodynamic effects of platelet activating factor. Neugarten, J; Schlondorff, D; Yoo, J, 1990) | 0.6 |
"Pretreatment with indomethacin or pilocarpine specifically attenuated the ability of MK-422 to lower IOP suggesting that biosynthesis of prostaglandins and uveoscleral outflow pathways are important in mediating the ocular hypotension." | ( Prostaglandins mediate the ocular hypotensive action of the angiotensin converting enzyme inhibitor MK-422 (enalaprilat) in African green monkeys. Lotti, VJ; Pawlowski, N, 1990) | 0.6 |
"Treatment with indomethacin briefly improved the symptoms, but within 72 hours the patient developed a fulminant illness with high fever and clinical as well as biochemical signs of a severe consumption coagulopathy." | ( [Atypical joint symptoms as initial symptoms of varicella infection in chronic myeloid leukemia]. Arning, M; Aul, C; Bürrig, KF; Reinecke, P; Schneider, W, 1990) | 0.62 |
"Treatment with indomethacin (5 x 10(-6) M) had no effect on endothelin-induced contraction in either WKY rat or SHRSP aortic rings." | ( Role of endothelium in the response to endothelin in hypertension. Bohr, DF; Wu, CC, 1990) | 0.62 |
"Pretreatment with indomethacin or HgII2 did not prevent the AGC, there suggesting that neither endogenous PGS nor gastric mucus take part in its mechanism." | ( [Role of protons and bicarbonate in adaptative gastric cytoprotection]. Bedini, OA; Cesolari, JA; Laudanno, OM; San Miguel, P, 1990) | 0.6 |
"Treatment with indomethacin or aspirin potentiated the contractile response of monkey mesenteric arteries, whereas treatment with ONO3708 and removal of endothelium did not alter the response significantly." | ( Modifications by endogenous prostaglandins of angiotensin II-induced contractions in dog and monkey cerebral and mesenteric arteries. Ayaziki, K; Okamura, T; Toda, N, 1990) | 0.62 |
"Treatment of indomethacin colon with 1 mM mucosal amiloride eliminated net Na(+)-Cl- absorption without affecting the short-circuit current (Isc)." | ( NaCl transport across equine proximal colon and the effect of endogenous prostanoids. Argenzio, RA; Clarke, LL, 1990) | 0.63 |
"Pretreatment with indomethacin caused a significant prolongation of ulcer healing, and this was accompanied by a significant reduction in PG and EGF formation, suggesting that both factors may be involved in ulcer healing." | ( Healing of chronic gastroduodenal ulcerations by antacids. Role of prostaglandins and epidermal growth factor. Brzozowski, T; Dembinski, A; Drozdowicz, D; Konturek, SJ; Nauert, C, 1990) | 0.6 |
"Pretreatment with indomethacin (5 mg/kg iv.) or verapamil (2 mg/kg iv.) 30 min prior to the dextran infusion prevented significantly a decrease in blood and pulse pressure, and also an increase in the hematocrit value, paw thickness and serum histamine level of rats." | ( [The effects of indomethacin and verapamil on dextran-induced shock in rats]. Ishizaki, M, 1985) | 0.94 |
"Pretreatment with indomethacin significantly improved CIn and CPAH, and potassium repletion abolished this effect entirely." | ( Captopril enhances aminoglycoside nephrotoxicity in potassium-depleted rats. Baker, JD; Boatman, JE; Klotman, PE; Volpp, BD; Yarger, WE, 1985) | 0.59 |
"Treatment with indomethacin partly but significantly inhibited the effect of spizofurone, but did not affect that of PGE2." | ( Spizofurone, a new anti-ulcer agent, increases alkaline secretion in isolated bullfrog duodenal mucosa. Inada, I; Inatomi, N; Maki, Y; Nagaya, H; Satoh, H, 1986) | 0.61 |
"Pretreatment with indomethacin and aprotinin prevented both the increased regional permeability of the blood-brain barrier along with regional cerebral blood flow." | ( Effect of captopril (a converting enzyme inhibitor) on blood-brain barrier permeability and cerebral blood flow in normotensive rats. Sharma, HS, 1987) | 0.6 |
"Pretreatment with indomethacin, or with BW 755 C, a dual inhibitor of both the cyclo- and lipoxygenase pathway did not prevent barrier opening by arachidonate for Na+-fluorescein." | ( Permeability and vasomotor response of cerebral vessels during exposure to arachidonic acid. Baethmann, A; Hammersen, F; Unterberg, A; Wahl, M, 1987) | 0.6 |
"Pretreatment with indomethacin prevented the leakage of fluorescein into the anterior chamber up to 2 hrs after intracameral injection of lens proteins." | ( Prevention of lens protein-induced ocular inflammation with cyclooxygenase and lipoxygenase inhibitors. Chang, MS; Chiou, GC, 1989) | 0.6 |
"The treatment with indomethacin, 75 mg/d for 3 d, did not alter AVP-induced forearm vasodilatation." | ( Biphasic forearm vascular responses to intraarterial arginine vasopressin. Ando, S; Hirooka, Y; Imaizumi, T; Nakamura, M; Suzuki, S; Takeshita, A; Yoshida, M, 1989) | 0.6 |
"Pre-treatment with indomethacin did not to any great extent affect the responses, which contradicts the involvement of prostaglandins." | ( Cardiovascular responses to intravenous calcitonin gene-related peptide (CGRP) in the albino rabbit. Andersson, SE, 1989) | 0.6 |
"Pretreatment with indomethacin did not affect its effect, thereby suggesting that endogenous prostaglandins will not be involved in the mechanism of action of MG111." | ( Effects of hEGF (MG111) on gastric mucosal potential difference in rats. Azuma, R; Gotoh, K; Ishikawa, T; Katamura, H; Kunisaki, C; Sugiyama, M; Tsuchiya, S; Yamazaki, Y, 1989) | 0.6 |
"Pretreatment with indomethacin completely inhibited this 6-keto-PGF1 alpha release." | ( Endothelin stimulates the release of prostacyclin from rat mesenteric arteries. Mikami, H; Nagano, M; Nakamaru, M; Ogihara, T; Rakugi, H; Tabuchi, Y, 1989) | 0.6 |
"Pretreatment with indomethacin (25 mg/hour) failed to influence this secretory response." | ( Effect of sucralfate on human gastric bicarbonate secretion and local prostaglandin E2 metabolism. Rees, WD; Shorrock, CJ, 1989) | 0.6 |
"Pretreatment with indomethacin 25 mg t.i.d." | ( A study of tolerance to the psychomotor effects of indomethacin in healthy volunteers. Bird, H; Dale, S; Lowe, J; Pullar, T, 1989) | 0.85 |
"Treatment with indomethacin and diclofenac sodium was found to increase granulocyte counts in the blood of sublethally gamma-irradiated mice. " | ( Effect of indomethacin, diclofenac sodium and sodium salicylate on peripheral blood cell counts in sublethally gamma-irradiated mice. Kozubík, A; Netíková, J; Pipalová, I; Pospísil, M, 1989) | 1.03 |
"Pretreatment with indomethacin 1 mg/kg i.p." | ( Indomethacin and acetylsalicylic acid block neurogenic plasma protein extravasation in rat dura mater. Buzzi, MG; Moskowitz, MA; Sakas, DE, 1989) | 2.04 |
"Treatment with indomethacin rapidly reduced the hemodynamic compromise, avoiding the need for pericardiocentesis." | ( Resolution of cardiac tamponade in systemic lupus erythematosus with indomethacin. Galve, E; Porcel, JM; Selva, A; Soler-Soler, J; Tornos, MP, 1989) | 0.85 |
"Pretreatment with indomethacin (IND) had little influence on the cytoprotective effects of OGT and glutathione, but attenuated the effect of sucralfate." | ( A possible mechanism for the gastric mucosal protection by oren-gedoku-to (OGT), a traditional herbal medicine. Imanishi, K; Miura, O; Takase, H; Yumioka, E, 1989) | 0.6 |
"Pretreatment with indomethacin completely prevented the ACTH response induced by either iv or icv injection of IL-1 beta." | ( Adrenocorticotropin release induced by intracerebroventricular injection of recombinant human interleukin-1 in rats: possible involvement of prostaglandin. Arimura, A; Dahl, RR; Gottschall, PE; Katsuura, G, 1988) | 0.6 |
"Pretreatment with indomethacin abolished the formation of PGF2 alpha but significantly enhanced the biosynthesis of immunoreactive LTC4-like material at 18 min after the beginning of seizures." | ( Characterization of seizure-induced cysteinyl-leukotriene formation in brain tissue of convulsion-prone gerbils. Hertting, G; Seregi, A; Simmet, T, 1988) | 0.6 |
"Pretreatment with indomethacin (5 mg/kg iv) markedly reduced postischemia SOD-inhibitable NBT reduction (2.8 +/- 1.1 pmol.mm-2.20 min-1)." | ( Postischemic generation of superoxide anion by newborn pig brain. Armstead, WM; Busija, DW; Leffler, CW; Mirro, R, 1988) | 0.6 |
"Co-treatment with indomethacin (1 microM) reduced this augmentation in PC activity by 33% (p less than 0.05)." | ( Concurrent expression of procoagulant and plasminogen activator activities by rabbit alveolar macrophages in vitro: opposite modulating effects of prostaglandin E2. Hasday, JD; Sitrin, RG, 1988) | 0.6 |
"Pretreatment with indomethacin prior to HCl application led to a reduction in HCO3- and caused a decrease in mucin phospholipid content, but had no effect on HCO3- secretion and the lipid content of mucins elaborated in response to taurocholate." | ( Intestinal release of mucin in response to HCl and taurocholate: effect of indomethacin. Bilski, J; Carter, SR; Konturek, SJ; Kosmala, M; Slomiany, A; Slomiany, BL, 1987) | 0.83 |
"Pretreatment with indomethacin (10 mg/kg), a cyclooxygenase inhibitor also significantly attenuated the diuresis and natriuresis elicited by diltiazem (100 mg/kg)." | ( Comparative renal effects of calcium channel blockers in conscious spontaneously hypertensive rats. Chiu, PJ; Sybertz, EJ; Vemulapalli, S, 1987) | 0.6 |
"Pretreatment with indomethacin for four days resulted in a 66% increase in maximal binding capacity (Bmax) without any change in affinity." | ( Prostaglandin-E2 receptors in the rat kidney: biochemical characterization and localization. Eriksen, EF; Gesser, BP; Jacobsen, NO; Richelsen, B; Stengaard-Pedersen, K, 1987) | 0.6 |
"Pretreatment with indomethacin or phentolamine had no effect on the inhibitory effect of somatostatin on the increase in gastric acid secretion during vagus nerve stimulation or bethanechol infusion." | ( Inhibitory effect of somatostatin on gastric acid secretion in rats. Fujiwara, M; Nishikawa, H; Yokotani, K, 1987) | 0.6 |
"Pretreatment with indomethacin (5 mg/kg) also prevented Cl-induced changes in GFR and CPAH and blunted (P less than 0.05) the Cl-induced increase in renal vascular resistance (RVR, vehicle +55 +/- 11%, n = 8, indomethacin +27 +/- 7%, n = 6)." | ( Intrarenal vasoconstriction during hyperchloremia: role of thromboxane. Bullivant, EM; Welch, WJ; Wilcox, CS, 1989) | 0.6 |
"Treatment with indomethacin or SQ 29548 prevented the decrease in cardiac index and attenuated the PAF-acether-induced rises in PAP and PVRI." | ( Circulatory effects of PAF-acether in newborn piglets. Bradley, LM; Czaja, JF; Feuerstein, G; Goldstein, RE, 1989) | 0.62 |
"Treatment with indomethacin reversed the IFN-gamma defect with most CBL tested, and the addition of physiologic amounts of PGE2 to indomethacin-treated cultures resulted in a profound impairment of IFN-gamma production similar to that of untreated CBL cultures." | ( Defective IFN-gamma production in the human neonate. II. Role of increased sensitivity to the suppressive effects of prostaglandin E. Arenzana-Seisdedos, F; Fiers, W; Huerta, JM; Rothhut, B; Russo-Marie, F; Virelizier, JL; Wakasugi, N, 1985) | 0.61 |
"Treatment with indomethacin and prednisone did not change baseline FEV1 and airway responsiveness." | ( Prednisone, indomethacin and airway responsiveness in toluene diisocyanate sensitized subjects. Dal Vecchio, L; De Marzo, N; Di Giacomo, R; Fabbri, LM; Maestrelli, P; Mapp, CE; Zocca, E, ) | 0.85 |
"Treatment with indomethacin after irradiation was found to increase the granulocyte and lymphocyte counts in peripheral blood." | ( Enhancement of hemopoietic recovery by indomethacin after sublethal whole-body gamma irradiation. Kozubík, A; Netíková, J; Pospísil, M, ) | 0.74 |
"Pretreatment with indomethacin or verapamil was also studied, since these drugs block the increase in pulmonary arterial pressure caused by t-bu-OOH." | ( Pharmacological modification of pulmonary vascular injury: possible role of cAMP. Farrukh, IS; Gurtner, GH; Michael, JR, 1987) | 0.6 |
"Pretreatment with indomethacin (10 mg/kg, ip) for 2 days also increased vascular renin activity (p less than 0.01)." | ( Effect of vasodilator prostaglandins on the vascular renin-angiotensin system. Inagami, T; Kumahara, Y; Nakamaru, M; Ogihara, T; Rakugi, H; Saito, H; Shimamoto, K, 1988) | 0.6 |
"Treatment with indomethacin substantially reduced the levels of PGs, particularly PGE2 in tumor tissue, inhibited the tumor growth, particularly the early stage of cell proliferation, prolonged the survival time, eliminated tumors in the abdominal cavity, and inhibited metastatic tumor recurrence after surgery." | ( [Anti-cancer treatment with prostaglandin synthetase inhibitor in animal models]. Masuda, T; Nagasawa, O; Narisawa, T; Niwa, M; Ogata, N; Takahashi, M, 1986) | 0.61 |
"Pretreatment with indomethacin caused reduction in the basal HCO3- and prostaglandin output, and prevented the increments evoked by arachidonic acid." | ( Mucus glycoprotein secretion by duodenal mucosa in response to luminal arachidonic acid. Carter, SR; Konturek, SJ; Kosmala, M; Slomiany, A; Slomiany, BL, 1986) | 0.59 |
"Pretreatment with indomethacin alone blunted the endotoxin- (8 mg/kg) induced hypoglycemia." | ( The effects of alpha adrenergic blockade on arachidonic acid metabolism and shock sequelae in endotoxemia. Armstrong, J; Cook, JA; Halushka, PV; Tempel, GE; Wise, WC, 1986) | 0.59 |
"The treatment with indomethacin substantially 1) inhibited the tumor growth, 2) prolonged the survival time, 3) caused a regression and disappearance of tumor with some cured mice and 4) reduced the levels of PGE2 and ornithine decarboxylase activity, a first rate limiting enzyme of polyamine synthesis in tumor tissue." | ( [Inhibition of the growth of a murine transplantable tumor, colon 26, by the prostaglandin synthetase inhibitor, indomethacin]. Koyama, H; Masuda, T; Nagasawa, O; Narisawa, T; Suzuki, K; Takahashi, M; Yoshioka, H, 1987) | 0.8 |
"Treatment with indomethacin prevented the 1-2 degrees C increase in body temperature observed in septic animals." | ( Fever is not responsible for the elevated glucose kinetics in sepsis. Bagby, GJ; Blakesley, HL; Lang, CH; Spitzer, JJ, 1987) | 0.61 |
"Treatment with indomethacin attenuated the AA-induced contraction in the intact strips and also the relaxation in the strips treated with ONO3708 or denuded of endothelium." | ( Endothelium-dependent and independent responses to prostaglandin H2 and arachidonic acid in isolated dog cerebral arteries. Bian, K; Inoue, S; Okamura, T; Toda, N, 1988) | 0.61 |
"Pretreatment with indomethacin (5 mg) prevented the increase in plasma renin activity as well as plasma catecholamine levels." | ( Effects of nonhypotensive endotoxemia in conscious rats: role of prostaglandins. Aubert, JF; Brunner, HR; Burnier, M; Nussberger, J; Waeber, B, 1988) | 0.6 |
"Treatment with indomethacin or dexamethasone failed to ameliorate the hyperoxic lung injury process." | ( Failure of non-selective inhibition of arachidonic acid metabolism to ameliorate hyperoxic lung injury. Hageman, JR; Holtzman, RB; Hunt, CE; Lee, SE; Smith, LJ; Zemaitis, J, 1988) | 0.61 |
"Pretreatment with indomethacin (8 mg/kg intraperitoneally) abolished the effects of the 10% linoleic acid diet on prostaglandin formation, acid secretion, and mucosal injury." | ( Modulation of rat gastric mucosal prostaglandin E2 release by dietary linoleic acid: effects on gastric acid secretion and stress-induced mucosal damage. Classen, M; Ruoff, HJ; Schepp, W; Schusdziarra, V; Steffen, B, 1988) | 0.6 |
"Pretreatment with indomethacin reduced peak FENa by 35%, but urinary delivery of piretanide was not altered." | ( The influence of nonsteroidal anti-inflammatory drugs and probenecid on the renal response to and kinetics of piretanide in man. Brewerton, DA; Dixey, JJ; Lant, AF; Noormohamed, FH; Pawa, JS, 1988) | 0.6 |
"Pretreatment with indomethacin while the dogs were under alpha-chloralose-urethan anesthesia gave similar results." | ( Histamine tachyphylaxis in canine airways despite prostaglandin synthesis inhibition. Antol, PJ; Gunst, SJ; Hyatt, RE, 1988) | 0.6 |
"Pretreatment with indomethacin had no effect on pressure/flow relations." | ( Detergent and methylene blue affect endothelium-dependent vasorelaxation and pressure/flow relations in rat blood perfused mesenteric arterial bed. Hiley, CR; Randall, MD, 1988) | 0.6 |
"Treatment with indomethacin, PGI2, and heparin eliminated neuron-disabling brain blood flows without altering early postischemic granulocyte accumulation." | ( Indomethacin, prostacyclin, and heparin improve postischemic cerebral blood flow without affecting early postischemic granulocyte accumulation. Dutka, AJ; Hallenbeck, JM; Kochanek, PM, ) | 1.91 |
"Treatment with indomethacin before feeding completely blocked the stimulation of protein synthesis." | ( The effect of indomethacin on the response of protein synthesis to feeding in rats and man. Broom, J; Fearns, LM; Garlick, PJ; McHardy, KC; McNurlan, MA; Milne, E; Reeds, PJ, 1987) | 0.97 |
"The treatment with indomethacin, however, clearly antagonized both events." | ( Short-term effects of an LHRH-agonist alone or in combination with testosterone propionate or indomethacin on rat testes. Evidence of testosterone independent effects. I. el Etreby, MF; Habenicht, UF; Neumann, F, ) | 0.67 |
"Treatment with indomethacin (10 mg/kg q 12 hr x 3) reduced both elevated water content and specific gravity values back to normal levels." | ( Indomethacin and dexamethasone treatment in experimental neoplastic spinal cord compression: Part 1. Effect on water content and specific gravity. Catane, R; Sandbank, U; Shapira, Y; Siegal, T, 1988) | 2.06 |
"Pretreatment with indomethacin blocked the histamine-induced cerebral vasodilation, but vasodilation after vehicle was intact." | ( Histamine dilates pial arterioles of newborn pigs through prostanoid production. Armstead, WM; Busija, DW; Leffler, CW; Mirro, R, 1988) | 0.6 |
"Pretreatment with indomethacin (5 mg kg-1, s.c.) one hour before the administration of 30 mg kg-1 endotoxin, significantly augmented the reduction in GMBF without affecting the reduction in BP." | ( Indomethacin potentiates endotoxin-induced blood flow reduction and histological injury in rat gastric mucosa. Guth, PH; Leung, FW; Piqué, JM; Whittle, BJ; Yonei, Y, 1988) | 2.04 |
"Pretreatment with indomethacin (4 or 20mg kg- p.o.) or aspirin in doses up to 25mg kg-1 p.o." | ( Effects of non-steroidal anti-inflammatory drugs on rat gastric mucosal leukotriene C4 and prostanoid release: relation to ethanol-induced injury. Hoppe, U; Lange, K; Peskar, BA; Peskar, BM, 1988) | 0.6 |
"Treatment with indomethacin lowered blood alcohol levels on day 7 and protected against the growth inhibition." | ( Alcohol metabolism and fetal hypoplasia in chick brain. Pennington, SN, ) | 0.47 |
"Pretreatment with indomethacin at a dose that inhibited gastric cyclooxygenase activity by an average of 88% did not affect the protective actions of sucralfate." | ( Effects of sucralfate on gastric prostaglandin and leukotriene synthesis: relationship to protective actions. Beck, PL; Gingras, GR; Morris, GP; Wallace, JL; Williamson, TE, 1988) | 0.6 |
"Pretreatment with indomethacin (10(-5) M) attenuated, but did not abolish, the increase in short-circuit current." | ( Effect of human eosinophil major basic protein on ion transport in dog tracheal epithelium. Gleich, GJ; Jacoby, DB; Loegering, DA; Nadel, JA; Ueki, IF; Widdicombe, JH, 1988) | 0.6 |
"Pretreatment with indomethacin (5 mg/kg, sc) significantly inhibited luminal alkalinization and PD recovery seen after exposure to TC." | ( Endogenous prostaglandins in gastric alkaline response in the rat stomach after damage. Takeuchi, K; Tanaka, H; Ueki, S, 1986) | 0.59 |
"Pretreatment with indomethacin (5 mg/kg, subcutaneously) significantly inhibited the increase of pH seen after exposure to 20 mM TC, but had no effect on the increase of pH caused by 40 mM SA." | ( Irritative and protective activity of mild irritants in rat stomach. Ohno, T; Okabe, S; Takeuchi, K, 1987) | 0.6 |
"Pretreatment with indomethacin partially reduced the protective effect of sucralfate." | ( Role of mucus and prostaglandins in the gastric mucosal protective actions of sucralfate against ethanol-induced injury in the rat. Quadros, E; Ramsamooj, E; Wilson, DE, 1987) | 0.6 |
"Treatment with indomethacin results in inhibition of tumor cell growth and elimination of all recoverable tumor cells." | ( Immune regulation of the L5178Y murine tumor-dormant state. I. In vivo and in vitro effects of prostaglandin E2 and indomethacin on tumor cell growth. Goldman, P; Liu, CM; Okayasu, T; Suzuki, K; Suzuki, Y; Wheelock, EF, 1986) | 0.82 |
"Treatment with indomethacin prolonged bleeding time, raised serum creatinine concentrations, and was associated with gastrointestinal haemorrhage in seven infants." | ( Early administration of indomethacin to preterm infants. Cooke, RW; Doyle, J; Rennie, JM, 1986) | 0.92 |
"Treatment with indomethacin attenuated the contraction-induced increase in mean arterial pressure and left ventricular dP/dt by 76% and 86%, respectively." | ( Prostaglandins contribute to cardiovascular reflexes evoked by static muscular contraction. Longhurst, JC; Maruoka, Y; Stebbins, CL, 1986) | 0.61 |
"Treatment with indomethacin, 10 mg/kg, induced hyperresponsiveness to NE in the sham operated rabbits and also produced a further increase in the response in the 3-day clipped rabbits: the enhanced responses with similar levels were not attenuated by AIIA in both groups." | ( Prostaglandins in enhanced pressor response in renal prehypertensive rabbits. Fujie, M; Fujita, H; Ichikawa, S; Kogure, M; Kumakura, H; Murata, K; Nakamura, T; Sato, K; Yagi, A; Yagi, S, 1987) | 0.61 |
"Pretreatment with indomethacin heightened the angiotensin pressor effect significantly in the pregnant group (p = 0.0001) and to a near-significant degree in the nonpregnant group (p = 0.074)." | ( The interaction between serotonin and angiotensin II in the chronically instrumented guinea pig and its alteration by indomethacin. Chestnut, D; Hdez, M; Herrig, J; Wang, JP; Weiner, C, 1987) | 0.81 |
"Treatment with indomethacin (5 mg/kg, intravenous) did not significantly alter either baseline levels of the catecholamines or the levels after 20 min of the asphyxiating gas." | ( Indomethacin does not alter the circulating catecholamine response to asphyxia in the neonatal piglet. Beasley, DG; Busija, DW; Fletcher, AM; Green, RS; Leffler, CW, 1987) | 2.06 |
"Pretreatment with indomethacin (15 mg/kg) prevented the fever occurring in unanesthetized rats immediately after unilateral anodal electrolytic lesions of the medial preoptic area. " | ( Indomethacin pretreatment inhibits fever after anodal, but not cathodal, medial preoptic lesions in rats. Levy, F; Satinoff, E; Szymusiak, R, 1987) | 2.05 |
"Pretreatment with indomethacin partly inhibited the increments in clearances of macromolecules." | ( Intravenously administered frusemide increases glomerular permeability. Ala-Houhala, I; Pasternack, A; Vapaatalo, H, 1987) | 0.6 |
"Pretreatment with indomethacin partly prevented the gastroprotective effects of Solon." | ( Antiulcer and gastroprotective effects of solon, a synthetic flavonoid derivative of sophoradin. Role of endogenous prostaglandins. Aihara, H; Brzozowski, T; Drozdowicz, D; Konturek, SJ; Muramatsu, M; Piastucki, I; Radecki, T; Tanaka, M, 1986) | 0.59 |
"pretreatment with indomethacin (5 mg/kg, s.c.) resulted in no reduction in the protection by NC-1300, excluding the possible participation of endogenous prostaglandins in the protective mechanism." | ( Cytoprotective effects of NC-1300 and omeprazole on Hcl . ethanol-induced gastric lesions in rats. Awane, Y; Miyake, H; Okabe, S, 1986) | 0.59 |
"Pretreatment with indomethacin or dexamethasone did not significantly alter either the preinsult or the postinsult slope." | ( Indomethacin and dexamethasone decrease oleic acid-induced pulmonary protein leak in rabbits. Butler, RR; Spicer, KM, 1986) | 2.04 |
"Treatment with indomethacin, propanolol, and ouabain did not alter the potentiating effect of temperature on contractions to norepinephrine in ground squirrel femoral arteries." | ( Effect of cooling on vascular smooth muscle from the thirteen-lined ground squirrel. Harker, CT; Webb, RC, 1987) | 0.61 |
"Pretreatment with indomethacin (5 mg/kg body wt) abolished the inhibitory effect of 1-84 and 1-34 PTH on the response of MAP to NE and ANG II and the hypotensive action of 1-34 PTH." | ( Effect of PTH on blood pressure and response to vasoconstrictor agonists. Campese, VM; Iseki, K; Massry, SG; Nadler, JL; Saglikes, Y, 1985) | 0.59 |
"Pretreatment with indomethacin (n = 6) or sodium salicylate (n = 4) almost completely blocked this rise in Qbr." | ( Regulation of increase in anastomotic blood flow following pulmonary arterial occlusion. Butler, J; Jindal, SK; Kirk, W; Lakshminarayanan, S, 1985) | 0.59 |
"Pretreatment with indomethacin completely prevented the cytoprotective effect of acetazolamide; this suggests that the cytoprotective effect may be mediated by endogenous release of prostaglandins by the stomach." | ( Ulcer formation and cytoprotection by acetazolamide. Davis, JP; Kolbasa, KP; Lancaster, C; Nezamis, JE; Robert, A, 1985) | 0.59 |
"Treatment with Indomethacin (INDO), 16, 16-dimethyl-PGE2(PGE2) and prostacyclin (PGI2) was assayed in the cultures." | ( Cytoprotective effect of prostaglandins on isolated rat liver cells. Fremont-Smith, M; Guarner, F; Prieto, J, 1985) | 0.61 |
"Pretreatment with indomethacin reduced sleep time in those animals injected with the 40% solution but was without effect in the animals injected with the 20% solution." | ( Indomethacin pretreatment blocks the effects of high concentrations of ethanol. Collins, AC; Gilliam, DM; Miner, LL, ) | 1.9 |
"Pretreatment with indomethacin abolished this response." | ( Effect of castration on prostaglandin-mediated changes in membrane potential and prostaglandin synthesis in guinea-pig seminal vesicle tissue. Carbonaro, C; Gerritsen, ME; Levine, N; Tarlin, N, 1985) | 0.59 |
"Pretreatment with indomethacin (5 X 10(-5) M) or U-51605 (5 micrograms/ml) inhibited the synthesis of these metabolites." | ( Absence of prostacyclin involvement in angiotensin-induced aldosterone secretion in rat adrenal cells. Campbell, WB; Gomez-Sanchez, CE, 1985) | 0.59 |
"Treatment with indomethacin methacin or meclofenamate 5 mg/kg given subcutaneously twice daily for 2 days had no effect on normoxic or hypoxic pulmonary tone." | ( The effects of eicosanoid synthesis inhibitors on normoxic and hypoxic pulmonary vascular tone in dogs. Hughes, JD; Lazar, JD; Rubin, LJ, 1985) | 0.61 |
"Treatment with indomethacin during asphyxia did not alter arterial pressure or cardiac output but decreased cerebral blood flow to the preasphyxiated level and decreased adrenal blood flow about 20%." | ( Effects of indomethacin on cardiac output distribution in normal and asphyxiated piglets. Beasley, DG; Busija, DW; Fletcher, AM; Green, RS; Leffler, CW, 1986) | 1 |
"Pretreatment with indomethacin inhibited the endotoxin-induced impairment in pulmonary gas exchange, but did not prevent pulmonary oedema." | ( Prophylactic and delayed treatment with indomethacin in a porcine model of early adult respiratory distress syndrome induced by endotoxaemia. Borg, T; Gerdin, B; Modig, J, 1986) | 0.86 |
"Treatment with indomethacin gave dramatic relief of pain within 72 hours in all six." | ( Indomethacin therapy for hypertrophic pulmonary osteoarthropathy in patients with bronchogenic carcinoma. Fan, P; Leung, FW; Williams, AJ, 1985) | 2.05 |
"Treatment with indomethacin was followed by significant improvement or normalization of the pressor response to NE in uremic patients." | ( Parathyroid hormone and the altered vascular response to norepinephrine in uremia. Campese, VM; Collins, J; Massry, SG, 1985) | 0.61 |
"Pretreatment with indomethacin abolished uterine contractions except on day 9 of the cycle, when progesterone levels are at their highest." | ( Influence of ovarian steroids on prostaglandin- and leukotriene-induced uterine contractions. Carraher, RP; Demers, LM; Hahn, DW; McGuire, JL, 1985) | 0.59 |
"Pretreatment with indomethacin in a dose of 5 mg/kg/d for 3 d did not change the serum half-life (T1/2), the total body clearance (CL), and the apparent volume of distribution (Vd) of TMO and antipyrine." | ( The effect of indomethacin on hepatic drug-oxidizing capacity in the rat: trimethadione and antipyrine metabolism as an indicator. Aramphongphan, A; Kobayashi, S; Kurata, N; Kuroiwa, Y; Oguchi, K; Tanaka, E; Yasuhara, H, 1985) | 0.95 |
"Treatment with indomethacin, aspirin, or prednisone has been shown to reduce urinary fibrin/fibrinogen degradation products (F.D.P.) in approximately two-thirds of patients with proliferative glomerulonephritis. " | ( Modification by drugs of urinary fibrin/fibrinogen degradation products in glomerulonephritis. Cash, JD; Clarkson, AR; MacDonald, MK; Robson, JS, 1972) | 0.6 |
"When treated with indomethacin, the rat stomach strip and chick rectum preparation slowly relaxed, whether they were bathed in Krebs solution or blood." | ( Prostaglandins, oxygen tension and smooth muscle tone. Eckenfels, A; Vane, JR, 1972) | 0.57 |
The influence of the free radical scavenger 2,4-tetra-O-methyl-furfurylidene-sorbitol (MSF) on the carrageenan-induced hind-paw inflammation in rats is evaluated. The hospital records of patients experiencing any postpartum complication between 1994 and 1999 were reviewed for adverse drug reactions (ADR) attributed to indomethacin.
The relationship between the pharmacokinetic properties and the analgesic effect of indomethacin (IDM) was evaluated on a carrageenin-induced inflammation model in the rat. There was an increase in the mean AUC of indometrichacins in plasma when probenecid was given, but there was no change in the plasma half-life of indometrycin. The pharmacokinetics profile of nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats.
Excerpt | Reference | Relevance |
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" From these observations it is concluded that a specific pharmacokinetic behaviour of acidic NSAID leading to high concentrations in inflamed tissue is a decisive aspect of their anti-inflammatory action." | ( Inhibition of prostaglandin synthesis in vivo by nonsteroid anti-inflammatory drugs: evidence for the importance of pharmacokinetics. Brune, K; Glatt, M; Graf, P, 1976) | 0.26 |
" According to the different elimination mechanisms of the drugs investigated the kinetics was infleunced in different way by the restriction of the renal elimination of these drugs: The half-life periods for the elimination of Metindol, Nevigramon and Mebacid remained unchanged in patients with renal diseases; the half-value period for the elimination of Sulfaclomid was prolonged." | ( [Studies on the pharmacokinetics of Sulfaclomid, Mebacid, Nevigramon and Metindol in patients with reduced kidney function]. Stein, G; Traeger, A, 1978) | 0.26 |
" There was an increase in the mean AUC of indomethacin in plasma from 2,553 +/- 213 hr ng/ml to 4,181 +/- 384 hr ng/ml when probenecid was given, but there was no change in the plasma half-life of indomethacin." | ( The interaction between indomethacin and probenecid. A clinical and pharmacokinetic study. Baber, N; Halliday, L; Littler, T; Orme, ML; Sibeon, R, 1978) | 0.83 |
" The elimination half-life (t1/2 beta) calculated during the washout interval (mean +/- SD) was 47 x 4 +/- 21 x 5 min which is close to that calculated in a reference group of rabbits." | ( Effect of indomethacin on the pharmacokinetics of methotrexate in rabbits. Khan, RM; Morad, AR; Najjar, TA, 1992) | 0.69 |
" It was applied to pharmacokinetic studies of glycyrrhizin in rabbit, after a 2 mg/kg intravenous administration." | ( Determination of glycyrrhizin in rabbit plasma by high-performance liquid chromatography with photodiode-array ultraviolet detection and its pharmacokinetics application. Chen, CF; Tsai, TH, 1992) | 0.28 |
"The steady-state pharmacokinetic profile of indomethacin was examined in twelve healthy volunteers (4 m, 8 f; 20-34 y) and in 12 elderly subjects (7 m, 5 f; 70-88 y)." | ( Steady state pharmacokinetic profile of indomethacin in elderly patients and young volunteers. Crawford, VL; McConnell, JG; McElnay, JC; Passmore, AP; Taylor, IC; Walker, FS, 1992) | 0.81 |
" The overall absorption as shown by the values for area under the concentration curve of indomethacin was unaffected by concurrent administration of misoprostol." | ( Effects of misoprostol on the pharmacokinetics of indomethacin in human volunteers. Hantsbarger, G; Hunt, RH; James, C; Karim, A; Nicholson, PA; Rainsford, KD; Rischke, JA; Smith, M; Stetsko, PI, 1992) | 0.76 |
" The mean area under the indomethacin plasma concentration curve AUC 0-alpha was 10." | ( Lack of effect of paracetamol on the pharmacokinetics of indomethacin and paracetamol in humans. Seideman, P, 1991) | 0.83 |
" The pharmacokinetic profile of indomethacin nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats; no difference in the mean concentration-time profiles of the drug was observed." | ( Jejunal absorption, pharmacological activity, and pharmacokinetic evaluation of indomethacin-loaded poly(d,l-lactide) and poly(isobutyl-cyanoacrylate) nanocapsules in rats. Ammoury, N; Benita, S; Devissaguet, JP; Dubrasquet, M; Fessi, H, 1991) | 0.79 |
" A one-compartment open model was used for pharmacokinetic analysis." | ( Population pharmacokinetics of intravenous indomethacin in neonates with symptomatic patent ductus arteriosus. Brown, Y; Brundage, RC; Gal, PS; Pinson, JB; Purohit, D; Ransom, JL; Schall, S; Weaver, RL; Wiest, DB, 1991) | 0.54 |
" INDO pharmacokinetic parameters varied from dose-to-dose within the same patient, and wide interpatient variability was also observed." | ( Indomethacin pharmacokinetics in neonates: the value of volume of distribution as a marker of permanent patent ductus arteriosus closure. Brown, Y; Carlos, RQ; Gal, P; Ransom, JL; Schall, S; Weaver, RL; Wyble, LE, 1991) | 1.72 |
" We compared a novel indomethacin dosing approach using individual pharmacokinetic and pharmacodynamic information (group A) with a control group from our institution (group B) and a level 3 university-based intensive care nursery (group C) who were dosed using current dosing guidelines." | ( Indomethacin for patent ductus arteriosus closure. Application of serum concentrations and pharmacodynamics to improve response. Bird, A; Brown, Y; Gal, P; Ransom, JL; Schall, S; Weaver, RL, 1990) | 2.04 |
" The plasma half-life of CsA increased with a corresponding decrease in total body clearance." | ( Pharmacokinetic analysis of cyclosporine in adjuvant arthritic rats. D'Souza, MJ; Matthews, HW; Pollock, SH, ) | 0.13 |
"We present pharmacokinetic data of prolonged, intra-arterial indomethacin treatment (i." | ( Pharmacokinetics of intra-arterial indomethacin treatment for patent ductus arteriosus. Pollak, A; Salzer, HR; Salzer-Muhar, U; Vergesslich, KA; Weninger, M, 1989) | 0.8 |
" Our data suggest that 300 mg ranitidine at night improves the gastroduodenal tolerability of both indomethacin and acemetacin without affecting main pharmacokinetic parameters of both antirheumatics." | ( [Ranitidine ameliorates acemetacin and indomethacin-induced changes of the gastroduodenal mucosa, without modifying the pharmacokinetic behavior of both antirheumatic drugs]. Dammann, HG; Langer, M; Leucht, U; Müller, P; Simon, B, 1989) | 0.76 |
"The pharmacokinetic effect of the combined treatment of penicillamine with indomethacin and chloroquine was investigated in patients with rheumatoid arthritis." | ( Pharmacokinetic interactions of penicillamine in rheumatoid arthritis. Lindström, B; Seideman, P, 1989) | 0.51 |
"A pharmacokinetic model with two parallel absorption processes from two fractions has been derived for the percutaneous absorption of indomethacin." | ( A pharmacokinetic model for the percutaneous absorption of indomethacin and the prediction of drug disposition kinetics. Atago, H; Ito, Y; Iwaki, M; Ogiso, T, 1989) | 0.72 |
" Calculated pharmacokinetic parameters were (mean +/- SD); alpha half-life 25." | ( Pharmacokinetics of postoperative intravenous indomethacin in children. Korpela, R; Maunuksela, EL; Olkkola, KT, 1989) | 0.54 |
"The reciprocal effects on pharmacokinetic parameters after a single oral dose of the nonsteroidal antiinflammatory drugs (NSAIDs) indomethacin and sulindac and repeated oral doses of the H2-receptor antagonists cimetidine and ranitidine were determined in two groups of nine healthy subjects each (indomethacin and sulindac groups)." | ( Pharmacokinetic interactions between NSAIDs (indomethacin or sulindac) and H2-receptor antagonists (cimetidine or ranitidine) in human volunteers. Abel, L; Carbon, C; Delhotal-Landes, B; Flouvat, B; Liote, F; Meyer, P; Vinceneux, P, 1988) | 0.74 |
" The pharmacokinetic parameters of felodipine (Cmax, tmax, t1/2 and AUC), the concentration-response curves for blood pressure lowering effects, the reflex tachycardia, diuretic properties and side-effects profile of felodipine were not significantly altered by indomethacin pretreatment in normal volunteers." | ( Effect of indomethacin on the pharmacokinetics and pharmacodynamics of felodipine. Bailey, DG; Bartle, WR; Edgar, B; Hardy, BG; Myers, M, 1988) | 0.86 |
" of indomethacin, it was observed that only the pharmacokinetic parameters which reflected the distribution process exhibited significant circadian variations." | ( Chronopharmacokinetics of indomethacin in rats. Cuisinaud, G; Guissou, P; Legheand, J; Sassard, J, 1987) | 1.13 |
" Although the time necessary to attain Cmax (tmax) for the three drugs tended to increase, only for indomethacin was this increase significant." | ( Single dose pharmacokinetics of ketoprofen, indomethacin, and naproxen taken alone or with sucralfate. Besner, JG; Caillé, G; Du Souich, P; Gervais, P, ) | 0.61 |
"Only recently have the pharmacokinetic characteristics of nonsteroidal anti-inflammatory drugs (NSAIDs) been recognized as decisive factors in understanding the effects and side effects of these drugs." | ( Clinical relevance of nonsteroidal anti-inflammatory drug pharmacokinetics. Brune, K, 1987) | 0.27 |
"Even the most widely used non-steroidal anti-inflammatory drugs (NSAID's) show considerable variations in their pharmacokinetic behaviour in volunteers and moreso in patients." | ( Pharmacokinetic factors as causes of variability in response to non-steroidal anti-inflammatory drugs. Brune, K, 1985) | 0.27 |
" Pharmacokinetic information on both dosage forms is reviewed." | ( Pharmacokinetic overview of indomethacin and sustained-release indomethacin. Yeh, KC, 1985) | 0.56 |
" As judged from several pharmacokinetic parameters, a dose of 150 mg gave significantly smaller values than the higher doses but there was no significant difference between 175 mg and 200 mg in sulindac sulfide and sulfone concentrations." | ( Pharmacokinetics of graded oral doses of sulindac in man. Lamminsivu, U; Männistö, P; Mäntylä, R; Mattila, J; Vuorela, A, 1984) | 0.27 |
" Plasma concentration data showed that peak plasma levels were reduced but the area under the plasma concentration curve was not significantly different between the four treatments." | ( Pharmacokinetics of an osmotically controlled delivery indomethacin preparation in normal volunteers. Bertouch, JV; Brooks, PM; Harrington, B; Maycock, S, ) | 0.38 |
" No pharmacodynamic interaction as assessed by changes in the systolic time intervals QA2 and LVET was found." | ( Pharmacokinetics of digoxin alone and in the presence of indomethacin therapy. Finch, MB; Johnston, GD; Kelly, JG; McDevitt, DG, 1984) | 0.51 |
"The pharmacokinetic profile of indomethacin administered either orally or intravenously in 13 preterm infants with significant patent ductus arteriosus (PDA) is reported." | ( Pharmacokinetics of oral and intravenous indomethacin in preterm infants. Bhat, R; Burns, L; Evans, M; Fisher, E; Hastreiter, A; Ramirez, JL; Vidyasagar, D, 1980) | 0.81 |
" Its metabolic half-life averages 13 hours." | ( Naproxen sodium (Anaprox): pharmacology, pharmacokinetics and drug interactions. Segre, EJ, 1980) | 0.26 |
"The effect of sustained release on the pharmacokinetic profile of indomethacin was examined by comparing to three reference regimens: an intravenous dose, a single 75 mg dose of conventional capsules, and three 25 mg conventional doses given at 4-h intervals." | ( Effect of sustained release on the pharmacokinetic profile of indomethacin in man. Berger, ET; Breault, GO; Lei, BW; McMahon, FG; Yeh, KC, ) | 0.61 |
" These results have important implications in the determination of bioavailability and pharmacokinetic parameters of this drug." | ( High-performance liquid chromatographic assay of indomethacin and its application in pharmacokinetics in healthy volunteers. Cooper, JK; Hawes, EM; McKay, G; Midha, KK, 1982) | 0.52 |
" The mean half-life of elimination (20." | ( Pharmacokinetics of intravenously administered indomethacin in premature infants. Carr, I; Luken, JA; Pildes, RS; Raval, D; Thalji, AA; Yeh, TF, 1980) | 0.52 |
" A possible mechanism of this effect of indomethacin, independent of prostaglandin synthetase inhibition, is a pharmacokinetic drug interaction in which indomethacin affects access of furosemide to its intratubular site of action." | ( Pharmacokinetic-dynamic analysis of the indomethacin-furosemide interaction in man. Brater, DC; Chennavasin, P; Seiwell, R, 1980) | 0.8 |
"A single dose pharmacokinetic study was conducted on two sustained-release formulations (75 mg) of indomethacin (Indocid capsules 'A' and Indogesic tablets 'B')." | ( A pharmacokinetic study on two sustained-release formulations of indomethacin in normal subjects following a single dose administration. Hasan, MM; Muti, HY; Najib, NM, 1994) | 0.74 |
" Drugs characterized by low accumulation indices (AI) showed virtually no change in the 90% confidence interval (CI) of AUC and CMAX upon multiple dosing." | ( Comparison of single and multiple dose pharmacokinetics using clinical bioequivalence data and Monte Carlo simulations. el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1994) | 0.29 |
" We have examined the pharmacokinetic behaviour in polymorphonuclear leucocytes (PMNs) of M1 and of indomethacin after oral administration to rats of Y-23023 and indomethacin, respectively." | ( Pharmacokinetic behaviour in polymorphonuclear leucocytes of N,N-dimethylcarbamoylmethyl alpha,2-dimethyl-5H-[1]benzopyrano[2,3-b]- pyridine-7-acetate (Y-23023), a new prodrug type of anti-inflammatory agent, and indomethacin after oral administrations in Imayoshi, T; Nagamatsu, Y; Shibata, M; Tsuji, A; Yamada, I, 1994) | 0.69 |
" To describe the time course of the plasma indomethacin and IM-OE after intravenous (iv) and oral administrations, a pharmacokinetic model with four compartments was developed." | ( Pharmacokinetics of indomethacin octyl ester (prodrug) and indomethacin produced from the prodrug. Iwaki, M; Kinoshita, T; Ogiso, T; Paku, T; Tanino, T, 1994) | 0.87 |
" The administration of I or S with M significantly blunted sodium excretion on a purely pharmacodynamic basis while the decline in urinary potassium excretion upon addition of I to M related probably to an attenuation of braking phenomenon induced kaliuresis." | ( The effect of nonsteroidal agents (NSAIDs) on the pharmacokinetics and pharmacodynamics of metolazone. Gehr, TW; Kish, C; Ripley, EB; Sica, DA; Wade, J; Wallace, H, 1994) | 0.29 |
" The individual posterior parameter estimates provided by the program are very useful for the detection of covariate relationships in population pharmacokinetic studies." | ( The estimation of population pharmacokinetic parameters using an EM algorithm. Aarons, L, 1993) | 0.29 |
" Pharmacokinetic analysis led to the conclusion that the uptake of nanocapsules by liver macrophages reduces the concentration of the drug by enhancing its total clearance." | ( Influence of poly(DL-lactide) nanocapsules on the biliary clearance and enterohepatic circulation of indomethacin in the rabbit. Bonini, F; Devissaguet, JP; Fawaz, F; Fessi, H; Guyot, M; Lagueny, AM, 1993) | 0.5 |
" A pharmacokinetic profile of indomethacin is shown, and some preliminary pharmacokinetic parameters of indomethacin obtained from one human volunteer are given." | ( Determination of indomethacin, its metabolites and their glucuronides in human plasma and urine by means of direct gradient high-performance liquid chromatographic analysis. Preliminary pharmacokinetics and effect of probenecid. van den Biggelaar-Martea, M; Verwey-van Wissen, CP; Vree, TB, 1993) | 0.91 |
"A Monte Carlo simulation study was done to investigate the effects of high intrasubject variation in clearance (CL), and volume of distribution (V) on the calculation of the 90% confidence interval (CI) for Cmax for single dose and multiple dose studies." | ( Evaluation of bioequivalence of highly variable drugs using Monte Carlo simulations. I. Estimation of rate of absorption for single and multiple dose trials using Cmax. el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1995) | 0.29 |
"Previous reviews and simulations have shown that the probability of failure for the Cmax for single dose studies was always greater than that for multiple dose studies." | ( Evaluation of bioequivalence of highly variable drugs using Monte Carlo simulations. I. Estimation of rate of absorption for single and multiple dose trials using Cmax. el-Tahtawy, AA; Jackson, AJ; Ludden, TM, 1995) | 0.29 |
" The effects of postnatal age and postnatal exposure to indomethacin on the pharmacokinetic parameters of ceftazidime (CAZ) were investigated in 23 preterm infants (gestational age 28." | ( Ceftazidime pharmacokinetics in preterm infants: effect of postnatal age and postnatal exposure to indomethacin. de Groot, R; Hop, WC; Neijens, HJ; Schoemaker, RC; van den Anker, JN; van der Heijden, BJ, 1995) | 0.75 |
"The goal of this study was to look for correlations between the severity of chronic inflammatory joint disease and pharmacokinetic parameters of nonsteroidal antiinflammatory drugs." | ( Influence of severity of chronic inflammatory joint disease on the pharmacokinetics of indomethacin and etodolac. Goasguen, J; Guggenbuhl, P; Jacquelinet, C; Lapicque, F; Le Dantec, P; Netter, P; Pawlotsky, Y; Perdriger, A; Veillard, E, 1996) | 0.52 |
"The objective of the present study was to analyze the pharmacokinetic behavior of vancomycin in neonates of postconceptional age < or = 32 weeks (n = 44)." | ( [Pharmacokinetics of vancomycin in neonates of postconceptional age less than or equal to 32 weeks]. Altirriba Valls, O; Demestre Guasch, X; Farré Riba, R; Ginovart Galiana, G; Lopes Santos, AP; Mangues Bafalluy, MA, 1996) | 0.29 |
"The relationship between the pharmacokinetic properties and the analgesic effect of indomethacin (IDM) was evaluated on a carrageenin-induced inflammation model in the rat." | ( Relationship between pharmacokinetics and the analgesic effect of indomethacin in the rat. Aoki, M; Hanano, M; Shimizu, R; Suganuma, T; Suzuki, T, 1997) | 0.76 |
" Furthermore, the ability of this method to measure IND over a wide concentration range makes it suitable for therapeutic drug monitoring and pharmacokinetic studies." | ( Plasma indomethacin assay using high-performance liquid chromatography-electrospray-tandem mass spectrometry: application to therapeutic drug monitoring and pharmacokinetic studies. Dodds, HM; Hogan, NS; Johnson, AG; Jones, CE; Taylor, PJ, 1998) | 0.76 |
" Thus, the pharmacokinetic data gave a quantitative evidence for high anti-inflammatory potential of lipo-indomethacin." | ( Pharmacodynamic and pharmacokinetic evaluation of lipid microspheres of indomethacin. Diwan, PV; Srinath, P, 1998) | 0.75 |
"010 h-1) and the half-life was long (t1/2 beta = 56." | ( Pharmacokinetics of indomethacin after intraruminal administration to sheep. Ballesteros, C; Encinas, T; Lázaro, R; Rodríguez, C; Ros, JM; San Andrés, MD; Vinagre, E, 1999) | 0.63 |
" The pharmacokinetic behavior of INDO (2 mg/kg) has been studied after intravenous (i." | ( Pharmacokinetics of indomethacin in poultry. Arboix, M; Cristòfol, C; Martí, G; Valladares, JE, ) | 0.45 |
" Pharmacodynamic evaluation of the liposomes was performed by carrageenan-induced rat paw edema (acute) and adjuvant arthritis (chronic) models." | ( Preparation and pharmacodynamic evaluation of liposomes of indomethacin. Diwan, PV; Srinath, P; Vyas, SP, 2000) | 0.55 |
"A physiological pharmacokinetic model describing the absorption and disposition of topically applied drugs was proposed, and the effect of various pharmacokinetic and physiological parameters on the drug delivery into the targeted muscle was simulated." | ( Drug targeting efficacy to underlying muscle following topical application. I. Evaluation based on a physiological pharmacokinetic model. Hatanaka, T; Katayama, K; Koizumi, T; Manabe, E; Mori, M; Ohtsuki, T; Okada, H; Okuyama, K, 2000) | 0.31 |
" For each pharmacokinetic parameter, an analysis of variance was performed to outline the existence of chronobiological variations." | ( Chronobiological variations of indomethacin pharmacokinetic parameters in sheep. Boggio, JC; McKellar, Q; Sánchez, S; Valtorta, SE, 2001) | 0.6 |
"These findings support the hypothesis that the poor PDA closure rates with INDO for neonates >10 days postnatal age are the result of pharmacokinetic differences only and that weight does not impact response rates." | ( Effect of age and birth weight on indomethacin pharmacodynamics in neonates treated for patent ductus arteriosus. Brown, YL; Carlos, RQ; Davey, AM; Dimaguila, MA; Gal, P; Ransom, JL; Schall, SA; Shaffer, CL; Smith, MS, 2002) | 0.59 |
" Non-availability of the parenteral preparation and lack of information regarding the pharmacokinetic disposition of indomethacin in the premature infants in north Indian population led us to conduct this pharmacokinetic study with oral indomethacin." | ( A preliminary study on pharmacokinetics of oral indomethacin in premature infants in north India. Garg, SK; Narang, A; Sharma, PK, 2003) | 0.78 |
"0 ng/ml), elimination half-life (t1/2 el; 21." | ( A preliminary study on pharmacokinetics of oral indomethacin in premature infants in north India. Garg, SK; Narang, A; Sharma, PK, 2003) | 0.57 |
" These preliminary results may be of use in designing future pharmacokinetic studies of oral indomethacin in preterm neonates on a larger sample." | ( A preliminary study on pharmacokinetics of oral indomethacin in premature infants in north India. Garg, SK; Narang, A; Sharma, PK, 2003) | 0.79 |
" Population analysis of the 185 plasma concentrations obtained was conducted using NONMEM and pharmacokinetic and demographic differences between responders and nonresponders were compared." | ( Intravenous indometacin in preterm infants with symptomatic patent ductus arteriosus. A population pharmacokinetic study. Collier, PS; Darwish, M; Halliday, HL; McElnay, JC; Millership, JS; Petersen, S; Smyth, JM, 2004) | 0.32 |
" Although the pharmacokinetic estimates will be affected by both interindividual and within-individual variation, it is anticipated that this approach will decrease the variability of exposure and optimize treatment outcome." | ( Intravenous indometacin in preterm infants with symptomatic patent ductus arteriosus. A population pharmacokinetic study. Collier, PS; Darwish, M; Halliday, HL; McElnay, JC; Millership, JS; Petersen, S; Smyth, JM, 2004) | 0.32 |
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data." | ( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. Jolivette, LJ; Ward, KW, 2005) | 0.33 |
" To investigate pharmacokinetic characteristics of IMC in rats, the IMC concentration in plasma was analyzed using a high-performance liquid chromatography system after intravenous bolus injection of free IMC and IMC-loaded ML50 nanospheres." | ( Indomethacin-loaded methoxy poly(ethylene glycol)/poly(D,L-lactide) amphiphilic diblock copolymeric nanospheres: pharmacokinetic and toxicity studies in rodents. Kang, JS; Kim, SY; Lee, YM, 2005) | 1.77 |
" In study 2, 90% confidence intervals for febuxostat C(max) and AUC extended above that range, with increases of 28% and 40% in Cmax and AUC24, respectively." | ( Pharmacokinetic interactions of concomitant administration of febuxostat and NSAIDs. Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006) | 0.33 |
"To evaluate whether the concomitant administration of ibuprofen or indomethacin plus amikacin may alter the latter drug s pharmacokinetic parameters, and hence amikacin plasma levels." | ( [Effect of the concomitant administration of indomethacin or ibuprofen on amikacin pharmacokinetics in premature newborns]. Cuesta Grueso, C; Gimeno Navarro, A; Marqués Miñana, MR; Morcillo Sopena, F; Peris Ribera, JE; Poveda Andrés, JL, ) | 0.63 |
" Pharmacokinetic parameters, distribution volume, and amikacin clearance were measured using the PKS program (a non-linear regression method)." | ( [Effect of the concomitant administration of indomethacin or ibuprofen on amikacin pharmacokinetics in premature newborns]. Cuesta Grueso, C; Gimeno Navarro, A; Marqués Miñana, MR; Morcillo Sopena, F; Peris Ribera, JE; Poveda Andrés, JL, ) | 0.39 |
" No statistically significant differences were found among pharmacokinetic parameters corresponding to each study group." | ( [Effect of the concomitant administration of indomethacin or ibuprofen on amikacin pharmacokinetics in premature newborns]. Cuesta Grueso, C; Gimeno Navarro, A; Marqués Miñana, MR; Morcillo Sopena, F; Peris Ribera, JE; Poveda Andrés, JL, ) | 0.39 |
" Observations collected in two population pharmacokinetic studies, in preterm neonates, investigating amikacin and vancomycin were used to estimate: i) the impact of ibuprofen administration on the clearance of these drugs; and ii) the difference between prophylactic and therapeutic administration of ibuprofen on this clearance." | ( Impact of ibuprofen administration on renal drug clearance in the first weeks of life. Allegaert, K; Anderson, BJ; Rayyan, M, 2006) | 0.33 |
" Pharmacokinetic study in beagle dogs showed that fastest absorption with the smallest Tmax and Tlag was observed for uncoated pellets." | ( In vitro evaluation and pharmacokinetics in dogs of guar gum and Eudragit FS30D-coated colon-targeted pellets of indomethacin. Ji, C; Wu, W; Xu, H, 2007) | 0.55 |
" Pharmacokinetic study in dogs gave Tmax/Cmax of 4h/604 ng/ml and 3h/1662 ng/ml for HPMC/pectin/calcium and HPMC/pectin tablet, respectively." | ( Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: II. Influencing variables, stability and pharmacokinetics in dogs. Deng, D; Lu, Y; Wu, B; Wu, W, 2008) | 0.67 |
"A population pharmacokinetic model was developed after administration of orogastric and/or intravenous indomethacin for the treatment of patent ductus arteriosus in preterm infants." | ( Orogastric and intravenous indomethacin administration to very premature neonates with patent ductus arteriosus: population pharmacokinetics, absolute bioavailability, and treatment outcome. Al Za'abi, M; Charles, B; Collie, LA; Donovan, T; Tudehope, D; Woodgate, P, 2007) | 0.85 |
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
" Furthermore, the terminal half-life predictions for all three compounds were within 2-fold of the observed values." | ( Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes. Gardiner, P; Paine, SW; Parker, AJ; Riley, RJ; Webborn, PJ, 2008) | 0.58 |
" This pharmacodynamic phenomenon is referred to in the present work as "teleantagonism"." | ( Teleantagonism: A pharmacodynamic property of the primary nociceptive neuron. Cunha, FQ; Duarte, DB; Ferrari, LF; Ferreira, SH; Funez, MI; Lorenzetti, BB; Parada, CA; Sachs, D, 2008) | 0.35 |
"Methods used included the in-vitro inhibition of cyclooxygenase-1 and -2, in-vivo evaluation of anti-inflammatory activity by air pouch and peritonitis models and the pharmacokinetic profile after intravenous (3 mg/kg) and oral (3 and 6 mg/kg) dosing to rats." | ( Preclinical pharmacokinetic and pharmacodynamic evaluation of thiazolidinone PG15: an anti-inflammatory candidate. da Silva, TG; Dalla Costa, T; de Lima, Mdo C; Galdino, SL; Pitta, Ida R; Uchôa, Fde T, 2009) | 0.35 |
"Preterm and term newborn infants show wide interindividual variability (IIV) in pharmacokinetic parameters of gentamicin." | ( Developmental pharmacokinetics of gentamicin in preterm and term neonates: population modelling of a prospective study. Ewald, U; Friberg, LE; Honoré, PH; Nielsen, EI; Sandström, M, 2009) | 0.35 |
" Population pharmacokinetic modelling was performed using nonlinear mixed-effects modelling (NONMEM) software." | ( Developmental pharmacokinetics of gentamicin in preterm and term neonates: population modelling of a prospective study. Ewald, U; Friberg, LE; Honoré, PH; Nielsen, EI; Sandström, M, 2009) | 0.35 |
" Pharmacokinetic alterations, as liver damage, are reversible, but do not require complete liver regeneration to return to basal conditions." | ( Pharmacokinetics of acemetacin and its active metabolite indomethacin in rats during acute hepatic damage and liver regeneration. Castañeda-Hernández, G; Chávez-Piña, AE; Favari, L, ) | 0.38 |
"Observations collected in two population pharmacokinetic studies in preterm neonates investigating amikacin and vancomycin disposition were used to estimate (i) the impact of ibuprofen administration and (ii) the difference between ibuprofen and indomethacin on renal drug clearance." | ( The impact of ibuprofen or indomethacin on renal drug clearance in neonates. Allegaert, K, 2009) | 0.83 |
" In a vancomycin pooled pharmacokinetic study, it was documented that the impact of indomethacin was significantly higher compared to ibuprofen (46 and 28%, respectively)." | ( The impact of ibuprofen or indomethacin on renal drug clearance in neonates. Allegaert, K, 2009) | 0.87 |
" Pharmacokinetic (PK) parameters along with liver and muscle tissue levels were collected, and their contributions to total V(ss) were calculated." | ( The impact of hepatic uptake on the pharmacokinetics of organic anions. Gardiner, P; Paine, SW, 2011) | 0.37 |
" Indomethacin ocular levels were measured by liquid chromatography mass spectrometry (LC-MS/MS), and the pharmacokinetic parameters--peak drug concentration (C(max)), time to peak value (T(max)), and area under the concentration-time curve between 0 and 240 min (AUC(0-240))--were determined." | ( Ocular pharmacokinetics profile of different indomethacin topical formulations. Bucolo, C; Drago, F; Melilli, B; Piazza, C; Zurria, M, 2011) | 1.54 |
"IND-HPMC treatment demonstrates a nonclinical ocular pharmacokinetic profile of indomethacin characterized by higher concentrations of drug in ocular tissues (4." | ( Ocular pharmacokinetics profile of different indomethacin topical formulations. Bucolo, C; Drago, F; Melilli, B; Piazza, C; Zurria, M, 2011) | 0.86 |
" The development of NSAIDs having safer therapeutic profile depends on the better understanding of their mechanisms, physicochemical and pharmacokinetic properties." | ( Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach. Kumar, M; Sinha, VR; Thareja, S, 2012) | 0.38 |
" This phase 1 clinical study characterizes the pharmacokinetic (PK) profile of an investigational, proprietary, nano-formulated, lower-dose oral indomethacin (nano-formulated indomethacin) compared with standard oral indomethacin in healthy subjects." | ( A phase I study evaluating the pharmacokinetic profile of a novel, proprietary, nano-formulated, lower-dose oral indomethacin. Altman, R; Daniels, S; Manvelian, G, 2012) | 0.79 |
" Pharmacokinetic parameters, including maximum measured plasma concentration (C(max)), time to maximum measured concentration (T(max)), elimination half-life (T(1/2)), and area under the concentration-time (AUC) curve, along with safety and tolerability, were assessed." | ( A phase I study evaluating the pharmacokinetic profile of a novel, proprietary, nano-formulated, lower-dose oral indomethacin. Altman, R; Daniels, S; Manvelian, G, 2012) | 0.59 |
"There was a more rapid mean (± standard deviation) Tmax for nano-formulated indomethacin 20 mg (1." | ( A phase I study evaluating the pharmacokinetic profile of a novel, proprietary, nano-formulated, lower-dose oral indomethacin. Altman, R; Daniels, S; Manvelian, G, 2012) | 0.82 |
" Method validation and pharmacokinetic study plasma analysis were performed as per FDA guidelines and the results met the acceptance criteria." | ( Development and validation of a liquid chromatography-tandem mass spectrometry method for quantitation of indomethacin in rat plasma and its application to a pharmacokinetic study in rats. Dixit, A; Giri, S; Mullangi, R; Rajagopal, S; Suresh, PS, 2013) | 0.6 |
" Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h." | ( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics. Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014) | 0.63 |
" The mean pharmacokinetic parameters of AC and IND from different formulations indicated increased t 1/2 and area under the curve (AUC) of both AC and IND for proniosomal tablets compared with both proniosomal powders and AC plain tablets." | ( Proniosomal oral tablets for controlled delivery and enhanced pharmacokinetic properties of acemetacin. Abdallah, MH; Ibrahim, MM; Shehata, TM, 2015) | 0.42 |
" Pharmacokinetic parameters and safety were assessed." | ( Pharmacokinetics and safety of low-dose submicron indomethacin 20 and 40 mg compared with indomethacin 50 mg. Olugemo, K; Sheridan, C; Solorio, D; Young, CL, 2015) | 0.67 |
"Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
"As numerous herbal products have been used as dietary supplements or functional foods, the demands of the pharmacokinetic and pharmacodynamic characteristics of active compounds are increasing in order to secure a consistent outcome (i." | ( In vivo gastroprotective effect along with pharmacokinetics, tissue distribution and metabolism of isoliquiritigenin in mice. Chae, HS; Chin, YW; Choi, YH; Kim, YJ, 2015) | 0.42 |
" Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) to investigate interactions of lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin." | ( Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and Commonly Used Drugs for Gout Treatment. Bucci, G; Gillen, M; Kerr, B; Lee, C; Shen, Z; Tieu, K; Wilson, D, 2017) | 0.63 |
"To determine the role of a pharmacokinetic interaction in the protective effect of curcumin against the gastric damage induced by indomethacin administration as such or as its prodrug acemetacin." | ( Evidence against the participation of a pharmacokinetic interaction in the protective effect of single-dose curcumin against gastrointestinal damage induced by indomethacin in rats. Castañeda-Hernández, G; Chávez-Piña, AE; Cruz-Antonio, L; Estela Díaz-Triste, N; Medina-Aymerich, L; Zazueta-Beltrán, L, 2017) | 0.86 |
" Data thus suggest that a pharmacokinetic mechanism of action is not involved in curcumin gastroprotection." | ( Evidence against the participation of a pharmacokinetic interaction in the protective effect of single-dose curcumin against gastrointestinal damage induced by indomethacin in rats. Castañeda-Hernández, G; Chávez-Piña, AE; Cruz-Antonio, L; Estela Díaz-Triste, N; Medina-Aymerich, L; Zazueta-Beltrán, L, 2017) | 0.65 |
" Pretreatment of the rats with thylakoid-rich spinach extract (100 or 300 mg/kg) for 15 min prior to oral administration of GF (50 mg/kg) or IM (10 mg/kg) did not significantly alter the pharmacokinetic properties of either drug." | ( Effects of Thylakoid-Rich Spinach Extract on the Pharmacokinetics of Drugs in Rats. Katoh, M; Nadai, M; Saito, Y; Usami, T, 2019) | 0.51 |
" In this paper, the antineoplastic effect of indomethacin and its pharmacokinetic effect were analysed." | ( Pharmacokinetics-based analysis of indomethacin's anti-tumor effect and drug efficacy. Jingjing, G; Jun, Z; Ke, L; Yan, Z; Zhu, Z, 2020) | 1.09 |
" In this study, we report the findings from pharmacokinetic (PK) analyses undertaken with an LNG-IUS (LNG-IUS 8) modified with an additional reservoir containing indomethacin (IND)." | ( Development of an Intrauterine Device Releasing Both Indomethacin and Levonorgestrel During the First Months of Use: Pharmacokinetic Characterization in Healthy Women. Ahola, M; Fels, LM; Hofmann, BM; Klein, S; Lindenthal, B; Pihlaja, J, 2023) | 1.36 |
Low-dose indomethacin combined with methylprednisolone may be a new choice for AFOP treatment.
Indomethacin bioavailability after oral administration of its precursor, acemetacin, is significantly reduced by acute hepatitis produced by CCl4.
Excerpt | Reference | Relevance |
---|---|---|
" Also the absorption rate was higher in fasting individuals." | ( Comparative bioavailability: influence of various diets on the bioavailability of indomethacin. Leopold, G; Netter, KJ; Nowak, H; Wallusch, WW, 1978) | 0.48 |
" The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays." | ( Flumizole, a new nonsteroidal anti-inflammatory agent. Bettis, JW; McIlhenny, HM; Wiseman, EH, 1975) | 0.25 |
"The biovailability of indomethacin from two indomethacin-antacid (aluminum hydroxide magnesium carbonate and magnesium hydroxide) combinations was compared with the bioavailability of oral indomethacin." | ( The effect of an antacid on the bioavailability of indomethacin. Galeazzi, RL, 1977) | 0.82 |
" Indomethacin was rapidly and well absorbed after oral dosing with peak plasma concentrations within 2 hr." | ( Pharmacokinetics of indomethacin. Alván, G; Bertilsson, L; Ekstrand, R; Orme, M; Palmér, L, 1975) | 1.49 |
" The absorption rate from alginate dispersions was enhanced in comparison with that from indomethacin alone, and enhanced only the rate of bioavailability in beagle dogs and volunteers." | ( Improvement of absorption rate of indomethacin and reduction of stomach irritation by alginate dispersions. Imai, T; Iwaoka, D; Otagiri, M; Shiraishi, S, 1991) | 0.78 |
" The result of this study also showed that the concurrent use of the CLO does not affect the bioavailability and anti-inflammatory activity of indomethacin while it inhibits the ulcerogenic effect of indomethacin in a dose dependent manner." | ( Cod liver oil inhibits indomethacin induced gastropathy without affecting its bioavailability and pharmacological activity. al-Meshal, MA; Lutfi, KM; Tariq, M, 1991) | 0.79 |
"The relationship between gastric acidity and the bioavailability of two kinds of sustained-release indomethacin (IM) formulations was investigated in gastric acidity-controlled beagle dogs, and compared with that of rapid-release IM formulations." | ( Gastric acidity-dependent bioavailability of commercial sustained release preparations of indomethacin, evaluated by gastric acidity-controlled beagle dogs. Goda, T; Kawata, M; Ogawa, K; Shiotuki, T; Yamada, I, 1990) | 0.72 |
" Serum indomethacin levels confirmed that indomethacin was well absorbed transperitoneally." | ( Indomethacin does not impair cellular potassium uptake in the rat. Akrawi, A; Spital, A, 1990) | 2.18 |
" The bioavailability of indomethacin in the three groups does not differ significantly." | ( Protective effect of rioprostil on indomethacin-induced lesions of gastric and duodenal mucosa in healthy volunteers. Gerova, Z; Kirkov, V; Popov, P; Vlahov, V, 1989) | 0.86 |
" Oral administration of the gel formulation did not result in any gastric ulceration and improved the bioavailability of indomethacin to 115." | ( Influence of indomethacin amphoteric gel on gastric ulcerogenicity and absorption of indomethacin in rats. Dent, J; Eickhoff, WM; Liversidge, GG, 1989) | 0.85 |
" It was clarified that indomethacin was absorbed via both pathways, with rapid and slow absorption rate constants at the initial time stage, and via the latter pathway at the later period." | ( A pharmacokinetic model for the percutaneous absorption of indomethacin and the prediction of drug disposition kinetics. Atago, H; Ito, Y; Iwaki, M; Ogiso, T, 1989) | 0.83 |
" The percutaneous absorption rate of ID from 1 or 3% CL-PG test solution through the intact skin of rats was observed to be faster than that from the control solution (without CL)." | ( Enhancing effect of cetyl lactate on the percutaneous absorption of indomethacin in rats. Dohi, M; Hara, H; Kaiho, F; Kato, Y; Koike, R; Maruoka, K; Nomura, H, 1989) | 0.51 |
" Following intragastric administration, the oral bioavailability of indomethacin in solution was 90%--indicating complete absorption of this drug from the gastrointestinal tract of the rat." | ( Pharmacokinetic evaluation of indomethacin nanocapsules. Andrieu, V; Benita, S; Devissaguet, JP; Dubrasquet, M; Fessi, H; Puisieux, F, 1989) | 0.8 |
" A preliminary bioavailability study of two of the lead structures is presented." | ( Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents. Blythin, DJ; Bober, LA; Chiu, PJ; Conn, DJ; Domalski, MS; Kaminski, JJ; Solomon, DM; Spitler, J; Verbiar, LL; Wong, SC, 1986) | 0.27 |
"The bioavailability of a new controlled release formulation of indomethacin lysine salt in tablets was tested in 6 healthy humans against a conventional indomethacin lysinate formulation in capsules." | ( Bioavailability of indomethacin from a modified release system containing indomethacin as the lysine salt. Arrigoni Martelli, E; Colombo, P; Conte, U; La Manna, A; Marzo, A; Reiner, A, 1987) | 0.84 |
" From the above results, it was concluded that this in situ experimental model of rectal absorption has advantages in that it can be used directly to measure the rectal absorption rate and to determine ratios of easily metabolized and poorly absorbed drugs." | ( An in situ experimental model in rabbits for the study of rectal absorption. Hiura, M; Kasama, T; Mayuzumi, K; Minato, M; Minohara, K; Nakai, M; Ohshiro, K; Sakaguchi, Y, 1986) | 0.27 |
" Sucralfate decreased significantly the rate of absorption (ka) of naproxen and indomethacin, but not that of ketoprofen; it had no significant effect on the elimination half-life and area under the plasma concentration as a function of time curves (AUC0----infinity) of the three drugs." | ( Single dose pharmacokinetics of ketoprofen, indomethacin, and naproxen taken alone or with sucralfate. Besner, JG; Caillé, G; Du Souich, P; Gervais, P, ) | 0.62 |
" An evaluation of the response-related pharmacokinetics of the three most widely used NSAIDs, diclofenac, indomethacin, and piroxicam, shows some obvious reasons for these differences: The onset of absorption and the bioavailability of diclofenac can vary considerably, and relevant inter-patient differences are found in the terminal plasma half-life of indomethacin and piroxicam." | ( Clinical relevance of nonsteroidal anti-inflammatory drug pharmacokinetics. Brune, K, 1987) | 0.49 |
" Bioavailability (AUC's between applications) was not significantly different." | ( [Retard effect of acemetacin from a commercial preparation--kinetics in humans following single and multiple administration]. Beckermann, B; Dell, HD; Doersing, M; Fischer, W; Kamp, R; Schierstedt, D; Weber, J, 1986) | 0.27 |
"Indomethacin bioavailability was compared in 22 healthy men who received two tablet dosage formulations and a capsule formulation of indomethacin in a three-way crossover study." | ( Bioavailability of indomethacin tablets in men volunteers. Dunn, JM; Groth, PE, 1986) | 2.04 |
" An evaluation of the response-related pharmacokinetic parameters of the three presently most widely used NSAID's, namely diclofenac, indomethacin and piroxicam shows some obvious reasons: While the onset of absorption and the bioavailability of diclofenac varies considerably, we find relevant differences in the terminal plasma half-life of indomethacin and particularly piroxicam." | ( Pharmacokinetic factors as causes of variability in response to non-steroidal anti-inflammatory drugs. Brune, K, 1985) | 0.47 |
" Azapropazone has been found to be well absorbed, and benoxaprofen and fenclofenac somewhat more slowly, so for the latter two drugs their low rate of absorption might also be a factor in their reduced ulcerogenicity." | ( Structural damage and changes in eicosanoid metabolites in the gastric mucosa of rats and pigs induced by anti-inflammatory drugs of varying ulcerogenicity. Rainsford, KD, 1986) | 0.27 |
" The bioavailabilities of the products increased in proportion to their in vitro dissolution rates, although one of the commercial products provided a relatively lower bioavailability than was expected." | ( Bioavailability of indomethacin capsules in humans. (I): Bioavailability and effects of gastric acidity. Aoyagi, N; Ejima, A; Kaniwa, N; Ogata, H, 1985) | 0.6 |
"The correlation between the dissolution rate and bioavailability in humans for five indomethacin capsules was investigated." | ( Bioavailability of indomethacin capsules in humans (II): correlation with dissolution rate. Aoyagi, N; Ejima, A; Kaniwa, N; Ogata, H, 1985) | 0.82 |
" The difference in bioavailability between two commercial products was smaller in dogs than in humans, which seemed to be due to strong disintegration forces in dogs." | ( Bioavailability of indomethacin capsules in humans (III): Correlation with bioavailability in beagle dogs. Amada, I; Aoyagi, N; Ejima, A; Fujita, T; Kaniwa, N; Nakata, H; Ogata, H; Tsutsumi, J, 1985) | 0.6 |
" The bioavailability after the two rectal forms was found to be almost the same, about 80%." | ( Bioavailability of indomethacin after intramuscular injection and rectal administration of solution and suppositories. Grenabo, L; Jensen, KM, 1985) | 0.6 |
" Phenylbutazone, aspirin and indomethacin were all well absorbed after oral administration, and the resultant plasma drug concentrations were closely similar to those produced when the drugs were administered intraperitoneally." | ( Factors influencing the inhibitory action of anti-inflammatory drugs on carrageenin induced oedema. Green, AY; Green, D; Murray, PA; Wilson, AB, 1971) | 0.54 |
" In vivo plasma level studies showed no difference in bioavailability between different microcapsule formulations or a conventional indomethacin capsule." | ( Comparison of the in vitro dissolution behaviour of various indomethacin formulations with their in vivo bioavailability. Carless, JE; Rowe, JS, 1981) | 0.71 |
"The permeability of phenolsulfonphthalein(phenol red), a poorly absorbed drug, was examined as an index of an assessment of gastrointestinal mucosal damage in-vivo." | ( An assessment of indomethacin-induced gastrointestinal mucosal damage in-vivo: enhancement of urinary recovery after oral administration of phenolsulfonphthalein in rats. Heya, T; Kimura, T; Nakamura, J; Ohtsuka, N; Sezaki, H; Takada, S; Yamamoto, A, 1983) | 0.61 |
" Enterohepatic cycling makes interpretation of bioavailability estimates of indomethacin dosage forms difficult." | ( Evaluation of new indomethacin dosage forms. Waller, ES, ) | 0.69 |
"Studies were performed in fasted rats to establish if the propensity of 4 non-steroidal anti-inflammatory (NSAI) drugs to elicit varying degrees of gastric mucosal damage following oral administration is related to their rate of absorption by the mucosal and subsequent inhibitory effects on prostaglandin (PG) production in vivo." | ( Comparative effects of some non-steroidal anti-inflammatory drugs on the ultrastructural integrity and prostaglandin levels in the rat gastric mucosa: relationship to drug uptake. Fox, SA; Osborne, DJ; Rainsford, KD, 1984) | 0.27 |
"A concomitant meal did not affect the extent of bioavailability of indomethacin from a multiple-units controlled-release capsule formulation containing enteric-coated pellets, but the presence of food delayed absorption." | ( The influence of food and repeated dosing on the bioavailability of indomethacin from a multiple-units controlled-release formulation. Bechgaard, H; Brodie, RR; Chasseaud, LF; Hunter, JO; Sharman, JM; Skinhøj, A; Taylor, T, 1984) | 0.74 |
"To clarify the mechanism of enhanced absorption of indomethacin (IND) when dosed with magnesium silicate, reported previously, magnesium (IND-Mg) and calcium (IND-Ca) salts of IND were prepared, and the bioavailability in rat and physical properties of these salts were studied in comparison with IND." | ( Bioavailability of indomethacin calcium and magnesium, and effect of the salts on drug metabolizing enzyme activities in rats. Iwaki, M; Ogiso, T; Tamaki, E, 1983) | 0.85 |
" The bioavailability and functionality of 'Osmosin' have been studied after single-dose and after repeated administrations in man." | ( Biopharmaceutical evaluation of 'Osmosin'. Rogers, JD, 1983) | 0.27 |
" These results show that the bioavailability of the CR and conventional indomethacin formulations under these multiple-dose conditions was not significantly different." | ( Comparative multiple dose kinetics of two formulations of indomethacin. Cook, T; De Schepper, PJ; Derouwaux, C; Hwang, S; Kramp, R; Mullie, A; Tjandramaga, TB; Verbesselt, R, 1983) | 0.74 |
" Bioavailability of the oral dosage based on AUC was 13% but no difference was observed in the plasma protein binding or distribution volume of drug as compared to adult values." | ( Pharmacokinetics of oral and intravenous indomethacin in preterm infants. Bhat, R; Burns, L; Evans, M; Fisher, E; Hastreiter, A; Ramirez, JL; Vidyasagar, D, 1980) | 0.53 |
"Two multiple-units controlled-release indomethacin capsule formulations containing enteric-coated pellets were bioequivalent to a standard capsule formulation (taken as the reference) in respect of extent of bioavailability in a crossover study with normal human subjects." | ( Bioavailability of indomethacin from two multiple-units controlled-release formulations. Bechgaard, H; Brodie, RR; Chasseaud, LF; Houmøller, P; Hunter, JO; Siklos, P; Taylor, T, 1982) | 0.86 |
" Flurbiprofen did not seem to alter the bioavailability of the chemotherapeutic agents." | ( Increased survival of cancer-bearing mice treated with inhibitors of prostaglandin synthesis alone or with chemotherapy. Bennett, A; Berstock, DA; Carroll, MA, 1982) | 0.26 |
"This investigation was designed to determine the in vitro release of indomethacin from suppository bases and the in vivo bioavailability in rabbits." | ( Medicament release from suppository bases I: Physicochemical characteristics and bioavailability of indomethacin in rabbits. Bohidar, NR; Plakogiannis, FM; Reid, VE; Vidras, NJ, 1982) | 0.72 |
" These results have important implications in the determination of bioavailability and pharmacokinetic parameters of this drug." | ( High-performance liquid chromatographic assay of indomethacin and its application in pharmacokinetics in healthy volunteers. Cooper, JK; Hawes, EM; McKay, G; Midha, KK, 1982) | 0.52 |
" The intestinal absorption rate constant of IND determined by in situ method was decreased after the multiple dosing of IND alone, but the constant was recovered to the control value after coadministration of the antacid." | ( Disposition, intestinal absorption and drug metabolizing enzyme activities after multiple doses of indomethacin in rat and effect of antacid and dicyclomine on the parameters. Iwaki, M; Ogiso, T; Tamaki, E, 1982) | 0.48 |
"l-1, resulting in a mean relative bioavailability of nimodipine of 111% with a 90%-confidence interval of 96-128% for the combined medication." | ( Steady-state pharmacokinetics of nimodipine during chronic administration of indometacin in elderly healthy volunteers. Breuel, HP; Heine, PR; Horkulak, J; Mück, W; Niklaus, H; Schmage, N, 1995) | 0.29 |
"Piroxicam-beta-cyclodextrin (PBC), a complex of piroxicam with beta-cyclodextrin, was developed with the aim of improving the hydrosolubility and bioavailability of piroxicam." | ( Effects of piroxicam-beta-cyclodextrin on the gastrointestinal tract. Warrington, S, 1993) | 0.29 |
" The great bioavailability was also shown by the high indomethacin level of the aqueous humor after instillation Indosol eye-drops." | ( [Indosol--a nonsteroidal anti-inflammatory drug with therapeutic efficacy]. Bögi, J; Farkas, A; Imre, G; Kahánné, LI; Tüdös, FH, 1994) | 0.54 |
" The absorption rate of IMC was lower and more prolonged after administration of beads containing IMC than IMC powder alone." | ( Controlled-release preparation of indomethacin using calcium alginate gel. Imai, T; Otagiri, M; Shiraishi, S, 1993) | 0.57 |
" These results suggested that the bioavailability of IND was increased by olive oil, fatty acid, and tristearin as absorbefacient agents." | ( Pharmacological and pharmaceutical properties of freeze-dried formulations of egg albumin, indomethacin, olive oil, or fatty acids. Kakegawa, H; Matsumoto, H; Miyataka, H; Satoh, T; Tsuji, Y, 1993) | 0.51 |
"To confirm the increased bioavailability of indomethacin (IND) when incorporated in a preparation with egg albumin and olive oil, we studied the detailed pharmaceutical characteristics of a ternary formulation consisting of egg albumin, IND and olive oil." | ( Pharmacological and pharmaceutical properties of freeze-dried formulations of egg albumin, indomethacin, olive oil, or fatty acids. II. Kakegawa, H; Matsumoto, H; Miyataka, H; Satoh, T; Tsuji, Y, 1993) | 0.77 |
" It is suggested that interindividual differences in dosage and timing to abolish the headaches may be due to different bioavailability or individual sensitivity." | ( Chronic paroxysmal hemicrania and hemicrania continua. Interval between indomethacin administration and response. Pareja, J; Sjaastad, O, 1996) | 0.53 |
"To compare the bioavailability and pupillary effect of flurbiprofen and indomethacin during phacoemulsification and intraocular lens implantation." | ( Intraocular availability and pupillary effect of flurbiprofen and indomethacin during cataract surgery. Cheetham, JK; DeGryse, R; Garcia, CG; Gimbel, H; Van Westenbrugge, J, 1996) | 0.76 |
" Again, due to the small number of subjects entered in the study (insufficient for a real bioequivalence study) equivalence could not be accepted in terms of extent and rate of absorption based on the decision procedures involving the 90% confidence interval and the two one-sided t-tests." | ( In vivo evaluation of an indomethacin monolithic, extended zero-order release hard-gelatin capsule formulation based on saturated polyglycolysed glycerides. Aiache, JM; Beyssac, E; Buri, P; Doelker, E; Duchaix, G; Vial-Bernasconi, AC, 1995) | 0.59 |
" CL316243 did not affect either indomethacin bioavailability or the inhibition of prostaglandin E2." | ( The beta 3-adrenoceptor agonist CL316243 prevents indomethacin-induced jejunal ulceration in the rat by reversing early villous shortening. Anthony, A; Bahl, AK; Dhillon, AP; Oakley, IG; Piasecki, C; Pounder, RE; Spraggs, CF; Trevethick, MA; Wakefield, AJ, 1996) | 0.83 |
"We wished to determine whether enhanced bioavailability of bradykinin (BK) and vasodilatory prostaglandins contribute to renovascular and sodium-handling effects of angiotensin-converting enzyme (ACE) inhibition after myocardial infarction (MI)." | ( Relative contribution of angiotensin II, bradykinin, and prostaglandins to the renal effects of converting enzyme inhibition in rats after chronic myocardial infarction. Deck, CC; Gaballa, MA; Raya, TE, 1996) | 0.29 |
" The plasma levels of IM after the oral administration of IM-OE and IM-BE were comparatively low compared with those after IM, with a small bioavailability (2." | ( Pharmacokinetics of indomethacin ester prodrugs: gastrointestinal and hepatic toxicity and the hydrolytic capacity of various tissues in rats. Iwaki, M; Muraoka, O; Nagai, T; Ogiso, T; Tanabe, G; Tanino, T; Ueda, Y, 1996) | 0.62 |
"The ability of different drug carriers to improve the ocular bioavailability of drugs was investigated in the rabbit eye." | ( Improved ocular bioavailability of indomethacin by novel ocular drug carriers. Alonso, MJ; Calvo, P; Robinson, JR; Vila-Jato, JL, 1996) | 0.57 |
"Representative nonsteroidal anti-inflammatory drug (NSAID) cyclooxygenase inhibitors such as ibuprofen, naproxen, and indomethacin were used as orally bioavailable scaffolds to design selective 5-lipoxygenase (5-LO) inhibitors." | ( Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. Bell, RL; Bouska, J; Brooks, CD; Carter, GW; Dellaria, JF; Hulkower, KI; Kolasa, T; Rodriques, KE; Summers, JB, 1997) | 0.51 |
" The effect of 20 ml of Riopan, given 1 h after oral administration of Indocid capsules (MSD, 25 mg) to fed dogs, on the bioavailability of indomethacin was also studied." | ( Effect of antacid magaldrate oral suspension on in-vitro and in-vivo availability of indomethacin in dogs. al-Gohary, OM; Hosny, EA, 1997) | 0.72 |
"51 min) and the mean bioavailability was 91." | ( Pharmacokinetics of indomethacin in sheep after intravenous and intramuscular administration. Boggio, JC; Encinas, T; Rodríguez, C; San Andrés, MD; San Andrés, MI; Vinagre, E, 1998) | 0.62 |
" There was no significant difference in bioavailability of indomethacin when administered by these two vehicles." | ( Thermally reversible xyloglucan gels as vehicles for rectal drug delivery. Attwood, D; Kawasaki, N; Miyazaki, S; Shirakawa, M; Suisha, F; Yamatoya, K, 1998) | 0.54 |
"Investigation of furans, pyrroles and pyrazolones identified 3-pyridyl-2,5-diaryl-pyrroles as potent, orally bioavailable inhibitors of p38 kinase." | ( Pyrroles and other heterocycles as inhibitors of p38 kinase. Agarwal, L; Chang, L; Chin, J; Croft, G; de Laszlo, SE; Fletcher, D; Forsyth, A; Frantz, B; Hacker, C; Hanlon, W; Harper, C; Kostura, M; Li, B; Luell, S; MacCoss, M; Mantlo, N; O'Keefe, SJ; O'Neill, EA; Orevillo, C; Pang, M; Parsons, J; Rolando, A; Sahly, Y; Sidler, K; Visco, D, 1998) | 0.3 |
"To determine if intestinal secretion occurs for the poorly bioavailable diuretic, furosemide." | ( Net secretion of furosemide is subject to indomethacin inhibition, as observed in Caco-2 monolayers and excised rat jejunum. Benet, LZ; Flanagan, SD, 1999) | 0.57 |
" These preliminary results indicate that furosemide bioavailability may be limited by an intestinal transporter." | ( Net secretion of furosemide is subject to indomethacin inhibition, as observed in Caco-2 monolayers and excised rat jejunum. Benet, LZ; Flanagan, SD, 1999) | 0.57 |
" This particulate system may have potential use as a carrier for drugs that are poorly absorbed after oral administration." | ( Alginate-pectin-poly-L-lysine particulate as a potential controlled release formulation. Krishnan, TR; Liu, P, 1999) | 0.3 |
" Bioavailability of indomethacin from xyloglucan gels formed in situ was increased approximately threefold compared with that from the suspension." | ( Thermally reversible xyloglucan gels as vehicles for oral drug delivery. Attwood, D; Kawasaki, N; Miyazaki, S; Ohkura, R; Sugimoto, S; Uno, Y, 1999) | 0.63 |
" Indomethacin was irregularly and poorly absorbed from the rumen after intraruminal administration to sheep." | ( Pharmacokinetics of indomethacin after intraruminal administration to sheep. Ballesteros, C; Encinas, T; Lázaro, R; Rodríguez, C; Ros, JM; San Andrés, MD; Vinagre, E, 1999) | 1.54 |
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents." | ( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000) | 0.31 |
" Papp of IDM was greater than that of TAT, indicating that the order corresponded with that of in vivo bioavailability after oral administration of their PEG 600 solutions." | ( Evaluation of absorbability of poorly water-soluble drugs: validity of the use of additives. Hayashi, M; Sudo, R; Takahashi, M; Watanabe, E, 2000) | 0.31 |
" This formulation was evaluated for stability, bioavailability and anti-inflammatory activity in comparison with an ophthalmic IND solution currently on the market." | ( Pharmacokinetics and anti-inflammatory activity in rabbits of a novel indomethacin ophthalmic solution. Benelli, U; Burgalassi, S; Chetoni, P; Panichi, L; Saettone, MF, 2000) | 0.54 |
" In both groups no effect was found on the transcapillary ultrafiltration and the effective lymphatic absorption rate during the 4-h dwell." | ( Prostaglandin inhibition by intraperitoneal indomethacin has no effect on peritoneal permeability during stable CAPD. de Waart, DR; Douma, CE; Krediet, RT; Struijk, DG; Zemel, D, 2001) | 0.57 |
"This paper describes a graphical model for simplifying in vitro absorption, metabolism, distribution, and elimination (ADME) data analysis through the estimation of oral bioavailability (%F) of drugs in humans and other species." | ( Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. Hwang, KK; Mandagere, AK; Thompson, TN, 2002) | 0.31 |
" Using larger particles and a higher helium pressure, produced an increase in the plasma IDM concentration and the area under the plasma concentration-time curve (AUC) and resultant F (relative bioavailability with respect to intracutaneous injection) of IDM increased by an amount depending on the particle size and helium pressure." | ( Effects of particle size, helium gas pressure and microparticle dose on the plasma concentration of indomethacin after bombardment of indomethacin-loaded poly-L-lactic acid microspheres using a Helios gun system. Kobayashi, D; Morimoto, Y; Natsume, H; Sugibayashi, K; Uchida, M, 2002) | 0.53 |
" Tablets and capsules, formulated from the solid dispersions showed significantly better dissolution and enhanced absorption rate in human volunteers, compared to commercial capsule of indomethacin." | ( Bioavailability studies on fast release formulations of indomethacin. Balasubramaniam, J; Kumar, MT; Pandit, JK; Verma, MM, ) | 0.57 |
" Bioavailability and Cmax were also dependent on the helium pressure." | ( [Transdermal microparticle delivery by a supersonic-Helios gun system]. Jin, Y; Morimoto, Y; Natsume, H; Sugibayashi, K; Uchida, M; Wang, CF, 2001) | 0.31 |
" These results suggest that prolonged exposure of rabbits to oral arsenate may impair the bioavailability of BH(4) in endothelial cells and, as a consequence, disrupt the balance between NO and O2(." | ( A potential mechanism for the impairment of nitric oxide formation caused by prolonged oral exposure to arsenate in rabbits. Hayashi, T; Horiguchi, S; Itoh, K; Kumagai, Y; Nikaido, M; Pi, J; Shimojo, N; Sun, G; Sun, Y; Waalkes, MP; Yamamoto, M; Yamauchi, H, 2003) | 0.32 |
" MRP type efflux pumps may limit the bioavailability of EGCG." | ( Involvement of multidrug resistance-associated proteins in regulating cellular levels of (-)-epigallocatechin-3-gallate and its methyl metabolites. Hong, J; Lambert, JD; Lee, SH; Sinko, PJ; Yang, CS, 2003) | 0.32 |
" This study set out to test the hypothesis that in vivo gene transfer of GTPCH I to endothelial cells could increase bioavailability of BH4, enhance biosynthesis of nitric oxide and thereby enhance endothelium-dependent relaxations mediated by nitric oxide." | ( In vivo expression and function of recombinant GTPCH I in the rabbit carotid artery. Hynes, SO; Katusic, ZS; Kovesdi, I; O'Brien, T; Richardson, DM; Smith, LA, 2004) | 0.32 |
"In an effort to improve the bioavailability of the insoluble drug indomethacin, three complexes were prepared with indomethacin and the soluble complexing agents beta-, hydroxyethyl-beta-, and hydroxypropyl-beta-cyclodextrin." | ( The physicochemical characteristics and bioavailability of indomethacin from beta-cyclodextrin, hydroxyethyl-beta-cyclodextrin, and hydroxypropyl-beta-cyclodextrin complexes. Casella, R; Jambhekar, S; Maher, T, 2004) | 0.8 |
"The poor bioavailability and therapeutic response exhibited by the conventional ophthalmic solutions due to pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems, which upon instillation as drops into the eye undergo a sol-gel transition in the cul-de-sac." | ( In vitro and in vivo evaluation of the Gelrite gellan gum-based ocular delivery system for indomethacin. Balasubramaniam, J; Kant, S; Pandit, JK, 2003) | 0.54 |
" The results suggest that these supramolecular assemblies with high drug loadings and pH-dependent release kinetics can potentially enhance the oral bioavailability of poorly water-soluble drugs." | ( Novel pH-sensitive supramolecular assemblies for oral delivery of poorly water soluble drugs: preparation and characterization. Leroux, JC; Sant, VP; Smith, D, 2004) | 0.32 |
" Bioavailability and Cmax were also dependent on the helium pressure." | ( Transdermal microparticle delivery by a supersonic-Helios gun system. Chao, W; Hideshi, N; Mashaki, U; Yasunori, M; Yi, J, 2004) | 0.32 |
" This method has been used to determine plasma drug concentration and bioavailability of indomethacin controlled release capsule for healthy volunteers." | ( [Determination of plasma drug concentration and bioavailability of indomethacin controlled release capsule by high performance liquid chromatography]. Jiang, X; Zeng, J; Zhang, D, 1997) | 0.75 |
"It is known that secretory transport limits the oral bioavailability of certain drugs." | ( Characterization of secretory intestinal transport of phenolsulfonphthalein. Chiba, M; Hirano, T; Iseki, K; Itagaki, S; Kobayashi, M; Miyazaki, K; Shimamoto, S; Sugawara, M, 2005) | 0.33 |
" The results from tape stripping technique confirmed the trend obtained by the former in vivo method and indicated that IND topical bioavailability in the stratum corneum varied substantially depending upon the formulations (A-D)." | ( Evaluation of indomethacin percutaneous absorption from nanostructured lipid carriers (NLC): in vitro and in vivo studies. Bonina, F; Di Giovanni, C; Giovagnoli, S; Puglia, C; Ricci, M; Rossi, C, 2005) | 0.69 |
" It was found that the indomethacin entrapped in liposomes has a favorable influence on the bioavailability in comparison to sole indomethacin suspension." | ( Bioavailability of indomethacin in liposomes. Stozek, T, 1992) | 0.92 |
"Previously, we have demonstrated that patients with normoalbuminuric Type 1 diabetes are characterized by impaired nitric oxide bioavailability compensated for by increased vasodilatory prostanoid-mediated vasodilation." | ( Angiotensin II does not affect endothelial tone in Type 1 diabetes-results of a double-blind placebo controlled trial. Allard, SE; Browne, DL; Cummings, MH; Meeking, DR; Munday, JL; Shaw, KM, 2006) | 0.33 |
"We previously demonstrated that a novel hydrophilic gamma-tocopherol (gamma-Toc) derivative, gamma-tocopherol-N,N-dimethylglycinate hydrochloride (gamma-TDMG) converts to gamma-Toc in the mouse skin and has a higher bioavailability than gamma-Toc itself." | ( Topical application of a novel, hydrophilic gamma-tocopherol derivative reduces photo-inflammation in mice skin. Karube, Y; Kobayashi, S; Takata, J; Watanabe, T; Yamazaki, A; Yoshida, E, 2006) | 0.33 |
" A one-compartment model was fitted to the data to obtain estimates of clearance (CL), volume of distribution (V), absorption rate constant (Ka) and orogastric bioavailability (F), using NONMEM." | ( Orogastric and intravenous indomethacin administration to very premature neonates with patent ductus arteriosus: population pharmacokinetics, absolute bioavailability, and treatment outcome. Al Za'abi, M; Charles, B; Collie, LA; Donovan, T; Tudehope, D; Woodgate, P, 2007) | 0.64 |
" Our aim in this study was to investigate the anti-inflammatory effects, absorption, and bioavailability of Artepillin C in mice." | ( Anti-inflammatory effects of a bioavailable compound, Artepillin C, in Brazilian propolis. Abreu, SR; Bretz, WA; Dirsch, VM; Hori, H; Koyama, D; Nagasawa, H; Paulino, N; Scremin, A; Uto, Y; Vollmar, AM, 2008) | 0.35 |
" The bioavailability study of IND was performed in rats." | ( Effect of adhesive matrix composition and terpinolene on indomethacin bioavailability in rats from transdermal therapeutic system. Cal, K; Janicki, S; Sznitowska, M, 2008) | 0.59 |
"Two different chitosan (CS) nanocarriers namely nanoparticles and nanoemulsion were developed to prolong Indomethacin (IM) precorneal residence time and to improve its ocular bioavailability the main limitations in its management of post-operative inflammation and intraocular irritation after cataract extraction." | ( Chitosan based nanocarriers for indomethacin ocular delivery. Badawi, AA; El dally, M; El Mofty, H; El Qidra, RK; El-Laithy, HM, 2008) | 0.84 |
" Consequently, a highly functional anti-inflammatory patch in terms of its adhesive properties and bioavailability was successfully obtained." | ( Formulation optimization of an indomethacin-containing photocrosslinked polyacrylic acid hydrogel as an anti-inflammatory patch. Isowa, K; Nishikawa, M; Onuki, Y; Takayama, K, 2008) | 0.63 |
" Thus, our results show that polymeric nanocapsules are able to increase the intratumoral bioavailability of indomethacin and reduce the growth of implanted gliomas." | ( Indomethacin-loaded nanocapsules treatment reduces in vivo glioblastoma growth in a rat glioma model. Battastini, AM; Bernardi, A; Braganhol, E; Edelweiss, MI; Figueiró, F; Guterres, SS; Jäger, E; Pohlmann, AR, 2009) | 2.01 |
"We tested two hypotheses, first that exercise training reverses age-related decrements in endothelium-dependent dilation in soleus muscle feed arteries and second that this improved endothelium-dependent dilation is the result of increased nitric oxide (NO) bioavailability due to increased content and phosphorylation of endothelial NO synthase (eNOS) and/or increased antioxidant enzyme content." | ( Exercise training reverses age-related decrements in endothelium-dependent dilation in skeletal muscle feed arteries. Gunduz, F; Laughlin, MH; Trott, DW; Woodman, CR, 2009) | 0.35 |
" We then evaluated the following properties of these parenterally administered test drugs: (i) GI toxicity (luminal and faecal haemoglobin; intestinal perforations and adhesions; and haematocrit); (ii) bioavailability (plasma indomethacin); and (iii) therapeutic efficacy (analgesia from sensitivity to pressure; anti-inflammatory from ankle thickness; cyclo-oxygenase (COX) inhibition from synovial fluid prostaglandin E(2) concentration) in rats with adjuvant-induced joint inflammation." | ( Gastrointestinal safety and therapeutic efficacy of parenterally administered phosphatidylcholine-associated indomethacin in rodent model systems. Dial, EJ; Lichtenberger, L; Romero, JJ, 2009) | 0.75 |
" Acemetacin bioavailability was increased, although not in a statistically significant manner." | ( Pharmacokinetics of acemetacin and its active metabolite indomethacin in rats during acute hepatic damage and liver regeneration. Castañeda-Hernández, G; Chávez-Piña, AE; Favari, L, ) | 0.38 |
"Indomethacin bioavailability after oral administration of its precursor, acemetacin, is significantly reduced by acute hepatitis produced by CCl4." | ( Pharmacokinetics of acemetacin and its active metabolite indomethacin in rats during acute hepatic damage and liver regeneration. Castañeda-Hernández, G; Chávez-Piña, AE; Favari, L, ) | 1.82 |
" In conclusion, gastroprotective effect on ethanol and indomethacin-induced ulcer promoted by (-)-alpha-bisabolol may be associated with an increase of gastric sulfydryl groups bioavailability leading to a reduction of gastric oxidative injury induced by ethanol and indomethacin." | ( Gastroprotection of (-)-alpha-bisabolol on acute gastric mucosal lesions in mice: the possible involved pharmacological mechanisms. Aquino Neto, MR; de França Fonteles, MM; de Sousa, DP; de Sousa, FC; Gomes Silva, MI; Mendes Vasconcelos, SM; Moura Rocha, NF; Moura, BA; Vasconcelos Rios, ER; Venâncio, ET, 2010) | 0.61 |
" Recently, we described a novel series of potent, selective, and orally bioavailable delta opioid receptor agonists." | ( Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747). Ajello, CW; Barker, WM; Belanger, S; Brogdon, BL; Cassel, JA; Chu, GH; DeHaven, RN; DeHaven-Hudkins, DL; Derelanko, MJ; Dolle, RE; Feschenko, MS; Graczyk, TM; Gu, M; Koblish, M; Kutz, S; Le Bourdonnec, B; Leister, LK; Little, PJ; Smith, SA; Tuthill, PA; Wiant, DD; Windh, RT; Zhou, QJ, 2009) | 0.35 |
"Endothelial dysfunction has been linked to a decrease in nitric oxide (NO) bioavailability and attenuated endothelium-derived hyperpolarizing factor (EDHF)-mediated relaxation." | ( Upregulation of intermediate calcium-activated potassium channels counterbalance the impaired endothelium-dependent vasodilation in stroke-prone spontaneously hypertensive rats. Carneiro, FS; Carneiro, ZN; Dorrance, A; Giachini, FR; Lima, VV; Tostes, RC; Webb, RC, 2009) | 0.35 |
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)." | ( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010) | 0.36 |
" Orally dosed in-vivo studies in rats showed complete drug absorption and statistically higher fasted state bioavailability (F) (p<0." | ( An oral delivery system for indomethicin engineered from cationic lipid emulsions and silica nanoparticles. Davey, AK; Hui, H; Prestidge, CA; Rades, T; Simovic, S; Song, Y, 2010) | 0.36 |
" In conclusion, many human pathological conditions characterized by a decline in endothelial function are associated with a progressive decrease in NO bioavailability and increase in the production of EDCFs." | ( Human endothelial dysfunction: EDCFs. Ghiadoni, L; Taddei, S; Virdis, A, 2010) | 0.36 |
"The crystallization of amorphous drugs during dissolution is a type of solution mediated phase transformation that can reduce the bioavailability enhancement one hoped to gain from the amorphous state." | ( Crystallization of amorphous indomethacin during dissolution: effect of processing and annealing. Bogner, R; Greco, K, 2010) | 0.65 |
" The antiulcerogenic effects of erythropoietin may be related to its intrinsic ability to sustain the activities of free-radical scavenging enzymes and the bioavailability of glutathione." | ( The role of erythropoietin in the protection of gastric mucosa from indometacin-induced gastric injury and its relationship with oxidant and antioxidant parameters in rats. Albayrak, F; Albayrak, Y; Bayir, Y; Dursun, H; Halici, Z; Koc, F; Odabasoglu, F; Polat, B; Suleyman, H; Uyanik, A, 2010) | 0.36 |
" However, the in-vivo bioavailability of cocrystals has rarely been addressed." | ( Bioavailability of indomethacin-saccharin cocrystals. Alhalaweh, A; Cho, W; Hwang, SJ; Jung, MS; Kim, JS; Kim, MS; Velaga, SP, 2010) | 0.69 |
" Finally, a bioavailability study for the formulations was conducted in beagle dogs." | ( Bioavailability of indomethacin-saccharin cocrystals. Alhalaweh, A; Cho, W; Hwang, SJ; Jung, MS; Kim, JS; Kim, MS; Velaga, SP, 2010) | 0.69 |
" The in-vivo bioavailability of the IND-SAC cocrystals in dogs was significantly higher (ANOVA, P<0." | ( Bioavailability of indomethacin-saccharin cocrystals. Alhalaweh, A; Cho, W; Hwang, SJ; Jung, MS; Kim, JS; Kim, MS; Velaga, SP, 2010) | 0.69 |
"The study indicates that the improved aqueous solubility of the cocrystals leads to improved bioavailability of IND." | ( Bioavailability of indomethacin-saccharin cocrystals. Alhalaweh, A; Cho, W; Hwang, SJ; Jung, MS; Kim, JS; Kim, MS; Velaga, SP, 2010) | 0.69 |
" Furthermore, one selected compound was tested for peroral bioavailability in mice." | ( 1-(5-Carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α: effect of substituents in position 3 of the indole scaffold on inhibitory potency, metabolic stability, solubility, and bioavailability. Bovens, S; Kaptur, M; Lehr, M; Reinhardt, D; Schäfers, M; Schulze Elfringhoff, A, 2010) | 0.36 |
"Formulations that produce supersaturated solutions after their oral administration have received increased attention as a means to improve bioavailability of poorly water-soluble drugs." | ( Maintenance of supersaturation I: indomethacin crystal growth kinetic modeling using an online second-derivative ultraviolet spectroscopic method. Anderson, BD; Joguparthi, V; Patel, DD; Wang, Z, 2011) | 0.65 |
" These nano-assemblies can function as gastro-OFF/intestinal-ON delivery systems to selectively transport payload to enteric sites, thereby dramatically increasing the oral bioavailability of the loaded therapeutic, which can also serve as multifunctional nano-platforms for multiple delivery of various therapeutics." | ( Highly efficient nanomedicines assembled via polymer-drug multiple interactions: Tissue-selective delivery carriers. Che, L; He, H; Jia, Y; Li, X; Zhang, J; Zhu, Y, 2011) | 0.37 |
"Nanosizing techniques are important tools for improving the bioavailability of water insoluble drugs." | ( Nanosuspensions of poorly soluble drugs: preparation and development by wet milling. Hirvonen, J; Kiesvaara, J; Laaksonen, T; Laru, J; Liu, P; Peltonen, L; Rong, X; van Veen, B, 2011) | 0.37 |
" The particle kinetic energy, which depended on the particle velocity and particle mass, was increased with increasing helium pressure and particle size, decreasing bombardment dose, resulting in the increased percentage introduction and relative bioavailability (F(0-24 h))." | ( Relationships between the particle velocity and introduction of drug-loaded microparticles into the skin in a microparticulate bombardment system. Morimoto, Y; Natsume, H; Seki, T; Uchida, M; Uchida, T, 2011) | 0.37 |
"Amorphous solid dispersions (ASDs) are widely utilized in the pharmaceutical industry for bioavailability enhancement of low solubility drugs." | ( Dissolution and precipitation behavior of amorphous solid dispersions. Alonzo, DE; Gao, Y; Mo, H; Taylor, LS; Zhang, GGZ; Zhou, D, 2011) | 0.37 |
" These findings provide the first evidence of the ability of poorly water-soluble inorganic salts to enhance the de-agglomeration and dissolution of micronized powders, potentially translating to improved bioavailability of poorly water-soluble drugs." | ( Counter-intuitive enhancement in the dissolution of indomethacin with the incorporation of cohesive poorly water-soluble inorganic salt additives. Allahham, A; Morton, DA; Stewart, PJ; Tay, T, 2011) | 0.62 |
"This paper report the development of a new dosage form - self-microemulsifying mouth dissolving films, which can improve the oral bioavailability of water insoluble drugs and have good compliance." | ( [Optimization of novel self-microemulsifying mouth dissolving films by response surface methodology]. He, JK; Huan, D; Liu, Y; Xiao, L; Yi, T, 2011) | 0.37 |
"76/microg x h/mL in IGNP and IDM respectively (relative bioavailability 500%)." | ( In-vitro and in-vivo study of indomethacin loaded gelatin nanoparticles. Dhanawat, M; Kumar, R; Nagarwal, RC; Pandit, JK, 2011) | 0.66 |
"Amorphous drugs have higher solubility, better oral bioavailability and are easier to be absorbed than their crystalline counterparts." | ( [Microcosmic mechanisms of amorphous indomethacin crystallization and the influence of nano-coating on crystallization]. Hui, OY; Liu, F; Yi, T; Zheng, Q, 2011) | 0.64 |
" The plasma profile and bioavailability of IMC after oral administration of both types of liposomes were improved, compared with oral administration of IMC solution." | ( Effectiveness of submicronized chitosan-coated liposomes in oral absorption of indomethacin. Kawashima, Y; Sugihara, H; Takeuchi, H; Yamamoto, H, 2012) | 0.61 |
" Drug bioavailability after its peroral administration to rats was more than 2 fold higher as compared with free indomethacin." | ( [The increase of bioavailability and anti-inflammatory effect of indomethacin loaded into phospholipid nanoparticles]. Ipatova, OM; Medvedeva, NV; Prozorovskiĭ, VN; Sanzhakov, MA; Shironin, AV; Tikhonova, EG; Torkhovskaia, TI; Zakharova, TS, ) | 0.58 |
"Reduced intrahepatic nitric oxide (NO) bioavailability and increased cyclooxygenase-1 (COX-1)-derived vasoconstrictor prostanoids modulate the hepatic vascular tone in cirrhosis." | ( Interaction between NO and COX pathways modulating hepatic endothelial cells from control and cirrhotic rats. Bosch, J; García-Pagán, JC; Gracia-Sancho, J; Monclús, M; Rodríguez-Vilarrupla, A; Rosado, E, 2012) | 0.38 |
" Lipid-based formulations showed an increase of relative bioavailability of IND versus Indocid®." | ( Formulations based on alpha cyclodextrin and soybean oil: an approach to modulate the oral release of lipophilic drugs. Bochot, A; Bourasset, F; Domergue-Dupont, V; Fattal, E; Gueutin, C; Hamoudi, MC; Nicolas, V, 2012) | 0.38 |
" Compared with the commercial tablet, the relative oral bioavailability of IND-nanomedicines was significantly enhanced." | ( Assembled nanomedicines as efficient and safe therapeutics for articular inflammation. Che, L; He, H; Jia, Y; Li, S; Li, X; Liu, Y; Zhang, J; Zhou, J; Zhou, X; Zhu, Y, 2012) | 0.38 |
"Results from this study suggest that topical IN-SLNs could significantly improve ocular bioavailability of indomethacin." | ( Indomethacin-loaded solid lipid nanoparticles for ocular delivery: development, characterization, and in vitro evaluation. Adelli, GR; Hippalgaonkar, K; Majumdar, S; Repka, MA, 2013) | 2.05 |
" Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h." | ( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics. Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014) | 0.63 |
"Dry foam technology was developed to overcome insufficient oral bioavailability of poorly soluble and wettable active pharmaceutical ingredients (APIs)." | ( Influence of process parameters and equipment on dry foam formulation properties using indomethacin as model drug. Kleinebudde, P; Page, S; Sprunk, A, 2013) | 0.61 |
"Drug nanosuspensions are very promising for enhancing the dissolution and bioavailability of drugs that are poorly soluble in water." | ( Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution. Chen, L; He, W; Lu, Y; Qi, J; Wu, W; Yin, L, 2013) | 0.66 |
"Oral IND@RNP(O) administration is a useful approach for improving the oral bioavailability of IND and suppressing its adverse effects." | ( Indomethacin-loaded redox nanoparticles improve oral bioavailability of indomethacin and suppress its small intestinal inflammation. Chonpathompikunlert, P; Matsui, H; Nagasaki, Y; Sha, S; Vong, LB; Yoshitomi, T, 2014) | 1.85 |
" In rats, the oral bioavailability of isotretinoin is twofold enhanced with uncoated beads as compared to the lipid content of a soft capsule." | ( Oil-cyclodextrin based beads for oral delivery of poorly-soluble drugs. Bochot, A; Hamoudi, MC, 2014) | 0.4 |
" Hence, inflammatory diseases may impose variability in drug bioavailability through alterations in the intestinal expression and activity of drug transporters." | ( Changes of Absorptive and Secretory Transporting System of (1 → 3) β-D-glucan Based on Efflux Transporter in Indomethacin-induced Rat. Aketagawa, J; Hayashi, M; Iida, A; Ito, Y; Oda, T; Ouchi, S; Takizawa, Y; Tomita, M, 2015) | 0.63 |
" It is known that decreasing direct cell stimulation and reducing the amount applied via increasing bioavailability are useful for improving these issues." | ( A nanoparticle formulation reduces the corneal toxicity of indomethacin eye drops and enhances its corneal permeability. Ito, Y; Nagai, N; Okamoto, N; Shimomura, Y, 2014) | 0.65 |
"gov NCT01747252) revealed relatively high bioavailability and two distinctly separated plasma concentration peaks at 1 and 5 h." | ( A novel red grape cells complex: health effects and bioavailability of natural resveratrol. Azachi, M; Danon, A; Hagay, Y; Katz, A; Yatuv, R, 2014) | 0.4 |
" ASDs are employed to improve the bioavailability of drugs which are poorly soluble in aqueous solutions." | ( Stability of indomethacin with relevance to the release from amorphous solid dispersions studied with ATR-FTIR spectroscopic imaging. Clarke, GS; Ewing, AV; Kazarian, SG, 2014) | 0.77 |
"Assessment of oral drug bioavailability is an important parameter for new chemical entities (NCEs) in drug development cycle." | ( A novel concentration dependent amino acid ion pair strategy to mediate drug permeation using indomethacin as a model insoluble drug. ElShaer, A; Hanson, P; Mohammed, AR, 2014) | 0.62 |
"We designed new oral formulations containing indomethacin (IMC) solid nanoparticles, and investigate their usefulness by evaluating bioavailability and gastrointestinal lesions." | ( Effect of solid nanoparticle of indomethacin on therapy for rheumatoid arthritis in adjuvant-induced arthritis rat. Ito, Y; Nagai, N, 2014) | 0.95 |
" The lead compound demonstrated very good oral bioavailability in mice, slow metabolic degradation, modest distribution into the brain and a remarkable anti-inflammatory efficacy in carrageenan-induced mouse paw edema model." | ( Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core. Gavalas, A; Geronikaki, A; Hammock, B; Hwang, SH; Iurchenko, V; Ivanenkov, Y; Krasavin, M; Morisseau, C; Mujumdar, P; Sarnpitak, P; Zozulya, S, 2014) | 0.4 |
"Amorphous drugs are used to improve the solubility, dissolution, and bioavailability of drugs." | ( A method to evaluate the effect of contact with excipients on the surface crystallization of amorphous drugs. de Villiers, MM; Derdour, L; Huang, J; Hussain, MA; Qian, F; Yu, L; Zhang, SW, 2014) | 0.4 |
", polymers) to formulate an amorphous solid dispersion is a promising strategy to improve the oral bioavailability of the API." | ( Influence of copolymer composition on the phase behavior of solid dispersions. Ji, Y; Kleetz, T; Korf, M; Prudic, A; Sadowski, G, 2014) | 0.4 |
" Vancomycin (VCM), a poorly absorbed drug, was administered intraduodenally to rats with SIUs." | ( Intestinal and hepatic expression of cytochrome P450s and mdr1a in rats with indomethacin-induced small intestinal ulcers. Hamaguchi, T; Horibe, S; Inoue, J; Kawauchi, S; Miki, I; Mizuno, S; Nakamura, T; Nishikawa, C; Tanahashi, T; Yasui, H, 2014) | 0.63 |
" The mechanisms for impaired cerebral artery endothelial function are reduced nitric oxide bioavailability and increased oxidative stress." | ( Greater impairments in cerebral artery compared with skeletal muscle feed artery endothelial function in a mouse model of increased large artery stiffness. Dobson, PS; Donato, AJ; Henson, GD; Lesniewski, LA; Li, DY; Ling, J; Mecham, RP; Morgan, RG; Nielson, EI; Reihl, KD; Walker, AE, 2015) | 0.42 |
"05), indicating that lower NO bioavailability contributed to the impaired EDD in Eln(+/-) mice." | ( Greater impairments in cerebral artery compared with skeletal muscle feed artery endothelial function in a mouse model of increased large artery stiffness. Dobson, PS; Donato, AJ; Henson, GD; Lesniewski, LA; Li, DY; Ling, J; Mecham, RP; Morgan, RG; Nielson, EI; Reihl, KD; Walker, AE, 2015) | 0.42 |
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates." | ( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. Bharate, SS; Vishwakarma, RA, 2015) | 0.42 |
" The solubility and dissolution properties of co-crystals can allow to increase the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs)." | ( Indomethacin co-crystals and their parent mixtures: does the intestinal barrier recognize them differently? Beggiato, S; Bertolasi, V; Dalpiaz, A; Ferraro, L; Ferretti, V; Pavan, B; Spisni, E; Spizzo, F, 2015) | 1.86 |
" The absorbed fraction of isoliquiritigenin was high, but the absolute bioavailability was low mainly due to its metabolism." | ( In vivo gastroprotective effect along with pharmacokinetics, tissue distribution and metabolism of isoliquiritigenin in mice. Chae, HS; Chin, YW; Choi, YH; Kim, YJ, 2015) | 0.42 |
" Taken together these data indicate that deletion of PTP1B protected endothelial function by compensating the reduction in NO bioavailability by increasing COX-2-mediated release of the vasodilator prostanoid PGI2, in T1DM mice." | ( Deletion of Protein Tyrosine Phosphatase 1B (PTP1B) Enhances Endothelial Cyclooxygenase 2 Expression and Protects Mice from Type 1 Diabetes-Induced Endothelial Dysfunction. Anderson, R; Belin de Chantemèle, EJ; Herre, DJ; Herren, DJ; Huby, AC; Norman, JB; Tremblay, ML, 2015) | 0.42 |
" Thus, it is of medical importance to develop gastroretentive (GR) formulations of BR to enhance its bioavailability and anti-ulcer efficacy." | ( Gastroretentive Matrix Tablets of Boswellia Oleogum Resin: Preparation, Optimization, In Vitro Evaluation, and Cytoprotective Effect on Indomethacin-Induced Gastric Ulcer in Rabbits. Abu Hashim, II; Badria, FA; Mohamed, EA; Yusif, RM, 2016) | 0.64 |
"For the solubility and bioavailability of poorly soluble active pharmaceutical ingredients (APIs) to be improved, the transformation of crystalline APIs to the amorphous state has often been shown to be advantageous." | ( Predicting the Solubility Advantage of Amorphous Pharmaceuticals: A Novel Thermodynamic Approach. Ji, Y; Paus, R; Sadowski, G; Vahle, L, 2015) | 0.42 |
" The influence of excipients on solubility and, hence, oral bioavailability was confirmed for ibuprofen, a second BCS class II compound." | ( Evaluation of changes in oral drug absorption in preterm and term neonates for Biopharmaceutics Classification System (BCS) class I and II compounds. Coboeken, K; Ince, I; Meyer, M; Schmidt, S; Schnizler, K; Somani, AA; Thelen, K; Trame, MN; Willmann, S; Zheng, S, 2016) | 0.43 |
" The in vivo evaluation, demonstrated a 10-fold enhancement in bioavailability of the optimized formulation, with absence of ulcerogenic side effect compared to the marketed product." | ( Optimization, physicochemical characterization and in vivo assessment of spray dried emulsion: A step toward bioavailability augmentation and gastric toxicity minimization. Alwattar, JK; Elmaradny, HA; Mehanna, MM, 2015) | 0.42 |
"A large percentage of drug compounds exhibit low water solubility and hence low bioavailability and therapeutic efficacy." | ( Drug nanoparticles by emulsion-freeze-drying via the employment of branched block copolymer nanoparticles. He, T; Jackson, AW; Wais, U; Xiang, Y; Zhang, H; Zuo, Y, 2016) | 0.43 |
"Although using spray-dried dispersions (SDDs) to improve the bioavailability of poorly water-soluble compounds has become a common practice in supporting the early phases of clinical studies, their performance evaluation, whether in solid dosage forms or alone, still presents significant challenges." | ( Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion. Li, J; Wang, Y; Wu, B, 2016) | 0.43 |
" We quantified inflammation, fibrosis, oxidative stress, nitric oxide (NO) bioavailability and thromboxane B2 levels." | ( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease. Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016) | 0.43 |
"Our study provides evidence that endothelial dysfunction at an early stage of NAFLD is associated with reduced NO bioavailability together with increased cyclooxygenase end products and oxidative stress, which suggests that both pathways are involved in the pathophysiology and may be worth exploring as therapeutic targets to prevent progression of the disease." | ( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease. Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016) | 0.43 |
" Compared with raw IND, the utilization of PEI-g-PZLL as a carrier significantly enhanced the oral bioavailability of IND and improved its protective effect on renal ischemia-reperfusion injury, as evidenced by in vivo pharmacokinetic and pharmacodynamic studies." | ( Poly(ε-benzyloxycarbonyl-L-lysine)-grafted branched polyethylenimine as efficient nanocarriers for indomethacin with enhanced oral bioavailability and anti-inflammatory efficacy. Li, X; Liu, D; Lu, C; Lu, S; Luo, H; Xia, W; Ye, D; Zhang, Y, 2017) | 0.67 |
" The low cytotoxicity and biodegradability, well-defined self-assembled nano-sized polymeric micelles, high loading capacity and loading efficiency, amorphous state of the encapsulated IND, as well as the enhanced oral bioavailability of IND, makes the copolymer PEI-g-PZLL a promising nanocarrier for the oral administration of IND and possibly other poorly water-soluble drugs." | ( Poly(ε-benzyloxycarbonyl-L-lysine)-grafted branched polyethylenimine as efficient nanocarriers for indomethacin with enhanced oral bioavailability and anti-inflammatory efficacy. Li, X; Liu, D; Lu, C; Lu, S; Luo, H; Xia, W; Ye, D; Zhang, Y, 2017) | 0.67 |
"Amorphous solid dispersions (SDs) are a promising approach to improve the dissolution rate of and oral bioavailability of poorly water-soluble drugs." | ( The formation and physical stability of two-phase solid dispersion systems of indomethacin in supercooled molten mixtures with different matrix formers. Antikainen, O; Ehlers, H; Heinämäki, J; Kogermann, K; Laidmäe, I; Semjonov, K; Strachan, CJ; Yliruusi, J, 2017) | 0.68 |
" Although higher supersaturation is known to result in faster precipitation, the overall effect of this faster precipitation on the bioavailability is not well understood." | ( Effect of Extent of Supersaturation on the Evolution of Kinetic Solubility Profiles. Han, YR; Lee, PI, 2017) | 0.46 |
" However, co-administration of curcumin did not produce any significant alteration in the bioavailability parameters of indomethacin and acemetacin after administration of either the active compound or the prodrug." | ( Evidence against the participation of a pharmacokinetic interaction in the protective effect of single-dose curcumin against gastrointestinal damage induced by indomethacin in rats. Castañeda-Hernández, G; Chávez-Piña, AE; Cruz-Antonio, L; Estela Díaz-Triste, N; Medina-Aymerich, L; Zazueta-Beltrán, L, 2017) | 0.86 |
"Curcumin exhibits a protective effect against indomethacin-induced gastric damage, but does not produce a reduction of the bioavailability of this nonsteroidal anti-inflammatory drug, indomethacin." | ( Evidence against the participation of a pharmacokinetic interaction in the protective effect of single-dose curcumin against gastrointestinal damage induced by indomethacin in rats. Castañeda-Hernández, G; Chávez-Piña, AE; Cruz-Antonio, L; Estela Díaz-Triste, N; Medina-Aymerich, L; Zazueta-Beltrán, L, 2017) | 0.91 |
" In conclusion, coatings might improve the bioavailability of co-amorphous formulations." | ( Solid state properties and drug release behavior of co-amorphous indomethacin-arginine tablets coated with Kollicoat® Protect. Grohganz, H; Leopold, CS; Löbmann, K; Petry, I; Rades, T, 2017) | 0.69 |
" In addition, the oral bioavailability and its resistance against crystallization were also enhanced; AASD samples have remained amorphous for more than two years of storage." | ( Two-phase amorphous-amorphous solid drug dispersion with enhanced stability, solubility and bioavailability resulting from ultrasonic dispersion of an immiscible system. Caballero, A; Castorena-Torres, F; Castro, S; Lara-Díaz, VJ; López Silva, T; Martínez, LM; Videa, M, 2017) | 0.46 |
" Oral bioavailability and anti-inflammation effect of IMC delivery systems established by CMSN and Amino-CMSN were enhanced compared with IMC, which was attributed to the primary cause of the improvement of IMC dissolution, and Amino-CMSN exhibited better biological effect." | ( Superiority of amino-modified chiral mesoporous silica nanoparticles in delivering indometacin. Guo, Y; Li, H; Li, J; Li, S; Shang, L, 2018) | 0.48 |
" However, its low oral bioavailability is a major obstacle to its potential use." | ( Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide. Chen, YC; Wang, CC; Wu, MT; Wu, YT; Yen, CC, 2018) | 0.48 |
" The pharmacokinetic results indicate that the absorption of AG from AG-NE was significantly enhanced in comparison with that from the AG suspension, with a relative bioavailability of 594." | ( Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide. Chen, YC; Wang, CC; Wu, MT; Wu, YT; Yen, CC, 2018) | 0.48 |
"We conclude that the developed AG-NE not only enhanced the oral bioavailability of AG in this study but may also prove to be an effective formulation of AG for preventing gastrointestinal inflammatory disorders." | ( Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide. Chen, YC; Wang, CC; Wu, MT; Wu, YT; Yen, CC, 2018) | 0.48 |
" We have demonstrated the utility of PAMAM dendrimers for enhancing solubility, stability and oral bioavailability of various drugs." | ( Dendrimers for Drug Delivery. Chauhan, AS, 2018) | 0.48 |
" However, oral bioavailability of JBP485 is limited due to the impaired absorptive function during intestinal injury." | ( Resveratrol enhances the protective effects of JBP485 against indomethacin-induced rat intestinal damage in vivo and vitro through up-regulating oligopeptide transporter 1 (Pept1). Huo, X; Liu, K; Liu, Z; Ma, X; Meng, Q; Shu, R; Sun, H; Sun, P; Wang, C; Wu, J, 2019) | 0.75 |
" Saccharification increases the functionality and bioavailability of these compounds thus can aid in the development of a natural product based medicine." | ( Protective effects of triple fermented barley extract (FBe) on indomethacin-induced gastric mucosal damage in rats. Bashir, KMI; Cho, HR; Choi, JS; Jung, GW; Ku, SK; Lim, JM; Park, DC; Park, SJ; Song, CH, 2019) | 0.75 |
"We previously found that ophthalmic formulations containing nanoparticles prepared by a bead mill method lead to an increase in bioavailability in comparison with traditional formulations (solution type)." | ( Energy-dependent endocytosis is responsible for drug transcorneal penetration following the instillation of ophthalmic formulations containing indomethacin nanoparticles. Kawasaki, N; Nagai, N; Nakazawa, Y; Ogata, F; Otake, H, 2019) | 0.71 |
"The current study proposes an original oral delivery system for the bioavailability enhancement of indomethacin (IND), a BCS class II drug, with the aim to overcome the common limitations of amorphous solid dispersion." | ( Exploring the use of spray congealing to produce solid dispersions with enhanced indomethacin bioavailability: In vitro characterization and in vivo study. Albertini, B; Beggiato, S; Bertoni, S; Dalpiaz, A; Ferraro, L; Passerini, N, 2019) | 0.96 |
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
"The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs." | ( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020) | 0.56 |
" This study revealed fundamental mechanisms of PVP/PC mixture effect on IND supersaturation and oral bioavailability, demonstrating that polymer/lipid mixture could be used as a promising carrier to alter supersaturation profile and oral bioavailability of SDDS products." | ( Polymer/lipid interplay in altering in vitro supersaturation and plasma concentration of a model poorly soluble drug. He, L; Huang, J; Mao, Y; Peng, R; Wang, C; Wang, L; Wei, W; Wen, Y; Xia, T; Yang, J; Zhao, L, 2020) | 0.56 |
" However, its oral bioavailability is low (8%) possibly due to cleavage at the upper gut." | ( Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits. Borg, TM; El Naggar, EE; El-Sheakh, AR; Hamed, MF; Mohamed, EA, 2020) | 0.8 |
" They are therefore considered an important tool in improving oral bioavailability of such APIs." | ( The influence of polymeric excipients on desupersaturation profiles of active pharmaceutical ingredients. 1: Polyethylene glycol. Ji, Y; Sadowski, G; Schneider, R; Taspinar, L, 2020) | 0.56 |
"Endothelial dysfunction is associated with a reduced bioavailability of nitric oxide (NO)." | ( Long-term nitric oxide synthase inhibition prevents 17β-estradiol-induced suppression of cyclooxygenase-dependent contractions and enhancement of endothelium-dependent hyperpolarization-like relaxation in mesenteric arteries of ovariectomized rats. Leung, SWS; Shi, Y, 2020) | 0.56 |
"Amorphous solid dispersion (ASD) is a formulation strategy extensively used to enhance the bioavailability of poorly water soluble drugs." | ( The design and development of high drug loading amorphous solid dispersion for hot-melt extrusion platform. Andrews, GP; Jacobs, E; Jones, DS; McCoy, CP; Tian, Y; Wu, H, 2020) | 0.56 |
"Supersaturating drug delivery systems are used to achieve higher oral bioavailability for poorly soluble drugs." | ( Mechanisms for the Slowing of Desupersaturation of a Weak Acid at Elevated pH. Bogner, RH; Li, N; Manchanda, A, 2020) | 0.56 |
"The use of eye drops is a well-established practice in the treatment of ophthalmic diseases, although the bioavailability of traditional eye drops, which are either solutions or suspensions, is insufficient, as the corneal barrier and dilution by lacrimation prevent the transcorneal penetration of drugs." | ( [Ocular Drug Delivery System-based on Solid Nanoparticles]. Nagai, N, 2021) | 0.62 |
" The pseudo-second-order model was successfully used to describe the oil absorption behavior, and the obtained absorption rate constant increased with increasing PHBV content." | ( Nonsolvent-induced phase separation of poly(3-hydroxybutyrate) and poly(hydroxybutyrate-co-hydroxyvalerate) blend as a facile platform to fabricate versatile nanofiber gels: Aero-, hydro-, and oleogels. Choi, J; Kang, J; Yun, SI, 2021) | 0.62 |
" Noteworthily, current researches around co-amorphous system (CAS) are mostly focused on preparation and characterization of these systems, but more detailed investigations of their supersaturation ("spring-parachute" process), stability, in vivo bioavailability and molecular mechanisms are inadequate and need to be clarified." | ( "Felodipine-indomethacin" co-amorphous supersaturating drug delivery systems: "Spring-parachute" process, stability, in vivo bioavailability, and underlying molecular mechanisms. Cai, JH; Cui, BJ; Feng, B; Guan, J; Hao, CY; Jin, Y; Li, YW; Qi, XR; Shi, NQ; Wang, D; Zhang, HM; Zhu, HY, 2021) | 1 |
" The therapeutic effects of drug molecules are majorly dependent on the bioavailability and, in essence, on the solubility of the used drug molecules." | ( Exploration on the drug solubility enhancement in aqueous medium with the help of endo-functionalized molecular tubes: a computational approach. Paul, R; Paul, S, 2021) | 0.62 |
"Targeted therapy from cells to mitochondria can improve the bioavailability and therapeutic effects of drugs." | ( FC-BBR/IND-induced glucose oxidase nanodrugs for targeted combination therapy. Cheng, Y; Ji, Y; Ouyang, D, 2022) | 0.72 |
"Rebamipide (REB) a potent anti-ulcer agent, has not been exploited to its full potential, owing to it extremely poor solubility, leading to highly diminutive bioavailability (<10%)." | ( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies. Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021) | 0.62 |
"5 folds enhancement in relative bioavailability and remarkable amplification in anti-ulcer, anti-inflammatory and the antioxidant potential of these cocrystals were observed." | ( Engineering a Remedy to Modulate and Optimize Biopharmaceutical Properties of Rebamipide by Synthesizing New Cocrystal: In Silico and Experimental Studies. Chadha, R; Dureja, J; Jindal, A; Karan, M; Singh, R; Tomar, S, 2021) | 0.62 |
" Both, [Formula: see text]- and A-IM are preferred over the more common [Formula: see text]- crystalline form, as they exhibit better water solubility, which can increase the oral bioavailability of the drug." | ( Non-destructive crystallinity assessment of indomethacin in tablets made from smartFilms Castro-Camus, E; Heidrich, L; Keck, CM; Koch, M; Ornik, J; Schesny, R, 2022) | 0.98 |
"Solubility and dissolution rate are essential for the oral absorption and bioavailability of poorly soluble drugs." | ( Combination of co-crystal and nanocrystal techniques to improve the solubility and dissolution rate of poorly soluble drugs. Bodmeier, R; Huang, Z; Staufenbiel, S, 2022) | 0.72 |
" The hydrophilic surface of the nanocellulose was modified using cetyltrimethylammonium bromide (CTAB) cationic surfactant to improve loading capacity of hydrophobic indomethacin drug which has a low bioavailability and poor solubility in water." | ( Extraction of carboxylated nanocellulose from oat husk: Characterization, surface modification and in vitro evaluation of indomethacin drug release. Bagheri, M; Dehkhoda, S; Heydari, M; Rabieh, S, 2022) | 1.12 |
"1% w/v hydroxypropyl-β-cyclodextrin-based eye drop formulation and its bioavailability is limited by several drawbacks such as the nasolacrimal duct draining, the reflex blinking and the low volume of the conjunctival sac." | ( Chitosan/sulfobutylether-β-cyclodextrin based nanoparticles coated with thiolated hyaluronic acid for indomethacin ophthalmic delivery. Arduino, I; Cutrignelli, A; Denora, N; Franco, M; Laquintana, V; Lopalco, A; Lopedota, A; Racaniello, GF; Ricci, F; Sigurdsson, HH, 2022) | 0.94 |
" These molecules have a limited bioavailability because of their low aqueous solubility, poor water wettability and low dissolution rate." | ( Comparison study of physicochemical and biopharmaceutics properties of hydrophobic drugs ground by two dry milling processes. Chamayou, A; Dandignac, M; Galet, L; Lacerda, SP, 2022) | 0.72 |
" The growth and lipid accumulation of Chlorella pyrenoidosa added with SP were enhanced, given their high bioavailability of the nutrients." | ( Focus on the role of synthetic phytohormone for mixotrophic growth and lipid accumulation by Chlorella pyrenoidosa. Guo, L; Jin, C; Wang, Y; You, X; Yu, J; Zhao, Y, 2022) | 0.72 |
" Aiming to improve bioavailability and efficacy, a poloxamer-based thermoresponsive in-situ gelling system containing hyaluronic acid and indomethacin was developed." | ( Thermoresponsive in-situ gel containing hyaluronic acid and indomethacin for the treatment of corneal chemical burn. Augusto de Castro, M; Fernandes, C; Geraldo de Sousa, R; Henrique Reis, P; Ligório Fialho, S; Silva-Cunha, A; Toshio Inoue, T, 2023) | 1.35 |
" This feature makes L-HPC particularly suitable as ASD carriers for fine tuning of supersaturation to achieve enhanced bioavailability for poorly soluble drugs." | ( Amorphous solid dispersions in high-swelling, low-substituted hydroxypropyl cellulose for enhancing the delivery of poorly soluble drugs. Christinne Rocha de Medeiros Schver, G; Danda, LJA; Felts de La Roca Soares, M; Lamartine Soares Sobrinho, J; Lee, PI, 2023) | 0.91 |
Oral administration of IAC dosed at 50 and 100 mg/kg was able to significantly prevent gastric ulceration induced by indomethacin and by stress. Prednisolone and indomet hacin also reduced the periosteal reaction when administered from one day before injection with FCA.
Excerpt | Relevance | Reference |
---|---|---|
" Step 7 spermatids decreased significantly at both dosage levels of PGE2 and at the higher dosage level of PGE1." | ( The effect of prostaglandins and prostaglandin inhibitors on spermatogenesis. Abbatiello, ER; Kaminsky, M; Weisbroth, S, 1975) | 0.25 |
" The angiotensin dose-response curves of tachyphylactic organs were shifted to the right, and the maximum responses were depressed in proportion to the conditioning doses of the hormone." | ( Specific desensitization (tachyphylaxis) of the guinea pig ileum to angiotensin II. Mendes, GB; Paiva, AC; Paiva, TB, 1977) | 0.26 |
" Parallel dose-response curves to bradykinin were observed in the presence of increasing amounts of indomethacin." | ( Indomethacin in low concentration potentiates the actions of some spasmogens on the isolated oestrous rat uterus. Sharma, JN; Zeitlin, IJ, 1977) | 1.92 |
"The effects of different antirheumatic drugs administered according to various dosing regimes on tuberculin hypersensitivity in rats have been assessed quantitating the changes of exudate volume and mononuclear cells immigration at the site of challenge." | ( Delayed hypersensitivity to tuberculin in rats: effects of antirheumatic drugs. Arrigoni-Martelli, E; Binderup, L; Bramm, E, 1979) | 0.26 |
" Salicylamide, an analgesic without effect on the prostaglandin synthesis was in the oral exposition test of 18 patients with proved analgesics-asthma-syndrome in the dosage of 500 mg subjectively and objectively tolerated without reaction." | ( [Salicylamide-- a potential pain-remedy alternative in the analgesic asthma syndrome]. Hummel, S; Jäger, L; Slapke, J, 1979) | 0.26 |
" The slope of the dose-response regression line for colchicine differs significantly from that of indomethacin and phenylbutazone." | ( Mechanism of action of colchicine. III. Antiinflammatory effects of colchicine compared with phenylbutazone and indomethacin. Chang, YH, ) | 0.56 |
" On the rat isolated uterus, angiotensin II and the heptapeptide displayed non-parallel dose-response curves." | ( A comparison of the effects of angiotensin II and heptapeptide on smooth muscle (vascular and uterine). HAll, MM; Khairallah, PA; Moore, AF, 1976) | 0.26 |
" Dose-response curves of classical hyperbolic shape are obtained in the first three preparations, but not in the others." | ( Application of drug receptor theories to the analysis of the myotropic effects of bradykinin. Barabe, J; Park, WK; Regoli, D, 1975) | 0.25 |
" It was planned that, unless withdrawn, patients from matched pairs received either flurbiprofen (150 mg to 300 mg daily) or indomethacin (75 mg to 150 mg daily) over a minimum period of 6 months, dosage being adjusted to suit exacerbations and remission of disease." | ( A comparative study of the long-term efficacy of flurbiprofen and indomethacin in the treatment of rheumatoid arthritis, with special reference to iron metabolism. Bulgen, DY; Hazleman, BL, 1977) | 0.7 |
" Lowering the antigen (ovalbumin) dosage from 400 microgram/ml to 10 microgram/ml reduced the control release of SRS-A by 70% and increased the inhibitory effect of prostaglandins I2, E1 and isoprenaline." | ( A possible modulatory role for prostacyclin (PGI2) INIgGa-induced release of slow-reacting substance of anaphylaxis in rats. Burka, JF; Garland, LG, 1977) | 0.26 |
"To investigate the effect of the therapeutic dosage (50 approximately 100 mg/day) of indomethacin (IDM), which is well-known to inhibit the synthesis of prostaglandins, on the human pituitary-gonadal axis, five experiments were performed." | ( [Studies on the effect of the therapeutic dosage of indomethacin on human gonadotropin secretion (author's transl)]. Ofuji, N, 1978) | 0.73 |
"A report is given on a long-term controlled trial in which diclofenac sodium (Voltaren) was compared with indomethacin in 36 patients with rheumatoid arthritis, both drugs being administered in a dosage of 75-125 mg daily." | ( The long-term efficacy and tolerability of Voltaren (diclofenac sodium) and indomethacin in rheumatoid arthritis. Bijlsma, A, 1978) | 0.7 |
" at the dosage of 100 mg/day for 12 days." | ( Parenteral administration of ketoprofen in osteoarthritis: a double-blind trial versus the N-methyl-d-glucamine salt of indomethacin. Franchi, R; Liverta, C; Pollini, C; Pontiroli, AE, 1979) | 0.47 |
" Indomethacin--in the same test--was 37 times more potent than A-162-ester and the PGI2 inhibition and ulcerogenic dose-response curves for indomethacin were parallel." | ( A new anti-inflammatory derivative of imidazole which is less ulcerogenic than indomethacin in rats. Corell, T; Jensen, KM; Splawinski, J, 1979) | 1.4 |
", with subsequent dosage adjustments according to response." | ( An open assessment of the efficacy and tolerability of diclofenac sodium (Voltarol) in patients with rheumatic disease and a comparative study of diclofenac sodium (Voltarol) with indomethacin in patients with osteoarthritis and rheumatoid arthritis. Cash, HC; McMahon, MF, 1979) | 0.45 |
" This article attempts to critically review these studies under seven different sections: furosemide pharmacokinetics in normal volunteers, furosemide pharmacokinetics in patients with decreased renal function, furosemide pharmacokinetics in patients with congestive heart failure, furosemide metabolism and assay methods, furosemide bioavailability, dose-response relationships, and the role of inhibitors and mediators on furosemide effects." | ( Pharmacokinetics/pharmacodynamics of furosemide in man: a review. Benet, LZ, 1979) | 0.26 |
") shifted all the dose-response curves for PGF2 alpha (i." | ( Central cardiovascular and thermal effects of prostaglandin F2 alpha in rats. Eskeli-Kaivosoja, A; Karppanen, H; Sirén, AL, 1979) | 0.26 |
" Sublingual isoproterenol (Isuprel) has been effective in a few cases but the every-two-hour dosage schedule is inconvenient on a long-term basis." | ( Primary pulmonary hypertension. Responses to indomethacin, terbutaline, and isoproterenol. Person, B; Proctor, RJ, 1979) | 0.52 |
" Pronase given in a small dosage as proteolytic enzyme aerosol only to the upper part of the airtract sensitises the lower part of the airways against acetylcholine." | ( Effect of intra-uterine administration of indomethacin on ovarian steroids. Aizawa, Y; Kogo, H; Takahashi, M, 1979) | 0.52 |
" The degree of gastric or intestinal irritation seen with dosing of other drugs was as follows; indomethacin greater than diclofenac Na greater than ibuprofen greater than aspirin greater than phenylbutazone or indomethacin greater than CH-800 = diclofenac Na greater than ibuprofen greater than phenylbutazone, respectively." | ( [Irritative activity of a new anti-inflammatory agent 4-(p-chorophenyl)-2-phenyl-5-thiazoleacetic acid (CH-800) on the gastrointestinal tract in rats (author's transl)]. Ohtsuki, H; Okabe, S; Tabata, K, 1979) | 0.48 |
" The progressive increase in fractional sodium excretion with the amounts of injected factor shows a dose-response curve." | ( Production and action of a natriuretic hormone in isolated rat kidneys: necessity of prostaglandins for its release. Cambier, P; Godon, JP, 1979) | 0.26 |
" These results suggest that Y-8004 may make feasible a reduction in dosage or a withdrawal of the steroid prescription." | ( [Pharmacological studies of 2-(5H-(1)benzopyrano[2,3-b]pyridin-7-yl)propionic acid (Y-8004). (3) Its interaction with anti-inflammatory agents]. Foto, K; Imayoshi, T; Kadobe, Y; Maruyama, Y, 1977) | 0.26 |
"The stability of liquid dosage forms of ethacrynic acid (1 mg/ml), indomethacin (2 mg/ml), methyldopate hydrochloride (25 mg/ml), prednisone (0." | ( Stability of pediatric liquid dosage forms of ethacrynic acid, indomethacin, methyldopate hydrochloride, prednisone and spironolactone. Das Gupta, V; Ghanekar, AG; Gibbs, CW, 1978) | 0.73 |
" Oviductal segments removed 2 h after endotoxin (26 h after hCG) showed electrical activity confined to the ampullary-isthmic-junction (AIJ), where ova were located; the dose-response curve for PE was shifted to the right and the maximum contraction was depressed." | ( Accelerated ovum transport in rabbits induced by endotoxin II. Changes in oviductal smooth muscle activity. Harper, MJ; Hodgson, BJ; Valenzuela, G, 1978) | 0.26 |
" Measurement of plasma indomethacin concentrations in sick, low-birthweight infants could help guide indomethacin dose and dosage interval, prevent drug accumulation, and reduce toxicity." | ( Indomethacin disposition and indomethacin-induced platelet dysfunction in premature infants. Berman, W; Friedman, Z; Maisels, MJ; Marks, KH; Vesell, ES; Whitman, V, ) | 1.88 |
" The effect of melittin was maximum at about 25 ng/ml, and the dose-response curve was biphasic." | ( Stimulation of prostaglandin production in bone by phorbol diesters and melittin. Delclos, B; Ivey, JL; Levine, L; Tashjian, AH, 1978) | 0.26 |
" Both drugs were injected intraperitoneally at the dosage of 4 mg/kg body weight daily during a 6-day period into 40 rats rendered nephritic by rabbit nephrotoxic serum injection." | ( Indomethacin and lysine acetylsalicylate in rats with autologous nephrotoxic serum nephritis. Biochemical and morphological studies. Cioffi, A; Conte, F; Di Belgiojoso, GB; Donati, MB; Saruggia, M; Sessa, A, 1978) | 1.7 |
" Higher dosage of indomethacin (5 mg/kg), on the contrary, markedly reduced the urinary kallikrein excretion." | ( The renal kallikrein-kinin system in various types of diuresis and under the effects of inhibitors of prostaglandin synthesis in rats. Nekrasova, AA; Shkhvatsabaya, IK; Zharova, EA, 1978) | 0.59 |
" The two drugs were each given in a dosage of 150 mg daily for a period of 14 days." | ( Clinical evaluation of ketoprofen (19.583 R.P.) in rheumatoid arthritis. Double-blind cross-over comparison with indomethacin. Fossgreen, J; Kirchheiner, B; Petersen, FO; Tophoj, E; Zachariae, E, 1976) | 0.47 |
" Further studies are underway to assess the value of ketoprofen administered in high dosage for longer duration." | ( A comparative trial of large doses of ketoprofen and indomethacin in the treatment of rheumatoid arthritis. El-Ghobarey, AF; Hadidi, T; Hamid, HA; Mavrikakis, M; Rennie, JA, 1976) | 0.51 |
"During a double-blind, randomized study on 30 patients affected with classic or definite rheumatoid arthritis, the efficacy and safety of treatment with diftalone in a per oral dosage of 500 mg/day were compared with those of indomethacin given orally at doses of 50-75 mg/day initially and 100 mg/day subsequently, for a treatment period of 24 months." | ( Comparative clinical trial with a new substance, Diftalone, versus indomethacin in 30 patients affected with rheumatoid arthritis. Bröll, H; Dunky, A; Eberl, R; Tausch, G, 1976) | 0.68 |
" In constrast, 3H-indometacin injected like ASA and PBZ in subtherapeutic dosage diappeared from the blood in a threephasic process." | ( [Antiphiogistic drugs. Sudies on the pharmocokinetics of anti-inflammatory agents]. Havemann, D, 1977) | 0.26 |
" Increases in dosage of PGE2 produced a progressive reduction in mean blood pressures, heart, and kidney weights." | ( Effects of prostaglandin E2 and prostaglandin inhibitors on adrenal regeneration hypertension. Eversole, WJ; Paulson, DJ, 1977) | 0.26 |
" Prednisolone and indomethacin also reduced the periosteal reaction when administered from one day before injection with FCA, but they were inactive in this respect when dosing was started on day 21 when the periosteal reaction was well established." | ( An X-ray analysis of adjuvant arthritis in the rat. The effect of prednisolone and indomethacin. Blackham, A; Burns, JW; Farmer, JB; Radziwonik, H; Westwick, J, 1977) | 0.82 |
" This method has provided us with an accurate evaluation of the corticosteroid dose-response curve and the effect of bases." | ( Effect of bases and accelerants on the anti-inflammatory activity of topical corticosteroids. Gaylarde, PM; Sarkany, I, 1976) | 0.26 |
" The dosage of PGEs required was 1 to 4 mug/kg/min." | ( Studies on the effects of prostaglandins E1, E2, A1, and A2 on the dustus arteriosus of swine in vivo using cineangiography. Elliott, RB; Elliott, RL; Neutze, JM; Starling, MB, 1976) | 0.26 |
" Dosing with D-penicillamine (25 mg/kg) and levamisole (5 mg/kg) at the time of challenge produced a significant enhancement of the reaction." | ( Pertussis vaccine pleurisy: a model of delayed hypersensitivity. Arrigoni-Martelli, E; Dieppe, PA; Huskisson, EC; Willoughby, DA, 1976) | 0.26 |
" When a total daily dose of 150 mg was given as 25 mg every 4 hours peak concentrations were the same but fluctuations were smaller and average concentrations were higher than with a dosage of 50 mg every 8 hours." | ( Indomethacin serum concentrations in man. Effects of dosage, food, and antacid. Bluestone, R; Champion, GD; Emori, HW; Paulus, H; Pearson, C, 1976) | 1.7 |
"The dose-response effect of PGF2alpha on the perfused oviduct of estrous and ovariectomized rabbits was determined." | ( Dose-response effects of prostaglandin F2alpha on the rabbit oviduct: reproductive endocrine influence and tachyphylaxis. Heilman, RD; Strainer, SM, 1976) | 0.26 |
" The dose-response curve for the thyroid gland factor was not parallel to that obtained using PTH and secretion was not under calcium control." | ( Secretion of a bone resorbing factor by chick thyroid glands in organ culture. Feinblatt, JD; Leone, RG; Tai, LR, 1976) | 0.26 |
" For higher initial contractions relaxation is slowed during the first minute of wash out, probably because of the sigmoid shape of the dose-response curve." | ( Relaxation of splenic strips during wash out with amine-free solution after an exposure to noradrenaline. Lindmark, E; Schlör, G; Trendelenburg, U, 1976) | 0.26 |
" Ibuprofen showed suppression in most tissues three hours after dosing with a return to control values by twenty-four hours." | ( In vivo suppression of prostaglandin biosynthesis by non-steroidal anti-inflammatory agents. Fitzpatrick, FA; Wynalda, MA, 1976) | 0.26 |
"Nordihydroguaiaretic acid inhibits prostaglandin (PG) biosynthesis in vitro (ID50=228 muM), with a slope of dose-response curve high (b=209) as compared with indomethacin (ID50=0." | ( Antioxidants as agents potentiating the antiinflammatory action of indomethacin. Cebo, B; Kieć-Dembińska, A; Krupińska, J; Mazur, J; Sobański, H, 1976) | 0.69 |
" Because of variation in the levels reached using a fixed dosage schedule, treatment should be individualised." | ( Salicylate therapy and drug interaction in rheumatoid arthritis. Barraclough, DR; Laby, B; Muirden, KD, 1975) | 0.25 |
" The very shallow dose-response curves for flurbiprofen compared with acetylsalicylic acid, especially in the mouse and the rat test systems, are not due to an unreliable or abnormal absorption, which suggests that in these species the mode of action of flurbiprofen is not identical with that of acetylsalicylic acid." | ( Some biological properties of flurbiprofen, an anti-inflammatory, analgesic and antipyretic agent. Adams, SS; McCullough, KF; Nicholson, JS, 1975) | 0.25 |
" Teoremac was given for 14 days at a dosage of 420 mg/day." | ( The therapeutic activity of 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid monohydrate glucosamide in rheumatoid arthritis (double blind trial). Capelli, L; Chianese, U; Giordano, M, 1975) | 0.25 |
" Indomethacin was rapidly and well absorbed after oral dosing with peak plasma concentrations within 2 hr." | ( Pharmacokinetics of indomethacin. Alván, G; Bertilsson, L; Ekstrand, R; Orme, M; Palmér, L, 1975) | 1.49 |
" One daily oral indomethacin dosage of 10 mg/kg body weight given for 3 weeks inhibited resorption of bone autografts in this type of vital chamber and thus inhibited disordered osteoclastic activity." | ( Effect of indomethacin on bone remodelling in rabbit ear chambers. Sudmann, E, 1975) | 1 |
" After three weeks to four months, the drug dosage could be tapered and discontinued." | ( Indomethacin treatment of pericarditis in chronic hemodialysis patients. Eknoyan, G; Minuth, AN; Nottebohm, GA; Suki, WN, 1975) | 1.7 |
" Prednisone in high dosage was associated in this series with 9 deaths and in 6 patients, with renal failure or an extra-renal complication." | ( [Lupus nephropathy. Treatment with the indomethacin-hydroxychloroquine combination and comparison with corticoids]. Conte, JJ; Fournie, GJ; Mignon-Conte, MA, 1975) | 0.52 |
" Cumlative dose-response curves (10-9-10-6M BK or NE) were done in the presence and absence of INDO (10-6M)." | ( Effects of indomethacin on venoconstrictor responses to bradykinin and norepinephrine. Goldberg, MR; Greenberg, S; Hyman, AL; Joiner, PD; Kadowitz, PJ, 1975) | 0.64 |
" Six mature female monkeys were treated with HMG-HCG for at least 2 control ovulatory cycles at dosage levels adjusted to induced ovulation while avoiding superovulation." | ( The effect of indomethacin of HMG-HCG induced ovulation in the phesus monkey. Cruz, A; Hunt, J; Stevens, VC; Wallach, EE; Wright, KH, 1975) | 0.62 |
" Dose-response relationships were demonstrated by topical and oral administration of Indomethacin which, as expected, had no effect on PGE2." | ( Arachidonic acid-induced elevation of intraocular pressure and anti-inflammatory agents. Conquet, P; Le Douarec, JC; Plazonnet, B, 1975) | 0.48 |
" The dose of agonist that produced a 35% fall in specific airways conductance (PD35 SGaw) was obtained by linear interpolation from the logarithmic dose-response curve." | ( Effect of indomethacin on leukotriene4-induced histamine hyperresponsiveness in asthmatic subjects. Christie, PE; Hawksworth, R; Lee, TH; Spur, BW, 1992) | 0.69 |
" Whereas IL-1 alpha and IL-1 beta significantly inhibited pentagastrin-stimulated acid secretion, the dose-response relationship and time course of actions suggested that effects on acid secretion did not fully account for the ability of these agents to reduce indomethacin-induced gastric injury." | ( Mechanisms underlying the protective effects of interleukin 1 in experimental nonsteroidal anti-inflammatory drug gastropathy. Cucala, M; Keenan, CM; Mugridge, KG; Parente, L; Wallace, JL, 1992) | 0.46 |
" The protective effect of inhibitors when administered before, but not after, 3MI dosing suggests it is the inhibition of PHS activity in activation of 3MI, not in production of prostanoids which prevented the disease process." | ( The role of prostaglandin H synthase in 3-methylindole-induced pneumotoxicity in goat. Acton, KS; Boermans, HJ; Bray, TM, 1992) | 0.28 |
" Dose-response curves of epithelium-denuded tracheas were shifted to the left by approximately one order of magnitude." | ( Endothelins constrict guinea pig tracheas by multiple mechanisms. Hasegawa, S; Hirata, F; Matsumoto, H; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y, 1992) | 0.28 |
") caused a rightward displacement of dose-response curves to Ang II or Ang III in both the mesenteric and renal vasculature." | ( A comparison of the characteristics of angiotensin receptors in the renal and mesenteric vascular beds of the anesthetized cat. Clark, KL; Drew, GM; Robertson, MJ, 1992) | 0.28 |
" A cicletanine concentration, which is attained by the dosage given to patients, is sufficient to produce these effects." | ( Potassium channel activation in vascular smooth muscle. Emden, J; Mironneau, J; Siegel, G; Stock, G; Wenzel, K, 1992) | 0.28 |
" In dose-response studies, INDO increased the systolic BP response but decreased the ANP response to AII, which is consistent with a direct effect of PG on ANP that is independent of systolic BP." | ( Prostaglandins and systolic blood pressure, but not angiotensin II, independently affect atrial natriuretic peptide levels in man. Finn, WL; Gordon, RD; Hornych, A; Klemm, SA; Tunny, TJ, 1992) | 0.28 |
" The mean dosage of pethidine used was 24 mg +or- 27 mg in the indomethacin group and 42 mg +or- 44 mg in the placebo group." | ( Preoperative rectal indomethacin for analgesia after laparoscopic sterilisation. Crocker, S; Paech, M, 1992) | 0.85 |
"The effects of chronic superficial injury on the stomach were studied in rats dosed with a mild irritant (2 mol/L NaCl intragastrically) every 48 hours for 1 month followed by 1-month recovery." | ( Effects of chronic superficial injury on the rat gastric mucosa. Cowart, KS; Hund, P; Lacy, ER, 1992) | 0.28 |
"Between 26 and 32 weeks' gestation, a single dosage of indomethacin or terbutaline increases fetal breathing movements by 103% and 78%, respectively." | ( The effect of tocolytic agents (indomethacin and terbutaline) on fetal breathing and body movements: a prospective, randomized, double-blind, placebo-controlled clinical trial. Cotton, DB; Dorman, KF; Hallak, M; Lira, N; Moise, K; Smith, EO, 1992) | 0.81 |
" during concomitant twice daily dosing with 400 micrograms misoprostol, 150 mg ranitidine or placebo." | ( Co-administration of misoprostol or ranitidine with indomethacin: effects on pharmacokinetics, abdominal symptoms and bowel habit. Gibson, R; Kendall, MJ; Walt, RP, 1992) | 0.53 |
"In a bid to minimise dosage and possible side-effects when relieving post episiotomy pain, the NSAID Indomethacin was studied in combination with a systemic haemostat Ethamsylate which has been shown to selectively inhibit some prostaglandins." | ( Indomethacin and ethamsylate alone and in combination for the relief of post episiotomy pain. Devitt, M; Harrison, RF, 1992) | 1.94 |
" We concluded that indomethacin, in the dosage schedule and regimen that we used, provides effective prophylaxis for heterotopic ossification after a Chiari pelvic osteotomy." | ( Prophylaxis with indomethacin for heterotopic ossification after Chiari osteotomy of the pelvis. Randelli, G; Romanò, CL, 1992) | 0.95 |
" The volume of UNDW causing a 20% fall in FEV1 (UNDW PD20) was calculated by linear interpolation on the dose-response curve." | ( Protective activity of inhaled nonsteroidal antiinflammatory drugs on bronchial responsiveness to ultrasonically nebulized water. Bianco, S; Pieroni, MG; Refini, RM; Robuschi, M; Sestini, P; Vaghi, A, 1992) | 0.28 |
" Thirty-six infants were selected to receive a continuous infusion of either placebo or dopamine at either a low dosage of 2 micrograms/kg per minute or a higher dosage of 5 micrograms/kg per minute, beginning 6 hours before the use of indomethacin and continuing until 12 hours after the third dose of indomethacin." | ( Effect of dopamine on failure of indomethacin to close the patent ductus arteriosus. Fajardo, CA; Steele, BT; Whyte, RK, 1992) | 0.75 |
"In this report we describe the conditions of collection, storage and handling of urine samples, collected after oral dosing with indomethacin in man, in order to maintain the integrity of the labile glucuronide formed." | ( Clearance of indomethacin occurs predominantly by renal glucuronidation. Crancrinus, S; De Zeeuw, D; Meijer, DK; Moolenaar, F; Visser, J, 1992) | 0.86 |
"6MNA, the active metabolite of the non-acidic anti-inflammatory drug nabumetone, was investigated using intravenous administration for effects on (a) carrageenan paw oedema and gastric irritancy compared to either oral nabumetone or both oral and intravenous indomethacin when given acutely and (b) gastrointestinal irritancy when given in repeat dosing studies." | ( Anti-inflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6MNA (6-methoxy-2-naphthylacetic acid): comparison with indomethacin. Blower, PR; Gentry, C; Kelvin, AS; Melarange, R; Neil, C; O'Connell, C; Toseland, CD, 1992) | 0.66 |
"6MNA, the active metabolite of the nonacidic antiinflammatory drug nabumetone, was investigated using intravenous administration for effects on (1) carrageenan paw edema and gastric irritancy compared with either oral nabumetone or both oral and intravenous indomethacin when given acutely and (2) gastrointestinal irritancy when given in repeat dosing studies." | ( Antiinflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Comparative studies with indomethacin. Blower, PR; Gentry, C; Kelvin, AS; Melarange, R; Neil, C; O'Connell, C; Toseland, CD, 1992) | 0.66 |
" A skin biopsy was taken at 24 h after each dosing with UVB." | ( Synergistic effects of oral nonsteroidal drugs and topical corticosteroids in the therapy of sunburn in humans. Bohan, DF; Caruana, C; Francom, SF; Holland, M; Hughes, GS; Means, LK, 1992) | 0.28 |
" We recommend the use of MA for closure of symptomatic PDA in preterms, especially in those cases where indomethacin is not tolerated or when minute titration of its dosage is impracticable." | ( Therapy of symptomatic patent ductus arteriosus in preterms using mefenemic acid and indomethacin. Merchant, RH; Sakhalkar, VS, 1992) | 0.72 |
" They showed intolerance to Indo at a dosage of 14 micrograms/ml, which was well tolerated by other mouse strains in previous studies, but tolerated the Ibu dosages used." | ( Immunotherapy of mammary adenocarcinoma metastases in C3H/HeN mice with chronic administration of cyclo-oxygenase inhibitors alone or in combination with IL-2. Chan, FP; Khoo, NK; Lala, PK; Saarloos, MN, 1992) | 0.28 |
" WCM stimulated adenylate cyclase in osteoblast like cells, the dose-response curve paralleling that of hPTHrP(1-34)." | ( Osteolytic activity of Walker carcinosarcoma 256 is due to parathyroid hormone-related protein (PTHrP). Grohe, U; Krieg, P; Lempert, UG; Maurer, E; Minne, HW; Rappel, S; Scharla, SH; Ziegler, R, 1991) | 0.28 |
" L-Serine borate (45 mM), an inhibitor of gamma-glutamyl transpeptidase, shifted the dose-response curve of LTC4 to the left by 161-fold, and L-cysteine (6 mM), an inhibitor of aminopeptidase, shifted the dose-response curves of LTC4 and LTD4 to the left by 67- and 23-fold, respectively." | ( Characterization of sulfidopeptide leukotriene responses in sheep tracheal smooth muscle in vitro. Abraham, WM; Jackowski, JT; Tomioka, K, 1991) | 0.28 |
" Perindopril alone tended to reduce serum and urinary thromboxane B2 (TxB2) and to raise urinary 6-ketoPGF1 alpha and PGE2 and inhibited serum ACE activity 24 h post dosing by about 85%." | ( Hemodynamic and humoral interactions between perindopril and indomethacin in essential hypertensive subjects. Abdel-Haq, B; Favilla, S; Magagna, A; Salvetti, A, 1991) | 0.52 |
" Studies using repeated full cumulative dose-response curves and repeated single-dosing techniques demonstrated tachyphylaxis to ET-1 in both rat and guinea pig." | ( The importance of tachyphylaxis and release of cyclooxygenase products in the modulation of endothelin-1-induced responses in rat and guinea pig tracheal chains. Kitchen, I; Peachey, JA, 1991) | 0.28 |
" A combination of FPL55712 (leukotriene antagonist), diphenhydramine (histamine antagonist), and indomethacin (cyclooxygenase inhibitor) shifted the dose-response curve of ET-1 to the right and suppressed the maximal constriction." | ( Multiple mechanisms of bronchoconstrictive responses to endothelin-1. Hasegawa, S; Hirata, F; Ishii, Y; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y, 1991) | 0.5 |
" Pretreatment with dexamethasone for 48 hours shifted the dose-response trisphosphate curves of angiotensin II- and arginine vasopressin-induced inositol trisphosphate production to the left, that is, it significantly reduced the half-maximal effective concentrations of angiotensin II (from 25 nM to 5 nM) and arginine vasopressin (from 50 nM to 25 nM)." | ( Potentiation of inositol trisphosphate production by dexamethasone. Iwaita, Y; Kato, H; Nakazato, Y; Saruta, T; Sato, A; Suzuki, H, 1992) | 0.28 |
" Allergen (Southern Grass Mix) was administered intradermally 2 h after last drug dosage and the surface areas of the immediate wheal-and-flare-reactions were measured 15 min later." | ( Effect of enalapril on allergen-induced cutaneous hypersensitivity reaction. Snyman, JR; Sommers, DK, 1991) | 0.28 |
"Infarct healing delay by prednisolone is dosage dependent, and smaller infarcts may be more sensitive to its effect." | ( Effect of prednisolone on myocardial infarct healing: characteristics and comparison with indomethacin. Iimura, O; Ishimoto, R; Itoya, M; Miura, T; Shizukuda, Y, 1991) | 0.5 |
" Mature ewes were treated during the preovulatory period with a systemic dosage of indomethacin that either consistently did (500 mg) or did not (100 mg) prevent follicular rupture." | ( Dose-dependent effects of indomethacin on ovulation in the sheep: relationship to follicular prostaglandin production, steroidogenesis, collagenolysis, and leukocyte chemotaxis. McCormick, RJ; Murdoch, WJ, 1991) | 0.81 |
" Dose-response curves were also obtained to the direct smooth muscle dilator nitroprusside during normoxia and hypoxia." | ( Effects of oxygen tension on endothelium dependent responses in canine coronary microvessels. Muller, JM; Myers, PR; Tanner, MA, 1991) | 0.28 |
" The growth factor bFGF (50 ng/ml) induced a 48% reduction versus the basal level, and a therapeutic dosage of indomethacin (1." | ( Regulation of interleukin 1 receptors in human articular chondrocytes. DiBattista, J; Martel-Pelletier, J; McCollum, R; Pelletier, JP, 1991) | 0.49 |
" The dose-response curves for the endothelium-dependent vasodilatation in response to carbachol were not significantly different in spontaneously hypertensive and Wistar-Kyoto rats." | ( Effect of destruction of the vascular endothelium upon pressure/flow relations and endothelium-dependent vasodilatation in resistance beds of spontaneously hypertensive rats. Hiley, CR; Randall, MD; Thomas, GR, 1991) | 0.28 |
" The 5-lipoxygenase inhibitor diethylcarbamazine and the LTD4/LTE4 receptor antagonist LY 171883 markedly reduced mortality in dose-response fashion." | ( Effects of some nonsteroidal anti-inflammatory agents on experimental radiation pneumonitis. Gross, NJ; Holloway, NO; Narine, KR, 1991) | 0.28 |
" Dose-response relations to norepinephrine, endothelium-dependent dilators (acetylcholine, histamine, and A23187), and nitroglycerin were done." | ( Depression of endothelium-dependent relaxation in aorta from rats with Brugia pahangi lymphatic filariasis. Kaiser, L; Lamb, VL; Tithof, PK; Williams, JF, 1991) | 0.28 |
" TNF alpha potentiated the release of [3H]arachidonate and PRL promoted by phospholipase-A2 and melittin, and markedly shifted the dose-response curve to the left." | ( Tumor necrosis factor-alpha increases release of arachidonate and prolactin from rat anterior pituitary cells. Hirota, K; Ikegami, H; Kadowaki, K; Koike, K; Miyake, A; Ohmichi, M; Tanizawa, O; Yamaguchi, M, 1991) | 0.28 |
" The four NSAID diclofenac, acemetacin, ibuprofen, and mefenamic acid administered to healthy volunteers at the recommended dosage led to significant suppression of thromboxane synthesis; this effect was more pronounced with acemetacin and ibuprofen than with diclofenac." | ( [Inhibition of thrombocyte function by non-steroidal anti-rheumatic agents: a comparative study between diclofenac, acemetacin, mefenamic acid and ibuprofen]. Raineri-Gerber, I; von Felten, A, 1991) | 0.28 |
" Comparative dose-response curves showed that gamma-IFN was most potent as inhibitor of bradykinin induced 45Ca release." | ( Inhibitory effects of gamma-interferon on bradykinin-induced bone resorption and prostaglandin formation in cultured mouse calvarial bones. Klaushofer, K; Lerner, UH; Ljunggren, O; Peterlik, M; Ransjö, M, 1991) | 0.28 |
" RPF was not consistently altered by subacute/chronic dosing of indomethacin, misoprostol, or the combination of the drugs." | ( Minimization of indomethacin-induced reduction in renal function by misoprostol. Brown, JA; Hall, PS; Klassen, DK; Schubert, C; Stromatt, SC; Voss, TE; Weir, MR, 1991) | 0.87 |
" Dose-response lines in response to the two agonists, expressed as percent maximal contraction, did not differ among the groups." | ( Muscarinic-receptor functioning in tracheas from normal and ovalbumin-sensitive guinea pigs. Biggs, DF; Yang, ZJ, 1991) | 0.28 |
"Indomethacin was given for the treatment of preterm labor in a twin pregnancy at a dosage of 200 mg/day for 7 days beginning at 34 weeks and 5 days' gestation." | ( Indomethacin for preterm labor: fetal toxicity in a dizygotic twin gestation. Ayres, NA; Hallak, M; Moise, KJ; Reiter, AA, 1991) | 3.17 |
" After hydroelectrolytic treatment, a PG synthetase inhibitor (indomethacin) was added to a dosage of 25 mg q/d PO." | ( [Treatment with indomethacin for the control of the metabolic disorder caused by a villous adenoma of the rectum]. Batalla Eiras, A; Casal Iglesias, L; Cutrin Prieto, C; Diéguez Gómez, P; Lorenzo Zúniga, V; Meniño Olveira, MJ, 1991) | 0.87 |
" Our data suggest that both the route of drug administration and dosing regimen employed affect the antiinflammatory potency and/or efficacy of compounds on colitis induced by acetic acid in the rat." | ( Antiinflammatory effects of various drugs on acetic acid induced colitis in the rat. Bostwick, JS; Decktor, DL; Fitzpatrick, LR; Pendleton, RG; Renzetti, M, 1990) | 0.28 |
" The coculture of indomethacin with interleukin-2 (IL-2) augmented LAK cell activity in an indomethacin dose-response manner, and diminished PGE2 content in the corresponding culture supernatant in a reverse dose-response manner." | ( Prostaglandin E2 from macrophages of murine splenocyte cultures inhibits the generation of lymphokine-activated killer cell activity. Chu, TM; Lin, TH; Nakajima, I; Ohnishi, H, 1991) | 0.62 |
" These mean population parameter estimates should prove useful in designing dosage regimens to achieve desired indomethacin concentrations for neonates from 0 to 20 days of age with symptomatic patent ductus arteriosus." | ( Population pharmacokinetics of intravenous indomethacin in neonates with symptomatic patent ductus arteriosus. Brown, Y; Brundage, RC; Gal, PS; Pinson, JB; Purohit, D; Ransom, JL; Schall, S; Weaver, RL; Wiest, DB, 1991) | 0.76 |
"The hemodynamic role of prostaglandins in the inflammatory phase of bone healing was studied on day 4 after creation of a nailed midtibial osteotomy in 40 rabbits, divided into groups of 10, treated with either indomethacin (oral dosage 10 mg/kg), subcutaneous (s." | ( Early hemodynamic response to tibial osteotomy in rabbits: influence of indomethacin and prostaglandin E2. Bünger, C; Hansen, ES; He, SZ; Keller, J; Kjaersgaard-Andersen, P, 1991) | 0.7 |
" Propranolol (1 mg/kg) produced a small shift to the left and atropine (1 mg/kg) and the serotonin antagonist, methysergide (1 mg/kg), produced a small shift to the right in the bombesin dose-response curve." | ( Bombesin-induced bronchoconstriction in the guinea pig: mode of action. Barnes, PJ; Belvisi, MG; Stretton, CD, 1991) | 0.28 |
" All test dosage forms were more rapidly dissolved in simulated intestinal fluid than in simulated gastric fluid." | ( Gastric acidity-dependent bioavailability of commercial sustained release preparations of indomethacin, evaluated by gastric acidity-controlled beagle dogs. Goda, T; Kawata, M; Ogawa, K; Shiotuki, T; Yamada, I, 1990) | 0.5 |
" All marmosets given 12 mg/kg/day and one marmoset given 6 mg/kg/day died during the dosing period (within 20 days)." | ( Evaluation of the toxicity of indomethacin in a 4-week study, by oral route, in the marmoset (Callithrix jacchus). Conz, A; Galli, CL; Giachetti, C; Oberto, G, 1990) | 0.57 |
"To assess the effect of indomethacin on gastric acidity and to identify a potential pharmacodynamic interaction between indomethacin and ranitidine, we measured nocturnal acidity on half-hourly aliquots of gastric contents from 10 volunteers on the seventh day of four dosing regimens given in a randomized double-blind manner." | ( Effect of ranitidine and indomethacin on nocturnal gastric acidity in normal subjects. Daneshmend, TK; Langman, MJ; Prichard, P; Walt, RP, 1990) | 0.89 |
" hLIF also stimulated incorporation of [3H] thymidine into calvaria, but the dose-response relationship was distinct from that for bone resorption, and this effect was not blocked by indomethacin." | ( Leukemia inhibitory factor: a novel bone-active cytokine. Cornish, J; Gearing, DP; Hilton, DJ; Lowe, C; Martin, TJ; Reid, LR; Skinner, SJ; Willson, TA, 1990) | 0.47 |
" Indomethacin inhibited PGI2 synthesis in a dose-response manner; at 7 x 10(-5) M, prostanoid synthesis was inhibited by greater than 80 per cent." | ( Synthesis of prostaglandins I2 and E2 by the canine gallbladder in vitro: studies using a new incubation chamber. England, DW; Hoover, EL; Jaffe, BM; Webb, H, 1990) | 1.19 |
"05) of both the vasopressin-urine osmolality and the vasopressin-urine flow dose-response curves." | ( Effect of cyclo-oxygenase blockade on the renal actions of vasopressin and SK&F 105494 in the rhesus monkey. Albrightson-Winslow, CR; Brooks, DP; Caldwell, NC; Kinter, LB; Koster, PF, 1990) | 0.28 |
" Preincubation of rat aorta with 10 microM SQ 29,548, a "selective" antagonist of thromboxane A2/prostaglandin H2 (TP) receptors, caused a rightward shift in the dose-response curve and a reduction in the maximal response to endothelin-1." | ( Role of thromboxane A2/prostaglandin H2 receptor in the vasoconstrictor response of rat aorta to endothelin. Mok, LL; Reynolds, EE, 1990) | 0.28 |
" A dose-response relationship was established between the amount of photosensitizer administered and the light dose delivered with the release of thromboxane immediately following PDT." | ( Role of thromboxane and prostacyclin release on photodynamic therapy-induced tumor destruction. Doak, KW; Fingar, VH; Wieman, TJ, 1990) | 0.28 |
" In addition, the similarity of the dose-response curves for the bradykinin-mediated increase in Ca2+, PGE2, and cAMP (half-maximal stimulation of 12, 11, and 13 nM, respectively) and the ability of the B2-antagonist (B4307) to block each of these effects of bradykinin suggest that all three effects are mediated by the same bradykinin (B2) receptor." | ( Effects of kinins on cultured arterial smooth muscle. Breckon, R; Dixon, BS; Fortune, J; Linas, SL; Marzec-Calvert, R; Stewart, JM; Vavrek, RJ, 1990) | 0.28 |
" Full dose-response curves to noradrenaline, vasopressin and potassium chloride were established." | ( Increased sensitivity to noradrenaline in glucocorticoid-treated rats: the effects of indomethacin and desipramine. Fraser, R; Kenyon, CJ; Russo, D, 1990) | 0.5 |
" In one patient with constriction a reduction of the indomethacin dosage was not associated with constriction, while in the other three, constriction was still evident at a reduced dosage." | ( Effect of indomethacin on the fetal ductus arteriosus during treatment of symptomatic polyhydramnios. Kirshon, B; Mari, G; Moise, KJ; Wasserstrum, N, 1990) | 0.93 |
" MIP-1 induced a biphasic or monophasic fever of short latency characterized by an inverse dose-response curve." | ( Macrophage inflammatory protein-1: unique action on the hypothalamus to evoke fever. Cerami, A; Davatelis, G; Fahey, T; Miñano, FJ; Myers, RD; Paez, X; Sancibrian, M; Sherry, B; Vizcaino, M, 1990) | 0.28 |
" The local therapy of alveolitis, is free of risk with solution out of Metindol--vials under dosage up to 6 milligram indomethacin substance." | ( [Etiology of alveolitis and its therapy with indomethacin]. Fischer, R; Schroeder, H, 1990) | 0.75 |
"Indomethacin dosing for patent ductus arteriosus closure has been standardized despite wide interpatient variability in indomethacin pharmacokinetics." | ( Indomethacin for patent ductus arteriosus closure. Application of serum concentrations and pharmacodynamics to improve response. Bird, A; Brown, Y; Gal, P; Ransom, JL; Schall, S; Weaver, RL, 1990) | 3.16 |
" Under this dosage schedule, cyclophosphamide and cyclosporin decreased the severity of arthritis, while indomethacin did not." | ( Effects of indomethacin, cyclosporin, cyclophosphamide, and placebo on collagen-induced arthritis of mice. Cannon, GW; Cole, BC; Griffiths, MM; McCall, S; Radov, LA; Ward, JR, 1990) | 0.88 |
" Drug studies were performed, using a 4-day dosing schedule, on optimal DTH elicited on day 10, suboptimal DTH elicited on day 15, and AA (day 16)." | ( Drug actions on delayed-type hypersensitivity in rats with developing and established adjuvant arthritis. Hambleton, P; McMahon, S, 1990) | 0.28 |
" Analgesic effect was assessed by the absolute and percentage variation in Huskisson's visual analogue scale between dosing and sampling." | ( Plasma and cerebrospinal fluid concentrations of indomethacin in humans. Relationship to analgesic activity. Bannwarth, B; Gaucher, A; Lapicque, F; Netter, P; Péré, P; Thomas, P, 1990) | 0.53 |
"9 micrograms tetrodotoxin intracamerally had no clear effect on the dose-response relationship for CCK-8." | ( Cholecystokinin causes contraction of the pupillary sphincter in monkeys but not in cats, rabbits, rats and guinea-pigs: antagonism by lorglumide. Almegård, B; Andersson, SE; Bill, A, 1990) | 0.28 |
" Anti-IgE dose-response curves reveal a region of dimeric cross-link dominance that may explain the peculiar differences observed in pharmacologic studies of basophil release induced with antigen vs anti-IgE." | ( Characteristics of human basophil sulfidopeptide leukotriene release: releasability defined as the ability of the basophil to respond to dimeric cross-links. Lichtenstein, LM; MacGlashan, DW; Peters, SP; Warner, J, 1986) | 0.27 |
" Thus, palytoxin exhibited a biphasic dose-response curve for enhanced bone resorption, with stimulation at low concentrations (0." | ( Palytoxin: an extraordinarily potent stimulator of prostaglandin production and bone resorption in cultured mouse calvariae. Fujiki, H; Lazzaro, M; Levine, L; Tashjian, AH, 1987) | 0.27 |
" In this study, we quantitated the dose-response effects of topically applied PAF on microvascular permselectivity and investigated the biochemical pathways of this compound." | ( Effect of platelet-activating factor on microvascular permselectivity: dose-response relations and pathways of action in the hamster cheek pouch microcirculation. Dillon, PK; Durán, WN, 1988) | 0.27 |
" Blocking the acetylcholine receptor shifted the dose-response relation for PGE-induced fusion to higher concentrations." | ( The control of chick myoblast fusion by ion channels operated by prostaglandins and acetylcholine. Bevan, S; Entwistle, A; Warner, AE; Zalin, RJ, 1988) | 0.27 |
"We performed three consecutive dose-response curves to rapid intravenous infusions of substance P (SP) in anesthetized, mechanically ventilated guinea pigs." | ( Enhanced airway responses to substance P after repeated challenge in guinea pigs. Drazen, JM; Shore, SA, 1989) | 0.28 |
" Dose-response curves with either arecoline or histamine on isolated tracheae from these animals display increased maximal contractions, and decreased EC50 values." | ( Endotoxin-induced hyperreactivity of the guinea-pig isolated trachea coincides with decreased prostaglandin E2 production by the epithelial layer. Engels, F; Folkerts, G; Nijkamp, FP, 1989) | 0.28 |
" Dose-response curves were obtained and statistical comparisons were based on the dose of norepinephrine producing 50% of maximal Rsma response (ED50)." | ( Prostacyclin mediates splanchnic vascular response to norepinephrine in portal hypertension. Li, SS; Lin, PW; Sitzmann, JV, 1989) | 0.28 |
" Regulation of dosage has to be individualized, and when one reaches the lower dose such as 5 to 10 mg per day, the drug may have to be tapered more slowly, or even maintained at that level for a period of time to prevent further recurrence of symptoms." | ( Cluster headaches. Ryan, RE, 1989) | 0.28 |
" This schedule was repeated at least twice more with a one-week interval between cycles, usually at the same dosage level." | ( Low-dose cyclophosphamide and low-dose interleukin-2 for malignant melanoma. Boswell, WD; Bradley, EC; Dean, G; Harel, W; Kempf, RA; Lind, S; Mitchell, MS; Moore, J; Shau, H, 1989) | 0.28 |
" The addition of indomethacin to the dosing regimen resulted in a significant increase in trough levels of CsA, indicating a drug interaction between these two compounds." | ( Pharmacokinetic analysis of cyclosporine in adjuvant arthritic rats. D'Souza, MJ; Matthews, HW; Pollock, SH, ) | 0.47 |
" The use of 20% ethanol as a dosage vehicle enhanced the protective effects of all drugs tested and the ethanol vehicle alone provided 45% protection." | ( Effects of cryptolepine alone and in combination with dipyridamole on a mouse model of arterial thrombosis. Okafor, JP; Oyekan, AO, 1989) | 0.28 |
" There was a dose-response effect for the indomethacin and aspirin groups, with higher doses having a greater inhibitory effect." | ( The effect of indomethacin, aspirin, and ibuprofen on bone ingrowth into a porous-coated implant. Mills, W; Trancik, T; Vinson, N, 1989) | 0.9 |
"3 mg/rat, or higher, and this dosage inhibited ovulation." | ( Increase in ovarian kallikrein activity during ovulation in the gonadotrophin-primed immature rat. Espey, LL; Okamura, H; Tanaka, N; Winn, V, 1989) | 0.28 |
" The dose-response relations for the increase in blood pressure of rats receiving endothelin were comparable with those of rats receiving angiotensin II." | ( Characteristics of pressor response to endothelin in spontaneously hypertensive and Wistar-Kyoto rats. Goto, K; Ishikawa, T; Ito, I; Kimura, S; Masaki, T; Miyauchi, T; Sugishita, Y; Tomobe, Y; Yanagisawa, M, 1989) | 0.28 |
" The dose of adenosine producing a 20% change in FEV1 (PD20) was calculated from the individual semilogarithmic dose-response curve; the results of PD20 were converted to log values for statistical analysis (Student's paired t test)." | ( Effect of indomethacin on adenosine-induced bronchoconstriction. Crimi, N; Maccarrone, C; Mistretta, A; Oliveri, R; Palermo, B; Palermo, F; Polosa, R, 1989) | 0.68 |
" In addition, indomethacin, at lower dosage (0." | ( Effects of pertussis toxin and indomethacin on murine lymphocytes in the bronchoalveolar lavage fluids. Pugliese, A; Quadrelli, C; Rossi, S; Sampietro, C; Torre, D, 1989) | 0.92 |
" The model, applied to data obtained after percutaneous dosing of ointments under occlusion, successfully described the plasma profile observed in the presence and absence of laurocapram (Azone) and sorbitan monooleate." | ( A pharmacokinetic model for the percutaneous absorption of indomethacin and the prediction of drug disposition kinetics. Atago, H; Ito, Y; Iwaki, M; Ogiso, T, 1989) | 0.52 |
" Inhibition of fibroblast prostaglandin (PG) synthesis enhanced TGF beta-induced stimulation of total protein, collagen, and fibronectin production and reversed the negative slope of the dose-response curve at high concentrations of TGF beta." | ( Transforming growth factor-beta stimulation of lung fibroblast prostaglandin E2 production. Diaz, A; Jimenez, SA; Varga, J, 1989) | 0.28 |
" An increase in malondialdehyde level was observed after ethanol exposure, whereas suppression of lipid peroxidation occurred after dosing with indomethacin." | ( Lipid peroxidation in normal and ulcerated gastric mucosa of rats treated with pentacaine and cimetidine. Nosál, R; Nosálová, V; Petríková, M, 1989) | 0.48 |
" Previous treatment with 1 microM indomethacin (IND) or 10 microM quinacrine (QUIN) markedly displaced the dose-response curves for Ach on OAS preparations to the left, whereas the EC50 of His was only increased by QUIN." | ( Tracheal responsiveness to histamine, PAF-acether and acetylcholine in normal and actively ovalbumin-sensitized guinea pigs. Calixto, JB; Medeiros, YS; Torres, RC, 1989) | 0.56 |
"8 mM), the dose-response curve for ATP was shifted to the left in a parallel fashion at this concentration." | ( Low calcium and calcium antagonists potentiate the contraction of guinea-pig vas deferens induced by ATP: a permissive role for P2-purinoceptors. Furukawa, T; Morishita, H, 1989) | 0.28 |
" It proved difficult to select an appropriate dosage of indomethacin due to its high potential to induce GI ulceration and bleeding in dogs." | ( Effects of phenylbutazone and indomethacin on the post-operative course following experimental orthopaedic surgery in dogs. Løkken, P; Mbugua, SW; Skoglund, LA, 1989) | 0.81 |
" In this indomethacin-treated preparation, when an intermittent dosing regimen was used, repeated exposure to either human or murine EGF-URO caused a persistent desensitization." | ( Contractile actions of epidermal growth factor-urogastrone in isolated smooth muscle preparations from guinea pig stomach: structure-activity relationships and comparison with the effects of human transforming growth factor-alpha. Hollenberg, MD; Itoh, H; Lederis, K; Muramatsu, I; Patel, P; Yang, SG, 1989) | 0.69 |
" In the order of potency L-648,051 greater than FPL-55712 greater than L-649,923, these agents antagonized contractions to LTD4 and produced parallel rightward shifts in the dose-response curves." | ( Leukotriene and anti-IgE induced contractions of human isolated trachea: studies with leukotriene receptor antagonists and a novel 5-lipoxygenase inhibitor. Charette, L; Denis, D; Jones, TR, 1988) | 0.27 |
" We investigated whether the maximal response plateau or the position of the dose-response curve is due to functional inhibition by neurogenic mechanisms or to prostaglandin release." | ( Limited maximal airway narrowing in nonasthmatic subjects. Role of neural control and prostaglandin release. Daniel, EE; Hargreave, FE; Sterk, PJ; Zamel, N, 1985) | 0.27 |
"The effect of serotonin on pentagastrin-stimulated gastric pepsin secretion in dogs was evaluated with regard to dose-response kinetics and receptor mediation." | ( Effect of serotonin on pentagastrin-stimulated gastric pepsin secretion in dogs with gastric fistula. Andersen, D; Bech, K, 1985) | 0.27 |
" Met (1 X 10(-6) M) increased the tension of both normal and diabetic atria, but in diabetic atria, the dose-response curve to Met was shifted to the left and the efficacy of Met was enhanced." | ( Hypersensitivity to methoxamine in atria isolated from streptozotocin-induced diabetic rats. Canga, L; Sterin-Borda, L, 1986) | 0.27 |
" Des-Arg9-bradykinin-mediated relaxation was inhibited by the specific B1 receptor antagonist [Leu8]des-Arg9-bradykinin which produced parallel shifts in the dose-response curve." | ( Relaxation of isolated mesenteric arteries by des-Arg9-bradykinin stimulation of B1 receptors. Churchill, L; Ward, PE, 1986) | 0.27 |
" A method that avoided tachyphylaxis encountered in prior investigations was developed for isometric measurement of multiple dose-response effects." | ( Parasympathetic involvement in PAF-induced contraction in canine trachealis in vivo. Leff, AR; Munoz, NM; Popovich, KJ; Shioya, T; Stimler-Gerard, NP; White, SR, 1987) | 0.27 |
" SC-19220 produced a competitive rightward shift of the dose-response curve for the contractile effect induced by PGE2 on strips of rat detrusor muscle in vitro, whereas the amplitude of nerve-mediated twitches was unaffected." | ( The effect of SC-19220, a prostaglandin antagonist, on the micturition reflex in rats. Conte, B; Furio, M; Giuliani, S; Gragnani, L; Maggi, CA; Meli, A; Meli, P; Patacchini, R; Santicioli, P, 1988) | 0.27 |
"The potential of chitosan granules as an oral sustained-release dosage form of indomethacin has been compared with conventional capsules in beagle dogs." | ( Sustained release of indomethacin from chitosan granules in beagle dogs. Hou, WM; Miyazaki, S; Takada, M; Yamaguchi, H; Yokouchi, C, 1988) | 0.82 |
" Intravenous administration of a pharmacologic dosage of epinephrine (222 ng/kg per min) caused gastric dysrhythmia in 8 of 12 healthy subjects." | ( Effect of inhibition of prostaglandin synthesis on epinephrine-induced gastroduodenal electromechanical changes in humans. Abell, TL; Hanson, RB; Kim, CH; Malagelada, JR, 1989) | 0.28 |
" The dosage of diflunisal was 500 mg twice daily (d-group) and the dosage of indomethacin 50 mg three times daily (i-group)." | ( Medical treatment of acute low back pain. Diflunisal compared with indomethacin in acute lumbago. Orava, S, 1986) | 0.74 |
" The induction of keratinocyte HLA-DR expression was greater for continuous compared with pulse dosage (0." | ( Human keratinocyte-lymphocyte reactions in vitro. Basham, TY; Merigan, TC; Morhenn, VB; Nickoloff, BJ; Torseth, JW, 1986) | 0.27 |
" However, the baseline control collections after chronic dosing did not differ from the no-drug control periods." | ( Effects of nonsteroidal antiinflammatory drugs on renal function in patients with renal insufficiency and in cirrhotics. Anderson, SA; Brater, DC; Brown-Cartwright, D; Toto, RD, 1986) | 0.27 |
"Over a 4-year period, 63 premature babies presenting with patent ductus arteriosus were treated with indomethacin at two different dosage levels (0." | ( [Treatment of patent ductus arteriosus in premature infants by indomethacin]. Bianchetti, G; Marchal, F; Monin, P; Morselli, P; Vert, P, 1987) | 0.73 |
" ANP produced dose-related coronary vasodilation with a threshold dosage of 2 ng/kg; a dosage of 2 micrograms/kg caused a 27 +/- 4% decrease in coronary vascular resistance." | ( Effects of atrial natriuretic peptide in the canine coronary circulation. Bache, RJ; Chen, DG; Dai, XZ; Schwartz, JS, 1988) | 0.27 |
" Analysis of the NE-cAMP dose-response curve indicates that the stress reduces the maximum cAMP response to NE but does not increase the EC50 value of NE." | ( Reduction of the cyclic adenosine 3',5'-monophosphate response to catecholamines in rat brain slices after repeated restraint stress. Platt, JE; Slucky, AV; Stone, EA; Trullas, R, 1985) | 0.27 |
" Dose-response experiments indicated that threshold contractions to oxytocin occur at 3 nM and were maximum at 10 microM with mean effective concentration of 125 nM." | ( Evidence for oxytocin receptors in the urinary bladder of the rabbit. Anderson, GF; Romine, MT, 1985) | 0.27 |
" In vitro perfusion of rat lungs with AA (3 X 10(-5)M for 20 min) reduced the relaxant effect of isoproterenol (ISO) on lung parenchymal strips, shown by a shift to the right of ISO dose-response curve, similar to that obtained using desensitizing concentration of specific beta-agonist." | ( Arachidonic acid metabolites induce beta-adrenoceptor desensitization in rat lung in vitro. Abbracchio, MP; Cattabeni, F; Daffonchio, L; Giani, E; Hernandez, A; Omini, C, 1985) | 0.27 |
" The dose-response curves of NA were shifted to the right." | ( Vasoconstriction induced by noradrenaline and angiotensin II is antagonized by eicosapentaenoic acid independent of formation of trienoic eicosanoids. Juan, H; Sametz, W, 1986) | 0.27 |
" A dose-response curve (0." | ( Differential effects of leukotrienes C4, D4, and E4 in the pulmonary and systemic vasculature of sheep. Ahmed, T; Marchette, B; Wanner, A; Wasserman, M; Yerger, L, ) | 0.13 |
"The relationship between occupancy of thrombin receptors on platelets and enhanced phosphoinositide hydrolysis was analysed by examination of the dose-response relationship, the effects of thrombin inhibitors and the contribution of secondary effects." | ( Thrombin-induced phosphoinositide hydrolysis in platelets. Receptor occupancy and desensitization. Detwiler, TC; Huang, EM, 1987) | 0.27 |
" Concentrations of TRK-100, a stable analog of PGI2, equipotent to those of PGI2 released by ANG II, estimated from dose-response curves for TRK-100 and enhancement by indomethacin of ANG II-induced contractions, did not differ in proximal and distal portions." | ( Comparison of the response to angiotensin II of isolated dog coronary and mesenteric arteries of proximal and distal portions. Minami, Y; Toda, N, ) | 0.33 |
" Inhibition by topical retinoic acid of ODC induction by TPA was partially overcome in a dose-response fashion by PGE." | ( The role of prostaglandin E1 in ornithine decarboxylase induction by tumor promoters. Boutwell, RK; Cleaveland, JS; Ordman, AB; Simsiman, RC, 1986) | 0.27 |
" Further increase in dosage of both prostaglandin synthesis inhibitors failed to induce further reduction of integrated areas of coronary vasodilatation." | ( Effects of prostaglandin synthesis inhibition on sympathetic-and parasympathetic-mediated coronary hemodynamic responses. Condorelli, M; Cuocolo, A; de Luca, N; Patrignani, P; Ricciardelli, B; Trimarco, B; Volpe, M, 1986) | 0.27 |
" A dose-response curve was achieved for all three cyclooxygenase products with the calcium ionophore A23187." | ( Human peritoneal eosinophils and formation of arachidonate cyclooxygenase products. Foegh, ML; Maddox, YT; Ramwell, PW, 1986) | 0.27 |
" Animals given dexamethasone were divided into three groups and the drug was administered at a constant dosage of 2 mg/kg: (a) 2 days, 1 day, and 3 h intraperitoneally before (chronic pretreatment), (b) 3 h intraperitoneally before (acute pretreatment), and (c) 5 min intravenously and 6 h and 1 day intraperitoneally after (chronic posttreatment) induction of ischemia." | ( Chronic dexamethasone pretreatment aggravates ischemic neuronal necrosis. Koide, T; Siesjö, BK; Wieloch, TW, 1986) | 0.27 |
" As the dosage of spores injected into the winter flounder increased from 3 X 10(3)/ml to 3 X 10(8)/ml, the level of serum IgM's decreased proportionally." | ( Immunoglobulin levels of the winter flounder (Pseudopleuronectes americanus) and the summer flounder (Paralichthys dentatus) injected with the microsporidan parasite Glugea stephani. Cali, A; Laudan, R; Stolen, JS, 1986) | 0.27 |
" Ulcerogenic effects of PGM on the gastric mucosa were approximately 1/7 and 1/10 times as potent as those of IND on a molar ratio 4 hr after single oral dosing to fasting and feeding rats, respectively." | ( [Pharmacological studies on proglumetacin maleate, a new non-steroidal anti-inflammatory drug. (3) Damaging effects on the gastrointestinal tract]. Miyake, H; Ono, N; Sunami, A; Yamamoto, N; Yamasaki, Y, 1986) | 0.27 |
" Cyclooxygenase inhibition with indomethacin displaced the dose-response curve to AA to the right but did not prevent the relaxant effects of the fatty acid." | ( Arachidonic acid-induced endothelial-dependent relaxations of canine coronary arteries: contribution of a cytochrome P-450-dependent pathway. Abraham, NG; Mullane, KM; Pinto, A, 1987) | 0.56 |
" Thus, these experiments suggest that thromboxane synthetase inhibition, within a narrow dosage range, potentiates furosemide-induced renin release while cyclooxygenase inhibition suppresses it." | ( Effect of cyclooxygenase and thromboxane synthetase inhibition on furosemide-stimulated plasma renin activity. Datar, S; McCauley, FA; Wilson, TW, 1987) | 0.27 |
"In normocapnic and deeply hypocapnic guinea-pig heart-lung-preparations (HLPs), dose-response relationships were estimated for the bronchoconstrictor and pulmonary hypertensive responses to histamine (H), 5 hydroxytryptamine (5HT), arachidonic acid (AA) and U-46619, a prostaglandin endoperoxide analogue acting on thromboxane (TXA2) receptors." | ( Arachidonic acid and pulmonary function in heart-lung-preparation of guinea-pig: modulation by PCO2. Argiolas, L; Bedetti, C; Carpi, A; Del Basso, P, 1987) | 0.27 |
" Indomethacin, in the dosage administered, was not found to cause regression of established tumors." | ( The effect of indomethacin on tumor regression in DMBA-induced epithelial neoplasia of hamster cheek pouch mucosa. Craig, GT; Franklin, CD, 1987) | 1.54 |
"Cumulative dose-response curves to leukotriene C4 (LTC4) and leukotriene D4 (LTD)4 were obtained on indomethacin (5 microM) treated isolated guinea pig tracheal spiral strips." | ( Pharmacological comparison of L-serine borate and glutathione as inhibitors of metabolism of LTC4 to LTD4 by the isolated guinea pig trachea. Hand, JM; Schwalm, SF, 1987) | 0.49 |
" After hospitalization of all in-patients needing glibenclamide therapy, a one-week period of adaptation to clinical conditions with optimized diet, antidiabetic dosage of the drug and the beginning of a diabetes learning programme followed." | ( [Interactions of non-steroidal antirheumatic drugs with oral antidiabetic agents: acemetacin--glibenclamide]. Haupt, E; Hoppe, FK; Rechziegler, H; Zündorf, P, ) | 0.13 |
" Such animals are then labeled with 51Cr-red blood cells from donor animals and dosed with the compound under evaluation." | ( Assessment of gastric bleeding in rats: effects of cyclooxygenase inhibitors and 16,16-dimethyl prostaglandin E2 on gastric bleeding. Argenbright, LW; Bailey, P; Bonney, RJ; Glinka, S; Hopple, S; Humes, JL, 1987) | 0.27 |
" Isolated rings (circular preparations) obtained from rat thoracic aortae responded to increasing concentrations of NE with dose-dependent tonic enhancement, not significantly affected by the presence of indomethacin (10(-6)M); whereas, preincubation with phentolamine (10(-6)M), yohimbine (10(-7)M) or prazosin (10(-8)M), shifted significantly to the right points of the positive inotropic dose-response curve for NE." | ( Possible prostacyclin involvement on disparate tonic responses to "in vitro" norepinephrine in circular and in longitudinal preparations from rat thoracic aorta. Chaud, M; Franchi, AM; Gimeno, AL; Gimeno, MA, 1987) | 0.46 |
" In this model no effect of the receptor site antagonist was noted, but due to the short half-life of this compound, a different dosing schedule may be needed before its efficacy can be determined." | ( Group B streptococcal (GBSS) newborn septic shock model: the role of prostaglandins. Miller, MK; Pan, J; Short, BL, 1988) | 0.27 |
" Wy-41,770 induced superficial erosions only in the cecum 26 hr after a single oral dose of 250 or 500 mg/kg of the drug, progressing to ulcers after 5 days dosing with ultrastructural evidence of bacteria in the mucosa." | ( Mucosal lesions induced in the rat intestinal tract by the anti-inflammatory drug, Wy-41,770, a weak inhibitor of prostaglandin synthesis, contrasted with those from the potent prostaglandin inhibitor, indomethacin. Rainsford, KD, 1988) | 0.46 |
"8 microM) was repeatedly dosed with acetylcholine (ACh, 10 microM)." | ( The relaxant and spasmogenic effects of some xanthine derivatives acting on guinea-pig isolated trachealis muscle. Boyle, JP; Cortijo, J; Curtis-Prior, PB; Davies, JM; Foster, RW; Hofer, P; Small, RC, 1988) | 0.27 |
" We determined the nebulizer concentration of PAF which reduced specific airway conductance (SGaw) 35% (PC35 SGaw) and the slope of the PAF dose-response curve." | ( Mechanism of platelet activating factor-induced bronchoconstriction in humans. Patterson, R; Rubin, AH; Smith, LJ, 1988) | 0.27 |
" Treatment of mice with a higher dosage of IM (20 micrograms/ml), decreased tumor metastasis even further compared to controls, but did not decrease tumor growth rate compared to the lower dosage of IM (10 micrograms/ml)." | ( Inhibition of growth and linoleate-enhanced metastasis of a transplantable mouse mammary tumor by indomethacin. Chapkin, RS; Erickson, KL; Hubbard, NE, 1988) | 0.49 |
"0 h after dosing compared with placebo or indomethacin alone." | ( Effect of indomethacin on the pharmacokinetics and pharmacodynamics of felodipine. Bailey, DG; Bartle, WR; Edgar, B; Hardy, BG; Myers, M, 1988) | 0.94 |
" Three consecutive histamine dose-response curves were obtained in nine dogs pretreated with 5 mg/kg indomethacin; two of these nine were also pretreated with 10 mg/kg indomethacin." | ( Histamine tachyphylaxis in canine airways despite prostaglandin synthesis inhibition. Antol, PJ; Gunst, SJ; Hyatt, RE, 1988) | 0.49 |
" AD-1590 and indomethacin at an oral dosage as high as 32 mg/kg did not show any significant inhibitory activity on rat passive cutaneous anaphylaxis, a type-I allergy, although prednisolone and cyproheptadine produced strong inhibition." | ( [Inhibitory effect of AD-1590, a non-steroidal anti-inflammatory drug, on allergic inflammation in mice and rats]. Ishii, K; Kadokawa, T; Motoyoshi, S; Nakamura, H, 1988) | 0.64 |
" After establishing a dose-response relationship, we chose a control dose that produced intermediate hypertensive responses." | ( Hemodynamic responses of chronically instrumented piglets to bolus injections of group B streptococci. Barefield, E; Godoy, G; Gray, BM; Graybar, G; Lyrene, RK; Philips, JB; Sams, JE, 1988) | 0.27 |
"When Indomethacin in a dosage of 175 mg/day was used to treat threatened premature labour more than 70% of cases carried on until 37 weeks." | ( [Value and dangers of indomethacin used in pregnancy. Apropos of 304 treated patients]. Barrat, J; Bouillie, J; Boyer, F; Keskes, J; Marpeau, L; Pigné, A; Vincenti, O, 1988) | 1.1 |
" The dosage regimen was 25 mg every four hours in four patients and 25 mg every six hours in the other four patients." | ( Influence of short-term indomethacin therapy on fetal urine output. Huhta, JC; Kirshon, B; Moise, KJ; Ou, CN; Wasserstrum, N, 1988) | 0.58 |
"Both drug disposition and effects vary as a function of dosing time." | ( Clinical chronopharmacology with special reference to NSAIDs. Lévi, F; Reinberg, A, 1987) | 0.27 |
" Dose-response studies comparing 0 to 50 micrograms/ml tannin with 0 to 1 U/ml human alpha-thrombin showed that tannin caused 5-HT secretion and protein phosphorylation changes that were very similar to those induced by human alpha-thrombin." | ( Protein phosphorylation during tannin-mediated activation of human platelets. Hempel, SL; Rohrbach, MS; Wheatley, CL, 1988) | 0.27 |
" Indomethacin (5 mg/kg) was administered as a bolus dosage 30 min before the induction of AHP in the IMP group." | ( Indomethacin in canine acute hemorrhagic pancreatitis. Kairaluoma, MI; Kiviniemi, H; Rämö, OJ; Ståhlberg, M, 1988) | 2.63 |
" Severe intestinal ulcers resulted following oral administration of indomethacin in either vehicle at daily 3-4-mg/kg doses, but did not result from EPCMPV formulations, whether dosed for 4 days or 14 days." | ( Encapsulation of indomethacin in liposomes provides protection against both gastric and intestinal ulceration when orally administered to rats. Fielder, FG; Ginsberg, RS; Godin-Ostro, E; Slusher, MA; Soehngen, EC; Weiner, AL, 1988) | 0.85 |
" As such dosage involves pronounced side-effects, it seems more appropriate to employ the combination of 50 mg indomethacin and 4 g paracetamol, whereby similar analgesia can be obtained without an increase in side-effects." | ( Equianalgesic effects of paracetamol and indomethacin in rheumatoid arthritis. Melander, A; Seideman, P, 1988) | 0.75 |
" 1) H2O2 dissolved in different concentrations produced arterial contractions similar to those by equimolar Oxy-Hb, showing similar dose-response curves." | ( [On the mechanism underlying spasmogenic actions of oxy-hemoglobin on the cerebral artery, analyzed from the inhibitory effects of nicardipine, procaine and indomethacin]. Doi, M, 1988) | 0.47 |
" At the dosage and duration administered, these maternal and fetal hemodynamic and fetal acid-base changes occurred independently of any effect upon uterine blood flow." | ( Effects of indomethacin on the acid-base balance and hemodynamics of chronically instrumented pregnant sheep. Ayromlooi, J; Steele, A, 1988) | 0.66 |
" Prostanoids and prostanoid-mimetics were injected bilaterally into the AH/PO region of conscious, indomethacin pretreated cats, and partial dose-response curves for pyrexic activity were obtained." | ( Comparative pyrogenic potency of endogenous prostanoids and of prostanoid-mimetics injected into the anterior hypothalamic/preoptic region of the cat. Gollman, HM; Rudy, TA, 1988) | 0.49 |
" We may conclude that this model is adequate and precise for selecting the most appropriate galenic dosage form for an active compound in terms of its clinical efficacy when topically administered." | ( UV-induced erythema model: a tool in dermatopharmacology for testing the topical activity of non-steroidal anti-inflammatory agents in man. Barbanoj, MJ; Izquierdo, I; Jané, F; Lauroba, J; Moreno, J; Torrent, J, 1988) | 0.27 |
" Dose-response curves to norepinephrine (SO, n = 9; BDL, n = 10) and angiotensin II (SO, n = 7; BDL, n = 9) were obtained." | ( Renal vascular reactivity in the bile duct-ligated rat. Kahng, KU; Monaco, DO; Schnabel, FR; Wait, RB, 1988) | 0.27 |
" The dose-response relationship indicated that both PGE2 and PGF2 alpha have the same efficacy." | ( Stimulatory effects of prostaglandins upon endometrial alkaline phosphatase activity during the decidual cell reaction in the rat. Kennedy, TG; Yee, GM, 1988) | 0.27 |
"The effect of norepinephrine (NE) stimulation of near-term pregnant rabbit myometrium was studied by comparing cumulative dose-response curves for NE and NE with prazosin or indomethacin." | ( Effects of prazosin and indomethacin on the alpha-adrenergic stimulation of rabbit myometrium. Barss, VA; Phillippe, M; Valles, L, 1988) | 0.78 |
" Intraperitoneal dosing of salicylate resulted after approximately 4 h in similar vascular and extravascular drug concentrations." | ( The cellular association of sodium salicylate and indomethacin in peritoneal fluid of ascites bearing mice. Huisman, JA; Raghoebar, M; van den Berg, WB; van Ginneken, CA, 1987) | 0.53 |
" Indomethacin (5 microM) shifted the dose-response curve to norepinephrine to the right in arteries from all groups of animals." | ( Effect of diabetes on vascular smooth muscle function in normotensive and spontaneously hypertensive rat mesenteric artery. Agrawal, DK; McNeill, JH, 1987) | 1.18 |
" By using a preincubation period in indomethacin, the dose-response curves for the stimulatory effect of PTH and PGE2 on mineral mobilization could be sensitized as compared to the curves obtained with fresh bones." | ( Modifications of the mouse calvarial technique improve the responsiveness to stimulators of bone resorption. Lerner, UH, 1987) | 0.55 |
" Before the fertility experiments, the pharmacokinetics of the drugs were determined to find dosage regimens by which drug concentrations known as active from human anti-inflammatory therapy could be reached and maintained in the animals." | ( Effect of non-steroidal anti-inflammatory drugs on fertility of male rats. Blazaki, D; Löscher, W, 1986) | 0.27 |
"We determined dose-response characteristics of indomethacin and prostaglandin E2 on the myoelectric activity in ileum of anesthetized New Zealand White rabbits." | ( Dose-response effects of indomethacin and PGE2 on electromechanical activity of in vivo rabbit ileum. Dwyer, A; Jeffries, GH; Koch, KL, 1986) | 0.83 |
" Intravenously administered PGE2 at a five times higher dosage failed to significantly alter net water and electrolyte fluxes." | ( Central nervous system influence of prostaglandin E2 on jejunal water and electrolyte transport in conscious dogs. Bueno, L; Primi, MP, 1986) | 0.27 |
"Histamine concentration-effect curves were obtained using either an individual or cumulative dosing method." | ( Histamine contraction of isolated human airway muscle preparations: role of prostaglandins. Bayol, A; Benveniste, J; Boullet, C; Brink, C; Cerrina, J; Haye-Legrand, I; Labat, C; Raffestin, B, 1986) | 0.27 |
" Dose-response curves for methoxamine documented its positive, but different, inotropic actions in the two groups and at the four periods of the estrous cycle." | ( Prostaglandin output from and the spontaneous inotropism of uterine horns isolated from underfed rats at different stages of the sex cycle. Smooth muscle contractile influences of indomethacin and of methoxamine. Gimeno, AL; Gimeno, MA; Goldraij, A; Sterin, AB, 1987) | 0.47 |
" when dosed before sensitization." | ( Immunomodulating activity of Wy-41,770 (5H-dibenzo[A,D]cyclohepten-5-ylidene) acetic acid. Carlson, RP; Datko, LJ; Lewis, AJ; O'Neill-Davis, L, 1986) | 0.27 |
" In contrast, auranofin administered to normal rats, in the same dosing regimen, did not affect interleukin production." | ( Effect of auranofin treatment on aberrant splenic interleukin production in adjuvant arthritic rats. Dimartino, MJ; Hanna, N; Lee, JC; Votta, BJ, 1987) | 0.27 |
" Dypiridamole, which in PRP has very little effect on the dose-response curve for ajoene, when assayed in whole blood decreases the ID50 for ajoene by a factor of four." | ( Ajoene, the antiplatelet principle of garlic, synergistically potentiates the antiaggregatory action of prostacyclin, forskolin, indomethacin and dypiridamole on human platelets. Apitz-Castro, R; Escalante, J; Jain, MK; Vargas, R, 1986) | 0.48 |
" UNDW responsiveness was assessed with dose-response curves of UNDW volume output versus the percent fall in FEV1." | ( The effect of indomethacin on the refractory period occurring after the inhalation of ultrasonically nebulized distilled water. Ciappi, G; Corbo, GM; Foresi, A; Mattoli, S; Valente, S, 1987) | 0.63 |
" Inter- and intra-individual indomethacin dispositions varied considerably with the need for marked dosage adjustments to maintain the drug level within the proposed therapeutic range." | ( Prolonged indomethacin treatment in preterm infants with symptomatic patent ductus arteriosus: efficacy, drug level monitoring, and patient selection. Isken, V; Kühl, PG; Leonhardt, A; Seyberth, HW, 1987) | 0.97 |
" However, there was no strong dose-response relation." | ( [Modulation of the oxidative metabolism of granulocytes by nonsteroidal anti-inflammatory agents]. Kapp, A; Schöpf, E, 1987) | 0.27 |
" The number of treatments was fewer and the dosage of interferon beta administered was less in the present study than in the preliminary one." | ( Intrathecally administered natural human fibroblast interferon reduces exacerbations of multiple sclerosis. Results of a multicenter, double-blind study. Cuetter, A; Ekes, R; Freeman, A; Herndon, R; Husain, F; Jacobs, L; Jozefowicz, R; Reese, PA; Salazar, AM; Smith, WA, 1987) | 0.27 |
" Oral dosing with U46619 or AH23848 produced a dose-related inhibition of ethanol-induced gastric mucosal damage in the conscious rat, and these effects were partially blocked by indomethacin treatment." | ( The effects of the stable thromboxane A2-mimetic, U46619, on gastric mucosal damage and gastric non-parietal secretion in the rat. Bunce, KT; Clayton, NM, 1987) | 0.47 |
" Patients with this renal disorder require a permanent high dosed indomethacin therapy." | ( [The significance of renal prostaglandins for kidney function in early childhood]. Seyberth, HW, 1987) | 0.51 |
"94, respectively) to neonatal mouse calvaria maintained in a chemically defined medium in tissue culture for 1 wk increased calcium release in a dose-response fashion." | ( H+ stimulation of cell-mediated bone resorption in tissue culture. Goldhaber, P; Rabadjija, L, 1987) | 0.27 |
"025-16 micrograms/paw) were followed by a bell-shaped dose-response curve for oedema." | ( Interactions between local inflammatory and systemic haematological effects of PAF-acether in the rat. Castro, HC; Cordeiro, RS; Lima, MC; Martins, MA; Neto, F; Silva, PM; Vargaftig, BB, 1987) | 0.27 |
" We calculated the provocative concentration of LTD4 required to produce a 35% fall in SGaw (PC35SGaw) or a 30% fall in V30P (PC30V30P) and the slope of the LTD4 dose-response curve." | ( Mechanism of leukotriene D4-induced bronchoconstriction in normal subject. Bernstein, PR; Kern, R; Krell, RD; Patterson, R; Smith, LJ, 1987) | 0.27 |
" Indomethacin in a dosage of 150 mg/day abolishes the headache completely." | ( "Hemicrania continua": a third Norwegian case. Sjaastad, O; Tjørstad, K, 1987) | 1.18 |
" When indomethacin was dosed in equipotent analgesic levels, the level of circulating drug was considerably higher than that seen for metabolically derived drug." | ( Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. Bélanger, P; Gillard, JW, 1987) | 0.98 |
" Dose-response curves were studied at 4 h following administration of indomethacin on the 19th, 20th, and 21st days, and flurbiprofen on the 20th and 21st days." | ( In vivo constriction of the ductus arteriosus by nonsteroidal antiinflammatory drugs in near-term and preterm fetal rats. Momma, K; Takao, A, 1987) | 0.51 |
" During the second phase, after 24 h, edema was more pronounced, presented a clear dose-response relationship and peaked at 72 h after injection." | ( Mouse paw edema. A new model for inflammation? Assreuy-Filho, J; Cordeiro, RS; Cunha, FQ; Flores, CA; Henriques, MG; Martins, MA; Silva, PM, 1987) | 0.27 |
" The dose-response curve to thyroxin was shallow, and the agent did not produce maximal resorption." | ( Indomethacin inhibits thrombin-, but not thyroxin-stimulated resorption of fetal rat limb bones. Hoffmann, O; Klaushofer, K; Koller, K; Mavreas, T; Peterlik, M; Stern, P, 1986) | 1.71 |
" The average daily dosage ranged from 50 to 150 mg; for 81% of patients, the average daily dosage was 75 to 100 mg." | ( Tolerability and efficacy of long-term daily administration of indomethacin for moderate to severe chronic arthritic disorders. Lockie, LM, 1986) | 0.51 |
" The dose-response curves were significantly depressed in both MRAs and ILAs from BDL animals." | ( Renal vascular reactivity in jaundice. Cioffi, WG; DeMeules, JE; Kahng, KU; Wait, RB, 1986) | 0.27 |
" Cimetidine shifted the dose-response curve for histamine to the right, but chlorpheniramine did not alter the response." | ( Mechanisms of histamine-induced relaxation in isolated monkey and dog coronary arteries. Toda, N, 1986) | 0.27 |
" Construction of dose-response curves for the indomethacin-responsive and indomethacin-unresponsive components of erythema shows that in human skin the difference in erythemal response to UVB and UVC radiation is not due to the formation of different mediators at these wavelengths." | ( A quantitative study of the effect of topical indomethacin on cutaneous erythema induced by UVB and UVC radiation. Diffey, BL; Farr, PM, 1986) | 0.79 |
"Indomethacin bioavailability was compared in 22 healthy men who received two tablet dosage formulations and a capsule formulation of indomethacin in a three-way crossover study." | ( Bioavailability of indomethacin tablets in men volunteers. Dunn, JM; Groth, PE, 1986) | 2.04 |
" Qualitative and quantitative differences in pharmacokinetics and pharmacodynamics of drugs should be considered before dosage regimens can be established." | ( [Peculiarities of drug therapy in childhood]. Kusenbach, G; Reinhardt, D, 1986) | 0.27 |
" Based on these findings, it can be concluded that although indomethacin is dialyzable, no dosage adjustment is required in patients receiving indomethacin for the management of their uremic pericarditis when undergoing maintenance hemodialysis." | ( Dialyzability and pharmacokinetics of indomethacin in adult patients with end-stage renal disease. Acchiardo, SR; Carter, CA; Meyer, MC; Skoutakis, VA; Straughn, AB; Wojciechowski, NJ, 1986) | 0.78 |
" Aerosol pretreatment with the cyclooxygenase inhibitor indomethacin had no significant effect on either LTC4 or LTD4 dose-response curves; however, at the highest doses of these agonists a notable, nonsignificant inhibition of effects on both Rp and Cdyn was seen." | ( Pharmacology of aerosol leukotriene C4- and D4-induced alteration of pulmonary mechanics in anesthetized cynomolgus monkeys. Giles, RE; Krell, RD; Williams, JC, 1986) | 0.52 |
"Chronopharmacologic studies of indomethacin have indicated that time of dosing influences tolerance and effectiveness." | ( Timing optimizes sustained-release indomethacin treatment of osteoarthritis. Le Louarn, C; Levi, F; Reinberg, A, 1985) | 0.83 |
"The effects of 2 days of oral dosing with sulindac (200 mg twice a day) or indomethacin (75 mg twice a day) on glomerular filtration rate, urinary excretion of prostaglandin E2, sodium homeostasis, and other renal function parameters were investigated in eight patients with chronic stable impaired renal function." | ( Acute renal effects of sulindac and indomethacin in chronic renal failure. Berg, KJ; Talseth, T, 1985) | 0.77 |
" Some rats were pretreated with indomethacin (5 mg/kg, iv) 30 min prior to the dose-response study." | ( Diminished pressor response to exogenous norepinephrine and angiotensin II in septic, unanesthetized rats: evidence for a prostaglandin-mediated effect. Fink, MP; Fletcher, JR; Homer, LD, 1985) | 0.55 |
" To reduce the physiological alterations induced by NSAIDs, short-half-life drugs such as ibuprofen, flurbiprofen or ketoprofen should be used at the maximally tolerable dosage interval." | ( Antirheumatic medication in pregnancy. Brooks, PM; Needs, CJ, 1985) | 0.27 |
" Piroxicam was comparable to indomethacin with respect to efficacy and offered better toleration and a simplified dosage regimen." | ( Piroxicam vs indomethacin: a double blind multicenter comparative study in osteoarthritis. A Canadian Multicenter Study. , 1985) | 0.93 |
"6 percent with isoxicam, at a dosage greater than 200 mg per day; 14." | ( Evaluation of the safety of isoxicam. Burch, FX, 1985) | 0.27 |
"Indomethacin has a moderately short half-life, usually requiring dosing twice a day or three times a day." | ( Pharmacokinetic overview of indomethacin and sustained-release indomethacin. Yeh, KC, 1985) | 2.01 |
" By virtue of its 12-hour dosage system, sustained-release indomethacin can be prescribed only once or twice daily, providing the anti-inflammatory efficacy of indomethacin while promoting patient compliance." | ( Sustained-release indomethacin in the management of ankylosing spondylitis. Calabro, JJ, 1985) | 0.85 |
" Further increase in dosage failed to induce further reduction of integrated areas of coronary vasodilatation, and a correlation was found between the extent of the reduction of the integrated areas of coronary vasodilatation and the dose of indomethacin (r = ." | ( Late phase of nitroglycerin-induced coronary vasodilatation blunted by inhibition of prostaglandin synthesis. Condorelli, M; Cuocolo, A; De Simone, A; Ricciardelli, B; Trimarco, B; Van Dorne, D; Volpe, M, 1985) | 0.45 |
" When cells were pretreated with ibuprofen, aspirin, or indomethacin to block prostaglandin synthesis and then exposed to 20:4, the dose-response effect was shifted to the left." | ( Morphological alterations in cultured endothelial cells induced by arachidonic acid. Bar, RS; Dolash, S; Kaduce, TL; Marshall, SJ; Sandra, A; Spector, AA, 1985) | 0.52 |
"Pretreatment with prostaglandin synthetase inhibitors (PGSI) significantly decreases the CNS effects of ethanol across the entire ethanol dose-response curve." | ( Indomethacin antagonism of ethanol-induced sleep time: sex and genotypic factors. Collins, AC; George, FR; Ritz, MC, 1985) | 1.71 |
" Acetylsalicylic acid inhibition, calculated as IC50 by a dose-response curve, is more than ten fold higher for leukocytes vs platelets." | ( Differential effects of aspirin and indomethacin on platelet and leukocyte thromboxane A2 formation. Colli, S; Maderna, P; Morazzoni, G; Stragliotto, E; Tremoli, E, 1985) | 0.54 |
" These results suggest that modulation of leukotaxis by NSAIDs may reflect a differential dose-response sensitivity of lipoxygenase and cycloxygenase pathways." | ( In vivo modulation of leukotaxis by non-steroidal anti-inflammatory drugs. diZerega, GS; Nakamura, RM; Shimanuki, T, 1985) | 0.27 |
" Ten animals received the same dosage of indomethacin beginning 2 h after the start of endotoxin infusion." | ( Prophylactic and delayed treatment with indomethacin in a porcine model of early adult respiratory distress syndrome induced by endotoxaemia. Borg, T; Gerdin, B; Modig, J, 1986) | 0.8 |
" Paired plasma and synovial fluid samples were obtained at regular intervals following a single dose of 'Osmosin' (19 patients) and after continuous daily dosing (15 patients)." | ( Osmosin: its effect on plasma and synovial fluid kinetics of indomethacin. Dawes, PT; Fowler, PD, 1985) | 0.51 |
"First and second derivative ultraviolet spectrometric methods are described for the estimation of indomethacin, naproxen, and ibuprofen in pharmaceutical dosage forms." | ( Quantitation of indomethacin, naproxen, and ibuprofen in pharmaceutical dosage forms by first and second derivative ultraviolet spectrometry. Abdel-Hamid, ME; Abdel-Khalek, MM; Mahrous, MS, ) | 0.69 |
" The dose-response relationships between these PGs and decidualization did not differ." | ( Evidence for the involvement of prostaglandins throughout the decidual cell reaction in the rat. Kennedy, TG, 1985) | 0.27 |
" Addition of indomethacin therapy (2 mg/kg/day) was followed by correction of the acidosis and allowed a decrease in the dosage of alkali." | ( Indomethacin in the treatment of proximal tubular acidosis. Garin, EH; Scott, DI, 1985) | 2.08 |
" To compare anti-inflammatory substances of different structure, different absorption characteristics and pharmacokinetics as regards their effect on rat cartilage, we used an equieffective dosage of the different anti-inflammatory drugs." | ( A new test method for the standardized evaluation of changes in the ultrastructure of chondrocytes. Annefeld, M, 1985) | 0.27 |
"Three consecutive dose-response curves to inhaled aerosolized histamine, separated by 1-h intervals, were obtained in 20 anesthetized mongrel dogs." | ( Tachyphylaxis to inhaled aerosolized histamine in anesthetized dogs. Martin, JG; Shore, S, 1985) | 0.27 |
"The platelet-activating factor (PAF) produced by mouse embryos showed similar kinetics of action and dose-response curve, in a bioassay, as did 1-0-alkyl-2-acetyl-sn-glyceryl-3-phosphocholine (PAF-acether)." | ( Partial characterization of the embryo-derived platelet-activating factor in mice. O'Neill, C, 1985) | 0.27 |
"75 to 750 pM) of alpha-thrombin prior to contracting in response to higher concentrations during cumulative dose-response experiments." | ( Thrombin-elicited contractile responses of aortic smooth muscle. Aiken, M; Anderson, GF; Ciaglowski, RE; Fenton, JW; Walz, DA, 1985) | 0.27 |
" Polyphloretin phosphate at a concentration of 10 mug/ml resulted in complete identity of dioestrus and metoestrus dose-response curves to angiotensin and oxytocin." | ( Effects of prostaglandin inhibitors on angiotensin, oxytocin and prostaglandin F2 alpha contractile effects on the rat uterus during the oestrous cycle. Baudouin-Legros, M; Meyer, P; Worcel, M, 1974) | 0.25 |
" Dose-response curves to intra-arterial administration of arachidonic acid (12 to 200 microgram kg-1), bradykinin (0." | ( Responses to arachidonic acid and other dilator agonists and their modification by inhibition of prostaglandin synthesis in the canine hindlimb. Morcillo, E, 1980) | 0.26 |
" On the other hand, in the presence of prostaglandin (PG)-inhibitors the dose-response curve of acetylcholine shifts to the right." | ( In vitro effect of acetylcholine and bethanechol on the contractions of the human detrusor muscle. Influence of prostaglandins. Borda, E; Contreras-Ortiz, N; Gimeno, MF; Gutnisky, R, 1982) | 0.26 |
"Miniaturised methods have been used to construct dose-response curves for the effects of inhibitory drugs on prostaglandin synthesis using individual rectal biopsies obtained from patients with ulcerative colitis." | ( Inhibition of prostaglandin synthetase in human rectal mucosa. Hawkey, CJ; Lo Casto, M, 1983) | 0.27 |
" Long Sleep (LS) and Short Sleep (SS) mice, lines bred for differential response to an hypnotic dose of ethanol, showed a four-fold difference in their dose-response curves for indomethacin antagonism of ethanol-induced hypnosis." | ( Antagonism of alcohol hypnosis by blockade of prostaglandin synthesis and activity: genotype and time course effects. Collins, AC; Elmer, GI; George, FR; Howerton, TC, 1983) | 0.46 |
" Cumulative dose-response effects of ovalbumin were obtained on paired parenchymal strips, one used as control and the other drug treated." | ( Pharmacological alteration of antigen-induced contraction of lung parenchymal strips isolated from the actively sensitized guinea pig. Buckner, CK; Busse, WW; Songsiridej, V, 1983) | 0.27 |
" Inhibition of LTB4-formation and cell migration by BW755C was dose-related, but the two dose-response curves were not parallel." | ( The effects of BW755C and other anti-inflammatory drugs on eicosanoid concentrations and leukocyte accumulation in experimentally-induced acute inflammation. Moncada, S; Salmon, JA; Simmons, PM, 1983) | 0.27 |
" N-OH-AAF dependent ODC induction displayed an almost linear dose-response in the dose range up to 94." | ( Induction of ornithine decarboxylase and augmentation of tyrosine aminotransferase activity by N-hydroxy-2-acetylaminofluorene and 2-acetylaminofluorene in rat liver. Influence of sex, retinylacetate, indomethacin, and pentachlorophenol. Bakker, O; Bisschop, A; Meerman, JH; Stavenuiter, JF; van der Heijden, CA; van Wijk, R, 1984) | 0.46 |
" The system was found to be useful as a sustained release dosage form." | ( Encapsulated hydrophilic polymer beads containing indomethacin as controlled release drug delivery systems. Jun, HW; Suryakusuma, H, 1984) | 0.52 |
" Both substance P and histamine produced sigmoid dose-response curves for the following parameters: 1 min and 5 min planimetrically measured areas of erythema, and mean diameter of weal." | ( Vascular responses of human skin to injection of substance P and mechanism of action. Coutts, AA; Eady, RA; Greaves, MW; Jorizzo, JL, 1983) | 0.27 |
"In spontaneously hypertensive rats (SHR), after 1 day of dosing with an angiotensin-converting enzyme (ACE) inhibitor (captopril or enalapril) plus a diuretic (hydrochlorothiazide), a synergistic antihypertensive effect was observed when a second dose of the combination or ACE inhibitor alone but not the diuretic alone was given the next day." | ( Acute antihypertensive synergism of angiotensin-converting enzyme inhibitors and diuretics. Cervoni, P; Chan, PS; Ronsberg, MA, 1984) | 0.27 |
" Maximum contraction occurred simultaneously with the maximum amount of histamine appearing in the superfusate, but the dose-response curves of ovalbumin were different for the two responses." | ( Studies on the relationship between contraction and mediator release produced by ovalbumin in superfused trachea isolated from the actively sensitized guinea pig. Buckner, CK; Fishleder, RI, 1984) | 0.27 |
" Dose-response experiments revealed two active ranges from 1 ng/kg to 100 ng/kg and from 10 micrograms/kg to 10 mg/kg or more." | ( Enhancement of antibody formation against herpes simplex virus in mice by the T-cell mitogen bestatin. Falke, D; Harle-Grupp, V; Knoblich, A; Müller, WE, 1984) | 0.27 |
" The compounds of most interest, 18 and 28, were further tested in a model of adjuvant-induced arthritis; in this system, both compounds were active when dosed intraperitoneally but failed to produce significant activity when dosed orally at subtoxic doses." | ( Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. Millonig, RC; Rovnyak, GC; Schwartz, J; Shu, V, 1982) | 0.26 |
" As measured by magnitude of inhibition and dose-response titration, ADCC activity is less sensitive to the effects of PGE1 than is NK activity in the 51Cr release assay and single-cell assay." | ( Natural killer (NK) and antibody-dependent cellular cytotoxicity (ADCC) activities can be differentiated by their different sensitivities to interferon and prostaglandin E1. Merrill, JE, 1983) | 0.27 |
" capsulatum ablated suppressor T cell activity in vitro; neither dosage of CY altered the suppression mediated by unseparated or nylon wool-adherent spleen cells." | ( Pharmacological modulation of suppressor cell activity in mice with disseminated histoplasmosis. Bullock, WE; Deepe, GS; Kravitz, GR, 1983) | 0.27 |
" Both PGE1 and PGE2 enhanced cellular release of parathyroid hormone, with dose-response characteristics similar to those seen with cAMP." | ( Prostaglandin-mediated stimulation of adenosine 3',5'-monophosphate accumulation and parathyroid hormone release in dispersed human parathyroid cells. Attie, MF; Aurbach, GD; Brown, EM; Gardner, DG, 1980) | 0.26 |
" Since this preparation has not been used previously to study the effects of PTH, we first determined the dose-response curve for cAMP release in response to the 1-34 fragment of synthetic bovine PTH." | ( Dose-related influence of indomethacin on parathyroid hormone-stimulated adenosine 3',5'-monophosphate release from the perfused rat hindlimb. Bliziotes, MM; Lewis, SB; Licht, JH, 1982) | 0.56 |
" Treatment of 20:4 with soybean lipoxygenase did not abolish its capacity to induce O2- production; native and lipoxygenase-treated 20:4 exhibited similar dose-response ratios." | ( Unsaturated fatty acids as second messengers of superoxide generation by macrophages. Bromberg, Y; Pick, E, 1983) | 0.27 |
" Animals were treated with a dosage regimen of aspirin which inhibited PES but had no effect on the cytochrome P-450-dependent oxidation of 7,8-dihydrodihydroxybenzo(a)pyrene." | ( Effect of aspirin and indomethacin on the formation of benzo(a)pyrene-induced pulmonary adenomas and DNA adducts in A/HeJ mice. Adriaenssens, PI; Anderson, MW; Boorman, GA; Eling, TE; Sivarajah, K, 1983) | 0.58 |
" Dose-response relationships for inhibition of 45Ca uptake were identical with controls in mitochondria isolated from normal or essential fatty acid-deficient Long-Evans rats even though PGE synthesis in essential fatty acid-deficient was only 20% of that in normal rats." | ( Prostaglandin-independent inhibition of calcium transport by nonsteroidal anti-inflammatory drugs: differential effects of carboxylic acids and piroxicam. Burch, RM; Halushka, PV; Wise, WC, 1983) | 0.27 |
" These findings indicate that: (i) increases in cAMP or Ca activity stimulate electrogenic Cl secretion by the columnar cells of the surface epithelium; (ii) cAMP mediates the effects of PGE1 and beta-adrenergic agonists; (iii) a strict correlation between cAMP levels and Cl secretion rate is not apparent from spontaneous variations in these parameters or from dose-response relations of Isc and cAMP to epinephrine concentration; and (iv) acetylcholine, histamine, and phenylephrine, agents that stimulate electrically-neutral NaCl secretion by submucosal glands, do not evoke cAMP-mediated responses by the surface epithelium." | ( Chloride secretion by canine tracheal epithelium: I. Role of intracellular c AMP levels. Frizzell, RA; Smith, PL; Stoff, JS; Welsh, MJ, 1982) | 0.26 |
" 92 patients received piroxicam in a daily dosage of 4 capsules (40 mg) during the first two days, then 20 mg during the following days." | ( Double blind comparative study of piroxicam and indomethacin in acute locomotor affections linked with sports activity. Commandre, F, 1983) | 0.52 |
" Group I goats served as controls, group II goats were treated (IV) with a single dose of 300 micrograms of synthetic luteinizing hormone-releasing hormone (LHRH); group III goats were treated with LHRH (similar to group II) and 24 hours later were given indomethacin (10 mg/kg; IM) which dosing was repeated every 6 hours for the next 90 hours." | ( Detection of ovulation in goats by blood prostaglandins concentrations. Akinlosotu, BA; Verma, OP, 1983) | 0.45 |
" Meclofenamate sodium, even at these high dosage levels, was better tolerated than indometacin." | ( Meclofenamate sodium in the treatment of acute gout. Results of a double-blind study. Dunky, A; Eberl, R, 1983) | 0.27 |
" Enterohepatic cycling makes interpretation of bioavailability estimates of indomethacin dosage forms difficult." | ( Evaluation of new indomethacin dosage forms. Waller, ES, ) | 0.69 |
" Indomethacin potentiated the effect of PGl2, shifting the anti-hypoxic dose-response curve of PGl2 to the left." | ( Anti-hypoxic effect of indomethacin and its interaction with prostacyclin. Milanova, D; Nikolov, R; Nikolova, M, 1983) | 1.49 |
" 200-300 mg of indomethacin was the total dosage in a 24 hours period." | ( Further study of the inhibition of premature labor by indomethacin. Part II double-blind study. Gilad, G; Katzuni, E; Shalev, E; Zuckerman, H, 1984) | 0.87 |
" Some of the newer NSAIDs seem at normal dosage to be far less damaging than traditional ASA or indomethacin." | ( Gastroduodenal damage due to drugs, alcohol and smoking. Domschke, S; Domschke, W, 1984) | 0.49 |
" The antigen dose-response relationship for the induction of PFC in cultures of CBMC is represented by a bell-shaped curve comparable to that found for mononuclear cells from adult peripheral blood (adult PBMC)." | ( Distinct role of neonatal and adult monocytes in the regulation of the in vitro antigen-induced plaque-forming cell response in man. Ballieux, RE; Thomas, CM; van Tol, MJ; Zegers, BJ; Zijlstra, J, 1984) | 0.27 |
" Indomethacin (10(-6)M), shifted to the left the dose-response curve for AII in preparations from ovariectomized animals; augmenting both, the efficacy and the potency of the agonist." | ( Prostaglandins and the contractile effect of angiotensin I and II in the uterus isolated from ovariectomized rats. Influences of indomethacin and 17-beta estradiol. Chaud, M; Gimeno, AL; Gimeno, MF; Viggiano, M, 1984) | 1.38 |
" It was shown that (1) all tested compounds inhibited the number and severity of the intestinal mucosal lesions, however, to different extent; (2) the inhibition of the development of small intestinal mucosal damage displayed a dose-response relationship; (3) 17-aza-PGF2 alpha was found to have the most potent effect on the development of the intestinal lesions as well as on the development of gastric mucosal damage produced by ethanol." | ( Preventive effect of PGI2, 7-oxo-PGI2 and 17-aza-PGF2 alpha derivate on the development of indomethacin-induced intestinal mucosal damage in rats. Beró, T; Garamszegi, M; Jávor, T; Mózsik, G, 1984) | 0.49 |
" Cumulative dose-response curves to oxytocin documented a greater sensitivity in uterine horns from restricted-diet rats than in those from controls or refed animals." | ( Dietary restriction alters the "in vitro" spontaneous or oxytocin-induced contractions of uterine smooth muscle from estrous rats. Possible participation of prostaglandins. Gimeno, AL; Gimeno, MF; Goldraij, A; Sterin, AB, 1983) | 0.27 |
" In order to evaluate the role of arachidonic acid metabolites in the C3a response, dose-response curves for C3a-induced contractions of guinea pig lung strips were compared in the presence and absence of several inhibitors which block metabolism of arachidonic acid at relatively specific steps in the pathways." | ( C3a-induced contraction of guinea pig lung parenchyma: role of cyclooxygenase metabolites. Bloor, CM; Hugli, TE; Stimler, NP, 1983) | 0.27 |
" Cumulative dose-response curves for isoproterenol, norepinephrine and methoxamine were made for the different groups." | ( In vitro contractile responses of the uterus from 'restricted diet' rats to adrenoceptor agonists. Influence of cyclo-oxygenase inhibitors. Gimeno, AL; Gimeno, MA; Goldraij, A; Sterin, AB, 1983) | 0.27 |
" Results show that the drug exhibiting almost no antiinflammatory activity in the rat at the dosage used, phenylbutazone, was the most powerful inhibitor of ossification." | ( Correlation between ossification and inflammation using a rat experimental model. de Medicis, R; Lussier, A, 1983) | 0.27 |
" In the presence of L (4 X 10(5) ml-1) the dose-response curve to NaA shifted to the left, the potency and the efficiency of NaA were enhanced and the chronotropic action was triggered." | ( Lymphocytes sensitize rat isolated atria to the inotropic and chronotropic effects of sodium arachidonate. Borda, ES; de Bracco, MM; Finiasz, M; Sterin-Borda, L, 1984) | 0.27 |
"1 X EC50) of NA were calculated from dose-response curves." | ( Effects of cyclooxygenase inhibitors and PGI2 on the adrenergic contractions of isolated rabbit arteries. Hadházy, P; Magyar, K; Malomvölgyi, B, 1984) | 0.27 |
") failed to elicit mucosal damage either ultrastructurally or even visually up to 23 h after dosing and did not affect the content of PG's even though the drug was present in the mucosa in sufficient concentration to elicit reduction in prostaglandin synthesis in vitro." | ( Comparative effects of some non-steroidal anti-inflammatory drugs on the ultrastructural integrity and prostaglandin levels in the rat gastric mucosa: relationship to drug uptake. Fox, SA; Osborne, DJ; Rainsford, KD, 1984) | 0.27 |
" Airway responsiveness was assessed with dose-response curves of acetylcholine aerosol versus pulmonary resistance in 2 sets of experiments: in one set, 5 dogs were given no indomethacin treatment and were studied both before and after ozone exposure (3." | ( Indomethacin inhibits the airway hyperresponsiveness but not the neutrophil influx induced by ozone in dogs. Aizawa, H; Fabbri, LM; Holtzman, MJ; Nadel, JA; O'Byrne, PM; Walters, EH, 1984) | 1.9 |
" No significant differences in anti-oedema activity were observed between the different preparations of indomethacin, but high blood levels of drug were observed following dosing with indomethacin, in a PEG 6000 melt." | ( The effect of incorporation of indomethacin with polyethylene glycol 6000 in a solid dispersion on its in vivo properties in the rat. Chan, KK; Elliott, PN; Ford, JL, 1984) | 0.77 |
" Moreover, a dose-response curve was obtained with increasing amounts of NF." | ( Role of prostaglandins in the production of natriuretic factor by the isolated rat kidney. Cambier, P; Godon, JP, ) | 0.13 |
" Using an equiefficient dosage of the active principles, referred to the ED50 in the model of adjuvant arthritis in the rat, the synthetic apparatus of the chondrocytes was stimulated by tiaprofenic acid while it was diminished by indometacin and phenylbutazone and particularly by dexamethasone." | ( [The effect of steroidal and nonsteroidal anti-inflammatory agents on the ultrastructure of chondrocytes in the rat. Electron microscope and morphometric study]. Annefeld, M; Cleres, C; Raiss, R, 1984) | 0.27 |
" For optimal dosage it would be necessary to know the levels of such compounds in inflamed tissue and not only in blood because the drugs inhibit prostaglandin synthesis in all cells of the body." | ( Pharmacokinetics of indomethacin i.m. in blood, synovial fluid, synovial membrane, muscle, fat, bone, and spinal fluid. Dittrich, P; Köhler, G; Kukovetz, WR; Primbs, P, 1984) | 0.59 |
") given 30 min prior to SU-88 dosing blocked this protective effect, whereas it was not affected when indomethacin was given 30 min after the SU-88 dosing." | ( Cytoprotective effect of SU-88, an anti-ulcer agent, in the rat. Kyogoku, K; Mori, Y; Nakazima, M; Shinozaki, A; Suwa, T, 1984) | 0.48 |
"To clarify the mechanism of enhanced absorption of indomethacin (IND) when dosed with magnesium silicate, reported previously, magnesium (IND-Mg) and calcium (IND-Ca) salts of IND were prepared, and the bioavailability in rat and physical properties of these salts were studied in comparison with IND." | ( Bioavailability of indomethacin calcium and magnesium, and effect of the salts on drug metabolizing enzyme activities in rats. Iwaki, M; Ogiso, T; Tamaki, E, 1983) | 0.85 |
"Analyses of bumetanide's dose-response relationship have been complicated by the hysteresis observed between the drug's urinary excretion rate and its sodium excretion." | ( Application of effect-compartment model to bumetanide-indomethacin interaction in dogs. Fox, JL; Lau, HS; Smith, DE, 1983) | 0.51 |
" Moreover the gastric lesions in FCE 20700 + I treated rats were markedly reduced, allowing the dosage of I to be increased by about three times without increasing its ulcerogenic effect." | ( FCE 20700, a cytoprotective PGE2 derivative, does not interfere with the antiinflammatory activity of indomethacin. Arrigoni, C; Buttinoni, A; Ceserani, R; Ferrari, M; Mizzotti, B; Tremolada, L, 1983) | 0.48 |
" These changes were dependent on the dosage of CPZ." | ( A protective action of coenzyme Q10 on chlorpromazine-induced cell damage in the cultured rat myocardial cells. Chiba, M, 1984) | 0.27 |
" Our data suggest that when indomethacin is added to digoxin therapy, the digoxin dosage should be reduced by 50% until urine output and digoxin serum levels can be better assessed." | ( Effects of indomethacin on digoxin pharmacokinetics in preterm infants. Koren, G; MacLeod, SM; Perlman, M; Zarfin, Y, 1984) | 0.95 |
" Contractility was examined in a randomized dose-response manner to both norepinephrine and the prostaglandin endoperoxide analog U-46619." | ( Vascular reactivity in endotoxin shock: effect of lidocaine or indomethacin pretreatment. Casey, L; Fletcher, JR; Pomerantz, K; Ramwell, PW, 1982) | 0.5 |
"001) in the dose-response relationship to submaximal concentrations of vasopressin (0." | ( Thromboxane and stable prostaglandin endoperoxide analogs stimulate water permeability in the toad urinary bladder. Burch, RM; Halushka, PV, 1980) | 0.26 |
" In keeping with these results, the systems in the GI tract of dogs delivered at the same rate as in vitro, which qualifies the in vitro test as a bioanalogous method predictive of the in vivo performance of the dosage forms." | ( Elementary osmotic pump for indomethacin. Bonsen, P; Heimlich, K; Kwan, KC; Place, V; Swanson, D; Theeuwes, F; Wong, P, 1983) | 0.56 |
" The margin between closure of the ductus arteriosus and the deterioration of kidney function in preterm infants treated with a presently recommended indomethacin dosage is too narrow." | ( [Therapeutic problems with indomethacin in preterm infants with persistent ductus arteriosus]. Müller, H; Plückthun, H; Seyberth, HW; Ulmer, HE; Wille, L; Wolf, D, 1983) | 0.76 |
" In normal calcium Krebs solution, dose-response curves to histamine were markedly reduced by verapamil while acetylcholine responses were relatively unaffected." | ( The effect of prostaglandin E2 on histamine-stimulated calcium mobilization as a possible explanation for histamine tachyphylaxis in canine tracheal smooth muscle. Anderson, WH; Krzanowski, JJ; Polson, JB; Szentivanyi, A, 1983) | 0.27 |
" This new dosage form has been referred to in other publications as the gastro-intestinal therapeutic system (GITS)." | ( Evolution and design of 'rate controlled' osmotic forms. Theeuwes, F, 1983) | 0.27 |
" In vitro testing of this oral precision-release dosage form has been paralleled by a high degree of in vivo predictability." | ( The evolution of precision drug delivery. Heimlich, KR, 1983) | 0.27 |
" Only recently has the importance of dosage form design been recognized as a vital component of effective therapy." | ( Innovations in drug delivery systems. Heilmann, K, 1983) | 0.27 |
" The constant-rate delivery of sodium indomethacin trihydrate to the gastro-intestinal tract from 'Osmosin' controls the rate of drug absorption, prolongs the effective half-life of drug in plasma, does not inhibit the efficiency of absorption, but does significantly decrease the extremes in plasma level fluctuation noted with conventional dosage forms." | ( Biopharmaceutical evaluation of 'Osmosin'. Rogers, JD, 1983) | 0.54 |
" On each occasion a regression line for the descending part of the log-cumulative dose-response curve was computed." | ( Prostaglandins and the control of airways responses to histamine in normal and asthmatic subjects. Walters, EH, 1983) | 0.27 |
" Similarly, LTC4 was found to have vasoconstrictor activity but was more potent and had a steeper dose-response curve than LTD4." | ( The effect of leukotrienes C4 and D4 on the microvasculature of guinea-pig skin. Peck, MJ; Piper, PJ; Williams, TJ, 1981) | 0.26 |
" The cerebral content of dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) was determined after some dosage schedules." | ( Participation of prostaglandins in the action of kinins on the central dopaminergic system in the rat. I. The action of kinins on the central dopaminergic system after pretreatment with indomethacin. Kościelak, M; Moniuszko-Jakoniuk, J; Wiśniewski, K, ) | 0.32 |
" Bioavailability of the oral dosage based on AUC was 13% but no difference was observed in the plasma protein binding or distribution volume of drug as compared to adult values." | ( Pharmacokinetics of oral and intravenous indomethacin in preterm infants. Bhat, R; Burns, L; Evans, M; Fisher, E; Hastreiter, A; Ramirez, JL; Vidyasagar, D, 1980) | 0.53 |
" Inhalation dose-response curves to PGE2 in doses from 10 to 400 micrograms were constructed on three separate occasions." | ( The effects of oral propranolol and indomethacin on the response to inhaled PGE2 in normal human subjects. Bevan, M; Davies, BH; Walters, EH, 1982) | 0.54 |
"Experiments were performed in pigs to examine the relationship between the effects of various nonsteroid antiinflammatory drugs on gastric (fundic) mucosal content of prostaglandin (PG)E2 and 6-keto-PGF1 alpha, and the development of damage to the fundic mucosa under acute and chronic dosage conditions." | ( Relationship of gastric mucosal damage induced in pigs by antiinflammatory drugs to their effects on prostaglandin production. Rainsford, KD; Willis, C, 1982) | 0.26 |
"Rats were dosed with the cathartics cascara, phenolphthalein, senna or ricinoleic acid with or without a 3 day pretreatment with indomethacin." | ( The effect of cathartics on prostaglandin synthesis by rat gastro-intestinal tract. Cohen, MM, 1982) | 0.47 |
" For diclofenac, indometacin and piroxicam proposals for a more rational procedure of their dose-response relationship determination are discussed." | ( [Transsynovial kinetics and correlation of dosage and effect of non-steroidal anti-rheumatic agents]. Fenner, H, 1982) | 0.26 |
" Computerized thermography showed that, at a dosage of 600 mg daily, benoxaprofen had a significant antiinflammatory effect; this observation was confirmed by the comparison with indomethacin." | ( Benoxaprofen--dose-range studies using quantitative thermography. Bacon, PA; Davies, J; Ring, FJ, 1980) | 0.45 |
" Naproxen has a high therapeutic index and a shallow dose-response curve, so the effect of other drugs on its pharmacokinetics is not likely to have a large clinical impact." | ( Naproxen sodium (Anaprox): pharmacology, pharmacokinetics and drug interactions. Segre, EJ, 1980) | 0.26 |
"In the isolated perfused hindlimb preparation of rats treated with corticosterone (2 x 20 mg/kg daily for 2 days), the dose-response curve to noradrenaline was shifted to the left, indicating supersensitivity of the vascular bed to noradrenaline." | ( Reversal of corticosterone-induced supersensitivity of vascular smooth muscle to noradrenaline by arachidonic acid and prostacyclin. Burkart, G; Dietz, R; Gross, F; Rascher, W; Schömig, A, 1980) | 0.26 |
" For most of the efficacy variables studied, the carprofen high dosage regimen at weeks 5 and 6 was shown statistically superior or at least not different from the indomethacin group; both of these were superior to the carprofen low dosage regimen." | ( Comparative evaluation of carprofen and indomethacin in rheumatoid patients. Caron, M; Lussier, A; Rouleau, L; Tétreault, L, 1980) | 0.72 |
" In general carprofen appears to be well tolerated, and at the dosage used its efficacy was good and equal to that of indomethacin." | ( Carprofen in soft-tissue rheumatism. A controlled trial. Schorn, D, 1981) | 0.47 |
" Dose-response experiments performed with 2 to 90 per cent (v/v) zymosan-activated plasma showed a direct correlation between the rate of neutrophil influx and the degree of vascular permeability in blood flow." | ( Vascular responses during acute neutrophilic inflammation. Their relationship to in vivo neutrophil emigration. Issekutz, AC, 1981) | 0.26 |
" The initial steroid dosage could be reduced 72% in the indoprofen group and 53% in the indomethacin group; 50% of the patients receiving indoprofen and 22." | ( Double-blind multicentre, between patients comparison of indoprofen and indomethacin in rheumatoid arthritis patients under basic steroid treatment. del Campo, JB, 1981) | 0.72 |
" In a comparison of two non-steroidal anti-inflammatory agents in this condition we attempted to overcome the difficulties by using a run-in period during which the dosage of one of the trial drugs was adjusted to suit the individual patient." | ( The run-in period in trial design: a comparison of two non-steroidal anti-inflammatory agents in psoriatic arthropathy. Bird, HA; Fowler, PD; Leatham, PA; Wright, V, 1982) | 0.26 |
"The safety and efficacy of benoxaprofen (300 or 600 mg) and indomethacin 75 to 150 mg) were compared in optimum dosage levels for 91 patients with rheumatoid arthritis or osteoarthritis." | ( Crossover comparison of benoxaprofen and indomethacin in rheumatoid arthritis and osteoarthritis. Chodock, AL, 1982) | 0.77 |
" The adsorption and disposition of hydrochlorothiazide demonstrate that this drug is rapidly absorbed and produces a diuretic and natriuretic response that peaks at approximately 2 hours after dosing and is essentially terminated 12 hours after dosing." | ( Hydrochlorothiazide pharmacokinetics and pharmacologic effect: the influence of indomethacin. Benet, LZ; Berman, RS; Davies, RO; Gee, WL; Holmes, GI; Huber, P; Lin, ET; Williams, RL, 1982) | 0.49 |
" The dose-response curve for prednisolone plateaued at high doses." | ( Influence of prednisolone on ethanol-induced gastric injury in the rat. Derelanko, MJ; Long, JF, 1982) | 0.26 |
"Two osmotically driven, controlled-release dosage forms of indomethacin were evaluated in a multiple-dose crossover study in 12 healthy subjects." | ( Kinetics of osmotically controlled indomethacin delivery systems after repeated dosing. Bayne, W; Davies, RO; Kwan, KC; Lee, RB; Place, V; Rogers, JD; Theeuwes, F, 1982) | 0.78 |
" After the washout period, and at the end of each 2 week active treatment period, blood samples were taken during a dosage interval for assay of indomethacin concentrations in plasma." | ( A clinical and pharmacokinetic study of indomethacin in standard and slow release formulations. Adams, KR; Baber, N; Halliday, LD; Littler, T; Orme, ML; Sibeon, RG, 1982) | 0.73 |
"5% for 25- and 50-mg dosage forms, respectively." | ( HPLC analysis of indomethacin and its impurities in capsule and suppository formulations. Kwong, E; McErlane, KM; Pillai, GK, 1982) | 0.6 |
" To produce an exact dosage form, a formula for the determination of the displacement value was derived, and it was found that theobroma oil greater than esterified fatty acids (C10-C18) greater than polyethylene glycol 1000." | ( Medicament release from suppository bases I: Physicochemical characteristics and bioavailability of indomethacin in rabbits. Bohidar, NR; Plakogiannis, FM; Reid, VE; Vidras, NJ, 1982) | 0.48 |
" It was found that in the rat and guinea pig the ratio of deacylated to demethylated metabolites was dependent on the substrate concentration of indomethacin, whereas in the rabbit the ratio remained constant in the dosage range investigated (1-10 mumoles)." | ( Investigations on the in vitro dose-related metabolism of indomethacin in four laboratory species. Carless, JE; Rowe, JS, 1982) | 0.71 |
" The dosage has to be established individually for each patient because the resorption is independent from body size and body weight." | ( [Distribution of non-steroidal anti-inflammatory agents in human tissues]. Köhler, G, 1982) | 0.26 |
"In a double-blind cross-over study 2 groups of 6 healthy volunteers were dosed with 2 x 75 mg and 3 x 75 mg/d oxametacin (1-p-chlorobenzoyl-2-methyl-5-methoxy-3-indolylacethydroxamic acid)." | ( [Pharmacokinetics of oxametacin in healthy volunteers following multiple administration (author's transl)]. Dittrich, P; Ferber, H; Kukovetz, WR; Vergin, H, 1981) | 0.26 |
" In therapeutic dosage it will adequately control joint symptoms in the majority of patients." | ( Pharmacotherapy of juvenile rheumatoid arthritis. Lindsley, CB, 1981) | 0.26 |
" However, the 10-week cessation of treatment following this effective dosage led to a rapid development of tumors." | ( Inhibition of development of methylnitrosourea-induced rat colon tumors by indomethacin treatment. Goto, A; Kudo, T; Narisawa, T; Sato, M; Takahashi, T; Tani, M, 1981) | 0.49 |
" The doses selected represented the manufacturer's highest recommended dosage for the treatment of arthritic disorders." | ( A comparative endoscopic evaluation of the damaging effects of nonsteroidal anti-inflammatory agents on the gastric and duodenal mucosa. Chen, TT; Lanza, FL; Nelson, RS; Rack, MF; Royer, GL; Seckman, CE, 1981) | 0.26 |
"9 patients with rheumatoid arthritis and one with activated gonarthrosis were treated by means of application of Amuno ointment to one knee in a dosage of 3 X 5 cm ribbon of ointment, rubbed in on an area of approximately 200 cm2, over a period of 3 days." | ( [Local rheumatoid therapy. Indomethacin level in the synovia and serum after application of Amuno ointment]. Miehle, W; Rehs, EL; Zollner, E, 1981) | 0.56 |
" Dose-response studies showed that the maximal excretion of urinary PGE and water was obtained by administration of theophylline (50 mg/kg), where the increase in PGE was about 20 times that of the control." | ( Effects of methylxanthines on urinary prostaglandin E excretion in rats. Aizawa, Y; Kogo, H; Takeuchi, K, 1981) | 0.26 |
" On the other hand, the degree of intestinal lesions induced by acemetacin which became apparent 24 hours after dosing were about the same as that induced by indomethacin." | ( [Irritative effects of acemetacin and indomethacin on the gastrointestinal tracts of rats (author's transl)]. Nakamura, M; Suzuki, H; Wada, Y; Yoshinaka, Y, 1981) | 0.73 |
" ETA did not affect the phenylephrine dose-response curves and nor did 8 micrograms/ml of indomethacin, whereas the high dose was inhibitory." | ( Role of prostaglandins in contractile activity of the ampulla of the rabbit oviduct. Coons, LW; Harper, MJ; Hodgson, BJ; Radicke, DA; Valenzuela, G, 1980) | 0.48 |
" The score classified the patients into three groups and enabled us to treat them with a correct dosage and period according to the clinical findings at admission of the patients." | ( Classification of threatened premature labor related to treatment with a prostaglandin inhibitor: indomethacin. Abramovici, H; Atad, J; David, A; Moise, J, 1980) | 0.48 |
" Based on the inhibitory effect of the steroidal anti-inflammatory drugs, non-steroidal agents, such as indomethacin, were also expected to show some degree of inhibition; however, repeated tumor experiments demonstrate that indomethacin enhances TPA promotion in a dose-response manner." | ( Indomethacin enhancement of TPA tumor promotion in mice. Fischer, SM; Gleason, GL; Mills, GD; Slaga, TJ, 1980) | 1.92 |
" These animals were then assigned randomly to dose groups (1, 2 or 4 mg/kg/day of indomethacin and 100, 200, or 300 mg/kg/day of aspirin) and were dosed for 21 days." | ( Indomethacin and aspirin: effect of nonsteroidal anti-inflammatory agents on the rate of fracture repair in the rat. Allen, HL; Bear, WT; Wase, A, 1980) | 1.93 |
" Indomethacin significantly altered dose-response curves of furosemide." | ( Pharmacokinetic-dynamic analysis of the indomethacin-furosemide interaction in man. Brater, DC; Chennavasin, P; Seiwell, R, 1980) | 1.44 |
" Dose-response curves to norepinephrine in the presence of hydralazine were shifted to the right in parallel fashion at an only slight reduction of the maximum response." | ( Studies on the direct vasodilator effect of hydralazine in the isolated rabbit renal artery. Gross, F; Khayyal, M; Kreye, VA, 1981) | 0.26 |
" An overestimation of rare side-effects of drugs should not block the application of certain medicaments, however, they should be given only in such a high dosage as it is necessary." | ( [Hematotoxic lesions caused by non-steroidal antirheumatic agents]. Hüge, W; Stobbe, H, 1980) | 0.26 |
" CAT, SOD, or both together, at a dosage of 5,000 U/kg each." | ( Oxygen radical scavengers are protective against indomethacin-induced intestinal ulceration in the rat. Dinari, G; Fisher, S; Heckelman, B; Kiro, A; Marcus, H; Zahavi, I, 1995) | 0.55 |
" Indomethacin shifted the G-CSF dose-response curve of cells treated with 10 nM RA to lower G-CSF concentrations." | ( Indomethacin potentiates the induction of HL60 differentiation to neutrophils, by retinoic acid and granulocyte colony-stimulating factor, and to monocytes, by vitamin D3. Brown, G; Bunce, CM; Durham, J; French, PJ; Michell, RH; Stockley, RA, 1994) | 2.64 |
" A rapid, transient relaxation was observed during the cumulative dose-response and a new plateau of equilibrium was seen following an increase in developed force after the last dose of SP." | ( Substance P induces biphasic endothelium-dependent relaxations in pig and rabbit carotid arteries. Arden, WA; Fiscus, RR; Gross, DR; Lanzo, S; Maley, RH; Salley, RK, 1994) | 0.29 |
" Results were presented as dose-response curves." | ( Local modulation of adrenergic responses in the hindlimb vasculature of the intact conscious rat. Chen, CY; Collins, HL; DiCarlo, SE; Patil, RD, 1995) | 0.29 |
" When the endothelium was removed, however, the dose-response curves of both groups of rats were shifted to the left with an increase in maximum responses and they were no longer significantly different (max." | ( Effect of swimming on vascular reactivity to phenylephrine and KC1 in male rats. Jansakul, C, 1995) | 0.29 |
" However SX6C was more potent than ETs and the dose-response curve was significantly steeper and achieved a higher maximum." | ( Actions of endothelins and sarafotoxin 6c in the rat isolated perfused lung. Lal, H; Williams, KI; Woodward, B, 1995) | 0.29 |
"The pharmacokinetics of Ind solution at a dosage of 3 mg." | ( Absorption of indomethacin from nasal cavity in rats. Huang, ZL; Kagawa, E; Kagoshima, M; Shimada, H, 1995) | 0.65 |
" The lower dosage of 4 mg was effective throughout and there was little to be gained by increasing the dose as further reduction of granuloma size was not obtained." | ( OM-89 modulation of chronic inflammation: relevance to clinical use. Gowland, G; Moore, AR; Willis, D; Willoughby, DA, 1995) | 0.29 |
" Indomethacin, 200 to 250 mg per day generally kept the headache at bay, but during exacerbations, especially during menstrual periods, the dosage transitorily had to be increased to 250 to 350 mg per day." | ( CPH and hemicrania continua: requirements of high indomethacin dosages--an ominous sign? Antonaci, F; Fredriksen, TA; Sjaastad, O; Stolt-Nielsen, A; Stovner, LJ, 1995) | 1.45 |
" The dose-response curves to angiotensin I (n = 6) were significantly displaced to the right by captopril in a concentration-dependent manner." | ( Effects of captopril on the human foetal placental circulation: an interaction with bradykinin and angiotensin I. de Moura, R; Lopes, MA, 1995) | 0.29 |
" Utilizing the dorsal hand vein technique, dose-response curves to bradykinin (maximum dose = 513 ng/min) were constructed in veins preconstricted with the alpha-adrenergic agonist phenylephrine in healthy young volunteers." | ( Mechanism of bradykinin-induced venodilation in humans. Blaschke, TF; Dachman, WD; Ford, GA; Hoffman, BB, 1993) | 0.29 |
" The two products were not found to be statistically different with respect to the lag time between dosing and first appearance of the drug in the serum (1." | ( A pharmacokinetic study on two sustained-release formulations of indomethacin in normal subjects following a single dose administration. Hasan, MM; Muti, HY; Najib, NM, 1994) | 0.53 |
" Baseline growth and survival of macrophages were established for cultures grown on standard medium, then effects of the following were examined: indomethacin (10(-6) M) as it influences initial production of macrophages from precursors and later survival of differentiated cells; and macrophage colony-stimulating factor (M-CSF), used alone at moderate dosage (50-100 U), and combined with granulocyte-macrophage CSF (both 200 U), for its importance to long-term survival of the population." | ( Exogenous cytokines enhance survival of macrophages from organ cultured embryonic rat tissues. Hoyt, RF; McNelly, NA; Sorokin, SP, 1994) | 0.49 |
" Analysis of dose-response curves for prostaglandin F2 alpha (PGF2 alpha), U46619, a stable thromboxane analog, and norepinephrine (NE) after pretreatment with INDO demonstrated that inhibition of endogenous eicosanoids significantly attenuated the vasoconstrictor response to PGF2 alpha and U46619 but not to NE." | ( The interaction between endothelium-derived relaxing factor (EDRF) and eicosanoids in the regulation of the mesenteric microcirculation. Farhat, M; Hoy, GR; Kodama, T; Marmon, LM; Ramwell, PW; Vargas, R, 1995) | 0.29 |
" Indomethacin dissolution from powder and capsule dosage forms, even in an acidic medium, was drastically accelerated by the hybridization." | ( Drug dissolution from indomethacin-starch hybrid powders prepared by the dry impact blending method. Honda, H; Ishizaka, T; Koishi, M, 1993) | 1.51 |
"Liquid and semi-solid enteric dosage forms were prepared by entrapping drug with an appropriate partition coefficient in a lipid base vehicle which would then be released by the action of intestinal enzymes." | ( Use of enzymatic activity for design of orally administered enteric dosing forms. Ishizaka, M; Nishihata, T; Yamamoto, K, 1993) | 0.29 |
" The YM022 dosage required in this model was much greater than that required in the inhibition of gastric acid." | ( YM022 [(R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl- 1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea], a potent and selective gastrin/cholecystokinin-B receptor antagonist, prevents gastric and duodenal lesions in rats. Akuzawa, S; Ito, H; Kamato, T; Kobayashi, A; Miyata, K; Nagakura, Y; Nishida, A; Takinami, Y; Yamano, M; Yuki, H, 1994) | 0.29 |
" Oral temperature was measured before dosing and then every 4 h until apyrexia." | ( Antipyretic efficacy of indomethacin and acetaminophen in uncomplicated falciparum malaria. Looareesuwan, S; Wilairatana, P, 1994) | 0.6 |
" In an attempt to reproduce a human dosing regimen, another group of rats, for a total of 30 weeks, received consecutive periods of indomethacin at 3 mg." | ( Ulceration, fibrosis and diaphragm-like lesions in the caecum of rats treated with indomethacin. Anthony, A; Dhillon, AP; Nygard, G; Pounder, RE; Sim, R; Wakefield, AJ, 1994) | 0.72 |
" The time course and dose-response to PGE2 of IL-6 production were determined." | ( Prostaglandin E2 stimulates the production of interleukin-6 by neonatal mouse parietal bones. Braidman, IP; Davie, MW; Holt, I; Marshall, MJ, 1994) | 0.29 |
"The phenomenon of supercooperativity in platelet aggregation is manifested by the occurrence of clear-cut thresholds in dose-response relationships; in such cases the Hill coefficient has unusually high values." | ( Supercooperativity in platelet aggregation: substituted pyridyl isoxazoles, a new class of supercooperative platelet aggregation inhibitors. Demina, OV; Shram, SI; Varfolomeev, SD; Vrzheshch, PV, 1994) | 0.29 |
" The high concentrations of IM-OE compared with indomethacin were detected in liver 3 h after oral dosing of the prodrug, although IM-OE was not detected in plasma." | ( Pharmacokinetics of indomethacin octyl ester (prodrug) and indomethacin produced from the prodrug. Iwaki, M; Kinoshita, T; Ogiso, T; Paku, T; Tanino, T, 1994) | 0.87 |
" In healthy volunteers full dose-response curves were constructed by infusing histamine, before and after administration of an H1 or H2 antagonist or both antagonists, into dorsal hand veins preconstricted with the alpha-adrenergic agonist phenylephrine." | ( Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. Bedarida, G; Blaschke, TF; Dachman, WD; Hoffman, BB, 1994) | 0.29 |
" The results demonstrated that, while indomethacin is effective in decreasing the formation of heterotopic bone, piroxicam--when used in the dosage previously demonstrated to have no deleterious effect on healing bone--is not." | ( Effect of two nonsteroidal antiinflammatory drugs on heterotopic bone formation in a rabbit model. Fakhouri, AJ; Moed, BR; Nallamothu, B; Resnick, RB; Wagner, RA, 1994) | 0.56 |
" Urine samples were obtained over 36 hours post-metolazone dosing for the determination of sodium, potassium and metolazone concentration." | ( The effect of nonsteroidal agents (NSAIDs) on the pharmacokinetics and pharmacodynamics of metolazone. Gehr, TW; Kish, C; Ripley, EB; Sica, DA; Wade, J; Wallace, H, 1994) | 0.29 |
"Isolated rabbit kidneys were perfused with Krebs-Henseleit solution in an open system designed to allow study of dose-response relationships." | ( The effect of indomethacin and reserpine on renal vascular escape. de Lima e Forti, CA; Fonteles, MC, 1993) | 0.65 |
" The importance of systemically mediated damage was further determined by gastrotoxicity dose-response curves and pyloric ligation experiments in which indomethacin was administered either orally or parenterally, or into stomach or duodenum with the pylorus occluded." | ( Gastric mucosal damage induced by nonsalicylate nonsteroidal antiinflammatory drugs in rats is mediated systemically. Giraud, AS; Skeljo, MV; Yeomans, ND, 1993) | 0.48 |
" Indomethacin did not affect the ET-1-induced pallor but significantly shifted to the right the flare dose-response curve to ET-1." | ( Cyclooxygenase products mediate the cutaneous vasodilation induced by endothelin-1 in humans. Bellofiore, S; Di Maria, GU; Mistretta, A; Novo, S; Puglisi, S; Ricciardolo, FL, 1993) | 1.2 |
" Differences were tested by analysis of covariance of the dose-response curves." | ( Influence of dietary fat on duodenal resistance to acid. Guarner, F; Lugea, A; Malagelada, JR; Salas, A, 1993) | 0.29 |
"Full dose-response curves were constructed in 13 hypercholesterolemic and 12 normocholesterolemic subjects by infusing bradykinin (0." | ( Responsiveness to bradykinin in veins of hypercholesterolemic humans. Bedarida, GV; Blaschke, TF; Bushell, E; Haefeli, WE; Hoffman, BB, 1993) | 0.29 |
" The PTHrP dose-response curve was not affected by 10 microM indomethacin." | ( Renin stimulating properties of parathyroid hormone-related peptide in the isolated perfused rat kidney. Helwig, JJ; Judes, C; Massfelder, T; Parnin, F; Saussine, C; Simeoni, U, 1993) | 0.53 |
"25 or 0h oral dosing of the 5-lipoxygenase inhibitor, MK-886, but not when only one of these doses was given." | ( Leukotrienes in the pathogenesis of NSAID-induced gastric and intestinal mucosal damage. Rainsford, KD, 1993) | 0.29 |
" NA increased mucociliary activity at a dosage of 10(-5) mol/kg, the maximal increase being 16." | ( The effect of noradrenaline on mucociliary activity in the rabbit maxillary sinus. Cervin, A; Lindberg, S; Mercke, U, 1993) | 0.29 |
" Dose-response curves, the hemodynamic effects of prostacyclin (20 micrograms/kg) and its inhibitor indomethacin and measurements of plasma and urinary levels of 6-keto-prostaglandin F1 alpha were compared in three groups of six rats each: normal, with portal vein stenosis and with secondary biliary cirrhosis." | ( Role of prostacyclin in hemodynamic alterations in conscious rats with extrahepatic or intrahepatic portal hypertension. Cailmail, S; Lebrec, D; Moreau, R; Oberti, F; Pipy, B; Sogni, P, 1993) | 0.5 |
" In both tests KT had a poor analgesic effect without dose-response relationships." | ( Ketorolac tromethamine: an experimental study of its analgesic effects in the rat. Bustamante, D; Paeile, C, 1993) | 0.29 |
" Neutrophil infiltration into the antrum was detectable 1 hour after dosing with indomethacin, at which time damage was apparent microscopically but not macroscopically." | ( Do infiltrating neutrophils contribute to the pathogenesis of indomethacin induced ulceration of the rat gastric antrum? Clayton, NM; Harman, IW; Strong, P; Trevethick, MA, 1993) | 0.75 |
" The dose-response relationship of indomethacin for inhibition of prostaglandin formation and rebamipide-induced protection correlated well and 5 mg/kg indomethacin completely prevented the protective effect of rebamipide." | ( Stimulation of prostaglandin biosynthesis mediates gastroprotective effect of rebamipide in rats. Kleine, A; Kluge, S; Peskar, BM, 1993) | 0.56 |
" In particular, the plasma levels observed with the hydrogel suppositories of 1% (w/v) gum concentration were sustained much longer than those after dosing with the commercial suppositories; the mean residence times had higher values without a decrease in the area under the plasma concentration vs." | ( Investigation on rectal absorption of indomethacin from sustained-release hydrogel suppositories prepared with water-soluble dietary fibers, xanthan gum and locust bean gum. Isowa, K; Machida, Y; Nagai, T; Takayama, K; Watanabe, K; Yakou, S, 1993) | 0.56 |
" Such a complex dose-response effect may have significant impact in explaining the pathologic effects of NO2." | ( Dual effect of nitrogen dioxide on rat alveolar macrophage arachidonate metabolism. Forman, HJ; Robison, TW, ) | 0.13 |
" However, when administered 24 hr before challenge, the same drug dosage had no effect in enhancing survival." | ( Accelerated hematopoietic recovery and protective effect of the cyclooxygenase inhibitor indomethacin in bacterial infection of neutropenic mice. Binaglia, L; Campanile, F; Fioretti, MC; Giampietri, A; Grohmann, U; Puccetti, P, 1993) | 0.51 |
" The leukotriene receptor antagonist ICI-198,615 (3 x 10(-8)M) produced an approximate 50-fold rightward shift of the leukotriene C4 dose-response curve (n = 5)." | ( Influence of atherosclerosis on the vascular reactivity of isolated human epicardial coronary arteries to leukotriene C4. Allen, SP; Chester, AH; Collins, M; Dashwood, MR; Piper, PJ; Tadjkarimi, S; Yacoub, MH, 1993) | 0.29 |
" It is concluded that (i) the protective effect of unmodified and acidified hydrotalcit is independent of the eicosanoid system; (ii) protection against indomethacin induced gastric lesions does not require treatment before dosing of the ulcerogen and does not interfere with absorption and anti-inflammatory actions of indomethacin; (iii) endogenous nitric oxide and afferent neurons contribute partly to the effect of unmodified, but not of acidified, hydrotalcit suggesting that different mechanisms mediate their mucosal protective activity." | ( Role of eicosanoids, nitric oxide, and afferent neurons in antacid induced protection in the rat stomach. Korolkiewicz, R; Lambrecht, N; Liszkay, M; Peskar, BM; Trautmann, M, 1993) | 0.48 |
" After pretreatment of myometrial explants with a cyclo-oxygenase inhibitor (indomethacin), the PGF2 alpha dose-response curve was shifted to the left and a maximal level of PGF2 alpha-induced IP accumulation was reached." | ( Prostaglandin F2 alpha stimulates inositol phosphate production in human pregnant myometrium. Breuiller-Fouche, M; Ferre, F; Geny, B; Maka, FD, 1993) | 0.51 |
" The addition of IL-1ra to a maximally effective antiinflammatory dosage of indomethacin (5 mg/kg) resulted in further reductions of cell number and exudate volume, suggesting that the antiinflammatory effects of IL-1ra in the 5-h model were not due solely to inhibition of IL-1-induced prostaglandin biosynthesis." | ( Effect of treatment with interleukin-1 receptor antagonist on the development of carrageenan-induced pleurisy in the rat. Coffey, JW; Czachowski, CL; Meyers, KP, 1993) | 0.52 |
" Angiotensin II dose-response studies were performed in conscious, chronically instrumented cirrhotic and control rats, and angiotensin II concentration-response studies were performed in isolated blood vessels obtained from similar groups of animals." | ( Dissociation between pressor sensitivity in vivo and contractile reactivity in vitro to angiotensin II in rats with experimental cirrhosis. Leehey, DJ, 1993) | 0.29 |
" Despite the sodium restriction, amiloride had no effect on FELi, although the dosage was sufficient to cause a 6-fold increase in sodium excretion, and potassium retention." | ( Indomethacin- and desamino-8-D-arginine vasopressin-induced lithium reabsorption is not amiloride sensitive in humans. Bijlsma, JA; Boer, WH; Dorhout Mees, EJ; Koomans, HA; van Rijn, HJ, 1993) | 1.73 |
" Compound 20 has an efficacy profile that is superior or comparable to that of the nonselective COX inhibitor indomethacin in animal models of inflammation, pain, and fever and appears to be nonulcerogenic within the dosage ranges required for functional efficacy." | ( Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. Black, WC; Chan, CC; Ford-Hutchinson, AW; Gauthier, JY; Gordon, R; Guay, D; Kargman, S; Lau, CK; Li, CS; Mancini, J, 1995) | 0.5 |
" We examined the effect of oral dosing with indomethacin on ovalbumin serum levels and the systemic immune response to ovalbumin in mice fed with ovalbumin." | ( Decrease in systemic tolerance to fed ovalbumin in indomethacin-treated mice. Belaiche, J; Deprez, M; Franchimont, D; Lamproye, A; Louis, E; Mahieu, P; Schaaf, N, 1996) | 0.81 |
" It was also demonstrable after subcutaneous dosing or when injury was measured by a change in mucosal potential difference." | ( Gastric mucosal adaptation to diclofenac injury. Cook, GA; Elliott, SL; Giraud, AS; Skeljo, MV; Yeomans, ND, 1996) | 0.29 |
" The fentanyl dose-response curve was unchanged by opioid receptor blockade with 10(-6)M naloxone and by alpha and beta adrenoceptor blockade produced by 10(-6)M prazosin and 10(-6)M propranolol." | ( Direct effects of fentanyl on canine coronary artery rings. Bridges, MT; Grover, TE; Introna, RP; Pruett, JK; Yodlowski, EH, 1995) | 0.29 |
"The interval between indomethacin dosage and clinical response was assessed in hemicrania continua (n = 12) and chronic paroxysmal hemicrania (n = 11) sufferers." | ( Chronic paroxysmal hemicrania and hemicrania continua. Interval between indomethacin administration and response. Pareja, J; Sjaastad, O, 1996) | 0.85 |
" These results indicate that the dosage regimen of CAZ should be adjusted after the first week of life except in infants who were postnatally exposed to indomethacin." | ( Ceftazidime pharmacokinetics in preterm infants: effect of postnatal age and postnatal exposure to indomethacin. de Groot, R; Hop, WC; Neijens, HJ; Schoemaker, RC; van den Anker, JN; van der Heijden, BJ, 1995) | 0.71 |
" Hourly dosing with hydrochloric acid reversed the protective effect of ranitidine, cimetidine and loxtidine on macroscopic damage and, histologically, this was associated with the widespread appearance of antral ulcers and a reduction in the proportion of mucosal damage caused by superficial erosions." | ( The role of acid in the pathogenesis of indomethacin-induced gastric antral ulcers in the rat. Clayton, NM; Oakley, I; Trevethick, MA; Williams, LV, 1996) | 0.56 |
"05) after dosing with indomethacin." | ( The effect of indomethacin-induced gastric mucosal injury on 24-h intragastric acidity and plasma gastrin concentration in healthy volunteers. Chiba, N; Hunt, RH; Johnson, DM; McDonald, TM; Rademaker, JW; Rainsford, KD; Stetsko, PI, 1995) | 0.97 |
"The dose-response relationship for the inhibitory effect of indomethacin on implantation and continuance of pregnancy was examined in four groups of rabbits administered with indomethacin (2." | ( Inhibitory effects of indomethacin on implantation and its related phenomena. Endo, T; Kanayama, K; Nariai, K; Osada, H, ) | 0.69 |
" The dosage of cation exchange resins was decreased, oral fluids were tolerated, and the patient's general condition improved." | ( Effect of hydrochlorothiazide in pseudohypoaldosteronism with hypercalciuria and severe hyperkalemia. Rosa, FC; Stone, RC; Vale, P, 1996) | 0.29 |
" Dose-response curves to topically applied Krebs' solution saturated with halothane at increasing concentrations of 0%, 1%, 3% and 5% were carried out in the presence of an inhibitor of nitric oxide synthesis (N omega-nitro-L-arginine (LNA), 300 mumol litre-1) or inhibitors of prostaglandin synthesis (mefenamic acid 20 mumol litre-1 or indomethacin 20 mol litre-1) or in the absence of any inhibitor." | ( Role of prostaglandins and nitric oxide on halothane-induced arteriolar dilatation in rat diaphragm. Aubier, M; Boczkowski, J; de Larminat, V; Desmonts, JM; Dureuil, B; Farinotti, R; Vicaut, E, 1996) | 0.47 |
"To examine abnormalities of prostanoid metabolism in lupus nephritis, which may affect renal function, and the effects of 4 day dosing of a selective thromboxane A2 (TXA2) synthetase inhibitor, DP-1904, on prostanoid metabolism." | ( Improvement of renal function with a selective thromboxane A2 synthetase inhibitor, DP-1904, in lupus nephritis. Homma, M; Ichikawa, Y; Kameda, H; Tojo, T; Yoshida, T, 1996) | 0.29 |
" Close monitoring of renal function of the neonate and vancomycin dosage individualization are mandatory when the above factors are present." | ( [Pharmacokinetics of vancomycin in neonates of postconceptional age less than or equal to 32 weeks]. Altirriba Valls, O; Demestre Guasch, X; Farré Riba, R; Ginovart Galiana, G; Lopes Santos, AP; Mangues Bafalluy, MA, 1996) | 0.29 |
" Dose-response curves to insulin (2 to 2000 microU/ml) were compared for extraluminal (EL), intraluminal (IL), and combined IL-EL application." | ( Direct vasodilatory effect of insulin on isolated retinal arterioles. Alder, VA; Cringle, SJ; Su, EN; Yu, DY; Yu, PK, 1996) | 0.29 |
" Exposure to EL insulin while the IL K+ contraction dose-response curve was measured had no effect." | ( Direct vasodilatory effect of insulin on isolated retinal arterioles. Alder, VA; Cringle, SJ; Su, EN; Yu, DY; Yu, PK, 1996) | 0.29 |
" The requirement that suspension eyedrops and similar dosage forms should be redispersable after sedimentation upon storage is stated in the monographs on eyedrops of the German Pharmacopoeia and can be found in similar contexts in other pharmacopoeias." | ( [Dosage problems in suspension eyedrops]. Diestelhorst, M; Kwon, KA; Süverkrüp, R, ) | 0.13 |
" A variable dosing pattern with acceptable mean was observed for Chibro-Amuno 3, while the results for Inflanefran-forte were fully satisfactory." | ( [Dosage problems in suspension eyedrops]. Diestelhorst, M; Kwon, KA; Süverkrüp, R, ) | 0.13 |
" Bk reduced the size of the pressor responses at relatively low concentrations (2-60 nM) but the dose-response curve was flat and the maximum inhibitory effect hardly exceeded 50 percent." | ( Comparison of the vasodilatory effects of bradykinin in isolated dog renal arteries and in buffer-perfused dog kidneys. Hadházy, P; Koltai, MZ; Malomvölgyi, B; Pogátsa, G; Tekes, K, 1996) | 0.29 |
" The effect of amylin on gastric ulcers induced by oral administration of indomethacin (Indo, 20 mg kg-1 at a dosing volume of 5 ml) or ethanol 50% (EtOH, 1 ml/rat) was investigated in conscious rats." | ( Protection by amylin of gastric erosions induced by indomethacin or ethanol in rats. Guidobono, F; Netti, C; Pagani, F; Pecile, A; Sibilia, V; Ticozzi, C, 1997) | 0.78 |
" Rats were dosed concomitantly with indomethacin (40 mg/kg, subcutaneously) and an amino or pyridinyl bisphosphonate (orally at." | ( Nonclinical model for assessing gastric effects of bisphosphonates. Berman, SK; Blank, MA; Ems, BL; Gibson, GW; Myers, WR; Phipps, RJ; Smith, PN, 1997) | 0.57 |
" Rats were injected with indomethacin to reduce endogenous prostaglandin synthesis and dosed with prostaglandin analogues or prostacyclin." | ( Absorption, retention and urinary excretion of chromium-51 in rats pretreated with indomethacin and dosed with dimethylprostaglandin E2, misoprostol or prostacyclin. Adeleye, BO; Davis-Whitenack, ML; Kamath, SM; Sangiah, S; Smith, MM; Stoecker, BJ, 1997) | 0.83 |
" Clentiazem dose-response curves for both coronary dilation and negative inotropic effects were determined under control conditions and in the presence of the nitric oxide (NO) synthase inhibitor, NG-nitro-L-arginine (L-NAME, 30 microM), and the cyclooxygenase inhibitor, indomethacin (10 microM)." | ( Coronary and cardiac sensitivity to the vasoselective benzothiazepine-like calcium antagonist, clentiazem, in experimental heart failure. Blaise, G; Dumont, L; Jasmin, G; Tanguay, M, 1997) | 0.48 |
" Gastrointestinal ulceration was assessed, four hours after a single dose and 24 hours following the last dose of a chronic four day dosing regimen, by counting the number of lesions and ulcers present." | ( Comparative evaluation of the severity of gastric ulceration by solid dispersions and coprecipitates of indomethacin. Degennaro, MD; Karnachi, AA; Khan, MA; Reddy, IK, 1997) | 0.51 |
" The alpha 1-AR antagonist prazosin shifted the NE dose-response curve to the right, and phenylephrine (alpha 1-AR agonist) induced a dose-dependent contraction that was potentiated by L-NAME or removal of the endothelium." | ( Norepinephrine-induced contraction of isolated rabbit bronchial artery: role of alpha 1- and alpha 2-adrenoceptor activation. Sielczak, MW; Smith, DA; Wanner, A; Zschauer, AO, 1997) | 0.3 |
"0 nmol kg-1), produced significant rightward displacements of the dose-response curve for 5-CT in methoxamine-infused pithed animals pretreated with ketanserin (0." | ( Role of 5-ht7 receptors in the long-lasting hypotensive response induced by 5-hydroxytryptamine in the rat. Terrón, JA, 1997) | 0.3 |
"5 mg/kg CyA/day and dosage was increased cautiously to 5 mg/kg/day or less if the serum creatinine rose by > or = 30% above baseline." | ( Interaction between cyclosporin A and nonsteroidal antiinflammatory drugs. Baker, P; Bensen, W; Gent, M; Grace, E; Ludwin, D; Roberts, R; Tugwell, P, 1997) | 0.3 |
" Male Sprague-Dawley rats were dosed with two doses of metronidazole (50 mg/kg, 12 and 1 h pre-NSAID) or a single 100 mg/kg dose of tempo 1 h prior to NSAIDs." | ( Pharmacological protection of NSAID-induced intestinal permeability in the rat: effect of tempo and metronidazole as potential free radical scavengers. Davies, NM; Jamali, F, 1997) | 0.3 |
"The influence of dosing time on the fever induced by interferon-alpha (IFN-alpha) was investigated in ICR male mice under light-dark cycle." | ( Circadian rhythm of fever induced by interferon-alpha in mice. Higuchi, S; Koyanagi, S; Ohdo, S; Yukawa, E, 1997) | 0.3 |
" The decrease in edema in the footpads of EFAD rats was nearly identical to the decrease in edema in the footpads of Control rats dosed with indomethacin." | ( Modulation of adjuvant-induced arthritis by dietary arachidonic acid in essential fatty acid-deficient rats. Chinn, KS; Mehta, A; Obukowicz, MG; Raz, A; Salsgiver, WJ; Welsch, DJ, 1997) | 0.5 |
" Lemakalim dose-response curves were also generated in rings pretreated with the nitric oxide synthase inhibitor, Nw-nitro-L-arginine methyl ester (L-NAME); the cyclooxygenase inhibitor, indomethacin; or the K+(ATP) channel antagonist, glybenclamide." | ( Halothane attenuates endothelium-dependent pulmonary vasorelaxant response to lemakalim, an adenosine triphosphate (ATP)-sensitive potassium channel agonist. Horibe, M; Murray, PA; Seki, S, 1997) | 0.49 |
" AA reduced the maximum amplitude of nIACh estimated from the dose-response relationship without causing an appreciable change in the apparent dissociation constant." | ( Inhibitory effects of arachidonic acid on nicotinic transmission in bullfrog sympathetic neurons. Minota, S; Watanabe, S, 1997) | 0.3 |
" They were found fairly potent in rat tail flick and mouse phenylquinone writhing assays but the dose-response curves were rather shallow as compared to that of morphine." | ( Apparent antinociceptive and anti-inflammatory effects of GYKI 52466. Kedves, R; Máté, I; Székely, JI; Tarnawa, I; Török, K, 1997) | 0.3 |
" Crisanole effect got higher with incrementing dosage of metallic gold." | ( [The effect of aurotherapy on the level of unsaturated fatty acids during the treatment of rheumatoid arthritis patients]. Virstiuk, NH, ) | 0.13 |
" Its use as a second agent in combination with another immunosuppressant might enable reduction in the dosage or time of application." | ( A low dose immunorestorative effect of aporphinoid alkaloid oxoglaucine on experimentally immunosuppressed and infected mice. Ivanovska, N; Philipov, S, 1997) | 0.3 |
" The use of a test dosage of 50 mg of indomethacin IM ('indotest') gives a clear-cut answer and may be a useful tool in the diagnostic arsenal in every unilateral headache for a proper clinical assessment." | ( Chronic paroxysmal hemicrania and hemicrania continua. Parenteral indomethacin: the 'indotest'. Antonaci, F; Caminero, AB; Pareja, JA; Sjaastad, O, 1998) | 0.81 |
" Mean dissolution time (MDT) of the drug was calculated from the release profile and it was used as a parameter to evaluate the influence of (a) polymer content in the dosage form, (b) ionic strength of the medium, and (c) the rotation speed of the paddle on the release characteristics of the drug." | ( The release mechanism of an oral controlled-release delivery system for indomethacin. Kinget, R; Rombaut, P; Talukdar, MM, 1998) | 0.53 |
" NMDA shifted the dose-response curve of AA to the right." | ( Further insights into the anti-aggregating activity of NMDA in human platelets. Alberti, L; De Montis, MG; Franconi, F; Miceli, M; Seghieri, G; Tagliamonte, A, 1998) | 0.3 |
") on gastric ulcers induced by the oral administration of ethanol 50% (EtOH, 2 ml/rat) or indomethacin (indomethacin, 20 mg kg(-1), at a dosing volume of 5 ml) were investigated in rats." | ( Investigation on the mechanisms involved in the central protective effect of amylin on gastric ulcers in rats. Guidobono, F; Netti, C; Pagani, F; Sibilia, V; Ticozzi, C, 1998) | 0.52 |
" The dosage of desmopressin (group A, n = 31 ) was 20 microg/day and the dosage of indomethacin (group B, n = 29) was 100 mg/day." | ( Desmopressin versus indomethacin treatment in primary nocturnal enuresis and the role of prostaglandins. Hasanoğlu, E; Sener, F; Söylemezoğlu, O, 1998) | 0.85 |
" However, when animals were pre-treated with BCG, the dose-response curves for both B1 agonists were shifted 2 to 8-fold to the left." | ( Systemic treatment with Mycobacterium bovis bacillus Calmette-Guérin (BCG) potentiates kinin B1 receptor agonist-induced nociception and oedema formation in the formalin test in mice. Calixto, JB; de Campos, RO; Henriques, MG, 1998) | 0.3 |
" The dose-response curve for methoxamine was shifted to the right and the maximum contractile response was impaired in mesenteric arterial beds from diabetic rats." | ( Possible modulation by endothelin-1, nitric oxide, prostaglandin I2 and thromboxane A2 of vasoconstriction induced by an alpha-agonist in mesenteric arterial bed from diabetic rats. Kamata, K; Makino, A, 1998) | 0.3 |
" To obtain dose-response curves, single doses (as boluses) of acetylcholine were infused and the maximal A-V delay induced by each dose was determined." | ( Endothelium-mediated negative dromotropic effects of intravascular acetylcholine. Ceballos, G; Rubio, R, 1998) | 0.3 |
"The pharmacokinetic parameters of vancomycin in a neonatal population have been characterized to enable development of optimum dosage guidelines for neonatal intensive-care units and to examine the relationship between these pharmacokinetic parameters and various demographic, developmental and clinical factors which might be associated with changes in the kinetic profile of vancomycin." | ( The kinetic profile of vancomycin in neonates. Almeida, AM; Bispo, MA; Costa, IM; Falcão, AC; Falcão, F; Palminha, JM; Reis, E; Silva, R, 1998) | 0.3 |
"We have determined the dose-response relationship between sulindac administration and inhibition of tumour growth in the rat." | ( Sulindac inhibits colorectal tumour growth, but not prostaglandin synthesis in the rat. Charalambous, D; O'Brien, PE; Skinner, SA, 1998) | 0.3 |
" Cumulative dose-response curves to insulin (10 microU/ml, 100 microU/ml, 1 mU/ml, and 10 mU/ml) were obtained in arterioles before and after endothelium removal or administration of either indomethacin (Indo, 10(-5) M) or NG-nitro-L-arginine (L-NNA, 10(-4) M)." | ( Inhibition of NO synthesis or endothelium removal reveals a vasoconstrictor effect of insulin on isolated arterioles. Chen, YL; Messina, EJ; Schroeder, CA, 1999) | 0.49 |
" In the dental pain study, total pain relief (TOTPAR) over the 6 hours after dosing was similar between 50 mg and 500 mg rofecoxib and 400 mg ibuprofen (P > ." | ( Characterization of rofecoxib as a cyclooxygenase-2 isoform inhibitor and demonstration of analgesia in the dental pain model. Dallob, A; De Lepeleire, I; De Schepper, P; Ehrich, EW; Gertz, BJ; Mehlisch, DR; Porras, A; Riendeau, D; Seibold, JR; Van Hecken, A; Wittreich, J; Yuan, W, 1999) | 0.3 |
"To evaluate whether a prolonged low-dose course of indomethacin would produce an improved closure rate and have fewer side effects compared with a short standard dosage schedule in the management of patent ductus arteriosus (PDA) in preterm infants." | ( Short versus prolonged indomethacin therapy for patent ductus arteriosus in preterm infants. Iivainen, T; Ikonen, S; Janas, M; Koivisto, M; Lautamatti, V; Ojala, R; Pokela, ML; Tammela, O, 1999) | 0.87 |
" To obtain dose-response curves, single doses (as boluses) of different concentrations of adenosine were infused and the maximal increase in A-V delay induced by each dose was determined." | ( Intravascular adenosine: the endothelial mediators of its negative dromotropic effects. Balcells, E; Ceballos, G; Rubio, R, 1999) | 0.3 |
" Dose-response curves were obtained with acetylcholine, sodium nitroprusside, and calcium ionophore A23187 following contraction with phenylephrine (10(-6) M) in the presence of indomethacin (10(-5) M)." | ( A model of xenograft hyperacute rejection attenuates endothelial nitric oxide production: a mechanism for graft vasospasm? Cable, DG; Hisamochi, K; Schaff, HV, 1999) | 0.5 |
" For some of these agents, the models also predict that toxicities seen at higher doses for prolonged periods would preclude dosing in humans at levels that might provide disease-modifying effects." | ( Animal models of arthritis: relevance to human disease. Bendele, A; Chlipala, E; Gould, T; Guy, M; McAbee, T; McComb, J; Sennello, G, ) | 0.13 |
"Nitroglycerin infusion caused a significant increase in maternal and fetal heart rate and a significant decrease in maternal and fetal mean arterial pressure at a dosage of 10 microram/kg per minute, without a change in blood gas values." | ( Effects of nitroglycerin and indomethacin on fetal-maternal circulation and on fetal cerebral blood flow and metabolism in sheep. Harrison, MR; Heymann, MA; Morris, JA; Roman, C; Skarsgard, ED; VanderWall, KJ, 1999) | 0.59 |
" Indomethacin did not alter the dose-response curves to KCl or Phe in either swimming or control groups." | ( Effects of exercise training on responsiveness of the mesenteric arterial bed to phenylephrine and KCl in male rats. Hirunpan, P; Jansakul, C, 1999) | 1.21 |
" CT-3 was devoid of GI ulceration when administered with DMSO either acutely at doses below 100 mg/kg or chronically at a dosage of 30 mg/kg/day for 5 days." | ( 1',1'-Dimethylheptyl-delta-8-tetrahydrocannabinol-11-oic acid: a novel, orally effective cannabinoid with analgesic and anti-inflammatory properties. Dajani, EZ; Dajani, NE; Dayton, MT; Larsen, KR; Mir, GN; Neeleman, SD; Shahwan, TG; Taylor, J; Taylor, MS, 1999) | 0.3 |
" The antisecretory action of YJA20379-1 was short lasting (less than 7 h at an oral dosing of 30 mg/kg)." | ( Biochemical and pharmacological characteristics of a newly synthesized H+-K+ ATPase inhibitor, YJA20379-1, 2-amino-4,5-dihydro-8-phenylimidazole[2,1-b]thiazolo[5,4-g]benzothiazol e. Chang, MS; Choi, WS; Chung, YK; Kim, KB; Lee, SB; Sohn, SK; Woo, TW, 1999) | 0.3 |
"To study the influence of meloxicam, a cyclooxygenase-2 (COX-2) preferential nonsteroidal anti-inflammatory drug, on serum thromboxane and platelet function in healthy volunteers with use of the maximum recommended daily dosage of 15 mg/day." | ( Meloxicam, 15 mg/day, spares platelet function in healthy volunteers. de Meijer, A; de Metz, M; Novakova, I; Thomas, C; Verbruggen, B; Vollaard, H, 1999) | 0.3 |
" Antenatal indomethacin treatment for longer than 2 days with a daily or cumulative dosage >/=150 mg correlated with a significantly higher incidence of grade I-II intraventricular haemorrhage." | ( Perinatal indomethacin treatment and neonatal complications in preterm infants. Ikonen, S; Ojala, R; Tammela, O, 2000) | 1.1 |
" In other experiments carried out on endothelium-removed preparations and in medium containing the calcium antagonist, diltiazem (10(-5) and 10(-6) M), the contraction dose-response curves were significantly reduced and the same happened in the presence of the inhibitor of sarcoplasmic reticulum Ca-2+-ATPase, cyclopiazonic acid (CPA) (3 x 10(-6) M)." | ( Endothelium modulates contractile response to simvastatin in rat aorta. Alvarez de Sotomayor, M; Herrera, MD; Marhuenda, E; Pérez-Guerrero, C, ) | 0.13 |
" Efficacy was evaluated on the basis of clinical and laboratory variables, radiographic signs of disease progression and daily dosage of indomethacin." | ( Efficacy of methotrexate in the treatment of ankylosing spondylitis: a three-year open study. Bambara, LM; Biasi, D; Caramaschi, P; Carletto, A; Maleknia, T; Pacor, ML, 2000) | 0.51 |
" Direct PGE(2) stimulation of cultures resulted in the bell shaped dose-response curve with concentrations of 1-100 nmol/l (which are within the range secreted in culture in response to FBS), stimulating significant latent MMP-9 secretion." | ( Prostaglandin E(2)-dependent production of latent matrix metalloproteinase-9 in cultures of human fetal membranes. Bell, SC; McLaren, J; Taylor, DJ, 2000) | 0.31 |
"5 g resting tensions, NOS inhibitors shifted the ACh dose-response curve to the right." | ( Mechanical stretch reveals different components of endothelial-mediated vascular tone in rat aortic strips. Bani, D; Ciuffi, M; Failli, P; Franchi-Micheli, S; Mazzetti, L; Zilletti, L, 2000) | 0.31 |
" However, they shifted the morphine antinociceptive dose-response curve to the left when coadministered with morphine during tolerance induction, and reduced the increase in the ED50 of morphine (dose producing 50% of the maximum response) three- to four-fold." | ( Intrathecal cyclooxygenase inhibitor administration attenuates morphine antinociceptive tolerance in rats. Chou, R; Chou, YY; Hsu, MM; Tung, CS; Wong, CS, 2000) | 0.31 |
" Both shifted the dose-response curve of morphine to the right and these actions were eliminated by intrathecal PGD(2." | ( Antianalgesic action of nociceptin originating in the brain is mediated by spinal prostaglandin E(2) in mice. Campbell, WB; Fujimoto, JM; Rady, JJ, 2001) | 0.31 |
" The effects of cyclooxygenase activity were evaluated by a dose-response curve to intrabrachial coinfusion of ACh and indomethacin (500 microg/min)." | ( Obesity and body fat distribution induce endothelial dysfunction by oxidative stress: protective effect of vitamin C. Candigliota, M; Ceravolo, R; Iacopino, S; Mattioli, PL; Perticone, F; Sinopoli, F; Ventura, G, 2001) | 0.52 |
" In dose-response studies, SLIGRL-NH(2) induced concentration-dependent increases in PGE(2) release (EC(50)=20." | ( Role of PGE(2) in protease-activated receptor-1, -2 and -4 mediated relaxation in the mouse isolated trachea. Henry, PJ; Knight, DA; Lan, RS; Stewart, GA, 2001) | 0.31 |
" To address this hypothesis, we used dosing with nimesulide, which inhibited COX-2 ex vivo, depressed urinary 2,3 dinor 6-keto PGF(1alpha) by approximately 60% but had no effect on thromboxane formation by platelets, which only express COX-1." | ( Acceleration of atherogenesis by COX-1-dependent prostanoid formation in low density lipoprotein receptor knockout mice. FitzGerald, GA; Li, H; Praticò, D; Tillmann, C; Zhang, ZB, 2001) | 0.31 |
" Bronchial rings were incubated with normal or immune serum (100 microl ml(-1) for 2 h) and dose-response curves to TDI (0." | ( Serum-mediated relaxant response to toluene diisocyanate (TDI) in isolated guinea-pig bronchi. Boschetto, P; Chitano, P; De Marzo, N; Fabbri, LM; Faggian, D; Jovine, L; Mapp, CE; Plebani, M, 2001) | 0.31 |
"5 x 10(-6)) to generate two cumulative dose-response curves (CDRC I and II)." | ( Endothelium-dependent desensitization to angiotensin II in rabbit aorta: the mechanisms involved. Coviello, A; de Bruno, MP; Jerez, S, 2001) | 0.31 |
"In vitro experiments followed the effect of the two substances at concentrations between 10(-8)-10(-4) M on purified human red cell CA I and II as well as on human gastric mucosa CA IV using dose-response relationships." | ( Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action. Baican, M; Coltau, M; Domuta, G; Hecht, A; Ifrim, M; Maghiar, T; Puscas, I, 2001) | 1.75 |
" Dose-response curves to acetylcholine (ACh) and sodium nitroprusside (SNP; an NO donor) were obtained with or without ET-1 receptor blockade." | ( Endothelium-derived endothelin-1 reduces cerebral artery sensitivity to nitric oxide by a protein kinase C-independent pathway. Gilbert, P; Thorin, E; Tremblay, J, 2001) | 0.31 |
" In HLPs perfused with homologous blood, dose-response curves for the haemodynamic and bronchial effects of PAF (1 - 32 ng) were carried out in the absence or presence of L-NNA (200 microM)." | ( Nitric oxide (NO) modulation of PAF-induced cardiopulmonary action: interaction between NO synthase and cyclo-oxygenase-2 pathways. Calabrese, R; del Basso, P; Fabi, F; Stati, T, 2001) | 0.31 |
"This study shows that indomethacin increased the cytotoxicity of both CDDP and 5FUra by increasing the intracellular incorporation of free-CDDP and 5FUra, and suggests the effectiveness of indomethacin in reducing the dosage of CDDP and 5FUra or increasing CDDP and 5FUra cytotoxicity when these agents are given without reducing the dose." | ( Indomethacin increases the cytotoxicity of cis-platinum and 5-fluorouracil in the human uterine cervical cancer cell lines SKG-2 and HKUS by increasing the intracellular uptake of the agents. Minoura, S; Ogino, M, 2001) | 2.07 |
"To determine patent ductus arteriosus (PDA) closure rates, and indomethacin (INDO) toxicity rates in neonates dosed with INDO using an individualized pharmacokinetic/pharmacodynamic (PK/PD) dosing approach." | ( Effect of age and birth weight on indomethacin pharmacodynamics in neonates treated for patent ductus arteriosus. Brown, YL; Carlos, RQ; Davey, AM; Dimaguila, MA; Gal, P; Ransom, JL; Schall, SA; Shaffer, CL; Smith, MS, 2002) | 0.83 |
" Individualized pharmacokinetic/pharmacodynamic dosing of INDO continues to achieve higher closure rate than current dosing standards." | ( Effect of age and birth weight on indomethacin pharmacodynamics in neonates treated for patent ductus arteriosus. Brown, YL; Carlos, RQ; Davey, AM; Dimaguila, MA; Gal, P; Ransom, JL; Schall, SA; Shaffer, CL; Smith, MS, 2002) | 0.59 |
" The dose-response curve for the acetylcholine-induced relaxation was slightly, but significantly attenuated in diabetic mice." | ( Contractile responses in spontaneously diabetic mice. I. Involvement of superoxide anion in enhanced contractile response of aorta to norepinephrine in C57BL/KsJ(db/db) mice. Kamata, K; Kanie, N, 2000) | 0.31 |
" Oxygen uptake by and energy charge in jejunal tissue were unaffected at 1 and 3 h after dosing by gavage with indomethacin." | ( Effects of indomethacin on energy metabolism in rat jejunal tissue in vivo. Bjarnason, I; Jacob, M; Simpson, RJ, 2002) | 0.92 |
" Despite having a molecular level structure akin to that of liquids, amorphous materials have macroscopic properties that are typical of solids and thus they may be presented to the patient in the form of a convenient solid dosage form." | ( Disordered drug delivery: destiny, dynamics and the Deborah number. Hancock, BC, 2002) | 0.31 |
" Cell viability, tetrazolium dye (MTT) reduction and oxygen uptake were significantly reduced in villus tip cells from rats dosed with the drug." | ( Indomethacin-induced mitochondrial dysfunction and oxidative stress in villus enterocytes. Balasubramanian, KA; Basivireddy, J; Jacob, M; Vasudevan, A, 2002) | 1.76 |
") administration of TGFalpha and UG had no effect, while EGF potentiated, both secretagogue-induced acid secretion in the same dosage schedule." | ( Comparison of the antisecretory and antiulcer activity of epidermal growth factor, urogastrone and transforming growth factor alpha and its derivative in rodents in vivo. Bastaki, SM; Chandranath, SI; Singh, J, 2002) | 0.31 |
"Contractile activity was assessed by calculating the area under the curve, to obtain a dose-response curve of each drug." | ( In vitro study of tocolytic effect of rofecoxib, a specific cyclo-oxygenase 2 inhibitor. Comparison and combination with other tocolytic agents. Benchaib, M; Doret, M; Gharib, C; Mellier, G; Pasquier, JC; Piacenza, JM, 2002) | 0.31 |
" AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6." | ( Presynaptic effects of moxonidine in isolated buffer perfused rat hearts: role of imidazoline-1 receptors and alpha2-adrenoceptors. Burgdorf, C; Engelhardt, A; Kurz, T; Richardt, G; Schäfer, U, 2002) | 0.31 |
" In this study, NS-398, a specific COX-2 inhibitor, and indomethacin, a COX-1 and COX-2 inhibitor, were administered 24 h after chloroform dosing to determine their effect on liver injury in Sprague-Dawley rats." | ( Late administration of COX-2 inhibitors minimize hepatic necrosis in chloroform induced liver injury. Begay, CK; Gandolfi, AJ, 2003) | 0.57 |
" Evidence of oxidative stress was found in the mucosa of the small intestine of rats dosed with indomethacin, as indicated by increased activity of xanthine oxidase with corresponding decrease in the levels of several free radical scavenging enzymes." | ( Indomethacin-induced free radical-mediated changes in the intestinal brush border membranes. Balasubramanian, KA; Basivireddy, J; Jacob, M; Pulimood, AB; Ramamoorthy, P, 2003) | 1.98 |
" Our goal was to develop a simplified dosage regimen for preterm infants which would result in therapeutic maximum serum concentrations early in the course of therapy." | ( Evaluation of a netilmicin-loading dose in very low birthweight infants. Berger, A; Gludovatz, P; Kohlhauser, C; Kretzer, V; Prusa, AR; Rohrmeister, K, 2003) | 0.32 |
" twice, 30 min before each dosing of dopamine." | ( Dopamine-induced protection against indomethacin-evoked intestinal lesions in rats--role of anti-intestinal motility mediated by D2 receptors. Kato, S; Matsumoto, M; Miyazawa, T; Takeuchi, K, 2003) | 0.59 |
"All 5 cell lines constantly showed growth suppression with positive dosage effect of indomethacin." | ( In vitro growth inhibition by indomethacin on human oral squamous cell carcinoma lines synergistically suppressed by all-trans retinoic acid correlating to apoptosis. Chang, RC; Kao, SY; Tu, SF; Wu, CH; Yang, CC, 2002) | 0.83 |
"2% at 1 and 2h after dosing (P<0." | ( The anti-inflammatory effects of the phosphodiesterase inhibitor pentoxifylline in the rat. Abdel-Salam, OM; Arbid, MS; Baiuomy, AR; El-Shenawy, SM, 2003) | 0.32 |
" Dose-response curves were made with gradually increasing doses of Phe using an isolated kidney preparation in the presence of a NO synthase (NOS) inhibitor (L-NAME, 1 microM), a PG-synthesis inhibitor (indomethacin, 1 microM), both, or neither." | ( Pregnancy influence on the vascular interactions between nitric oxide and other endothelium-derived mediators in rat kidney. Anguiano, L; Bobadilla, RA; López Sanchez, P; Pérez-Alvarez, V, 2003) | 0.51 |
"For biotherapeutic agents, there is a lack of information on dose-response relationships and mechanism of action." | ( Dose-response relationship and mechanism of action of Saccharomyces boulardii in castor oil-induced diarrhea in rats. Gillardin, JM; Girard, P; Lorette, I; Pansart, Y, 2003) | 0.32 |
" However, the margin between closure of the ductus arteriosus and the deterioration of kidney function in preterm infants treated with a presently recommended indomethacin dosage was narrow." | ( Recovery of prostaglandin production associated with reopening of the ductus arteriosus after indomethacin treatment in preterm infants with respiratory distress syndrome. Müller, H; Plückthun, H; Seyberth, HW; Ulmer, HE; Wille, L; Wolf, D, 1982) | 0.68 |
"Enalaprilat shifted the norepinephrine dose-response curve to the right (P=0." | ( Effects of enalaprilat on venoconstriction to norepinephrine: role of prostaglandins. Arnold, JM; Dzeka, TN; Townley, R, 2003) | 0.32 |
" After dosing at 08:00 h, indomethacin remarkably reduced the number of writhes during the critical span of 14:00-18:00 h--the time when writhing reaction was greatest during the 24 h, while the suppressive effect of the medicine after dosing at the other clock times was relatively small." | ( Evaluation of chronopharmacodynamics of indomethacin by the kaolin-induced pain model in mice. Araki, N; Cui, Y; Fujimura, A; Sugimoto, K, 2003) | 0.89 |
" We compared the efficacy of this regimen to conventional dosing in a cohort of very low birth weight infants." | ( Randomized trial of prolonged low-dose versus conventional-dose indomethacin for treating patent ductus arteriosus in very low birth weight infants. Lee, J; Leong, JY; Rajadurai, VS; Tan, KW; Wong, EH; Wong, KY, 2003) | 0.56 |
"There was no difference in efficacy between the 2 dosing regimens." | ( Randomized trial of prolonged low-dose versus conventional-dose indomethacin for treating patent ductus arteriosus in very low birth weight infants. Lee, J; Leong, JY; Rajadurai, VS; Tan, KW; Wong, EH; Wong, KY, 2003) | 0.56 |
" Pinane thromboxane, a selective thromboxane synthase inhibitor and receptor blocker, inhibited OxAA stimulation of TXB(2) and IL-8 in a dose-response manner." | ( Linoleic acid induces interleukin-8 production by Crohn's human intestinal smooth muscle cells via arachidonic acid metabolites. Alzoghaibi, MA; Fowler, AA; Graham, MF; Walsh, SW; Willey, A; Yager, DR, 2004) | 0.32 |
" Dosage forms were prepared by encapsulating the complexes without the addition of excipients." | ( The physicochemical characteristics and bioavailability of indomethacin from beta-cyclodextrin, hydroxyethyl-beta-cyclodextrin, and hydroxypropyl-beta-cyclodextrin complexes. Casella, R; Jambhekar, S; Maher, T, 2004) | 0.57 |
"Etoricoxib at a dosage of 120 mg once daily was confirmed to be an effective treatment for acute gout." | ( Efficacy and safety profile of treatment with etoricoxib 120 mg once daily compared with indomethacin 50 mg three times daily in acute gout: a randomized controlled trial. Antigua, J; Burton, R; Chen, E; Geba, GP; Londoño, J; Lund, M; Najarian, DK; Navarra, S; Ozturk, ZE; Petruschke, RA; Pryhuber, KG; Rubin, BR, 2004) | 0.55 |
" Rats fasted overnight were dosed with indomethacin (20 mg/kg) by gavage and sacrificed 24 hr later." | ( Indomethacin-induced renal damage: role of oxygen free radicals. Balasubramanian, KA; Basivireddy, J; Jacob, M; Pulimood, AB, 2004) | 2.04 |
" Accordingly, coating of the crystals can be performed in order to protect the mucosa of the gastrointestinal tract or to promote the preparation of solid dosage form." | ( Surface treatment of indomethacin agglomerates with eudragit. Bajdik, J; Eros, I; Pintye-Hódi, K; Planinsek, O; Regdon, G; Srcic, S; Tasic, L; Tüske, Z, 2004) | 0.64 |
"The objective of this study was to determine the rate of patent ductus arteriosus (PDA) closure in premature infants using an adjustable indomethacin (INDO) dosing strategy, based on a second-dose peak plasma INDO level." | ( Indomethacin therapy for patent ductus arteriosus in premature infants: efficacy of a dosing strategy based on a second-dose peak plasma indomethacin level and estimated plasma indomethacin levels. Adams, JM; Adams, K; Fernandes, CJ; Nguyen, NY; O'Donovan, DJ, 2004) | 1.97 |
" BQ123 (1 microm) caused a rightward shift in the ET-1 dose-response curve, while indomethacin at a threshold concentration (28 nm) tended to have an opposite effect." | ( Endothelin-induced constriction of the ductus venosus in fetal sheep: developmental aspects and possible interaction with vasodilatory prostaglandin. Adeagbo, AS; Coceani, F; Kelsey, L, 2004) | 0.55 |
" In the present report, we have analyzed the effect of the central nervous system (CNS) permissive, putatively neuroprotective, anti-inflammatory cyclooxygenase-1/-2 (COX-1/-2) inhibitor indomethacin in CNS effective dosage (2 mg/kg/day) on lesional RhoA expression following subacute spinal cord injury." | ( Lesional RhoA+ cell numbers are suppressed by anti-inflammatory, cyclooxygenase-inhibiting treatment following subacute spinal cord injury. Conrad, S; Elbert, T; Meyermann, R; Schluesener, HJ; Schwab, JM; Trautmann, K, 2004) | 0.51 |
" The present study is an evaluation of the potential synergism of EA and a subeffective dosage of indomethacin (INDO) in a rat model." | ( Electroacupuncture combined with indomethacin enhances antihyperalgesia in inflammatory rats. Berman, BB; Lao, L; Ren, K; Wang, X; Zhang, RX, 2004) | 0.82 |
" The use of key parameters estimated from the modeling of dissolution and de-agglomeration profiles provides a useful tool in dosage form development of formulations of poorly water soluble drugs." | ( Understanding agglomeration of indomethacin during the dissolution of micronised indomethacin mixtures through dissolution and de-agglomeration modeling approaches. Stewart, PJ; Zhao, FY, 2005) | 0.61 |
" 0 approximately 400 micromol/L of IN could down-regulate the expression of p-STAT1 or p-STAT5 in a dose-response manner, p-STATs were distributed mainly in the nucleus as scattering spots." | ( [Proliferation inhibition effect of indomethacin on CML cells associated with down-regulation of phosphorylated STAT1/STAT5 and inhibition of COX-2 expression]. Fu, YB; Xia, M; Zhang, GS, 2004) | 0.6 |
" The total dosage was the same for both groups." | ( Continuous indomethacin infusion may be less effective than bolus infusions for ductal closure in very low birth weight infants. Bos, AF; de Vries, NK; Elzenga, NJ; Jaarsma, AS; Jagroep, FK, 2005) | 0.72 |
" It is concluded that when amorphous forms of salts occur in solid dosage forms, the simultaneous effects of enhanced water vapor sorption on crystallization and chemical degradation must be considered, particularly when assessing solid-state chemical degradation at higher temperatures and RH (eg, 40 degrees C 75% RH)." | ( Effects of water vapor absorption on the physical and chemical stability of amorphous sodium indomethacin. Tong, P; Zografi, G, 2004) | 0.54 |
" Thoracic aorta was isolated and the dose-response curve of phenylephrine (PE) in the presence or absence of Nomega-nitro-L-arginine-methyl ester (L-NAME) was recorded." | ( Pioglitazone, a PPARgamma agonist, restores endothelial function in aorta of streptozotocin-induced diabetic rats. Balaraman, R; Majithiya, JB; Paramar, AN, 2005) | 0.33 |
" The presence of pioglitazone at higher concentrations (>10 muM), but not at lower concentrations, significantly changed the dose-response curve of PE or Ach." | ( Pioglitazone, a PPARgamma agonist, restores endothelial function in aorta of streptozotocin-induced diabetic rats. Balaraman, R; Majithiya, JB; Paramar, AN, 2005) | 0.33 |
"A significant problem with solid dispersion (SD) systems is the difficulty in preparing dosage forms." | ( Preparation, characterization, and tableting of a solid dispersion of indomethacin with crospovidone. Fujii, M; Kondoh, M; Okada, H; Shibata, Y; Teramachi, H; Watanabe, Y, 2005) | 0.56 |
" Rats, fasted overnight, were dosed with indomethacin (20 mg/kg) by gavage and sacrificed 24 h later." | ( Indomethacin induces free radical-mediated changes in renal brush border membranes. Balasubramanian, KA; Basivireddy, J; Jacob, M, 2005) | 2.04 |
" Dose-response curves were produced with the thromboxane-mimetics U46619 and U44069 (10(-10)-2 x 10(-6)M), arginine vasopressin (10(-10)-5 x 10(-8)M) and endothelin-1 (10(-11)-3 x 10(-7)M) in the presence or absence of 50 micromol l(-1) glibenclamide." | ( Glibenclamide inhibits agonist-induced vasoconstriction of placental chorionic plate arteries. Baker, PN; Fyfe, GK; Greenwood, SL; Taggart, MJ; Wareing, M, ) | 0.13 |
"Pre-incubation with 50 micromol l(-1) glibenclamide significantly right-shifted dose-response curves to all vasoconstrictive agonists tested (repeated measures ANOVA)." | ( Glibenclamide inhibits agonist-induced vasoconstriction of placental chorionic plate arteries. Baker, PN; Fyfe, GK; Greenwood, SL; Taggart, MJ; Wareing, M, ) | 0.13 |
" The dose-response study of AA and IDM demonstrated that the concentration of intracellular AA accumulated by IDM is less than 100 nm." | ( Enhancement of Ca2+-regulated exocytosis by indomethacin in guinea-pig antral mucous cells: arachidonic acid accumulation. Fujiwara, S; Kato, M; Katsu, K; Nakahari, T; Nakanishi, Y; Shimamoto, C, 2006) | 0.59 |
" To test this hypothesis, dose-response relations for endothelium-dependent (2-methylthioadenosine triphosphate and bradykinin) and endothelium-independent (nitroprusside) vasodilation were determined in vitro in middle cerebral arteries (MCAs) from HDT and control rats." | ( Endothelium-dependent vasodilation of cerebral arteries is altered with simulated microgravity through nitric oxide synthase and EDHF mechanisms. Bryan, RM; Delp, MD; Prisby, RD; Sokoya, EM; Wilkerson, MK; Wilson, E, 2006) | 0.33 |
" The drug has prolonged elimination (plasma half-life = ca 23 hours), suggesting that once daily dosing is appropriate." | ( Systematic review: intravenous Ibuprofen in preterm newborns. Aranda, JV; Thomas, R, 2006) | 0.33 |
" Our results suggest that the association between an antimuscarinic drug and an antagonist of P2X purinoceptors such as suramin might be helpful to reduce the therapeutic dosage of the antimuscarinic drug, along with its side effects." | ( Altered neurogenic and mechanical responses to acetylcholine, ATP and substance P in detrusor from rat with outlet obstruction. Pinna, C; Puglisi, L; Sanvito, P, 2006) | 0.33 |
"In the current study, the influence of plasticizer level on drug release was investigated for solid dosage forms prepared by hot-melt extrusion and film coating." | ( Influence of plasticizer level on the drug release from sustained release film coated and hot-melt extruded dosage forms. McGinity, JW; Mehta, KA; Zhu, Y, 2006) | 0.33 |
" Twenty-four hours later, they were dosed with indomethacin." | ( Role of bile in pathogenesis of indomethacin-induced enteropathy. Bjarnason, I; Foster, R; Jacob, M; Sigthorsson, G; Simpson, R, 2007) | 0.88 |
" After 4 hours of incubation, RBL-2H3 cells cultured with RANTES at 20 ng/mL released large amounts of PGD2 in a dose-response manner compared to control." | ( Rat basophilic leukemia cells (RBL-2H3) generate prostaglandin D2 (PGD2) after regulated upon activation, normal T-cell expressed and secreted (RANTES) activation. Castellani, ML; Conti, CM; Conti, P; Frydas, S; Petrarca, C; Salini, V; Shanmugham, LN, ) | 0.13 |
" Since the rate of drug release is not formulation dependent, the prodrug can be compounded even in a liquid dosage form." | ( A novel mechanism for oral controlled release of drugs by continuous degradation of a phospholipid prodrug along the intestine: in-vivo and in-vitro evaluation of an indomethacin-lecithin conjugate. Dahan, A; Duvdevani, R; Dvir, E; Elmann, A; Hoffman, A, 2007) | 0.53 |
" We demonstrate that a reduction of cyclooxygenase 2 gene dosage rescued the ovarian aging phenotype of the Wv mice, whereas homozygous deletion was accompanied by a compensatory increase in ovarian cyclooxygenase 1 expression and prostaglandin E(2) synthesis." | ( A reduction of cyclooxygenase 2 gene dosage counters the ovarian morphological aging and tumor phenotype in Wv mice. Cai, KQ; Hamilton, TC; Klein-Szanto, A; Smedberg, JL; Smith, ER; Xu, XX; Yang, WL, 2007) | 0.34 |
" Implications for researchThere is a paucity of data on optimal dosing and duration of indomethacin therapy for the treatment of PDA, in particular for extremely low birth weight infants (ELBW) premature infants." | ( Prolonged versus short course of indomethacin for the treatment of patent ductus arteriosus in preterm infants. Davis, P; Herrera, C; Holberton, J, 2007) | 0.84 |
" Ductal constriction, oligohydramnios, and composite morbidity were not associated with duration of therapy, gestational age at start or stop of therapy, time between dosing and delivery, or dose regimen." | ( The safety of prolonged indomethacin therapy. Anderson, BL; Savage, AH; Simhan, HN, 2007) | 0.65 |
"In this double-blind, double-dummy, randomised, parallel group, multicentre study, the efficacy of dosing and re-dosing of a fixed combination of indomethacin, prochlorperazine and caffeine (Indoprocaf) was compared with encapsulated sumatriptan in the acute treatment of two migraine attacks." | ( Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, double-dummy, randomised, parallel group, mu Cerbo, R; Del Bene, E; Ferrari, A; Genco, S; Grazioli, I; Martelletti, P; Nappi, G; Pinessi, L; Sandrini, G; Sarchielli, P; Tamburro, P; Uslenghi, C; Zanchin, G, 2007) | 0.78 |
"The study demonstrated that the efficacy of the initial dosing of Indoprocaf was not higher than that of sumatriptan, but that the strategy to use the lowest effective dose as soon as the headache occurred, followed by a second dose if the headache has not relieved or to treat a relapse, was very effective, especially with Indoprocaf." | ( Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, double-dummy, randomised, parallel group, mu Cerbo, R; Del Bene, E; Ferrari, A; Genco, S; Grazioli, I; Martelletti, P; Nappi, G; Pinessi, L; Sandrini, G; Sarchielli, P; Tamburro, P; Uslenghi, C; Zanchin, G, 2007) | 0.58 |
" Effects of GPR109A agonists on lipolysis were measured in both species after oral dosing of compounds, and measuring plasma levels of free fatty acids." | ( Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonists. Carballo-Jane, E; Colletti, SL; Forrest, MJ; Gerckens, LS; Luell, S; McCann, ME; Parlapiano, AS; Richman, JG; Taggart, AK; Tata, JR; Waters, MG; Wolff, M, ) | 0.13 |
" Acetylcholine dose-response relaxation curves revealed that SAM-R1 vessels were slightly more sensitive than those of SAM-P8." | ( The senescence-accelerated mouse (SAM-P8) as a model for the study of vascular functional alterations during aging. de Cabo, C; de Mera, RM; Jordán, J; Lloréns, S; Mendizábal, Y; Nava, E; Pascual, A; Prieto-Martín, A, 2007) | 0.34 |
" The method was applied to determination of 1 to 5% of I in semisolid dosage forms (gels and ointments)." | ( Sequential injection analysis (SIA)-chemiluminescence determination of indomethacin using tris[(2,2'-bipyridyl)]ruthenium(III) as reagent and its application to semisolid pharmaceutical dosage forms. Calatayud, JM; Mervartová, K; Polásek, M, 2007) | 0.57 |
" Administration of RBuOH at the same dosage (50, 100 and 200 mg/kg) reduced significantly (P<0." | ( Anti-ulcer, anti-inflammatory and antioxidant activities of the n-butanol fraction from Pteleopsis suberosa stem bark. Biasini, T; Braca, A; D'Angelo, V; De Leo, M; De Pasquale, R; Germanò, MP; Miano, TC; Sanogo, R, 2008) | 0.35 |
" There was no obvious dose-response relationship between systemic exposure to varying plasma indomethacin concentrations and ductus closure, which does not support individualized indomethacin dosing based on monitoring to a target plasma concentration." | ( Orogastric and intravenous indomethacin administration to very premature neonates with patent ductus arteriosus: population pharmacokinetics, absolute bioavailability, and treatment outcome. Al Za'abi, M; Charles, B; Collie, LA; Donovan, T; Tudehope, D; Woodgate, P, 2007) | 0.86 |
" Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg." | ( Imidazopyridines: a novel class of hNav1.7 channel blockers. Abbadie, C; Dean, B; Duffy, JL; Felix, JP; Garcia, ML; Hoyt, SB; Jochnowitz, N; Kaczorowski, GJ; Karanam, BV; Li, X; London, C; Lyons, KA; Martin, WJ; McGowan, E; Parsons, WH; Priest, BT; Smith, MM; Tschirret-Guth, R; Warren, VA; Williams, BS, 2008) | 0.35 |
" Although a 3-dose schedule has been commonly used, there is no consensus on optimal dosage and duration of indomethacin therapy for PDA closure." | ( Continuous infusion versus intermittent bolus doses of indomethacin for patent ductus arteriosus closure in symptomatic preterm infants. Bracken, MB; Ehrenkranz, RA; Görk, AS, 2008) | 0.81 |
" The BK dose-response curve was shifted to the right by topical indomethacin." | ( A novel model of pain sensation using superfused gastrosplenic omentum preparation of anesthetized rats. Katori, M; Majima, M; Yang, SJ, 2008) | 0.58 |
" These results collectively suggested that IDMC-PLLA/PLGA microparticles prepared using SEDS would have potentials in anti-tumor applications as a controlled drug release dosage form without harmful organic solvent residue." | ( Preparation, characterization and in vitro cytotoxicity of indomethacin-loaded PLLA/PLGA microparticles using supercritical CO2 technique. Chen, A; Huang, Z; Kang, Y; Liao, L; Liao, X; Pu, X; Wu, J; Yao, Y; Yin, G, 2008) | 0.59 |
"Increasing indomethacin concentrations above the levels achieved with a conventional dosing regimen had little effect on the rate of PDA closure but was associated with higher rates of moderate/severe ROP and renal compromise." | ( Increased indomethacin dosing for persistent patent ductus arteriosus in preterm infants: a multicenter, randomized, controlled trial. Buchh, B; Chorne, N; Clyman, R; Ewig, A; Fields, S; Ianus, V; Jegatheesan, P; Lin, E; Milstein, J; Moon-Grady, A; Padbury, J; Schreiber, M; Tacy, T; Yoon, G, 2008) | 1.14 |
" The interaction between these two agents was characterized by isobolographic analysis using a fixed-ratio dosing strategy." | ( Additive, but not synergistic antinociceptive effect of codeine and indomethacin combinations in the formalin test in the rat. Arredondo-Garza, T; Castañeda-Hernández, G; Jiménez-Andrade, M; Lozano-Cuenca, J, 2007) | 0.58 |
" The dose-response to vasoconstrictors and vasodilators was assessed in small resistance coronary arteries." | ( Effect of fetal anaemia on myocardial ischaemia-reperfusion injury and coronary vasoreactivity in adult sheep. Davis, LE; Giraud, GD; He, GW; Hohimer, AR; Underwood, MJ; Van Winkle, DM; Yang, Q, 2008) | 0.35 |
" Indomethacin dosing was withheld in the BNP-guided group if the 12 or 24 h BNP concentrations were found to be <100 pg/ml." | ( B-type natriuretic peptide concentrations to guide treatment of patent ductus arteriosus. Attridge, JT; Kaufman, DA; Lim, DS, 2009) | 1.26 |
"Methods used included the in-vitro inhibition of cyclooxygenase-1 and -2, in-vivo evaluation of anti-inflammatory activity by air pouch and peritonitis models and the pharmacokinetic profile after intravenous (3 mg/kg) and oral (3 and 6 mg/kg) dosing to rats." | ( Preclinical pharmacokinetic and pharmacodynamic evaluation of thiazolidinone PG15: an anti-inflammatory candidate. da Silva, TG; Dalla Costa, T; de Lima, Mdo C; Galdino, SL; Pitta, Ida R; Uchôa, Fde T, 2009) | 0.35 |
"The erratic absorption of PG15 observed after oral dosing could explain the lack of anti-inflammatory dose dependency." | ( Preclinical pharmacokinetic and pharmacodynamic evaluation of thiazolidinone PG15: an anti-inflammatory candidate. da Silva, TG; Dalla Costa, T; de Lima, Mdo C; Galdino, SL; Pitta, Ida R; Uchôa, Fde T, 2009) | 0.35 |
"The purpose of this study was to prepare modified-release dosage of indomethacin (IND) in the form of micromatrices based on a superabsorbent hydrogel (SAH), poly(acrylic acid), partly sodium salt-g-poly(ethylene oxide) (PAAc-Na-g-PEO)." | ( Preparation and optimization of superabsorbent hydrogel micromatrices based on poly(acrylic acid), partly sodium salt-g-poly(ethylene oxide) for modified release of indomethacin. Beba, L; Yuksel, N, 2009) | 0.78 |
"3 mg/kg group treated with indomethacin, but 8 of 10 rats in the 4 mg/kg group died or were sacrificed before completion of the dosing period." | ( Collaborative work on evaluation of ovarian toxicity. 12) Effects of 2- or 4-week repeated dose studies and fertility study of indomethacin in female rats. Fujiwara, M; Ito, S; Kushima, K; Matsumoto, M; Matsuo, S; Nakatsuji, S; Oishi, Y; Saegusa, T; Seki, J; Tsubota, K; Yamauchi, K, 2009) | 0.86 |
"Acute and chronic dosing with INDO-PC produced less GI bleeding and intestinal injury than indomethacin alone, whereas the bioavailability, analgesic, anti-inflammatory and COX inhibitory activity of INDO-PC were comparable to indomethacin." | ( Gastrointestinal safety and therapeutic efficacy of parenterally administered phosphatidylcholine-associated indomethacin in rodent model systems. Dial, EJ; Lichtenberger, L; Romero, JJ, 2009) | 0.79 |
" Male Wistar rats were pre-treated with zinc sulphate (50 mg/kg) and dosed with indomethacin (20 mg/kg) by oral gavage." | ( Zinc prevents indomethacin-induced renal damage in rats by ameliorating oxidative stress and mitochondrial dysfunction. Faith, M; Jacob, M; Varghese, J, 2009) | 0.94 |
"The different approaches for targeting orally administered drugs to the colon include coating with pH-dependent polymers, design of time-release dosage forms, and the utilization of carriers that are degraded exclusively by colonic bacteria." | ( Chitosan-chondroitin sulfate based matrix tablets for colon specific delivery of indomethacin. Amrutkar, JR; Gattani, SG, 2009) | 0.58 |
" Based on predictions from the developed model, preterm neonates do not reach targeted peak and trough gentamicin concentrations after a standard dosage regimen of 4 mg/kg given once daily, suggesting a need for higher loading doses and prolonged dosing intervals in this patient population." | ( Developmental pharmacokinetics of gentamicin in preterm and term neonates: population modelling of a prospective study. Ewald, U; Friberg, LE; Honoré, PH; Nielsen, EI; Sandström, M, 2009) | 0.35 |
" The effects of P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (MRP2), and breast cancer resistance protein (BCRP) inhibitors on sulfasalazine bidirectional permeability were studied across Caco-2 cell monolayers, including dose-response analysis." | ( Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Amidon, GL; Dahan, A, 2009) | 0.35 |
" Mucosal lesions in the small intestine were examined 24 h after the final dosing of IND." | ( Soluble dietary fiber protects against nonsteroidal anti-inflammatory drug-induced damage to the small intestine in cats. Hara, T; Matsuura, M; Murakawa, D; Satoh, H; Takata, K, 2010) | 0.36 |
" Dosage of gastric reduced glutathione (GSH) levels showed that ethanol and indomethacin reduced the content of non-protein sulfhydryl (NP-SH) groups, while (-)-alpha-bisabolol significantly decreased the reduction of these levels on ulcer-induced mice, but not in mice without ulcer." | ( Gastroprotection of (-)-alpha-bisabolol on acute gastric mucosal lesions in mice: the possible involved pharmacological mechanisms. Aquino Neto, MR; de França Fonteles, MM; de Sousa, DP; de Sousa, FC; Gomes Silva, MI; Mendes Vasconcelos, SM; Moura Rocha, NF; Moura, BA; Vasconcelos Rios, ER; Venâncio, ET, 2010) | 0.59 |
" In conclusion, after oral dosing of NC-IndOEt, IndOEt is converted into IndOH in the intestinal lumen and wall before reaching the blood stream." | ( Lipid-core nanocapsules restrained the indomethacin ethyl ester hydrolysis in the gastrointestinal lumen and wall acting as mucoadhesive reservoirs. Cattani, VB; Colomé, LM; Dalla Costa, T; Fiel, LA; Guterres, SS; Jäger, A; Jäger, E; Pohlmann, AR; Stefani, V; Uchoa, F, 2010) | 0.63 |
"Azoxymethane-induced adenocarcinoma rats were dosed with indomethacin and copper-indomethacin for 28 days and aberrant crypt foci were evaluated." | ( Inhibition of experimental colorectal cancer and reduction in renal and gastrointestinal toxicities by copper-indomethacin in rats. Bonin, AM; Davies, NM; Dillon, CT; Fukuda, C; Hambley, TW; Lay, PA; Teng, XW; Yáñez, JA, 2010) | 0.82 |
"0 mg/kg for 28 days, whereas copper-indomethacin at equimolar doses of indomethacin affected urine electrolytes after acute dosing but not after chronic dosing for 28 days." | ( Inhibition of experimental colorectal cancer and reduction in renal and gastrointestinal toxicities by copper-indomethacin in rats. Bonin, AM; Davies, NM; Dillon, CT; Fukuda, C; Hambley, TW; Lay, PA; Teng, XW; Yáñez, JA, 2010) | 0.85 |
"The effect of surfactant administration for respiratory distress syndrome (RDS) on indomethacin (INDO) pharmacodynamics and dosing requirements for patent ductus arteriosus (PDA) closure and renal toxicity was evaluated." | ( Indomethacin pharmacodynamics are altered by surfactant: a possible challenge to current indomethacin dosing guidelines created before surfactant availability. Carlos, RQ; Davonzo, C; Dimaguila, MA; Gal, P; McPherson, C; Ransom, JL; Smith, M; Wimmer, JE, 2010) | 2.03 |
" Orally dosed in-vivo studies in rats showed complete drug absorption and statistically higher fasted state bioavailability (F) (p<0." | ( An oral delivery system for indomethicin engineered from cationic lipid emulsions and silica nanoparticles. Davey, AK; Hui, H; Prestidge, CA; Rades, T; Simovic, S; Song, Y, 2010) | 0.36 |
" Similarly, total dosage of meperidine analgesic medication and postoperative time to use of rescue analgesia were evaluated." | ( Effect of preoperative rectal indomethacin on postoperative pain reduction after open appendectomy. Bahar, MM; Jangjoo, A; Soltani, E, ) | 0.42 |
"During dosing with probiotic, median FCCs were significantly increased only at day 17 with respect to T0 values, whereas during dosing with placebo, they were significantly increased at every day from day 17 to day 21 with respect to T0 values." | ( Clinical trial: the effects of a probiotic mixture on non-steroidal anti-inflammatory drug enteropathy - a randomized, double-blind, cross-over, placebo-controlled study. Covino, M; Curigliano, V; D'Onofrio, F; Dalvai, S; Gallo, A; Gasbarrini, A; Gasbarrini, G; Montalto, M; Santoro, L, 2010) | 0.36 |
" For these studies, animals were dosed with CP-154,526 (3, 10, 30 mg/kg) and NBI 27914 (1-30 mg/kg) 1 h prior to the assessment of tactile, thermal or mechanical hypersensitivity, respectively." | ( Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors. Cummons, T; Harrison, JE; Hummel, M; Kennedy, JD; Lu, P; Mark, L; Whiteside, GT, 2010) | 0.36 |
" Our previous protocol suggested an initial dose of 0·2 mg/kg followed by two 0·1 mg/kg, with doses infused over 4 h and a 24-h dosing interval." | ( Comparison of two neonatal indomethacin protocols: efficacy and outcome for patent ductus arteriosus closure. Chorne, N; Rosito, G; Sum, K, 2010) | 0.66 |
"In this small population of premature neonates, there was a trend, but no significant difference, towards increasing PDA closure and lower surgical ligation rates in neonates given indomethacin with more frequent dosing and shorter infusion time." | ( Comparison of two neonatal indomethacin protocols: efficacy and outcome for patent ductus arteriosus closure. Chorne, N; Rosito, G; Sum, K, 2010) | 0.85 |
" These parameters can be judiciously used in predicting and modifying drug release from dosage forms." | ( Cross-linked chitosan films: effect of cross-linking density on swelling parameters. Rana, V; Tiwary, AK, 2010) | 0.36 |
" Animals were orally dosed with dexamethasone (0." | ( Contributions of angiogenesis to inflammation, joint damage, and pain in a rat model of osteoarthritis. Ashraf, S; Mapp, PI; Walsh, DA, 2011) | 0.37 |
"A solid dispersion (SD) powder of indomethacin (IM) with crospovidone (CrosPVP) shows useful characteristics for manufacturing dosage forms." | ( Evaluation of the physicochemical characteristics of crospovidone that influence solid dispersion preparation. Fujii, M; Koizumi, N; Nakanishi, S; Shibata, Y; Sugamura, Y; Suzuki, A; Watanabe, Y, 2011) | 0.65 |
" The outcomes of this work would therefore allow more careful control and selection of the excipient specifications in producing solid dosage formulations with improved dissolution of poorly water-soluble drugs." | ( Understanding improved dissolution of indomethacin through the use of cohesive poorly water-soluble aluminium hydroxide: effects of concentration and particle size distribution. Allahham, A; Morton, DA; Stewart, PJ; Tay, T, 2011) | 0.64 |
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
"This paper report the development of a new dosage form - self-microemulsifying mouth dissolving films, which can improve the oral bioavailability of water insoluble drugs and have good compliance." | ( [Optimization of novel self-microemulsifying mouth dissolving films by response surface methodology]. He, JK; Huan, D; Liu, Y; Xiao, L; Yi, T, 2011) | 0.37 |
" Facilitation of osteoblast apoptosis occurred regardless of IND dosage under hypoxic conditions." | ( Facilitation of human osteoblast apoptosis by sulindac and indomethacin under hypoxic injury. Chang, CH; Chen, YC; Fan, SC; Huang, CH; Liu, C; Tsai, AL; Wu, CC, 2012) | 0.62 |
" Oral administration of IAC dosed at 50 and 100 mg/kg was able to significantly prevent gastric ulceration induced by indomethacin and by stress." | ( Further evidence of the antiulcer activity of IAC, a novel free radical scavenger. Baraldi, M; Carnevale, G; Zanoli, P; Zavatti, M, 2011) | 0.58 |
" Once a day dosage forms for drugs differing in solubility have been developed using a single polymer matrix which is easy to manufacture." | ( pH Sensitive graft copolymers for zero order drug release: a mechanistic analysis. Kulkarni, MG; Muthusamy, R, 2012) | 0.38 |
"Bioadhesive buccal films are innovative dosage forms with the ability to adhere to the mucosal surface and subsequently hydrate to release and deliver drugs across the buccal membrane." | ( Novel films for drug delivery via the buccal mucosa using model soluble and insoluble drugs. Antonijevic, MD; Boateng, JS; Chowdhry, BZ; Kianfar, F, 2012) | 0.38 |
"Multiple indomethacin courses using the standard dosing approach result in high PDA closure rates for infants < 29 weeks gestation." | ( Patent ductus arteriosus in infants <29 weeks gestation--outcomes and factors affecting closure. Kapoor, V; Popat, H; Travadi, J, 2012) | 0.8 |
" Bolus injections of GA elicited dose-response vasodilation, which was abolished after endothelium removal." | ( Endothelium-dependent vascular relaxation induced by Globularia alypum extract is mediated by EDHF in perfused rat mesenteric arterial bed. Ben Cheikh, R; Chokri, A; El Abida, K; Zegzouti, YF, 2012) | 0.38 |
" The explanation of the reduced pharmacodymanic effect in such population is unclear; so far, studies using increased dosing of ibuprofen have failed to show a clear benefit." | ( Ibubrofen in the treatment of patent ductus arteriosus in preterm infants: what we know, what we still do not know. Boubred, F; Buffat, C; Fayol, L; Grandvuillemin, I; Ligi, I; Mercanti, I; Millet, V; Simeoni, U, 2012) | 0.38 |
" Furthermore, 5b could significantly suppress the progression of carrageenan-induced hind paw edema compared to indomethacin at a dosage of 10 mg/kg/day, and dose-dependently ameliorated the development of adjuvant-induced arthritis (AIA) validated by arthritic scores and H&E staining of joints." | ( Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. Cao, D; Chen, J; Chen, L; Deng, C; Li, X; Liang, X; Ma, L; Peng, A; Peng, F; Qiu, J; Ran, Y; Wang, G; Wei, Y; Xiang, M; Xie, C; Yang, Z; Ye, H, 2012) | 0.59 |
" mPEG-PDLLA micelles were found to be efficient carriers for oral administration of IND as solid dosage forms by adsorption on polyplasdone XL-10." | ( Novel oral delivery system of indomethacin by solidified mPEG-PDLLA micelles: in vivo study. Ouahab, A; Shen, Y; Tu, JS, 2012) | 0.67 |
"0-10 mg/mL relaxed high K+ (80 mM) and phenylephrine (PE, 1 μM)-induced contractions and shifted Ca++ dose-response curves to right, similar to that caused by verapamil." | ( Hypotensive effect of Gentiana floribunda is mediated through Ca++ antagonism pathway. Khan, AU; Murugan, DD; Mustafa, MR, 2012) | 0.38 |
"As the main intent of delivering maximum concentration of drug available from the dosage form, an oral compression coated tablet (CCT) was intended to develop with a predetermined lag time of 6 hrs before immediate release of drug to target circadian rhythms of rheumatoid arthritis." | ( Chronotherapeutic drug delivery from indomethacin compression coated tablets for early morning pain associated rheumatoid arthritis. Murthy, KV; Rao, NS; Srikanth, MV; Sunil, SA, 2013) | 0.66 |
" Even the low dose of nanomedicines offered the comparable results to those of control groups at the high dosage in most cases." | ( Assembled nanomedicines as efficient and safe therapeutics for articular inflammation. Che, L; He, H; Jia, Y; Li, S; Li, X; Liu, Y; Zhang, J; Zhou, J; Zhou, X; Zhu, Y, 2012) | 0.38 |
"Acetaminophen is a safe antipyretic and analgesic drug within the clinically recommended dosage range, but overdose can cause fatal liver and or kidney damage." | ( Effect of acetaminophen on the progression of renal damage in adenine induced renal failure model rats. Arimizu, K; Chuang, VT; Hirata, S; Irie, T; Ishitsuka, Y; Kadowaki, D; Kitamura, K; Maruyama, T; Narita, Y; Otagiri, M; Sumikawa, S; Taguchi, K, 2012) | 0.38 |
" Teduglutide, a recombinant human GLP2 variant (GLP2-2G), has increased half-life and stability as compared to the native GLP2 peptide, but still requires twice daily dosing in preclinical models and daily dosing in the clinic." | ( GLP2-2G-XTEN: a pharmaceutical protein with improved serum half-life and efficacy in a rat Crohn's disease model. Alters, SE; Lachinyan, T; McLaughlin, B; Podust, V; Schellenberger, V; Spink, B; Stemmer, WP; Wang, CW, 2012) | 0.38 |
"GLP2-2G-XTEN is intestinotrophic and demonstrates efficacy in a rat Crohn's disease model requiring a lower molar dose and less frequent dosing relative to GLP2-2G peptide." | ( GLP2-2G-XTEN: a pharmaceutical protein with improved serum half-life and efficacy in a rat Crohn's disease model. Alters, SE; Lachinyan, T; McLaughlin, B; Podust, V; Schellenberger, V; Spink, B; Stemmer, WP; Wang, CW, 2012) | 0.38 |
" This study also shows that both agents have similar adverse effects and the choice of one agent over the other should be based on local availability and dosing preference." | ( Effectiveness and safety of indomethacin versus ibuprofen for the treatment of patent ductus arteriosus in preterm infants. Bali, V; Harabor, A; Kamaluddeen, M; Sivanandan, S; Soraisham, AS, 2013) | 0.68 |
" Dose-response curves were also constructed for pre-incubation of vascular rings with Nω-nitro-L-arginine methyl ester (L-NAME) (a non-specific nitric oxide synthase inhibitor), indomethacin (an unspecific cyclooxygenase inhibitor), and 1H-[1,2,4] oxadiazolo [4,3-a]quinoxalin-1-one (ODQ) (a guanylyl cyclase inhibitor)." | ( The lignan (-)-cubebin inhibits vascular contraction and induces relaxation via nitric oxide activation in isolated rat aorta. Andrade E Silva, ML; Bastos, JK; Carvalho, MT; Celotto, AC; Cunha, WR; Evora, PR; Rezende, KC, 2013) | 0.58 |
" More research is needed to determine appropriate dosage and duration of treatment in pediatric indomethacin-responsive headache." | ( Preadolescent indomethacin-responsive headaches without autonomic symptoms. Myers, KA; Smyth, KA, 2013) | 0.97 |
" The aspirin doses were chosen to span the clinical dosing range." | ( Effect of aspirin on bone healing in a rabbit ulnar osteotomy model. Donovan, M; Femino, JE; Fredericks, D; George, M; Lack, WD; Nepola, J; Petersen, E; Smucker, J, 2013) | 0.39 |
"Aspirin delayed bone healing, as demonstrated radiographically and with mechanical testing, in a dose-dependent fashion at salicylate levels equivalent to those resulting from typical human dosing (low-dose aspirin)." | ( Effect of aspirin on bone healing in a rabbit ulnar osteotomy model. Donovan, M; Femino, JE; Fredericks, D; George, M; Lack, WD; Nepola, J; Petersen, E; Smucker, J, 2013) | 0.39 |
"01) were observed 6 h after oral dosage of lactulose." | ( Assessment of gastrointestinal permeability by lactulose test in sheep after repeated indomethacin treatment. Ahmed, S; Bani, P; Bertoni, G; Minuti, A; Piccioli-Cappelli, F; Trevisi, E, 2013) | 0.61 |
" Dose-response curves were obtained with phenylephrine, acetylcholine and sodium nitroprusside." | ( Influence of decompression sickness on vasomotion of isolated rat vessels. Belhomme, M; Buzzacott, P; Guerrero, F; Lambrechts, K; Mansourati, J; Mazur, A; Theron, M; Wang, Q, 2014) | 0.4 |
" Patients were assigned to receive either oral ibuprofen at a dosage of 10, 5, 5 mg/kg every 24 h or three doses of oral indomethacin (0." | ( Comparison of oral ibuprofen with oral indomethacin for PDA closure in Indian preterm neonates: a randomized controlled trial. Agarwal, S; Anand, P; Dubey, NK; Dudeja, A; Maria, A; Yadav, DK; Yadav, S, 2014) | 0.88 |
" We found no dose-response effect." | ( Fetal exposure to nonsteroidal anti-inflammatory drugs and spontaneous abortions. Bilenko, N; Daniel, S; Koren, G; Levy, A; Lunenfeld, E; Ratzon, R, 2014) | 0.4 |
" And the recommended dosage of indomethacin- both test and long-term dosages-is unallowably high." | ( Hemicrania continua: major shortcomings in the new classification. Antonaci, F; Fredriksen, TA; Sjaastad, O, 2014) | 0.69 |
" There was a significant dose-response relationship, with the risk increasing with longer duration of inhaled corticosteroids (P for trend < 0." | ( Cohort study of corticosteroid use and risk of hospital admission for diverticular disease. Abraham-Nordling, M; Håkansson, N; Hjern, F; Mahmood, MW; Wolk, A, 2015) | 0.42 |
" Early detection of crystallization could be pivotal in the successful design of a dosage form where, in order to obtain the desired bioavailability, the drug may be in a high energy state." | ( Compression-induced crystallization of amorphous indomethacin in tablets: characterization of spatial heterogeneity by two-dimensional X-ray diffractometry. Mohapatra, S; Stephenson, GA; Suryanarayanan, R; Thakral, NK, 2015) | 0.67 |
" However, these preventive effects of SAC were dependent on dosage of SAC; higher dose above 10 μM paradoxically aggravated NSAID-induced inflammation." | ( S-allyl cysteine alleviates nonsteroidal anti-inflammatory drug-induced gastric mucosal damages by increasing cyclooxygenase-2 inhibition, heme oxygenase-1 induction, and histone deacetylation inhibition. Hahm, KB; Han, YM; Jung, MK; Kangwan, N; Kim, EH; Lee, SY; Park, JM, 2014) | 0.4 |
"The main goal of the current work was to investigate the possible use of flexographic printing for the conversion of nanosuspensions into solid dosage forms." | ( Fabrication of drug-loaded edible carrier substrates from nanosuspensions by flexographic printing. Genina, N; Kolakovic, R; Laaksonen, T; Määttänen, A; Palo, M; Peltonen, J; Salonen, J; Sandler, N, 2015) | 0.42 |
" It is a major determinant of half-life and dosing frequency of a drug." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
" Accurately dosed samples were generated as a result of the ink and droplet formation optimization." | ( Improvement of dissolution rate of indomethacin by inkjet printing. de Beer, T; Genina, N; Ihalainen, P; Kolakovic, R; Löbmann, K; Määttänen, A; Nyman, JO; Palo, M; Peltonen, J; Rades, T; Rijckaert, K; Sandler, N; Wickström, H, 2015) | 0.69 |
" Furthermore, 1c could suppress the progress of carrageenan-induced hind paw edema at a dosage of 50 mg/kg/day and dose-dependently ameliorate the development of adjuvant-induced arthritis (AIA)." | ( Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. Chen, L; He, J; He, L; Lei, L; Ma, L; Peng, F; Shao, M; Tang, M; Wei, Z; Wu, Y; Zhu, J, 2015) | 0.42 |
"The aim of this work was to prepare a combined drug dosage form of famotidine (FAM) and quercetin (QRT) to augment treatment of gastric ulcer." | ( Evaluation of combined famotidine with quercetin for the treatment of peptic ulcer: in vivo animal study. Abourehab, MA; Ahmed, OA; Khaled, KA; Sarhan, HA, 2015) | 0.42 |
" Dose-response curves to KCl (30-300 mM) were used to bypass G protein-coupled receptor mechanisms." | ( Neuropeptide Y restores non-receptor-mediated vasoconstrictive action in superior mesenteric arteries in portal hypertension. Dietrich, P; Hartl, J; Moleda, L; Müller-Schilling, M; Wiest, R, 2015) | 0.42 |
"(i) Prepare a freeze-dried injectable indomethacin (IMC) dosage form." | ( Salt formation during freeze-drying--an approach to enhance indomethacin dissolution. Suryanarayanan, R; Thakral, S, 2015) | 0.93 |
" Novel semisolid formulations with IND described for the first time in this paper can be considered as an alternative for commercially available conventional topical dosage forms." | ( Rheological and textural properties of microemulsion-based polymer gels with indomethacin. Białas, W; Froelich, A; Kunstman, P; Osmałek, T; Roszak, R, 2016) | 0.66 |
"The acceleration of solid dosage form product development can be facilitated by the inclusion of excipients that exhibit poly-/multi-functionality with reduction of the time invested in multiple excipient optimisations." | ( A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets. Akhtar, N; Alany, R; ElShaer, A; Hussain, T; Iyire, A; Kaialy, W; Mohammed, AR, 2015) | 0.42 |
" Firstly, formulations of indomethacin and nicotinamide in varying weight ratios were studied since novel tablet dosage forms containing multi-drugs are of industrial interest." | ( Comparison of pharmaceutical formulations: ATR-FTIR spectroscopic imaging to study drug-carrier interactions. Biggart, GD; Clarke, GS; Ewing, AV; Hale, CR; Kazarian, SG, 2015) | 0.72 |
" The lesions in the small intestine were examined 24 h after the final dosing of indomethacin." | ( Soluble Dietary Fibers Can Protect the Small Intestinal Mucosa Without Affecting the Anti-inflammatory Effect of Indomethacin in Adjuvant-Induced Arthritis Rats. Hirakawa, T; Matsumoto, H; Satoh, H; Wada, N, 2016) | 0.87 |
" Our PBPK/PD model suggested a higher indomethacin dosing requirement during pregnancy." | ( Development of Physiologically Based Pharmacokinetic/Pharmacodynamic Model for Indomethacin Disposition in Pregnancy. Alqahtani, S; Kaddoumi, A, 2015) | 0.92 |
" Maintaining the amorphous state of drug in a solid dosage form is extremely important to ensure product quality." | ( Thermoanalytical and Fourier transform infrared spectral curve-fitting techniques used to investigate the amorphous indomethacin formation and its physical stability in Indomethacin-Soluplus® solid dispersions. Chi, YT; Hsieh, WH; Huang, YT; Kao, CY; Lin, HL; Lin, SY, 2015) | 0.63 |
" Deep sequencing analysis showed that indomethacin exposure was associated with alterations in the structure of the intestinal microbiota in both dosing models." | ( Bidirectional interactions between indomethacin and the murine intestinal microbiota. Abernethy, DR; Bittinger, K; Bushman, FD; FitzGerald, GA; Li, X; Liang, X, 2015) | 0.97 |
"Although using spray-dried dispersions (SDDs) to improve the bioavailability of poorly water-soluble compounds has become a common practice in supporting the early phases of clinical studies, their performance evaluation, whether in solid dosage forms or alone, still presents significant challenges." | ( Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion. Li, J; Wang, Y; Wu, B, 2016) | 0.43 |
" faecalisovergrowth was independent of the route of administration of the drug, as similar findings were observed in rats orally dosed with theNSAID Bile secretion plays an important role inINDO-induced gut injury and appears to support enterococcal overgrowth of the intestine." | ( Indomethacin injury to the rat small intestine is dependent upon biliary secretion and is associated with overgrowth of enterococci. Cruz, MR; Dial, EJ; Garsin, DA; Lichtenberger, LM; Mayo, SA; Murray, BE; Phan, TM; Singh, KV; Song, YK, 2016) | 1.88 |
" Peak inhibition of urinary metabolite excretion across 8 hours following dosing was the primary end point." | ( Inhibition of prostacyclin and thromboxane biosynthesis in healthy volunteers by single and multiple doses of acetaminophen and indomethacin. Gottesdiener, KM; Greenberg, HE; Mehta, A; Musser, BJ; Schwartz, JI; Taggart, WV; Tanaka, WK, 2015) | 0.62 |
" Each rat to receive nebivolol and omeprazole was given the agent orally (by gavage) daily for 10 days prior to induction of ulcer by oral dosing with INDO." | ( Nebivolol prevents indomethacin-induced gastric ulcer in rats. El-Ashmawy, NE; El-Bahrawy, HA; Khedr, EG; Selim, HM, 2016) | 0.76 |
" In this work we use hot-melt extrusion for manufacturing of medicinal films containing indomethacin (IND) and polycaprolactone (PCL), extruded strands with nitrofurantoin monohydrate (NFMH) and poly (ethylene oxide) (PEO), and feedstocks for 3D printed dosage forms with nitrofurantoin anhydrate (NFAH), hydroxyapatite (HA) and poly (lactic acid) (PLA)." | ( Near-infrared chemical imaging (NIR-CI) of 3D printed pharmaceuticals. Aho, J; Bøtker, J; Edinger, M; Khorasani, M; Raijada, D; Rantanen, J, 2016) | 0.66 |
" The potential use of albumin as solubility enhancer for poorly soluble drugs, particularly, for immediate release volume-limited dosage forms is reported." | ( Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin. Abdelkader, H; Alany, RG; ElShaer, A; Karam, A; Khoder, M; Najlah, M, 2016) | 0.43 |
", dose) on the resulting kinetic solubility profiles of supersaturating dosage forms." | ( Effect of Extent of Supersaturation on the Evolution of Kinetic Solubility Profiles. Han, YR; Lee, PI, 2017) | 0.46 |
"In situ amorphization is a concept that allows to amorphize a given drug in its final dosage form right before administration." | ( Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ. Doreth, M; Grohganz, H; Holm, R; Hussein, MA; Löbmann, K; Lopez de Diego, H; Priemel, PA; Rades, T, 2017) | 0.46 |
" In this study, fluid bed coating is proposed for the production of controlled release dosage forms of glass solutions by applying a second, rate controlling membrane on top of the glass solution." | ( Controlling the Release of Indomethacin from Glass Solutions Layered with a Rate Controlling Membrane Using Fluid-Bed Processing. Part 1: Surface and Cross-Sectional Chemical Analysis. Dereymaker, A; Roberts, CJ; Scurr, DJ; Steer, ED; Van den Mooter, G, 2017) | 0.75 |
"Microemulsion-based semisolid systems may be considered as an interesting alternative to the traditional dosage forms applied in topical drug delivery." | ( Novel microemulsion-based gels for topical delivery of indomethacin: Formulation, physicochemical properties and in vitro drug release studies. Białas, W; Froelich, A; Jadach, B; Kunstman, P; Olejniczak, M; Osmałek, T; Roszak, G; Snela, A, 2017) | 0.7 |
" Orodispersible films (ODF) have increasingly been evaluated as a suitable dosage form for extemporaneous oral preparations." | ( Application of miniaturized near-infrared spectroscopy for quality control of extemporaneous orodispersible films. Chan, SY; Foo, WC; Gokhale, R; Khong, YM; Widjaja, E, 2018) | 0.48 |
" In the present study, a robust electromagnetic (valvejet) inkjet technology has been successfully applied to deposit prototype dosage forms from solutions with a wide range of viscosities, and from suspensions with particle sizes exceeding 2 μm." | ( Inkjet printing of paracetamol and indomethacin using electromagnetic technology: Rheological compatibility and polymorphic selectivity. Croker, DM; Glowacki, BA; Hopkins, SC; Kollamaram, G; Walker, GM, 2018) | 0.76 |
"Three- dimensional (3D) printing has received significant attention as a manufacturing process for pharmaceutical dosage forms." | ( 3D Printed "Starmix" Drug Loaded Dosage Forms for Paediatric Applications. Douroumis, D; Ross, SA; Scoutaris, N, 2018) | 0.48 |
" Using an in vitro experimental approach, the physiological role of the airway epithelium on smooth muscle relaxation has been investigated by analyzing the dose-response curves for carbachol- or histamine-induced contractions on epithelium intact versus denuded tracheal tissue." | ( Relaxant effect of ghrelin on guinea pig isolated tracheal smooth muscle: role of epithelial NO and PGE Al-Ayed, MSZ, 2018) | 0.48 |
" The recommended phase II dose is 75 mg indomethacin TID given 8 days surrounding standard dosed CAPOX." | ( Phase I study of combined indomethacin and platinum-based chemotherapy to reduce platinum-induced fatty acids. Bloemendal, HJ; Boot, H; Cirkel, GA; Daenen, LGM; De Vos, FY; Gerrits, J; Grootscholten, C; Houthuijzen, JM; Kaing, S; Roodhart, JML; Sessa, C; van der Velden, DL; van Werkhoven, E; Verhoeven-Duif, NM; Voest, EE, 2018) | 1.05 |
" Therefore, it is of increasing importance to configure new dosing strategies and alleviate the side effects of NSAIDs." | ( Anti-inflammatory polymersomes of redox-responsive polyprodrug amphiphiles with inflammation-triggered indomethacin release characteristics. Deng, Z; Hu, J; Liu, G; Liu, S; Tan, J, 2018) | 0.7 |
" Aim of this study was to prepare chitosan-lipid hybrid delivery systems for indomethacin dosage through a novel continuous method based on microfluidic principles." | ( Polymer-lipid hybrid nanoparticles as enhanced indomethacin delivery systems. Barba, AA; Bertoncin, P; Bochicchio, S; Dalmoro, A; Lamberti, G; Moustafine, RI; Nasibullin, SF, 2018) | 0.97 |
" We sought to determine whether a relationship exists between preoperative indomethacin dosing and fetal DA constriction." | ( Indomethacin Dosing and Constriction of the Ductus Arteriosus During Open Fetal Surgery for Myelomeningocele Repair. Behrendt, N; Chatterjee, D; Crombleholme, TM; Cuneo, BF; Galan, HL; Howley, LW; Marwan, AI; Patel, SS; Wood, C; Zaretsky, MV; Zuk, J, 2019) | 2.19 |
" QD indomethacin and greater magnesium sulfate dosing was associated with reduced DA constriction." | ( Indomethacin Dosing and Constriction of the Ductus Arteriosus During Open Fetal Surgery for Myelomeningocele Repair. Behrendt, N; Chatterjee, D; Crombleholme, TM; Cuneo, BF; Galan, HL; Howley, LW; Marwan, AI; Patel, SS; Wood, C; Zaretsky, MV; Zuk, J, 2019) | 2.51 |
" Overall, this study demonstrates the potential value of nonlinear optical imaging, together with more established solid-state analysis methods, to understand complex surface crystallization behavior and its influence on drug dissolution during the development of amorphous drugs and dosage forms." | ( Understanding Dissolution and Crystallization with Imaging: A Surface Point of View. Fraser-Miller, SJ; Isomäki, A; Laaksonen, T; Novakovic, D; Peltonen, L; Pleunis, B; Strachan, CJ, 2018) | 0.48 |
"Co-amorphous mixtures have rarely been formulated as oral dosage forms, even though they have been shown to stabilize amorphous drugs in the solid state and enhance the dissolution properties of poorly soluble drugs." | ( Preparation and characterization of multi-component tablets containing co-amorphous salts: Combining multimodal non-linear optical imaging with established analytical methods. Korhonen, O; Laitinen, R; Ojarinta, R; Saarinen, J; Strachan, CJ, 2018) | 0.48 |
"The aim of this study was to demonstrate the usefulness of the time domain nuclear magnetic resonance (TD-NMR) method to characterize the crystalline state of active pharmaceutical ingredients (APIs) containing solid dosage forms." | ( Hayashi, Y; Hirai, D; Kosugi, A; Kumada, S; Okada, K; Onuki, Y, 2019) | 0.51 |
" Although promising, acetaminophen treatment requires further studies regarding long-term safety as well as ideal dosing and route of administration." | ( Pharmacotherapy for patent ductus arteriosus closure. Ferguson, JM, 2019) | 0.51 |
"The in vitro dissolution absorption system 2 (IDAS2), a recent invention comprised a conventional dissolution vessel containing 2 permeation chambers with Caco-2 cell monolayers mounted with their apical side facing the dissolution media, permits simultaneous measurement of dissolution and permeation of drugs from intact clinical dosage forms." | ( Simultaneous Analysis of Dissolution and Permeation Profiles of Nanosized and Microsized Formulations of Indomethacin Using the In Vitro Dissolution Absorption System 2. Hidalgo, C; Hidalgo, IJ; Huang, Y; Li, J; Li, LB; Nessah, N; Owen, A, 2019) | 0.73 |
" This work thus highlights the importance of having both complimentary IDR and whole dosage imaging techniques in giving a better understanding of solid dispersion systems." | ( Effect of preparation method on the surface properties and UV imaging of indomethacin solid dispersions. Adebisi, AO; Alshafiee, M; Asare-Addo, K; Conway, BR; Diza, C; Elawad, S; Mawla, N; Taheri, S; Timmins, P; Totea, AM; Walton, K; Ward, A, 2019) | 0.75 |
"Oral administration of a solid dosage form requires drug dissolution in the gastrointestinal tract before absorption." | ( Topography of Simulated Intestinal Equilibrium Solubility. Dunn, C; Halbert, GW; Khadra, I; Perrier, J; Wilson, CG, 2019) | 0.51 |
"There is a trend in pharmaceutical research and development to develop depot formulations with dosing once weekly, once monthly, or even less frequently." | ( Nanoshells prepared by atomic layer deposition - Long acting depots of indomethacin. Hellrup, J; Johansson, A; Mårtensson, E; Rooth, M; Sigfridsson, K, 2019) | 0.75 |
" The concentration of ETV in the liver was not obviously altered during pregnancy, which indicates that dosage adjustment in pregnancy is not necessary." | ( Roles of organic anion transporter 2 and equilibrative nucleoside transporter 1 in hepatic disposition and antiviral activity of entecavir during non-pregnancy and pregnancy. Bai, M; Jiang, H; Jiang, T; Lin, N; Lu, S; Ma, Z; Sun, D; Zeng, S; Zhou, H, 2019) | 0.51 |
"Pharmaceutical manufacturing processes are necessary to make solid dosage form even in cocrystal formation." | ( Kinetics Study of Cocrystal Formation Between Indomethacin and Saccharin Using High-Shear Granulation With In Situ Raman Spectroscopy. Ashizawa, K; Hattori, Y; Otsuka, M; Tanaka, R, 2019) | 0.77 |
" In a proof-of-concept preclinical application, we utilize this system to investigate the way in which rapid dosing of human whole blood with isoform selective inhibitors of phosphatidylinositol 3-kinase dose dependently modulate platelet thrombus dynamics." | ( Active Micropump-Mixer for Rapid Antiplatelet Drug Screening in Whole Blood. Akbaridoust, F; Brazilek, RJ; de Silva, C; Hamilton, JR; Marusic, I; Mitchell, A; Moon, M; Nandurkar, HH; Nesbitt, WS; Ooi, ASH; Szydzik, C, 2019) | 0.51 |
"Few studies exist that have evaluated the effects of indomethacin dosing frequency as a factor associated with successful patent ductus arteriosus closure in very low birth weight neonates." | ( Indomethacin dosing strategy and neonatal patent ductus arteriosus closure. Messina, C; Mintzer, JP; Rathi, P, 2019) | 2.21 |
" Less ligation of the patent ductus arteriosus occurred with every 12 hour versus every 24 hour dosing (11% vs." | ( Indomethacin dosing strategy and neonatal patent ductus arteriosus closure. Messina, C; Mintzer, JP; Rathi, P, 2019) | 1.96 |
" Further prospective analysis of indomethacin dosing strategy is warranted." | ( Indomethacin dosing strategy and neonatal patent ductus arteriosus closure. Messina, C; Mintzer, JP; Rathi, P, 2019) | 2.24 |
"Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation." | ( Formation of Indomethacin-Saccharin Cocrystals during Wet Granulation: Role of Polymeric Excipients. Duggirala, NK; Hattori, Y; Otsuka, M; Suryanarayanan, R; Tanaka, R, 2020) | 0.93 |
"2 ml 35 µM indomethacin solution (resulting in a final concentration of 8 µg/ml in the follicular fluid) was the minimal dosage leading to COF formation." | ( Induction of cystic ovarian follicles (COFs) in cattle by using an intrafollicular injection of indomethacin. Lapp, R; Röttgen, V; Vernunft, A; Viergutz, T; Weitzel, JM, 2020) | 1.17 |
" The association of DA constriction and low BMI suggests that BMI-based dosing of indomethacin may be recommended for perioperative tocolysis in fetal MMC surgery." | ( Maternal low body mass index is a risk factor for fetal ductal constriction following indomethacin use among women undergoing fetal repair of spina bifida. Belfort, MA; Cortes, MS; Donado, MY; Erfani, H; Espinoza, J; Furtun, BY; Nassr, AA; Olutoye, O; Shamshirsaz, AA; Velez, MP; Whitehead, WE, 2020) | 1.01 |
" Our objective was to show that indomethacin could be considered as a promising candidate for the treatment of SARS-CoV-2 and to provide criteria for comparing benefits of alternative dosage regimens using a model-based approach." | ( Model based approach for estimating the dosage regimen of indomethacin a potential antiviral treatment of patients infected with SARS CoV-2. Bressolle-Gomeni, F; Gao, X; Gomeni, R; Xu, T, 2020) | 1.09 |
" Through this work, we have demonstrated that by the implementation of predictive thermodynamic modelling, HDASD formulation design can be integrated into the HME process design to ensure the desired quality of the final dosage form." | ( The design and development of high drug loading amorphous solid dispersion for hot-melt extrusion platform. Andrews, GP; Jacobs, E; Jones, DS; McCoy, CP; Tian, Y; Wu, H, 2020) | 0.56 |
" It is of great importance to configure new dosing strategies for alleviating the side effects of NSAIDs." | ( An Enzyme-Responsive Prodrug with Inflammation-Triggered Therapeutic Drug Release Characteristics. Gong, M; Liao, M; Meng, Q; Shi, R; Xie, W; Xue, J; Ye, J; Zhang, L; Zhang, X, 2020) | 0.56 |
" In this paper, we explore different pharmaceutical-grade feedstock materials for creating tablet-like dosage forms using a binder jet 3D printing method." | ( Binder-Jet 3D Printing of Indomethacin-laden Pharmaceutical Dosage Forms. Chang, SY; Chaudhuri, B; Kowsari, K; Li, SW; Ma, AWK; Nagapudi, K; Sen, K; Shetty, A; Sorrells, L, 2020) | 0.86 |
"We previously designed an ophthalmic dispersion containing indomethacin nanocrystals (IMC-NCs), showing that multiple energy-dependent endocytoses led to the enhanced absorption of drugs from ocular dosage forms." | ( In Situ Gelling Systems Using Pluronic F127 Enhance Corneal Permeability of Indomethacin Nanocrystals. Deguchi, S; Isaka, T; Minami, M; Nagai, N; Nakazawa, Y; Okamoto, N; Otake, H; Yamaguchi, M, 2020) | 1.03 |
" Initial dosing consisted of indomethacin, followed by ibuprofen in most cases." | ( Effect of In Utero Non-Steroidal Anti-Inflammatory Drug Therapy for Severe Ebstein Anomaly or Tricuspid Valve Dysplasia (NSAID Therapy for Fetal Ebstein anomaly). Beroukhim, RS; Cumbermack, KM; Ferrer, Q; Freud, LR; Glickstein, JS; LaFranchi, T; Makhoul, M; Morris, SA; Pedra, SR; Phoon, CK; Sun, HY; Tworetzky, W; Wilkins-Haug, LE, 2021) | 0.91 |
" However, increasing the dosage increases the oxidative stress." | ( Early closure mechanisms of the ductus arteriosus in immature infants. Aikio, O; Hallman, M; Rozé, JC; Treluyer, JM, 2021) | 0.62 |
" Additional studies are warranted to understand the exposure-response relationship and provide appropriate dosing recommendations during pregnancy that consider both safety and efficacy." | ( Prediction of maternal and fetal pharmacokinetics of indomethacin in pregnancy. Ahmed, MS; Caritis, SN; Clark, SM; Hankins, GDV; Nanovskaya, TN; Pillai, VC; Rytting, E; Shah, M; Venkataramanan, R; Wang, X, 2022) | 0.97 |
" The mechanism underpinning pain relief induced by the GlyT2 inhibitor at 10 mg/kg is likely due to increased glycinergic inhibition in the lumbar spinal cord, although the bell-shaped dose-response curve warrants further translational considerations." | ( Assessment of the Anti-Allodynic and Anti-Hyperalgesic Efficacy of a Glycine Transporter 2 Inhibitor Relative to Pregabalin, Duloxetine and Indomethacin in a Rat Model of Cisplatin-Induced Peripheral Neuropathy. Corradini, L; Kuo, A; Nicholson, JR; Smith, MT, 2021) | 0.82 |
" For salt formation, a salt form with high crystallinity and sufficient solid-state stability is required for solid dosage form development." | ( Effect of Counterions on Dissolution of Amorphous Solid Dispersions Studied by Surface Area Normalized Dissolution. Chen, Y; Lubach, JW; Narang, AS; Tang, S, 2021) | 0.62 |
" Precisely, the surface properties of APIs and excipients affect the compatibility of the resulting dosage form." | ( Influence of active pharmaceutical ingredient structures on Hansen solubility parameters. Gorlová, O; Patera, J; Petříková, E, 2021) | 0.62 |
" AF-PTIR microscopy has the potential to assist in the early identification of crystal form impurities in the solid dosage forms development pipeline." | ( Parts-per-Million Detection of Trace Crystal Forms Using AF-PTIR Microscopy. Li, M; Razumtcev, A; Simpson, GJ, 2022) | 0.72 |
" This study explored whether higher concentrations of the biologically active S-enantiomer or increased R- to S-conversion following oral dosing could explain this finding." | ( Oral Ibuprofen Is More Effective than Intravenous Ibuprofen for Closure of a Patent Ductus Arteriosus: Can Pharmacokinetic Modeling Help Us to Understand Why? Engbers, AGJ; Flint, RB; Knibbe, CAJ; Pfister, M; Samiee-Zafarghandy, S; Simons, SHP; Smit, C; van den Anker, JN; van Donge, T, 2023) | 0.91 |
" Concentration-time profiles in typical neonates were explored and compared in different dosing or R- to S-conversion scenarios." | ( Oral Ibuprofen Is More Effective than Intravenous Ibuprofen for Closure of a Patent Ductus Arteriosus: Can Pharmacokinetic Modeling Help Us to Understand Why? Engbers, AGJ; Flint, RB; Knibbe, CAJ; Pfister, M; Samiee-Zafarghandy, S; Simons, SHP; Smit, C; van den Anker, JN; van Donge, T, 2023) | 0.91 |
" Upon oral dosing, S-ibuprofen concentrations were lower compared to IV ibuprofen for a large part of the dosing interval." | ( Oral Ibuprofen Is More Effective than Intravenous Ibuprofen for Closure of a Patent Ductus Arteriosus: Can Pharmacokinetic Modeling Help Us to Understand Why? Engbers, AGJ; Flint, RB; Knibbe, CAJ; Pfister, M; Samiee-Zafarghandy, S; Simons, SHP; Smit, C; van den Anker, JN; van Donge, T, 2023) | 0.91 |
" While a fraction of up to 45% presystemic R- to S-conversion could not be ruled out, the impact of such a low conversion might be only relevant for the standard but not high dosing regimens, considering reported exposure-response targets." | ( Oral Ibuprofen Is More Effective than Intravenous Ibuprofen for Closure of a Patent Ductus Arteriosus: Can Pharmacokinetic Modeling Help Us to Understand Why? Engbers, AGJ; Flint, RB; Knibbe, CAJ; Pfister, M; Samiee-Zafarghandy, S; Simons, SHP; Smit, C; van den Anker, JN; van Donge, T, 2023) | 0.91 |
" Firstly, the hypotensive dose-response relationship of pulegone was evaluated in normotensive anesthetized rats using the invasive method." | ( Pulegone Prevents Hypertension through Activation of Muscarinic Receptors and Cyclooxygenase Pathway in L-NAME-Induced Hypertensive Rats. Alsahli, TG; Bashir, A; Ehsan, R; Gasparotto Junior, A; Jahan, S; Malik, MNH; Razzaq, MA; Younis, W, 2023) | 0.91 |
" To investigate the mechanism of action, conducted assays of antioxidant activity, measured the dosage of inflammatory cytokines, quantified mucus, treated with inhibitors (IND, L-NAME, glibenclamide, and yohimbine), performed histopathological analysis, and measured gastric acid secretion." | ( Antiulcer activity and mechanism of action of the hydroethanolic extract of leaves of Terminalia argentea Mart. In different in vivo and in vitro experimental models. Arunachalam, K; Damazo, AS; Figueiredo, FF; Martins, DTO; Muller, JAI; Oliveira, DM; Serio, BFD; Silva, MJD; Venturini, CL, 2024) | 1.44 |
"Intestinal drug solubility is a key parameter controlling absorption after the administration of a solid oral dosage form." | ( Structured solubility behaviour in fed simulated intestinal fluids. Halbert, GW; Khadra, I; Pyper, K; Silva, MI, 2023) | 0.91 |
Role | Description |
---|---|
non-steroidal anti-inflammatory drug | An anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. |
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor | A compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes. |
analgesic | An agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms. |
gout suppressant | A drug that increases uric acid excretion by the kidney (uricosuric drug), decreases uric acid production (antihyperuricemic), or alleviates the pain and inflammation of acute attacks of gout. |
drug metabolite | null |
xenobiotic metabolite | Any metabolite produced by metabolism of a xenobiotic compound. |
xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
indole-3-acetic acids | An indol-3-yl carboxylic acid in which the carboxylic acid specified is acetic acid. |
N-acylindole | A carboxamide resulting from the formal condensation of a carboxylic acid with the nitrogen of an indole. |
monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Pathway | Proteins | Compounds |
---|---|---|
Indomethacin Action Pathway | 30 | 67 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.9953 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 25.1574 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 10.0000 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 21.3313 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
interleukin 8 | Homo sapiens (human) | Potency | 66.8242 | 0.0473 | 49.4806 | 74.9780 | AID651758 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 24.5412 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 34.1509 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
SMAD family member 2 | Homo sapiens (human) | Potency | 7.1093 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
SMAD family member 3 | Homo sapiens (human) | Potency | 7.1093 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
TDP1 protein | Homo sapiens (human) | Potency | 31.6768 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 19.9526 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
AR protein | Homo sapiens (human) | Potency | 16.2644 | 0.0002 | 21.2231 | 8,912.5098 | AID588516; AID743035; AID743036; AID743053; AID743063 |
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 7.5397 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 40.9268 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
progesterone receptor | Homo sapiens (human) | Potency | 21.4946 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 19.4971 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 15.4754 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259256 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 12.8968 | 0.0002 | 14.3764 | 60.0339 | AID588532; AID720691; AID720692 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 18.0339 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID588544; AID588546 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 37.8932 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 17.4788 | 0.3758 | 27.4851 | 61.6524 | AID588527; AID743220 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 12.8114 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID588513; AID588514; AID743069; AID743075 |
G | Vesicular stomatitis virus | Potency | 10.9640 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
67.9K protein | Vaccinia virus | Potency | 5.0119 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
glucocerebrosidase | Homo sapiens (human) | Potency | 0.6310 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
Parkin | Homo sapiens (human) | Potency | 20.5962 | 0.8199 | 14.8306 | 44.6684 | AID720572 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 100.0000 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 12.4588 | 0.0010 | 24.5048 | 61.6448 | AID588534; AID588535; AID743212; AID743215 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 7.8990 | 0.0010 | 19.4141 | 70.9645 | AID588536; AID588537; AID743094; AID743140; AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 6.5911 | 0.0237 | 23.2282 | 63.5986 | AID588541; AID588543; AID743222; AID743223; AID743241 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.1854 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 14.1254 | 0.0165 | 25.3078 | 41.3999 | AID602332 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 33.4915 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 35.6278 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 0.0020 | 7.5337 | 39.8107 | AID891 |
peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 84.9214 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 29.8816 | 0.0063 | 6.9043 | 39.8107 | AID883 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 31.3540 | 0.0100 | 39.5371 | 1,122.0200 | AID588547 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0003 | 23.4451 | 159.6830 | AID743065 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 33.4889 | 0.0420 | 27.3789 | 61.6448 | AID743210 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 6.3096 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 4.6451 | 0.0037 | 8.6189 | 23.2809 | AID2668 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 57.1055 | 0.0006 | 27.2152 | 1,122.0200 | AID651741 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 63.0957 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 12.5893 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 7.5193 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 0.7943 | 0.1778 | 24.7352 | 79.4328 | AID488949 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.2202 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 1.5849 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 15.1017 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 10.9640 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.9640 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 3.4376 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 15.1017 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 29.8816 | 0.0063 | 8.2350 | 39.8107 | AID883 |
Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 9.4392 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 3.9811 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 7.9433 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.9640 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.9640 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Albumin | Homo sapiens (human) | Kd | 60.3500 | 0.0893 | 3.3135 | 8.0000 | AID1450923; AID1821157 |
Androgen receptor | Homo sapiens (human) | EC50 (µMol) | 0.0001 | 0.0000 | 0.2079 | 4.3000 | AID729242 |
Prostaglandin G/H synthase 2 | Homo sapiens (human) | Kd | 1.0200 | 0.0090 | 1.8725 | 8.4000 | AID1802596 |
Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | EC50 (µMol) | 50.0000 | 0.0000 | 0.9922 | 10.0000 | AID381056 |
Prostaglandin D2 receptor 2 | Homo sapiens (human) | EC50 (µMol) | 0.3890 | 0.0240 | 0.2673 | 0.3890 | AID705365 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Prostaglandin G/H synthase 1 | Bos taurus (cattle) | ID50 | 0.4300 | 0.4300 | 3.6650 | 6.9000 | AID160715 |
Prostaglandin G/H synthase 2 | Bos taurus (cattle) | ID50 | 0.4300 | 0.4300 | 3.6650 | 6.9000 | AID160715 |
Prostaglandin G/H synthase 1 | Ovis aries (sheep) | Kinact | 3.9000 | 3.9000 | 3.9000 | 3.9000 | AID328898 |
Polyunsaturated fatty acid 5-lipoxygenase | Rattus norvegicus (Norway rat) | ID50 | 25.0000 | 0.1400 | 0.3100 | 0.4800 | AID3620 |
Prostaglandin G/H synthase 2 | Mus musculus (house mouse) | Activity | 0.2500 | 0.2500 | 0.2500 | 0.2500 | AID313120 |
Solute carrier family 22 member 7 | Rattus norvegicus (Norway rat) | Km | 0.3660 | 0.3660 | 0.3900 | 0.4140 | AID678818 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1802223 | COX Enzyme Inhibition Assay (Table 2) from Article 10.1021/acschembio.6b00560: \\Antitumor Activity of Cytotoxic Cyclooxygenase-2 Inhibitors.\\ | 2016 | ACS chemical biology, 11-18, Volume: 11, Issue:11 | Antitumor Activity of Cytotoxic Cyclooxygenase-2 Inhibitors. |
AID1802056 | In vitro COX Inhibition Assay from Article 10.1016/j.bioorg.2016.10.003: \\Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibi | 2016 | Bioorganic chemistry, 12, Volume: 69 | Design, synthesis, evaluation and molecular modelling studies of some novel 5,6-diphenyl-1,2,4-triazin-3(2H)-ones bearing five-member heterocyclic moieties as potential COX-2 inhibitors: A hybrid pharmacophore approach. |
AID1799750 | Paraoxonase Activity Assay from Article 10.1080/14756360802608351: \\Effect of some analgesics on paraoxonase-1 purified from human serum.\\ | 2009 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 24, Issue:4 | Effect of some analgesics on paraoxonase-1 purified from human serum. |
AID1800287 | Cyclooxygenase activity assay from Article 10.1111/cbdd.12280: \\Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1.\\ | 2014 | Chemical biology & drug design, Jun, Volume: 83, Issue:6 | Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1. |
AID1801102 | Cyclooxygenase Assay from Article 10.1111/cbdd.12457: \\Synthesis, Molecular Modeling, and Biological Evaluation of Novel 1, 3-Diphenyl-2-propen-1-one Based Pyrazolines as Anti-inflammatory Agents.\\ | 2015 | Chemical biology & drug design, Jun, Volume: 85, Issue:6 | Synthesis, Molecular Modeling, and Biological Evaluation of Novel 1, 3-Diphenyl-2-propen-1-one Based Pyrazolines as Anti-inflammatory Agents. |
AID1802222 | COX Enzyme Inhibition Assay (Table 1) from Article 10.1021/acschembio.6b00560: \\Antitumor Activity of Cytotoxic Cyclooxygenase-2 Inhibitors.\\ | 2016 | ACS chemical biology, 11-18, Volume: 11, Issue:11 | Antitumor Activity of Cytotoxic Cyclooxygenase-2 Inhibitors. |
AID1798273 | Time-Dependent Inhibition Assay from Article 10.1073/pnas.97.2.925: \\Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.\\ | 2000 | Proceedings of the National Academy of Sciences of the United States of America, Jan-18, Volume: 97, Issue:2 | Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors. |
AID1802596 | In Vitro COX Inhibition Assay from Article 10.1016/j.bioorg.2017.02.006: \\Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analg | 2017 | Bioorganic chemistry, 04, Volume: 71 | Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents. |
AID1797638 | 3alpha-Androstanediol Oxidation Inhibition Assay from Article 10.1158/0008-5472.can-03-2847: \\Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.\\ | 2004 | Cancer research, Mar-01, Volume: 64, Issue:5 | Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin. |
AID1799729 | Enzyme Inhibition Assay from Article 10.1080/14756360802188404: \\Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.\\ | 2009 | Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 24, Issue:1 | Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents. |
AID1797639 | Androsterone Reduction Inhibition Assay from Article 10.1158/0008-5472.can-03-2847: \\Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.\\ | 2004 | Cancer research, Mar-01, Volume: 64, Issue:5 | Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin. |
AID1801084 | In vitro Cyclooxygenase Inhibition Assay from Article 10.1111/cbdd.12435: \\1,2-Diaryl-2-hydroxyiminoethanones as dual COX-1 and u00DF-amyloid aggregation inhibitors: biological evaluation and in silico study.\\ | 2015 | Chemical biology & drug design, Apr, Volume: 85, Issue:4 | 1,2-Diaryl-2-hydroxyiminoethanones as dual COX-1 and β-amyloid aggregation inhibitors: biological evaluation and in silico study. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID188070 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 1 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 21nd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID328898 | Binding affinity to ovine COX1 at 1 uM to 25 uM | 2007 | The Journal of biological chemistry, Sep-21, Volume: 282, Issue:38 | Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides. |
AID1330202 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 4 hrs before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID177073 | Efficacy in rat pyresis assay upon oral administration | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors. |
AID161660 | Inhibition of human Prostaglandin G/H synthase 1 | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID181451 | Evaluated for the carrageenan-induced paw edema on 32-day after 3.16 mg/kg dose of peroral administration of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents. |
AID1220787 | Fraction unbound in dog plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID681928 | TP_TRANSPORTER: inhibition of E217betaG in the presence of Indomethacin at a concentration of 50uM in membrane vesicles from MRP4-expressing Sf9 cells | 2003 | Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16 | The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. |
AID1392323 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 50 mg/kg, po measured at 2 hrs relative to control | |||
AID674728 | Inhibition of COX2 by by Cayman's COX activity assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID289293 | Antiinflammatory activity against carrageenan-induced hind paw oedema in Swiss Albino mouse assessed as swelling thickeness at 100 mg/kg, po after 270 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID396332 | Analgesic activity in mouse assessed as protection against phenylquinone-induced writhing at 7.5 mg/kg, po administered 1 hr before phenylquinone challenge measured for 5 mins relative to controll | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents. |
AID63427 | Antagonist activity was measured by maximum urine flow with a dose of 100 ug/kg peptide | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity. |
AID752636 | Antiplatelet activity in human platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation preincubated for 3 mins before arachidonic acid challenge by turbidimetric method | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Pyrazole derivatives as inhibitors of arachidonic acid-induced platelet aggregation. |
AID1510615 | Inhibition of Bacillus cereus 569/H9 beta-lactamase incubated for 10 mins followed by nitrocefin substrate challenge and measured for 5 mins by spectrophotometric analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors. |
AID1241840 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 12 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID753750 | Gastrointestinal toxicity in albino rat assessed as ulcer index at 0.28 mmol/kg, po (Rvb = 0.60 +/- 0.05) | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1192209 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat assessed as edema volume at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 3 hrs (Rvb = 1.73 +/- 0.09 mL) | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID177889 | Inhibition of carrageenan edema in adrenalectomized rats was determined after peroral administration | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones. |
AID1220242 | Unbound intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID178643 | Antiinflammatory activity by using Rat paw edema assay | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile. |
AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1136205 | Analgesic activity in po dosed dog knee joint pain model | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Novel analgesic-antiinflammatory salicylates. |
AID1713248 | Inhibition of ovine COX-2 assessed as appearance of oxidized TMPD level by EIA method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study. |
AID426478 | Cytotoxicity against mouse L1.2 cells assessed as cell viability by trypan blue dye exclusion assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors. |
AID536469 | Antiinflammatory activity against carrageenan-induced fisher 344 rat paw edema model assessed as reduction of paw volume at 50 mg/kg, ip after 3.5 hrs by plethysmometer | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Use of phosphonyl carbanions in the synthesis of anti-inflammatory active phosphorus-containing fused heterocycles and relevance phosphonates. |
AID595367 | Antiinflammatory activity against human THP1 cells of assessed as inhibition of LPS-induced TNFalpha gene expression at 10 uM pretreated for 1 hr before LPS challenge measured after 2 to 10 hrs by RT-qPCR | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID176996 | In vivo antiinflammatory activity by rat carrageenan-induced paw edema assay | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Synthesis and In vivo anti-inflammatory activity of long-chain 2-amino-alcohols. |
AID1153843 | Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as residual activity at 10 uM preincubated for 5 mins followed by substrate addition measured after 5 mins by HPLC analysis relative to control | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID1175391 | Inhibition of human TRPV1 overexpressed in BEAS-2B cells assessed as residual activity at 250 uM after 30 mins by Fluo-4 AM fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates. |
AID1351162 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA (Rvb = 175.2 +/- 10.2 pg/m | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID1063317 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured by ELISA | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID448017 | Inhibition of COX2-mediated PGH2 production by enzyme immunoassay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain. |
AID1409613 | Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID540221 | Volume of distribution at steady state in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1199431 | Inhibition of carrageenan-induced COX-2 expression in paw tissue (unknown origin) by immunohistochemistry | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID1311788 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as PGE2 levels by ELISA (Rvb = 33.2 +/- 2.33 pg/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID1254090 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 1 hr before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID681536 | TP_TRANSPORTER: uptake in Ntcp-expressing COS-7 cells | 2000 | Pharmaceutical research, Apr, Volume: 17, Issue:4 | Pharmacokinetic study of the hepatobiliary transport of indomethacin. |
AID1568918 | Inhibition of recombinant human COX-2 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method | |||
AID161005 | Inhibition of Prostaglandin G/H synthase in intact RBL-1 cell line | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase. |
AID647951 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced malondialdehyde level in paw serum at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 5 hrs by TRARS method | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID128182 | Compound was tested for hyperalgesia activity in mice after perorally administered at 1 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1063660 | Antiinflammatory activity in Wistar rat assessed as change in carrageenan-induced hind paw thickness at 5 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 1 hr (Rvb = 1.84 +/- 0.41 mm) | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors. |
AID160721 | In vitro inhibitory activity against cyclooxygenase of human platelets was determined | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Benzimidazole derivatives with atypical antiinflammatory activity. |
AID185020 | Minimum effective dose is the lowest dose preventing any futher increase in body temperature | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID1743653 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID179451 | Analgesic activity on peroral administration against Scald induced pain in rat paw | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
AID187314 | Relative Oral Anti inflammatory activity in the 5-h Evans Blue-Carrageenan pleural assay using indomethacin as reference compound | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives. |
AID1730826 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL6 production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 22 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice. |
AID1426399 | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID640712 | Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid induced writhing at 10 mg/kg, po measured every 5 mins for 45 mins | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation. |
AID355094 | Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release at 100 uM by Ellman's method relative to control | 1996 | Journal of natural products, Dec, Volume: 59, Issue:12 | Antiinflammatory activity of coumarins from Santolina oblongifolia. |
AID1220796 | Drug metabolism in bile duct-cannulated rat assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID703844 | Inhibition of 5-lipoxygenase in A23187-stimulated human neutrophils assessed as inhibition of enzyme product formation by RP-HPLC analysis | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX. |
AID399405 | Inhibition of sheep placental cotyledons COX2 assessed as PGE2 production preincubated for 10 mins | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID464514 | Selectivity for human HepG2 cells over human HMEC | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID181831 | Compound was evaluated in developing adjuvant arthritis model rats for its effect on paw edema. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID176483 | Compound administered perorally for inhibition of carrageenan induced paw edema after 3h in rat | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | 2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents. |
AID1357042 | Inhibition of COX1 in human whole blood assessed as A23187-stimulated TxB2 production at 1 uM pre-incubated for 60 mins before A23187 addition and measured after 30 mins by ELISA (Rvb = 2 ng/ml) | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID113300 | Dose required for the inhibition of phenylquinone-induced writhing in male mice | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids. |
AID172638 | Analgesic activity was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 4 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1473958 | Ratio of drug concentration at steady state in human at 25 to 50 mg, po TID after 8 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1689632 | Inhibition of human COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID1667494 | Anti-inflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 uM/kg, ip measured at 0.5 hrs by calliper method relative to control | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1165101 | Antiinflammatory activity in mouse assessed as reduction in PMA-induced ear edema at 3 mg/ear administered topically relative to control | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Synthesis and evaluation of anti-inflammatory activity of derivatives of the marine natural products fuscol and eunicol. |
AID260554 | Increase in paw weight in Fischer rats at 300 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties. |
AID748518 | Inhibition of mouse COX2 Y355F mutant using [1-14C]-arachidonic acid as substrate up to 100 uM incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1437460 | Ulcerogenic effect in albino rat assessed as ulcer index at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose | |||
AID1403471 | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study. |
AID502272 | Inhibition of sheep COX1 at 10 uM by enzyme immunoassay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors. |
AID1426406 | Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as leucocytic infiltration in sub mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID1241869 | Renal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as histological changes at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 by hematoxylin and | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID482172 | Partition coefficient, log P at 5 mM by reverse phase HPLC analysis | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | 1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A(2)alpha with reduced lipophilicity: synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activity. |
AID1195153 | Inhibition of human recombinant COX-2 using PGH2 as substrate incubated for 10 mins prior to arachidonic acid addition measured after 2 mins by EIA | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID664543 | Inhibition of human recombinant GST-tagged AKR1C4 expressed in Escherichia coli using S-tetralol as substrate by fluorometry | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4 | Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. |
AID356060 | Antiinflammatory activity against Swiss mouse chronic dermatitis model assessed as inhibition of TPA-induced tissue myeloperoxidase activity at 0.5 mg/ear applied twice daily for 4 days measured after 6 hrs relative to control | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID1576172 | Ulcerogenic activity in rat assessed as average number of ulcers formed at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID177532 | In vivo inhibitory activity against carrageenan induced paw edema in the rat. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
AID177358 | In vivo inhibition of adjuvant arthritis in rats | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID464325 | Cytotoxicity against HEK293 cells after 72 hrs by luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID176984 | In vivo antiinflammatory activity by the Carrageenan-induced rat paw edema assay. | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
AID591440 | Antiarthritic activity in heat-killed mycobacterium tuberculosis-induced Lewis rat arthritis model assessed as decrease in arthritic score at 50 mg/kg, po QD for 28 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID1542912 | Antiproliferative activity against human VCaP cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID132250 | Effective dose to inhibit 50% of mouse arachidonic acid induced ear edema assay | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity. |
AID1330204 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 24 hrs before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID688471 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as dermal swelling at 0.4 umol administered topically per cm'2 of ear after 9 hrs of post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID679614 | TP_TRANSPORTER: inhibition of Daunorubicin, LDS-751 and Rhodamine 123 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID1568921 | Inhibition of COX-2 in ASA treated human whole blood assessed as reduction in LPS-stimulated prostaglandin E2 production by measuring prostaglandin E2 level at 1 uM preincubated for 15 mins followed by LPS stimulation and measured after 18 hrs by ELISA (R | |||
AID492324 | Inhibition of Pgp expressed in mouse L5178Y cells at 10 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators. |
AID1217727 | Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1333293 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 50 mg/Kg, po administered 30 mins before carrageenan challenge measured after 1 hr relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents. |
AID1689627 | Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 2 hr by plethysmometer analysis relative to control (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID440889 | Toxicity in Fisher 344 rat assessed as mortality at 0.01 mmol/kg, ip administered daily once for 4 days measured after 24 hrs final post dose | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins. |
AID703840 | Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX. |
AID1852376 | Anti-inflammatory activity in rat H9c2 cells assessed as inhibition of endogenous IL-6 protein expression in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by DAPI staining based immunofluores | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID751124 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip measured at 2 hrs by plethysmometric analysis relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID177369 | ED50 measured by hyperalgesia assay | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID1783309 | Ulcerogenic activity in fasted albino rat assessed as ulcer index at 28 uM/kg, po administered for 3 consecutive days (Rvb = 0 No_unit) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID1134831 | Inhibition of prostaglandin synthetase (unknown origin) | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | 2-(Substituted phenyl)oxazolo[4,5-b]pyridines and 2-(substituted phenyl)oxazolo[5,4-b]pyridines as nonacidic antiinflammatory agents. |
AID328209 | Induction of gastric ulcer formation in Sprague-Dawley rat at 10 mg/kg, po after 5 hrs | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID1891747 | Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl-2 expression measured after 24 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID184175 | In vivo anti-inflammatory activity against carrageenan-induced paw edema assay in rats at dose 0.11 mM/kg | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Synthesis, in vitro cytotoxicity and in vivo anti-inflammatory activity of long chain 3-amino-1,2-diols. |
AID328104 | Antiinflammatory activity against corton oil-induced ear edema in mouse | 2008 | Journal of natural products, Feb, Volume: 71, Issue:2 | Isoprenoid glycosides from Liriosma ovata. |
AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID162643 | Inhibitory activity against Prostaglandin G/H synthase 2 | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
AID464518 | Selectivity for human Raji cells over human HMEC | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1576166 | Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 3 hrs relative to control | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID400235 | Antiinflammatory activity against carrageenan-induced paw edema in Wistar rat at 5 mg/kg, po | 2004 | Journal of natural products, Mar, Volume: 67, Issue:3 | New compounds from an extract of Vernonia colorata leaves with anti-inflammatory activity. |
AID401492 | Inhibition of PMA-induced ear edema in Swiss mouse at 3 mg/ear after 1 hr | 1997 | Journal of natural products, Feb, Volume: 60, Issue:2 | Isolation of two flavonoids from Tanacetum microphyllum as PMA-induced ear edema inhibitors. |
AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID409564 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema volume at 10 mg/kg, po administered 60 mins before carrageenan challenge after 4 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1131130 | Antiinflammatory activity against adjuvant-induced arthritis rat model assessed as inhibition of swelling at 0.5 mg/kg, po measured on day 21 (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Potential antiarthritic agents. 2. Benzoylacetonitriles and beta-aminocinnamonitriles. |
AID384264 | Inhibition of arachidonic acid-induced platelet aggregation in human blood after 3 mins by turbidimetric assay | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs. |
AID1128712 | Antioxidant activity in rat liver microsome membrane assessed as inhibition of lipid peroxidation after 45 mins by TBARS-based spectrophotometric assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID763523 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 30 mins prior to carrageenan challenge measured at 4 hrs by plethysmometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID1303387 | Inhibition of bovine testis hyaluronidase using hyaluronic acid as substrate preincubated with CaCl2 for 20 mins followed by incubation with compound for 20 mins and substrate for 10 mins by colorimetric Morgan-Elson method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Interpreting the behavior of concentration-response curves of hyaluronidase inhibitors under DMSO-perturbed assay conditions. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID173702 | Percent decrease in serum haemoglobin evaluated in a developing adjuvant arthritis model rats; No significant effect | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID178471 | Antiinflammatory activity evaluated as Minimum effective oral dose that inhibits bradykinin paw edema in rat | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID184187 | In vivo effect on prostaglandin and leukotriene mediated production in rat pleural cavity was assessed by the inhibition of LTE4 in 5-lipoxygenase/ cyclooxygenase at dose 1.0 mg/kg | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents. |
AID1195154 | Selectivity ratio of IC50 for ovine recombinant COX-1 to IC50 for human recombinant COX-2 | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID699542 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID478749 | Antiinflammatory activity against carrageenan-induced paw edema in po dosed rat administered 1 hr before carrageenan challenge assessed after 2 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis of 3-((2,4-dichlorophenoxy)methyl)-1,2,4-triazolo(thiadiazoles and thiadiazines) as anti-inflammatory and molluscicidal agents. |
AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1557571 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent-based assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. |
AID1503671 | Inhibition of human COX-1 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by thin layer chromatographic method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID1891739 | Induction of mitochondrial outer membrane damage in human MCF7 cells assessed as increase in mitochondrial depolarization by measuring increase in green fluorescence measured after 24 hrs by JC1 dye based confocal microscopy | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID1557575 | Cytotoxicity against LPS-induced mouse RAW264.7 cells assessed as reduction in cell viability | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. |
AID1730822 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 40 uM measured after 24 hrs by MTT assay relative to control | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice. |
AID1557574 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. |
AID1143904 | Inhibition of purified ovine COX1 assessed as residual activity preincubated at 10 uM for 5 mins by HPLC analysis | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase. |
AID1253840 | Inhibition of ovine COX-2 using arachidonic acid after 5 mins by colorimetric method | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties. |
AID326234 | Analgesic activity against sodium chloride-induced abdominal constriction in rat at 84 umol/kg, po after 60 mins | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Second-generation aspirin and indomethacin prodrugs possessing an O(2)-(acetoxymethyl)-1-(2-carboxypyrrolidin-1-yl)diazenium-1,2-diolate nitric oxide donor moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID1199420 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs (Rvb = 1.68 +/- 0.029 ml) | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID213140 | Inhibition of PGE-2 synthesis in bovine platelet suspension | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | 1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase. |
AID128886 | Percent analgesia in phenylquinone writhing assay at 0.3 mg/kg | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID161308 | Inhibitory activity against Prostaglandin G/H synthase | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid. |
AID304224 | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID77819 | Inhibition of Collagen-induced Thromboxane (TXB2) generation in guinea pig whole blood ex vivo by oral 10 mg/kg administration of test compound. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids. |
AID240796 | In vitro inhibitory concentration against COX-2 enzyme | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID591629 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs by plethysmograph relative to control | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID183089 | Inhibition of adjuvant-induced arthritis (AA) in SD rats upon peroral administration (BID) at 0.3 mg/kg/day | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | A prodrug approach to COX-2 inhibitors with methylsulfone. |
AID222769 | Inhibition of platelet aggregation induced by arachidonic acid(AA) in human platelet-rich plasma | 1988 | Journal of medicinal chemistry, May, Volume: 31, Issue:5 | Synthesis and pharmacological evaluation of 5,6-exo-epoxy-7-oxabicyclo[2.2.1]heptane derivatives. |
AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1204221 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 1 hr relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID188069 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 0.3 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 23rd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID303595 | Antiarthritic activity against adjuvant-induced arthritis in Wistar rat assessed as weight change at 10 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1783300 | Analgesic activity against p-benzoquinone induced writhing in albino rat model assessed as protection rate at 28 uM/kg, ip measured after 30 mins relative to indomethacin | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID188081 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 3 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 23rd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID136448 | Compound was evaluated for the percent reduction of carrageenan induced edema in mice at dose of 1.0 mg/kg | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID332631 | Antiinflammatory activity in Swiss mouse assessed as inhibition of 12-O-tetradecanoylphorbol acetate-induced ear edema at 0.5 mg/ear administered tropically | 1995 | Journal of natural products, Jan, Volume: 58, Issue:1 | Anti-inflammatory activity of saikosaponins from Heteromorpha trifoliata. |
AID1884335 | Inhibition of LPS induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent based assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis. |
AID680599 | TP_TRANSPORTER: increase in Etoposide intracellular accumulation (Etoposide: 2 uM, Indomethacin: 500 uM) in MRP3-expressing fibroblast from kidney of mdr1a/1b and mrp1 (-/-) mouse | 2001 | The Journal of biological chemistry, Dec-07, Volume: 276, Issue:49 | Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3). |
AID1529186 | Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID373867 | Hepatic clearance in human hepatocytes in absence of fetal calf serum | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | First-principle, structure-based prediction of hepatic metabolic clearance values in human. |
AID177018 | Antiinflammatory activity was evaluated in rat carrageenan foot edema assay in experiment 1 | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID7812 | In vitro rate of absorption observed as Caco-2 permeability in humans | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1150267 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of adjuvant-induced arthritis at 0.5 mg/kg, po administered for 14 days followed by adjuvant challenge relative to control | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID1156827 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID176214 | Effective dose was determined in vivo in male Dawley rats by rat carrageenan-induced hyperalgesia assay | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9 | Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). |
AID701949 | Inhibition of ovine COX2 by colorimetric assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity. |
AID1188643 | Antiinflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced NO production treated 2 hrs before LPS challenge measured after 20 hrs | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | Weakly anti-inflammatory limonoids from the seeds of Xylocarpus rumphii. |
AID1195148 | Analgesic activity in Swiss albino mouse assessed as time of licking paws at 50 mg/kg, po measured after 2 hrs by tail flick test relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID1336953 | Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G2 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.08%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID475505 | Binding affinity to amyloid beta (1 to 42) oligomers by change in fluorescence at 100 uM after 10 mins | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta. |
AID162636 | Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines. |
AID444054 | Oral bioavailability in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1503675 | In vivo inhibition of rat COX-2 assessed as decrease in plasma PGE2 level by EIA relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID1737623 | Analgesic activity in albino mouse assessed as forepaw licking/jumping latency time at 10 mg/kg, ip measured after 60 mins by hot plate test (Rvb = 3.42 +/- 0.03 sec) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID133223 | Percentage inhibition of the mouse arachidonic acid induced ear edema assay (AA) at a dose of 100 ug/ear | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity. |
AID189411 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 12 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1402009 | Antiinflammatory activity in carrageenan-induced paw edema Fisher 344 rat model assessed as protection against carrageenan-induced edema at 0.01 mmol/kg, ip administered simultaneously with carrageenan measured at 3.5 hrs post carrageenan injection relati | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Quinoxaline: An insight into the recent pharmacological advances. |
AID430148 | Antiinflammatory activity against bradykinin-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before bradykinin challenge measured after 240 mins by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID1353377 | Inhibition of serum COX2 level in Swiss mouse model of carragenan-induced paw edema at 100 mM/kg, po pretreated for 1 hr followed by carrageenan treatment measured after 3 hrs by ELISA | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
AID703401 | Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID449632 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po after 2 hrs relative to control | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines. |
AID688453 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 1 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID162632 | Inhibition activity against recombinant human Prostaglandin G/H synthase 2 | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5 | Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. |
AID24263 | Ability to undergo in vitro ester hydrolysis in 80% human plasma ( pH of 7.4) at 37 degree Celsius expressed as half life of N,N-diethylglycolamide ester hydrolysis | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents. |
AID1172864 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors. |
AID178919 | Effective dose required for antiinflammatory activity by rat paw hyperalgesia assay tested in vivo | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID172636 | Analgesic activity was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 1 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID464326 | Cytotoxicity against human Raji cells after 72 hrs by luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1055831 | Antinociceptive activity in albino Wistar rat assessed as thermal-stimulus induced tail flick latency at 0.05 mmol/kg, po after 30 mins (Rvb = 2.22 +/- 0.20 mins) | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID614601 | Inhibition of ovine COX-1 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | SAR studies of acidic dual γ-secretase/PPARγ modulators. |
AID678490 | Inhibition of COX2 peroxidase activity assessed as formation of TMPD at 100 uM by colorimetric analysis | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Synthesis, biological evaluation, and docking studies of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines as potent anti-inflammatory and antioxidant agents. |
AID223721 | Activity against arthritis on adjuvant-untreated paw in rats at 1 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID170869 | Percent changes of hind paw edema and severity scores compared to control animals at 7.0 micro mol/kg/day | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID1319557 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | New labdane diterpenoids from Croton laui and their anti-inflammatory activities. |
AID648861 | Inhibition of ovine COX1 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs. |
AID1330199 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 1 hr before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID186127 | Radiographic change was judged in the area of the talus joint, using an arbitrary scoring system upon termination of the test (14 days dosing of 1 mg/kg) in a model of type II collagen arthritis in the rat. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID420033 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID579633 | Antiinflammatory activity against human neutrophil assessed as inhibition of N-formyl-l-methionyl phenylalanine/cytochalasin B-induced elastase release | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl-β-carboline and 1-benzoyl-3-carboxy-β-carboline derivatives. |
AID688466 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as reduction in vascular changes at 0.4 umol administered topically per cm'2 of ear measured after 6 hrs post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID681023 | TP_TRANSPORTER: inhibition of PAH uptake (PAH: 20 uM, Indomethacin: 1000 uM) in OAT-expressing COS-7 cells | 1999 | The Journal of biological chemistry, Jan-15, Volume: 274, Issue:3 | Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells. |
AID1055540 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr by plethysmometer | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, biological evaluation and molecular modeling study of 5-trifluoromethyl-Δ²-pyrazoline and isomeric 5/3-trifluoromethylpyrazole derivatives as anti-inflammatory agents. |
AID748509 | Binding affinity to wild type human COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID287610 | Antiinflammatory activity in Wistar Albino rat assessed as inhibition of carrageenan-induced paw oedema at 5 mg/kg, ip after 4 hrs | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID678721 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID165495 | In vitro of platelet aggregation of citreated rabbit platelet-rich plasma, induced by arachidonic acid at 200 uM | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID224212 | Inhibitory activity against IL-1 on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID1455833 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition carrageenan-induced paw edema at 5 mg/kg, ip pretreated for 15 mins followed by carrageenan challenge measured at 1 hr post carrageenan challenge | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
AID548101 | Inhibition of soybean lipoxygenase at 100 uM by UV spectrophotometry | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives. |
AID399401 | Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID1203979 | Anti-inflammatory activity in ICR mouse model of carrageenan-induced edema assessed as inhibition of paw thickness at 10 mg/kg, ip | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. |
AID1136456 | Antitumor activity against mouse P388 cells allografted in DBA/2 mouse assessed as host survival on day 7 at 20 mg/kg, ip qd for 2 weeks | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids. |
AID648868 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, po after 3 hrs relative to control | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs. |
AID1891746 | Induction of apoptosis in human MCF7 cells assessed as increase in red fluorescence at IC50 measured after 24 hrs by propidium iodide staining based confocal laser scanning microscopy | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID1336926 | Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID688467 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as reduction in cellular changes at 0.4 umol administered topically per cm'2 of ear measured after 6 hrs post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1441591 | Antiinflammatory activity in arachidonic acid-induced ear dermatitis ICR mouse model assessed as reduction in ear swelling at 0.1 mg administered twice tropically 30 mins prior and 15 mins after arachidonic acid addition measured 60 mins post arachidonic | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID185775 | Percentage dose required to prevent lesion formation in gastric mucosa of unanesthetized rats upon intraperitoneal administration of 3 mg/kg dose in the HCl/ethanol-induced lesion model | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | Novel angucycline compound with both antigastrin- and gastric mucosal protective-activities. |
AID1171126 | Antinociceptive activity in Swiss Webster mouse assessed as inhibition of formalin-induced late phase pain response at 10 mg/kg, ip dosed 40 mins before formalin injection | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Antinociceptive properties of physalins from Physalis angulata. |
AID91335 | Inhibitory activity against elastase release by human neutrophils | 1995 | Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14 | Synthesis and pharmacological evaluation of 2'-hydroxychalcones and flavones as inhibitors of inflammatory mediators generation. |
AID1392322 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 125 mg/kg, po measured at 2 hrs relative to control | |||
AID286231 | Inhibition of human platelet COX1 by EIA assay | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1180074 | Inhibition of ovine COX1 using arachidonic acid substrate assessed as PGE2 production ELISA method after 2 mins | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pharmacological evaluation and docking studies of α,β-unsaturated carbonyl based synthetic compounds as inhibitors of secretory phospholipase A₂, cyclooxygenases, lipoxygenase and proinflammatory cytokines. |
AID1505050 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by griess assay | 2018 | Journal of natural products, 01-26, Volume: 81, Issue:1 | Rearranged Phloroglucinol-Monoterpenoid Adducts from Callistemon rigidus. |
AID187756 | Antiinflammatory activity evaluated by measuring % reduction of edema, 3h after oral administration of 1 mg/kg in carrageenan model | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID393850 | Gastrointestinal toxicity in albino rat assessed as ulcer index at 10 mg/kg, po after 6 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. |
AID486185 | Gastrointestinal toxicity in Wistar rat assessed as ulcerogenic effect at 9 mg/kg, po after 7 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis, biological evaluation and molecular docking of novel series of spiro [(2H,3H) quinazoline-2,1'- cyclohexan]-4(1H)- one derivatives as anti-inflammatory and analgesic agents. |
AID178669 | Antiinflammatory activity was determined to inhibit cotton pellet granuloma in rats with respcet to Indomethacin | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds. |
AID186449 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 10 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID313121 | Inhibition of mouse COX2 V349L mutant | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Structural and functional basis of cyclooxygenase inhibition. |
AID386959 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat at 10 mg/kg, ip administered 1 hr before inflammation induction assessed after 3 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Facile synthesis of dithiatetraaza-macrocycles of potential anti-inflammatory activity. |
AID724085 | Inhibition of ovine COX1 peroxidase activity assessed as appearance of oxidized N,N,N,N'-tetramethyl-p-phenylenediamine by colorimetric analysis relative to control | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Design, synthesis, characterization and biological evaluation of novel pyrazole integrated benzophenones. |
AID587454 | Ulcerogenic activity in 12 fasting Sprague-Dawley rat assessed as ulcer index at 80 umol/kg, po measured after 6 hrs by magnifier lenses | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies. |
AID1409608 | AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID393849 | Toxicity in ip dosed albino mouse assessed as mortality after 24 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. |
AID707118 | Hepatotoxicity in Swiss mouse assessed as change in plasma AST level at 2.5 mg/kg, po for 7 days measured over 7 days relative to vehicle-treated control | 2012 | Journal of natural products, May-25, Volume: 75, Issue:5 | Kaurenoic acid from Sphagneticola trilobata Inhibits Inflammatory Pain: effect on cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID1357043 | Inhibition of COX2 in human whole blood assessed as LPS-stimulated PGE2 production at 1 uM pre-incubated for 15 mins before LPSaddition and measured after 18 hrs by ELISA (Rvb = 1.98 ng/ml) | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID1125124 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 1 hr relative to control | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID1125137 | Inhibition of ovine COX1 assessed as prostaglandin F2alpha level | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID1192211 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat assessed as edema volume at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 4 hrs (Rvb = 1.88 +/- 0.20 mL) | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID1464290 | Inhibition of ovine COX1 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | |||
AID1359536 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as hind paw thickness at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 3 hrs by caliper method (Rvb = 8.45 +/- 0.64 millime | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID618603 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 1 hr by plethysmograph | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, pharmacological evaluation and docking studies of coumarin derivatives. |
AID183643 | Antiinflammatory activity was evaluated by the inhibition of rat carrageenan foot edema (CFE) assay at the dose of 10 mg/kg | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. |
AID1220557 | Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1568917 | Inhibition of ovine COX-1 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method | |||
AID729257 | Selectivity ratio of IC50 for human recombinant AKR1C2 to IC50 for human recombinant AKR1C3 | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID399406 | Selectivity ratio of IC50 for sheep placental cotyledons COX2 to IC50 for bovine seminal microsomal COX1 preincubated for 10 mins | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID604021 | Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID748512 | Inhibition of wild type human COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analys | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID404568 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced edema at 50 mg/kg, po after 4 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID1145138 | Gastrointestinal toxicity in 8 hrs starved po dosed Charles River rat assessed as ulcerogenic effect after 18 hrs | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1, 3, 4, 9-tetrahydropyrano[3, 4-b]indole-1-acetic acids. |
AID162665 | Tested for inhibition against Prostaglandin G/H synthase 2 | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors. |
AID396345 | Antiinflammatory activity against cotton pellets-induced inflammation in Wistar rat assessed as wet weight of granuloma at 5 mg/kg, po after 7 days | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and anti-inflammatory activity evaluation of unsymmetrical selenides. |
AID192162 | Weight change of rat was determined; + = significant increase in weight change from control | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents. |
AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1852425 | Antiinflammatory activity against LPS/talc powder induced pericarditic Wistar rat assessed as elimination of pericardial effusion at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-oxo- | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID698889 | Growth inhibition of human NCI60 cells incubated for 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Mechanism inspired development of rationally designed dihydrofolate reductase inhibitors as anticancer agents. |
AID1195043 | Antiinflammatory activity in CD-1 mouse ear edema model assessed as reduction in TPA-induced edema size at 2 mg/ear, topically administered 30 mins prior to TPA-challenge measured after 6 hrs relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis, antinociceptive and anti-inflammatory effects of porphyrins. |
AID392748 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip after 3.5 hrs | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | Synthesis of hydroxycoumarins and hydroxybenzo[f]- or [h]coumarins as lipid peroxidation inhibitors. |
AID393658 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat assessed as inhibition of edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured after 1 hr relative to control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Regioselective synthesis of dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones of potential anti-tumor properties. |
AID453646 | Antiinflammatory activity in CD1 mouse assessed as inhibition of carrageenan-induced paw edema at 5 mg/kg, ip administered 30 mins before carrageenan challenge relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID1336952 | Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at S phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 27.1%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID304240 | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 0.1 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID666600 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 22 hrs by Griess method relative to untreated control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. |
AID1128739 | In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in triglyceride level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1810796 | Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, ip administered 30 mins prior to acetic acid challenge and measured after 30 mins relative to control | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID190376 | Concentration at which gastric damage will occur was determined in rat | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9 | Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). |
AID1416193 | Anti-inflammatory activity in human RBC assessed as inhibition of hypotonic solution-induced hemolysis after 10 mins by spectrophotometric method | |||
AID1464068 | Ulcerogenic activity in Wistar albino rat assessed as abdominal perforation in stomach after 48 hrs by hematoxylin and eosin staining based microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids. |
AID1695482 | Antiinflammatory activity in ICR mouse model of carrageenan-induced paw edema assessed as paw edema inhibition rate at 22 mg/kg, po pretreated with compound followed by carrageenan challenge and measured after 4 hrs post-treatment by dial thickness gage | 2020 | RSC medicinal chemistry, Jul-01, Volume: 11, Issue:7 | A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception. |
AID186594 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 10 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1667502 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured at 2 hrs by calliper method (Rvb = 7.67 +/- 0.17 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1131124 | Antiinflammatory activity against adjuvant-induced arthritis rat model assessed as inhibition of swelling at 0.5 mg/kg, po measured on day 14 (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Potential antiarthritic agents. 2. Benzoylacetonitriles and beta-aminocinnamonitriles. |
AID1568739 | Anti-inflammatory activity in rat assessed as inhibition of formalin-induced paw edema at 20 mg/kg, po pretreated for 1 hr followed by formalin addition measured up to 6 hrs relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Medicinal prospects of antioxidants: A review. |
AID1568922 | Analgesic activity in Wistar rat model of formalin-induced hyperalgesia assessed as reduction in number of formalin-evoked paw flinching during inflammatory phase at 10 mg/kg preincubated for 30 mins followed by formalin treatment and measured after 15 to | |||
AID446961 | Antiinflammatory activity in BALB/c mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po after 90 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of 3,6-disubstituted 7H-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines as novel analgesic/anti-inflammatory compounds. |
AID748527 | Inhibition of wild type ovine COX1 expressed in ram seminal vesicles using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographi | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1545123 | Toxicity in mouse RAW264.7 cells assessed as cell viability at 10 uM by MTT assay | 2019 | Journal of natural products, 08-23, Volume: 82, Issue:8 | Antibacterial and Inhibitory Activities against Nitric Oxide Production of Coumaronochromones and Prenylated Isoflavones from |
AID1136451 | Antiinflammatory activity in CF1 mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 3 hrs and 30 mins prior to carrageenan-challenge measured after 3 hrs (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids. |
AID1712477 | Inhibition of LPS-induced NO production in mouse RAW264.7 cells incubated for 24 hrs by Griess reagent based assay | 2016 | Journal of natural products, 06-24, Volume: 79, Issue:6 | Sesquiterpenes from Inula japonica with Inhibitory Effects on Nitric Oxide Production in Murine Macrophage RAW 264.7 Cells. |
AID1171120 | Antinociceptive activity in Swiss Webster mouse assessed as inhibition of acetic acid-induced abdominal constrictions at 10 mg/kg, ip dosed 40 mins before acetic acid injection | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Antinociceptive properties of physalins from Physalis angulata. |
AID112732 | Antiinflammatory activity, administered ip at 150 uM/kg dose was determined against carrageenan-induced mice paw edema model | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID680473 | TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.1 uM, Indomethacin: 1000 uM) in Oatp1-expressing LLC-PK1 cells | 2002 | Pharmaceutical research, Feb, Volume: 19, Issue:2 | Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. |
AID481239 | Ratio of ED50 for BALB/c mouse collagen antibody induced arthritis model to tolerated dose for BALB/c mouse collagen antibody induced arthritis model | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III. |
AID1441589 | Antiinflammatory activity in arachidonic acid-induced ear dermatitis ICR mouse model assessed as reduction in ear swelling at 3 mg administered tropically 30 mins prior and 15 min after arachidonic acid addition measured 60 mins post arachidonic acid chal | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID1174277 | Inhibition of ovine COX2 using arachidonic acid substrate incubated for 5 mins by colorimetry | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents. |
AID1175392 | Inhibition of human TRPV1 overexpressed in BEAS-2B cells assessed as residual activity at 50 uM after 30 mins by Fluo-4 AM fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates. |
AID355097 | Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced PGE2 release by Ellman's method | 1996 | Journal of natural products, Dec, Volume: 59, Issue:12 | Antiinflammatory activity of coumarins from Santolina oblongifolia. |
AID1675153 | Anti-inflammatory activity in human HaCaT cells assessed as inhibition of LPS-induced TNF-alpha production at 10 uM after 24 hrs by ELISA relative to LPS alone | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Labdane-Type Diterpenes from the Aerial Parts of |
AID326233 | Analgesic activity against sodium chloride-induced abdominal constriction in rat at 84 umol/kg, po after 30 mins | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Second-generation aspirin and indomethacin prodrugs possessing an O(2)-(acetoxymethyl)-1-(2-carboxypyrrolidin-1-yl)diazenium-1,2-diolate nitric oxide donor moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID117413 | Gastric ulcerogenic activity at a dose of 10 mg/kg | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID322002 | Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 10 mg/kg, po after 1 hr | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones. |
AID1220554 | Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID54559 | In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22 | A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors. |
AID755664 | Cytotoxicity against mouse BV2 cells assessed as maximum non-toxic concentration after 24 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | New eudesmane sesquiterpenes from Alpinia oxyphylla and determination of their inhibitory effects on microglia. |
AID179690 | Acute gastric toxicity (single oral dose) in male fasted rats | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID1359985 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 1 hr by plethysmometer relative to control | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent. |
AID1543430 | Antiinflammatory activity in ICR mouse assessed as inhibition of TPA-induced ear edema by measuring reduction in weight of ear punches up to 1.25 mg/ear applied topically measured 4 hrs post TPA-challenge relative to control | |||
AID1241870 | Analgesic activity in Swiss albino mouse assessed as reduction in number of writhing episodes at 10 mg/kg, po measured 30 mins following acetic acid injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1156828 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID1134828 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced foot edema | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | 2-(Substituted phenyl)oxazolo[4,5-b]pyridines and 2-(substituted phenyl)oxazolo[5,4-b]pyridines as nonacidic antiinflammatory agents. |
AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID642874 | Inhibition of COX1 at 100 uM | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity. |
AID389444 | Antiinflammatory activity against carrageenan-induced paw edema in ICR mouse at 4 mg/kg, ip administered 30 mins before carrageenan challenge assessed after 1 hr | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Anti-inflammatory activities of furanoditerpenoids and other constituents from Fibraurea tinctoria. |
AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID371495 | Antiinflammatory activity against carrageenan-induced paw edema in Wistar rat at 10 mg/kg, po dose administered 1 hr before carrageenan challenge assessed after 3 hrs | 2008 | European journal of medicinal chemistry, Aug, Volume: 43, Issue:8 | 1,8-Naphthyridines VII. New substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity. |
AID173359 | Hypolipidemic action at 500 uM/kg was determined as reduction in low density lipoprotein in rat plasma | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID158620 | Inhibitory activity against phospholipase A2 of Croatalus adamanteus | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
AID502275 | Selectivity index, ratio of IC50 for sheep COX1 to IC50 for sheep COX2 | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors. |
AID187424 | Reaction time in Hot plate test at a dose of 5 mg/kg perorally in rats after 120 min (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID288821 | Inhibition of ovine COX1 by enzyme immuno assay | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies. |
AID618605 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs by plethysmograph | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, pharmacological evaluation and docking studies of coumarin derivatives. |
AID190359 | Compound was tested for intestinal Ulcerogenic effect in rats, activity expressed as ulcer incidence | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents. |
AID227084 | Relative binding affinity to 5-lipoxygenase and cyclooxygenase | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase. |
AID1743652 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID169230 | In vivo oral activity by air pouch assay on Sprague-Dawley rats at dose 2 mg/kg administered intragastrically in a volume of 5 mL/kg 2 hr prior to injection. | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9 | Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. |
AID1128732 | Inhibition of bovine COX-1 assessed as PGF2-alpha formation using arachidonic acid as substrate at 20 uM by enzyme immunoassay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1333294 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw oedema at 50 mg/Kg, po administered 30 mins before carrageenan challenge measured after 2 hrs relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents. |
AID1519097 | Antiinflammatory activity against albino rats assessed as inhibition of carrageenan-induced paw edema at 15 mg/kg, po measured after 4 hrs relative to control | |||
AID397001 | Gastrointestinal toxicity in fasted albino rat assessed ulcer index at 10 mg/kg, po administered for 3 days measured after 1 hr of last dose | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Facile synthesis of bis(4,5-dihydro-1H-pyrazole-1-carboxamides) and their thio-analogues of potential PGE(2) inhibitory properties. |
AID641291 | Antiinflammatory activity in ICR mouse assessed as decrease in carrageenan-induced serum NO level at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID729251 | Selectivity ratio of IC50 for COX1 (unknown origin) to IC50 for human recombinant AKR1C3 | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID1667499 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured immediately by calliper method (Rvb = 6.83 +/-0.17 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1162913 | Acute gastrolesivity in Wistar rat assessed as stomach lesions at 10 mg/kg, po measured after 5 hrs | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | 1,8-Naphthyridines IX. Potent anti-inflammatory and/or analgesic activity of a new group of substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides, of some their Mannich base derivatives and of one novel substituted 5-amino-10-oxo-10H- |
AID1409607 | IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells). | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID182298 | Compound was evaluated for its antiinflammatory activity by adjuvant-induced polyarthritis test in rats at a dosage of 1 mg/kg administered orally | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID1565361 | Ulcerogenicity in Sprague-Dawley rat assessed as formation of ulcer at 20 mg/kg, po after 1 hr by microscopic analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities. |
AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID598527 | 1-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design. |
AID205268 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
AID448128 | Antinociceptive activity in po dosed mouse assessed as inhibition of acetic acid-induced abdominal constrictions | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH). |
AID180549 | The compound was tested in vivo for activity against yeast -induced hyperalgesia in rat after peroral administration | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID305968 | Anticoagulant activity assessed as inhibition of arachidonic acid induced rabbit platelet aggregation | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents. |
AID1055825 | Ulcerogenicity in albino Wistar rat assessed as gastric muscular layer damage at 0.15 mmol/kg, po by hematoxylin and eosin staining-based assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID675145 | Analgesic activity in Albino rat assessed as reaction time at 10 mg/kg, po after 2 hrs by Hot plate test | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
AID1209585 | Drug uptake in Sprague-Dawley rat brain slices in presence of 50 nM of monensin | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID1852355 | Protection against LPS/hypoxia induced apoptosis in rat H9c2 cells assessed as reduction in green fluorescence in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by confocal microscopy analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID322003 | Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 10 mg/kg, po after 2 hrs | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones. |
AID747930 | Inhibition of COX-1 in human washed platelet assessed as inhibition of 0.5 uM arachidonic acid-induced TXB2 formation at 0.01 to 100 uM incubated for 25 mins prior to arachidonic acid challenge measured after 30 mins by radioimmunoassay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID1242113 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs by plethysmometric analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Molecular docking design and one-pot expeditious synthesis of novel 2,5-diarylpyrazolo[1,5-a]pyrimidin-7-amines as anti-inflammatory agents. |
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AID381056 | Activation of GAL4 fused human PPARgamma ligand binding domain transfected in african green monkey CV1 cells by CAT reporter assay | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4 | Bioassay for the identification of natural product-based activators of peroxisome proliferator-activated receptor-gamma (PPARgamma): the marine sponge metabolite psammaplin A activates PPARgamma and induces apoptosis in human breast tumor cells. |
AID52139 | Inhibitory activity against prostaglandin biosynthesis in stimulated chondrocyte cell culture | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Structure-activity relationships among analogues of pemedolac, cis-1-ethyl-1,3,4,9-tetrahydro-4-(phenylmethyl)pyrano[3,4-b]indo le-1-a cetic acid, a potent analgesic agent. |
AID1241823 | Anti-inflammatory activity in rat model of acute inflammation assessed as inhibition of carrageenan-induced paw oedema dosed at 10 mg/kg, po dosed 1 hr before carrageenan injection and measured 4 hrs after carrageenan injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID271286 | Inhibition of ovine COX1 | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID115722 | The compound was evaluated for inhibition of edema induced by arachidonic acid at 1 mg/mL | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID1784595 | Antiinflammatory activity in human HBE cells assessed as inhibition of LPS-induced IL-6 production at 5 uM pretreated with compound for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury. |
AID492867 | Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity. |
AID1153377 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema measured as paw thickness at 0.03 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 6 hrs (Rvb = 1.081 +/- 0.257 mm) | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13 | Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties. |
AID184310 | Compound was evaluated for the inhibition of adjuvant-induced arthritis model in rats at a dose of 1 mg/kg | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID1737609 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hr relative to indomethacin | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
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AID679408 | TP_TRANSPORTER: inhibition of NEM-GS by Indomethacin at a concentration of 100uM in membrane vesicles from MRP6-expressing Sf9 cells | 2002 | The Journal of biological chemistry, May-10, Volume: 277, Issue:19 | Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). |
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AID178777 | Reduction in exudate volume in rat pleural carrageenan test. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | 2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents. |
AID1409052 | Antiinflammatory activity in carrageenan-induced Swiss mouse assessed as paw volume at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 1 hr by plethysmometric method (Rvb = 59.39 +/- 10.59 mL) | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. |
AID1390454 | Antiinflammatory activity in carrageenan-induced BALB/c mouse peritonitis model assessed as reduction in number of neutrophils in peritoneal fluid at 80 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge measured after 4 hrs by hematoxylin an | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Structural design, synthesis and substituent effect of hydrazone-N-acylhydrazones reveal potent immunomodulatory agents. |
AID1426404 | Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 5 hrs relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID91480 | Ability to bind to human serum albumin (HSA) | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Accumulation of drugs by guinea pig isolated atria. Quantitative correlations. |
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AID1195152 | Inhibition of ovine recombinant COX-1 using PGH2 as substrate incubated for 10 mins prior to arachidonic acid addition measured after 2 mins by EIA | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID161014 | In vitro inhibitory activity against polymorphonuclear leukocyte Prostaglandin G/H synthase | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis. |
AID1849925 | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NO production incubated for 2 hrs followed by LPS stimulation measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats. |
AID452088 | Inhibition of PDE1 | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | A new therapeutic approach in Parkinson's disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents. |
AID687440 | Gastric toxicity in Swiss mouse assessed as necrosis index at 10 mg/kg administered as single dose (Rvb = 0 +/- 0 necrosis index) | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Mechanisms involved in the antinociceptive effects of 7-hydroxycoumarin. |
AID675144 | Analgesic activity in Albino rat assessed as reaction time at 10 mg/kg, po after 1 hr by Hot plate test | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
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AID492323 | Inhibition of Pgp expressed in mouse L5178Y cells at 1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators. |
AID1464291 | Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | |||
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AID1832224 | Antinociceptive activity in Swiss Webster mouse model of formalin-induced biphasic nociceptive response assessed as reduction in pain during early phase at 5 mg/kg, ip administered 40 mins before formalin injection and measured after 10 mins post formalin | |||
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AID1172862 | Inhibition of ovine COX1 | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors. |
AID304223 | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID1550478 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 3 hrs post-carrageenan injection (Rvb = 4.79 +/- | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID287011 | Inhibition of LPS-induced TNFalpha secretion in C57BL/6J mouse peritoneal macrophages at 10 uM after 24 hrs | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Glycosides from the stem bark of Fraxinus sieboldiana. |
AID177368 | ED50 measured by CFE assay | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID224062 | Antiinflammatory activity against D-adjuvant arthritis in injected rat paw at the dose of 1.0 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2 | Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents. |
AID592743 | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrate production at 100 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess reagent method relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID1220793 | Ratio of drug level in blood to plasma in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID748506 | Antiinflammatory activity in po dosed Sprague-Dawley rat assessed as reduction of carrageenan-induced paw edema administered 1 hr measured after 2 hrs by plethysmometric analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1542913 | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1353366 | Antinociceptive activity in carrageenan-induced Swiss mouse model of mechanical hyperalgesia assessed as mechanical hyperalgesic index pretreated orally for 1 hr followed by carrageenan challenge by Von Frey filament assay | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
AID381196 | Inhibition of cyclooxygenase in Wistar rat peritoneal leukocytes at 50 ug/mL | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation. |
AID753753 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po after 3 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1592996 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX2 | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones. |
AID24142 | Gastric toxicity of the compound. | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | 1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: a new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite. |
AID184160 | Compound was evaluated for its antiinflammatory activity in the cotton pellet induced granuloma(CPG) in normal rats at the dose 3 mg/kg p.o. | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID1193882 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Rapid 'one-pot' synthesis of a novel benzimidazole-5-carboxylate and its hydrazone derivatives as potential anti-inflammatory and antimicrobial agents. |
AID287343 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 10 mg/kg, po after 270 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID287294 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 100 mg/kg, po after 270 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID228468 | Chronic therapeutic index as ratio of potency in adjuvant-induced arthritis assay to that of potency in intestinal toxicity assay | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID170141 | Compound was evaluated for its antipyretic activity by antipyresis effect in comparison with that of Aspirin. | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID1131122 | Antiinflammatory activity against adjuvant-induced arthritis rat model assessed as inhibition of swelling at 2 mg/kg, po measured on day 14 (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Potential antiarthritic agents. 2. Benzoylacetonitriles and beta-aminocinnamonitriles. |
AID124989 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 2 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID464511 | Selectivity ratio for IC50 for human BJ cells to IC50 for Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID181446 | Evaluated for the carrageenan-induced paw edema on 11-day after 3.16 mg/kg dose of peroral administration of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents. |
AID547631 | Gastrointestinal toxicity in albino rat assessed as ulcerogenicity at 30 uM/kg, po bid for 3 days measured after 6 hrs of last post dose | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID185333 | Compound was tested for intestinal Ulcerogenic effect in rats, activity expressed as lesion score | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents. |
AID313770 | Inhibition of ovine COX2 at 0.01 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | 1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities. |
AID352495 | Inhibition of ovine COX1 by enzyme immunoassay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: synthesis, biological evaluation and nitric oxide release studies. |
AID189983 | Gastrointestinal tolerability was evaluated under acute conditions, in rats. The ulcerogenic dose was reported. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID680415 | TP_TRANSPORTER: inhibition of glyburide accumulation by indomethacin at a concentration of 200uM in MRP3-expressing MDCK cells | |||
AID1125139 | Selectivity ratio IC50 for ovine COX1 to IC50 for human recombinant COX2 | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID591432 | Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID1510602 | Inhibition of Enterobacter cloacae beta-lactamase incubated for 10 mins followed by nitrocefin substrate challenge and measured for 5 mins by spectrophotometric analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors. |
AID91154 | Compound is evaluated for inhibitory effect on the generation of Leukotriene B4 (LTB4) from human neutrophils; Not active | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID287293 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 100 mg/kg, po after 180 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID420037 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID444052 | Hepatic clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID183650 | Inhibition of carrageenan-induced rat foot oedema following 3 mg/kg administration. | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives. |
AID1125138 | Inhibition of human recombinant COX2 assessed as prostaglandin F2alpha level | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID703842 | Inhibition of ovine COX1 assessed as inhibition of 12-HHT formation measuring remaining activity preincubated at 10 uM for 5 mins before arachidonic acid addition by HPLC analysis | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX. |
AID381058 | Activation of PPARgamma transfected in human MDA-MB-231 cells at 100 to 300 uM after 48 hrs by luciferase reporter gene assay | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4 | Bioassay for the identification of natural product-based activators of peroxisome proliferator-activated receptor-gamma (PPARgamma): the marine sponge metabolite psammaplin A activates PPARgamma and induces apoptosis in human breast tumor cells. |
AID1384639 | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 2 hrs followed by LPS stimulation measured after 24 hrs by Griess reagent based assay | 2018 | Journal of natural products, 08-24, Volume: 81, Issue:8 | Bioactive Sesquiterpenoids from the Peeled Stems of Syringa pinnatifolia. |
AID430042 | Antiinflammatory activity against carrageenan-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before carrageenan challenge measured after 6 hrs by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID1659919 | Analgesic activity in mouse assessed as inhibition of acetic acid-induced writhing at 3 mg/kg, ip relative to control | |||
AID130472 | Carrageenan-induced edema was determined value for oral administration | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID591626 | Gastrointestinal toxicity in Wistar rat assessed as appearance ulcer area of 1 to 3 mm diameter at 100 mg/kg, po administered as single dose after 6 hrs by Vernier caliper | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID1131123 | Antiinflammatory activity against adjuvant-induced arthritis rat model assessed as inhibition of swelling at 1 mg/kg, po measured on day 14 (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Potential antiarthritic agents. 2. Benzoylacetonitriles and beta-aminocinnamonitriles. |
AID753748 | Gastrointestinal toxicity in albino rat assessed as capillary vasodilatation associated with accumulation of edema fluid in lamina propria at 0.28 mmol/kg, po using haematoxylin and eosin staining by light microscopic analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID310932 | Permeability across human Skin | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
AID430048 | Antiinflammatory activity against bradykinin-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before bradykinin challenge measured after 15 mins by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID649080 | Analgesic activity in albino mouse assessed as inhibition of acetic acid-induced abdominal constriction at 100 umol/kg, po administered 1 hr before acetic acid challenge measured after 60 mins relative to control | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives. |
AID193990 | Lesion frequency was measured in rats. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID170138 | Inhibition of carrageenan-induced inflammation of rat paw relative to phenylbutazone. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
AID591628 | Gastrointestinal toxicity in Wistar rat assessed as ulcerogenic index at 100 mg/kg, po administered as single dose | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID699543 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1202782 | Anti-inflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as inhibition of ear edema at 0.1 to 1 umol/ear applied to right ear 10 mins after TPA-stimulation and measured 4 hrs post compound dose | 2015 | Journal of natural products, Feb-27, Volume: 78, Issue:2 | Absolute configuration of labdane diterpenoids from Physalis nicandroides. |
AID177016 | Antiinflammatory activity was determined by inhibition of carrageenan-induced edema in rat paw with respect to phenylbutazone | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds. |
AID313119 | Inhibition of mouse COX2 V349A mutant | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Structural and functional basis of cyclooxygenase inhibition. |
AID427305 | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NO production after 24 hrs by Griess reagent method | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Cytotoxic activity and inhibitory effect on nitric oxide production of triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae). |
AID178915 | Effective dose required for antiinflammatory activity by adjuvant arthritis assay tested in vivo | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID1846816 | Anti-inflammatory activity against carrageenan-induced hind paw edema in rat at 20 mg/kg, PO measured after 5 hrs relative to control | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Contemporary advances of cyclic molecules proposed for inflammation. |
AID492327 | Inhibition of BCRP expressed in human EPG-257RNOV cells at 0.1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators. |
AID679487 | TP_TRANSPORTER: uptake in Xenopus laevis oocytes | 1999 | Molecular pharmacology, May, Volume: 55, Issue:5 | Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. |
AID1412712 | Inhibition of sheep COX1 at 10 uM assessed as reduction in PGE2 formation using arachidonic acid as substrate by enzyme immunoassay relative to control | |||
AID488203 | Inhibition of COX2 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID1136444 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 12 mg/kg, sc administered post-challenge measured at 3 hrs post compound treatment relative to vehicle-treated control | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Syntheses of N-substituted 2(3,4)-pyridylcarboxylic acid hydrazides with analgesic and antiinflammatory activity. |
AID1204223 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 2 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID183037 | Compound was tested for the inhibition of rat reversed passive Arthus pleurisy after peroral administration of 3 mg/kg dose at 4.01*10e6 no of cells with 2.77*10e6 cells of control | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel synthesis and potent antiinflammatory activity of 4-hydroxy-2(1H)-oxo-1-phenyl-1,8-naphthyridine-3-carboxamides. |
AID235863 | In vitro selectivity against COX-1 to that of COX-2 was determined | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
AID1195160 | Acute toxicity in Swiss albino mouse assessed as mortality at 50 mg/kg, po after 12 hrs | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID641289 | Antiinflammatory activity in ICR mouse assessed as decrease in carrageenan-induced MDA level at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1351160 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by ELISA (Rvb = 24216 +/- 498. | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID1365598 | Ulcerogenic activity in albino rat assessed as ulcer index at 20 mg/kg, po administered daily for 3 successive days in two equal doses at 0 and 12 hrs measured at 6 hrs post last dose by magnifying lens based assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Recently reported biological activities of pyrazole compounds. |
AID1498929 | Inhibition of human COX1 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by TLC | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1128731 | Inhibition of squalene synthase in rat liver microsomes assessed as decrease in conversion of [3H]FPP to squalene | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID162635 | Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay) | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models. |
AID1601228 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as reduction in ear edema formation administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID1659917 | Antiinflammatory activity against dimethylbenzene-induced ear edema mouse model assessed as inhibition of ear edema at 3 mg/kg, ip pretreated with compounds followed by dimethylbenzene challenge relative to control | |||
AID1550476 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 2 hrs post-carrageenan injection (Rvb = 4.72 +/- | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID356318 | Antiinflammatory activity in mouse assessed as inhibition of TPA-induced ear edema at 560 nmol | 2003 | Journal of natural products, Aug, Volume: 66, Issue:8 | Anti-inflammatory lanostane-type triterpene acids from Piptoporus betulinus. |
AID7779 | Oral bioavailability in human | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1473960 | Ratio of drug concentration at steady state in human at 25 to 50 mg, po TID after 8 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1243713 | Inhibition of LPS-activated nitric oxide production in mouse BV2 cells pre-treated for 60 mins before LPS challenge for 24 hrs by Griess assay | 2015 | Journal of natural products, Sep-25, Volume: 78, Issue:9 | Anti-inflammatory Labdane Diterpenoids from Leonurus macranthus. |
AID1689628 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 3 hr by plethysmometer analysis (Rvb = 3.94 +/- 0.65 mm) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID1783310 | Inhibition of ovine COX-1 using arachidonic acid as substrate by fluorescence assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID1244194 | Inhibition of sheep placental cotyledons COX-2 using arachidonic acid as substrate at 50 ug/ml preincubated for 5 mins followed by substrate addition after 20 mins by competitive PGE2 EIA method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis of new 4-phenylpyrimidine-2(1H)-thiones and their potency to inhibit COX-1 and COX-2. |
AID1424665 | Antiinflammatory activity in carrageenan-induced Swiss albino mouse assessed as inhibition of paw edema at 10 mg/kg, po administered 0.5 hrs prior to carrageenan challenge measured 6 hrs post challenge | 2018 | European journal of medicinal chemistry, Jun-10, Volume: 153 | Indolyl-isoxazolidines attenuate LPS-stimulated pro-inflammatory cytokines and increase survival in a mouse model of sepsis: Identification of potent lead. |
AID1062921 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan-challenge measured after 4 hrs relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID266765 | Effective permeability coefficient in 70% silicon-30% IPM membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability. |
AID1311789 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as NO levels by ELISA (Rvb = 0.95 +/- 0.052 umol/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID178757 | Effective dose was evaluated in the carrageenan induced model of para edema in the rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | 1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents. |
AID1359549 | Anti-inflammatory activity in Wistar albino rat assessed as inhibition of cotton pellet-induced granuloma at 10 mg/kg administered once daily for 7 days measured on day 8 relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID414504 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced foot paw edema at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 2 hrs | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent. |
AID134755 | The compound was tested for acute toxicity in mice after oral administration | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID658413 | Inhibition of ovine COX1 at 10 uM by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents. |
AID615922 | Antiinflammatory activity in Wistar albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 0.5 hr relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, characterization and pharmacological activity of 4-{[1-substituted aminomethyl-4-arylideneamino-5-sulfanyl-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl}-2H-1,4-benzothiazin-3(4H)-ones. |
AID415883 | Antipyretic activity against brewer's yeast-induced hyperthermia in Wistar rat assessed as change in rectal temperature at 5 mg/kg, po after 60 mins | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and spectral characterization of a new class of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-ones: antimicrobial, analgesic and antipyretic studies. |
AID449531 | Analgesic activity in albino mouse assessed as decrease in acetic acid-induced writhing at 10 mg/kg, po administered 1 hr prior to acetic acid challenge relative to control | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines. |
AID701950 | Inhibition of ovine COX1 by colorimetric assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity. |
AID747931 | Inhibition of COX-1 in human washed platelet assessed as inhibition of 10 uM arachidonic acid-induced TXB2 formation at 0.01 to 100 uM incubated for 25 mins prior to arachidonic acid challenge measured after 30 mins by radioimmunoassay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID1764398 | Substrate activity at P-gp (unknown origin) assessed as net efflux ratio | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID364306 | Activity at PPARgamma in human Caco-2 cells assessed as luciferase activity at 50 uM relative to control | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | NSAIDs revisited: putative molecular basis of their interactions with peroxisome proliferator-activated gamma receptor (PPARgamma). |
AID1852354 | Protection against LPS/hypoxia induced apoptosis in rat H9c2 cells assessed as reduction in red fluorescence in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by confocal microscopy analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID687241 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 40 mg/kg, po administered 1 hr prior to carrageenan challenge measured 2 hrs post carrageenan challenge relative to control | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents. |
AID1203976 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 24 hrs in absence of LPS by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. |
AID763526 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 30 mins prior to carrageenan challenge measured at 1 hr by plethysmometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
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AID587451 | Antiinflammatory activity in po dosed Sprague-Dawley rat assessed as inhibition of carrageenam-induced paw edema administered 1 hr before carrageenan challenge measured after 3 hrs by Plethysmometer | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies. |
AID1854717 | Antiinflammatory activity in LPS-stimulated mouse BV-2 cells assessed as inhibition of NO production at 10 uM and measured after 24 hrs by Griess method | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
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AID192180 | Antiinflammatory efficacy is measured by the weight gain in rats during the 3 week adjuvant arthritis test at 0.011 mM/kg (3.94 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID227554 | Acute therapeutic index as ratio of potency in pleural effusion to that of potency in gastric toxicity assay | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
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AID1503670 | Ulcerogenicity in albino rat assessed as at 30 umol/kg, po administered daily for 3 successive days in two equal doses at 0 and 12 hrs measured at 6 hrs post last dose by magnifying lens based assay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID387968 | Antiproliferative activity against mouse RAW264.7 cells at 10 uM after 48 hrs relative to control | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Acylamido analogs of endocannabinoids selectively inhibit cancer cell proliferation. |
AID1550471 | Inhibition of human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
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AID634942 | Gastric toxicity in albino rat assessed as apoptotic glandular epithelial cells appearance at 100 mg/kg, po after 5 hrs by hematoxylin and eosin staining | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
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AID640224 | Antiinflammatory activity in carrageenan-stimulated ICR mouse assessed as reduction in COX2 immunoreactive cells at 8 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1594240 | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production up to 2000 nM using arachidonic acid as substrate incubated for 10 mins by EIA method | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9 | Structural modification of indomethacin toward selective inhibition of COX-2 with a significant increase in van der Waals contributions. |
AID678053 | Antiinflammatory activity in CD1 mouse ear edema model assessed as reduction in phorbol myristate acetate-induced edema at 3 mg/ear administered topically at right ear 1 hr before phorbol myristate acetate challenge and measured 24 hrs post dose | 2012 | Journal of natural products, Jul-27, Volume: 75, Issue:7 | Eunicidiol, an anti-inflammatory dilophol diterpene from Eunicea fusca. |
AID1737629 | Analgesic activity in albino mouse assessed as protection at 10 mg/kg, ip measured after 120 mins by hot plate test relative to indomethacin | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
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AID688617 | Inhibition of ram seminal vesicle COX1 assessed as PGE2 production by enzyme immunoassay | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
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AID604742 | Displacement of radiolabeled dansylsarcosine from fatty acid-free human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
AID634935 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 30 mins prior to challenge measured after 5 hrs relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID172637 | Analgesic activity was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 24 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
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AID1742604 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs in absence of LPS by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Novel phthalide derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo. |
AID303575 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 2 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
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AID724083 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po administered 1 hr before carrageenan-challenge measured after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Design, synthesis, characterization and biological evaluation of novel pyrazole integrated benzophenones. |
AID604522 | Antinociceptive activity in rat assessed as suppression of carrageenan-induced nociception in right hind paw at 2 mg/kg, po measured after 1 hr | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 | Design, synthesis, and pharmacological activity of nonallergenic pyrazolone-type antipyretic analgesics. |
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AID486180 | Antiinflammatory activity in rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 4 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis, biological evaluation and molecular docking of novel series of spiro [(2H,3H) quinazoline-2,1'- cyclohexan]-4(1H)- one derivatives as anti-inflammatory and analgesic agents. |
AID304236 | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 1 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID382811 | Antiinflammatory activity in albino rat assessed as protection against carrageenan-induced paw edema at 10 umol/kg, sc administered 1 hr prior to carrageenan challenge | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. |
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AID1852384 | Antiinflammatory activity in LPS/hypoxia induced CA9 knockdown rat H9c2 cells assessed as decrease in TNF-alpha protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID160264 | In vitro inhibition of human Prostaglandin G/H synthase 2 (expressed in sf9 insect cells using baculovirus) enzyme at a concentration of 10 M | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
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AID1576169 | Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 12 hrs relative to control | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
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AID1153382 | Analgesic activity in rat assessed as inhibition of acetic acid-induced writhing measured as potency at 0.03 mM/kg | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13 | Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties. |
AID182282 | Percent inhibition of cellular migration by the compound at a dose of 100 umol/kg was evaluated in the carrageenan-induced rat pleurisy assay | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID303580 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 7 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
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AID304225 | Selectivity for human COX2 over human COX1 | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
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AID751104 | Antiinflammatory activity in Swiss mouse assessed as reduction of carrageenan-induced paw myeloperoxidase activity measured per mg of tissue at 10 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 4 hrs (Rvb = 10.9 +/- 1.2 U) | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID172364 | Gain in the body weight of rat was measured at 7.0 micro mol/kg/day. (+ means significant body weight) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID409563 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema volume at 10 mg/kg, po administered 60 mins before carrageenan challenge after 6 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1737628 | Analgesic activity in albino mouse assessed as protection at 10 mg/kg, ip measured after 120 mins by hot plate test (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1254097 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 12.5 mg/kg, po administered 3 hrs before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID396322 | Antiinflammatory activity in albino Charles-Foster rat assessed as inhibition of carrageenan-induced paw oedema at 50 mg/kg, po measured before 1 hr and after 3 hrs of carrageenan challenge relative to control | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents. |
AID414771 | Inhibition of ovine COX1 by colorimetric assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Phenolic compounds with radical scavenging and cyclooxygenase-2 (COX-2) inhibitory activities from Dioscorea opposita. |
AID189988 | Gastrointestinal tolerability was evaluated under chronic conditions, in rats. The ulcerogenic dose was reported. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID674713 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 2 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID703402 | Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID1178553 | Elimination rate constant in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID1543422 | Antiinflammatory activity in ICR mouse assessed as inhibition of TPA-induced ear edema by measuring reduction in weight of ear punches applied topically measured 4 hrs post TPA-challenge | |||
AID492158 | Inhibition of compound 48/80-induced histamine release in Wister rat Peritoneal mast cells | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Tetracyclic chromane derivatives from Rhododendron anthopogonoides. |
AID188027 | Pharmacological potency relative to indomethacin for prodrug candidate by intestinal toxicity assay. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid. |
AID647936 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 3 hrs by plethysmometer analysis | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID374110 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 3 hrs | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
AID763784 | Neurotoxicity in Swiss albino mouse assessed as minimal motor impairment at 300 mg/kg after 0.5 hrs by rotarod test | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: synthesis and neuropharmacology. |
AID1852410 | Inhibition of intracellular ROS level in LPS/hypoxia induced rat H9c2 cells in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by DCFH-DA probe based fluorescence confocal microscopy analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID177289 | Effect in rat pleural Carrageenan test (exudate volume) | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | 3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation. |
AID235519 | Selectivity ratio of IC50s from COX-1 and COX-2 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. |
AID189412 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 1 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID174433 | Plasma drug level was measured in rat yeast induced hyperalgesia assay in presence of indomethacin at a dose of 10 mg/kg for 8 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID213141 | Inhibition of PGE-2 synthesis in bovine platelet suspension | 2000 | Journal of medicinal chemistry, May-04, Volume: 43, Issue:9 | 1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase. |
AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
AID187727 | Evaluated for the antiinflammatory activity in the 5-h Evans Blue-Carrageenan induced pleural effusion assay at the dose of 4.0 mg/kg (p.o.) | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | Antiinflammatory agents. 2. Syntheses and antiinflammatory activity of substituted 2-aminophenylacetic acid derivatives. |
AID74200 | Antiinflammatory activity measured as effect on ultraviolet induced erythema in guinea pigs | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID162019 | In vitro inhibitory activity against ovine Prostaglandin G/H synthase 1 (44 nM) using [14C]AA (50 uM) was determined | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. |
AID492151 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
AID745191 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr prior to carrageenan-challenge measured after 3 hrs relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Novel quinolone substituted thiazolidin-4-ones as anti-inflammatory, anticancer agents: design, synthesis and biological screening. |
AID430155 | Antiinflammatory activity against carrageenan-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before carrageenan challenge measured after 2 hrs by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID684466 | Inhibition of human recombinant COX-2 at 10 uM by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine. |
AID24265 | Ability to undergo in vitro ester hydrolysis in 80% human plasma ( pH of 7.4) at 37 degree Celsius expressed as half life of methyl ester hydrolysis | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents. |
AID404566 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced edema at 50 mg/kg, po after 1 hr | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID180548 | The compound was tested in vivo for activity against carrageenan induced paw edema in rat after peroral administration | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID674726 | Selectivity index, ratio of inhibition of COX1 to inhibition of COX2 by Cayman's COX activity assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID289298 | Inhibition of carrageenan-induced hind paw oedema in Swiss Albino mouse at 100 mg/kg, po after 360 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID387967 | Antiproliferative activity against human WI38 cells at 10 uM after 48 hrs relative to control | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Acylamido analogs of endocannabinoids selectively inhibit cancer cell proliferation. |
AID326226 | Antiinflammatory activity against carrageenan-induced foot paw edema in rat | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Second-generation aspirin and indomethacin prodrugs possessing an O(2)-(acetoxymethyl)-1-(2-carboxypyrrolidin-1-yl)diazenium-1,2-diolate nitric oxide donor moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID223074 | Concentration required to inhibit production of LDH from whole blood stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID1497264 | Hemolytic activity in human RBC assessed as membrane mortification by absorbance method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective. |
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AID446964 | Antiinflammatory activity in BALB/c mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po after 360 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of 3,6-disubstituted 7H-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines as novel analgesic/anti-inflammatory compounds. |
AID492314 | Antiinflammatory activity against zymosan A-induced peritonitis in Swiss mouse assessed as inhibition of granulocyte infiltration in to peritoneal cavity at 100 mg/kg, po administered 40 mins before zymosan A challenge measured after 6 hrs relative to con | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates. |
AID681053 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, Indomethacin: 5 uM) in Xenopus laevis oocytes | 2001 | Molecular pharmacology, May, Volume: 59, Issue:5 | Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. |
AID112434 | Inhibition of TPA-induced inflammatory ear edema in mice(compound was applied 30 min before TPA (1 mg),Ear thickness was determined 6 hr after TPA treatment) | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Alkane-6,8-diol: inhibitor of tumor promotion in two-stage carcinogenesis in mouse skin. |
AID1667492 | Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1576170 | Ulcerogenic activity in rat assessed as ulcer index at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1145137 | Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenin-induced paw edema | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1, 3, 4, 9-tetrahydropyrano[3, 4-b]indole-1-acetic acids. |
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AID1416047 | Binding affinity to calf thymus DNA at 50 uM in presence of NaCl by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID1134902 | Inhibition of arachidonic acid-induced diarrhea in po dosed mouse treated for 1 hr prior to arachidonic acid-challenge measured after 30 mins | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
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AID1667496 | Anti-inflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 uM/kg, ip measured at 2 hrs by calliper method relative to control | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1456099 | Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and biological evaluation of novel podophyllotoxin-NSAIDs conjugates as multifunctional anti-MDR agents against resistant human hepatocellular carcinoma Bel-7402/5-FU cells. |
AID138456 | In vivo inhibitory activity in a phorbol myristyl acetate (PMA) ear edema model at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
AID1392319 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, po measured at 3 hrs relative to control | |||
AID229532 | Ratio of IC50 values at Cyclooxygenase-1 and Cyclooxygenase-2 | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID382810 | Gastrointestinal toxicity in albino rat assessed as ulcerogenic effect at 30 umol/kg, po for 3 days | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. |
AID1667498 | Anti-inflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 uM/kg, ip measured at 4 hrs by calliper method relative to control | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID774821 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 1 hr before carrageenan challenge measured at 3 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Design, synthesis and biological evaluation of novel anti-cytokine 1,2,4-triazine derivatives. |
AID1251041 | Inhibition of COX2 (unknown origin) assessed as PGH2 production at 100 uM by measuring PGH2alpha level by enzyme immunoassay | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis. |
AID1663611 | Anticancer activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis and anticancer activity of open-resorcinarene conjugates. |
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AID160707 | Inhibition of prostaglandin G/H synthase obtained from bovine seminal vesicles. | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID703400 | Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID185018 | Minimum effective dose against adjuvant arthritis on prophylactic dosing (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID695145 | Selectivity ratio of IC50 for human recombinant COX2 to IC50 for ovine COX1 | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21 | Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors. |
AID1501860 | Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach. |
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AID1136209 | Toxicity in po dosed rat assessed as intestinal perforating ulcer | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Novel analgesic-antiinflammatory salicylates. |
AID229902 | Relative binding to COX-1 and COX-2 (ratio of IC50) | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
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AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
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AID1730824 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 22 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice. |
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AID1241860 | Renal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as total albumin level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 1.77 +/- 0.12 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID717358 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured at 90 mins after carrageenan challenge by plethysmographic analysis | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24 | Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones. |
AID604024 | Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1674100 | Inhibition of AKR1C1 (unknown origin) using 9,10-phenanthrenequinone as substrate | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Overview of AKR1C3: Inhibitor Achievements and Disease Insights. |
AID688468 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as preservance of mast cell degranulation at 0.4 umol administered topically per cm'2 of ear measured after 6 hrs post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
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AID434301 | Antiinflammatory activity in Norwegian albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po after administered 60 mins prior to carrageenan-challenge measured after 1 hr | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID1550482 | Ulcerogenicity in albino rat assessed as gastric lesions at 10 mg/kg, po administered as single dose after 18 hrs of starvation challenge and measured after 4 hrs | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID1810798 | Antiinflammatory activity in Swiss albino mouse model of carrageenan-induced paw edema assessed as reduction in paw thickness at 10 mg/kg, administered 30 mins prior to carrageenan challenge and measured upto 360 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID647948 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced decrease in SOD activity in liver at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 5 hrs | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID1576176 | Ulcerogenic activity in rat assessed as effect on gastric submucosa at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID176342 | Compound was tested in vivo for its efficacy in the rat paw edema assay | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12 | 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. |
AID190173 | Ulcer index at 30 mg/kg concentration | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID177511 | In vivo inhibition of carrageenan-induced hyperalgesia in rats | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID674714 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 3 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID1542242 | Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
AID693573 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan-challenge after 3 hrs relative to vehicle-treated control | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives. |
AID188080 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 3 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 22nd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID190326 | Potency in adjuvant-induced arthritis assay/ potency in intestinal toxicity assay. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid. |
AID751214 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Guaiane-type sesquiterpenes from Curcuma phaeocaulis and their inhibitory effects on nitric oxide production. |
AID649270 | Inhibition of human recombinant COX-2 by enzyme immuno assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation. |
AID356716 | Antiinflammatory activity against TPA-induced ear edema in mouse assessed inhibition of edema | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Antiinflammatory constituents from Heterotheca inuloides. |
AID1133923 | Gastrointestinal toxicity in po dosed rat assessed as induction of gastric irritation | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 2. Dihydro-10-oxofuro-and -thieno[3,2-c][1]benzoxepin-8-acetic acids. |
AID284327 | Effect on gastric damage in rat assessed as induction of gastric ulcer at 30 mg/kg, po after 5 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
AID1172776 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Anti-inflammatory secoiridoid glycosides from Gentianella azurea. |
AID223739 | The compound was tested for IL-1 generation on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID402403 | Inhibition of COX1-catalyzed prostaglandin biosynthesis 10 mins of preincubation | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis. |
AID1459160 | Antiarthritic activity in Lewis rat Freund's adjuvant-induced arthritis model assessed as reduction in mechanical withdrawal threshold at 2.5 mg/kg, ig administered through gavage pretreated for 1 hr followed by adjuvant challenge subsequent treatment for | 2016 | Journal of natural products, 10-28, Volume: 79, Issue:10 | Effects of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. |
AID260543 | Anti-inflammatory activity against paw edema induced by carrageenan in fischer rat at 300 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties. |
AID1311786 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as TNFalpha levels by ELISA (Rvb = 183.21 +/- 5.36 pg/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID492316 | Antiedematogenic activity in Swiss mouse assessed as inhibition of capsaicin-induced paw edema at 100 umol/kg, po administered 40 mins before capsaicin challenge measured after 30 mins relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates. |
AID1852360 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as reduction of TNF-alpha protein expression at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1852413 | Inhibition of intracellular ROS level in LPS/hypoxia induced rat H9c2 cells in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid and Na2WO4 by DCFH-DA probe based fluorescence confocal microscopy | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID161503 | Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay) | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models. |
AID332234 | Antiinflammatory activity against ICR mouse assessed as inhibition ratio of TPA-induced ear edema at 1 mg/ear, topically preincubated 30 mins before TPA challenge relative to TPA | 2002 | Journal of natural products, Feb, Volume: 65, Issue:2 | Anti-inflammatory and anti-tumor-promoting effects of cucurbitane glycosides from the roots of Bryonia dioica. |
AID1334717 | Inhibition of human recombinant COX-2 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | |||
AID1869463 | Anti-inflammatory activity against LPS-induced inflammatory pain-like behaviour ICR mouse model assessed as reduction in TNF-alpha levels in plasma at 10 mg/kg, ip treated with LPS for 2 hrs followed by drug administration for 1 hr by ELISA | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID464327 | Cytotoxicity against human BJ cells after 72 hrs by luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID177770 | Analgesic activity against AcOH writhing after po administration. | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Nonsteroidal antiinflammatory agents. 2. Synthesis of 4',5-disubstituted 3-biphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities. |
AID416488 | Antiinflammatory activity in Wister albino rat assessed as inhibition carrageenan-induced paw edema at 2 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis, analgesic, anti-inflammatory and antimicrobial studies of 2,4-dichloro-5-fluorophenyl containing thiazolotriazoles. |
AID1330410 | Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production after 24 hrs in presence of LPS by colorimetric analysis | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Dimeric sesquiterpene and thiophenes from the roots of Echinops latifolius. |
AID382813 | Inhibition of human recombinant COX2 | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. |
AID617129 | Cytotoxicity against mouse RAW264.7 cells at 100 uM after 24 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Diarylheptanoids from Curcuma kwangsiensis and their inhibitory activity on nitric oxide production in lipopolysaccharide-activated macrophages. |
AID184192 | In vivo effect on prostaglandin and leukotriene mediated production in rat pleural cavity was assessed by the inhibition of cell influx in 5-lipoxygenase/ cyclooxygenase at dose 1.0 mg/kg | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents. |
AID162141 | Inhibition concentration against Prostaglandin G/H synthase 1 | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9 | Enantiospecific, selective cyclooxygenase-2 inhibitors. |
AID430156 | Antiinflammatory activity against carrageenan-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before carrageenan challenge measured after 4 hrs by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID399402 | Inhibition of sheep placental cotyledons COX2 assessed as PGE2 production | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID1742601 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent-based assay relative to control | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Novel phthalide derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo. |
AID687240 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 40 mg/kg, po administered 1 hr prior to carrageenan challenge measured 1 hr post carrageenan challenge relative to control | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents. |
AID182609 | Antiinflammatory activity on peroral administration against carrageenan paw edema | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
AID161493 | Inhibition of Prostaglandin G/H synthase 1 in human whole blood (HWB) assay | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12 | 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. |
AID1456100 | Antiproliferative activity against human LO2 cells after 72 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and biological evaluation of novel podophyllotoxin-NSAIDs conjugates as multifunctional anti-MDR agents against resistant human hepatocellular carcinoma Bel-7402/5-FU cells. |
AID1852416 | Antiinflammatory activity against LPS/talc powder induced pericarditic Wistar rat assessed as reduction in torsion T wave inversion at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-ox | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID162484 | In vitro inhibition against human Prostaglandin G/H synthase 2 | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
AID288823 | Selectivity index COX1 over COX2 | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies. |
AID1737624 | Analgesic activity in albino mouse assessed as protection at 10 mg/kg, ip measured after 60 mins by hot plate test (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID351265 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 1 hr of induction of inflammation relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones. |
AID161472 | IC50 value against Prostaglandin G/H synthase 1 of human platelet rich plasma | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID611506 | Antiinflammatory activity against Swiss mouse assessed as inhibition of 12-O-tetradecanoylphorbol acetate-induced ear edema at 1 mg/ear, topically administered measured after 4 hrs of 12-O-tetradecanoylphorbol acetate-challenge | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6 | Vicenin-2, a potential anti-inflammatory constituent of Urtica circularis. |
AID183014 | Analgesic activity was determined as its ability to inhibit abdominal writhing after intraperitoneal administration of phenylbenzoquinone (PBQ) at dose of 15 mg/kg | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. |
AID194098 | Antiinflammatory activity was evaluated for the compound in rat adjuvant arthritis model and the percent of inhibition was determined at 1 mg/kg dose administered orally | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Benzimidazole derivatives with atypical antiinflammatory activity. |
AID1668166 | Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells incubated for 24 hrs by Griess reagent-based assay | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | α-Glucosidase inhibitory and nitric oxide production inhibitory activities of alkaloids isolated from a twig extract of Polyalthia cinnamomea. |
AID295671 | Antinociceptive activity in sc dosed Sprague-Dawley rat assessed as increase in latency time after 1 hr by hot plate method | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Evaluation of the anti-inflammatory and anti-nociceptive activities of novel synthesized melatonin analogues. |
AID700995 | Inhibition of ovine COX-1 mediated formation of 12-HHT from arachidonic acid assessed as remaining activity at 10 uM after 5 mins by HPLC analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid. |
AID1293532 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 4 hrs before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID1721656 | Antiinflammatory activity in mouse assessed as xylene-induced ear edema at 100 mg/kg, ip administered prior to xylene stimulation and measured after 1 hr (Rvb = 2.05 +/- 0.40 mg) | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs. |
AID1228721 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 6.3 uM after 24 hrs by Griess assay relative to control | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Anti-inflammatory Terpenoids from the Leaves and Twigs of Dysoxylum gotadhora. |
AID196876 | Lengths of bleeding ulcer of drug-administered group | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID634934 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 30 mins prior to challenge measured after 4 hrs relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID1437773 | Analgesic activity in Swiss albino mouse assessed as inhibition of formalin-induced paw flinching at 10 mg/kg administered for 30 mins followed by formalin challenge measured during 10 to 30 mins post formalin challenge relative to vehicle-treated control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Rationally designed benzopyran fused isoxazolidines and derived β |
AID1551030 | Ulcerogenicity in albino rat assessed as ulcer index at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose (Rvb = 0 No_unit) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors. |
AID1351158 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 6 hrs by ELISA (Rvb = 11922 +/- 628.4 | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID724082 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po administered 3 hrs before carrageenan-challenge measured after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Design, synthesis, characterization and biological evaluation of novel pyrazole integrated benzophenones. |
AID396326 | Antiinflammatory activity in albino Charles-Foster rat assessed as inhibition of carrageenan-induced paw oedema at 7.5 mg/kg, po measured before 1 hr and after 3 hrs of carrageenan challenge relative to control | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents. |
AID724081 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po administered 6 hrs before carrageenan-challenge measured after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Design, synthesis, characterization and biological evaluation of novel pyrazole integrated benzophenones. |
AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
AID1164052 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors. |
AID1737603 | Antiinflammatory activity in Wistar rat model of carrageenan-induced paw edema assessed as reduction in thickness of paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hrs (Rvb = 1.79 +/-0.07 mm) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID509687 | Inhibition of COX2 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 3-Formylchromones: potential antiinflammatory agents. |
AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
AID753755 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po after 1 hr relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID551388 | Inhibition of ovine COX1 after 5 mins by microplate reader assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors. |
AID1437465 | Ulcerogenic effect in albino rat assessed as exfoliation of superficial epithelial cells at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID1409614 | Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID181587 | Percent Edema variation in Carrageenan-induced paw edema test at a dose of 5 mg/kg perorally in rats after 180 min (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID188015 | Evaluated for chronic potency in adjuvant arthritis assay | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1852365 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as reduction of IL-6 protein expression at 10 uM in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by Western blot ana | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID178497 | Antiinflammatory activity was assessed from the ability to inhibit adjuvant-induced arthritis in rats | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-ca rboxyl ic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids. |
AID1220794 | Plasma clearance in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID433912 | Antinociceptive activity against acetic acid-induced writhing in sc dosed KM mouse for 30 mins relative to indomethacin | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Synthesis and antinociceptive activity of capsinoid derivatives. |
AID748524 | Inhibition of mouse COX2 V349L mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID537734 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
AID239789 | Ratio of IC50 of Prostaglandin G/H synthase 1 and Prostaglandin G/H synthase 2 | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | 1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors. |
AID649271 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2 | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation. |
AID1153375 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema measured as paw thickness at 0.03 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs (Rvb = 1.260 +/- 0.172 mm) | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13 | Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties. |
AID653313 | Antiinflammatory activity in transgenic zebrafish larvae harboring Fli-1 gene assessed as LPS-stimulated leukocyte migration to injury zone of tail transected larvae at 30 uM after 20 to 22 hrs by microscopy | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID1336956 | Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at greater G2 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 0.20%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1576180 | Hepatotoxicity in rat assessed as effect on hepatocytes in periportal area at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1254093 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 4 hrs before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID123499 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 2 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID703403 | Selectivity ratio of IC50 for AKR1C1 to IC50 for AKR1C3 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID1650569 | Analgesic activity in Wistar rat assessed as reduction in formalin-induced flitching in neurogenic phase at 10 mg/kg, ip incubated for 30 mins followed by formalin addition and observed for 60 mins | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID614602 | Inhibition of human recombinant COX-2 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | SAR studies of acidic dual γ-secretase/PPARγ modulators. |
AID753745 | Gastrointestinal toxicity in albino rat assessed as severe atrophic gastritis and gland atrophy at 0.28 mmol/kg, po using haematoxylin and eosin staining by light microscopic analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1241825 | Anti-inflammatory activity in rat model of acute inflammation assessed as inhibition of carrageenan-induced paw oedema dosed at 10 mg/kg, po dosed 1 hr before carrageenan injection and measured 5 hrs after carrageenan injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID452091 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip treated 60 mins before carrageenan challenge measured after 90 mins | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | A new therapeutic approach in Parkinson's disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents. |
AID1251040 | Inhibition of COX2 (unknown origin) assessed as PGH2 production at 35 uM by measuring PGH2alpha level by enzyme immunoassay | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis. |
AID1139566 | Inhibition of human COX-2 using arachidonic acid at 10 uM after 5 mins by HPLC analysis | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase. |
AID464517 | Selectivity ratio for IC50 for human BJ cells to IC50 for human Raji cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID551387 | Inhibition of ovine COX2 at 100 uM after 5 mins by microplate reader assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors. |
AID313774 | Selectivity index, Ratio of IC50 for ovine COX2 to IC50 for ovine COX1 | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | 1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities. |
AID382809 | Antiinflammatory activity in Sprague-Dawley rat cotton pellet-induced granuloma model | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. |
AID313120 | Inhibition of mouse wild type COX2 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Structural and functional basis of cyclooxygenase inhibition. |
AID1662948 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 3 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID177038 | Dose required for 30% inhibition of carrageenan-induced edema | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID567091 | Drug absorption in human assessed as human intestinal absorption rate | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Prediction of drug intestinal absorption by new linear and non-linear QSPR. |
AID304226 | Antiinflammatory activity against intrapouch dosed Sprague-Dawley rat carrageenan air-pouch model assessed as reduction of prostaglandin E2 at 45 umol/kg | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID356054 | Antiinflammatory activity against carrageenan-induced Swiss mouse paw edema assessed as inhibition of paw volume at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 1 hr relative to control | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID1220248 | Activity of human UGT1A9 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID687437 | Gastric toxicity in Swiss mouse assessed as inflammatory cell index at 10 mg/kg administered as single dose (Rvb = 0.2 +/- 0.2 inflammatory cell index) | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Mechanisms involved in the antinociceptive effects of 7-hydroxycoumarin. |
AID1178534 | Antinociceptive activity in Complete Freund's adjuvant-induced inflammatory pain CD rat model assessed as mechanical hypersensitivity measured as weight bearing capacity at 30 mg/kg, po measured up to 15 mins relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID309363 | Antiinflammatory activity in CD1 mouse assessed as inhibition of croton oil-induced ear oedema at 0.3 umol/cm^2 after 6 hrs | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Synthesis and anti-inflammatory activity of 3-(4'-geranyloxy-3'-methoxyphenyl)-2-trans propenoic acid and its ester derivatives. |
AID173361 | Hypolipidemic action at 500 uM/kg was determined as reduction in triglycerides in rat plasma | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID1055537 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 4 hrs by plethysmometer | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, biological evaluation and molecular modeling study of 5-trifluoromethyl-Δ²-pyrazoline and isomeric 5/3-trifluoromethylpyrazole derivatives as anti-inflammatory agents. |
AID671249 | Antiinflammatory activity in CD-1 mouse assessed as inhibition of TPA-induced ear edema at 0.1 to 1.0 uM applied topically 10 mins before compound challenge measured after 4 hrs | 2012 | Journal of natural products, May-25, Volume: 75, Issue:5 | Neo-clerodane diterpenes from Salvia herbacea. |
AID386854 | Antiinflammatory activity in Wistar rat assessed as inhibition of formalin-induced paw oedema volume at 10 mg/kg, po administered 30 mins before formalin challenge after 3 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID162646 | Inhibition of Prostaglandin G/H synthase 2 in human whole blood | 1999 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15 | SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. |
AID1674102 | Inhibition of N-terminal His-tagged human AKR1C3 (1 to 323 residues) expressed in Escherichia coli using 4-adione as substrate in presence of NADPH by fluorescence method | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Overview of AKR1C3: Inhibitor Achievements and Disease Insights. |
AID1426407 | Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as blood vessel dilation in sub-mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID1157960 | Antiinflammatory activity against TPA-induced CD1 mouse ear edema model assessed as neutrophil infiltration by measuring myeloperoxidase content at 1 umol/ear administered topically 10 mins prior to TPA challenge measured after 4 hrs relative to control | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Sesquiterpenoids from Pittocaulon filare. |
AID1241827 | Anti-inflammatory activity in rat model of acute inflammation assessed as inhibition of carrageenan-induced paw oedema dosed at 10 mg/kg, po dosed 1 hr before carrageenan injection and measured 6 hrs after carrageenan injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID161672 | Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. |
AID192178 | Antiinflammatory efficacy is measured by the weight gain in rats during the 3 week adjuvant arthritis test at 0.008 mM/kg (2.86 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID169646 | Compound is evaluated for gastric ulceration in rats at a dose of 30 mg/kg(7/12) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID161740 | The synthesis of cyclooxygenase or lipoxygenase derived products (HHT and HETE) in human washed platelets at dose of 20 uM | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid. |
AID1195147 | Analgesic activity in Swiss albino mouse assessed as latancy of withdrawing tail at 100 mg/kg, po measured after 2 hrs by tail flick test relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID595375 | Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-induced NFKB p65 subunit translocation to nucleus at 10 uM pretreated for 1 hr before LPS challenge relative to control | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID1228725 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Anti-inflammatory Terpenoids from the Leaves and Twigs of Dysoxylum gotadhora. |
AID1136458 | Antiinflammatory activity in CF1 mouse assessed as increase in foot weight at 20 mg/kg, ip administered 3 hrs and 30 mins prior to carrageenan-challenge measured after 3 hrs (Rvb = 97 +/- 10 mg) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids. |
AID1810793 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-2 | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID1503672 | Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID1067408 | Inhibition of ovine COX1 at 50 uM by peroxidase activity-based colorimetric assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles. |
AID1062920 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan-challenge measured after 3 hrs relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID46861 | IC50 value was determined against Prostaglandin G/H synthase 2 of J7744A.1 cell lines. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID1336923 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1409054 | Antiinflammatory activity in carrageenan-induced Swiss mouse assessed as paw volume at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 4 hrs by plethysmometric method (Rvb = 48.95 +/- 6.59 mL) | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. |
AID177550 | Ability to inhibit phenylquinone induced writhing in rat administered perorally | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 4. Synthesis and evaluation of 4-(4,10-dihydro-10-oxothieno[3,2-c] [1]benzoxepin-8-yl)butanol and -butyric acid and related derivatives. |
AID186598 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 1 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1713249 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-2 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study. |
AID1123743 | Ulcerogenic activity in po dosed rat assessed as induction of lesions in gastric mucosa measured after 24 hrs | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids. |
AID1181044 | Inhibition of LPS-induced IL-1beta production in mouse RAW264.7 cells after 24 hrs by ELISA | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | 2-Phenoxychromones and prenylflavonoids from Epimedium koreanum and their inhibitory effects on LPS-induced nitric oxide and interleukin-1β production. |
AID492859 | Inhibition of ovine COX1 after 5 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity. |
AID679545 | TP_TRANSPORTER: inhibition of MTX uptake (MTX: 1 uM, Indomethacin: 500 uM) in OAT1-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 302, Issue:2 | Characterization of methotrexate transport and its drug interactions with human organic anion transporters. |
AID169642 | Compound is evaluated for gastric ulceration in rats at a dose of 3 mg/kg(1/6) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID1311790 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as iNOS levels by ELISA (Rvb = 31.63 +/- 3.26 U/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID186452 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 10 mg/kg at time interval- 4 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID386952 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat at 10 mg/kg, ip administered 1 hr before inflammation induction assessed after 4 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Facile synthesis of dithiatetraaza-macrocycles of potential anti-inflammatory activity. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID475504 | Binding affinity to amyloid beta (1 to 42) fibrils by change in fluorescence at 100 uM after 10 mins | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta. |
AID587450 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies. |
AID160714 | Ability to inhibit Prostaglandin G/H synthase was evaluated in vitro using bovine seminal vesicle preparations. | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and quantitative structure-activity relationships of diclofenac analogues. |
AID393660 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat assessed as inhibition of edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured after 3 hrs relative to control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Regioselective synthesis of dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones of potential anti-tumor properties. |
AID684833 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | COX inhibitors Indomethacin and Sulindac derivatives as antiproliferative agents: synthesis, biological evaluation, and mechanism investigation. |
AID230227 | Inhibitory ratio at 1.0 mg/ear | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Alkane-6,8-diol: inhibitor of tumor promotion in two-stage carcinogenesis in mouse skin. |
AID729244 | Inhibition of AKR1C3 (unknown origin)-mediated testosterone-17beta-glucuronide formation expressed in human LNCAP cells at 30 uM after 48 hrs in presence of 4-androstene-3,17-dione | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID178376 | Effective dose against gastroulcerogenic activity (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID287142 | Toxicity assessed as ulcerogenic effect in Albino rat at 30 mg/kg, po twice a day after 3 days | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Non-carboxylic analogues of arylpropionic acids: synthesis, anti-inflammatory activity and ulcerogenic potential. |
AID187425 | Reaction time in Hot plate test at a dose of 5 mg/kg perorally in rats after 180 min (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID134741 | Lethal dose in mice determined by Litchfield and Wilcoxon methods after peroral administration. | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID19262 | Aqueous solubility | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Prediction of drug solubility from Monte Carlo simulations. |
AID1426405 | Ulcerogenicity in Wistar albino rat model of carragenan-induced paw edema assessed as degenrative changes with necrotic changes in gastric mucosa at 50 mg/kg, po by hematoxylin and eosin staining based histopathological analysis | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID186600 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 1 mg/kg at time interval- 2 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID171209 | Persent change of the antiinflammatory activity in the 5-h Evans Blue-Carrageenan induced pleural effusion assay at the dose of 4.0 mg/kg (p.o.) | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | Antiinflammatory agents. 2. Syntheses and antiinflammatory activity of substituted 2-aminophenylacetic acid derivatives. |
AID1311787 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as IL1beta levels by ELISA (Rvb = 8.70 +/- 0.365 pg/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID540230 | Dose normalised AUC in rat after po administration | 2005 | Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2 | Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. |
AID54545 | Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22 | Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. |
AID644804 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po dosed 30 mins after carrageenan challenge measured after 5 hrs by plethysmograph analysis relative to control | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis, evaluation and docking studies on 3-alkoxy-4-methanesulfonamido acetophenone derivatives as non ulcerogenic anti-inflammatory agents. |
AID1063661 | Antiinflammatory activity in Wistar rat assessed as change in carrageenan-induced hind paw thickness at 5 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 2 hrs (Rvb = 1.86 +/- 0.38 mm) | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors. |
AID1667493 | Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of human recombinant COX-2 | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID599064 | Plasma protein binding in human | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design. |
AID239787 | Ratio of IC50 against COX-1 to that of COX-2 | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID647949 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced decrease in GPx activity in liver at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 5 hrs | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
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AID1463764 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, ip pretreated for 30 mins followed by xylene challenge measured after 30 mins relative to control | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Design, synthesis, anti-inflammatory activity, and molecular docking studies of perimidine derivatives containing triazole. |
AID640226 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced hind paw edema at 10 mg/kg, ip measured after 4 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1585083 | Antiinflammatory activity in mouse primary peritoneal macrophages assessed as inhibition of LPS-induced TNF-alpha production at 10 uM preincubated for 30 mins followed by LPS addition and measured after 24 hrs by ELISA relative to control | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Design, synthesis and biological evaluation of novel 2-sulfonylindoles as potential anti-inflammatory therapeutic agents for treatment of acute lung injury. |
AID763000 | Inhibition of ovine COX1 assessed as PGF2alpha production by reduction of PGH2 with stannous chloride at 40 uM by enzyme immunoassay relative to control | 2013 | Journal of natural products, Aug-23, Volume: 76, Issue:8 | Rotenoids from Boerhaavia diffusa as potential anti-inflammatory agents. |
AID233584 | Ratio of IC50 of COX-1 to COX-2. | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | 1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. |
AID409548 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 4 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID365463 | Inhibition of human MRP1 in human 2008 cells | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins. |
AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1196198 | Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases. |
AID452089 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, po treated 60 mins before carrageenan challenge measured after 90 mins | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | A new therapeutic approach in Parkinson's disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents. |
AID124990 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 4 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1663616 | Anticancer activity against human SKLU1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis and anticancer activity of open-resorcinarene conjugates. |
AID1351161 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 6 hrs by ELISA (Rvb = 94.6 +/- 5.9 pg/ml) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID1242114 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 4 hrs by plethysmometric analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Molecular docking design and one-pot expeditious synthesis of novel 2,5-diarylpyrazolo[1,5-a]pyrimidin-7-amines as anti-inflammatory agents. |
AID371494 | Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid-induced writhing response at 10 mg/kg, po administered 1 hr before acetic acid challenge measured for 30 mins | 2008 | European journal of medicinal chemistry, Aug, Volume: 43, Issue:8 | 1,8-Naphthyridines VII. New substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity. |
AID160715 | Compound was evaluated for the inhibition of Prostaglandin G/H synthase | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis. |
AID389639 | Antiinflammatory activity against carrageenan-induced paw edema in ICR mouse at 4 mg/kg, ip administered 30 mins before carrageenan challenge assessed after 3 hrs | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Anti-inflammatory activities of furanoditerpenoids and other constituents from Fibraurea tinctoria. |
AID1241856 | Hepato-toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as alkaline phosphatase level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 17.82 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID138596 | Inhibitory activity against carrageenan induced paw edema at a oral dose of 10 mg/kg in mouse 5 hours after carrageenan administration | 1998 | Journal of medicinal chemistry, Aug-13, Volume: 41, Issue:17 | Synthesis and comparison of the antiinflammatory activity of manoalide and cacospongionolide B analogues. |
AID399404 | Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production preincubated for 10 mins | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID188751 | Intestinal toxicity in fed rat at the dose of 16 mg/Kg (ig)(number of animals with damage/number of animals treated=6/6) | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
AID444055 | Fraction absorbed in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1125125 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 2 hrs relative to control | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID703404 | Inhibition of AKR1C3 using 9,10-phenanthroquinone as substrate | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID1241838 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 9 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID396325 | Antiinflammatory activity in albino Charles-Foster rat assessed as inhibition of carrageenan-induced paw oedema at 5 mg/kg, po measured before 1 hr and after 3 hrs of carrageenan challenge relative to control | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents. |
AID592742 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID1436689 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 5 hrs by plethysmometer relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID7132 | Inhibitory activity against 5-lipoxygenase obtained from rat basophilic leukemia cells at 30 uM concentration; NT=Not tested | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid. |
AID171711 | Antiinflammatory effect at a dose of 100 umol/kg administered orally in the carrageenan-induced rat pleurisy assay (10e6 Cells/cavity) | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID1866133 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL-6 production at 84 uM incubated for 2 hrs followed by LPS stimulation for 20 hrs by ELISA relative to control | 2022 | Journal of natural products, 04-22, Volume: 85, Issue:4 | Synthesis, Biological Evaluation, and Molecular Docking Study of 3-Amino and 3-Hydroxy- |
AID260546 | Gastrointestinal toxicity in rat at 84 umol/kg, sc | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties. |
AID1437464 | Ulcerogenic effect in albino rat assessed as submucosal edema at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID174679 | Percentage of [51Cr]- secreted in feces was determined by fecal drug-induced bleeding method in rat at 100 mg/kg, bid for 5 days | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID403340 | Inhibition of COX2 | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID509683 | Antiinflammatory activity in human neutrophils assessed as inhibition of respiratory burst | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 3-Formylchromones: potential antiinflammatory agents. |
AID1884334 | Inhibition of LPS induced NO production in mouse RAW264.7 cells at 30 uM preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent based assay relative to control | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis. |
AID577992 | Cardiotoxicity in Kunming mouse assessed as pathological changes at 100 mg/kg, po after 12 days | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | Design, synthesis and biological evaluation of novel 4-hydroxybenzene acrylic acid derivatives. |
AID547625 | Antiinflammatory activity in Sprague-Dawley rat assessed as reduction of cotton pellet-induced dry weight of granuloma measured after 7 days | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID187729 | Evaluated for the carrageenan-induced pleural volume in rats at a dose of 3.16 mg/kg after peroral administration. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents. |
AID1392314 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, ip administered 30 mins prior to para-xylene challenge measured after 30 mins relative to control | |||
AID114342 | Effective dose by mouse phenyl-p-benzoquinone writhing (PQW)assay after peroral administration; 0.23-0.53 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Preparation and antiarthritic and analgesic activity of 4,5-diaryl-2-(substituted thio)-1H-imidazoles and their sulfoxides and sulfones. |
AID591625 | Gastrointestinal toxicity in Wistar rat assessed as appearance ulcer area of <1 mm diameter at 100 mg/kg, po administered as single dose after 6 hrs by Vernier caliper | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID160266 | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 (COX-2) at 10 uM expressed in sf-9 cells infected with baculovirus | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors. |
AID415885 | Antipyretic activity against brewer's yeast-induced hyperthermia in Wistar rat assessed as change in rectal temperature at 5 mg/kg, po after 120 mins | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and spectral characterization of a new class of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-ones: antimicrobial, analgesic and antipyretic studies. |
AID747927 | Irreversible inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID1229623 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as LPS-stimulated inhibition of nitric oxide production incubated simultaneously with LPS for 24 hrs by Griess reagent based assay | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Ervatamines A-I, Anti-inflammatory Monoterpenoid Indole Alkaloids with Diverse Skeletons from Ervatamia hainanensis. |
AID1576326 | Antiinflammatory activity against carrageenan-induced air pouch inflammatory Swiss mouse model assessed as IL-1beta level in air pouch exudate at 10 mg/kg, po treated 1 hr prior to carrageenan administration and measured after 6 hrs by sandwich ELISA (Rvb | 2019 | MedChemComm, Nov-01, Volume: 10, Issue:11 | Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives. |
AID186448 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 10 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID481937 | Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 10 to 100 uM by flow cytometry | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells. |
AID1416048 | Binding affinity to calf thymus DNA assessed as melting temperature at 50 uM by UV-visible spectroscopic method (Rvb = 66.3 +/- 1 degC) | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID357286 | Inhibition of A23187-induced PGE2 formation in human polymorphonuclear leukocytes at 1 to 100 uM | |||
AID1220798 | Half life in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID1192213 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 1 hr relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID618604 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 2 hrs by plethysmograph | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, pharmacological evaluation and docking studies of coumarin derivatives. |
AID1576174 | Ulcerogenic activity in rat assessed as effect on gastric mucosa at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID223078 | Concentration required to inhibit production of arachidonic acid from whole blood stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID1192206 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat assessed as edema volume at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 1 hr (Rvb = 1.11 +/- 0.12 mL) | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID186451 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 10 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID166603 | In vitro platelet aggregation of citreated rabbit platelet-rich plasma induced by collagen at 5 ug/mL | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID1700186 | Analgesic activity in mouse assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, ip measured after 60 mins relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel piperazine-2,5-dione analogs bearing 1H-indole: Synthesis and biological effects. |
AID1832223 | Antinociceptive activity in Swiss Webster mouse model of formalin-induced biphasic nociceptive response assessed as reduction in pain during late phase at 5 mg/kg, ip administered 40 mins before formalin injection and measured after 10 to 30 mins post for | |||
AID642877 | Inhibition of COX2 | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity. |
AID168892 | Analgesic activity evaluated by measuring % analgesic effect, after oral administration of 1.0 mg/kg in acetic acid writhing test | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID723695 | Competitive inhibition of human recombinant COX2 assessed as inhibition of PGF2a production at 200 uM by enzyme immunoassay | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
AID1128737 | In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in total cholesterol level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1542906 | Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1134827 | Acute toxicity in po dosed mouse | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | 2-(Substituted phenyl)oxazolo[4,5-b]pyridines and 2-(substituted phenyl)oxazolo[5,4-b]pyridines as nonacidic antiinflammatory agents. |
AID499200 | Inhibition of COX2 | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases. |
AID1902040 | Inhibition of human COX-2 at 5 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID190509 | Ulcerogenic activity administered once daily at 84 uM/kg for 4 days was determined as no of animals showing perforating ulcers | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID184914 | Percent inhibition of adjuvant-induced arthritis at 10 mg/kg po; no data | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID1155578 | Inhibition of COX1-mediated PGE2 production in human platelets assessed as residual activity by measuring formation of 12-HHT from arachidonic acid preincubated at 10 uM for 5 mins measured after 5 mins by RP-HPLC analysis relative to control | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID183700 | Evaluated in vivo for antiinflammatory activity at 30 mg/kg oral dose in the carrageenan-induced rat paw edema (male Wistar rat); Not determined | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
AID161667 | Inhibitory concentration against human recombinant Prostaglandin G/H synthase 1 cloned and expressed in baculovirus (Sf9) | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors. |
AID1278584 | Antiinflammatory activity in mouse RAW264.7 assessed as decrease in LPS-induced TNF-alpha production at 10 uM pretreated with 1 ug/ml LPS for 22 hrs followed by addition of compound for 24 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5 | Hesperetin derivatives: Synthesis and anti-inflammatory activity. |
AID580340 | Inhibition of COX1 at 30 uM | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents. |
AID464515 | Selectivity ratio for IC50 for human BJ cells to IC50 for human HEK293 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID746654 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Conjugation of l-NAME to prenyloxycinnamic acids improves its inhibitory effects on nitric oxide production. |
AID1542918 | solubility in pH 7.0 simulated intestinal fluid | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1264568 | Inhibition of Ovine COX-1 preincubated for 15 mins by fluorescence analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents. |
AID1055835 | Antiinflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 0.05 mmol/kg, po administered 1 hr prior to carrageenan challenge measured after 5 hrs by plethysmometric analysis relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID192648 | Dose required for Ulcerogenic effect | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID1134898 | Inhibition of PGF2-alpha formation in po dosed rat serum after 1 hr by radioimmunoassay | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID1151354 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay | 2014 | Journal of natural products, May-23, Volume: 77, Issue:5 | Dammarane-type triterpenoids from Gentianella azurea. |
AID162493 | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors. |
AID303030 | Antiinflammatory activity against carrageenan-induced paw edema rat model at 0.01 mmol/ml/kg | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues. |
AID162016 | IC50 value against ovine Prostaglandin G/H synthase 1 | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID1756550 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess reagent based assay | 2021 | Journal of natural products, 02-26, Volume: 84, Issue:2 | Cytotoxic and Anti-Inflammatory Sesquiterpenes from the Whole Plants of |
AID1576159 | Ulcerogenic activity in rat assessed as effect on mucosal blood vessel at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1183335 | Inhibition of human recombinant COX2 using fluorometric substrate at 10 mM by fluorescent inhibitor screening assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core. |
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AID509686 | Inhibition of COX1 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 3-Formylchromones: potential antiinflammatory agents. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID757493 | Inhibition of ovine COX1 | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity. |
AID177015 | Antiinflammatory activity assessed by inhibition of carrageenan-induced edema in rats at a dose of 15 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-ca rboxyl ic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids. |
AID1172863 | Inhibition of ovine COX2 | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Synthesis of novel pyrazole–thiadiazole hybrid as potential potent and selective cyclooxygenase-2 (COX-2) inhibitors. |
AID748526 | Inhibition of mouse COX2 V349A mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1601222 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as inhibition of ear edema at 2 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration relative to control | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID1220259 | Oral absorption in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID1241844 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 18 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1696528 | Antiinflammatory activity in Swiss-Taconi mouse assessed as reduction in TPA-induced ear edema | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Isolation, reactivity, pharmacological activities and total synthesis of hispanolone and structurally related diterpenes from Labiatae plants. |
AID1409045 | Antiinflammatory activity in carrageenan-induced Swiss mouse assessed as inhibition of paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 6 hrs by plethysmometric method | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. |
AID303565 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 2 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID399388 | Antiplatelet activity in human whole blood assessed as inhibition of ADP-induced platelet aggregation at 100 ug/mL relative to control | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | A new antiplatelet diarylheptanoid from Alpinia blepharocalyx. |
AID1228720 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 3.1 uM after 24 hrs by Griess assay relative to control | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Anti-inflammatory Terpenoids from the Leaves and Twigs of Dysoxylum gotadhora. |
AID440892 | Toxicity in Fisher 344 rat assessed as melena defecation at 0.01 mmol/kg, ip administered daily once for 4 days measured after 24 hrs final post dose | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins. |
AID176482 | Inhibition of adjuvant-induced polyarthritis in rat following p.o. administration. | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | 2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents. |
AID681168 | TP_TRANSPORTER: uptake in Oat3-expressing oocyte cells | 2004 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3 | Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. |
AID312248 | Effect on acetic acid-induced chronic gastric ulcer Wistar rat assessed as area of ulcer at 2.0 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | New celecoxib derivatives as anti-inflammatory agents. |
AID162658 | Inhibitory concentration against human recombinant Prostaglandin G/H synthase 2 cloned and expressed in baculovirus (Sf9) | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors. |
AID402987 | Inhibition of compound 48/80-induced histamine release in Wistar rat peritoneal mast cells | 2004 | Journal of natural products, Jul, Volume: 67, Issue:7 | Structures and histamine release inhibitory effects of prenylated orcinol derivatives from Rhododendron dauricum. |
AID420034 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID127503 | Inhibition of human PGE-2 production. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID249066 | In vivo antiinflammatory activity after 3 hr of oral administration was determined using rat carrageenan induced paw edema model | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID478750 | Antiinflammatory activity against carrageenan-induced paw edema in po dosed rat administered 1 hr before carrageenan challenge assessed after 3 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis of 3-((2,4-dichlorophenoxy)methyl)-1,2,4-triazolo(thiadiazoles and thiadiazines) as anti-inflammatory and molluscicidal agents. |
AID1689629 | Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 3 hr by plethysmometer analysis relative to control (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID1301940 | Inhibition of COX2 in healthy human whole blood assessed as LPS-induced PGE2 level at 1 uM preincubated for 15 mins followed by LPS addition measured after 18 hrs by ELISA (Rvb = 15.5 ng/ml) | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent. |
AID408273 | Antiinflammatory activity in sc dosed Albino rat assessed as protection against carrageenan-induced paw edema measured 4 hrs after carrageenan challenge | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity. |
AID190168 | compound was evaluated for the induction no of gastric ulcers in rats when administered perorally | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID515504 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered prior to carrageenan challenge measured after 3 hrs post carrageenan challenge | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 | Synthesis and characterization of novel indole derivatives reveal improved therapeutic agents for treatment of ischemia/reperfusion (I/R) injury. |
AID162015 | IC50 against ovine Prostaglandin G/H synthase 1 | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID634855 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 30 mins prior to challenge measured after 1 hr relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID186450 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 10 mg/kg at time interval- 2 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1241807 | In-vitro antiinflammatory activity assessed as inhibition of denaturation of bovine serum albumin at 10 mg | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID440888 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip after 3.5 hrs | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins. |
AID162663 | Inhibitory potency against cyclooxygenase-2 in human whole blood assay | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. |
AID1150596 | Chronic antiinflammatory activity against adjuvant-induced arthritis in po dosed rat assessed as decrease in volume of paw administered for 9 days starting 14 days after adjuvant injection and continued until day 22 by therapeutic test | 1976 | Journal of medicinal chemistry, Jun, Volume: 19, Issue:6 | Cycloalkanoindoles. 1. Syntheses and antiinflammatory actions of some acidic tetrahydrocarbazoles, cyclopentindoles, and cycloheptindoles. |
AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID699544 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID409537 | Antiarthritic activity in Freund's complete adjuvant challenged Albino rat model assessed as change in body weight at 10 mg/kg, po administered for 14 days daily once starting a day before adjuvant challenge | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1129361 | Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | A high-throughput cell-based method to predict the unbound drug fraction in the brain. |
AID209202 | Effect of pyrrolidine derivatives on production of eicosanoids from THP-1 cells stimulated with A-23187 using cellular assay on PGE-2, LTC-4 | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Pyrrolidine inhibitors of human cytosolic phospholipase A(2). |
AID1135112 | Antiinflammatory activity in rabbit assessed as inhibition of edema at 200 ug per site by reversed passive arthus test | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Synthesis and antiinflammatory activity of cis-4,5,6,7,8,8a,9-hexahydro-alpha-methyl-5H-fluorene-2-acetic acid. |
AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID1499674 | Inhibition of ovine COX1 at 20 uM using arachidonic acid as substrate by ELISA | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity. |
AID751128 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip measured at 1 hr by plethysmometric analysis relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID128487 | Analgesic activity was assessed from the ability to inhibit phenylquinone-induced writhing in mouse | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-ca rboxyl ic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids. |
AID623641 | Antinociceptive activity against formalin-induced pain in mouse assessed as paw licking during early phase (0 to 10 mins) at 10 mg/kg, ip administered 40 mins before formalin challenge | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antinociceptive properties of bergenin. |
AID1203973 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM pre-incubated for 2 hrs before LPS stimulation for 18 hrs by Griess reagent based colorimetric method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. |
AID1171108 | Hepatotoxicity in Swiss mouse assessed as plasma ALT level at 2.5 mg/kg, po daily for 7 days | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Pimaradienoic acid inhibits inflammatory pain: inhibition of NF-κB activation and cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID6746 | Inhibitory activity against 5-lipoxygenase at 10 uM concentration | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | Antiinflammatory 2,6-di-tert-butyl-4-(2-arylethenyl)phenols. |
AID1717039 | Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents. |
AID492326 | Inhibition of MRP2 expressed in human A2780 cells at 10 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators. |
AID357287 | Inhibition of A23187-induced 12-hydroxy-5,8,10-heptadecatrienoic acid formation in human polymorphonuclear leukocytes at 1 to 100 uM | |||
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AID535924 | Antiinflammatory activity in in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr before carrageenan challenge and measured 2 hrs post carrageenan challenge relative to untreated control | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines. |
AID1149354 | Antiinflammatory activity against Mycobacterium butyricum adjuvant-induced polyarthritis in po dosed Lewis albino rat assessed as decrease in non-injected paw edema administered daily for 21 days prior to adjuvant injection | 1977 | Journal of medicinal chemistry, Jan, Volume: 20, Issue:1 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 1. 6,11-Dihydro-11-oxodibenz]b,e]oxepin-2-acetic acids. |
AID1241852 | Hepato-toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as SGOT level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 92.48 +/- 7.8 U/mL) | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID287611 | Antiinflammatory activity against carrageenan-induced paw oedema in Wistar Albino rat assessed as mean swelling paw volume at 5 mg/kg, ip after 1 hr | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID124002 | Intestinal ulcerogenic activity at a dose of 10 mg/kg; 8 mice were considered for the test | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID303574 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID644807 | Antiinflammatory activity in po dosed Wistar rat assessed as inhibition of carrageenan-induced paw oedema compound administered 30 mins after carrageenan challenge measured after 5 hrs by plethysmograph analysis | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis, evaluation and docking studies on 3-alkoxy-4-methanesulfonamido acetophenone derivatives as non ulcerogenic anti-inflammatory agents. |
AID611829 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured after 270 min by Plethysmograph | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents. |
AID1181043 | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess reagent based assay | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | 2-Phenoxychromones and prenylflavonoids from Epimedium koreanum and their inhibitory effects on LPS-induced nitric oxide and interleukin-1β production. |
AID374236 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 4 hrs | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
AID1869460 | Anti-inflammatory activity against LPS-induced inflammatory pain-like behaviour ICR mouse model assessed as improvement in locomotor activity by measuring decrease in immobility behaviour at 10 mg/kg, ip treated with LPS for 2 hrs followed by drug adminis | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID1852443 | Toxicity in Wistar rat assessed as change in CRE level in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1123070 | Inhibition of cyclooxygenase activity in bovine seminal vesicles assessed as arachodonic acid dependent formation of adenochrome from L-epinephrine at 20 uM | 1979 | Journal of medicinal chemistry, Jul, Volume: 22, Issue:7 | Azaprostanoic acid derivatives. Inhibitors of arachidonic acid induced platelet aggregation. |
AID1063668 | Antinociceptive activity in Swiss albino mouse assessed as licking time in secondary inflammatory period at 5 mg/kg, ip administered 30 mins prior to formalin-challenge (Rvb = 217 +/- 68.5 seconds) | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors. |
AID379574 | Antiinflammatory activity against TPA-induced ear edema in mouse | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12 | Anti-inflammatory, anti-tumor-promoting, and cytotoxic activities of constituents of marigold (Calendula officinalis) flowers. |
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID177150 | In vivo effective concentration of compound in rat adjuvant arthritis | 1999 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15 | SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. |
AID1264567 | Inhibition of EGFR (unknown origin) using tyrosine 4 as substrate by fluorescence analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents. |
AID1846855 | Anti-inflammatory activity against carrageenan-induced paw edema in Wistar rat at 20 mg/kg, po assessed as paw edema volume measured after 4 hrs by plethysmometric analysis relative to control | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Contemporary advances of cyclic molecules proposed for inflammation. |
AID1241836 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 6 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1133924 | Therapeutic index, ratio of ID50 for po dosed rat to ED50 for po dosed rat | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 2. Dihydro-10-oxofuro-and -thieno[3,2-c][1]benzoxepin-8-acetic acids. |
AID393848 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 5 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. |
AID187426 | Reaction time in Hot plate test at a dose of 5 mg/kg perorally in rats after 60 min (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID303564 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID621753 | Antiinflammatory activity in mouse assessed as inhibition of TPA-induced mouse ear edema at 0.5 mg/ear administered relative to untreated control | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Fuscoside E: a strong anti-inflammatory diterpene from Caribbean octocoral Eunicea fusca. |
AID190174 | Ulcer index at 50 mg/kg concentration | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1436690 | Antiinflammatory activity in carrageenan-induced rat paw edema model assessed as inhibition of COX-2 level in paw at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 5 hrs relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID1550473 | Antiinflammatory activity against carrageenan-induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured immediately after carrageenan injection (Rvb = 3.46 | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID612633 | Inhibition of human platelets COX1 assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 15 mins by EIA | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Bioactive sulfoximines: syntheses and properties of Vioxx analogs. |
AID304235 | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 3 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID432724 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered before 60 mins of carrageenan-challenge measured after 180 mins | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives. |
AID1576301 | Antiinflammatory activity against carrageenan-induced air pouch inflammatory Swiss mouse model assessed as TNF-alpha level in air pouch exudate at 10 mg/kg, po treated 1 hr prior to carrageenan administration and measured after 6 hrs by sandwich ELISA (Rv | 2019 | MedChemComm, Nov-01, Volume: 10, Issue:11 | Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives. |
AID181152 | Hemoglobin levels in the different assays ranged from 11.5-14.7 g/dl. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID408271 | Antiinflammatory activity against carrageenan-induced paw edema in sc dosed Albino rat assessed as inhibition of paw edema volume measured 4 hrs after carrageenan challenge | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity. |
AID717357 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured at 180 mins after carrageenan challenge by plethysmographic analysis | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24 | Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones. |
AID1737618 | Analgesic activity in albino mouse assessed reduction in acetic acid-induced abdominal writhing by measuring writing reflex at 10 mg/kg, ip pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 1 | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID751100 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced total leukocytes migration into peritoneal cavity at 10 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 4 hrs relative to carrageenan-treat | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID536610 | Antiinflammatory activity in rat assessed as inhibition of formaldehyde-induced paw edema at 100 mg/kg, po qd for 4 days administered 1 hr before formaldehyde challenge measured 2 hrs post formaldehyde challenge relative to untreated control | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives. |
AID1713250 | Inhibition of potato 5-LOX assessed as reduction in hydroperoxide level by EIA method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study. |
AID500932 | Inhibition of COX2 in heat-stimulated heterozygous transgenic zebrafish embryo assessed as MPO-positive granulocytic cell accumulation at 20 uM by in situ hybridization analysis in presence of PGE2 | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4 | Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation. |
AID177523 | In vivo inhibitory activity against adjuvant induced arthritis in the rat. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
AID302058 | Inhibition of IL1-beta induced MMP3 secretion in human articular chondrocytes at 100 ug/ml | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and in vitro evaluation of 5-arylidene-3-hydroxyalkyl-2-phenylimino-4-thiazolidinones with antidegenerative activity on human chondrocyte cultures. |
AID1241851 | Gastro-intestinal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as histological changes at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 by hema | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1743654 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID364550 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip after 3 hrs | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives. |
AID745281 | Antiinflammatory activity in Fisher 344 rat assessed as reduction of carrageenan-induced paw oedema at 0.01 mmol/kg, ip after 3.5 hrs | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Analysis of the antioxidant properties of differently substituted 2- and 3-indolyl carbohydrazides and related derivatives. |
AID453623 | Inhibition of human recombinant COX2 assessed as residual enzyme activity at 10 uM relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID647942 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced neutrophil infiltration in paw at 10 mg/kg, ip administered 30 mins before carrageenan challenge | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID328212 | Analgesic activity in ICR mouse assessed as reduction in number of acetic acid-induced writhing at 10 mg/kg, po after 10 mins | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID34786 | In vitro inhibition of rabbit lens aldose reductase at 10e-4 M. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
AID161166 | Inhibition of Prostaglandin G/H synthase activity in sheep seminal vesicle was determined | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | 3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors. |
AID288824 | Antiinflammatory activity against carrageenan-induced rat paw edema in orally dosed rat after 3 hrs | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies. |
AID190165 | Ulcerogenic dose that produced gastric lesions, ulcers and/or hemorrhage in 50% of the animals tested | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID115376 | Inhibitory activity against carrageenan induced mouse paw edema in mice. | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID1585085 | Cytotoxicity against mouse primary peritoneal macrophages assessed as reduction in cell viability at 10 uM after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Design, synthesis and biological evaluation of novel 2-sulfonylindoles as potential anti-inflammatory therapeutic agents for treatment of acute lung injury. |
AID409547 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 5 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1437461 | Ulcerogenic effect in albino rat assessed as maceration of gastric mucosa at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID1193492 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID274903 | Activity at COX1 assessed as inhibition of arachidonic acid-induced PGE2 production in J774 cells at 100 uM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage. |
AID428388 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po treated for 30 mins measured after 1 hr of carrageenan challenge | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. |
AID1376962 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by measuring nitrite accumulation by Griess method | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6 | Anti-inflammatory 12,20-Epoxypregnane and 11,12-seco-Pregnane Glycosides from the Stems of Hoya kerrii. |
AID1592992 | Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones. |
AID1139290 | Antiinflammatory activity in ICR mouse ear edema model assessed as inhibition of TPA-induced ear edema at 20 mg/kg, po administered 30 mins prior to TPA challenge measured after 4 hrs relative to vehicle-treated control | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Suppression of inflammatory responses by handelin, a guaianolide dimer from Chrysanthemum boreale, via downregulation of NF-κB signaling and pro-inflammatory cytokine production. |
AID664541 | Inhibition of human recombinant AKR1C2 expressed in Escherichia coli using S-tetralol as substrate by fluorometry | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4 | Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. |
AID1869457 | Anti-inflammatory activity against LPS-induced inflammatory pain-like behaviour ICR mouse model assessed as improvement in locomotor activity by measuring increased mobile behaviours at 10 mg/kg, ip treated with LPS for 2 hrs followed by drug administrati | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID173977 | Dose that inhibits paw swelling by 25% compared with control in carrgeenin rat paw edema assay | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID139179 | Therapeutic index was expressed as LD50/ED50 carragreenin model | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID190670 | Ulcerogenicity was measured in intestine during the 3 week adjuvant arthritis test.(animals with ulcers/animals in test) at 0.0014 mM/kg (0.50 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID640128 | Antioxidant activity in carrageenan-stimulated ICR mouse assessed as increase in GPx activity at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID387679 | Antiinflammatory activity against carrageenan-induced albino rat hind paw edema model assessed as edema rate at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 2 hrs | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities. |
AID434302 | Antiinflammatory activity in Norwegian albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po after administered 60 mins prior to carrageenan-challenge measured after 3 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID1319556 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reagent based assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | New labdane diterpenoids from Croton laui and their anti-inflammatory activities. |
AID1319558 | Selectivity index, ratio of CC50 for mouse RAW264.7 cells to antiinflammatory IC50 for mouse RAW264.7 cells | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | New labdane diterpenoids from Croton laui and their anti-inflammatory activities. |
AID160262 | Inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood at 10 uM | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID183912 | Inhibitory activity on carrageenan-induced paw edema in rats 3h after po administration of 2 mg/kg | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Nonsteroidal antiinflammatory agents. 2. Synthesis of 4',5-disubstituted 3-biphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities. |
AID235831 | Safety index is the ratio of UD50 to ED50 in carrageenan hind paw edema | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID396714 | Inhibition of human platelet COX1 assessed as effect on prostaglandin E2 production by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Synthesis and evaluation of dithiolethiones as novel cyclooxygenase inhibitors. |
AID190175 | Ulcer index at 5 mg/kg concentration | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID305970 | Antiinflammatory activity in neutrophils assessed as inhibition of oxygen radical generation | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents. |
AID409534 | Gastrointestinal toxicity in Wistar rat assessed as ulcer index at 1 mg/kg, po after 14 days | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID129290 | Antiinflammatory activity was assessed from the ability to inhibit cotton pellet granuloma in mice | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-ca rboxyl ic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids. |
AID1193495 | Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID516449 | Inhibition of ovine COX2 by enzyme immunoassay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Synthesis and biological evaluation of indomethacin analogs possessing a N-difluoromethyl-1,2-dihydropyrid-2-one ring system: a search for novel cyclooxygenase and lipoxygenase inhibitors. |
AID178668 | Antiinflammatory activity was determined to inhibit adjuvant-induced arthritis in rats with respect to naproxen | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds. |
AID1529182 | Protein binding in plasma (unknown origin) | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID649083 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 umol/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs by plethysmometric analysis relative to control | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives. |
AID1852377 | Protection against LPS/hypoxia induced cell injury in rat H9c2 cells assessed as recovery of cell viability at 10 uM by CCK-8 assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID402402 | Inhibition of COX2-catalyzed prostaglandin biosynthesis after 10 mins of preincubation | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis. |
AID113098 | Analgesic activity in mice by phenyl quinone-induced writhing assay with respect to aspirin. | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds. |
AID1293534 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 6 hrs before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID185773 | Percentage dose required to prevent lesion formation in gastric mucosa of unanesthetized rats upon intraperitoneal administration of 1 mg/kg dose in the HCl/ethanol-induced lesion model | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | Novel angucycline compound with both antigastrin- and gastric mucosal protective-activities. |
AID182306 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 8 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID547629 | Inhibition of human platelets COX1 after 2 mins | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID1242111 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr by plethysmometric analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Molecular docking design and one-pot expeditious synthesis of novel 2,5-diarylpyrazolo[1,5-a]pyrimidin-7-amines as anti-inflammatory agents. |
AID453622 | Inhibition of ovine COX1 assessed as residual enzyme activity at 10 uM relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID46862 | IC50 value against Prostaglandin G/H synthase 2 of murine J774A.1 cell line | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID1529185 | Protein binding in human serum albumin after 4.5 hrs by LC-MS based rapid equilibrium dialysis method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID1717038 | Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents. |
AID717355 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured at 360 mins after carrageenan challenge by plethysmographic analysis | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24 | Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones. |
AID396564 | Safety ratio for toxicity to antiinflammatory activity in po dosed mouse | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and anti-inflammatory activity evaluation of unsymmetrical selenides. |
AID287076 | Inhibition of TPA-induced inflammation in mouse assessed per ear by edema assay | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Anti-inflammatory and potential cancer chemopreventive constituents of the fruits of Morinda citrifolia (Noni). |
AID123498 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 1 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID178754 | Inhibitory activity in the adjuvant induced arthritis model of chronic inflammation in rat | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | 1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents. |
AID386954 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat at 10 mg/kg, ip administered 1 hr before inflammation induction assessed after 1 hr | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Facile synthesis of dithiatetraaza-macrocycles of potential anti-inflammatory activity. |
AID1136449 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 12 mg/kg, sc administered post-challenge measured at 5 hrs post compound treatment relative to vehicle-treated control | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Syntheses of N-substituted 2(3,4)-pyridylcarboxylic acid hydrazides with analgesic and antiinflammatory activity. |
AID1902044 | Selectivity index, ratio of IC50 for human COX-2 to IC50 for full-length ovine COX-1 | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID453648 | Antiinflammatory activity in Wistar Han rat assessed as reduction in exudate volume at 5 mg/kg, ip administered 30 mins before carrageenan challenge | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID303572 | Analgesic activity in Swiss Albino mouse assessed as inhibition of acetic acid-induced writhing responses at 100 mg/kg, po after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID184600 | Acute toxicity evaluated as oral lethal dose in rat; Range is 12-25 | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID1204225 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 3 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID186469 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 0.1 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID183658 | Antiinflammatory activity was evaluated by carrageenan induced rat paw edema (6 rats/ dose) at peroral dose of 10 mg/kg by inhibition of leukotriene B4 (LTB4) synthesis. | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8 | N-substituted oxazolo[5,4-b]pyridin-2(1H)-ones: a new class of non-opiate antinociceptive agents. |
AID679815 | TP_TRANSPORTER: biliary excretion in SD rat | 2000 | Pharmaceutical research, Apr, Volume: 17, Issue:4 | Pharmacokinetic study of the hepatobiliary transport of indomethacin. |
AID1576182 | Nephrotoxicity in rat assessed as effect on proximal tubule at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID492305 | Analgesic activity against formalin-induced acute pain in Swiss mouse assessed inhibition of nociception at 100 umol/kg, po administered 40 mins before formalin challenge measured for 15 to 30 mins relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates. |
AID591668 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 mM after 60 mins by HPLC analysis | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID228173 | In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1510605 | Inhibition of alpha-chymotrypsin in bovine pancreas using SPpNA as substrate pretreated with enzyme for 30 mins followed by substrate addition and measured for 12 mins by spectrophotometric analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors. |
AID679816 | TP_TRANSPORTER: biliary excretion in EHBR rat | 2000 | Pharmaceutical research, Apr, Volume: 17, Issue:4 | Pharmacokinetic study of the hepatobiliary transport of indomethacin. |
AID1357039 | Inhibition of ovine COX1 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID1783299 | Analgesic activity against p-benzoquinone induced writhing in albino rat model assessed as protection rate at 28 uM/kg, ip measured after 30 mins relative to control | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID304238 | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 0.1 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID287290 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 100 mg/kg, po after 270 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1453447 | Anti-inflammatory activity in rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, po measured after 5 hrs by plethysmographic method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Synthesis of methanesulphonamido-benzimidazole derivatives as gastro-sparing antiinflammatory agents with antioxidant effect. |
AID492145 | Agonist activity at human PPARgamma expressed in Escherichia coli BL21 assessed as stimulation of binding between receptor and steroid receptor coactivator-1 at 320 uM by ELISA relative to untreated control | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
AID1293531 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 3 hrs before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID415884 | Antipyretic activity against brewer's yeast-induced hyperthermia in Wistar rat assessed as change in rectal temperature at 5 mg/kg, po after 90 mins | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and spectral characterization of a new class of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-ones: antimicrobial, analgesic and antipyretic studies. |
AID747923 | Irreversible inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID467611 | Dissociation constant, pKa of the compound | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID195801 | Anti-inflammatory activity against carrageenan-induced paw edema in female rats relative to phenylbutazone by p.o. administration. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids. |
AID182047 | In vivo inhibition of contralateral paw swelling after oral treatment for 28 days (1 mg/kg od) was determined by adjuvabt arthritis in rat | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID160888 | Tested for Prostaglandin synthetase inhibition in Bovine seminal vesicle microsomes using Beckman liquid scintillation counter at 10 e-5 M | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID1846836 | Analgesic activity in albino Wistar mouse assessed as increase in reaction on paw licking at 100 mg/kg, po pretreated for 1 hrs followed by hot plate treatment measured after 90 mins by analgesiometer based analysis relative to control | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Contemporary advances of cyclic molecules proposed for inflammation. |
AID1254089 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, ip administered 30 mins before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID183128 | Inhibition of secondary paw swelling in rat adjuvant arthritis model | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID223907 | Antiinflammatory activity dosed orally against D-adjuvant arthritis in rat. | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2 | Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents. |
AID1150259 | Antiinflammatory activity in rat with prolonged phase of inflammation assessed as inhibition of adjuvant-carrageenan-induced paw edema at 2 mg/kg, po relative to control | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID1316778 | Analgesic activity in rat assessed as reversal of complete Freund's adjuvant-induced mechanical hyperalgesia at 30 mg/kg, po after 3 hrs relative to control | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. |
AID1359543 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as reduction in nitrite level at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge by Griess assay relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID183644 | Antiinflammatory activity was evaluated by the inhibition of rat carrageenan foot edema (CFE) assay at the dose of 3 mg/kg | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. |
AID1852346 | Protection against LPS/ hypoxia induced cell injury in rat H9c2 cells assessed as recovery of cell viability at 1 to 10 uM by CCK-8 assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1743648 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID116838 | Antirheumatic effect was determined in mice after combined treatment of TAS-202 (30 mg/kg/day) and indomethacin (1 mg/kg/day) at day 14 | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Synthesis of a magnosalin derivative, 4-(3,4,5-trimethoxyphenyl)-6-(2,4,5-trimethoxyphenyl)-2-diethylaminopyrimidine, and the anti-angiogenic and anti-rheumatic effect on mice by oral administration. |
AID1689621 | Analgesic activity in albino mouse assessed as protection against acetic acid-induced writhing at 0.028 mM/kg, po pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to control | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID1819027 | Antiinflammatory activity in transgenic fluorescent zebrafish expressing EGFP assessed as reduction in CuSO4 induced number of macrophages surrounding the neuromast at 20 uM preincubated for 2 hrs followed by Cuso4 addition and measured after 1 hr by fluo | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Dolabellane Diterpenes and Elemane Alkaloids from the Soft Coral |
AID1220239 | Unbound intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID77213 | Tested for effect on the production of cyclooxygenase (COX) metabolite, PGE-2 (prostaglandin E2) of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID176243 | Inhibitory effect for increase in plasma prostaglandin E2 (PGE2) level after arachidonic acid (AA) injection intoCOX-1 non-lipopolysaccharide-treated rats | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID186442 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 0.1 mg/kg at time interval- 4 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID225628 | Antiinflammatory activity dosed orally against carrageenan induced rat paw edema(CPE) | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2 | Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents. |
AID1134895 | Inhibition of prostaglandin synthetase (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID397227 | Inhibition of ovine COX2 at 10 uM by enzyme immunoassay relative to control | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and biological evaluation of 4,5-diphenyloxazolone derivatives on route towards selective COX-2 inhibitors. |
AID1737599 | Antiinflammatory activity in Wistar rat model of carrageenan-induced paw edema assessed as reduction in thickness of paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr (Rvb = 2.41 +/-0.05 mm) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1199383 | Acute ulcerogenicity in male Wistar rat assessed as severity index measured as ulcer in stomach at 10 mg/kg, po after 17 hrs with normal diet | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres. |
AID303596 | Toxicity in 24 hrs fasted Wistar rat assessed as ulcer index at 30 mg/kg, po after 6 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID428417 | Inhibition of MRP1/MRP2 in White Wistar rat ileum assessed as increase in drug uptake at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID287089 | Antiinflammatory activity in ICR mouse assessed as inhibition of TPA-induced edema per ear applied topically 30 mins before TPA treatment | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Triterpene glycosides from the flower petals of sunflower (Helianthus annuus) and their anti-inflammatory activity. |
AID178375 | Effective dose against carrageenan edema(peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID386852 | Antiinflammatory activity in Wistar rat assessed as inhibition of formalin-induced paw oedema volume at 10 mg/kg, po administered 30 mins before formalin challenge after 2 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID1902042 | Inhibition of full-length ovine COX-1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID409551 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 1 hr | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID675142 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 10 mg/kg, po administered 60 mins before carrageenan challenge measured after 3 hr (Rvb = 96.2 +/- 2.5 mL) | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
AID1062926 | Gastrointestinal toxicity in albino rat carrageenan-induced paw edema model assessed as acute inflammatory cell infiltrating its whole thickness at 0.28 mmol/kg, po by hematoxylin and eosin staining-based light microscopic analysis | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID186597 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 10 mg/kg at time interval- 4 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1193883 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema administered 30 mins prior to carrageenan challenge measured after 2 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Rapid 'one-pot' synthesis of a novel benzimidazole-5-carboxylate and its hydrazone derivatives as potential anti-inflammatory and antimicrobial agents. |
AID1241854 | Hepato-toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as SGPT level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 34.23 +/- 2.5 U/mL) | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID549590 | Antiinflammatory activity in CD1 mouse assessed as inhibition of croton oil-induced ear edema per cm'2 administered topically | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives. |
AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1177984 | Inhibition of ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug. |
AID178373 | Effective dose against analgesic activity (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID751120 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip measured at 3 hrs by plethysmometric analysis relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID1149350 | Antiinflammatory activity in po dosed Wistar rat assessed as inhibition of carrageenan-induced paw edema administered 1 hr prior to carrageenan challenge measured 3 hrs post-carrageenan injection | 1977 | Journal of medicinal chemistry, Jan, Volume: 20, Issue:1 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 1. 6,11-Dihydro-11-oxodibenz]b,e]oxepin-2-acetic acids. |
AID1254091 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 2 hrs before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID1737613 | Ulcerogenic activity in fasted albino mouse assessed as ulcer index in gastric mucosa at 10 mg/kg, po for 3 days (Rvb = 0 No_unit) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID499199 | Inhibition of COX1 | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases. |
AID234944 | Ratio of IC50 for COX-1 and COX-2 binding inhibitors | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors. |
AID591642 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 mM after 30 mins by HPLC analysis | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID287337 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 10 mg/kg, po after 90 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1357044 | Inhibition of COX2 in human whole blood assessed as reduction in LPS-stimulated PGE2 production at 1 uM pre-incubated for 15 mins before LPSaddition and measured after 18 hrs by ELISA relative to control | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID364549 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip after 2 hrs | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives. |
AID611096 | Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID675696 | Inhibition of COX2 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold. |
AID356055 | Antiinflammatory activity against carrageenan-induced Swiss mouse paw edema assessed as inhibition of paw volume at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs relative to control | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID132669 | In vitro inhibition of electrically stimulated contractions of isolated mouse vas deferens. | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
AID729242 | Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID1171107 | Hepatotoxicity in Swiss mouse assessed as plasma AST level at 2.5 mg/kg, po daily for 7 days | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Pimaradienoic acid inhibits inflammatory pain: inhibition of NF-κB activation and cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID729250 | Inhibition of ovine COX1 by discontinuous radioactive TLC assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID136457 | Compound was evaluated for the percent reduction of carrageenan induced edema in mice at dose of 3.0 mg/kg | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID1254094 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 5 hrs before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID386845 | Acute toxicity in po dosed albino mouse after 24 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID138594 | Inhibition of arachidonic acid induced mouse ear edema at 30 ug/ear | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | 3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors. |
AID193992 | Gastrointestinal tolerability was evaluated in rats and compound dose that causes lethality was reported. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID1815260 | Antiviral activity against Canine coronavirus infected in dog A-72 cells assessed as inhibition of viral replication | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID753749 | Gastrointestinal toxicity in albino rat assessed as decreased in thickness with marked loss of mucosal membrane at areas of ulceration at 0.28 mmol/kg, po using haematoxylin and eosin staining by light microscopic analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID303567 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 4 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1545421 | Analgesic activity in Swiss albino mouse assessed as protection against acetic acid-induced writhing at 15 mg/kg, po pretreated for 30 mins followed by acetic acid challenge and measured after 20 mins relative to control | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
AID1220801 | Drug metabolism in bile duct-cannulated dog assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID1852361 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as reduction of IL-1 beta protein expression at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1435528 | Anti-inflammatory activity in TPA-induced CD1 mouse ear acute inflammation model assessed as reduction in TPA-induced ear edema administered topically 10 mins prior to TPA challenge measured after 4 hrs | 2016 | Journal of natural products, 11-23, Volume: 79, Issue:11 | Terpenoids from Melampodium perfoliatum. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID190366 | Compound was tested for intestinal ulcerogenic effect in rats at a dose of 10 mg/kg | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents. |
AID1150275 | Acute toxicity in po dosed rat after 7 days | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1501868 | Selectivity index, ratio of IC50 for human COX2 to IC50 for AKR1C3 (unknown origin) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach. |
AID186586 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 0.1 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1713247 | Inhibition of ovine COX-1 assessed as appearance of oxidized TMPD level by EIA method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: Synthesis, biological activities in vitro and docking study. |
AID332061 | Inhibition of TPA-induced inflammation in mouse assessed per ear by edema assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | New anti-inflammatory ergostane-type ecdysteroids from the sclerotium of Polyporus umbellatus. |
AID303576 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 3 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID428415 | Inhibition of MRP1/MRP2 in White Wistar rat colon assessed as permeability at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID185017 | Minimum effective dose against adjuvant arthritis on administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1359545 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as reduction in PGE2 level at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge by ELISA relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID1624749 | Antiinflammatory activity in Fisher 344 rat model of carrageenan-induced edema assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip dosed simultaneously with carrageenan injection relative to control | 2019 | Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4 | New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment. |
AID1764402 | Unbound brain-to-plasma concentration ratio in P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID1532673 | In vitro anti-inflammatory activity at 100 mg/ml incubated for 15 mins followed by heating for 10 mins and cooling by albumin denaturation assay relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Anti-inflammatory activity of triazine derivatives: A systematic review. |
AID1852444 | Toxicity in Wistar rat assessed as change in BUN level in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1237266 | Inhibition of COX2 (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Synthesis and characterization of novel oxazines and demonstration that they specifically target cyclooxygenase 2. |
AID194778 | Percent inhibition after administration at 2 mg/kg perorally using carrageenan induced rat paw edema method | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Nonsteroidal antiinflammatory agents. 3. Synthesis of the positional isomers of 4'-chloro-5-methoxy-3-biphenylylacetic acid and their antiinflammatory and analgesic activities. |
AID1405602 | Cytotoxicity against C57BL6 mouse peritoneal cells assessed as cell viability measured at 5 hrs time interval by LDH release assay (Rvb = 98.9 +/- 1.6%) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Influence of the C-5 substitution in polysubstituted pyrimidines on inhibition of prostaglandin E |
AID729249 | Inhibition of wild type mouse COX2 by discontinuous radioactive TLC assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID287233 | Antiinflammatory effect on carrageenan-induced paw oedema Sprague-Dawley rat assessed as reduction of paw oedema at 10 mg/kg, ip | 2007 | European journal of medicinal chemistry, Feb, Volume: 42, Issue:2 | Synthesis, antimicrobial, and anti-inflammatory activities of novel 2-(1-adamantyl)-5-substituted-1,3,4-oxadiazoles and 2-(1-adamantylamino)-5-substituted-1,3,4-thiadiazoles. |
AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID196176 | Effect on non perforated ulcers(NPU) at the dose of 10 mg/kg. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID412946 | Inhibition of ovine COX1 assessed as remaining activity at 10 uM relative to control | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. |
AID1209582 | Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID1852422 | Antiinflammatory activity against LPS/talc powder induced pericarditic Wistar rat assessed as reduction in heart swelling at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-oxo-5-((5-su | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID160737 | Inhibitory activity against Prostaglandin G/H synthase 2 obtained from sheep placenta | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid. |
AID1662945 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, ip relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID176481 | Chronic gastrointestinal erosive activity in male rats by the oral administration was determined. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids. |
AID1502659 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 3,5-Dimethylorsellinic Acid Derived Meroterpenoids from Penicillium chrysogenum MT-12, an Endophytic Fungus Isolated from Huperzia serrata. |
AID355225 | Inhibition of cyclooxygenase assessed as rate of disappearance of dissolved oxygen at 2.4 uM relative to control | 1997 | Journal of natural products, Apr, Volume: 60, Issue:4 | Modulation of lipoxygenase activity by bacterial hopanoids. |
AID179689 | Percentage of gastric damage was measured in rats. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID177772 | Analgesic activity on peroral administration against Bradykinin induced pain in rat paw | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
AID681851 | TP_TRANSPORTER: inhibition of Digoxin uptake (Digoxin: 0.05 uM, Indomethacin: 1000 uM) in Oatp2-expressing LLC-PK1 cells | 2002 | Pharmaceutical research, Feb, Volume: 19, Issue:2 | Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. |
AID1237663 | Anti-nociceptive activity in Swiss mouse assessed as reduction in paw licking response during inflammatory phase at 10 umol/kg, ip dosed 40 mins before formalin injection | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of the anti-nociceptive and anti-inflammatory activity of 4-aminoquinoline derivatives. |
AID1784597 | Antiinflammatory activity in human HBE cells assessed as inhibition of LPS-induced IL-8 production at 5 uM pretreated with compound for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury. |
AID193129 | inhibition of swelling in rat paw edema was measured at a dose of 1.4 micro mol/kg/day for days 14-25 | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID645026 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 3 hrs by plethysmometer relative to control | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents. |
AID1416042 | Binding affinity to calf thymus DNA by isothermal calorimetric titration method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID303591 | Antiarthritic activity against adjuvant-induced arthritis in Wistar rat assessed as inhibition of paw edema at 10 mg/kg, po on day 3 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1136203 | Analgesic activity in po dosed rat assessed as inhibition of yeast-induced inflammatory pain | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Novel analgesic-antiinflammatory salicylates. |
AID185238 | Percent inhibition of pleural inflammation in carrageenan-induced rat model was determined by comparing with vehicle control group when tested on 10 rats at peroral dose of 100 umol/Kg | 1998 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2 | Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole. |
AID92239 | Inhibition of arachidonic acid (AA) induced human platelet aggregation | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Synthetic aci-reductones: 3,4-dihydroxy-2H-1-benzopyran-2-ones and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers. Antiaggregatory, antilipidemic, and redox properties compared to those of the 4-substituted 2-hydroxytetronic acids. |
AID1700037 | Inhibition of LPS-induced NO production in mouse RAW264.7 cells assessed as NO production activity at 10 uM by Griess reagent based assay | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Design, synthesis and biological evaluation of novel osthole-based derivatives as potential neuroprotective agents. |
AID177019 | Antiinflammatory activity was evaluated in rat carrageenan foot edema assay in experiment 2 | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID376764 | Inhibition of sheep placental COX2 by liquid scintillation counter | 2005 | Journal of natural products, Jan, Volume: 68, Issue:1 | Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2. |
AID640134 | Down regulation of COX-2 protein expression in carrageenan-stimulated ICR mouse at 10 mg/kg, ip measured after 5 hrs by Western blot analysis | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID161604 | Tested for in vitro inhibition of collagen-induced aggregation of human platelets | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Synthesis and biological activity of 5-(4-chlorobenzoyl)-4-(hydroxymethyl)-1-methyl-1H-pyrrole-2-acetic acid, a major metabolite of zomepirac sodium. |
AID680790 | TP_TRANSPORTER: inhibition of glyburide accumulation in MRP2-expressing MDCK cells | |||
AID178491 | Antiinflammatory activity in the rat foot edema at the dose of 1.0-10 mg/kg po | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | 1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity. |
AID688454 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID178644 | Antiinflammatory activity by using Rat pyresis assay | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile. |
AID681036 | TP_TRANSPORTER: inhibition of Ochratoxin A uptake (OTA: 1 uM, Indomethacin: 200 uM) in OAT3-expressing S2 cells | 2001 | Life sciences, Sep-21, Volume: 69, Issue:18 | Characterization of ochratoxin A transport by human organic anion transporters. |
AID237685 | Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk). |
AID1591951 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of lipopolysaccharide-induced nitric oxide production incubated for 24 hrs coincubated with LPS by Griess reagent based assay | 2019 | Journal of natural products, 08-23, Volume: 82, Issue:8 | Ophiobolin-Type Sesterterpenoids from the Mangrove Endophytic Fungus |
AID184196 | In vivo effect on prostaglandin and leukotriene mediated production in rat pleural cavity was assessed by the inhibition of fluid volume in 5-lipoxygenase/ cyclooxygenase at dose 1.0 mg/kg | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents. |
AID1585084 | Antiinflammatory activity in mouse primary peritoneal macrophages assessed as inhibition of LPS-induced IL-6 production at 10 uM preincubated for 30 mins followed by LPS addition and measured after 24 hrs by ELISA relative to control | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Design, synthesis and biological evaluation of novel 2-sulfonylindoles as potential anti-inflammatory therapeutic agents for treatment of acute lung injury. |
AID128887 | Percent analgesia in phenylquinone writhing assay at 1 mg/kg | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID1810794 | Inhibition of COX1 in human whole blood assessed as reduction in calcium ionophore-stimulated TXB2 production by ELISA (Rvb = 1.80 ng/ml ) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID315580 | Antiinflammatory activity against croton oil-induced ear edema in mouse at 0.5 mg/ear | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. |
AID428389 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po treated for 30 mins measured after 2 hrs of carrageenan challenge | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. |
AID190163 | The compound was tested for gastric ulcerogenicity in rats; ca. 8 | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID128036 | Compound was tested for antianalgesic activity in mice after perorally administered at 1 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1737607 | Antiinflammatory activity in Wistar rat model of carrageenan-induced paw edema assessed as reduction in thickness of paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 24 hrs (Rvb = 0.83 +/-0.08 mm) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID209204 | Effect on production of eicosanoids from THP-1 cells stimulated with A-23187 using cellular assay on PGE-2, LTC-4 | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Pyrrolidine inhibitors of human cytosolic phospholipase A(2). |
AID481439 | Absolute bioavailability in human | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID674724 | Gastrointestinal toxicity in Wistar albino rat assessed as incidence of stomach ulceration at 0.029 mmol/kg, po followed by another two compound doses in second and third days measured on fourth day post dose by acute ulcerogenicity study | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID1663617 | Cytotoxicity against African green monkey COS7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis and anticancer activity of open-resorcinarene conjugates. |
AID1330206 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 25 mg/kg, po administered 2 hrs before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID172635 | Analgesic activity was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 12 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1125128 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs relative to control | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID763517 | Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha at 30 uM preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
AID337154 | Inhibition of carrageenan-induced edema in Wistar rat paw at 5 mg/kg, po | |||
AID1133360 | Analgesic activity against po dosed yeast-induced inflamed foot Sprague-Dawley rat model assessed as increase in pain threshold in inflamed paw measured after 2 hrs | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Analgesic activity of novel spiro heterocycles. 2-Amino-7-oxa-3-thia-1-azaspiro[5,5]undec-1-enes and related compounds. |
AID1178548 | Cmax in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID467613 | Volume of distribution at steady state in human | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID181586 | Percent Edema variation in Carrageenan-induced paw edema test at a dose of 5 mg/kg perorally in rats after 120 min | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID670255 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, ip dosed 30 mins before carrageenan challenge measured at 24 hrs post carrageenan challenge | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | In vitro stability and in vivo anti-inflammatory efficacy of synthetic jasmonates. |
AID1055827 | Ulcerogenicity in albino Wistar rat assessed as gastric superficial mucosal damage at 0.15 mmol/kg, po by hematoxylin and eosin staining-based assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1891748 | Induction of apoptosis in human MCF7 cells assessed as reduction in caspase-3 expression measured after 24 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID1601224 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as inhibition of ear edema at 0.5 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration relative to control | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID132251 | Inhibition of arachidonic acid oedema in mouse ear. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity. |
AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID161163 | Inhibition of Prostaglandin G/H synthase of ram seminal vesicle microsomes | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. |
AID352496 | Inhibition of ovine COX2 by enzyme immunoassay | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: synthesis, biological evaluation and nitric oxide release studies. |
AID732775 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs by plethysmometer analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and pharmacological evaluation of some novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles. |
AID751105 | Antiinflammatory activity in Swiss mouse assessed as inhibition of histamine-induced paw edema at 10 mg/kg, ip administered 30 mins prior to histamine challenge measured after 60 mins relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID1639500 | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production measured after 24 hrs | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Anti-inflammatory Mono- and Dimeric Sorbicillinoids from the Marine-Derived Fungus Trichoderma reesei 4670. |
AID1545420 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs by mercury plethysmometer relative to control | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
AID615924 | Antiinflammatory activity in Wistar albino rat assessed as reduction of carrageenan-induced paw volume at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 2 hrs relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, characterization and pharmacological activity of 4-{[1-substituted aminomethyl-4-arylideneamino-5-sulfanyl-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl}-2H-1,4-benzothiazin-3(4H)-ones. |
AID1351159 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA (Rvb = 21561.3 +/- 85 | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID1139565 | Inhibition of ovine COX1 using arachidonic acid at 10 uM after 5 mins by HPLC analysis | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase. |
AID1062928 | Gastrointestinal toxicity in albino rat carrageenan-induced paw edema model assessed as severe atrophic gastritis and gland atrophy at 0.28 mmol/kg, po by hematoxylin and eosin staining-based light microscopic analysis | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID1519091 | Selectivity index, ratio of IC50 for inhibition of human COX1 to IC50 for inhibition of human COX2 | |||
AID170862 | Percent changes of hind paw edema and severity scores compared to control animals at 1.4 micro mol/kg/day | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID128860 | Acute toxicity was evaluated as number of mice died (tested = 7) after 72nd hour when 12 mg/kg is administered intraperitoneally | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1416040 | Binding affinity to calf thymus DNA assessed as Stern-Volmer quenching constant at 50 uM at pH 7.2 by spectrofluorophotometric method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID1174766 | Antioxidant activity in Wistar rat assessed as catalase level measured per mg of protein at 150 umol/kg, po administered for 3 days measured on day 4 (Rvb = 22.14 +/- 1.19 umol) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Benzimidazole--ibuprofen/mesalamine conjugates: potential candidates for multifactorial diseases. |
AID1178551 | Tmax in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID604023 | Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID172777 | Animals with Ulcers in Carrageenan-induced paw edema test at a dose of 5 mg/kg perorally in rats | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID1359541 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as reduction in TNFalpha level at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge by ELISA relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
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AID243653 | Percentage inhibition of Prostaglandin G/H synthase 2 in murine J774 cells at 1 uM | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | 1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors. |
AID604949 | Partition coefficient, log P of the compound by reverse phase HPLC analysis | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | 1-(5-Carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α: effect of substituents in position 3 of the indole scaffold on inhibitory potency, metabolic stability, solubility, and bioavailability. |
AID235767 | Ratio of UD50 to that of ED50 | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID420032 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 50 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 2 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID177071 | Compound was evaluated for efficacy in rat paw edema assay upon oral administration | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors. |
AID1192219 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 4 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID389640 | Antiinflammatory activity against carrageenan-induced paw edema in ICR mouse at 4 mg/kg, ip administered 30 mins before carrageenan challenge assessed after 4 hrs | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Anti-inflammatory activities of furanoditerpenoids and other constituents from Fibraurea tinctoria. |
AID310933 | Permeability across PAMPA membrane after 7 hrs | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
AID336479 | Inhibition of COX1 by scintillation proximity assay | 2002 | Journal of natural products, Nov, Volume: 65, Issue:11 | Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. |
AID409546 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 6 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID289296 | Inhibition of carrageenan-induced hind paw oedema in Swiss Albino mouse at 100 mg/kg, po after 180 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID209205 | Inhibition of arachidonic acid production from THP-1 cells stimulated with A-23187 using cellular assay | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Pyrrolidine inhibitors of human cytosolic phospholipase A(2). |
AID751116 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip measured at 4 hrs by plethysmometric analysis relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID1815257 | Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as inhibition of viral replication measured after 48 hrs by yield reduction assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID648872 | Ulcerogenic effect in rat assessed as gastric ulcer overall length at 0.08 mmol/kg, po administered for 6 hrs | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs. |
AID732776 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs by plethysmometer analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and pharmacological evaluation of some novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles. |
AID1739495 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2 | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases. |
AID174431 | Plasma drug level was measured in rat yeast induced hyperalgesia assay in presence of indomethacin at a dose of 10 mg/kg for 24 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID355124 | Inhibition of arachidonic acid-induced platelet aggregation in rabbit platelet-rich blood by turbidimetric method | 1996 | Journal of natural products, Dec, Volume: 59, Issue:12 | Antiplatelet arylnaphthalide lignans from Justicia procumbens. |
AID189998 | Dose which produced lesions in 50% of the treated animals | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID379636 | Inhibition of COX1 in ram seminal vesicle microsomes assessed as reduction of PGE2 formation | 2000 | Journal of natural products, Mar, Volume: 63, Issue:3 | Two new prenylated 3-benzoxepin derivatives as cyclooxygenase inhibitors from Perilla frutescens var. acuta. |
AID1891738 | Cytotoxicity against human RPE-1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID537733 | Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
AID1174284 | Antiinflammatory activity in Sprague-Dawley rat model of LPS-induced sepsis assessed as serum MDA level at 5 mg/kg/day dosed through gastric intubation for 6 days (Rvb = 4.7 +/- 2.8 mg/L) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents. |
AID774820 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 1 hr before carrageenan challenge measured at 4 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Design, synthesis and biological evaluation of novel anti-cytokine 1,2,4-triazine derivatives. |
AID1433579 | Thermodynamic solubility of the compound in phosphate buffer at pH 7.4 at 1 mg sonicated for 10 mins measured after 20 hrs by reverse phase HPLC analysis | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A |
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AID74199 | Antiinflammatory activity evaluated as Minimum effective oral dose that inhibits dextran UV erythema in guinea pig | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID179509 | Compound was evaluated for percentage recovery from GAG in adjuvant-induced arthritic model of rat at a dose of 2 mg/kg | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. |
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AID1592998 | Inhibition of human recombinant COX2 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones. |
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AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
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AID430146 | Antiinflammatory activity against bradykinin-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before bradykinin challenge measured after 60 mins by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID1854715 | Antiinflammatory activity in LPS-stimulated mouse BV-2 cells assessed as inhibition of IL-6 release at 10 uM and measured after 8 hrs by ELISA | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
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AID420035 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 1 hr | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID1616664 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs followed by LPS challenge and measured after 12 hrs by Griess assay | 2019 | Journal of natural products, 10-25, Volume: 82, Issue:10 | Bipolaricins A-I, Ophiobolin-Type Tetracyclic Sesterterpenes from a Phytopathogenic |
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AID1737620 | Analgesic activity in albino mouse assessed protection against acetic acid-induced abdominal writhing at 10 mg/kg, ip pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to ind | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
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AID1576311 | Antiinflammatory activity against carrageenan-induced air pouch inflammatory Swiss mouse model assessed as inhibition of PMNL cell migration in air pouch at 10 mg/kg, po treated 1 hr prior to carrageenan administration and measured after 6 hrs relative to | 2019 | MedChemComm, Nov-01, Volume: 10, Issue:11 | Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives. |
AID161609 | Effect on the synthesis of Thromboxane A2 at dose of 20 uM | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid. |
AID547630 | Selectivity ratio of IC50 for human recombinant COX2 to IC50 for human platelets COX1 | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID453650 | Antiinflammatory activity in Wistar Han rat assessed as reduction in inflammatory cell numbers at 5 mg/kg, ip administered 30 mins before carrageenan challenge | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID481938 | Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 100 uM by flow cytometry | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells. |
AID1815259 | Antiviral activity against SARS-CoV infected in African green monkey Vero E6 cells assessed as inhibition of viral replication | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
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AID1542243 | Selectivity index, ratio of IC50 of ovine COX-1 to IC50 of ovine COX-2 | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
AID178910 | Reduction in leukocyte numbers in rat pleural RPAR exudate; Nonactive. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | 2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents. |
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AID1241848 | Gastro-intestinal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as ulcer index at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID322005 | Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 10 mg/kg, po after 4 hrs | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones. |
AID1150257 | Antiinflammatory activity in rat with acute phase of inflammation assessed as inhibition of adjuvant-carrageenan-induced paw edema at 2 mg/kg, po relative to control | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID162177 | In vitro inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
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AID1267732 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1 | ent-Abietane-type diterpenoids from the roots of Euphorbia ebracteolata with their inhibitory activities on LPS-induced NO production in RAW 264.7 macrophages. |
AID724352 | Toxicity against Fischer-344 rat up to 0.1 mmol/kg, ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Syntheses and evaluation of the antioxidant activity of novel methoxypsoralen derivatives. |
AID767618 | Antinociceptive activity in po dosed Albino-Swiss mouse assessed as acetic acid-induced abdominal writhing compound administered 30 mins prior challenge measured over 30 mins post acetic acid challenge | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | High analgesic and anti-inflammatory in vivo activities of six new hybrids NSAIAs tetrahydropyran derivatives. |
AID399403 | Selectivity ratio of IC50 for sheep placental cotyledons COX2 to IC50 for bovine seminal microsomal COX1 | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. |
AID1353372 | Anti-inflammatory activity in po dosed Swiss mouse assessed as reduction in carrageenan-induced paw edema pretreated for 1 hr followed by carrageenan injection and measured after 1 to 5 hrs by plethysmometric method | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
AID1156826 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID1852351 | Protection against LPS/hypoxia induced apoptosis in rat H9c2 cells assessed as reduction in green fluorescence by confocal microscopy analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID400126 | Inhibition of COX1 | 1998 | Journal of natural products, Mar, Volume: 61, Issue:3 | 5-Lipoxygenase and cyclooxygenase-1 inhibitory active compounds from Atractylodes lancea. |
AID1501867 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for AKR1C3 (unknown origin) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach. |
AID314422 | Analgesic activity in rat assessed as reversal of CFA-induced hyperalgesia at 3 mg/kg, po after 2 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Imidazopyridines: a novel class of hNav1.7 channel blockers. |
AID464500 | Inhibition of mouse COX2 | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1262453 | Gastrointestinal toxicity in rat assessed as ulcer incidence at 100 mg/kg | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors. |
AID134423 | Compound was evaluated for the toxicity in mice | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID1464067 | Ulcerogenic activity in Wistar albino rat assessed as loss of mucous in stomach after 48 hrs by hematoxylin and eosin staining based microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18 | Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids. |
AID313126 | Inhibition of COX1 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Structural and functional basis of cyclooxygenase inhibition. |
AID1852387 | Inhibition of COX-2 (unknown origin) | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID546254 | Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors. |
AID399411 | Inhibition of bovine seminal vesicle microsomal COX1-mediated prostaglandin production | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Two new isoflavones from Ceiba pentandra and their effect on cyclooxygenase-catalyzed prostaglandin biosynthesis. |
AID115240 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 4 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID453203 | Lipophilicity, log D of the compound | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay. |
AID1180665 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma plus LPS-induced NO production | 2014 | Journal of natural products, Jul-25, Volume: 77, Issue:7 | Cytotoxic and anti-inflammatory prenylated benzoylphloroglucinols and xanthones from the twigs of Garcinia esculenta. |
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AID1251039 | Inhibition of COX2 (unknown origin) assessed as PGH2 production at 10 uM by measuring PGH2alpha level by enzyme immunoassay | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis. |
AID77220 | Tested for effect on the production of cyclooxygenase (COX) metabolite, TXB2 of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID237416 | Distribution coeeficient for the compound at pH7.4 (Log D7.4) | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction. |
AID196726 | In vivo antiinflammatory activity against edema formation in the noninjected(secondary) paw of the rat (before edema stimulation) at dose 2.0 mg/kg | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents. |
AID1852357 | Inhibition of COX-2 in LPS/hypoxia induced rat H9c2 cells using arachidonic acid as substrate incubated for 5 mins by microplate reader method | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID178232 | Inhibition of pleural reverse passive Arthus reactions (exudate white blood cells (WBC)); No significant inhibition at 56 umol/kg (Inactive) | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | 3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation. |
AID1226814 | Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes. |
AID197598 | Lysozyme-conjugated prodrugs: in vitro stability at pH 7.4 | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Low molecular weight proteins as carriers for renal drug targeting. Preparation of drug-protein conjugates and drug-spacer derivatives and their catabolism in renal cortex homogenates and lysosomal lysates. |
AID1737602 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 2 hr relative to control (Rvb = 0.00 +/-0.03 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID488196 | Selectivity ratio of IC50 for COX2 in human whole blood to IC50 for COX1 in human whole blood | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID1220790 | Ratio of drug level in blood to plasma in rat | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID187056 | Compound was evaluated for its antiinflammatory activity by adjuvant-induced polyarthritis test in rats at a dosage of 1 mg/kg administered orally | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID22293 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID293408 | Antiinflammatory activity in Wister Albino rat assessed as inhibition of paw edema at 1.5 mg/kg, po after 3hrs | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5 | Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives. |
AID1891741 | Induction of mitochondrial outer membrane damage in human MCF7 cells assessed as morphological changes by measuring appearance of threadlike structure at IC50 measured after 24 hrs by mitotracker red based confocal microscopy | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID1783308 | Ulcerogenic activity in fasted albino rat assessed as severity of ulcers at 28 uM/kg, po administered for 3 consecutive days (Rvb = 0 %) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID322004 | Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 10 mg/kg, po after 3 hrs | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Synthesis, analgesic, anti-inflammatory, and antimicrobial activity of some novel pyrimido[4,5-b]quinolin-4-ones. |
AID647940 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced iNOS protein expression in paw at 10 mg/kg, ip administered 30 mins before carrageenan challenge by Western blotting relative to control | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID1063319 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 12 hrs by ELISA (Rvb = 13.9 +/- 2.6 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID409565 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema volume at 10 mg/kg, po administered 60 mins before carrageenan challenge after 3 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID177545 | Ability to inhibit Carrageenan-induced paw edema in rat administered perorally | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 4. Synthesis and evaluation of 4-(4,10-dihydro-10-oxothieno[3,2-c] [1]benzoxepin-8-yl)butanol and -butyric acid and related derivatives. |
AID131689 | Effective dose for analgesic activity in mice | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID241918 | In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | 1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors. |
AID1178550 | AUC (0 to infinity) in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID1220788 | Fraction unbound in human plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID397003 | Antiinflammatory activity against carrageenan-induced inflammation in albino rat 6-day-old air pouch model assessed as inhibition of PGE2 level at 10 mg/kg, po administered prior to carrageenan challenge measured after 6 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Facile synthesis of bis(4,5-dihydro-1H-pyrazole-1-carboxamides) and their thio-analogues of potential PGE(2) inhibitory properties. |
AID1055830 | Antinociceptive activity in albino Wistar rat assessed as thermal-stimulus induced tail flick latency at 0.05 mmol/kg, po after 60 mins (Rvb = 2.54 +/- 0.05 mins) | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID568009 | Inhibition of glyoxalase 1 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Identification of curcumin derivatives as human glyoxalase I inhibitors: A combination of biological evaluation, molecular docking, 3D-QSAR and molecular dynamics simulation studies. |
AID541261 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip administered simultaneously with carrageenan | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | 1,5-Benzoxazepines vs 1,5-benzodiazepines. one-pot microwave-assisted synthesis and evaluation for antioxidant activity and lipid peroxidation inhibition. |
AID1055828 | Ulcerogenicity in albino Wistar rat assessed as gastric surface epithelial damage at 0.15 mmol/kg, po by hematoxylin and eosin staining-based assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID1576171 | Ulcerogenic activity in rat assessed as incidence of gastric ulceration at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days relative to control | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1866131 | Anti-inflammatory activity against TPA-induced auricular edema CD-1 mouse model assessed as inhibition of ear edema at 1 mg per ear applied immediately after TPA application and measured after 4 hrs relative to control | 2022 | Journal of natural products, 04-22, Volume: 85, Issue:4 | Synthesis, Biological Evaluation, and Molecular Docking Study of 3-Amino and 3-Hydroxy- |
AID1067406 | Inhibition of ovine COX2 by peroxidase activity-based colorimetric assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles. |
AID274904 | Activity at COX1 assessed as inhibition of arachidonic acid-induced PGE2 production in J774 cells at 10 uM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage. |
AID1437463 | Ulcerogenic effect in albino rat assessed as lymphocytic infiltration at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID168049 | Ability of compound to cause gastric ulcerogenicity was determined in rats at 5 mg/kg when administered daily once | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives. |
AID415882 | Antipyretic activity against brewer's yeast-induced hyperthermia in Wistar rat assessed as change in rectal temperature at 5 mg/kg, po after 30 mins | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and spectral characterization of a new class of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-ones: antimicrobial, analgesic and antipyretic studies. |
AID591438 | Antiinflammatory activity against acetic acid-induced vascular permeability in ICR mouse assessed as evans blue peritoneal leakage at 10 mg/kg, ip administered 30 mins before acetic acid challenge measured after 50 mins | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID1055538 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs by plethysmometer | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis, biological evaluation and molecular modeling study of 5-trifluoromethyl-Δ²-pyrazoline and isomeric 5/3-trifluoromethylpyrazole derivatives as anti-inflammatory agents. |
AID1452924 | Inhibition of recombinant human COX-2 assessed as reduction in PGH2 production using arachidonic acid as substrate preincubated for 5 mins followed by substrate and hematin addition measured after 2 mins by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and mechanistic evaluation of novel N'-benzylidene-carbohydrazide-1H-pyrazolo[3,4-b]pyridine derivatives as non-anionic antiplatelet agents. |
AID1498926 | Antiinflammatory activity in Wistar rat assessed as inhibition of formalin-induced paw oedema at 20 mg/kg, po pretreated for 1 hr followed by formalin addition measured up to 6 hrs post dose by plethysmographic method relative to control | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
AID196724 | In vivo antiinflammatory activity against edema formation in the noninjected(secondary) paw of the rat (after edema stimulation) at dose 2.0 mg/kg | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents. |
AID592744 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID393852 | Gastrointestinal toxicity in albino rat assessed as ulcer index at 100 mg/kg, po after 6 hrs | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. |
AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID131340 | Dose giving one-half of average maximal [40%] response in phenylquinone writhing assay | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID34329 | Inhibition of Aldose reductase (AR) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Discovery of novel aldose reductase inhibitors using a protein structure-based approach: 3D-database search followed by design and synthesis. |
AID162494 | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID184504 | Antiinflammatory activity was assessed in therapeutic adjuvant induced polyarthritis(AIP) test after po administration. | 1982 | Journal of medicinal chemistry, Jan, Volume: 25, Issue:1 | Isoxicam and related 4-hydroxy-N-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides. Potent nonsteroidal antiinflammatory agents. |
AID1810792 | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID183034 | Compound was tested for the inhibition of rat reversed passive Arthus pleurisy after peroral administration of 3 mg/kg dose at 0.59 mL of exudate volume with 0.55 mL of control (injected intrapleurally) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel synthesis and potent antiinflammatory activity of 4-hydroxy-2(1H)-oxo-1-phenyl-1,8-naphthyridine-3-carboxamides. |
AID678787 | TP_TRANSPORTER: inhibition of MTX uptake in Xenopus laevis oocytes | 2000 | European journal of pharmacology, Dec-01, Volume: 409, Issue:1 | Interaction between methotrexate and nonsteroidal anti-inflammatory drugs in organic anion transporter. |
AID634941 | Gastric toxicity in albino rat assessed as capillary inflammatory cells appearance at 100 mg/kg, po after 5 hrs by hematoxylin and eosin staining | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
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AID116672 | Analgesic activity was measured by phenylquinone writhing test in male Swiss albino mice at dose of 12 mg/Kg sc after 3h | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Synthesis of N-[[(substituted-phenyl)carbonyl]amino]-1,2,3,6-tetrahydropyridines with analgesic and hyperglycemic activity. |
AID177134 | In vivo antipyretic activity by endotoxin-induced rat pyresis assay. | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
AID190695 | Ulcerogenicity was measured in stomach during the 3 week adjuvant arthritis test.(animals with ulcers/animals in test) at 0.0014 mM/kg (0.50 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID271283 | Inhibition of COX1 assessed as TBX2 production in human whole blood | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID1783312 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2 | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID300447 | Antiinflammatory activity against carrageenan-induced hind paw oedema in mouse assessed as inhibition of swelling thickness at 10 mg/kg, po after 180 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | 1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities. |
AID1695503 | Antiinflammatory activity in ICR mouse model of carrageenan-induced paw edema assessed as paw edema inhibition rate at 22 mg/kg, po pretreated with compound followed by carrageenan challenge and measured after 1 hr post-treatment by dial thickness gage | 2020 | RSC medicinal chemistry, Jul-01, Volume: 11, Issue:7 | A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception. |
AID640120 | Antioxidant activity in carrageenan-stimulated ICR mouse assessed as increase in CAT activity at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1063316 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured by ELISA | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID1220785 | Fraction unbound in rat plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID1667500 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured at 0.5 hrs by calliper method (Rvb = 7.33 +/- 0.17 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID288829 | Gastric damage production in rat assessed as gastric ulcer index at 0.08 mmol/kg, po after 6 hrs | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies. |
AID1854723 | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID464513 | Selectivity ratio for IC50 for human BJ cells to IC50 for human HepG2 cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1737610 | Ulcerogenic activity in fasted albino mouse assessed as incidence of gastric ulceration at 10 mg/kg, po for 3 days (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID681882 | TP_TRANSPORTER: inhibition of bimane-GS efflux in the presence of Indomethacin at a concentration of 50uM in MRP4-expressing HepG2 cells | 2004 | The international journal of biochemistry & cell biology, Feb, Volume: 36, Issue:2 | Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione. |
AID620322 | Inhibition of COX1-mediated 12-HHT production in human platelet after 5 mins by HPLC analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Pyrazol-3-propanoic acid derivatives as novel inhibitors of leukotriene biosynthesis in human neutrophils. |
AID183657 | Antiinflammatory activity was evaluated by carrageenan induced rat paw edema (6 rats/ dose) at peroral dose of 10 mg/kg by inhibition of Prostaglandin E2 (PGE2). | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8 | N-substituted oxazolo[5,4-b]pyridin-2(1H)-ones: a new class of non-opiate antinociceptive agents. |
AID161485 | In vitro inhibitory activity against human whole cells Prostaglandin G/H synthase 1 | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID1743649 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID1695495 | Antiinflammatory activity in ICR mouse model of carrageenan-induced paw edema assessed as paw edema inhibition rate at 22 mg/kg, po pretreated with compound followed by carrageenan challenge and measured after 3 hrs post-treatment by dial thickness gage | 2020 | RSC medicinal chemistry, Jul-01, Volume: 11, Issue:7 | A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception. |
AID1193497 | Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID178473 | Antiinflammatory activity evaluated as Minimum effective oral dose that inhibits dextran paw edema in rat | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID682092 | TP_TRANSPORTER: uptake in Oatp1-expressing COS-7 cells | 2000 | Pharmaceutical research, Apr, Volume: 17, Issue:4 | Pharmacokinetic study of the hepatobiliary transport of indomethacin. |
AID1132865 | Antiinflammatory activity in po dosed Donryu rat assessed as inhibition of carrageenan-induced paw edema | 1978 | Journal of medicinal chemistry, Jul, Volume: 21, Issue:7 | Nonsteroidal antiinflammatory agents. 2. Derivatives/analogues of dibenz[b,e]oxepin-3-acetic acid. |
AID183914 | Inhibitory activity on carrageenan-induced paw edema in rats 3h after po administration of 5 mg/kg | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Nonsteroidal antiinflammatory agents. 2. Synthesis of 4',5-disubstituted 3-biphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities. |
AID7103 | Ability to inhibit 5-lipoxygenase by using a crude preparation of the cytosolic enzyme from the rat basophilic leukemia (RBL-1) cell line at a concentration of 25 uM | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity. |
AID271285 | Selectivity index, IC50 for COX1/IC50 for COX2 in human whole blood | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID1198262 | Antiproliferative activity against human U373MG cells assessed reduction in cell number at 10 uM incubated for 6 days by trypan blue dye exclusion dye based inverted microscopy | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Effect of new hybrids based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug on the growth of a human astrocytoma cell line (U373). |
AID210502 | Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of TXB2 formation) in rat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists. |
AID1667501 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured at 1 hr by calliper method (Rvb = 7.33 +/- 0.17 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID271288 | Selectivity index, IC50 for ovine COX1/IC50 for ovine COX2 | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID1359547 | Antiinflammatory activity in mouse assessed as inhibition of croton oil-induced ear edema at 0.5 mg/ear administered topically pretreated for 1 hr followed by croton oil addition and measured after 4 hrs relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
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AID502274 | Inhibition of sheep COX1 by enzyme immunoassay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors. |
AID6870 | Inhibition of 5-lipoxygenase in rat RBL-1 cells | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes. |
AID397232 | Inhibition of ovine COX1 by enzyme immunoassay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and biological evaluation of 4,5-diphenyloxazolone derivatives on route towards selective COX-2 inhibitors. |
AID209197 | Concentration required to inhibit production of PGE-2 from THP-1 cells stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID1674098 | Selectivity ratio of IC50 for AKR1C2 (unknown origin) to IC50 for AKR1C3 (unknown origin) | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Overview of AKR1C3: Inhibitor Achievements and Disease Insights. |
AID1385400 | Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization at >30 uM after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay relative to control | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID549588 | Antiinflammatory activity in CD1 mouse assessed as inhibition of croton oil-induced ear edema at 0.3 umol administered topically per cm'2 of ear relative to control | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives. |
AID110863 | Inhibitory activity against mouse uM/cm**2 (control=7.0) | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins. |
AID1783302 | Anti-inflammatory activity in Wistar albino rat model of carragenan-induced paw edema assessed as reduction in edema thickness at 28 uM/kg, ip measured after 2 hrs by plethysmometer (Rvb =1.6 +/- 0.12 millimeter) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID634940 | Gastric toxicity in albino rat assessed as degeneration of fundic gland at 100 mg/kg, po after 5 hrs by hematoxylin and eosin staining | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID274912 | Gastric damage in rat at 100 mg/kg, po by GI damage assay | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage. |
AID185156 | Compound was tested for intestinal Ulcerogenic effect in rats, activity expressed as lesion length | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents. |
AID1199421 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 5 hrs (Rvb = 1.70 +/- 0.020 ml) | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID535925 | Antiinflammatory activity in in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr before carrageenan challenge and measured 4 hrs post carrageenan challenge relative to untreated control | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines. |
AID1241872 | Analgesic activity in Swiss albino mouse assessed as reduction in formalin-induced paw licking by measuring time spent on licking during phase-1 at 10 mg/kg, po dosed 1 hr before formalin challenge and measured 30 mins after formalin injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1220789 | Ratio of drug level in blood to plasma in mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID184144 | Inhibition of carrageenan hind paw edema in rats after oral administration of a dose of 5 mg/kg | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID1498925 | Antiinflammatory activity in Holtzman rat assessed as inhibition of carrageenan-induced paw edema pretreated via oral gavage for 1 hr followed by carrageenan challenge relative to control | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
AID642875 | Inhibition of COX1 | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity. |
AID1241862 | Renal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as creatinine level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 0.62 +/- 0.049 m | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1450923 | Binding affinity to human serum albumin | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Peptide Half-Life Extension: Divalent, Small-Molecule Albumin Interactions Direct the Systemic Properties of Glucagon-Like Peptide 1 (GLP-1) Analogues. |
AID1918192 | Inhibition of human OAT2 tv.1 variant expressed in HEK293 cells assessed as inhibition of [3H]cGMP uptake by scintillation analysis | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment. |
AID115723 | The compound was evaluated for inhibition of edema induced by bradykinin at 100 micro g/mL | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID1416041 | Binding affinity to calf thymus DNA assessed as quenching constant at 50 uM at pH 7.2 by spectrofluorophotometric method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID1196212 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 2 hrs | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases. |
AID488194 | Inhibition of COX1 in human whole blood | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID188072 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 1 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 23rd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID134578 | Lethal dose evaluated in NPP assay | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID1232309 | Unbound fraction in human plasma | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID1359984 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 0.5 hrs by plethysmometer relative to control | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent. |
AID1193493 | Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID155359 | Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of PGE-2 formation) in rat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists. |
AID305971 | Antiinflammatory activity in neutrophil assessed as inhibition of fMLP induced elastase release | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents. |
AID172640 | Analgesic activity was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 8 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1192217 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 3 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID707119 | Hepatotoxicity in Swiss mouse assessed as change in plasma ALT level at 2.5 mg/kg, po for 7 days measured over 7 days relative to vehicle-treated control | 2012 | Journal of natural products, May-25, Volume: 75, Issue:5 | Kaurenoic acid from Sphagneticola trilobata Inhibits Inflammatory Pain: effect on cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID492143 | Antiinflammatory activity in NIH mouse assessed as inhibition of TPA-induced mouse ear edema measured per ear administered to right ear relative to untreated control | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Labdanes and sucrose esters from Physalis sordida. |
AID492147 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
AID1737604 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 3 hr relative to control (Rvb = 0.00 +/-0.1 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1737627 | Analgesic activity in albino mouse assessed as forepaw licking/jumping latency time at 10 mg/kg, ip measured after 120 mins by hot plate test (Rvb = 2.62 +/- 0.06 sec) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1359987 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 3 hrs by plethysmometer relative to control | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent. |
AID1902041 | Inhibition of human COX-2 at 50 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID1743651 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID527190 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production by MTT assay | 2010 | Journal of natural products, Oct-22, Volume: 73, Issue:10 | Diarylheptanoids from the Rhizomes of Curcuma kwangsiensis. |
AID360928 | Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | 2001 | Journal of natural products, Jun, Volume: 64, Issue:6 | Cox-2 inhibitory effects of naturally occurring and modified fatty acids. |
AID587449 | Inhibition of human recombinant COX-2 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies. |
AID1183331 | Inhibition of ovine COX1 using fluorometric substrate at 100 uM by fluorescent inhibitor screening assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core. |
AID187761 | Antiinflammatory activity evaluated by measuring % reduction of edema, 3h after oral administration of 5 mg/kg in carrageenan model | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID328205 | Inhibition of COX1 | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID34486 | Percentage inhibition of Aldose Reductase (AR) at a concentration of 5 ug/mL; Experiment 2 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Discovery of novel aldose reductase inhibitors using a protein structure-based approach: 3D-database search followed by design and synthesis. |
AID178593 | Effective dose determined against rat adjuvant arthritis after peroral administration | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Preparation and antiarthritic and analgesic activity of 4,5-diaryl-2-(substituted thio)-1H-imidazoles and their sulfoxides and sulfones. |
AID172651 | Animals with Hyperemia in Carrageenan-induced paw edema test at a dose of 5 mg/kg perorally in rats | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID675141 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 10 mg/kg, po administered 60 mins before carrageenan challenge measured after 2 hr (Rvb = 89.4 +/- 7.3 mL) | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
AID393659 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat assessed as inhibition of edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured after 2 hrs relative to control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Regioselective synthesis of dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones of potential anti-tumor properties. |
AID1409609 | Cytotoxicity of compound against Vero E6 cells by MTT assay. | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
AID477758 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 60 mins before carrageenan challenge measured after 270 mins | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents. |
AID1289451 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 1 hr followed by LPS stimulation measured after 20 hrs by Griess assay | 2016 | Journal of natural products, Jan-22, Volume: 79, Issue:1 | (±)-Homocrepidine A, a Pair of Anti-inflammatory Enantiomeric Octahydroindolizine Alkaloid Dimers from Dendrobium crepidatum. |
AID695144 | Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21 | Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors. |
AID1852429 | Antiinflammatory activity in LPS/talc powder induced pericarditic Wistar rat model assessed as increase in CK-MB level in serum at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-oxo-5- | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID161484 | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1 | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID178662 | Antiinflammatory activity was determined by measuring adjuvant-induced arthritis in rats using preventive method; Range is 0.2~0.3 (dose administered daily twice) | 2004 | Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4 | In vitro structure-activity relationship and in vivo studies for a novel class of cyclooxygenase-2 inhibitors: 5-aryl-2,2-dialkyl-4-phenyl-3(2H)furanone derivatives. |
AID446970 | Antiinflammatory activity in BALB/c mouse assessed as inhibition of carrageenan-induced paw edema at 200 mg/kg, po after 180 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of 3,6-disubstituted 7H-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines as novel analgesic/anti-inflammatory compounds. |
AID688452 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.30 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID314423 | Analgesic activity in rat assessed as reversal of CFA-induced hyperalgesia at 3 mg/kg, po after 4 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Imidazopyridines: a novel class of hNav1.7 channel blockers. |
AID1737600 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 1 hr relative to control (Rvb = 0.00 +/-0.02 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID289292 | Antiinflammatory activity against carrageenan-induced hind paw oedema in Swiss Albino mouse assessed as swelling thickeness at 100 mg/kg, po after 180 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID1199379 | Potency ratio of compound to Indomethacin for inhibition of carrageenan-induced paw edema in po dosed male Wistar rat | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres. |
AID1232307 | Lipophilicity, log P of the compound | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID477756 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 60 mins before carrageenan challenge measured after 90 mins | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents. |
AID580345 | Antiinflammatory activity against TPA-induced mouse edema model assessed as reduction in ear edema at 0.5 mg/ear | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents. |
AID1220795 | Plasma clearance in po dosed human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID1125134 | Ulcerogenic effect in albino rat assessed as apoptotic glandular epithelial cells using hematoxylin and eosin staining at 0.28 mmol/kg, po by light microscopic analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID1063326 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release at 10 uM treated 2 hrs before LPS challenge measured after 48 hrs by Griess assay relative to control | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID684465 | Inhibition of isolated ovine COX-1 at 10 uM by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19 | Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine. |
AID162651 | Inhibition of human Prostaglandin G/H synthase 2 | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID1576165 | Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 1 hr relative to control | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID641287 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced hind paw edema at 10 mg/kg, ip | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID736887 | Antiinflammatory activity in mouse assessed as inhibition of acetic acid-induced vascular permeability by measuring Evan's blue dye leakage at 100 mg/kg, po administered 1 hr before acetic acid challenge measured after 30 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Design, synthesis, characterization and anti-inflammatory evaluation of novel pyrazole amalgamated flavones. |
AID1153381 | Analgesic activity in rat assessed as inhibition of acetic acid-induced writhing at 0.03 mM/kg | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13 | Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties. |
AID183501 | Antiinflammatory activity in vivo by carrageenan paw edema assay in rat at a dose of 10 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors. |
AID1178540 | Toxicity in Complete Freund's adjuvant-induced inflammatory pain CD rat model assessed as sedation at 30 mg/kg, po measured at 2 hrs post dose | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID1195045 | Antiinflammatory activity in po dosed CD-1 mouse ear edema model assessed as reduction in TPA-induced edema size administered 30 mins prior to TPA-challenge for every 48 hrs for 10 days relative to vehicle treated control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis, antinociceptive and anti-inflammatory effects of porphyrins. |
AID179746 | In vitro inhibition of prostaglandin synthesis was tested in rat | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | 2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents. |
AID295042 | Inhibition of COX1 | 2007 | Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9 | Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill). |
AID1550484 | Ulcerogenicity in albino rat assessed as severity of gastric lesions at 10 mg/kg, po administered as single dose after 18 hrs of starvation challenge and measured after 4 hrs | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID365464 | Inhibition of human MRP2 expressed in dog MDCK2 cells | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins. |
AID616299 | Anti-inflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced superoxide anion generation | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9 | Anti-inflammatory principles from Cordyceps sinensis. |
AID186593 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 10 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1055833 | Antiinflammatory activity in macrophages (unknown origin) assessed as inhibition of TNF-alpha secretion incubated for 2 hrs by ELISA relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID7974 | Metabolic stability observed at 30 min after administration in human liver microsomes | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1155580 | Inhibition of purified ovine COX-1 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid preincubated at 10 uM for 5 mins before substrate addition measured after 5 mins by HPLC analysis relative to control | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID1667504 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured at 4 hrs by calliper method (Rvb = 8.50 +/- 0.58 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1436688 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 3 hrs by plethysmometer relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID1854725 | Inhibition of soybean 5-LOX | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
AID337407 | Antiinflammatory activity against TPA-induced Swiss mouse ear edema assessed as reduction in ear swelling at 0.5 mg/ear topically after 4 hrs relative to control | 2003 | Journal of natural products, Sep, Volume: 66, Issue:9 | Griffonianone D, an isoflavone with anti-inflammatory activity from the root bark of Millettia griffoniana. |
AID551386 | Inhibition of ovine COX1 at 100 uM after 5 mins by microplate reader assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors. |
AID580341 | Inhibition of COX2 at 30 uM | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents. |
AID1253841 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for ovine COX-2 | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties. |
AID673511 | Inhibition of bovine 5-LOX assessed as inhibition of calcium ionophore A23187-induced leukotriene B4 formation by reversed phase HPLC analysis | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives. |
AID444874 | Analgesic activity in Swiss mouse assessed as inhibition of acetic acid-induced writhing response at 10 mg/kg, po administered 1 hr before acetic acid challenge measured for 30 mins relative to control | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | 1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoi |
AID178653 | Antiinflammatory activity was determined against rats carrageenan hind paw edema after oral administration | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID488201 | Inhibition of COX1 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID182302 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 1 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID414773 | Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Phenolic compounds with radical scavenging and cyclooxygenase-2 (COX-2) inhibitory activities from Dioscorea opposita. |
AID399390 | Antiplatelet activity in human whole blood assessed as inhibition of ristocetin-induced platelet aggregation at 100 ug/mL relative to control | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | A new antiplatelet diarylheptanoid from Alpinia blepharocalyx. |
AID1568920 | Inhibition of COX-1 in human whole blood assessed as reduction in calcium ionophore A23187-stimulated thromboxane B2 production by measuring thromboxane B2 level at 1 uM preincubated for 60 mins followed by calcium ionophore A23187 stimulation and measure | |||
AID303592 | Antiarthritic activity against adjuvant-induced arthritis in Wistar rat assessed as inhibition of paw edema at 10 mg/kg, po on day 8 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID162644 | Inhibitory activity against prostaglandin G/H synthase 2 | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID178845 | Antipyretic activity measured as yeast induced fever assay in rats | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID46853 | Inhibition of recombinant human prostaglandin G/H synthase 2 (COX-2) | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID1062918 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan-challenge measured after 1 hr relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID409539 | Antiarthritic activity in Albino rat assessed as inhibition of Freund's complete adjuvant-induced paw volume at 10 mg/kg, po administered for 14 days daily once starting a day before adjuvant challenge measured on day 13 | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1145139 | Therapeutic index, ratio of UD50 for 8 hrs starved po dosed Charles River rat to ED50 for rat assessed as inhibition of adjuvant-induced arthritis | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1, 3, 4, 9-tetrahydropyrano[3, 4-b]indole-1-acetic acids. |
AID753754 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po after 2 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1455835 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition carrageenan-induced paw edema at 5 mg/kg, ip pretreated for 15 mins followed by carrageenan challenge measured at 4 hrs post carrageenan challenge | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
AID162020 | In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors. |
AID180550 | The compound was tested in vivo for activity against yeast -induced hyperthermia in rat after peroral administration | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID1149355 | Ulcerogenicity in po dosed Wistar rat assessed as induction of gastric irritation | 1977 | Journal of medicinal chemistry, Jan, Volume: 20, Issue:1 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 1. 6,11-Dihydro-11-oxodibenz]b,e]oxepin-2-acetic acids. |
AID162501 | In vitro inhibitory activity towards human recombinant Prostaglandin G/H synthase 2 enzyme | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | 4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors. |
AID182814 | Gastric lesion activity on peroral administration in rat. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
AID682172 | TP_TRANSPORTER: inhibition of benzylpenicillin uptake by Indomethacin at a concentration of 1000uM in Oat3-expressing oocyte cells | 2004 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3 | Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. |
AID1204229 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 24 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID748513 | Selectivity ratio of IC50 for wild type mouse COX2 to IC50 for mouse COX2 R120Q mutant | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID337404 | Antiinflammatory activity against carrageenan-induced Swiss mouse paw edema at 10 mg/kg, po | 2003 | Journal of natural products, Sep, Volume: 66, Issue:9 | Griffonianone D, an isoflavone with anti-inflammatory activity from the root bark of Millettia griffoniana. |
AID667789 | Inhibition of ovine COX1 assessed as PGE2 formation at 1 uM by enzyme immunoassay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Indole based cyclooxygenase inhibitors: synthesis, biological evaluation, docking and NMR screening. |
AID1128736 | In vivo antiinflammatory activity in mouse assessed as decrease in carrageenan-induced paw edema at 0.30 mmol/kg, ip administered immediately after carrageenan injection measured after 3.5 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID192169 | Antiinflammatory efficacy is measured by the weight gain in rats during the 3 week adjuvant arthritis test at 0.0014 mM/kg (0.50 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID178472 | Antiinflammatory activity evaluated as Minimum effective oral dose that inhibits carrageenan paw edema in rat | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID1667506 | Ulcerogenic activity in albino rat assessed as damage of gastric mucosa surface epithelium at 10 to 50 mg/kg, po measured after 6 hrs by H and E staining based light microscopic assay | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID162339 | Biochemical index for Prostaglandin G/H synthase 2 measured as, PGE-2 levels in lipopolysaccharide (LPS)-challenged human whole blood | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors. |
AID1550477 | Antiinflammatory activity against carrageenan-induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 2 hrs post-carrageenan injection (Rvb = 36.4%) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID656843 | Antiinflammatory activity in human neutrophils assessed as inhibition of opsonized zymosan A-mediated superoxide anions production by WST-1 based respiratory burst assay | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Synthesis of new bergenin derivatives as potent inhibitors of inflammatory mediators NO and TNF-α. |
AID1392324 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 25 mg/kg, po measured at 2 hrs relative to control | |||
AID1550480 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw diameter at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 4 hrs post-carrageenan injection (Rvb = 4.88 +/- | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID338729 | In vivo antineoplastic activity against mouse Ehrlich ascite carcinoma cells xenografted in CF1 mouse assessed as inhibition of tumor growth at 10 mg/kg after 9 days relative to control | |||
AID688470 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as reduction in leukocyte infiltration-based myeloperoxidase at 0.4 umol administered topically per cm'2 of ear measured after 6 hrs post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID445753 | Antiinflammatory activity against arachidonic acid-induced ear edema in Balb/C mouse at 300 ug/ear administered topically 1 hr before arachidonic acid challenge measured after 60 mins | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Diastereoisomers of 2-benzyl-2, 3-dihydro-2-(1H-inden-2-yl)-1H-inden-1-ol: potential anti-inflammatory agents. |
AID723698 | Inhibition of ovine COX1 assessed as inhibition of PGF2a production by enzyme immunoassay | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
AID1503673 | Selectivity ratio of IC50 for human COX-1 to IC50 for human COX-2 | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID653188 | Antiinflammatory activity in transgenic zebrafish larvae harboring Fli-1 gene assessed as LPS-stimulated leukocyte migration to injury zone of tail transected larvae at 0.3 uM after 20 to 22 hrs by microscopy | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID404570 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced edema at 50 mg/kg, po after 6 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID591430 | Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW 264.7 cells after 24 hrs by ELISA | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID379443 | Antiinflammatory activity against Swiss mouse assessed as inhibition of TPA-induced edema at 0.5 mg/ear applied simultaneously with TPA measured after 4 hrs | 1999 | Journal of natural products, Apr, Volume: 62, Issue:4 | A glycosyl analogue of diacylglycerol and other antiinflammatory constituents from Inula viscosa. |
AID187766 | Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in right primary lesion in rats(volume change in the injected paw measured from day 0 to day 8) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID185019 | Minimum effective dose against adjuvant arthritis on therapeutic dosing (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID193127 | inhibition of swelling in rat paw edema was measured at a dose of 0.7 micro mol/kg/day for days 14-25 | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID384267 | Inhibition of U46619-induced platelet aggregation in human blood after 3 mins by turbidimetric assay | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs. |
AID1569917 | Inhibition of ovine COX-1 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay | |||
AID492315 | Antiedematogenic activity in Swiss mouse assessed as decrease of capsaicin-induced paw edema weight at 100 umol/kg, po administered 40 mins before capsaicin challenge measured after 30 mins relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates. |
AID591431 | Cytotoxicity against LPS-stimulated mouse RAW264.7 cells after 24 hrs by MTT assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID186470 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 0.1 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID409536 | Gastrointestinal toxicity in Wistar rat assessed as ulcer index at 30 mg/kg, po after 6 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1293533 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 5 hrs before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID263727 | Drug level in mouse brain at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. |
AID304228 | Antiinflammatory activity against Sprague-Dawley rat carrageenan air-pouch model assessed as reduction of prostaglandin E2 at 22.5 umol/kg, po | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID1232306 | Dissociation constant of the compound | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID595374 | Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-induced ZFP36 gene expression at 10 uM pretreated for 1 hr before LPS challenge measured after 2 hrs by RT-qPCR relative to control | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID328203 | Inhibition of COX1 at 100 uM | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID547626 | Antiinflammatory activity in albino rat assessed as reduction of carrageenan-induced paw edema at 10 umol/kg, sc administered 1 hr before carrageenan challenge measured after 4 hrs by plethysmometry | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID1695499 | Antiinflammatory activity in ICR mouse model of carrageenan-induced paw edema assessed as paw edema inhibition rate at 22 mg/kg, po pretreated with compound followed by carrageenan challenge and measured after 2 hrs post-treatment by dial thickness gage | 2020 | RSC medicinal chemistry, Jul-01, Volume: 11, Issue:7 | A practical synthesis of amino limonin/deoxylimonin derivatives as effective mitigators against inflammation and nociception. |
AID753744 | Gastrointestinal toxicity in albino rat assessed as apoptotic glandular epithelial cells at 0.28 mmol/kg, po using haematoxylin and eosin staining by light microscopic analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID611100 | Displacement of [3H]-PGD2 from mouse DP receptor expressed in CHO cells after 20 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID763525 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 30 mins prior to carrageenan challenge measured at 2 hrs by plethysmometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
AID1815258 | Cytotoxicity against African green monkey Vero E6 cells infected with SARS-CoV-2 assessed as reduction of cell viability measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID1061772 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX2 | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities. |
AID193232 | Compound was evaluated for edema density in adjuvant-induced arthritis model in rats at a dose of 1 mg/kg (Experiment # 1) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID548103 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip measured 3.5 hrs after carrageenan challenge relative to control | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives. |
AID642876 | Inhibition of COX2 at 100 uM | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity. |
AID1674505 | Anti-inflammatory activity in TPA-induced CD-1 mouse ear edema model assessed as inhibition of ear edema at 1 mg relative to control | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Cacalol Acetate, a Sesquiterpene from |
AID1204915 | Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced NO production after 24 hrs | 2015 | Journal of natural products, Feb-27, Volume: 78, Issue:2 | Anti-inflammatory coumarin and benzocoumarin derivatives from Murraya alata. |
AID170140 | Compound was evaluated for its analgesic activity by Randall-Selitto test in comparison with that of Aspirine | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID492858 | Inhibition of human recombinant COX2 after 5 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity. |
AID402404 | Ratio of IC50 for COX2 to IC50 for COX1 | 1998 | Journal of natural products, Oct, Volume: 61, Issue:10 | Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis. |
AID162630 | In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID1874823 | Synergistic antiproliferative activity against human MCF7-DOX cells assessed as reduction in cell viability at 50 to 200 uM incubated for 48 hrs in presence of doxorubicin by MTT assay | 2022 | ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8 | Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance. |
AID1662944 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as edema at 100 mg/kg, ip (Rvb = 8.70 +/- 0.90 mg) | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID356046 | Antiinflammatory activity against TPA-induced ear edema in Swiss mouse chronic dermatitis model assessed as inhibition of increase in ear weight | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID1196196 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 2 hrs before LPS challenge measured 18 hrs post LPS challenge by Griess method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases. |
AID1852383 | Antiinflammatory activity in LPS/hypoxia induced CA9 knockdown rat H9c2 cells assessed as decrease in IL-6 protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1209592 | Dissociation constant, pKa of the basic compound by capillary electrophoresis-mass spectrometry analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID177520 | In vivo inhibition of pyresis in rats | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID1455834 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition carrageenan-induced paw edema at 5 mg/kg, ip pretreated for 15 mins followed by carrageenan challenge measured at 2 hrs post carrageenan challenge | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
AID315577 | Inhibition of carrageenan-induced hind paw edema in rat assessed as decrease in paw volume at 10 mg/kg | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. |
AID54711 | Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22 | Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. |
AID414772 | Inhibition of ovine COX2 by colorimetric assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Phenolic compounds with radical scavenging and cyclooxygenase-2 (COX-2) inhibitory activities from Dioscorea opposita. |
AID683094 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX2 | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity. |
AID1902043 | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID255261 | Inhibitory concentration against human cyclooxygenase-2 at 10 uM concentration | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Synthesis and pharmacological evaluation of 1H-imidazoles as ligands for the estrogen receptor and cytotoxic inhibitors of the cyclooxygenase. |
AID1307705 | Activation of TREK1 (unknown origin) expressed in HEK293 cells assessed as increase in current density at 100 uM relative to control | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target? |
AID1199426 | Analgesic activity in Swiss Albino acetic acid-induced writhing mouse model assessed as number of writhes at 20 mg/kg, po administered 30 mins before to acetic acid challenge measured for 10 mins (Rvb = 92.8 +/- 1.49 No_unit) | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID338726 | Antiinflammatory activity against CF1 mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg administered 30 mins before carrageenan challenge measured after 3 hrs relative to control | |||
AID1601227 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as ear edema formation at 1 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration (Rvb = 17.61 to 19.82 mg) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID1136457 | Antitumor activity against mouse P388 cells allografted in DBA/2 mouse assessed as tumor growth inhibition at 20 mg/kg, ip qd for 2 weeks (Rvb = 100%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids. |
AID393661 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat assessed as inhibition of edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured after 4 hrs relative to control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Regioselective synthesis of dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones of potential anti-tumor properties. |
AID1852347 | Protection against LPS/hypoxia induced apoptosis in rat H9c2 cells assessed as reduction in necrotic cells at 10 umol/L incubated for 4 hrs under hypoxia condition by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 31.02%) | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID775267 | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21 | Inhibitory constituents from the aerial parts of Polygala tenuifolia on LPS-induced NO production in BV2 microglia cells. |
AID1576183 | Nephrotoxicity in rat assessed as effect on distal tubule at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID184640 | Lethal dose determined in rats when administered perorally | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID162156 | In vitro inhibitory activity against prostaglandin G/H synthase 1 (COX-1) from the microsomal fraction of ram seminal vesicles at 10 uM concentration | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors. |
AID1459158 | Antiarthritic activity in Lewis rat Freund's adjuvant-induced arthritis model assessed as reduction in arthritis index score at 2.5 mg/kg, ig administered through gavage pretreated for 1 hr followed by adjuvant challenge subsequent treatment for 9 days me | 2016 | Journal of natural products, 10-28, Volume: 79, Issue:10 | Effects of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. |
AID592741 | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrate production at 10 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess reagent method relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID1178552 | Half life in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID161325 | In vitro activity at a concentration of 10 uM against Prostaglandin G/H synthase 1 | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22 | Synthesis and pharmacological evaluation of some 8-cyanopyrido[3', 2':4,5]thieno[3,2-d]triazine derivatives as inhibitors of nitric oxide and eicosanoid biosynthesis. |
AID751107 | Antiinflammatory activity in Swiss mouse assessed as inhibition of serotonin-induced paw edema at 10 mg/kg, ip administered 30 mins prior to serotonin challenge measured after 4 hrs relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID679519 | TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Indomethacin: 2000 uM) in Xenopus laevis oocytes | 1999 | The American journal of physiology, 01, Volume: 276, Issue:1 | Molecular cloning and functional expression of a multispecific organic anion transporter from human kidney. |
AID34481 | Percentage inhibition of Aldose Reductase (AR) at a concentration of 15 ug/mL | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Discovery of novel aldose reductase inhibitors using a protein structure-based approach: 3D-database search followed by design and synthesis. |
AID1055832 | Antinociceptive activity in mouse assessed as inhibition of acetic acid-induced writhing at 0.05 mmol/kg, po administered 30 mins prior to acetic acid-challenge measured after 20 mins relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID396327 | Antiinflammatory activity in albino Charles-Foster rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po measured before 1 hr and after 3 hrs of carrageenan challenge relative to control | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Synthesis of new substituted azetidinoyl and thiazolidinoyl-1,3,4-thiadiazino (6,5-b) indoles as promising anti-inflammatory agents. |
AID1220560 | Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID184311 | Compound was evaluated for the inhibition of adjuvant-induced arthritis model in rats at a dose of 3 mg/kg | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID444058 | Volume of distribution at steady state in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1228722 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 12.5 uM after 24 hrs by Griess assay relative to control | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Anti-inflammatory Terpenoids from the Leaves and Twigs of Dysoxylum gotadhora. |
AID399387 | Antiplatelet activity in human whole blood assessed as inhibition of collagen-induced platelet aggregation at 100 ug/mL relative to control | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | A new antiplatelet diarylheptanoid from Alpinia blepharocalyx. |
AID1155600 | Inhibition of COX2-mediated PGF2alpha formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID1357048 | Anti-inflammatory activity in Swiss albino mouse model of carrageenan-induced-paw edema assessed as inhibition of paw edema at 10 mg/kg, ip after 3 hrs | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID187767 | Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in right secondary lesion in rats (volume change in the injected paw measured from day 9 to day 18) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID403354 | Inhibition of COX2 at 0.01 mM | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID177780 | Analgesic activity was determined by measuring the dose required to inhibit acetic acid induced writhing | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids. |
AID1852373 | Anti-inflammatory activity in rat H9c2 cells assessed as downregulation of cytochrome C expression at 10 uM in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1689631 | Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 4 hr by plethysmometer analysis relative to control (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID224060 | % inhibition against arthritis on adjuvant-untreated paw in rats at 1 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID1294603 | Inhibition of ovine COX1 at 25 uM by ELISA relative to control | 2016 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10 | Synthesis of unsymmetrical monocarbonyl curcumin analogues with potent inhibition on prostaglandin E2 production in LPS-induced murine and human macrophages cell lines. |
AID399389 | Antiplatelet activity in human whole blood assessed as inhibition of arachidonic acid-induced platelet aggregation at 100 ug/mL relative to control | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | A new antiplatelet diarylheptanoid from Alpinia blepharocalyx. |
AID1156829 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 4 hrs relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID1689623 | Analgesic activity in albino mouse assessed as reduction in acetic acid-induced number of writhes at 0.028 mM/kg, po pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to cont | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID404571 | Analgesic activity in Albino mouse at 50 mg/kg, po assessed as thermal stimuli reaction time change after 30 mins by hot plate method relative to basal level | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID351269 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 24 hrs of induction of inflammation relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones. |
AID161335 | In vitro inhibition of prostaglandin G/H synthase 1. | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | 1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. |
AID256340 | Percent inhibition of carrageenan 2% (0.1 mL intradermal) induced paw edema at the i.p. dose of 0.01 m mol/kg in fisher 344 rats; n=5 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Synthesis and antiinflammatory activity of coumarin derivatives. |
AID227272 | The compound was tested for PGE-2 generation on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID274905 | Activity at COX1 assessed as inhibition of arachidonic acid-induced PGE2 production in J774 cells | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage. |
AID187762 | Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in left secondary lesion in rats (volume change in the injected paw measured from day 9 to day 18) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID624615 | Specific activity of expressed human recombinant UGT2B10 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID223076 | Concentration required to inhibit production of PGE-2 from whole blood stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID492146 | Binding affinity to human PPARgamma expressed in Escherichia coli BL21 assessed as binding constant by fluorescence quenching assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
AID431710 | Antihyperalgesic effect in Freund's complete adjuvant-induced rat inflammatory pain model assessed as reversal of hyperalgesia at 30 mg/kg, sc | 2009 | Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18 | Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747). |
AID442514 | Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase. |
AID1198256 | Antiproliferative activity against human U373MG cells assessed as effect on cell number at 1 nM to 10 uM incubated for 1 to 6 days by trypan blue dye exclusion dye based inverted microscopy | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Effect of new hybrids based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug on the growth of a human astrocytoma cell line (U373). |
AID1357040 | Inhibition of human COX2 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID224209 | Inhibitory activity against Granuloma on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID188207 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 3 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 21st day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID128863 | Acute toxicity was evaluated as number of mice died (tested = 7) after 72nd hour when 8 mg/kg is administered intraperitoneally | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1455997 | Antinociceptive activity in carrageenan-induced Swiss mouse model of mechanical hyperalgesia at 100 umol/kg, po pretreated for 1 hr followed by carrageenan challenge measured at 3 hrs post dose by Von Frey filament assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
AID1237664 | Anti-inflammatory activity in Swiss mouse assessed as inhibition of zymosan-induced peritonitis by measuring reduction in leukocyte migration at 10 umol/kg, ip administered 30 min before the zymosan injection | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of the anti-nociceptive and anti-inflammatory activity of 4-aminoquinoline derivatives. |
AID178033 | Effective dose for antiinflammatory activity in carrageenan paw edema assay in rats after oral administration | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID393214 | Inhibition of iNOS in LPS-stimulated mouse J774 cells assessed as inhibition of nitric oxide generation at 10 uM | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives. |
AID114287 | Antiinflammatory activity against CPE in mice following peroral administration of 10 mg/kg | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID673509 | Inhibition of bovine COX1 assessed as inhibition of calcium ionophore A23187-induced 12-hydroxyheptadecatrienoic acid formation by reverse-phase HPLC analysis | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives. |
AID186277 | Radiographic change was judged in the area of the tarsus region, using an arbitrary scoring system upon termination of the test (14 days dosing of 1 mg/kg) in a model of type II collagen arthritis in the rat. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID356713 | Antiinflammatory activity against TPA-induced ear edema in mouse assessed inhibition of edema at 0.10 mg/ear | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Antiinflammatory constituents from Heterotheca inuloides. |
AID1204227 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 4 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID500930 | Inhibition of COX2 in heterozygous transgenic zebrafish embryo assessed as MPO-positive granulocytic cell accumulation at 20 uM by in situ hybridization analysis | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4 | Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation. |
AID1737611 | Ulcerogenic activity in fasted albino mouse assessed as average number of ulcers in gastric mucosa at 10 mg/kg, po for 3 days (Rvb = 0 No_unit) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID286752 | Inhibition of carrageenan-induced Fischer 344 rat paw edema at 0.01 mmol/kg, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents. |
AID736890 | Inhibition of ovine COX2 assessed as appearance of oxidized N,N,N,N'- tetramethyl-p-phenylenediamine at 100 uM | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Design, synthesis, characterization and anti-inflammatory evaluation of novel pyrazole amalgamated flavones. |
AID34782 | In vitro inhibition of rabbit lens aldose reductase. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
AID393211 | Inhibition of COX2 in LPS-stimulated human whole blood assessed as inhibition of PGE2 production at 10 uM by radioimmunoassay | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives. |
AID1125126 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID649079 | Analgesic activity in albino mouse assessed as inhibition of acetic acid-induced abdominal constriction at 100 umol/kg, po administered 1 hr before acetic acid challenge measured after 30 mins relative to control | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives. |
AID1192215 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 2 hrs relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID1663614 | Anticancer activity against human HCT15 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis and anticancer activity of open-resorcinarene conjugates. |
AID173360 | Hypolipidemic action at 500 uM/kg was determined as reduction in total cholesterol in rat plasma | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID452093 | Toxicity in Sprague-Dawley rat assessed as gastrointestinal ulceration at 200 mg/kg, po once daily for 5 days | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | A new therapeutic approach in Parkinson's disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents. |
AID1316780 | Analgesic activity in rat assessed as reversal of complete Freund's adjuvant-induced mechanical hyperalgesia at 30 mg/kg, po after 5 hrs relative to control | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. |
AID42828 | In vitro inhibition of human recombinant IL-1-beta-induced breakdown of bovine cartilage in a cartilage organ culture assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown. |
AID1359535 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as hind paw thickness at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured immediately by caliper method (Rvb = 3.58 +/- 0.34 millime | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID540218 | Clearance in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1784599 | Cytotoxicity against human HBE cells assessed as reduction in cell survival at 10 uM by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury. |
AID1852397 | Reversal of LPS/hypoxia induced mitochondrial membrane potential loss in rat H9c2 cells in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by JC-1 dye based flow cytometry analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID748523 | Inhibition of mouse COX2 S530A mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
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AID1150262 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of adjuvant-induced arthritis at 0.5 mg/kg, po administered for 14 days prior to adjuvant challenge relative to control | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID186440 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 0.1 mg/kg at time interval- 2 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1293529 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 1 hr before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID707340 | Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid-induced writhing at 5 mg/kg, ip administered 30 mins prior to acetic acid challenge | 2012 | Journal of natural products, May-25, Volume: 75, Issue:5 | Kaurenoic acid from Sphagneticola trilobata Inhibits Inflammatory Pain: effect on cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID763515 | Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
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AID162505 | Inhibition of Prostaglandin G/H synthase 2 in CHO whole cell assay | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12 | 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. |
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AID409566 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema volume at 10 mg/kg, po administered 60 mins before carrageenan challenge after 2 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
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AID1416039 | Binding affinity to calf thymus DNA by UV-visible spectrophotometric method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
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AID284323 | Inhibition of ovine COX2 at 100 uM | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
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AID393846 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 5 mg/kg, po administered 30 mins before carrageenan challenge measured after 1 hr | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. |
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AID1416050 | Binding affinity to calf thymus DNA assessed as conformational change up to 100 uM by circular dichroism spectral analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
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AID184537 | Mortality caused by the compound in rats after administration at 84 uM/kg for 4 days | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
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AID322957 | Inhibition of synthetic amyloid beta-42 fibrillation by ThT fluorescence analysis relative to control | 2007 | The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14 | Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct. |
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AID653311 | Antiinflammatory activity in transgenic zebrafish larvae harboring Fli-1 gene assessed as LPS-stimulated leukocyte migration to injury zone of tail transected larvae at 3 uM after 20 to 22 hrs by microscopy | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID1416043 | Inhibition of ethidium bromide binding to calf thymus DNA up to 80 uM by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID492148 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
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AID1667491 | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
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AID186438 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 0.1 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1810791 | Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
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AID1436695 | Analgesic activity in Swiss albino mouse assessed as protection against acetic acid-induced writhing at 20 mg/kg, po administered 30 mins followed by acetic acid challenge measured over 10 mins relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
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AID1743650 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
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AID1689630 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 4 hr by plethysmometer analysis (Rvb = 3.98 +/- 0.34 mm) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
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AID1783306 | Ulcerogenic activity in fasted albino rat assessed as incidence of ulceration at 28 uM/kg, po administered for 3 consecutive days (Rvb = 0 %) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID604743 | Displacement of radiolabeled warfarin from fatty acid containing human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
AID703399 | Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID78477 | Ability to bind to guinea pig atrial homogenate | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Accumulation of drugs by guinea pig isolated atria. Quantitative correlations. |
AID1063321 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 24 hrs by ELISA (Rvb = 38.3 +/- 3.3 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID509685 | Antioxidant activity assessed as xanthin/xanthin oxidase superoxide scavengeing activity | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 3-Formylchromones: potential antiinflammatory agents. |
AID1416049 | Binding affinity to calf thymus DNA assessed as change in viscosity at compound to DNA ratio of 0.2 to 1 by viscometry | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID681160 | TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells | 2000 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1 | Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1. |
AID1409044 | Antiinflammatory activity in carrageenan-induced Swiss mouse assessed as inhibition of paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 2 hrs by plethysmometric method | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. |
AID223172 | Percent reduction of edema in mice 3h after oral administration of 3 mg/kg in carrageenan model | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID184499 | Antiinflammatory activity was assessed in carrageenan-induced rat paw edema(CIRPE) test after po administration | 1982 | Journal of medicinal chemistry, Jan, Volume: 25, Issue:1 | Isoxicam and related 4-hydroxy-N-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides. Potent nonsteroidal antiinflammatory agents. |
AID356056 | Antiinflammatory activity against carrageenan-induced Swiss mouse paw edema assessed as inhibition of paw volume at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 5 hrs relative to control | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID595370 | Inhibition of human recombinant COX-2 assessed as PGE2 production from arachidonic acid after 20 mins enzyme immunoassay | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID675695 | Inhibition of COX1 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold. |
AID515505 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered prior to carrageenan challenge measured after 5 hrs post carrageenan challenge | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 | Synthesis and characterization of novel indole derivatives reveal improved therapeutic agents for treatment of ischemia/reperfusion (I/R) injury. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID723697 | Antiinflammatory activity in AKR mouse assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip measured after 3.5 hrs of carrageenan-challenge | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
AID1436691 | Inhibition of COX1 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID1650565 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human COX2 | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID162488 | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (66 nM) using [14C]AA (50 uM) was determined | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. |
AID647947 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced decrease in CAT activity in liver at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 5 hrs | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID287609 | Antiinflammatory activity in Wistar Albino rat assessed as inhibition of carrageenan-induced paw oedema at 5 mg/kg, ip after 3 hrs | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID759379 | Antiinflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured at 1 hr post carrageenan challenge by plethysmometeric analysis relative to c | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents. |
AID1424663 | Antinociceptive activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing by measuring reduction in number of abnormal muscle constrictions at 10 mg/kg, ip treated 30 mins prior to test followed by acetic acid challenge measure | 2018 | European journal of medicinal chemistry, Jun-10, Volume: 153 | Indolyl-isoxazolidines attenuate LPS-stimulated pro-inflammatory cytokines and increase survival in a mouse model of sepsis: Identification of potent lead. |
AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
AID481442 | Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID1333296 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw oedema at 50 mg/Kg, po administered 30 mins before carrageenan challenge measured after 4 hrs relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents. |
AID444056 | Fraction escaping gut-wall elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID177291 | Effect in rat pleural Carrageenan test (exudate white blood cells (WBC)); No significant effect at 28 umol/kg (Not active) | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | 3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation. |
AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID485995 | Antiinflammatory activity in rat assessed as reduction in carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis, biological evaluation and molecular docking of novel series of spiro [(2H,3H) quinazoline-2,1'- cyclohexan]-4(1H)- one derivatives as anti-inflammatory and analgesic agents. |
AID3620 | Compound was evaluated for the inhibition of 5-LO (5-lipoxygenase). | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis. |
AID649269 | Inhibition of ovine COX-1 by enzyme immuno assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation. |
AID681430 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 40 uM, Indomethacin: 1000 uM) in Xenopus laevis oocytes | 1999 | The Journal of biological chemistry, May-07, Volume: 274, Issue:19 | Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. |
AID160710 | Inhibitory activity against Prostaglandin G/H synthase (bovine seminal vesicles) | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
AID1716957 | Antagonist activity at human P2X2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx at 10 uM preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon G | |||
AID1542902 | Inhibition of N-terminal GST-tagged recombinant human AKR1C3 His5Gln mutant expressed in Escherichia coli BL21 (DE) Codon Plus RP cells assessed as reduction in NADPH production | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID595364 | Cytotoxicity against human THP1 cells after 24 hrs by erythrosin B staining | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID178934 | Effective dose required for the inhibition of adjuvant arthritis in Sprague-Darley rats | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | 2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors. |
AID263728 | Drug level in mouse plasma at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. |
AID303569 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 24 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1815252 | Antiviral activity against SARS-COV2/Padova/2020 infected in African green monkey Vero E6 cells assessed as inhibition of plaque formation measured after 3 days by Plaque reduction assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID680176 | TP_TRANSPORTER: inhibition of MTX uptake (MTX: 1 uM, Indomethacin: 500 uM) in OAT4-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 302, Issue:2 | Characterization of methotrexate transport and its drug interactions with human organic anion transporters. |
AID289294 | Antiinflammatory activity against carrageenan-induced hind paw oedema in Swiss Albino mouse assessed as swelling thickeness at 100 mg/kg, po after 360 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID1674101 | Inhibition of AKR1C3 (unknown origin) using 9,10-phenanthrenequinone as substrate | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Overview of AKR1C3: Inhibitor Achievements and Disease Insights. |
AID1257023 | Anti-inflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip after 3.5 hrs | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22 | Synthesis and biological evaluation of new C-10 substituted dithranol pleiotropic hybrids. |
AID611095 | Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID478748 | Antiinflammatory activity against carrageenan-induced paw edema in po dosed rat administered 1 hr before carrageenan challenge assessed after 1 hr | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis of 3-((2,4-dichlorophenoxy)methyl)-1,2,4-triazolo(thiadiazoles and thiadiazines) as anti-inflammatory and molluscicidal agents. |
AID634939 | Gastric toxicity in albino rat assessed as loss of mucosal membrane at the area of ulceration at 100 mg/kg, po after 5 hrs by hematoxylin and eosin staining | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID1452937 | Inhibition of ovine COX-1 assessed as reduction in PGH2 production using arachidonic acid as substrate preincubated for 5 mins followed by substrate and hematin addition measured after 2 mins by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and mechanistic evaluation of novel N'-benzylidene-carbohydrazide-1H-pyrazolo[3,4-b]pyridine derivatives as non-anionic antiplatelet agents. |
AID1517247 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human recombinant COX-2 | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies. |
AID326240 | Toxicity in rat assessed as ulcer index at 0.08 mmol/kg, po after 6 hrs | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6 | Second-generation aspirin and indomethacin prodrugs possessing an O(2)-(acetoxymethyl)-1-(2-carboxypyrrolidin-1-yl)diazenium-1,2-diolate nitric oxide donor moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID271287 | Inhibition of ovine COX2 | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID1134829 | Antiarthritic activity in rat assessed as reduction in adjuvant-induced arthritic pain | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | 2-(Substituted phenyl)oxazolo[4,5-b]pyridines and 2-(substituted phenyl)oxazolo[5,4-b]pyridines as nonacidic antiinflammatory agents. |
AID1852393 | Protection against LPS/hypoxia induced cell injury in rat H9c2 cells assessed as recovery of cell viability in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid and Na2WO4 by CCK-8 assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID243647 | In vitro inhibitory activity against ovine cyclooxygenase-1 (COX-1) at 200 uM; Inactive | 2004 | Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20 | Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints. |
AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID289295 | Inhibition of carrageenan-induced hind paw oedema in Swiss Albino mouse at 100 mg/kg, po after 90 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID172889 | Percent change in avg. volume of pleural fluid at a dose of 0.16 mg/kg and 5-h response is evaluated by Evans blue-carrageenan induced pleural effusion assay | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID1568929 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip preincubated for 1 hr followed by carrageenan challenge and measured for 6 hrs | |||
AID1601223 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as ear edema formation at 2 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration (Rvb = 17.61 to 19.82 mg) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID653321 | Antiinflammatory activity against TPA-induced ear edema in Swiss mouse assessed as inhibition of increase in ear weight at 0.5 mg/ear administered topically measured after 4 hrs relative to control | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID107291 | Analgesic activity in mice by mouse phenylquinone writhing assay relative to aspirin. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
AID287607 | Antiinflammatory activity in Wistar Albino rat assessed as inhibition of carrageenan-induced paw oedema at 5 mg/kg, ip after 1 hr | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID537735 | Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
AID1869452 | Analgesic activity against formalin-induced inflammatory pain-like behaviour ICR mouse model assessed as inhibition of hind paw licking behaviour at 10 mg/kg, ip administered 60 mins prior to formalin challenge and measured after 10 to 40 mins by formalin | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID224215 | Inhibitory activity against PGE-2 on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID221973 | In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID287340 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 10 mg/kg, po after 360 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1220258 | Renal clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID751156 | Hepatotoxicity in Swiss mouse assessed as increase in plasma AST level at 2.5 mg/kg, ip for 7 days | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Vitexin inhibits inflammatory pain in mice by targeting TRPV1, oxidative stress, and cytokines. |
AID374106 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 1 hr | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
AID1532668 | Inhibition of COX2 in LPS-induced human whole blood at 10 uM after 24 hrs by EIA relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Anti-inflammatory activity of triazine derivatives: A systematic review. |
AID162145 | Inhibitory activity against Prostaglandin G/H synthase 1 isolated from ram (sheep) seminal vesicle | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid. |
AID1674504 | Anti-inflammatory activity in TPA-induced CD-1 mouse ear edema model assessed as ear weight at 1 mg | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Cacalol Acetate, a Sesquiterpene from |
AID1821157 | Binding affinity to human serum albumin assessed as dissociation constant and measured after 5 mins by MST assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | "Clickable" Albumin Binders for Modulating the Tumor Uptake of Targeted Radiopharmaceuticals. |
AID403347 | Inhibition of COX1 at 5 uM | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID1178549 | AUC (0 to t) in CD rat at 27 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID186457 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 1 mg/kg at time interval- 4 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID287289 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 100 mg/kg, po after 180 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1473835 | Stimulation of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID591669 | Metabolic stability in rat plasma assessed as compound remaining at 5 mM after 60 mins by HPLC analysis | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID1783305 | Anti-inflammatory activity Wistar albino rat model of carragenan-induced paw edema assessed as inhibition of inflammation at 28 uM/kg, ip measured after 3 hrs by plethysmometer relative to control | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID1330205 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 2 hrs before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID1136207 | Inhibition of PG synthase (unknown origin) | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Novel analgesic-antiinflammatory salicylates. |
AID1397089 | Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Synthesis and biological properties of aryl methyl sulfones. |
AID426426 | Inhibition of soybean lipoxygenase assessed as conversion of sodium linoleate to 13-hydroperoxylinoleic acid at 0.1 mM | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts. |
AID748514 | Selectivity ratio of IC50 for wild type mouse COX2 to IC50 for mouse COX2 S530A mutant | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1437772 | Analgesic activity in Swiss albino mouse assessed as inhibition of formalin-induced paw flinching at 10 mg/kg administered for 30 mins followed by formalin challenge measured during first 5 mins post formalin challenge | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Rationally designed benzopyran fused isoxazolidines and derived β |
AID1783311 | Inhibition of human recombinant COX-2 using arachidonic acid as substrate by fluorescence assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID781330 | pKa (acid-base dissociation constant) as determined by potentiometric titration | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID1405601 | Inhibition of LPS-induced PGE2 production in C57BL6 mouse peritoneal cells measured at 5 hrs time interval by ELISA | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Influence of the C-5 substitution in polysubstituted pyrimidines on inhibition of prostaglandin E |
AID1737612 | Ulcerogenic activity in fasted albino mouse assessed as average severity of ulcers in gastric mucosa at 10 mg/kg, po for 3 days (Rvb = 0 No_unit) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1178536 | Antinociceptive activity in Complete Freund's adjuvant-induced inflammatory pain CD rat model assessed as time required for maximal effect at 30 mg/kg, po relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14 | DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
AID688451 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.10 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1902038 | Inhibition of full-length ovine COX-1 at 5 uM using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry relative to control | 2022 | Bioorganic & medicinal chemistry, 03-01, Volume: 57 | Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity. |
AID289297 | Inhibition of carrageenan-induced hind paw oedema in Swiss Albino mouse at 100 mg/kg, po after 270 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID647950 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced TNFalpha level in paw serum at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 5 hrs by ELISA | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID176241 | Inhibitory effect for increase in plasma prostaglandin E2 (PGE2) level after arachidonic acid (AA) injection into COX-2 lipopolysaccharide-treated rats | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID240795 | In vitro inhibitory concentration against COX-1 enzyme | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Novel nonsteroidal antiinflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies. |
AID186455 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 1 mg/kg at time interval- 2 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID263722 | Inhibition of beta amyloid protein 42 in HEK cell lines overexpressing APP695 at 100 uM | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. |
AID254438 | In vitro binding affinity (agonistic) towards human CRTH2 receptor expressed in CHO cells; range 15 to 25 nM | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. |
AID729248 | Selectivity ratio of IC50 for ovine COX1 to IC50 for mouse COX2 | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID1542904 | Selectivity index, ratio of IC50 for N-terminal GST-tagged recombinant human AKR1C2 expressed in Escherichia coli BL21 (DE) Codon Plus RP cells to IC50 for N-terminal GST-tagged recombinant human AKR1C3 expressed in Escherichia coli BL21 (DE) Codon Plus R | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1819028 | Antiinflammatory activity in transgenic fluorescent zebrafish expressing EGFP assessed as reduction in CuSO4 induced macrophage migration at 20 uM preincubated for 2 hrs followed Cuso4 addition and measured after 1 hr by fluorescence microscopic analysis | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Dolabellane Diterpenes and Elemane Alkaloids from the Soft Coral |
AID1241830 | Anti-inflammatory activity in rat assessed as inhibition of arachidonic acid-induced paw edema at 10 mg/kg, po dosed 30 mins before arachidonic acid injection and measured 1 hr after arachidonic acid injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID177223 | Inhibition of carrageenan paw edema in rats | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID409549 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 3 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1484252 | Anti inflammatory in CD-1 mouse assessed as reduction in zymosan-induced inflammatory cell infiltration by measuring inflammatory cell level in peritoneal exudates at 5 mg/kg, ip preincubated for 30 mins followed by zymosan addition measured after 4 hrs b | 2017 | Journal of natural products, 03-24, Volume: 80, Issue:3 | Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones. |
AID255251 | Inhibitory concentration against human cyclooxygenase-1 at 10 uM | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Synthesis and pharmacological evaluation of 1H-imidazoles as ligands for the estrogen receptor and cytotoxic inhibitors of the cyclooxygenase. |
AID1134897 | Inhibition of PGF2-alpha formation in ip dosed rat serum after 1 hr by radioimmunoassay | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID751108 | Antiinflammatory activity in Swiss mouse assessed as inhibition of dextran sulfate-induced paw edema at 10 mg/kg, ip administered 30 mins prior to dextran sulfate challenge measured after 4 hrs relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID568008 | Inhibition of human recombinant His-tagged glyoxalase 1 expressed in Escherichia coli BL21 (DE3) preincubated for 20 mins by Dixon plot analysis | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Identification of curcumin derivatives as human glyoxalase I inhibitors: A combination of biological evaluation, molecular docking, 3D-QSAR and molecular dynamics simulation studies. |
AID674725 | Gastrointestinal toxicity in Wistar albino rat assessed as stomach ulcer index at 0.029 mmol/kg, po followed by another two compound doses in second and third days measured on fourth day post dose by acute ulcerogenicity study | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID189094 | Number of writhings in Acetic acid Writhing test at a dose of 5 mg/kg perorally in rats | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID515501 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 | Synthesis and characterization of novel indole derivatives reveal improved therapeutic agents for treatment of ischemia/reperfusion (I/R) injury. |
AID1497262 | Hemolytic activity in human RBC assessed as mean absorbance (Rvb = 0.1868 +/- 0.033 No_unit) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective. |
AID1261691 | Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo. |
AID1650567 | Inhibition of LPS-activated COX2 in human whole blood assessed as PGE2 level at 1 uM by ELISA (Rvb = 1.40 ng/ml) | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID1737621 | Analgesic activity in albino mouse assessed as forepaw licking/jumping latency time at 10 mg/kg, ip measured after 30 mins by hot plate test (Rvb = 5.02 +/- 0.09 sec) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID178918 | Effective dose required for antiinflammatory activity by rat paw edema assay tested in vivo | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID1301943 | Analgesic activity in Swiss albino mouse assessed as reduction in capsaicin-induced paw licking at 10 mg/kg, ip dosed 30 mins before capsaicin injection measured for 10 mins | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent. |
AID1783303 | Anti-inflammatory activity in Wistar albino rat model of carragenan-induced paw edema assessed as inhibition of inflammation at 28 uM/kg, ip measured after 2 hrs by plethysmometer relative to control | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID287341 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 10 mg/kg, po after 90 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID763524 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 30 mins prior to carrageenan challenge measured at 3 hrs by plethysmometric analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
AID552766 | Antiinflammatory activity against histamine-induced mouse edema model assessed as antiinflammatory effect 20 mg/kg, po (untreated control = 0%) | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Rapid access to new bioconjugates of betulonic acid via click chemistry. |
AID181588 | Percent Edema variation in Carrageenan-induced paw edema test at a dose of 5 mg/kg perorally in rats after 60 min | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID604741 | Displacement of radiolabeled warfarin from fatty acid-free human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
AID748517 | Selectivity ratio of IC50 for wild type mouse COX2 to IC50 for mouse COX2 V349I mutant | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID179432 | In vivo percent inhibition of carrageenan foot-pad edema (CFE) after peroral administration was determined. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase. |
AID419901 | Gastrointestinal toxicity in albino rat assessed as ulcer index at 100 mg/kg, po | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Design, synthesis and biological investigation of certain pyrazole-3-carboxylic acid derivatives as novel carriers for nitric oxide. |
AID430157 | Antiinflammatory activity against carrageenan-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before carrageenan challenge measured after 5 hrs by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID161501 | Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells incubated in low concentration of arachidonic acid | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors. |
AID1576179 | Hepatotoxicity in rat assessed as effect on bile ducts at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1484251 | Anti inflammatory activity in CD-1 mouse assessed as reduction in zymosan-induced PGE2 by measuring PGE2 level in peritoneal exudates at 5 mg/kg, ip preincubated for 30 mins followed by zymosan addition measured after 30 mins by enzyme immunoassay (Rvb = | 2017 | Journal of natural products, 03-24, Volume: 80, Issue:3 | Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones. |
AID1918193 | Dissociation constant, pKa of the compound | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment. |
AID648862 | Inhibition of human recombinant COX2 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2 | Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs. |
AID162650 | Inhibitory activity against recombinant human Prostaglandin G/H synthase 2 | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. |
AID1754199 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Design and synthesis of novel diosgenin-triazole hybrids targeting inflammation as potential neuroprotective agents. |
AID182301 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 12 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1742602 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent-based assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Novel phthalide derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo. |
AID1532671 | Anti-inflammatory activity in carrageenan-induced Swiss albino rat assessed as reduction in paw edema by measuring swelling thickness at 10 ml/kg, po pretreated for 1 hr followed by carrageenan addition and measured up to 6 hrs at 1 hr interval relative t | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Anti-inflammatory activity of triazine derivatives: A systematic review. |
AID428390 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po treated for 30 mins measured after 3 hrs of carrageenan challenge | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. |
AID224362 | Intestinal ulcerogenic activity at a dose of 10 mg/kg | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID748508 | Binding affinity to wild type mouse COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1264569 | Inhibition of recombinant human COX-2 preincubated for 15 mins by fluorescence analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
AID680610 | TP_TRANSPORTER: inhibition of Estradiol-17beta-D-glucuronide uptake by Indomethacin at a concentration of 10 uM in membrane vesicle from MRP8-expressing LLC-PK1 cells | 2005 | Molecular pharmacology, Feb, Volume: 67, Issue:2 | Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). |
AID176212 | Effective dose was determined in vivo in male lewis rats by rat adjuvant-induced arthritis assay | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9 | Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). |
AID115720 | The compound was evaluated for inhibition of edema induced by PGE at 2 micro/mL | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID432726 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered before 60 mins of carrageenan-challenge measured after 360 mins | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives. |
AID415886 | Antipyretic activity against brewer's yeast-induced hyperthermia in Wistar rat assessed as change in rectal temperature at 5 mg/kg, po after 150 mins | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and spectral characterization of a new class of N-(N-methylpiperazinoacetyl)-2,6-diarylpiperidin-4-ones: antimicrobial, analgesic and antipyretic studies. |
AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID130719 | In vivo inhibitory activity against arachidonic acid(AA) ear edema at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
AID675016 | Ulcerogenic activity in albino rat assessed as hyperemia at 300 mg/kg/day administered as equal doses at 0 and 12 hrs for three consecutive days measured at 6 hrs post last dose | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis and biological evaluation of some novel thienopyrimidines and fused thienopyrimidines as anti-inflammatory agents. |
AID1716958 | Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM d | |||
AID115726 | The compound was evaluated for inhibition of edema induced by histamine at 10 mg/mL | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID1385398 | Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID384823 | Antiinflammatory activity against carrageenan-induced paw oedema in albino rat at 1.5 mg/kg, po, relative to control | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis, antimicrobial and anti-inflammatory activities of some 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines bearing trichlorophenyl moiety. |
AID587233 | Inhibition of ovine COX1 assessed as PGE2 formation at 125 nM by LC-MS-MS analysis | 2011 | Journal of natural products, Feb-25, Volume: 74, Issue:2 | Bioactive compounds from the fern Lepisorus contortus. |
AID1232310 | Volume of distribution at steady state in human | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID1737605 | Antiinflammatory activity in Wistar rat model of carrageenan-induced paw edema assessed as reduction in thickness of paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hrs (Rvb = 1.40 +/-0.10 mm) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID757496 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw oedema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs by plethysmometer relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity. |
AID115378 | Inhibitory against carrageenan induced paw edema in mice at 12 mg/kg, sc dose after 3h | 1982 | Journal of medicinal chemistry, Feb, Volume: 25, Issue:2 | Synthesis of N-(carbonylamino)-1,2,3,6-tetrahydropyridines with analgesic, antiinflammatory, and hyperglycemic activity. |
AID190671 | Ulcerogenicity was measured in intestine during the 3 week adjuvant arthritis test.(animals with ulcers/animals in test) at 0.008 mM/kg (2.86 mg) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID680944 | TP_TRANSPORTER: inhibition of NEM-GS in the presence of Indomethacin at a concentration of 100uM in membrane vesicles from MRP6-expressing Sf9 cells | 2002 | The Journal of biological chemistry, May-10, Volume: 277, Issue:19 | Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). |
AID1187257 | Anti-inflammatory activity in Wistar rat model of carrageenan-induced edema assessed as reduction in right hind paw thickness at 1 mg/kg, po dosed 1 hour before carrageenan injection measured 3 hrs post carrageenan challenge by digital plethysmometry | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Indole-3-ethylsulfamoylphenylacrylamides: potent histone deacetylase inhibitors with anti-inflammatory activity. |
AID751106 | Antiinflammatory activity in Swiss mouse assessed as inhibition of bradykinin-induced paw edema at 10 mg/kg, ip administered 30 mins prior to bradykinin challenge measured after 60 mins in presence of captopril relative to untreated control | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
AID303593 | Antiarthritic activity against adjuvant-induced arthritis in Wistar rat assessed as inhibition of paw edema at 10 mg/kg, po on day 13 | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID502273 | Inhibition of sheep COX2 by enzyme immunoassay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors. |
AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1221821 | Cytotoxicity against HEK293 cells expressing UGT1A3 assessed as decrease in cell viability at 1 mM measured at 24 hrs by MTT assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1 | Toxicological evaluation of acyl glucuronides of nonsteroidal anti-inflammatory drugs using human embryonic kidney 293 cells stably expressing human UDP-glucuronosyltransferase and human hepatocytes. |
AID701948 | Inhibition of human recombinant P-glycoprotein after 40 mins by Pgp-Glo assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity. |
AID1150270 | Analgesic activity in po dosed mouse assessed as inhibition of acetic acid-induced writhing | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID169240 | Incidence of melena defecation was recorded 24 hrs of last treatment given once daily for 4 days; Positive | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID434303 | Antiinflammatory activity in Norwegian albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po after administered 60 mins prior to carrageenan-challenge measured after 5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and pharmacological investigation of 3-(substituted 1-phenylethanone)-4-(substituted phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylates. |
AID591631 | Partition coefficient, log P of the compound in 1-octanol-citric acid buffer at pH 3 by HPLC analysis | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID189614 | Compound was evaluated for percentage recovery from paw edema in adjuvant-induced arthritic model of rat at a dose of 2 mg/kg | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. |
AID1061773 | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities. |
AID1543431 | Antiinflammatory activity in ICR mouse assessed as inhibition of TPA-induced ear edema by measuring reduction in weight of ear punches applied topically measured 4 hrs post TPA-challenge relative to control | |||
AID404577 | Analgesic activity against visceral pain in Albino mouse assessed as acetic acid-induced writhing at 50 mg/kg, po after 30 mins | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
AID645022 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 1 hr by plethysmometer relative to control | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents. |
AID1403472 | Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study. |
AID1542917 | solubility in pH 2.0 simulated gastric fluid | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID188068 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 0.3 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 22nd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID681859 | TP_TRANSPORTER: inhibition of glyburide accumulation in the presence of indomethacin at a concentration of 200uM in MRP1-expressing HeLa cells | |||
AID197602 | Lysozyme-conjugated prodrugs: in vitro stability in rat cortical homogenate at pH 7.4 | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Low molecular weight proteins as carriers for renal drug targeting. Preparation of drug-protein conjugates and drug-spacer derivatives and their catabolism in renal cortex homogenates and lysosomal lysates. |
AID1310782 | Inhibition of LPS-induced TNF-alpha production in mouse RAW264.7 cells at 10 uM preincubated for 30 mins prior to LPS challenge measured after 24 hrs by ELISA | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Design, Synthesis, and Structure-Activity Relationship Study of Novel Indole-2-carboxamide Derivatives as Anti-inflammatory Agents for the Treatment of Sepsis. |
AID1334716 | Inhibition of ovine COX-1 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | |||
AID1550481 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 4 hrs post-carrageenan injection (Rvb = 41%) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID1062919 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan-challenge measured after 2 hrs relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID447798 | Antiinflammatory activity against carrageenan-induced paw edema in mouse assessed as decrease in index of hind paw edema at 20 mg/kg, po administered 1 hr prior to carrageenan challenge | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Efficient synthesis of the first betulonic acid-acetylene hybrids and their hepatoprotective and anti-inflammatory activity. |
AID521209 | Antiproliferative activity against mouse astrocyte cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
AID1125129 | Ulcerogenic effect in albino rat assessed as ulcer index at 0.28 mmol/kg, po | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID161490 | In vitro inhibitory activity towards human platelet recombinant Prostaglandin G/H synthase 1 | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | 4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors. |
AID239884 | pKa value of the compound | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction. |
AID401494 | Inhibition of PMA-induced ear edema in Swiss mouse at 3 mg/ear after 5 hrs | 1997 | Journal of natural products, Feb, Volume: 60, Issue:2 | Isolation of two flavonoids from Tanacetum microphyllum as PMA-induced ear edema inhibitors. |
AID194136 | Ability to inhibit Mycobacterium butyricum induced inflammatory hind paw edema in rats | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and quantitative structure-activity relationships of diclofenac analogues. |
AID1454302 | Analgesic activity in mouse at 100 mg/kg, ip measured after 60 mins at 58 degC by hot plate method | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides. |
AID160706 | In vitro inhibition of Prostaglandin G/H synthase in BSV cell line. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity. |
AID1650568 | Analgesic activity in Wistar rat assessed as reduction in acetic acid-induced writhing at 10 mg/kg, ip incubated for 30 mins followed by acetic acid addition and observed for 30 mins relative to control | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID683869 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip measured 3.5 hrs after carrageenan challenge | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Α-aryl-N-alkyl nitrones, as potential agents for stroke treatment: synthesis, theoretical calculations, antioxidant, anti-inflammatory, neuroprotective, and brain-blood barrier permeability properties. |
AID681136 | TP_TRANSPORTER: inhibition of Taurocholate uptake in OAT-K2-expressing MDCK cells | 1999 | Molecular pharmacology, Apr, Volume: 55, Issue:4 | Cloning and functional characterization of a new multispecific organic anion transporter, OAT-K2, in rat kidney. |
AID1601226 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as ear edema formation at 0.5 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration (Rvb = 17.61 to 19.82 mg) | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID747928 | Inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins prior to arachidonic acid challenge measured after 30 mins by radioimmunoassay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID1764401 | Ratio of drug concentration in brain to plasma of P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID161470 | Concentration required to inhibit human prostaglandin G/H synthase 1 (COX-1) by 50% | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | 1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents. |
AID488198 | Inhibition of 5-lipoxygenase in human whole blood assessed as inhibition of 5-hydroxyeicosatetraenoic acid production by HPLC method | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID1866127 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of TNF-alpha production at 84 uM incubated for 2 hrs followed by LPS stimulation for 20 hrs by ELISA relative to control | 2022 | Journal of natural products, 04-22, Volume: 85, Issue:4 | Synthesis, Biological Evaluation, and Molecular Docking Study of 3-Amino and 3-Hydroxy- |
AID567037 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw oedema at 0.01 mmol/kg, ip | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities. |
AID337153 | Inhibition of carrageenan-induced edema in po dosed Wistar rat paw | |||
AID748529 | Selectivity ratio for human COX1 over human COX2 | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1251036 | Inhibition of COX1 (unknown origin) assessed as PGH2 production at 10 uM by measuring PGH2alpha level by enzyme immunoassay | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis. |
AID170722 | Percent changes of hind paw edema and severity scores compared to control animals at 0.7 micro mol/kg/day | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID597265 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip administered simultaneously with carrageenan measured after 3.5 hrs relative to control | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis, in silico docking experiments of new 2-pyrrolidinone derivatives and study of their anti-inflammatory activity. |
AID1737622 | Analgesic activity in albino mouse assessed as protection at 10 mg/kg, ip measured after 30 mins by hot plate test (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID222778 | In vitro inhibition of collagen-induced human platelet aggregation. | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | 6-Aryl-4,5-dihydro-3(2H)-pyridazinones. A new class of compounds with platelet aggregation inhibiting and hypotensive activities. |
AID393213 | Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production by radioimmunoassay | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | Inhibition of iNOS and COX-2 in human whole blood ex vivo and monocyte-macrophage J774 cells by a new group of aminothiopyrimidone derivatives. |
AID182707 | Compound was tested for the inhibition of rat reversed passive Arthus pleurisy after peroral administration of 10 mg/kg dose at 0.44 mL of exudate volume with 0.55 mL of control (injected intrapleurally) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel synthesis and potent antiinflammatory activity of 4-hydroxy-2(1H)-oxo-1-phenyl-1,8-naphthyridine-3-carboxamides. |
AID184915 | Percent inhibition of carrageenan-induced foot-pad edema at 30 mg/kg po; no data | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID1150252 | Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced paw edema | 1976 | Journal of medicinal chemistry, Jul, Volume: 19, Issue:7 | 6,11-Dihydro-11-oxodibenz [b,e] oxepinacetic acids with potent antiinflammatory activity. |
AID1397090 | Selectivity ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Synthesis and biological properties of aryl methyl sulfones. |
AID266763 | Membrane retention in 70% silicon-30% IPM membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability. |
AID666602 | Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay in the absence of LPS | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. |
AID1060437 | Selectivity index, ratio of IC50 for mouse J774 cells to IC50 for human KB-3-1 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis of novel 2-cyano substituted glycyrrhetinic acid derivatives as inhibitors of cancer cells growth and NO production in LPS-activated J-774 cells. |
AID1576178 | Hepatotoxicity in rat assessed as effect on portal veins at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID131592 | Tested for ability to inhibit the topical inflammatory response in the topical mouse ear(TME) model | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Antioxidant-based inhibitors of leukotriene biosynthesis. The discovery of 6-[1-[2-(hydroxymethyl)phenyl]-1-propen-3-yl]-2,3-dihydro-5- benzofuranol, a potent topical antiinflammatory agent. |
AID448016 | Inhibition of COX1-mediated PGH2 production by enzyme immunoassay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain. |
AID1416420 | Anti-inflammatory activity in human RBC assessed as inhibition of hypotonic solution-induced hemolysis after 10 mins by spectrophotometric method | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Synthesis and molecular docking studies of xanthone attached amino acids as potential antimicrobial and anti-inflammatory agents. |
AID681118 | TP_TRANSPORTER: transepithelial transport in Caco-2 cells | 2003 | International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2 | Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. |
AID173209 | Gastrointestinal tolerability was evaluated in rats and amount blood loss was reported. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID351820 | Growth inhibition of human NCI60 cells | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Design, synthesis and anticancer activities of hybrids of indole and barbituric acids--identification of highly promising leads. |
AID649092 | Inhibition of human recombinant COX-2 at 6 uM | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives. |
AID717356 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured at 270 mins after carrageenan challenge by plethysmographic analysis | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24 | Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones. |
AID409540 | Antiarthritic activity in Albino rat assessed as inhibition of Freund's complete adjuvant-induced paw volume at 10 mg/kg, po administered for 14 days daily once starting a day before adjuvant challenge measured on day 8 | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID462318 | Inhibition of mouse COX2 | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. |
AID205269 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
AID396997 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema volume at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 4 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Facile synthesis of bis(4,5-dihydro-1H-pyrazole-1-carboxamides) and their thio-analogues of potential PGE(2) inhibitory properties. |
AID1156830 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 5 hrs relative to control | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID1336924 | Cytotoxicity against human HCT116 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID386858 | Antiinflammatory activity in Wistar rat assessed as inhibition of formalin-induced paw oedema volume at 10 mg/kg, po administered 30 mins before formalin challenge after 5 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID1743655 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID640124 | Antioxidant activity in carrageenan-stimulated ICR mouse assessed as increase in SOD activity at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID692103 | Inhibition of gamma secretase assessed as reduction in Abeta42 production | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs. |
AID1351156 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID1569919 | Selectivity index, ratio of IC50 for ovine COX-1 to IC50 for human COX-2 | |||
AID1455865 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition carrageenan-induced paw edema at 5 mg/kg, ip pretreated for 30 mins followed by carrageenan challenge measured up to 8 hrs post carrageenan challenge | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
AID1441594 | Antiinflammatory activity in arachidonic acid-induced ear dermatitis ICR mouse model assessed as reduction in ear swelling at 3 mg administered twice tropically 30 mins prior and 15 mins after arachidonic acid addition measured 60 mins post arachidonic ac | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID1716956 | Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPT | |||
AID114055 | Oral analgesic activity was determined in mice by the acetylcholine-induced abdominal constriction assay upon ip administration of acetylcholine bromide 5 hours following oral administration | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID1455998 | Antiinflammatory activity in formalin-induced nociception Swiss mouse model assessed as reduction in time spent licking formalin injected hind paw during neurogenic phase at 100 umol/kg, po pretreated for 1 hr followed by formalin challenge measured up to | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
AID409550 | Antipyretic activity in Wistar rat assessed as change in LPS-induced rectal temperature at 10 mg/kg, po administered 30 mins before LPS challenge after 2 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID381055 | Activation of PPARgamma transfected in human MCF7 cells at 100 to 300 uM after 48 hrs by luciferase reporter gene assay | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4 | Bioassay for the identification of natural product-based activators of peroxisome proliferator-activated receptor-gamma (PPARgamma): the marine sponge metabolite psammaplin A activates PPARgamma and induces apoptosis in human breast tumor cells. |
AID355028 | Inhibition of prostaglandin synthesis in bovine seminal vesicle microsomes using [14C]arachidonic acid | 1996 | Journal of natural products, Jun, Volume: 59, Issue:6 | Isolation of two new antiinflammatory biflavanoids from Sarcophyte piriei. |
AID284325 | Inhibition of ovine COX2 | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
AID1454298 | Anti-inflammatory activity in mouse model of xylene-induced ear edema assessed as inhibition of ear edema at 10 mg/kg, ip pre-treated before xylene injection and measured 1 hr post xylene injection relative to untreated control | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides. |
AID161987 | Percentage of inhibition of Prostaglandin G/H synthase 1 activity in human whole blood (HWB) at 10 uM | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines. |
AID1402010 | Antiinflammatory activity in carrageenan-induced paw edema rat model assessed as inhibition of carrageenan-induced edema relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Quinoxaline: An insight into the recent pharmacological advances. |
AID1456028 | Antiinflammatory activity in formalin-induced nociception Swiss mouse model assessed as reduction in time spent licking formalin injected hind paw during inflammatory phase at 100 umol/kg, po pretreated for 1 hr followed by formalin challenge measured aft | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
AID6860 | Inhibition of 5-lipoxygenase in intact RBL-1 cell line | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase. |
AID1543425 | Antiinflammatory activity in TPA-induced ICR mouse ear edema model assessed as reduction in neutrophil content AUC at 1 mg/ear applied topically measured 4 hrs post-TPA challenge by giemsa staining-based microscopic method relative to control | |||
AID178647 | Antiinflammatory activity was evaluated in an carrageenan edema (acute inflammation) test, after administering compound orally in rats. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID598196 | Inhibition of ram seminal vesicle COX1 assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Synthesis and evaluation of carbaborane derivatives of indomethacin as cyclooxygenase inhibitors. |
AID1392317 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, po measured at 1 hr relative to control | |||
AID178641 | Antiinflammatory activity by using Rat hyperalgesia assay | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile. |
AID1852379 | Antiinflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as decrease in IL-1 beta protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID540232 | Dose normalised AUC in monkey after po administration | 2005 | Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2 | Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. |
AID1699364 | Inhibition of human COX1 | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. |
AID1063325 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID1220556 | Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID287608 | Antiinflammatory activity in Wistar Albino rat assessed as inhibition of carrageenan-induced paw oedema at 5 mg/kg, ip after 2 hrs | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID536472 | Acute toxicity in ip dosed albino mouse after 24 hrs | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Use of phosphonyl carbanions in the synthesis of anti-inflammatory active phosphorus-containing fused heterocycles and relevance phosphonates. |
AID1174282 | Antiinflammatory activity in Sprague-Dawley rat model of LPS-induced sepsis assessed as MPO level at 5 mg/kg/day dosed through gastric intubation for 6 days (Rvb = 4.2 +/- 1.8 mg/L) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents. |
AID1662947 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 2 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID1334728 | Ulcerogenic effect in albino rat assessed as ulcer index at 20 mmol/kg, po administered 2 to 3 days | |||
AID1123741 | Antiarthritic activity in po dosed rat assessed as reduction of adjuvant-induced foot volume administered as qd for 14 days starting on day 14 after adjuvant inoculation measured on day 28 | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids. |
AID1569920 | Inhibition of soyabean 15-LOX preincubated for 5 mins followed by susbtrate addition measured after 10 mins by colorimetric method | |||
AID640116 | Antiinflammatory activity in ICR mouse assessed as decrease in carrageenan-induced serum TNFalpha level at 10 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1141758 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors. |
AID1241858 | Renal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as total protein level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 1.78 +/- 0.11 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1353368 | Antinociceptive activity in formalin-induced Swiss mouse model of hyperalgesia assessed as time spent licking the injected paw in last phase at 100 mM/kg, po pretreated for 1 hr followed by formalin injection and measured at 20 to 30 mins (Rvb = 135.8 +/- | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
AID224065 | Antiinflammatory activity against D-adjuvant arthritis in uninjected rat paw at the dose of 50 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2 | Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents. |
AID168893 | Analgesic activity evaluated by measuring % analgesic effect, after oral administration of 120 mg/kg in acetic acid writhing test | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID77205 | Tested for effect on the production of Lipoxygenase (LO) metabolite, 5,12-diHETE in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID1675146 | Anti-inflammatory activity in human HaCaT cells assessed as inhibition of LPS-induced IL-6 production at 10 uM after 24 hrs by ELISA relative to LPS alone | 2020 | Journal of natural products, 08-28, Volume: 83, Issue:8 | Labdane-Type Diterpenes from the Aerial Parts of |
AID1810795 | Inhibition of COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production by ELISA (Rvb = 2.0 ng/mL ) | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID430147 | Antiinflammatory activity against bradykinin-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before bradykinin challenge measured after 120 mins by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID1209583 | Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID116673 | Analgesic activity was measured by phenylquinone writhing test in male Swiss albino mice at dose of 12 mg/Kg sc after 5 hr | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Synthesis of N-[[(substituted-phenyl)carbonyl]amino]-1,2,3,6-tetrahydropyridines with analgesic and hyperglycemic activity. |
AID178917 | Effective dose required for antiinflammatory activity by pyresis assay tested in vivo | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID1852381 | Antiinflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as decrease in TNF-alpha protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID667602 | Antiinflammatory activity in Wistar albino rat assessed as reduction of carrageenan-induced paw edema at 20 mg/kg, po measured after 2 hrs by plethysmometer | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Regioselective reaction: synthesis, characterization and pharmacological activity of some new Mannich and Schiff bases containing sydnone. |
AID688624 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as reduction in AUC of global leukocyte infiltration-based myeloperoxidase activity at 0.4 umol administered topically per cm'2 of ear measured 3 to 48 hrs post dermatitis induction rela | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID114543 | Tested for inhibitory activity after administration of compound at 50 mg/kg perorally using AcOH writhing method; 1.5-6.5 | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Nonsteroidal antiinflammatory agents. 3. Synthesis of the positional isomers of 4'-chloro-5-methoxy-3-biphenylylacetic acid and their antiinflammatory and analgesic activities. |
AID295467 | Antiinflammatory activity in Swiss mouse assessed as inhibition of carrageenan-induced hind paw oedema at 35 mg/kg, po after 4 hrs | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents. |
AID1336955 | Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at lesser G1 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 1.59%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID178493 | Antiinflammatory activity against adjuvant induced arthritis in male charles river rats | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Antiinflammatory 4,5-diarylpyrroles: synthesis and QSAR. |
AID1854722 | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
AID592803 | Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. |
AID1145133 | Antiinflammatory activity in rat assessed as inhibition of adjuvant-induced arthritis administered for 9 days into foot pad 14 days after adjuvant challenge measured on day 22 by mercury displacement analysis | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1, 3, 4, 9-tetrahydropyrano[3, 4-b]indole-1-acetic acids. |
AID376763 | Inhibition of COX1 from ram seminal vesicles by liquid scintillation counter | 2005 | Journal of natural products, Jan, Volume: 68, Issue:1 | Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2. |
AID404565 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced edema at 50 mg/kg, po after 2 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID1220241 | Intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID1241877 | Inhibition of ovine COX2 by oxidized TMPD detection based colorimetric assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID123810 | Inhibition of phenylquinone -induced writhing in male mice by p.o. administration 20 min prior to i.p. phenylquinone (relative to aspirin). | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids. |
AID295471 | Effect on thermal pain in Swiss mouse at 35 mg/kg, po after 1 hr by hot plate test | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents. |
AID1852367 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as reduction of IL-1beta protein expression at 10 uM in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by Western blot | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1392321 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, po measured at 5 hrs relative to control | |||
AID364548 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip after 1 hrs | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives. |
AID77217 | Tested for effect on the production of cyclooxygenase (COX) metabolite, PGF2-alpha (prostaglandin F2-alpha) of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID124988 | Inhibition of phenylbenzoquinone writhing in mice was tested at the dose of 3 mg/kg for 1 hr | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID160863 | Inhibition of PGE-2 production in 3T3 (murine fibroblast) cell culture. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity. |
AID1199427 | Analgesic activity in Swiss Albino acetic acid-induced writhing mouse model assessed as protection at 20 mg/kg, po administered 30 mins before to acetic acid challenge measured for 10 mins | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID178378 | Effective dose against nystatin edema(peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
AID666601 | Inhibition of iNOS in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production for 2 hrs by DAF-FMDA dye based fluorometric assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. |
AID624700 | Mechanism based inhibition of rat cytochrome P450 CYP3A2 | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1254095 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 50 mg/kg, po administered 24 hrs before xylene challenge relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. |
AID304242 | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 1 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID114054 | Oral analgesic activity was determined in mice by the acetylcholine-induced abdominal constriction assay upon ip administration of acetylcholine bromide 20 min following oral administration | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID288822 | Inhibition of ovine COX2 by enzyme immuno assay | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | O2-acetoxymethyl-protected diazeniumdiolate-based NSAIDs (NONO-NSAIDs): synthesis, nitric oxide release, and biological evaluation studies. |
AID241917 | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | 1,5-Diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors. |
AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID223906 | The compound was tested for Granuloma generation on CMC-LPS air-pouch model at 3 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives. |
AID600514 | Antiinflammatory activity in mouse assessed as inhibition of TPA-induced ear edema measured per ear | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Hop (Humulus lupulus)-derived bitter acids as multipotent bioactive compounds. |
AID1576177 | Hepatotoxicity in rat assessed as effect on central veins in liver at 50 mg/kg by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1301939 | Inhibition of COX1 in healthy human whole blood assessed as calcium ionophore A23187-stimulated TXB2 level at 1 uM preincubated for 60 mins followed by A23187 addition measured after 30 mins by ELISA (Rvb = 8.5 ng/ml) | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent. |
AID77483 | Inhibition of Collagen-induced serum Thromboxane (TXB2) in guinea pig whole blood ex vivo after 10 mg/kg oral administration of compound. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids. |
AID1278583 | Antiinflammatory activity in mouse RAW264.7 assessed as decrease in LPS-induced IL-6 production at 10 uM pretreated with 1 ug/ml LPS for 22 hrs followed by addition of compound for 24 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5 | Hesperetin derivatives: Synthesis and anti-inflammatory activity. |
AID453641 | Inhibition of COX1 in platelets assessed as inhibition of 12-HHT formation at 10 uM by RP-HPLC | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID249667 | Effect of compound (10 uM) on doxorubicin-induced cytotoxicity towards T98G cell line expressing multidrug resistance associated protein 1 (MRP-1); Active | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Modulation of MRP-1-mediated multidrug resistance by indomethacin analogues. |
AID1662946 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 1 hr followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID1193494 | Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1852382 | Antiinflammatory activity in LPS/hypoxia induced CA9 knockdown rat H9c2 cells assessed as decrease in IL-1 beta protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID426422 | Antioxidant activity against hydroxyl radical assessed as inhibition of formaldehyde production at 0.1 mM after 30 mins relative to DMSO | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts. |
AID753751 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po after 5 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1155601 | Inhibition of COX2-mediated PGD2 formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID1437462 | Ulcerogenic effect in albino rat assessed as congestion of blood vessels at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID186587 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 0.1 mg/kg at time interval- 4 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID449634 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po after 4 hrs relative to control | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines. |
AID763777 | Antinociceptive activity in Swiss albino mouse assessed as inhibition of formalin-induced flinching at 5 mg/kg administered 30 mins prior to test measured for 10 to 30 mins relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: synthesis and neuropharmacology. |
AID92677 | In vitro inhibition of arachidonic acid induced platelet aggregation of human platelet-rich plasma | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | 9,11-Epoxy-9-homo-14-oxaprosta-5-enoic acid derivatives. Novel inhibitors of fatty acid cyclooxygenase. |
AID705365 | Partial antagonist activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced shape change by FACS analysis | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. |
AID409541 | Antiarthritic activity in Albino rat assessed as inhibition of Freund's complete adjuvant-induced paw volume at 10 mg/kg, po administered for 14 days daily once starting a day before adjuvant challenge measured on day 3 | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID1568915 | Analgesic activity in Wistar rat model of acetic-acid-induced writhing assessed as inhibition of writhing numbers at 10 mg/kg, ip preincubated for 30 mins followed by acetic acid induction and measured for 30 mins | |||
AID1891740 | Induction of mitochondrial outer membrane damage in human MCF7 cells assessed as morphological changes by measuring elongated mitochondria at IC50 measured after 24 hrs by mitotracker red based confocal microscopy | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID300444 | Antiinflammatory activity against carrageenan-induced hind paw oedema in mouse assessed as inhibition of swelling thickness at 10 mg/kg, po after 90 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | 1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities. |
AID688457 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.4 umol administered topically per cm'2 of ear measured 3 hrs after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1852404 | Reversal of ATP level in LPS/hypoxia induced rat H9c2 cells in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by multimode plate reader analysis (Rvb = 21.37 nmol/mg) | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1336925 | Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID192058 | Compound was tested for reduction of streptococcal cell wall(SCW) in rats at a dose of 0.67 mg/kg | 1998 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14 | Novel cytokine release inhibitors. Part I: Triterpenes. |
AID196878 | Compound was evaluated for its gastroulcerogenic effect in rats at a peroral dose of 200 mg/kg, P<0.05. | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. |
AID464516 | Selectivity for human HEK293 cells over human HMEC | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1199430 | Inhibition of carrageenan-induced NFkappaB expression in paw tissue (unknown origin) by immunohistochemistry | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID182956 | In vivo inhibitory dose in adjuvant-induced arthritis in rats | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors. |
AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID748511 | Selectivity ratio of IC50 for wild type mouse COX2 to IC50 for mouse COX2 V523I mutant | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID420036 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema volume at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 2 hrs | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis of [1,2,4]triazolo[1,5-a]pyridines of potential PGE2 inhibitory properties. |
AID409567 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema volume at 10 mg/kg, po administered 60 mins before carrageenan challenge after 1 hr relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID464324 | Cytotoxicity against human HepG2 cells after 72 hrs by luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID757494 | Gastrointestinal toxicity in Wistar rat assessed as ulcerogenic index at 60 mg/kg, po after 6 hrs relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity. |
AID774823 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 1 hr before carrageenan challenge measured at 1 hr relative to control | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Design, synthesis and biological evaluation of novel anti-cytokine 1,2,4-triazine derivatives. |
AID209198 | Concentration required to inhibit production of arachidonic acid from THP-1 cells stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID1220257 | Ratio of drug level in blood to plasma in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID1550475 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 1 hr post-carrageenan injection (Rvb = 30.3%) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID161610 | Effect on the synthesis of metabolites of arachidonic acid in human platelets | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid. |
AID1204235 | Ulcerogenic activity in Wistar rat assessed as ulcer index at 10 mg/kg, po administered 3 days relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. |
AID1203974 | Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells using L-Arginine substrate incubated for 2 hrs by fluorescence spectrometry | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | Synthesis and biological evaluation of novel pyrazoline derivatives as potent anti-inflammatory agents. |
AID1667503 | Antiinflammatory activity in albino rat assessed as reduction in carrageenan-induced paw edema by measuring thickness of right paw at 28 uM/kg, ip measured at 3 hrs by calliper method (Rvb = 7.83 +/- 0.33 cm) | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1241842 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 15 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID396558 | Antiinflammatory activity against cotton pellets-induced inflammation in Wistar rat assessed as final weight of granuloma at 5 mg/kg, po after 7 days | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and anti-inflammatory activity evaluation of unsymmetrical selenides. |
AID161596 | In vitro inhibitory activity on platelet aggregation induced by arachidonic acid (AA) | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3 | Synthesis of 4-alkoxy-2-phenylquinoline derivatives as potent antiplatelet agents. |
AID1220791 | Ratio of drug level in blood to plasma in monkey | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID1199423 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 5 hrs relative to vehicle-treated control | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID1193498 | Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1310741 | Antiinflammatory activity in BALB/c mouse assessed as inhibition of croton oil-induced ear edema at 33 mg/kg administered topically on ear measured at 6 hrs | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | 2-Aryl-3-(2-morpholinoethyl)thiazolidin-4-ones: Synthesis, anti-inflammatory in vivo, cytotoxicity in vitro and molecular docking studies. |
AID634933 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 30 mins prior to challenge measured after 3 hrs relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID1502266 | Inhibition of LPS-induced TNFalpha production in mouse BV2 cells at 100 uM pre-incubated before LPS stimulation by ELISA | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | TNF-α and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents. |
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AID181418 | Antiinflammatory activity evaluated as Minimum effective oral dose that inhibits adjuvant arthritis in rats | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | 1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities. |
AID748521 | Inhibition of mouse COX2 V523I mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID182304 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 4 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1333295 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw oedema at 50 mg/Kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents. |
AID1540295 | Antiinflammatory activity against carrageenan-induced paw oedema in ICR mouse assessed as inhibition of paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured at 2 hrs post carrageenan challenge relative to control | |||
AID135221 | Inhibitory activity against carrageenan induced paw edema at a oral dose of 10 mg/kg in mouse 3 hours after carrageenan administration | 1998 | Journal of medicinal chemistry, Aug-13, Volume: 41, Issue:17 | Synthesis and comparison of the antiinflammatory activity of manoalide and cacospongionolide B analogues. |
AID1057593 | Inhibition of ovine COX1 using arachidonic acid as substrate at 10 uM incubated 5 mins prior to substrate addition measured after 5 mins by HPLC analysis | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. |
AID449538 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po after 1 hr relative to control | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines. |
AID1174767 | Antioxidant activity in Wistar rat assessed as thiobarbituric acid reactive substance level measured per mg of protein at 150 umol/kg, po administered for 3 days measured on day 4 (Rvb = 3.72 +/- 00.23 nmol) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Benzimidazole--ibuprofen/mesalamine conjugates: potential candidates for multifactorial diseases. |
AID1436698 | Antiinflammatory activity in carrageenan-induced rat paw edema model assessed as inhibition of lipid peroxidation at 20 mg/kg, po administered 1 hr followed by carrageenan challenge | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID23672 | Partition coefficient (logP) | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Accumulation of drugs by guinea pig isolated atria. Quantitative correlations. |
AID328206 | Inhibition of COX2 | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID1426401 | Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID693576 | Analgesic activity in mouse assessed as inhibition of acetic-acid induced writhing at 10 mg/kg administered 15 mins prior to acetic acid-challenge measured for 15 mins relative to vehicle-treated control | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives. |
AID310931 | Partition coefficient, log P of the compound | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
AID703405 | Selectivity ratio of IC50 for AKR1C2 to IC50 for AKR1C3 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
AID1155582 | Inhibition of 12-LO in human neutrophils assessed as residual activity relative to control | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID420058 | Inhibition of COX2 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives. |
AID1852356 | Stability of the compound assessed as NTR (unknown origin) mediated hydrolysis by measuring half life by UV spectrophotometry | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID55271 | Concentration required to inhibit human Cytosolic phospholipase A2 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID1067405 | Inhibition of ovine COX2 at 50 uM by peroxidase activity-based colorimetric assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles. |
AID337675 | Antiinflammatory activity against TPA-induced Swiss mouse ear edema assessed as reduction in ear swelling at 0.25 mg/ear topically after 4 hrs relative to control | 2003 | Journal of natural products, Sep, Volume: 66, Issue:9 | Griffonianone D, an isoflavone with anti-inflammatory activity from the root bark of Millettia griffoniana. |
AID183403 | Inhibition of secondary paw swelling in rat adjuvant arthritis model at 1 mg/kg b.i.d. | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID549591 | Antiinflammatory activity in CD1 mouse assessed as inhibition of croton oil-induced ear edema at 1 umol administered topically per cm'2 of ear relative to control | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives. |
AID177102 | ED50 was measured by CFE assay method. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID339130 | Inhibition of platelet activity factor-induced platelet aggregation in rabbit platelet-rich plasma at 100 ug/mL after 3 mins by turbidimetric method | 1993 | Journal of natural products, Jun, Volume: 56, Issue:6 | Antiplatelet effects and vasorelaxing action of some constituents of Formosan plants. |
AID193133 | inhibition of swelling in rat paw edema was measured at a dose of 2.8 micro mol/kg/day for days 14-25 | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID729243 | Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 after 20 mins by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
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AID305969 | Anticoagulant activity assessed as inhibition of thrombin induced rabbit platelet aggregation | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents. |
AID674715 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 4 hrs before carrageenan challenge measured 1 hr post carrageenan-induced inflammation | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID115379 | Inhibitory against carrageenan induced paw edema in mice at 12 mg/kg, sc dose after 5 hr | 1982 | Journal of medicinal chemistry, Feb, Volume: 25, Issue:2 | Synthesis of N-(carbonylamino)-1,2,3,6-tetrahydropyridines with analgesic, antiinflammatory, and hyperglycemic activity. |
AID266764 | Membrane permeability, CA(t)/CD(0) in 70% silicon-30% IPM membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability. |
AID687439 | Gastric toxicity in Swiss mouse assessed as edema index at 10 mg/kg administered as single dose (Rvb = 0.6 +/- 0.2 edema index) | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Mechanisms involved in the antinociceptive effects of 7-hydroxycoumarin. |
AID418091 | Toxicity in carrageenan treated Albino mouse liver assessed as cholestasis at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs by hematoxilen eosine staining | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent. |
AID432717 | Gastrointestinal toxicity in Swiss albino mouse assessed as ulcerogenic effect at 100 mg/kg, po | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID160716 | Inhibition of Prostaglandin G/H synthase from bovine seminal vesicle at 20 uM concentration | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes. |
AID469575 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema measured after 2 hrs at 6 mg/kg, po administered 1 hr before carrageenan challenge | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs. |
AID592747 | Antiamyloidogenic activity in mouse N2A cells transfected with human APP Swedish mutant assessed as reduction of amyloid beta (1 to 42) level at 100 uM after 24 hrs by ELISA relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID382815 | Selectivity for human recombinant COX2 over human platelet COX1 | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents. |
AID180759 | Exudate volume was determined after administration at a dose of 100 umol/kg in the carrageenan-induced rat pleurisy assay | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID1262452 | Ulcerogenic activity in rat assessed as ulcer index at 100 mg/kg | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors. |
AID1155584 | Inhibition of 15-LO in human neutrophils assessed as residual activity relative to control | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. |
AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1332269 | Antiinflammatory activity in Wistar rat assessed as inhibition of PGE2-induced paw edema at 10 mg/kg, po administered 30 mins prior to PGE2 treatment measured after 3 hrs | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2 | In vivo and in silico anti-inflammatory mechanism of action of the semisynthetic (-)-cubebin derivatives (-)-hinokinin and (-)-O-benzylcubebin. |
AID536609 | Analgesic activity against heat induced nociception in Swiss albino mouse assessed as increase in latency at 100 mg/kg, po measured 60 mins post compound dose by hot plate method relative to pretreatment level | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives. |
AID1737625 | Analgesic activity in albino mouse assessed as forepaw licking/jumping latency time at 10 mg/kg, ip measured after 90 mins by hot plate test (Rvb = 2.72 +/- 0.01 sec) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
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AID302758 | Solubility by shake flask method | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Poorly soluble marketed drugs display solvation limited solubility. |
AID403341 | Inhibition of COX1 | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID188014 | Evaluated for acute potency in pleural effusion assay | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
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AID186441 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 0.1 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID592801 | Inhibition of ovine COX-1 at 100 uM after 2 mins by fluorescence assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. |
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AID674727 | Inhibition of COX1 by by Cayman's COX activity assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID176343 | Compound was tested in vivo for its efficacy in the rat pyresis assay | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12 | 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. |
AID1131301 | Antiinflammatory activity against rat adjuvant arthritis model assessed as reduction of swelling in non-injected foot at 1 mg/kg, po administered for 16 days | 1979 | Journal of medicinal chemistry, Dec, Volume: 22, Issue:12 | Potential antiinflammatory compounds. 3. Compounds derived from acenaphthene and indan. |
AID1717040 | Selectivity index, ratio of IC50 for sheep COX1 to IC50 for recombinant human COX2 expressed in baculovirus infected Sf21 cells | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents. |
AID674712 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po dosed 1 hr before carrageenan challenge measured 1 hr post carrageenan-induced inflammation | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID1667511 | Ulcerogenic activity in albino rat assessed as congestion of blood vessel at 10 to 50 mg/kg, po measured after 6 hrs by H and E staining based light microscopic assay | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID160599 | In vitro inhibitory concentration against rat Prostaglandin G/H synthase 2 | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors. |
AID377009 | Inhibition of ovine COX1 | 2006 | Journal of natural products, Jun, Volume: 69, Issue:6 | Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2. |
AID287288 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 100 mg/kg, po after 90 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID263719 | Inhibition of beta amyloid protein 42 in SH-SY5Y cell lines overexpressing SPA4CT at 100 uM | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. |
AID598197 | Inhibition of human COX2 expressed in SF-9 insect cells assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis | 2011 | Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10 | Synthesis and evaluation of carbaborane derivatives of indomethacin as cyclooxygenase inhibitors. |
AID1455836 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition carrageenan-induced paw edema at 5 mg/kg, ip pretreated for 15 mins followed by carrageenan challenge measured at 6 hrs post carrageenan challenge | 2018 | Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7 | Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
AID1737619 | Analgesic activity in albino mouse assessed protection against acetic acid-induced abdominal writhing at 10 mg/kg, ip pretreated for 1 hr followed by acetic acid challenge and measured starting 5 mins post acetic acid challenge for 10 mins relative to con | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1357046 | Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhings at 10 mg/kg, ip measured 30 mins post acetic acid challenge | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID640135 | Down regulation of iNOS protein expression in carrageenan-stimulated ICR mouse at 10 mg/kg, ip measured after 5 hrs by Western blot analysis | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID1459159 | Antiarthritic activity in Lewis rat Freund's adjuvant-induced arthritis model assessed as reduction in hind paw volume at 2.5 mg/kg, ig administered through gavage pretreated for 1 hr followed by adjuvant challenge subsequent treatment for 9 days measured | 2016 | Journal of natural products, 10-28, Volume: 79, Issue:10 | Effects of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. |
AID1193499 | Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1397088 | Inhibition of ovine COX1 assessed as reduction in PGH2 production by enzyme immunoassay | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14 | Synthesis and biological properties of aryl methyl sulfones. |
AID238402 | Binding affinity for mouse Prostanoid EP2 receptor | 2004 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17 | Discovery of new chemical leads for prostaglandin D2 receptor antagonists. |
AID386848 | Analgesic activity in albino mouse assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, po | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID1226816 | Selectivity index, ratio of IC50 for ovine COX-1 to human recombinant COX-2 | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes. |
AID1174768 | Antioxidant activity in Wistar rat assessed as GSH level measured per 100 mg of protein at 150 umol/kg, po administered for 3 days measured on day 4 (Rvb = 184.10 +/- 4.19 umol) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Benzimidazole--ibuprofen/mesalamine conjugates: potential candidates for multifactorial diseases. |
AID1199377 | Antiinflammatory activity in male Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured at 2 hrs of carrageenan treatment | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres. |
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AID1412713 | Inhibition of sheep COX2 at 10 uM assessed as reduction in PGE2 formation using arachidonic acid as substrate by enzyme immunoassay relative to control | |||
AID1918194 | Lipophilicity, log D of the compound | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment. |
AID1241864 | Renal toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as blood urea nitrogen level at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 (Rvb = 23.48 + | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID679945 | TP_TRANSPORTER: inhibition of MTX uptake in OAT-K1-expressing LLC-PK1 cells | 1997 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 283, Issue:3 | Interactions of nonsteroidal anti-inflammatory drugs with rat renal organic anion transporter, OAT-K1. |
AID1866121 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NO production incubated for 2 hrs followed by LPS stimulation for 20 hrs by Griess reagent based assay | 2022 | Journal of natural products, 04-22, Volume: 85, Issue:4 | Synthesis, Biological Evaluation, and Molecular Docking Study of 3-Amino and 3-Hydroxy- |
AID1437468 | Ulcerogenic effect in albino rat assessed as complete shedding of surface mucous cells leaving underlying gastric pit walls and openings with honeycomb shape at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by scanning electron mi | |||
AID403345 | Inhibition of COX1 at 0.01 mM | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1436697 | Toxicity in albino Wistar rat assessed as epithelial layer damage in stomach wall at 60 to 90 mg/kg, po after 5 hrs | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID1125127 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins before carrageenan challenge measured after 4 hrs relative to control | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID1416045 | Inhibition of Hoechst 33258 binding to calf thymus DNA up to 70 uM by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID384123 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis of novel 4,6-disubstituted quinazoline derivatives, their anti-inflammatory and anti-cancer activity (cytotoxic) against U937 leukemia cell lines. |
AID52790 | Inhibition of chymotrypsin at 250 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
AID174432 | Plasma drug level was measured in rat yeast induced hyperalgesia assay in presence of indomethacin at a dose of 10 mg/kg for 4 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1892073 | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 1 hr followed by LPS stimulation and measured after 36 hrs by Griess reagent based assay | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Phenethoxy Derivatives with Anti-inflammatory Activities from the Betelnut Endophytic |
AID161471 | IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID549589 | Antiinflammatory activity in CD1 mouse assessed as inhibition of croton oil-induced ear edema at 0.1 umol administered topically per cm'2 of ear relative to control | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives. |
AID1061774 | Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | 2014 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1 | Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities. |
AID1128714 | Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1141756 | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors. |
AID192291 | Percent swelling was measured on untreated rat paw at different dosage forms | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | 3-(5-Alkyl-4-hydroxy-3-methoxy-1-naphthalenyl)-2-methyl-2-propenoic acids as orally active inhibitors of IL-1 generation. |
AID449633 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.029 mmol/kg, po after 3 hrs relative to control | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines. |
AID408272 | Toxicity in Albino rat assessed as gastric-ulcerogenic effect at 30 uM/kg, po twice daily for 3 days | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity. |
AID116723 | Acute toxicity as LD50 value was determined in mice administered orally | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
AID623639 | Antinociceptive activity in mouse assessed as inhibition of acetic acid-induced abdominal constrictions at 10 mg/kg, ip administered 40 mins before acetic acid challenge measured for 30 mins | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antinociceptive properties of bergenin. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID304239 | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production at 0.03 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID759377 | Antiinflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured at 3 hrs by plethysmometeric analysis relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents. |
AID428416 | Inhibition of MRP1/MRP2 in White Wistar rat jejunum assessed as increase in drug uptake at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID603857 | Antiinflammatory activity in carrageenan-induced Fischer-344 rat paw oedema at 0.01 mmol/kg, ip after 3.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Curcumin analogues as possible anti-proliferative & anti-inflammatory agents. |
AID426392 | Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors. |
AID409559 | Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 10 mg/kg, po administered 60 mins before acetic acid challenge after 5 to 15 mins relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological evaluation of amide derivatives of (5,6-dimethoxy-2,3-dihydro-1H-inden-1-yl)acetic acid as anti-inflammatory agents with reduced gastrointestinal ulcerogenecity. |
AID387677 | Antiinflammatory activity against carrageenan-induced albino rat hind paw edema model assessed as edema rate at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 1 hr | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities. |
AID287613 | Antiinflammatory activity against carrageenan-induced paw oedema in Wistar Albino rat assessed as mean swelling paw volume at 5 mg/kg, ip after 3 hrs | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID303566 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 3 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID232623 | Relative inhibitory activity against COX-1 and COX-2 | 1999 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12 | 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors. |
AID1330203 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, po administered 5 hrs before xylene challenge measured after 3 hrs | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID54712 | Inhibition of PGE-2 production in CHO cells expressing human COX-2. | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22 | Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors. |
AID578766 | Inhibition of MRP1 expressed in human 2008 cells assessed as calcein AM accumulation by cell based assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP). |
AID1416044 | Inhibition of acridine orange binding to calf thymus DNA up to 80 uM by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID177361 | Antiinflammatory activity was evaluated in an adjuvant arthritis (subchronic inflammation) test, after administering compound orally in rats. | 1984 | Journal of medicinal chemistry, Mar, Volume: 27, Issue:3 | Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid. |
AID604020 | Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID315578 | Inhibition of carrageenan-induced hind paw edema in rat assessed as decrease in paw volume at 10 mg/kg, po after 5 hrs | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. |
AID1256770 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw oedema at 0.15 mmol/kg, ip administered 5 mins before carrageenan challenge measured after 3.5 hrs | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Esters of some non-steroidal anti-inflammatory drugs with cinnamyl alcohol are potent lipoxygenase inhibitors with enhanced anti-inflammatory activity. |
AID77209 | Tested for effect on the production of Lipoxygenase (LO) metabolite, 5-HETE in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID287614 | Antiinflammatory activity against carrageenan-induced paw oedema in Wistar Albino rat assessed as mean swelling paw volume at 5 mg/kg, ip after 4 hrs | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Novel synthesis of [1]-benzothiepino[5,4-b]pyridine-3-carbonitriles and their anti-inflammatory properties. |
AID1437466 | Ulcerogenic effect in albino rat assessed as induction of necrosis in gastric mucosal cells at 50 umol/kg, po qd administered for 3 days measured 1 hr post last dose by hematoxylin/eosin staining-based light microscopic method | |||
AID192518 | Percent inhibition of carrageenan induced rat paw edema 3 hr after a peroral administration of 0.5 mg/kg | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Nonsteroidal antiinflammatory agents. 3. Synthesis of the positional isomers of 4'-chloro-5-methoxy-3-biphenylylacetic acid and their antiinflammatory and analgesic activities. |
AID763783 | Neurotoxicity in Swiss albino mouse assessed as minimal motor impairment at 300 mg/kg after 4 hrs by rotarod test | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: synthesis and neuropharmacology. |
AID420059 | Inhibition of COX1 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives. |
AID396562 | Acute toxicity in po dosed mouse assessed as death within 7 days | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis and anti-inflammatory activity evaluation of unsymmetrical selenides. |
AID46852 | IC50 against recombinant human Prostaglandin G/H synthase 2 | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID502271 | Inhibition of sheep COX2 at 10 uM by enzyme immunoassay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors. |
AID674721 | Gastrointestinal toxicity in Wistar albino rat assessed as incidence of stomach ulceration at 0.029 mmol/kg, po | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID374108 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po after 2 hrs | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1456101 | Resistant factor, ratio of IC50 for human Bel7402/5-FU cells to IC50 for human Bel7402 cells | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and biological evaluation of novel podophyllotoxin-NSAIDs conjugates as multifunctional anti-MDR agents against resistant human hepatocellular carcinoma Bel-7402/5-FU cells. |
AID1852400 | Reversal of LPS/hypoxia induced mitochondrial membrane potential loss in rat H9c2 cells assessed as increase in JC-1 polymer morphology in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by JC- | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID303578 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 5 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID721753 | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
AID155902 | Compound was evaluated for the inhibition of PLA2. | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis. |
AID386856 | Antiinflammatory activity in Wistar rat assessed as inhibition of formalin-induced paw oedema volume at 10 mg/kg, po administered 30 mins before formalin challenge after 4 hrs relative to control | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins. |
AID1228723 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 25 uM after 24 hrs by Griess assay relative to control | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Anti-inflammatory Terpenoids from the Leaves and Twigs of Dysoxylum gotadhora. |
AID1852370 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as increase in VEGF expression at 10 uM in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID552764 | Antiinflammatory activity against histamine-induced mouse edema model assessed as inflammation index 20 mg/kg, po (untreated control = 32.6+/-3.1%) | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Rapid access to new bioconjugates of betulonic acid via click chemistry. |
AID181536 | Antiinflammatory efficacy is measured by the percent inhibition of edema in carrageenan induced rats during the 3 week adjuvant arthritis test | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID1181953 | Apparent permeability in human Caco2 cells | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Straightforward entry to pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones and their ADME properties. |
AID1244193 | Inhibition of rat seminal vesicles COX-1 using arachidonic acid as substrate at 50 ug/ml preincubated for 5 mins followed by substrate addition after 20 mins by competitive PGE2 EIA method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis of new 4-phenylpyrimidine-2(1H)-thiones and their potency to inhibit COX-1 and COX-2. |
AID693575 | Ulcerogenic activity in Wistar albino rat assessed as ulcer index at 10 mg/kg, ip administered QD for 3 days | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives. |
AID1150001 | Antiinflammatory activity in po dosed Wistar rat assessed as inhibition of carrageenan-induced paw edema administered 1 hr prior to carrageenan challenge measured after 3 hrs of carrageenan challenge | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 3. omega-(6,11-Dihydro-11-oxodibenz[b,e]oxepin-2-yl)alkanoic acids. |
AID1149353 | Antiinflammatory activity against Mycobacterium butyricum adjuvant-induced polyarthritis in po dosed Lewis albino rat assessed as decrease in adjuvant treated paw edema administered daily for 21 days prior to adjuvant injection | 1977 | Journal of medicinal chemistry, Jan, Volume: 20, Issue:1 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 1. 6,11-Dihydro-11-oxodibenz]b,e]oxepin-2-acetic acids. |
AID177164 | In vivo effective dose required for antiinflammatory activity in rat adjuvant arthritis model | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition. |
AID1576173 | Ulcerogenic activity in rat assessed as average severity of ulcers formed at 50 mg/kg, sc qd for 4 days post 18 hrs fasting measured after 4 days | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID611507 | Antiinflammatory activity against Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 5 hrs | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6 | Vicenin-2, a potential anti-inflammatory constituent of Urtica circularis. |
AID165496 | In vitro of platelet aggregation of citreated rabbit platelet-rich plasma, induced by collagen at 5 uM; value expressed as slope | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID640222 | Antiinflammatory activity in carrageenan-stimulated ICR mouse assessed as decrease in neutrophil number at 8 mg/kg, ip measured after 5 hrs | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions. |
AID169639 | Compound is evaluated for gastric ulceration in rats at a dose of 100 mg/kg; Not tested | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID649272 | Dissociation constant, pKa of the compound | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation. |
AID670254 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, ip dosed 30 mins before carrageenan challenge measured before 6 hrs post carrageenan challenge | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | In vitro stability and in vivo anti-inflammatory efficacy of synthetic jasmonates. |
AID591429 | Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse RAW 264.7 cells treated 2 hrs before LPS challenge measured after 18 hrs by Griess reaction method | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID748515 | Selectivity ratio of IC50 for wild type mouse COX2 to IC50 for mouse COX2 V349L mutant | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID325066 | Inhibition of ovine COX1 pre-incubated before addition of [1-14C]arachidonic acid | 2007 | The Journal of biological chemistry, Jun-01, Volume: 282, Issue:22 | Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib. |
AID1241846 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID579632 | Antiinflammatory activity against human neutrophil assessed as inhibition of N-formyl-l-methionyl phenylalanine/cytochalasin B-induced superoxide anion generation by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl-β-carboline and 1-benzoyl-3-carboxy-β-carboline derivatives. |
AID184061 | Inhibitory effect of compound on carrageenan-induced rat paw edema administered p.o. at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | 2,3-diarylpyran-4-ones: a new series of selective cyclooxygenase-2 inhibitors. |
AID1542903 | Inhibition of N-terminal GST-tagged recombinant human AKR1C2 expressed in Escherichia coli BL21 (DE) Codon Plus RP cells assessed as reduction in NADPH production | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1852380 | Antiinflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as decrease in IL-6 protein level at 10 uM by Western blot analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID128868 | Percentage acute toxicity after 12 mg/kg administered intraperitoneally to rats | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID46859 | In vitro activity at a concentration of 10 uM against Prostaglandin G/H synthase 2 | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22 | Synthesis and pharmacological evaluation of some 8-cyanopyrido[3', 2':4,5]thieno[3,2-d]triazine derivatives as inhibitors of nitric oxide and eicosanoid biosynthesis. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID313771 | Inhibition of ovine COX1 at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | 1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities. |
AID1220797 | Volume of distribution at steady state in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID185528 | Antiinflammatory activity in rats, activity expressed as minimum ulcerogenic dose(MUD) for a period of 24 hr. | 1983 | Journal of medicinal chemistry, Oct, Volume: 26, Issue:10 | Substituted (2-phenoxyphenyl)acetic acids with antiinflammatory activity. 2. |
AID1063323 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 6 hrs by ELISA (Rvb = 5.9 +/- 0.5 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID482170 | Thermodynamic solubility in sodium phosphate buffer of pH 7.4 by UV-reverse phase HPLC analysis | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | 1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A(2)alpha with reduced lipophilicity: synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activity. |
AID404573 | Analgesic activity in Albino mouse at 50 mg/kg, po assessed as thermal stimuli reaction time change after 1 hr by hot plate method relative to basal level | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID1662949 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 4 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID1123740 | Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced paw edema preincubated for 1 hr followed by carrageenan challenge relative to control | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids. |
AID763778 | Antinociceptive activity in Swiss albino mouse assessed as inhibition of formalin-induced flinching at 5 mg/kg administered 30 mins prior to test measured up to 5 mins relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: synthesis and neuropharmacology. |
AID701952 | Inhibition of human MRP1 in human T98G cells assessed as potentiation of doxorubicin induced cytotoxicity at 50 uM pre-incubated for 2 hrs before doxorubicin addition and measured 4 days after doxorubicin exposure by MTT assay relative to untreated contro | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity. |
AID241074 | Inhibition of mouse Prostanoid DP receptor | 2004 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17 | Discovery of new chemical leads for prostaglandin D2 receptor antagonists. |
AID1149805 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced edema measured as increase in foot volume at 5 mg/kg, po administered 1 hr prior challenge measured 7 hrs after carrageenin injection (Rvb = 178.8 %) | 1977 | Journal of medicinal chemistry, Oct, Volume: 20, Issue:10 | Nonsteroidal antiinflammatory agents. 2. Synthesis and biological activity of 2-chloroindolecarboxylic acids. |
AID1557572 | Inhibition of iNOS in LPS-stimulated mouse RAW 264.7 cells preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by fluorescence based assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. |
AID1650563 | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID464501 | Half life in mouse plasma by UPLC-MS analysis | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID428414 | Inhibition of MRP1/MRP2 in White Wistar rat ileum assessed as permeability at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID645028 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 4 hrs by plethysmometer relative to control | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents. |
AID1062929 | Gastrointestinal toxicity in albino rat carrageenan-induced paw edema model assessed as apoptotic glandular epithelial cells at 0.28 mmol/kg, po by hematoxylin and eosin staining-based light microscopic analysis | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID1854714 | Antiinflammatory activity in LPS-stimulated mouse BV-2 cells assessed as inhibition of IL-1beta release at 10 uM and measured after 8 hrs by ELISA | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment. |
AID1721655 | Antiinflammatory activity in mouse assessed as reduction in xylene-induced ear edema at 100 mg/kg, ip administered after prior to xylene stimulation and measured after 1 hr relative to control | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs. |
AID464498 | Inhibition of tubulin polymerization at 10 uM by fluorescence method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID160906 | Inhibition of prostaglandin synthetase in rat renal medulla | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Romazarit: a potential disease-modifying antirheumatic drug. |
AID171178 | Body weight change after once daily administration at 84 uM/kg for 4 days in rats was determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
AID486708 | Gastrointestinal toxicity in Sprague-Dawley rat assessed as lengths of longest diameters of lesions at 20 mg/kg, po after 6 hrs | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents. |
AID580342 | Inhibition of COX1 | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents. |
AID379635 | Inhibition of COX1 in ram seminal vesicle microsomes assessed as reduction of PGE2 formation at 5 uM | 2000 | Journal of natural products, Mar, Volume: 63, Issue:3 | Two new prenylated 3-benzoxepin derivatives as cyclooxygenase inhibitors from Perilla frutescens var. acuta. |
AID224064 | Antiinflammatory activity against D-adjuvant arthritis in uninjected rat paw at the dose of 1.0 mg/kg by oral administration | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2 | Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents. |
AID1251038 | Inhibition of COX1 (unknown origin) assessed as PGH2 production at 100 uM by measuring PGH2alpha level by enzyme immunoassay | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis. |
AID426393 | Cytotoxicity against of human polymorphonuclear leukocytes assessed as cell viability by trypan blue dye exclusion assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors. |
AID477759 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 60 mins before carrageenan challenge measured after 360 mins | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents. |
AID1220240 | Unbound fraction during CYP4500-mediated metabolism in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID197726 | Lysozyme-conjugated prodrugs: in vitro stability in lysosomal lysate at pH 5 | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Low molecular weight proteins as carriers for renal drug targeting. Preparation of drug-protein conjugates and drug-spacer derivatives and their catabolism in renal cortex homogenates and lysosomal lysates. |
AID442513 | Antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/Kg, ip administered simultaneously with carrageenan measured after 3.5 hrs relative to control | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Syntheses and evaluation of the antioxidant activity of acitretin analogs with amide bond(s) in the polyene spacer. |
AID284322 | Inhibition of ovine COX1 at 100 uM | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
AID1662952 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 50 mg/kg, po treated for 2 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID1351163 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by ELISA (Rvb = 407.6 +/- 16.7 pg/m | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | 4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection. |
AID440890 | Toxicity in Fisher 344 rat assessed as gastrointestinal ulcer at 0.01 mmol/kg, ip administered daily once for 4 days measured after 24 hrs final post dose | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins. |
AID1601225 | Antiinflammatory activity in CD1 mouse model of TPA-induced ear edema assessed as inhibition of ear edema at 1 mg/ear administered topically after TPA challenge for 30 mins and measured after 6 hrs post administration relative to control | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID1133358 | Analgesic activity in po dosed CF-1 mouse assessed as reduction in phenylquinone-induced writhing responses administered 15 mins prior to phenylquinone challenge | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Analgesic activity of novel spiro heterocycles. 2-Amino-7-oxa-3-thia-1-azaspiro[5,5]undec-1-enes and related compounds. |
AID1131129 | Antiinflammatory activity against adjuvant-induced arthritis rat model assessed as inhibition of swelling at 1 mg/kg, po measured on day 21 (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Potential antiarthritic agents. 2. Benzoylacetonitriles and beta-aminocinnamonitriles. |
AID611093 | Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID464499 | Inhibition of ovine COX1 | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID182303 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 24 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID618607 | Analgesic activity in mouse assessed as inhibition of acetic acid-induced writhing administered 30 mins before acetic acid challenge measured after 30 mins relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, pharmacological evaluation and docking studies of coumarin derivatives. |
AID1241834 | Anti-inflammatory activity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as inhibition of right hind paw swelling at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 3 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID757491 | Inhibition of ovine COX2 | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity. |
AID404569 | Antiinflammatory activity in Albino mouse assessed as inhibition of carrageenan-induced edema at 50 mg/kg, po after 5 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Synthesis and analgesic/anti-inflammatory evaluation of fused heterocyclic ring systems incorporating phenylsulfonyl moiety. |
AID136446 | Compound was evaluated for the percent reduction of carrageenan induced edema in mice at dose of 0.3 mg/kg | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID1689634 | Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID413192 | Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 10 uM by cell-intact assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. |
AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
AID186454 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 1 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1662950 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 5 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID186599 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 1 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID19006 | Calculated membrane partition coefficient (Kmemb) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability. |
AID266771 | Permeability in human skin | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability. |
AID759376 | Antiinflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured at 4 hrs by plethysmometeric analysis relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents. |
AID287342 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 10 mg/kg, po after 180 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID177152 | In vivo effective concentration of compound in rat paw edema | 1999 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15 | SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. |
AID667604 | Antiinflammatory activity in Wistar albino rat assessed as reduction of carrageenan-induced paw edema at 20 mg/kg, po measured after 30 mins by plethysmometer | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Regioselective reaction: synthesis, characterization and pharmacological activity of some new Mannich and Schiff bases containing sydnone. |
AID166601 | In vitro percent inhibition of platelet aggregation in citreated rabbit platelet-rich plasma induced by arachidonic acid at 200 uM | 2002 | Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1 | Design, synthesis and pharmacological evaluation of novel pyrazolo[3,4-b]thieno[2,3-d]pyridine acid derivatives: a new class of anti-inflammatory and anti-platelet agents. |
AID180546 | The compound was tested in vivo for activity against adjuvant-induced arthritis in rat after peroral administration | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID172361 | Gain in the body weight of rat was measured at 2.8 micro mol/kg/day. (+ means significant body weight) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID722041 | Cytotoxicity against human MIAPaCa2 cells | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Organosilicon molecules with medicinal applications. |
AID1174279 | Antiinflammatory activity in Sprague-Dawley rat model of LPS-induced sepsis assessed as ALT level at 5 mg/kg/day dosed through gastric intubation for 6 days (Rvb = 70.3 +/- 7.9 U/L) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents. |
AID351267 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 3 hrs of induction of inflammation relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones. |
AID1846817 | Anti-inflammatory activity against LPS induced mouse RAW264.7 cells assessed as suppression of TNFalpha cytokine level at 20 uM incubated for 24 hrs by ELISA assay relative to control | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Contemporary advances of cyclic molecules proposed for inflammation. |
AID1497263 | Hemolytic activity in human RBC assessed as membrane mortification by measuring cell wall stabilization by absorbance method relative to control | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective. |
AID1055836 | Antiinflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 0.05 mmol/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs by plethysmometric analysis relative to control | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID237474 | Percentage of drug bound in bovine plasma albumin | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction. |
AID271284 | Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. |
AID338667 | Antiinflammatory activity in Wistar rat peritoneal mast cells assessed as inhibition of concanavalin A-induced histamine release treated 10 mins before concanavalin A challenge measured after 30 mins | |||
AID54540 | In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells | 1999 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 9, Issue:22 | A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors. |
AID185416 | Percent inhibition was measured on untreated rat paw at different dosage forms | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8 | 3-(5-Alkyl-4-hydroxy-3-methoxy-1-naphthalenyl)-2-methyl-2-propenoic acids as orally active inhibitors of IL-1 generation. |
AID492328 | Inhibition of BCRP expressed in human EPG-257RNOV cells at 1 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Novel structure-activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators. |
AID492302 | Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid-induced abdominal constrictions at 100 umol/kg, po administered 40 mins before acetic acid challenge measured for 25 mins relative to control | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates. |
AID591428 | Inhibition of iNOS in LPS-stimulated mouse RAW 264.7 cells after 2 hrs by fluorescence plate reader analysis | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Synthesis and biological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of inflammatory diseases. |
AID1293522 | Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, ip administered 0.5 hrs before xylene challenge measured after 30 mins relative to vehicle treated control | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Synthesis and anti-inflammatory activity evaluation of a novel series of 6-phenoxy-[1,2,4]triazolo[3,4-a]phthalazine-3-carboxamide derivatives. |
AID1156831 | Antiinflammatory activity against albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to indomethacin | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies. |
AID289271 | Inhibition of carrageenan-induced paw edema in Fisher 344 rat at 0.01 mol/kg, ip relative to control | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents. |
AID117726 | Percent uM/cm**2 | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins. |
AID1667509 | Ulcerogenic activity in albino rat assessed as damage of scarred mucosal epithelium at 10 to 50 mg/kg, po measured after 6 hrs by H and E staining based light microscopic assay | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1601229 | Antiinflammatory activity in mouse J774A.1 cells LPS-induced NO production at 25 ug/ml incubated for 2 hrs followed by LPS-stimulation measured after 24 hrs by Griess assay relative to control | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Synthesis and highly potent anti-inflammatory activity of licofelone- and ketorolac-based 1-arylpyrrolizin-3-ones. |
AID707116 | Gastrointestinal toxicity in Swiss mouse assessed as increase in stomach MPO activity at at 2.5 mg/kg, po for 7 days measured over 7 days relative to vehicle-treated control | 2012 | Journal of natural products, May-25, Volume: 75, Issue:5 | Kaurenoic acid from Sphagneticola trilobata Inhibits Inflammatory Pain: effect on cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. |
AID188071 | Compound was evaluated in the developed adjuvant arthritis assay at a dose of 1 mg/kg for the percent reduction of carrageenan induced edema (LHF) on 22nd day | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID93812 | Compound was evaluated for the inhibition of IL-1 beta converting enzyme biosynthesis. | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis. |
AID161674 | Tested for inhibition against Prostaglandin G/H synthase 1 | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors. |
AID1501859 | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach. |
AID653310 | Antiinflammatory activity in transgenic zebrafish larvae harboring Fli-1 gene assessed as LPS-stimulated leukocyte migration to injury zone of tail transected larvae at 1 uM after 20 to 22 hrs by microscopy | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID289291 | Antiinflammatory activity against carrageenan-induced hind paw oedema in Swiss Albino mouse assessed as swelling thickeness at 100 mg/kg, po after 90 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID1423032 | Inhibition of COX1 in human platelet microsomes assessed as reduction in formation of oxidized TMPD using arachidonic acid as substrate preincubated for 3 to 5 mins followed by arachidonic acid addition measured for 25 secs by spectrophotometric assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides. |
AID1242112 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs by plethysmometric analysis relative to control | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Molecular docking design and one-pot expeditious synthesis of novel 2,5-diarylpyrazolo[1,5-a]pyrimidin-7-amines as anti-inflammatory agents. |
AID365465 | Inhibition of P-gp in human A2780 cells | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins. |
AID1453453 | Anti-inflammatory activity in po dosed rat assessed as reduction in carrageenan-induced paw edema measured after 5 hrs by plethysmographic method | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Synthesis of methanesulphonamido-benzimidazole derivatives as gastro-sparing antiinflammatory agents with antioxidant effect. |
AID418086 | Toxicity in carrageenan treated Albino mouse stomach assessed as gastric ulcer at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs by hematoxilen eosine staining | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent. |
AID497222 | Toxicity in Wistar albino rat assessed as ulcerogenic activity at 300 mg/kg, po qd for 3 days | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Synthesis and biological evaluation of novel pyrazole compounds. |
AID753746 | Gastrointestinal toxicity in albino rat assessed as acute inflammatory cell infiltrating its whole thickness and apparently destroying epithelial lining of gastric pits at 0.28 mmol/kg, po using haematoxylin and eosin staining by light microscopic analysi | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID1199429 | Inhibition of carrageenan-induced TNFalpha expression in paw tissue (unknown origin) by immunohistochemistry | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID1195146 | Analgesic activity in Swiss albino mouse assessed as latancy of withdrawing tail at 50 mg/kg, po measured after 2 hrs by tail flick test relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID1700185 | Anti-inflammatory activity against dimethylbenzene-induced ear edema mouse model assessed as inhibition of ear edema at 10 mg/kg, ip measured after 60 mins relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel piperazine-2,5-dione analogs bearing 1H-indole: Synthesis and biological effects. |
AID1689624 | Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced paw edema at 0.028 mM/kg, po measured after 1 hr by plethysmometer analysis (Rvb = 2.08 +/- 0.16 mm) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID160400 | In vitro percent inhibition of prostaglandin G/H synthase 2 (COX-2) in human whole blood at 1 uM | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID93591 | In vitro methemoglobin Induction at 10e-4 M in lysed human red blood cells; Not tested | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes. |
AID1815249 | Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID1852442 | Toxicity in Wistar rat assessed as change in ALT level in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID645030 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 24 hrs by plethysmometer relative to control | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents. |
AID295677 | Antinociceptive activity in sc dosed Sprague-Dawley rat assessed as increase in latency time after 2 hrs by hot plate method | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Evaluation of the anti-inflammatory and anti-nociceptive activities of novel synthesized melatonin analogues. |
AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID173577 | Dose required to prevent lesion formation in gastric mucosa of unanesthetized rats upon subcutaneous administration. | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | Novel angucycline compound with both antigastrin- and gastric mucosal protective-activities. |
AID1336927 | Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID587448 | Inhibition of ovine COX-1 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies. |
AID592745 | Antiamyloidogenic activity in mouse N2A cells transfected with human APP Swedish mutant assessed as reduction of amyloid beta (1 to 42) level at 1 uM after 24 hrs by ELISA relative to control | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates. |
AID454686 | Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw edema at 10 umol/kg, ip | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole. |
AID1436693 | Selectivity index, ratio of IC50 for COX1 (unknown origin) to IC50 for COX2 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID442515 | Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation at 50 uM | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase. |
AID1852432 | Antiinflammatory activity in LPS/talc powder induced pericarditic Wistar rat assessed as increase in cTNI level in serum at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-oxo-5-((5-sul | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID666603 | Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay in the presence of LPS | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. |
AID1180075 | Inhibition of human recombinant COX2 using arachidonic acid substrate assessed as PGE2 production ELISA method after 2 mins | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Pharmacological evaluation and docking studies of α,β-unsaturated carbonyl based synthetic compounds as inhibitors of secretory phospholipase A₂, cyclooxygenases, lipoxygenase and proinflammatory cytokines. |
AID618606 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins before carrageenan challenge measured after 4 hrs by plethysmograph | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, pharmacological evaluation and docking studies of coumarin derivatives. |
AID464519 | Half life in stimulated gastric fluid of pH 1.0 | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID284326 | Effect on gastric damage in rat assessed as induction of gastric ulcer at 10 mg/kg, po after 5 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
AID1237267 | Inhibition of COX1 (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Synthesis and characterization of novel oxazines and demonstration that they specifically target cyclooxygenase 2. |
AID1667510 | Ulcerogenic activity in albino rat assessed as ulcer formation with distorted gastric gland at 10 to 50 mg/kg, po measured after 6 hrs by H and E staining based light microscopic assay | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID414507 | Antiinflammatory activity against carrageenan-induced inflammation in Albino mouse air ppouch model assessed as number of polymorphonuclear leukocytes infiltration at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs by air | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent. |
AID693571 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan-challenge after 1 hr relative to vehicle-treated control | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives. |
AID1357041 | Selectivity index, ratio of IC50 for inhibition of ovine COX1 to IC50 for human COX2 | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice. |
AID688458 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.4 umol administered topically per cm'2 of ear measured 48 hrs after induction of dermatitis relative to untreated control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1434439 | Inhibition of ovine COX1 at 100 uM using arachidonic acid as substrate after 2 mins by fluorometric substrate-based fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Chemical synthesis and biological evaluation of ω-hydroxy polyunsaturated fatty acids. |
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AID1557573 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent-based assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model. |
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AID189416 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 8 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
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AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID303570 | Analgesic activity in Swiss Albino mouse assessed as number of acetic acid-induced writhing at 100 mg/kg, po after 1 hr relative to control | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1852391 | Protection against LPS/hypoxia induced cell injury in rat H9c2 cells assessed as recovery of cell viability in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by CCK-8 assay (Rvb = 69.0%) | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
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AID1815251 | Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero E6 cells to EC50 for antiviral activity against SARS-COV2/NL/2020 infected in African green monkey Vero E6 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
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AID432725 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered before 60 mins of carrageenan-challenge measured after 270 mins | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives. |
AID1591460 | Anti-inflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 30 mg/kg, ip dosed prior to xylene challenge and measured 1 hr post xylene injection relative to control | 2019 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 29, Issue:15 | Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities. |
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AID1700184 | Anti-inflammatory activity against dimethylbenzene-induced ear edema mouse model assessed as inhibition of ear edema at 10 mg/kg, ip measured after 60 mins (Rvb = 6.93 +/- 1.05 mg) | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel piperazine-2,5-dione analogs bearing 1H-indole: Synthesis and biological effects. |
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AID386957 | Antiinflammatory activity against carrageenan-induced paw edema in Wister albino rat at 10 mg/kg, ip administered 1 hr before inflammation induction assessed after 2 hrs | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Facile synthesis of dithiatetraaza-macrocycles of potential anti-inflammatory activity. |
AID681340 | TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes | 1999 | Molecular pharmacology, May, Volume: 55, Issue:5 | Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. |
AID1199378 | Antiinflammatory activity in male Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured at 3 hrs of carrageenan treatment | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres. |
AID693574 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan-challenge after 4 hrs relative to vehicle-treated control | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis pharmacological evaluation and docking studies of pyrimidine derivatives. |
AID313772 | Inhibition of ovine COX2 | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | 1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities. |
AID680594 | TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation by indomethacin at a concentration of 200uM in MRP3-expressing MDCK cells | |||
AID537736 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
AID177103 | ED50 was measured by hyperalgesia assay method. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID132689 | Inhibitory activity against PG synthesis was measured in mouse brain microsomes. | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
AID1667495 | Anti-inflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 uM/kg, ip measured at 1 hr by calliper method relative to control | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID469573 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema measured after 1 hr at 6 mg/kg, po administered 1 hr before carrageenan challenge | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs. |
AID640716 | Antiphlogistic activity in Wistar rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation. |
AID552765 | Antiinflammatory activity against histamine-induced mouse edema model assessed as edema size 20 mg/kg, po (untreated control = 100%) | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Rapid access to new bioconjugates of betulonic acid via click chemistry. |
AID1662951 | Antiinflammatory activity in para-xylene-induced mouse model of ear swelling assessed as inhibition in swelling rate at 100 mg/kg, po treated for 24 hrs followed by xylene addition relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents. |
AID351268 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 4 hrs of induction of inflammation relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones. |
AID1392318 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, po measured at 2 hrs relative to control | |||
AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1542241 | Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
AID356718 | Antiinflammatory activity against TPA-induced ear edema in mouse assessed inhibition of edema at 1 mg/ear | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Antiinflammatory constituents from Heterotheca inuloides. |
AID464323 | Antitrypanosomal activity against Trypanosoma brucei brucei after 48 hrs by luminescence assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID1815250 | Antiviral activity against SARS-CoV-2/NL/2020 infected in African green monkey Vero E6 cells assessed as inhibition of plaque formation measured after 3 days by Plaque reduction assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID179010 | Compound was evaluated for percentage recovery from femur weight in adjuvant-induced arthritic model of rat at a dose of 2 mg/kg | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Synthesis and bioactivities of novel bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. |
AID611828 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured after 180 min by Plethysmograph | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents. |
AID1241878 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for ovine COX2 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1576306 | Antiinflammatory activity against carrageenan-induced air pouch inflammatory Swiss mouse model assessed as number of polymorphonuclear leucocytes in air pouch at 10 mg/kg, po treated for 1 hr prior to carrageenan administration and measured after 6 hrs (R | 2019 | MedChemComm, Nov-01, Volume: 10, Issue:11 | Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives. |
AID1852349 | Protection against LPS/hypoxia induced apoptosis in rat H9c2 cells assessed as reduction in necrotic cells at 10 umol/L incubated for 4 hrs under hypoxia condition in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-tri | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID364551 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip after 4 hrs | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives. |
AID604744 | Displacement of radiolabeled dansylsarcosine from fatty acid containing human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
AID653322 | Inhibition of MPO activity in TPA-induced Swiss mouse ear tissue homogenates after 3 mins relative to control | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID75982 | Inhibition of CCl4 induced lipid peroxidation (LPO) of guinea pig hepatic microsomes at 300 uM concentration; NT=Not tested | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid. |
AID161659 | Inhibitory activity against recombinant human prostaglandin G/H synthase 1 | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. |
AID185328 | Lesion frequency measured in rats | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID1233393 | Gastroprotective activity in Swiss albino mouse model of HCl/EtOH-induced lesion assessed as gastric lesion index at 10 mg/kg, po dosed 50 mins before HCl/EtOH challenge and measured 1 hr post HCl/EtOH challenge (Rvb = 42 +/- 1.9 mm) | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14 | Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls. |
AID1315276 | Antineuroinflammatory activity in human BV2 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 10 mins followed by LPS stimulation for 24 hrs by Griess assay | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Nitric Oxide Inhibitory Meroterpenoids from the Fungus Penicillium purpurogenum MHZ 111. |
AID1689625 | Antiinflammatory activity in Wistar albino rat assessed as protection against carrageenan-induced paw edema at 0.028 mM/kg, po measured after 1 hr by plethysmometer analysis relative to control (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID190154 | Median ulcerogenic dose was determined at 30 mg/kg dose | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1336928 | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition at 100 uM after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1220558 | Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1220800 | Drug metabolism in bile duct-cannulated monkey assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID604022 | Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
AID197600 | Lysozyme-conjugated prodrugs: in vitro stability in rat cortical homogenate at pH 5 | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Low molecular weight proteins as carriers for renal drug targeting. Preparation of drug-protein conjugates and drug-spacer derivatives and their catabolism in renal cortex homogenates and lysosomal lysates. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID172570 | Antiinflammatory activity was evaluated by carrageenan induced rat paw edema volume was determined. | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8 | N-substituted oxazolo[5,4-b]pyridin-2(1H)-ones: a new class of non-opiate antinociceptive agents. |
AID461316 | Inhibition of human recombinant MGL at 100 uM | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors. |
AID664540 | Inhibition of human recombinant GST-tagged AKR1C1 expressed in Escherichia coli using S-tetralol as substrate by fluorometry | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4 | Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. |
AID183012 | Analgesic activity was determined using acetic acid writing test at a dose of 5 mg/kg perorally in rats. (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID1060438 | Cytotoxicity against human KB-3-1 cells assessed as cell survival after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Synthesis of novel 2-cyano substituted glycyrrhetinic acid derivatives as inhibitors of cancer cells growth and NO production in LPS-activated J-774 cells. |
AID681104 | TP_TRANSPORTER: inhibition of Glutathione efflux (Indomethacin: 400 uM) in MRP1-expressing MDCKII cells | 2000 | British journal of cancer, Aug, Volume: 83, Issue:3 | Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. |
AID160431 | Percentage of inhibition of Prostaglandin G/H synthase 2 activity in human whole blood(HWB) at 1 uM | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines. |
AID174428 | Plasma drug level was measured in rat yeast induced hyperalgesia assay in presence of indomethacin at a dose of 10 mg/kg for 12 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID687242 | Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 40 mg/kg, po administered 1 hr prior to carrageenan challenge measured 4 hrs post carrageenan challenge relative to control | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents. |
AID729258 | Inhibition of human recombinant AKR1C3-mediated NADP+-dependent oxidation of S-(+)-1,2,3,4-tetrahydro-1-naphthol | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID611094 | Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1311791 | Inhibition of NFkappaB signaling pathway in LPS-stimulated mouse RAW264.7 cells assessed as protein levels by ELISA (Rvb = 1.23 +/- 0.06 pg/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID1177996 | Binding affinity to COX-2 (unknown origin) by ESI mass spectrometry | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug. |
AID303568 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, after 6 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID1543421 | Antiinflammatory activity in TPA-induced ICR mouse ear edema model assessed as reduction in number of neutrophils at 1 mg/ear applied topically measured 4 hrs post-TPA challenge by giemsa staining-based microscopic method | |||
AID287292 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 100 mg/kg, po after 90 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1220786 | Fraction unbound in monkey plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
AID194775 | Percentage inhibition of the prostaglandin synthesis was measured in rats. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. |
AID1136459 | Antiinflammatory activity in CF1 mouse assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, ip administered 3 hrs and 30 mins prior to carrageenan-challenge measured after 3 hrs (Rvb = 0%) | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids. |
AID1532672 | Inhibition of ovine COX2 by colorimetric assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Anti-inflammatory activity of triazine derivatives: A systematic review. |
AID92236 | Inhibition of adenosine diphosphate (ADP) induced human platelet aggregation | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Synthetic aci-reductones: 3,4-dihydroxy-2H-1-benzopyran-2-ones and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers. Antiaggregatory, antilipidemic, and redox properties compared to those of the 4-substituted 2-hydroxytetronic acids. |
AID681108 | TP_TRANSPORTER: inhibition of E217betaG in the presence of Indomethacin at a concentration of 50uM in membrane vesicles from MRP1-expressing Sf9 cells | 2003 | Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 100, Issue:16 | The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. |
AID287344 | Inhibition of carrageenan-induced paw edema in Swiss albino mouse at 10 mg/kg, po after 360 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
AID1456098 | Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK-8 assay | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and biological evaluation of novel podophyllotoxin-NSAIDs conjugates as multifunctional anti-MDR agents against resistant human hepatocellular carcinoma Bel-7402/5-FU cells. |
AID688469 | Antiinflammatory effect in CD1 mouse ear dermatitis model assessed as reduction in mast cell degranulation at 0.4 umol administered topically per cm'2 of ear measured after 6 hrs post dermatitis induction relative to control | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID345950 | Inhibition of zymosan-induced peritonitis inflammation in BALB/c mouse assessed as blocking of neutrophil influx at 10 umol/kg, sc administered 30 mins after zymosan challenge measured after 2 hrs | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
AID192519 | Percent inhibition of carrageenan induced rat paw edema 3 hr after a peroral administration of 50 mg/kg | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | Nonsteroidal antiinflammatory agents. 3. Synthesis of the positional isomers of 4'-chloro-5-methoxy-3-biphenylylacetic acid and their antiinflammatory and analgesic activities. |
AID233634 | Ratio of inhibitory concentration of COX-1 and COX-2 measured for their oral activity in an acute inflammation model | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9 | Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. |
AID595393 | Inhibition of ram seminal vesicle COX-1 assessed as PGE2 production from arachidonic acid after 20 mins enzyme immunoassay | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. |
AID1128738 | In vivo antidyslipidemic activity against Triton WR 1339-induced hyperlipidemic Wistar rat model assessed as decrease in LDL-cholesterol level in plasma at 56 umol/kg, ip administered as single dose 1 hr after Triton WR 1339 challenge measured after 24 hr | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1550472 | Selectivity index, ratio of IC50 for human COX1 to IC50 for human COX2 | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID162306 | In vitro inhibition of Prostaglandin G/H synthase 1 (from ram seminal vesicles) at a concentration of 10 M | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
AID162662 | Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models. |
AID1663403 | Anti-inflammatory activity against croton oil-induced ear edema in Swiss mouse model assessed as inhibition of myeloperoxidase activity at 1 mg/ear administered topically immediately after croton oil-stimulation and measured after 6 hrs by microplate spec | 2020 | Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12 | Synthesis of novel 3,5,6-trisubstituted 2-pyridone derivatives and evaluation for their anti-inflammatory activity. |
AID1542911 | Antiproliferative activity against human LNCAP cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID232419 | Ratio of inhibition of COX-1 to COX-2 | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase. |
AID664542 | Inhibition of human recombinant AKR1C3 expressed in Escherichia coli JM109 cells using S-tetralol as substrate by fluorometry | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4 | Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. |
AID1663612 | Anticancer activity against human PC3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis and anticancer activity of open-resorcinarene conjugates. |
AID745272 | Selectivity ratio for COX1 (unknown origin) over COX2 (unknown origin) | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents. |
AID1667497 | Anti-inflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 28 uM/kg, ip measured at 3 hrs by calliper method relative to control | 2020 | Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7 | Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. |
AID1663466 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production measured after 18 hrs by Griess assay | |||
AID1199384 | Analgesic activity in Swiss albino mouse assessed as maximal possible effect on nociception measured as time of licking forepaws or jump response at 10 mg/kg, po after 3 hrs of treatment by Eddys hot plate method | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres. |
AID186468 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema at dose of 1 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID135276 | Neurotoxic dose that causes minimal recognizable neurotoxicity in 50% of animals tested | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles. |
AID277214 | Reduction of edema formation in rat reverse passive arthus model at 3 mg/kg, po | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity. |
AID397231 | Inhibition of ovine COX2 by enzyme immunoassay | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and biological evaluation of 4,5-diphenyloxazolone derivatives on route towards selective COX-2 inhibitors. |
AID1852366 | Anti-inflammatory activity in LPS/hypoxia induced rat H9c2 cells assessed as reduction of TNF-alpha protein expression at 10 uM in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid by Western blo | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID675140 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 10 mg/kg, po administered 60 mins before carrageenan challenge measured after 1 hr (Rvb = 59.2 +/- 6.4 mL) | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
AID679529 | TP_TRANSPORTER: inhibition of PAH uptake (Indomethacin: 200 uM) in OAT1-expressing HeLa cells | 1999 | The American journal of physiology, 02, Volume: 276, Issue:2 | Cloning of the human kidney PAH transporter: narrow substrate specificity and regulation by protein kinase C. |
AID1134899 | Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma after 5 mins | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID1311792 | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as COX2 levels by ELISA (Rvb = 159.64 +/- 13.56 pg/mL) | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Anti-inflammatory polyphenol constituents derived from Cissus pteroclada Hayata. |
AID182289 | Percent inhibition of edema in carrageenan-induced rat paw edema was determined by comparing with vehicle control group when tested on 5 rats at peroral dose of 100 umol/Kg | 1998 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2 | Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole. |
AID681379 | TP_TRANSPORTER: inhibition of EGCG in MRP1-expressing MDCKII cells | 2003 | Biochemical and biophysical research communications, Oct-10, Volume: 310, Issue:1 | Involvement of multidrug resistance-associated proteins in regulating cellular levels of (-)-epigallocatechin-3-gallate and its methyl metabolites. |
AID1136206 | Analgesic activity in po dosed rat assessed as inhibition of adjuvant-induced arthritis pain | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Novel analgesic-antiinflammatory salicylates. |
AID234761 | Ratio of inhibitory activity against COX-1 and COX-2 | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors. |
AID186456 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 1 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID1576181 | Nephrotoxicity in rat assessed as effect on glomeruli at 50 mg/kg surrounded by Bowmann's capsule by hematoxylin and eosin staining based assay | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID1153376 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.03 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13 | Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties. |
AID1473959 | Ratio of drug concentration at steady state in human at 25 to 50 mg, po TID after 8 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1286239 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay | 2016 | Journal of natural products, Jan-22, Volume: 79, Issue:1 | Diterpenoids from the Roots of Euphorbia fischeriana with Inhibitory Effects on Nitric Oxide Production. |
AID1316776 | Analgesic activity in rat assessed as reversal of complete Freund's adjuvant-induced mechanical hyperalgesia at 30 mg/kg, po after 1 hr relative to control | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. |
AID1195044 | Antiinflammatory activity in CD-1 mouse ear edema model assessed as reduction in TPA-induced edema size at 8 mg/kg, po administered 30 mins prior to TPA-challenge for every 48 hrs for 10 days relative to vehicle treated control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis, antinociceptive and anti-inflammatory effects of porphyrins. |
AID1330198 | Antiinflammatory activity in mouse assessed as inhibition of xylene-induced ear edema at 100 mg/kg, ip administered 30 mins before xylene challenge measured after 30 mins relative to DMSO-control | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24 | Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties. |
AID591630 | Partition coefficient, log P of the compound in n-octanol-phosphate buffer at pH 7.4 by HPLC analysis | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID1815261 | Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in virus induced cytopathic effect measured after 4 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Indomethacin-based PROTACs as pan-coronavirus antiviral agents. |
AID469577 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema measured after 3 hrs at 6 mg/kg, po administered 1 hr before carrageenan challenge | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs. |
AID1473956 | Cmax in human at 25 to 50 mg, po TID after 8 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID401493 | Inhibition of PMA-induced ear edema in Swiss mouse at 3 mg/ear after 3 hrs | 1997 | Journal of natural products, Feb, Volume: 60, Issue:2 | Isolation of two flavonoids from Tanacetum microphyllum as PMA-induced ear edema inhibitors. |
AID452090 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, po treated 60 mins before carrageenan challenge measured after 180 mins | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | A new therapeutic approach in Parkinson's disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents. |
AID683093 | Inhibition of human recombinant COX2 assessed as inhibition of PGF2alpha production from PGH2 by enzyme immunoassay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity. |
AID1543429 | Antiinflammatory activity in TPA-induced ICR mouse ear edema model assessed as reduction in monocytes content AUC at 1 mg/ear applied topically measured 4 hrs post TPA-challenge giemsa staining-based microscopic method | |||
AID162495 | In vitro inhibitory activity against human whole cells (CHO) Prostaglandin G/H synthase 2 | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor. |
AID1192207 | Antiinflammatory activity against carrageenan-induced paw edema male Wistar albino rat assessed as edema volume at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured after 2 hrs (Rvb = 1.21 +/- 0.16 mL) | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents. |
AID644806 | Ulcerogenicity in Wistar rat assessed as lesion score at 100 mg/kg, po after 6 hrs | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis, evaluation and docking studies on 3-alkoxy-4-methanesulfonamido acetophenone derivatives as non ulcerogenic anti-inflammatory agents. |
AID170866 | Percent changes of hind paw edema and severity scores compared to control animals at 2.8 micro mol/kg/day | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides). |
AID1128733 | Inhibition of human recombinant COX-2 assessed as PGF2-alpha formation using arachidonic acid as substrate at 20 uM by enzyme immunoassay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity. |
AID1551028 | Ulcerogenicity in albino rat assessed as average severity score at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose (Rvb = 0 No_unit) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors. |
AID287291 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 100 mg/kg, po after 360 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID591627 | Gastrointestinal toxicity in Wistar rat assessed as appearance ulcer area of >3 mm diameter at 100 mg/kg, po administered as single dose after 6 hrs by Vernier caliper | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Synthesis and biological evaluation of orally active prodrugs of indomethacin. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1689636 | Ulcerogenic activity in albino rat assessed as average number of gastric ulcers at 0.028 mM/kg, po measured after 4 hrs by microscopic analysis (Rvb = 0 No_unit) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors. |
AID336476 | Inhibition of COX2 at 6 uM by scintillation proximity assay | 2002 | Journal of natural products, Nov, Volume: 65, Issue:11 | Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. |
AID1232308 | Distribution coefficient, log D of the compound | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
AID748516 | Selectivity ratio of IC50 for mouse COX2 V349A mutant to IC50 for wild type mouse COX2 | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID300450 | Antiinflammatory activity against carrageenan-induced hind paw oedema in mouse assessed as inhibition of swelling thickness at 10 mg/kg, po after 270 mins | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | 1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities. |
AID160432 | Percentage of inhibition of Prostaglandin G/H synthase 2 activity in human whole blood(HWB) at 10 uM | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines. |
AID634932 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 30 mins prior to challenge measured after 2 hrs relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids. |
AID680190 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, Indomethacin: 500 uM) in Xenopus laevis oocytes | 2000 | The Journal of biological chemistry, Feb-11, Volume: 275, Issue:6 | Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. |
AID160887 | Inhibition of PG synthetase activity obtained from bovine seminal vesicles | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives. |
AID161496 | Inhibition activity against recombinant human Prostaglandin G/H synthase 1 | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5 | Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. |
AID284339 | Antiinflammatory activity assessed as reduction of carrageenan-induced paw volume in Wistar rat at 10 mg/kg, ip after 3 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Antinociceptive and antiinflammatory activities and QSAR studies on 2-substituted-4,5-diphenyl-1H-imidazoles. |
AID1139284 | Antiinflammatory activity in rat paw edema model assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 4 hrs relative to vehicle-treated control | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Suppression of inflammatory responses by handelin, a guaianolide dimer from Chrysanthemum boreale, via downregulation of NF-κB signaling and pro-inflammatory cytokine production. |
AID616386 | Antioxidant activity assessed DPPH scavenging activity at 500 uM | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9 | Anti-inflammatory principles from Cordyceps sinensis. |
AID1164048 | Inhibition of ovine COX1 assessed as reduction in PGF2alpha formation at 10 uM incubated for 18 hrs by enzyme immunoassay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors. |
AID178230 | Inhibition of pleural reverse passive Arthus reactions (RPAR) in rat (exudate volume); No significant inhibition at 56 umol/kg (Inactive) | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | 3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation. |
AID303577 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 4 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID186453 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 1 mg/kg at time interval- 0.5 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID747925 | Inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins prior to arachidonic acid challenge measured after 30 mins by radioimmunoassay relative to vehicle-treated cont | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. |
AID1392320 | Antiinflammatory activity in mouse assessed as inhibition of para-xylene-induced ear edema at 100 mg/kg, po measured at 4 hrs relative to control | |||
AID403351 | Inhibition of COX1 at 0.1 mM | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Expanding the ChemGPS chemical space with natural products. |
AID666604 | Antiinflammatory activity in ICR mouse assessed as decrease in carrageenan-induced paw edema at 10 mg/kg, ip administered 30 mins prior to carrageenan-challenge measured at 4 hrs relative to vehicle treated control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents. |
AID239780 | Percentage plasma protein binding towards human serum albumin | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach. |
AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1125133 | Ulcerogenic effect in albino rat assessed as capillary inflammatory cells using hematoxylin and eosin staining at 0.28 mmol/kg, po by light microscopic analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | 1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity. |
AID456181 | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as reduction of iNOS protein expression at 50 uM after 24 hrs by Western blot analysis relative to control | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Anti-inflammatory diterpenes from the seeds of Vitex negundo. |
AID1220256 | Total clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID781326 | pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID161483 | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 1. | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9 | Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. |
AID295044 | Inhibition of 3alphaHSD | 2007 | Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9 | Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill). |
AID1743645 | Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID1409053 | Antiinflammatory activity in carrageenan-induced Swiss mouse assessed as paw volume at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 3 hrs by plethysmometric method (Rvb = 43.53 +/- 5.06 mL) | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives. |
AID428418 | Inhibition of MRP1/MRP2 in White Wistar rat colon assessed as increase in drug uptake at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID312246 | Increase in body weight in acetic acid-induced chronic gastric ulcer Wistar rat at 2.0 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1 | New celecoxib derivatives as anti-inflammatory agents. |
AID478751 | Antiinflammatory activity against carrageenan-induced paw edema in po dosed rat administered 1 hr before carrageenan challenge assessed after 4 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis of 3-((2,4-dichlorophenoxy)methyl)-1,2,4-triazolo(thiadiazoles and thiadiazines) as anti-inflammatory and molluscicidal agents. |
AID1542916 | Lipophilicity, logD of the compound at pH 7.4 | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID92240 | Inhibition of arachidonic acid (AA) induced serotonin secretion | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | Synthetic aci-reductones: 3,4-dihydroxy-2H-1-benzopyran-2-ones and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers. Antiaggregatory, antilipidemic, and redox properties compared to those of the 4-substituted 2-hydroxytetronic acids. |
AID1764400 | Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID193234 | Compound was evaluated for edema density in adjuvant-induced arthritis model in rats at a dose of 3 mg/kg (Experiment # 1) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID304237 | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production at 0.3 uM relative to control | 2007 | Journal of medicinal chemistry, Dec-13, Volume: 50, Issue:25 | Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. |
AID177762 | Analgesic activity measured as silver nitrate induced arthritic pain in rats | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b, f]oxepinacetic acids and related compounds. |
AID616383 | Anti-inflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced elastase release | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9 | Anti-inflammatory principles from Cordyceps sinensis. |
AID1852406 | Reversal of ATP level in LPS/hypoxia induced rat H9c2 cell in presence of 2-(4-(5-oxo-5-((5-sulfamoyl-1,3,4-thiadiazol-2-yl)amino)pentyl)-1H-1,2,3-triazol-1-yl)acetic acid and Na2WO4 by multimode plate reader analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID456180 | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as reduction of COX2 protein expression at 50 uM after 24 hrs by Western blot analysis relative to control | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Anti-inflammatory diterpenes from the seeds of Vitex negundo. |
AID1551029 | Ulcerogenicity in albino rat assessed as incidence of gastric ulceration at 18 mg/kg, po administrated once daily for 3 successive days and measured after 6 hrs from last dose relative to control | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors. |
AID212000 | Peroral dose causing 50% death of the mice population | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | Synthesis and antiinflammatory, analgesic activity of 3,3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds. Part 10. |
AID263729 | Ratio of drug level in brain against plasma in mice at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent. |
AID1199425 | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 20 uM after 24 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents. |
AID477757 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 60 mins before carrageenan challenge measured after 180 mins | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents. |
AID1195156 | Gastrointestinal toxicity in Swiss albino mouse assessed as ulcer index at 100 mg/kg, po measured after 2 hrs | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID481238 | Toxicity in po dosed BALB/c mouse collagen antibody induced arthritis model assessed as tolerated dose | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III. |
AID1062925 | Gastrointestinal toxicity in albino rat carrageenan-induced paw edema model assessed as capillary vasodilatation of lamina propria associated with accumulation of edema fluid at 0.28 mmol/kg, po by hematoxylin and eosin staining-based light microscopic an | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID430145 | Antiinflammatory activity against bradykinin-induced paw oedema in mouse at 1 mg/kg, ip treated 30 mins before bradykinin challenge measured after 30 mins by plethysmometry analysis | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Evaluation of anti-inflammatory effect of synthetic 1,5-bis(4-acetoxy-3-methoxyphenyl)-1,4-pentadien-3-one, HB2. |
AID1194323 | Induction of SCL expression in human HaCaT cells at 5 uM by qRT-PCR analysis relative to control | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Cell-based biological evaluations of 5-(3-bromo-4-phenethoxybenzylidene)thiazolidine-2,4-dione as promising wound healing agent. |
AID172892 | Percent change in average volume of pleural fluid at a dose of 4.0 mg/kg and 5-h response by Evans blue-carrageenan induced pleural effusion assay. | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues. |
AID1359537 | Anti-inflammatory activity against carrageenan-induced paw oedema in Wistar albino rat assessed as hind paw thickness at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 5 hrs by caliper method (Rvb = 8.37 +/- 0.64 millime | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition. |
AID1062922 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po administered 30 mins prior to carrageenan-challenge measured after 5 hrs relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | 1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities. |
AID177075 | Compound was evaluated for highest non-ulcerogenic dose (less than 50% ulcer incidence) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Bulky amine analogues of ketoprofen: potent antiinflammatory agents. |
AID186439 | Tested for acute anti-inflammatory activity of carrageenan-induced foot edema in rats at dose of 0.1 mg/kg at time interval- 1 hr | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID161656 | Inhibitory activity against Prostaglandin G/H synthase 1 in human whole blood | 1999 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15 | SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. |
AID736892 | Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw volume at 100 mg/kg, po measured after 3 hrs of carrageenan challenge (Rvb = 1.17 +/- 0.1 ml) | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Design, synthesis, characterization and anti-inflammatory evaluation of novel pyrazole amalgamated flavones. |
AID389443 | Antiinflammatory activity against carrageenan-induced paw edema in ICR mouse at 4 mg/kg, ip administered 30 mins before carrageenan challenge assessed after 0.5 hrs | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Anti-inflammatory activities of furanoditerpenoids and other constituents from Fibraurea tinctoria. |
AID604955 | Drug level in C57Bl6 mouse plasma at 10 mg/kg, po after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | 1-(5-Carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α: effect of substituents in position 3 of the indole scaffold on inhibitory potency, metabolic stability, solubility, and bioavailability. |
AID313125 | Inhibition of COX2 | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Structural and functional basis of cyclooxygenase inhibition. |
AID488195 | Inhibition of COX2 in human whole blood | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Synthesis and biological activity of N-aroyl-tetrahydro-gamma-carbolines. |
AID1650581 | Analgesic activity in Wistar rat assessed as reduction in formalin-induced flitching in inflammatory phase at 10 mg/kg, ip incubated for 30 mins followed by formalin addition and observed for 60 mins | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID1663400 | Anti-inflammatory activity against croton oil-induced ear edema in Swiss mouse model assessed as inhibition of ear edema at 1 mg/ear administered topically immediately after croton oil-stimulation and measured after 6 hrs relative to control | 2020 | Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12 | Synthesis of novel 3,5,6-trisubstituted 2-pyridone derivatives and evaluation for their anti-inflammatory activity. |
AID1891737 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID453204 | Permeability in human skin after 48 hrs by Franz cell permeability assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay. |
AID174429 | Plasma drug level was measured in rat yeast induced hyperalgesia assay in presence of indomethacin at a dose of 10 mg/kg for 1 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1542915 | Dissociation constant, pKa of the compound | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID183642 | Antiinflammatory activity was evaluated by the inhibition of rat carrageenan foot edema (CFE) assay at the dose of 1 mg/kg | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. |
AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
AID428413 | Inhibition of MRP1/MRP2 in White Wistar rat jejunum assessed as permeability at 1 mM after 30 mins by HPLC analysis | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps. |
AID1426403 | Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 3 hrs relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID182711 | Compound was tested for the inhibition of rat reversed passive Arthus pleurisy after peroral administration of 10 mg/kg dose at 3.2*10e6 no of cells with 2.77*10e6 cells of control | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | A novel synthesis and potent antiinflammatory activity of 4-hydroxy-2(1H)-oxo-1-phenyl-1,8-naphthyridine-3-carboxamides. |
AID721754 | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
AID1164049 | Inhibition of ovine COX2 assessed as reduction in PGF2alpha formation at 10 uM incubated for 18 hrs by enzyme immunoassay | 2014 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19 | Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors. |
AID1416038 | Binding affinity to calf thymus DNA assessed as hyperchromic shift at 281 nm at 50 uM by UV-visible spectrophotometric method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach. |
AID351266 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw oedema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 2 hrs of induction of inflammation relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones. |
AID536095 | Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 5 mg/kg, ip administered 1 hrs before carrageenan challenge relative to untreated control | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis, antimicrobial and anti-inflammatory activities of novel 5-(1-adamantyl)-1,3,4-thiadiazole derivatives. |
AID6861 | Inhibitory activity against 5-lipoxygenase catalysis (5-LO) in sonicated rat basophilic leukemia cell lysate | 1997 | Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5 | Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. |
AID115727 | The compound was evaluated for inhibition of edema induced by serotonin at 250 micro g/mL | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID1220238 | Intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID1241819 | Anti-inflammatory activity in rat model of acute inflammation assessed as inhibition of carrageenan-induced paw oedema dosed at 10 mg/kg, po dosed 1 hr before carrageenan injection and measured 2 hrs after carrageenan injection | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID604025 | Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID188026 | Pharmacological potency relative to indomethacin for prodrug candidate by adjuvant-induced arthritis assay | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid. |
AID1328529 | Gastroprotective activity in Swiss albino mouse assessed as reduction in HCl/EtOH-induced gastric lesions by measuring lesion index at 30 mg/kg, sc pretreated followed by HCl/EtOH challenge measured after 1 hr (Rvb = 38.8 +/- 1.6 millimeter) | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors. |
AID192889 | Percentage of gastric damage was measured in rats. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID352502 | Antiinflammatory activity against carrageenan-induced rat inflammation model assessed as inhibition of paw edema at 11.7 umol/kg, po after 3 hrs | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: synthesis, biological evaluation and nitric oxide release studies. |
AID1055826 | Ulcerogenicity in albino Wistar rat assessed as gastric deep mucosal damage at 0.15 mmol/kg, po by hematoxylin and eosin staining-based assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation. |
AID653312 | Antiinflammatory activity in transgenic zebrafish larvae harboring Fli-1 gene assessed as LPS-stimulated leukocyte migration to injury zone of tail transected larvae at 10 uM after 20 to 22 hrs by microscopy | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: the nitroindazolinone chemotype. |
AID128861 | Acute toxicity was evaluated as number of mice died (tested = 7) after 72nd hour when 15 mg/kg is administered intraperitoneally | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1464292 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for human recombinant COX2 | |||
AID428391 | Gastrotoxicity in albino rat assessed as ulcer index at 100 mg/kg, po after 5 hrs | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. |
AID1294604 | Inhibition of human recombinant COX2 at 25 uM by ELISA relative to control | 2016 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10 | Synthesis of unsymmetrical monocarbonyl curcumin analogues with potent inhibition on prostaglandin E2 production in LPS-induced murine and human macrophages cell lines. |
AID1542907 | Selectivity index, ratio of IC50 for inhibition of ovine COX1 to IC50 for N-terminal GST-tagged recombinant human AKR1C3 expressed in Escherichia coli BL21 (DE) Codon Plus RP cells | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID667790 | Inhibition of recombinant human COX2 assessed as PGE2 formation at 1 uM by enzyme immunoassay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Indole based cyclooxygenase inhibitors: synthesis, biological evaluation, docking and NMR screening. |
AID1063322 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 12 hrs by ELISA (Rvb = 11.8 +/- 1.2 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID1195151 | Antiinflammatory activity in Swiss albino mouse assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 2 hrs relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID1220237 | Unbound fraction during UGT-mediated glucuronidation in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID130718 | In vivo inhibitory activity against A-23187 ear edema at a dose of 100 ug/ear | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity. |
AID169634 | Compound is evaluated for gastric ulceration in rats at a dose of 10 mg/kg(5/12) | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID1576168 | Anti-inflammatory activity in albino rat model of carrageenan-induced paw edema assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po administered as single dose prior to carrageenan challenge measured after 8 hrs relative to control | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents. |
AID487177 | Inhibition of human recombinant COX2 assessed as PGE2 level at 50 uM by ELISA | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis and cyclooxygenase inhibitory activities of some N-acylhydrazone derivatives of isoxazolo[4,5-d]pyridazin-4(5H)-ones. |
AID1540293 | Antiinflammatory activity against carrageenan-induced paw oedema in ICR mouse assessed as inhibition of paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge after 5 hrs post carrageenan challenge | |||
AID1067407 | Inhibition of ovine COX1 by peroxidase activity-based colorimetric assay | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles. |
AID128882 | Percentage acute toxicity after 8 mg/kg administered intraperitoneally to rats | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID254389 | Binding affinity towards human CRTH2 receptor expressed in CHO cells; range 25 nM to 8 uM | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. |
AID1303389 | Inhibition of bovine testis hyaluronidase using hyaluronic acid as substrate preincubated with CaCl2 for 20 mins followed by incubation with compound for 20 mins and substrate for 10 mins by colorimetric Morgan-Elson method in presence of BSA | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Interpreting the behavior of concentration-response curves of hyaluronidase inhibitors under DMSO-perturbed assay conditions. |
AID303579 | Antipyretic activity against LPS-induced pyresis in Wistar rat assessed as change in rectal temperature at 100 mg/kg, po after 6 hrs | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Aromatic amide derivatives of 5,6-dimethoxy-2,3-dihydro-1H-inden(-1-yl)acetic acid as anti-inflammatory agents free of ulcerogenic liability. |
AID356058 | Antiinflammatory activity against TPA-induced ear edema Swiss mouse chronic dermatitis model assessed as inhibition of increase in ear weight at 0.5 mg/ear relative to control | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Warangalone, the isoflavonoid anti-inflammatory principle of Erythrina addisoniae stem bark. |
AID624619 | Specific activity of expressed human recombinant UGT2B7 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1213540 | Retention time of the compound by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance. |
AID1426400 | Anti-inflammatory activity in Wistar albino rat assessed as inhibition of carragenan-induced paw edema thickness at 50 mg/kg, po measured after 1 hr relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC. |
AID188746 | Gastric toxicity in fasted rat at the dose of 16 mg/Kg (ig)(number of animals with damage/number of animals treated=6/6) | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16 | Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
AID1550479 | Antiinflammatory activity against carrageenan induced albino Sprague-Dawley rat paw edema model assessed as paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge and measured at 3 hrs post-carrageenan injection (Rvb = 38.4%) | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID748525 | Inhibition of mouse COX2 V349I mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID1193496 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1456026 | In vivo inhibition of COX-2 activity in carrageenan-induced Swiss mouse serum at 100 umol/kg, po pretreated for 1 hr followed by carrageenan challenge after 3 hrs by ELISA relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
AID1542914 | Antiproliferative activity against human HT-29 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID1783304 | Anti-inflammatory activity in Wistar albino rat model of carragenan-induced paw edema assessed as reduction in edema thickness at 28 uM/kg, ip measured after 3 hrs by plethysmometer (Rvb = 1.64 +/- 0.04 millimeter) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential. |
AID680808 | TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation by indomethacin at a concentration of 200uM in MRP2-expressing MDCK cells | |||
AID1737606 | Anti-inflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip pretreated for 1 hr followed by carrageenan challenge and measured after 4 hr relative to control (Rvb = 0.00 +/-0.4 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID1220255 | Apparent permeability by PAMPA method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
AID1869458 | Anti-inflammatory activity against LPS-induced inflammatory pain-like behaviour ICR mouse model assessed as improvement in locomotor activity by measuring increase in animal's movement speed in LABORAS arena at 10 mg/kg, ip treated with LPS for 2 hrs foll | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID1134900 | Inhibition of ADP-induced platelet aggregation in human platelet-rich plasma after 5 mins | 1979 | Journal of medicinal chemistry, Aug, Volume: 22, Issue:8 | 3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation. |
AID179452 | Analgesic activity on peroral administration against scald induced pain in rat paw | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
AID580344 | Antiinflammatory activity against TPA-induced mouse edema model assessed as ear thickness at 0.5 mg/ear (Rbv = 0.270 +/- 0.008 mm) | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents. |
AID1136193 | Toxicity in dog assessed as gastrointestinal intolerance at 10 to 30 mg/kg, po administered as single dose | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | Synthesis and antiinflammatory activity of 6,11-dihydro-11-oxodibenzo[b,e]thiepinalkanoic acids and related compounds. |
AID1869464 | Anti-inflammatory activity against LPS-induced inflammatory pain-like behaviour ICR mouse model assessed as reduction in IL-6 levels in plasma at 10 mg/kg, ip treated with LPS for 2 hrs followed by drug administration for 1 hr by ELISA | 2022 | Journal of natural products, 07-22, Volume: 85, Issue:7 | Batatasin III, a Constituent of |
AID313773 | Inhibition of ovine COX1 | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | 1-Toluene-sulfonyl-3-[(3'-hydroxy-5'-substituted)-gamma-butyrolactone]-indoles: synthesis, COX-2 inhibition and anti-cancer activities. |
AID611830 | Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po measured after 360 min by Plethysmograph | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Analogue-based design, synthesis and molecular docking analysis of 2,3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents. |
AID160556 | Compound is evaluated for inhibitory effect on the generation of Prostaglandin E2 (PGE2) from rat synovial cells | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID186596 | Tested for acute anti-inflammatory activity of the antirat serum-induced edema in rats at dose of 10 mg/kg at time interval- 3h | 1994 | Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18 | Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity. |
AID23265 | Partition coefficient (logD7.4) | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and quantitative structure-activity relationships of diclofenac analogues. |
AID162011 | In vitro inhibitory concentration against rat prostaglandin G/H synthase 1 | 2001 | Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20 | Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors. |
AID274909 | Antiinflammatory activity in carrageenan-induced mouse paw edema | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage. |
AID1455999 | Anti-inflammatory activity in Swiss mouse assessed as reduction in carrageenan-induced paw edema at 100 umol/kg, po pretreated for 1 hr followed by carrageenan challenge after 3 hrs by plethysmometer | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
AID547628 | Inhibition of human recombinant COX2 after 45 mins | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents. |
AID492149 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Cytotoxic flavonoids as agonists of peroxisome proliferator-activated receptor gamma on human cervical and prostate cancer cells. |
AID448127 | Antinociceptive activity in mouse assessed as inhibition of acetic acid-induced abdominal constrictions at 100 umol/kg, po relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH). |
AID1241876 | Inhibition of ovine COX1 by oxidized TMPD detection based colorimetric assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID178489 | Antiinflammatory activity in carrageenan model, activity is expressed as ED50 values | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1454303 | Analgesic activity in mouse at 10 mg/kg, ip measured after 60 mins at 58 degC by hot plate method | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15 | Synthesis, potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides. |
AID43581 | Inhibition of beta-lactamase at 100 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
AID1436694 | Antiinflammatory activity in carrageenan-induced rat paw edema model assessed as inhibition of TNFalpha level in paw at 20 mg/kg, po administered 1 hr followed by carrageenan challenge by ELISA relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening. |
AID364552 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip after 5 hrs | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives. |
AID1453464 | Ulcerogenicity in rat model of carrageenan-induced paw edema assessed as diameter of lesion in gastric wall at 10 mg/kg, po measured after 5 hrs | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | Synthesis of methanesulphonamido-benzimidazole derivatives as gastro-sparing antiinflammatory agents with antioxidant effect. |
AID1764399 | Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID238375 | Binding affinity for mouse Prostanoid DP receptor | 2004 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17 | Discovery of new chemical leads for prostaglandin D2 receptor antagonists. |
AID1529184 | Protein binding in immobilized human serum albumin by HPLC analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID681860 | TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation in the presence of indomethacin at a concentration of 200uM in MRP1-expressing HeLa cells | |||
AID1743656 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Synthesis and biological evaluation of organoselenium (NSAIDs-SeCN and SeCF |
AID322955 | Inhibition of synthetic amyloid beta-42 oligomerization by ELISA | 2007 | The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14 | Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct. |
AID678492 | Antiinflammatory activity in AKR mouse assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg dosed intradermally after 3.5 hrs relative to vehicle-treated control | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Synthesis, biological evaluation, and docking studies of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines as potent anti-inflammatory and antioxidant agents. |
AID128871 | Percentage acute toxicity after 15 mg/kg administered intraperitoneally to rats | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID177375 | Inhibition of dermal RPAR in rats following p.o. administration; Not significant. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | 2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents. |
AID209196 | Concentration required to inhibit production of LTC4 from THP-1 cells stimulated with A-23187 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'. |
AID162637 | Inhibition of Prostaglandin G/H synthase 2 was measured by the inhibition of PGE-2 produced by lipopolysaccharide-challenged HWB | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors. |
AID604299 | Inhibition of human glyoxalase 1 | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I. |
AID190152 | In vivo ulcerogenicity was determined after peroral administration in rat | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase. |
AID1403473 | Selectivity index, ratio of IC50 for ovine COX1 to IC50 for recombinant human COX2 | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study. |
AID675143 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 10 mg/kg, po administered 60 mins before carrageenan challenge measured after 4 hr (Rvb = 91.2 +/- 2.3 mL) | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Design, synthesis, antimicrobial, anti-inflammatory and analgesic activity of novel isoxazolyl pyrimido[4,5-b]quinolines and isoxazolyl chromeno[2,3-d]pyrimidin-4-ones. |
AID540216 | Clearance in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID192860 | Antiinflammatory activity expressed as minimum effective dose was screened by using adjuvant-induced local hyperthermia in rats | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones. |
AID1550470 | Inhibition of human COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents. |
AID160567 | Inhibition concentration against Prostaglandin G/H synthase 2 | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9 | Enantiospecific, selective cyclooxygenase-2 inhibitors. |
AID161327 | Biochemical index for Prostaglandin G/H synthase 1 measured as, thromboxane 2 (TXB2) levels following blood coagulation | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors. |
AID190164 | The compound was tested in vivo for gastric ulcerogenic activity in rat after peroral administration | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | 4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1) |
AID162481 | Concentration required to inhibit human Prostaglandin G/H synthase 2 (COX-2) by 50% | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | 1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents. |
AID723699 | Inhibition of soybean lipoxygenase assessed as inhibition of sodium linolate conversion to 13-hydroperoxylinoleic acid after 4 mins by spectrophotometry | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents. |
AID161986 | Percentage of inhibition of Prostaglandin G/H synthase 1 activity in human whole blood (HWB) at 1 uM | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines. |
AID189414 | Vocalization threshold value was measured in rat yeast induced hyperalgesia assay at a dose of 10 mg/kg for 4 hr. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin. |
AID1195149 | Analgesic activity in Swiss albino mouse assessed as time of licking paws at 100 mg/kg, po measured after 2 hrs by tail flick test relative to control | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies. |
AID187770 | Antiinflammatory activity was assessed improvement of adjuvant induced arthritis in rats, determined by joint mobility of the paw | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | 5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents. |
AID444875 | Antiinflammatory activity against carrageenan-induced paw edema in Wistar rat assessed as inhibition of hind paw edema at 10 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 3 hrs relative to control | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | 1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoi |
AID1532667 | Anti-inflammatory activity in carrageenan-induced albino rat assessed as reduction in paw edema volume at 20 umol/kg, po measured at 1 hr intervals up to 4 hrs relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Anti-inflammatory activity of triazine derivatives: A systematic review. |
AID289300 | Inhibition of acetic acid-induced capillary permeability in Swiss Albino mouse at 10 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. |
AID389156 | Antiinflammatory activity against carrageenan-induced foot paw edema in rat at 0.01 mmol/kg, ip | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity. |
AID687438 | Gastric toxicity in Swiss mouse assessed as erosion index at 10 mg/kg administered as single dose (Rvb = 0 +/- 0 erosion index) | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Mechanisms involved in the antinociceptive effects of 7-hydroxycoumarin. |
AID177891 | Inhibition of carrageenan edema in rats was determined after peroral administration of 100 mg/kg | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones. |
AID1891743 | Induction of mitochondrial outer membrane damage in human MCF7 cells assessed as increase in mitochondrial depolarization by measuring reduction in red fluorescence measured after 24 hrs by TMRM dye based confocal microscopy | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Small molecule NSAID derivatives for impairing powerhouse in cancer cells. |
AID549980 | Antiinflammatory activity in mouse assessed as TPA-induced mouse ear edema administered to right ear after 4 hrs | 2010 | Journal of natural products, Nov-29, Volume: 73, Issue:11 | Lupane triterpenes with a δ-lactone at ring E, from Lippia mexicana. |
AID763516 | Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Synthesis of novel celecoxib analogues by bioisosteric replacement of sulfonamide as potent anti-inflammatory agents and cyclooxygenase inhibitors. |
AID1241868 | Hepato-toxicity in rat Freund's adjuvant induced arthritis model of chronic inflammation assessed as assessed as histological changes at 10 mg/kg, po dosed after 14 days from day of adjuvant injection until day 21 and measured on day 21 by hematoxylin and | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents. |
AID1123742 | Analgesic activity in po dosed mouse assessed as inhibition of acetic acid-induced writhing | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids. |
AID177372 | Effective dose of compound for 40% inhibition of rat dermal reverse passive Arthus reaction (RPAR) on peroral administration; No significant inhibition at 56 umol/kg (Inactive) | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | 3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation. |
AID1650566 | Inhibition of calcium ionophore-activated COX1 in human whole blood assessed as TXB2 level at 1 uM by ELISA (Rvb = 1.20 ng/ml) | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats. |
AID49194 | Compound was evaluated for percent inhibition of carrageenan induced rat paw edema at 0.005 mmol/kg | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Synthesis and biological evaluation of novel coumarin derivatives with a 7-azomethine linkage. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID322958 | Inhibition of synthetic amyloid beta-42 fibrillation by light scattering analysis relative to control | 2007 | The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14 | Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct. |
AID284324 | Inhibition of ovine COX1 | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. |
AID426427 | In vivo antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip administered simultaneously with carrageenan measured after 3.5 hrs | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts. |
AID642879 | Potentiation of doxorubicin-induced cytotoxicity against multidrug-resistant human T98G cells expressing MRP-1 at 50 uM pretreated for 2 hrs prior addition of doxorubicin measured after 3 days by crystal violet staining analysis | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity. |
AID753752 | Antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 0.28 mmol/kg, po after 4 hrs relative to control | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13 | New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities. |
AID193141 | Percentage inhibition of the prostaglandin synthesis was measured in rats. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series. |
AID1737626 | Analgesic activity in albino mouse assessed as protection at 10 mg/kg, ip measured after 90 mins by hot plate test (Rvb = 0 %) | 2020 | European journal of medicinal chemistry, Jun-15, Volume: 196 | Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates. |
AID381197 | Inhibition of 5-lipoxygenase in Wistar rat peritoneal leukocytes at 50 ug/mL | 1999 | Journal of natural products, Sep, Volume: 62, Issue:9 | Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation. |
AID598526 | 1-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design. |
AID1852417 | Antiinflammatory activity against LPS/talc powder induced pericarditic Wistar rat assessed as reduction in U wave flattening at 20 mg/kg, ip pretreated for 2 hrs followed by LPS/tal powder stimulation measured after 48 hrs in presence of 2-(4-(5-oxo-5-((5 | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia. |
AID1063318 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 24 hrs by ELISA (Rvb = 45.1 +/- 5.6 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID161671 | Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production | 2002 | Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7 | Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models. |
AID729259 | Inhibition of human recombinant AKR1C2-mediated NADP+-dependent oxidation of S-(+)-1,2,3,4-tetrahydro-1-naphthol | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
AID1773228 | Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Greiss reagent based assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Identification, semisynthesis, and anti-inflammatory evaluation of 2,3-seco-clavine-type ergot alkaloids from human intestinal fungus Aspergillus fumigatus CY018. |
AID177221 | In vivo inhibition of carrageenan-induced air pouch in rats | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors. |
AID1141757 | Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Synthesis, biological evaluation, molecular docking and theoretical evaluation of ADMET properties of nepodin and chrysophanol derivatives as potential cyclooxygenase (COX-1, COX-2) inhibitors. |
AID1336951 | Induction of cell cycle arrest in human LNCAP cells assessed as accumulation at G1 phase at 40 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 69.5%) | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase. |
AID1063320 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 6 hrs by ELISA (Rvb = 7.2 +/- 0.9 pg/ml) | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives. |
AID287339 | Antiinflammatory activity against carrageenan-induced paw edema in Swiss albino mouse assessed as swelling thickness at 10 mg/kg, po after 270 mins | 2007 | Bioorganic & medicinal chemistry, Feb-15, Volume: 15, Issue:4 | Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. |
AID1542905 | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. |
AID178776 | Reduction in exudate volume in rat pleural RPAR test; Nonactive. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | 2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents. |
AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID481237 | Antiarthritic activity in po dosed BALB/c mouse collagen antibody induced arthritis model assessed as increase of arthritis score administered qd for 2 days after collagen antibody challenge measured after 2 days | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10 | Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III. |
AID677462 | Dissociation constant, pKa of the compound | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach. |
AID1540291 | Antiinflammatory activity against carrageenan-induced paw oedema in ICR mouse assessed as reduction in NO level in serum at 20 mg/kg, po administered 30 mins prior to carrageenan challenge after 5 hrs post carrageenan | |||
AID688462 | Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as reduction in AUC of of Croton oil-induced ear edema response at 0.4 umol administered topically per cm'2 of ear measured 48 hrs after induction of dermatitis relative to untreated con | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. |
AID1674099 | Inhibition of AKR1C2 (unknown origin) using 9,10-phenanthrenequinone as substrate | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Overview of AKR1C3: Inhibitor Achievements and Disease Insights. |
AID1063665 | Antinociceptive activity in Swiss albino mouse assessed as licking time in primary neurogenic period at 5 mg/kg, ip administered 30 mins prior to formalin-challenge (Rvb = 80 +/- 19 seconds) | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors. |
AID1517245 | Inhibition of ovine COX-1 by EIA method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies. |
AID184174 | In vivo anti-inflammatory activity determined by rat carrageenan paw edema method at 10 mg/kg perorally | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID681372 | TP_TRANSPORTER: inhibition of MTX uptake in OAT3-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 302, Issue:2 | Characterization of methotrexate transport and its drug interactions with human organic anion transporters. |
AID748522 | Inhibition of mouse COX2 R120Q mutant using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. |
AID287090 | Inhibitory ratio of TPA-induced edema in presence of drug to TPA-induced edema in ICR mouse | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Triterpene glycosides from the flower petals of sunflower (Helianthus annuus) and their anti-inflammatory activity. |
AID1568914 | Analgesic activity in Wistar rat model of formalin-induced hyperalgesia assessed as reduction in number of formalin-evoked paw flinching during neurogenic phase at 10 mg/kg preincubated for 30 mins followed by formalin treatment and measured during first | |||
AID380766 | Antiinflammatory activity against croton oil-induced ear edema in mouse | 2006 | Journal of natural products, Mar, Volume: 69, Issue:3 | Bioactive triterpenoids from Salvia species. |
AID1153844 | Inhibition of human recombinant COX-2 using arachidonic acid as substrate assessed as residual activity at 10 uM preincubated for 5 mins followed by substrate addition measured after 5 mins by HPLC analysis relative to control | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1. |
AID683092 | Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 by enzyme immuno assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity. |
AID487176 | Inhibition of sheep COX1 assessed as PGE2 level at 50 uM by ELISA | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6 | Synthesis and cyclooxygenase inhibitory activities of some N-acylhydrazone derivatives of isoxazolo[4,5-d]pyridazin-4(5H)-ones. |
AID1226815 | Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes. |
AID1303390 | Inhibition of bovine testis hyaluronidase using hyaluronic acid as substrate at 3000 uM preincubated with CaCl2 for 20 mins followed by incubation with compound for 20 mins and substrate for 10 mins by colorimetric Morgan-Elson method in presence of 0.05% | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Interpreting the behavior of concentration-response curves of hyaluronidase inhibitors under DMSO-perturbed assay conditions. |
AID611099 | Displacement of [3H]-Iloprost from human IP receptor expressed in CHO cells after 30 mins by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of selective indole-based prostaglandin D₂ receptor antagonist. |
AID647941 | Antiinflammatory activity in ICR mouse assessed as inhibition of carrageenan-induced COX2 protein expression in paw at 10 mg/kg, ip administered 30 mins before carrageenan challenge by Western blotting relative to control | 2012 | Journal of natural products, Jan-27, Volume: 75, Issue:1 | Sclareol exhibits anti-inflammatory activity in both lipopolysaccharide-stimulated macrophages and the λ-carrageenan-induced paw edema model. |
AID1353367 | Antinociceptive activity in formalin-induced Swiss mouse model of hyperalgesia assessed as time spent licking the injected paw in early phase at 100 mM/kg, po pretreated for 1 hr followed by formalin injection and measured up to 5 mins (Rvb = 74 +/- 7.7 s | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
AID168746 | Analgesic activity in acetic acid writhing test, activity is expressed as ED50 values | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID389641 | Antiinflammatory activity against carrageenan-induced paw edema in ICR mouse at 4 mg/kg, ip administered 30 mins before carrageenan challenge assessed after 5 hrs | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Anti-inflammatory activities of furanoditerpenoids and other constituents from Fibraurea tinctoria. |
AID1608415 | Anti-inflammatory activity against carrageenan-induced Albino Wistar rat paw edema model assessed as inhibition of rat paw edema at 10 mg/kg, po pretreated for 1 hr followed by carrageenan addition measured after 1 to 4 hrs relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Role of sulphur-heterocycles in medicinal chemistry: An update. |
AID1149356 | Therapeutic ratio of ID50 for ulcerogenicity in Wistar rat to ED50 for antiinflammatory activity against Mycobacterium butyricum adjuvant-induced polyarthritis in Lewis albino rat non-injected paw | 1977 | Journal of medicinal chemistry, Jan, Volume: 20, Issue:1 | Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 1. 6,11-Dihydro-11-oxodibenz]b,e]oxepin-2-acetic acids. |
AID617128 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess reaction based spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Diarylheptanoids from Curcuma kwangsiensis and their inhibitory activity on nitric oxide production in lipopolysaccharide-activated macrophages. |
AID444057 | Fraction escaping hepatic elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID464512 | Selectivity for Trypanosoma brucei brucei over human HMEC | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Podophyllotoxin analogues active versus Trypanosoma brucei. |
AID162489 | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
AID644721 | Selectivity ratio of IC50 for human recombinant COX2 to IC50 for ram seminal vesicle COX1 | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis of novel 2-mercapto benzothiazole and 1,2,3-triazole based bis-heterocycles: their anti-inflammatory and anti-nociceptive activities. |
AID540220 | Clearance in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1545122 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells incubated for 24 hrs by Griess reagent based assay | 2019 | Journal of natural products, 08-23, Volume: 82, Issue:8 | Antibacterial and Inhibitory Activities against Nitric Oxide Production of Coumaronochromones and Prenylated Isoflavones from |
AID645024 | Antiinflammatory activity in Wister albino rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 1 hr before carrageenan challenge measured after 2 hrs by plethysmometer relative to control | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents. |
AID168894 | Analgesic activity evaluated by measuring % analgesic effect, after oral administration of 3.0 mg/kg in acetic acid writhing test | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12 | 2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity. |
AID1174280 | Antiinflammatory activity in Sprague-Dawley rat model of LPS-induced sepsis assessed as AST level at 5 mg/kg/day dosed through gastric intubation for 6 days (Rvb = 148.9 +/- 41.3 U/L) | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents. |
AID1639501 | Cytotoxicity against mouse RAW264.7 cells by MTT assay | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Anti-inflammatory Mono- and Dimeric Sorbicillinoids from the Marine-Derived Fungus Trichoderma reesei 4670. |
AID642994 | Antiinflammatory activity in Sprague-Dawley rat assessed as reduction in carrageenan-induced paw edema at 20 mg/kg, ip administered 30 mins before carrageenan challenge measured after 4 hrs by plethysmometer analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands. |
AID674722 | Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 0.029 mmol/kg. po dosed 1 hr before acetic acid challenge and measured during 30 mins post acetic acid challenge | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies. |
AID328204 | Inhibition of COX2 at 100 uM | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. |
AID540231 | Dose normalised AUC in dog after po administration | 2005 | Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2 | Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. |
AID184502 | Antiinflammatory activity was assessed in prophylactic adjuvant induced polyarthritis(AIP) test after po administration. | 1982 | Journal of medicinal chemistry, Jan, Volume: 25, Issue:1 | Isoxicam and related 4-hydroxy-N-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides. Potent nonsteroidal antiinflammatory agents. |
AID123872 | Gastric ulcerogenic activity at a dose of 10 mg/kg: 8 mice were considered for the test | 1992 | Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7 | Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2. |
AID680169 | TP_TRANSPORTER: inhibition of Ochratoxin A uptake (OTA: 1 uM, Indomethacin: 200 uM) in OAT4-expressing S2 cells | 2002 | Biochimica et biophysica acta, Jun-12, Volume: 1590, Issue:1-3 | Role of human organic anion transporter 4 in the transport of ochratoxin A. |
AID1193500 | Thermodynamic equilibrium solubility, log S of the compound | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
AID1346326 | Human DP2 receptor (Prostanoid receptors) | 2002 | British journal of pharmacology, Dec, Volume: 137, Issue:8 | Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. |
AID1346401 | Mouse DP2 receptor (Prostanoid receptors) | 2005 | The Journal of biological chemistry, Sep-16, Volume: 280, Issue:37 | Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2. |
AID1345284 | Human COX-1 (Cyclooxygenase) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID1345155 | Human Proton-coupled folate transporter (SLC46 family of folate transporters) | 2006 | Cell, Dec-01, Volume: 127, Issue:5 | Identification of an intestinal folate transporter and the molecular basis for hereditary folate malabsorption. |
AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 2001 | European journal of pharmacology, Apr-06, Volume: 417, Issue:1-2 | Binding of prostaglandins to human PPARgamma: tool assessment and new natural ligands. |
AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 1997 | The Journal of biological chemistry, Feb-07, Volume: 272, Issue:6 | Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs. |
AID1345206 | Human COX-2 (Cyclooxygenase) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities. |
AID1346401 | Mouse DP2 receptor (Prostanoid receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 306, Issue:2 | Expression and molecular pharmacology of the mouse CRTH2 receptor. |
AID1346326 | Human DP2 receptor (Prostanoid receptors) | 2005 | European journal of pharmacology, Nov-07, Volume: 524, Issue:1-3 | CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2013 | ChemMedChem, Sep, Volume: 8, Issue:9 | Zopolrestat as a human glyoxalase I inhibitor and its structural basis. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2005 | Journal of molecular biology, May-20, Volume: 348, Issue:5 | Crystal structure and possible catalytic mechanism of microsomal prostaglandin E synthase type 2 (mPGES-2). |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2005 | Journal of molecular biology, May-20, Volume: 348, Issue:5 | Crystal structure and possible catalytic mechanism of microsomal prostaglandin E synthase type 2 (mPGES-2). |
AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 12874 (45.76) | 18.7374 |
1990's | 7078 (25.16) | 18.2507 |
2000's | 4394 (15.62) | 29.6817 |
2010's | 3081 (10.95) | 24.3611 |
2020's | 705 (2.51) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (108.86) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1,838 (6.22%) | 5.53% |
Reviews | 947 (3.21%) | 6.00% |
Case Studies | 1,311 (4.44%) | 4.05% |
Observational | 14 (0.05%) | 0.25% |
Other | 25,417 (86.08%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Phase I/II Study of Enzalutamide in Combination With Indomethacin in Castration-Resistant Prostate Cancer (CRPC) [NCT02935205] | Phase 1/Phase 2 | 38 participants (Anticipated) | Interventional | 2017-01-17 | Recruiting | ||
An Escalating Dose Indomethacin for the Treatment of Persistent Patent Ductus Arteriosus (PDA) In Preterm Infants- A Randomized Pilot Study [NCT00750581] | Phase 2/Phase 3 | 9 participants (Actual) | Interventional | 2008-08-31 | Terminated(stopped due to Study medication was no longer available for study) | ||
Effect of Selective and Nonselective Cyclooxygenase Enzyme Inhibition on Arterial Blood Pressure and Cerebral Blood Flow With Exposure to Intermittent Hypoxia in Humans [NCT01280006] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
Clinical Research on the Prophylactic Efficacy of Pancreatic Duct Stenting Combined With Rectal Indomethacin Drug on Post Endoscopic Retrograde Cholangiopancreatography Pancreatitis [NCT03643900] | 618 participants (Actual) | Interventional | 2018-08-08 | Completed | |||
Comparative Evaluation of Standard Prophylaxis Versus Divided-dose NSAIDs or Hybrid NSAID and N-acetylcysteine Therapy for the Prevention of Post-ERCP Pancreatitis [NCT03708458] | Phase 4 | 250 participants (Anticipated) | Interventional | 2017-04-01 | Recruiting | ||
A Phase I, Open-label, Randomized, 4-period Crossover Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Multiple Doses of K-285 Compared With a Single Oral Dose of Indomethacin Capsule in Healthy Adult Volunteers [NCT03712241] | Phase 1 | 15 participants (Actual) | Interventional | 2018-10-04 | Completed | ||
The Effect of Dehydration on Intestinal Permeability [NCT03620825] | 20 participants (Actual) | Interventional | 2018-03-17 | Completed | |||
Rectal Indomethacin Decreases the Incidence of Pancreatitis Following Endoscopic Retrograde Cholangiopancreatography in High-risk Patients [NCT02110810] | Phase 3 | 160 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
A Randomized Controlled Trial of Indomethacin in Acute Pancreatitis- Effectiveness and Safety [NCT03547232] | Phase 3 | 240 participants (Anticipated) | Interventional | 2018-07-01 | Recruiting | ||
Dubbelblind Crossover Study for Validation of New Tests for Gastrointestinal (GI) Permeability [NCT00943345] | Early Phase 1 | 34 participants (Anticipated) | Interventional | 2009-09-30 | Enrolling by invitation | ||
Quantification of Postoperative Coagulation Following Administration of Indomethacin to Expedite Fast-tracking of Cardiac Surgical Patients [NCT01073670] | Phase 4 | 82 participants (Actual) | Interventional | 2000-08-31 | Completed | ||
LCH-IV, International Collaborative Treatment Protocol for Children and Adolescents With Langerhans Cell Histiocytosis [NCT02205762] | Phase 2/Phase 3 | 1,400 participants (Anticipated) | Interventional | 2016-11-02 | Recruiting | ||
A Phase Ib Study to Assess the Safety, Tolerability and Immunologic Activity of Preoperative IRX 2 In Early Stage Breast Cancer [NCT02950259] | Phase 1 | 16 participants (Actual) | Interventional | 2017-02-09 | Active, not recruiting | ||
Indomethacin for Refractory Chronic Cough: a Randomized, Double-blind, Placebo-controlled Trial [NCT03662269] | Phase 3 | 84 participants (Anticipated) | Interventional | 2018-10-22 | Recruiting | ||
Relative Effectiveness and Safety of Pharmacotherapeutic Agents for Patent Ductus Arteriosus (PDA) in Preterm Infants: A National Comparative Effectiveness Research (CER) Project [NCT04347720] | 1,350 participants (Anticipated) | Observational [Patient Registry] | 2020-01-01 | Recruiting | |||
Rectal Disclofenac Versus Indomethacin for Prevention of Post-ERCP Pancreatitis (DIPPP): A Multicentre, Double-blind, Randomised, Controlled Trial [NCT05947461] | 3,612 participants (Anticipated) | Interventional | 2023-06-01 | Recruiting | |||
A Randomized Trial Comparing Rectal Indomethacin Alone Versus a Combination of Rectal Indomethacin and Oral Tacrolimus for Post-ERCP Pancreatitis Prophylaxis [NCT05252754] | Phase 3 | 4,874 participants (Anticipated) | Interventional | 2023-01-18 | Recruiting | ||
Comparison of the Efficacy of IV Acetaminophen Versus IV Indomethacin in Treatment of Hemodynamically Significant PDA in VLBW Infants [NCT03537144] | Phase 3 | 37 participants (Actual) | Interventional | 2016-06-30 | Terminated(stopped due to Difficulty enrolling patients) | ||
Nifedipine vs. Indomethacin in the Treatment of Preterm Labour and Short Cervix. A Randomized, Controlled Trial. [NCT01360034] | Phase 3 | 216 participants (Anticipated) | Interventional | 2015-12-31 | Not yet recruiting | ||
A Phase II Neoadjuvant Study of Apalutamide, Abiraterone Acetate, Prednisone, Degarelix and Indomethacin in Men With Localized Prostate Cancer Pre-Prostatectomy [NCT02849990] | Phase 2 | 22 participants (Actual) | Interventional | 2017-03-09 | Completed | ||
A Prospective Open-label Randomized Controlled Trial Comparing Effectiveness of Aggressive Hydration Versus High-dose Rectal Indomethacin in the Prevention of Post-ERCP Pancreatitis (PEP) [NCT03629600] | Phase 2/Phase 3 | 352 participants (Actual) | Interventional | 2017-10-15 | Completed | ||
A Randomized Phase 2 Trial of Neoadjuvant and Adjuvant Therapy With the IRX 2 Regimen in Patients With Newly Diagnosed Stage II, III, or IVA Squamous Cell Carcinoma of the Oral Cavity [NCT02609386] | Phase 2 | 105 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
Timing of Indomethacin Administration for the Prevention of Post-ERCP Pancreatitis (PEP) [NCT02111707] | Phase 4 | 534 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
Rectal Indomethacin Versus Intraperitoneal Lidocaine for Analgesia After Laparoscopic Cholecystectomy [NCT04964180] | 80 participants (Actual) | Interventional | 2020-05-01 | Completed | |||
A Randomized, Double-Blind, Placebo-Controlled, Single, Repeat Dose Escalation and Indomethacin Challenge Study to Evaluate Safety, Tolerability and Pharmacokinetics of GSK4381406 in Healthy Participants [NCT05999708] | Phase 1 | 0 participants (Actual) | Interventional | 2023-10-31 | Withdrawn(stopped due to Study terminated prior to FSFV for strategic business reasons.) | ||
Comparative Effectiveness Between Rectally Administered Indomethacin and Pancreatic Stenting in the Prevention of Post Endoscopic Retrograde Cholangio-panceaticography (ERCP) Pancreatitis: a Randomized Trial [NCT03713879] | Phase 3 | 1,734 participants (Anticipated) | Interventional | 2019-03-21 | Recruiting | ||
A Double Blind, Randomized, Parallel Group Trial to Compare the Effect of Three Doses of Meloxicam Tablets (7.5, 15 and 30 mg) With Placebo on Bleeding Time in Healthy Subjects; With Extended-release Indomethacin Capsules 75 mg (Open-label) as an Active C [NCT02183155] | Phase 4 | 82 participants (Actual) | Interventional | 2000-05-31 | Completed | ||
Indomethacin Prior to Difficult Embryo Transfer is it a Solution? [NCT03533803] | Phase 3 | 200 participants (Actual) | Interventional | 2018-06-02 | Completed | ||
An Investigation of the Influence of Different Intrathecal Opioids on the Post-operative Pain Experiences of Woman at Rahima Moosa Mother and Child Hospital [NCT02577809] | Phase 4 | 100 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
Effect of Common Neonatal Procedures Over the Amplitude- Integrated Electroencephalography Register in <30 Weeks Preterms. [NCT00722033] | Phase 2 | 10 participants (Anticipated) | Interventional | 2008-08-31 | Not yet recruiting | ||
[NCT00904904] | Phase 4 | 120 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
Azithromycin to Improve Latency in Exam Indicated Cerclage: a Randomized Control Trial [NCT05132829] | Phase 4 | 50 participants (Anticipated) | Interventional | 2021-12-20 | Recruiting | ||
Vitreous Nonsteroidal Antiinflammatory Drus Concentrations And Prostaglandin E2 Levels in Vitrectomy Patients Treated With Indomethacin 0.5%, Bromfenac 0.09%, and Nepafenac 0.1% [NCT02361645] | Phase 3 | 70 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
Zushima Plaster for Patients in Knee Osteoarthritis: a Random, Positive Drug Controlled, Multi-center Clinical Research [NCT02770950] | Phase 4 | 396 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
Rectal Indomethacin Use in Pain Relief During Intrauterine Device Insertion: A Randomized Controlled Trial [NCT02711358] | Phase 4 | 120 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
Role of Indomethacin in Cases of Difficult Embryo Transfer in Intra Cytoplasmic Sperm Injection Cycles [NCT02642601] | Phase 2/Phase 3 | 100 participants (Anticipated) | Interventional | 2014-03-31 | Recruiting | ||
New Therapeutic Approaches to the Resistant Patent Ductus Arteriosus (PDA) in Low Birth Weight Neonates [NCT00616382] | Phase 2 | 68 participants (Anticipated) | Interventional | 2008-03-31 | Not yet recruiting | ||
Cerebral Vasodilator Responses in Sedentary and Exercise Trained Humans [NCT02653638] | Early Phase 1 | 80 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
Post ERCP Pancreatitis Prophylaxis, Effectiveness of Rectal Indomethacin vs Intravenous Ketorolac in the Pediatric Population [NCT05664074] | Phase 4 | 192 participants (Anticipated) | Interventional | 2022-11-07 | Recruiting | ||
Rectally Administered Indomethacin to Prevent Post-ESWL-pancreatitis (RIPEP) [NCT02797067] | Phase 4 | 1,370 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
Stent vs. Indomethacin for Preventing Post-ERCP Pancreatitis: The SVI Trial [NCT02476279] | Phase 3 | 1,950 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
Treatment of Orthostatic Intolerance [NCT00262470] | Phase 1/Phase 2 | 150 participants (Anticipated) | Interventional | 1997-04-30 | Active, not recruiting | ||
Efficacy of Ibuprofen Versus Indomethacin as Perioperative Prophylactic Treatment Following Emergent Cerclage Placement for Pregnancy Prolongation: A Randomized Controlled Trial [NCT04726085] | 100 participants (Anticipated) | Interventional | 2021-02-01 | Enrolling by invitation | |||
7 cm vs. 5 cm Pancreatic Stents for the Prevention of Post-ERCP Pancreatitis in High-risk Patients: a Multicentre, Single-blinded, Randomised Controlled Trial [NCT04145336] | 800 participants (Anticipated) | Interventional | 2019-10-15 | Active, not recruiting | |||
A Multi-Center, Randomized, Double-Blind, Active-Controlled Study of the Safety and Efficacy of Rilonacept Administered Subcutaneously for the Treatment of an Acute Gout Flare [NCT00855920] | Phase 3 | 225 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
Performance of 13C Mannitol for in Vivo Measurement of Small Intestinal Permeability [NCT02603822] | Phase 1 | 25 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
A Randomized, Open Label, 3-arm Evaluation of Efficacy and Safety of Meloxicam Suppository (15mg Daily) and Tablet (15 mg Daily) Compared to Indomethacin Suppository (50 mg Daily) in Patients With Ankylosing Spondylitis [NCT02183168] | Phase 3 | 192 participants (Actual) | Interventional | 2001-07-01 | Completed | ||
A Randomized, Double-Blind, Active-Comparator-Controlled 5-Day Trial of the Effect of Etoricoxib 120 mg Versus Indomethacin 150 mg in the Treatment of Acute Gout [NCT00142558] | Phase 4 | 180 participants (Actual) | Interventional | 2005-01-01 | Completed | ||
Apremilast Therapy for Acute Gouty Arthritis [NCT00997581] | Phase 2 | 0 participants (Actual) | Interventional | 2010-04-30 | Withdrawn(stopped due to Colaborator withdrew support.) | ||
Phase 1, Open-label Study, in Healthy Male Volunteers to Evaluate the Potential Effect of Indomethacin on the Pharmacokinetics Parameters of Elafibranor [NCT03985969] | Phase 1 | 26 participants (Actual) | Interventional | 2019-09-23 | Completed | ||
Non Interventional Study on Indomethacin-responsive Headaches [NCT03967483] | 100 participants (Anticipated) | Observational | 2019-06-01 | Not yet recruiting | |||
A Phase 3, Randomized, Double-Blind, Multicenter, Active-Controlled Trial To Evaluate The Efficacy And Safety Of Celecoxib (Celebrex®) And Indomethacin In The Treatment Of Moderate To Severe Acute Gouty Arthritis [NCT00549549] | Phase 3 | 402 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
Clinical Efficacy of Indomethacin in Early Treatment of Acute Pancreatitis [NCT05637281] | 188 participants (Anticipated) | Interventional | 2022-12-11 | Recruiting | |||
Ibuprofen vs. Indomethacin as Second Course of Therapy for Resistant PDA in Low Birth Weight Neonates [NCT01070745] | Phase 2 | 0 participants (Actual) | Interventional | 2010-06-30 | Withdrawn(stopped due to Changes in approach to PDA therapy) | ||
A Scientific & Clinical Review of Minimal Stimulation Protocol Using AROMEK (Letrozole) and Follitrope (Recombinant FSH)Combined With INVOCell(Intravaginal Culturing) - Effectiveness as Low Cost IVF [NCT01058252] | 30 participants (Anticipated) | Observational | 2021-05-31 | Recruiting | |||
A Phase 1 Study to Evaluate the Potential Two-Way Pharmacokinetic Interaction Between Lesinurad and Naproxen and Between Lesinurad and Indomethacin in Healthy Adult Male Subjects [NCT01884272] | Phase 1 | 24 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
The Effect of Indomethacin in Monosymptomatic Enuresis Nocturnal [NCT00226122] | Phase 4 | 56 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
Evaluation and Treatment of Autonomic Failure. [NCT00223691] | Phase 1 | 389 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
Multi-center, Randomized Non-inferiority Trial of Early Treatment Versus Expectative Management of Patent Ductus Arteriosus in Preterm Infants (BeNeDuctus Trial - Belgium Netherlands Ductus Trial) [NCT02884219] | 273 participants (Actual) | Interventional | 2016-12-23 | Completed | |||
Ketotifen and Indomethacin Combination Treatment Clinical Trial for COVID-19 A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Proof-of-Concept Clinical Trial to Evaluate the Efficacy of Ketotifen and Indomethacin for Mild and Moderate COVID-19 in A [NCT05007522] | Phase 3 | 150 participants (Anticipated) | Interventional | 2022-05-03 | Recruiting | ||
Routine Rectal Indomethacin Given Before Procedure Reduced Overall Pancreatitis in Patients Undergoing Endoscopic Retrograde Cholangiopancreatography (ERCP): A Multi-center, Single-blinded, Randomized Controlled Trial [NCT02002650] | 2,600 participants (Actual) | Interventional | 2013-12-31 | Completed | |||
Phase III Study of LI [Multikine®] Plus SOC (Surgery + Radiotherapy or Surgery + Concurrent Radiochemotherapy) in Subjects With Advanced Primary Squamous Cell Carcinoma of the Oral Cavity/Soft Palate vs. SOC Only [NCT01265849] | Phase 3 | 928 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
A Clinical Study on the Optimal Dose of Indomethacin Suppository for Preventing Post-ERCP Pancreatitis [NCT06031363] | 192 participants (Anticipated) | Interventional | 2022-11-01 | Recruiting | |||
A Phase IIA, Open-label, Safety and Pharmacokinetic Study of Indomethacin Capsules in Pediatric Subjects 6 to <17 Years of Age With Mild to Moderate Acute Postoperative Pain Following Elective Surgery [NCT02633969] | Phase 2 | 30 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
Role in Emergent Cerclage of Indomethacin and Antibiotics [NCT01114516] | 53 participants (Actual) | Interventional | 2010-03-31 | Completed | |||
A Relative Bioavailability Study of 75mg Indomethacin Extended-Release Capsules Under Fasting Conditions [NCT00858195] | Phase 1 | 36 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
Prophylaxis of Post-ERCP Acute Pancreatitis: a Randomized, Multicenter, Open-label Study Comparing Indomethacin Versus Indomethacin-ringer Lactate Combination [NCT05381428] | Phase 3 | 1,250 participants (Anticipated) | Interventional | 2022-05-13 | Recruiting | ||
Tocolysis for Preterm Labor [NCT00811057] | 301 participants (Actual) | Interventional | 2004-06-30 | Completed | |||
Effect of Indomethacin on the Progression of Alzheimer's Disease [NCT00432081] | Phase 3 | 160 participants | Interventional | 2000-05-31 | Completed | ||
Changes of Cerebral Tissue Oxygen Saturation During Treatment of Patent Ductus Arteriosus in Neonates [NCT01428180] | 35 participants (Actual) | Observational | 2011-04-30 | Completed | |||
Comparison of Two Combined Therapeutic Methods for Treatment of Lateral Epicondylitis: A Randomized Clinical Trial [NCT00554476] | Phase 4 | 50 participants | Interventional | 2003-01-31 | Terminated(stopped due to Because the sample volume was completed during three years.) | ||
Phase 1/2 Trial of Indomethacin in Chronic Pancreatitis (The PAIR Trial) [NCT04207060] | Phase 2 | 29 participants (Actual) | Interventional | 2020-07-15 | Completed | ||
A Randomised Controlled Trial Comparing Ibuprofen And Indomethacin For The Treatment Of The Patent Ductus Arteriosus In Very Premature Infants [NCT00470743] | Phase 4 | 0 participants (Actual) | Interventional | 2007-05-31 | Withdrawn(stopped due to Funding withdrawn) | ||
The Influence of Cerebral Blood Flow and PETCO2 on Neuromuscular Function During Passive Heat Stress [NCT01848665] | Phase 4 | 8 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
A Two-Cohort Randomized Phase 2 Trial of the IRX-2 Regimen in Women With Squamous Cervical Intraepithelial Neoplasia 3 (CIN 3) or Vulvar Intraepithelial Neoplasia 3 (VIN 3) [NCT03267680] | Phase 2 | 11 participants (Actual) | Interventional | 2017-11-08 | Active, not recruiting | ||
Pharmacokinetics and Pharmacodynamics of Indomethacin Used for PDA Treatment in Extremely Preterm Neonates <27 Weeks Gestational Age [NCT04025177] | Phase 2 | 0 participants (Actual) | Interventional | 2020-01-31 | Withdrawn(stopped due to Halted due to feasibility issues) | ||
A Phase 2, Randomized, Double-Blind, Single-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Indomethacin Test Capsules for the Treatment of Pain After Surgical Removal of Impacted Third Molars [NCT00964431] | Phase 2 | 203 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
A Double-blinded Randomized Controlled Trial With Indomethacin Versus Placebo in Women With Preterm Premature Rupture of Membranes (PPROM) Between 24 and 32 Weeks Gestation [NCT00466128] | Phase 2 | 116 participants (Anticipated) | Interventional | 2007-04-30 | Recruiting | ||
Effect of Indomethacin on Reaction Time, Postural Balance and the Ability to Avoid Suddenly Appearing Obstacles During Gait in Healthy Middle-aged Individuals. [NCT00462111] | Phase 4 | 20 participants (Anticipated) | Interventional | 2007-04-30 | Completed | ||
Comparison of Intravenous Ibuprofen vs. Continuous Indomethacin in the Treatment of Patent Ductus Arteriosus [NCT00485160] | Phase 3 | 70 participants (Anticipated) | Interventional | 2002-02-28 | Completed | ||
Oral Resveratrol Before ERCP Redused Overall Pancreatitis in Patients Undergoing Endoscopic Retrograde Cholangiopancreatography (ERCP): A Multi-center, Single-blinded, Randomized Controlled Trial [NCT02947932] | Phase 4 | 2,700 participants (Anticipated) | Interventional | 2016-12-31 | Not yet recruiting | ||
Phase I-II Study of Fluorouracil in Combination With Phenylbutyrate, Indomethacin and Recombinant Human Interferon-Gamma in Advanced Colorectal Cancer [NCT00002796] | Phase 1/Phase 2 | 46 participants (Actual) | Interventional | 1997-05-31 | Terminated(stopped due to Administratively complete.) | ||
Use of Zinc Carnosine on Intestinal Permeability in Healthy Volunteers Taking Non-steroidal Anti-inflammatory Drugs (NSAIDs) [NCT00149149] | Phase 1 | 10 participants (Actual) | Interventional | 2005-05-01 | Completed | ||
New Management Strategy of PDA for VLBW Preterm--Comparison of Indomethacin and Ibuprofen [NCT00239512] | 60 participants | Interventional | 2005-03-31 | Terminated | |||
Assessment of Analgesic Efficacy of Intranasal Desmopressin in the Treatment of Acute Pain in Patients With Renal Colic [NCT01742689] | Phase 3 | 88 participants (Anticipated) | Interventional | 2012-03-31 | Recruiting | ||
Preoperative Treatment With NSAID in Colorectal Cancer Patients in Relationship to Tumor Host Reactions [NCT00473980] | Phase 4 | 28 participants (Actual) | Interventional | 1998-12-31 | Completed | ||
Etude de la Reserve Vasomotrice Microcirculatoire cutanée [NCT00152724] | 85 participants (Actual) | Observational | 1996-01-31 | Completed | |||
A Prospective, Multicenter, Randomized, Double-blind Controlled Study to Determine Whether a Single Dose of Intraduodenal Indomethacin Can Decrease the Incidence and Severity of Post-ERCP Pancreatitis [NCT00727740] | 117 participants (Actual) | Interventional | 2005-08-31 | Completed | |||
Trial of Indomethacin Prophylaxis in Preterm Infants (TIPP) [NCT00009646] | Phase 3 | 1,202 participants (Actual) | Interventional | 1993-11-30 | Completed | ||
[NCT00116623] | Phase 4 | 0 participants | Interventional | 2003-02-28 | Terminated(stopped due to Funding completed) | ||
[NCT00000494] | Phase 3 | 0 participants | Interventional | 1978-09-30 | Completed | ||
Effect Observation Study of COX-2 Inhibitor to Prevent Post-ERCP Pancreatitis [NCT02964403] | Phase 4 | 2,700 participants (Anticipated) | Interventional | 2016-12-31 | Not yet recruiting | ||
Effects of Indomethacin on Retinal and Choroidal Blood Flow in Healthy Volunteers [NCT00275730] | 12 participants | Interventional | 2006-01-31 | Completed | |||
Rectal Indomethacin Versus Rectal Indomethacin and Sublingual Nitrate to Prevent Post-ERCP Pancreatitis: a Multicentre, Non-inferiority, Double-blind, Randomised Trial [NCT04425993] | 2,700 participants (Actual) | Interventional | 2020-07-01 | Active, not recruiting | |||
Comparison of 2 Different Indomethacin Dosing Protocols to Treat Infants Delivered at <28 Weeks Gestation With a Persistent Patent Ductus Arteriosus [NCT00187447] | Phase 2 | 100 participants (Anticipated) | Interventional | 2003-08-31 | Completed | ||
Effect of Continuous Administration of Different Therapeutic Dosages of Indomethacin and Etoricoxib in the Management of Axial Spondyloarthritis: A Randomized Controlled Trial [NCT03582332] | Phase 4 | 64 participants (Actual) | Interventional | 2016-01-02 | Completed | ||
Vaginal Indomethacin Versus Oral Nifedipine for Preterm Labor; a Randomized Controlled Trial [NCT04404686] | Phase 2/Phase 3 | 300 participants (Anticipated) | Interventional | 2020-10-31 | Not yet recruiting | ||
Indocin Versus Nifedipine for Preterm Labor Tocolysis - A Randomized Double-Blinded Clinical Trial [NCT00486824] | Phase 1/Phase 2 | 29 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Rectal Indomethacin in the Prevention of Post-ERCP Pancreatitis in High Risk Patients: Searching for the Optimal Dose. A Prospective, Randomized Trial [NCT01912716] | Phase 2/Phase 3 | 1,037 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
Efficacy of Rectal Indomethacin in Prevention of Post-pancreatectomy Acute Pancreatitis-A Randomized Controlled Trial [NCT05722548] | Phase 2 | 200 participants (Anticipated) | Interventional | 2023-02-01 | Not yet recruiting | ||
The Effect on Knee Joint Loads of Instruction in Analgesic Use Compared With NEUROMUSCULAR Exercise in Patients With Knee Osteoarthritis - A Single Blind RCT [NCT01638962] | 93 participants (Actual) | Interventional | 2012-08-31 | Completed | |||
Phase I Study Evaluating Indomethacin in Combination With Platinum-based Chemotherapy [NCT01719926] | Phase 1 | 13 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
Electrophilic Fatty Acid Derivatives in Asthma [NCT01733485] | Phase 1 | 50 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
Indomethacin Prophylaxis for Heterotopic Ossification After Surgical Treatment of Elbow Trauma: A Randomized Prospective Double-blinded Study. [NCT01744314] | 150 participants (Anticipated) | Interventional | 2012-11-30 | Recruiting | |||
Comparison of Nifedipine Versus Indomethacin for Acute Preterm Labor [NCT03129945] | 36 participants (Actual) | Interventional | 2017-01-17 | Completed | |||
Rectal Indomethacin to Prevent Post-ERCP Pancreatitis [NCT01774604] | Phase 3 | 449 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to Futility) | ||
TUMOR INFILTRATING LYMPHOCYTE THERAPY FOR ADVANCED MELANOMA USING IMMUNOMODULATION, A PHASE II STUDY [NCT00002535] | Phase 2 | 0 participants | Interventional | 1993-07-31 | Completed | ||
A Randomized Trial of Rectal Indomethacin and Papillary Spray of Epinephrine Versus Rectal Indomethacin to Prevent Post-ERCP Pancreatitis in High Risk Patients [NCT02116309] | 948 participants (Actual) | Interventional | 2014-08-31 | Completed | |||
Randomized Indomethacin Germinal Matrix Hemorrhage/Intraventricular Hemorrhage (GMH/IVH) Prevention Trial [NCT00033917] | Phase 3 | 630 participants (Actual) | Interventional | 1989-09-30 | Completed | ||
Effect of Papillary Epinephrine Spraying on Post-ERCP Pancreatitis in Patients Received Rectal Indomethacin: A Multi-center, Double-blind, Randomized Controlled Trial [NCT03057769] | 3,300 participants (Actual) | Interventional | 2017-02-01 | Terminated(stopped due to This study was terminated because of an interim analysis suggesting futility of papillary epinephrine spraying in PEP prevention.) | |||
The Influence of Cerebral Blood Flow and Alkalosis on Neuromuscular Function During Environmental Stress [NCT01830335] | Phase 4 | 8 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
Evaluation of the Utility of Indomethacin as Support Treatment in Women With Preterm Labor With Intact Membranes and High Risk of Intraamniotic Inflammation [NCT01577121] | Phase 2 | 16 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
Effects of Saccharomyces Boulardii CNCM I-745 on Intestinal Barrier Function [NCT05538247] | Early Phase 1 | 56 participants (Anticipated) | Interventional | 2023-04-13 | Recruiting | ||
A Randomized Controlled Pilot Trial of Indomethacin in Acute Pancreatitis [NCT02692391] | Phase 3 | 42 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
Efficacy of Rectal Indomethacin in Prevention of Post-operative Pancreatitis After Pancreaticoduodenectomy - a Randomized Controlled Trial [NCT05109143] | 44 participants (Actual) | Interventional | 2020-10-17 | Completed | |||
A Prospective, Open Label Randomized Controlled Trial of Prophylactic Rectal Indomethacin Versus Combined Pancreatic Duct Stent Placement and Rectal Indomethacin for Prevention of Post-ERCP Pancreatitis [NCT05857514] | 384 participants (Anticipated) | Interventional | 2023-05-10 | Recruiting | |||
Epinephrine Sprayed on the Papilla and Rectal Indomethacin Versus Sterile Water Sprayed on the Papilla and Rectal Indomethacin for Preventing Pancreatitis After Endoscopic Retrograde Cholangiopancreatography: A Prospective, Randomized, Controlled Trial [NCT02959112] | 548 participants (Actual) | Interventional | 2016-05-31 | Terminated(stopped due to Because previous studies had found no difference, and one recent study even reported a higher incidence of PEP in treatment arm) | |||
An Open-Label, Single-Arm, Phase II Study to Evaluate the Efficacy and Safety of Oral Hydroxychloroquine, Indomethacin and Zithromax in Subjects Positive With SARS-CoV-2 With Mild Symptoms [NCT04344457] | Phase 1/Phase 2 | 80 participants (Anticipated) | Interventional | 2020-04-16 | Recruiting | ||
Prevention of Post-Endoscopic Retrograde Cholangiopancreatography (ERCP) - Induced Pancreatitis Using Aggressive Lactated Ringer's Infusion and/or Rectal Indomethacin [NCT02641561] | Phase 3 | 192 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
Non-Steroidal Anti-inflammatory Drugs in Axial Spondyloarthritis: a Pilot Study [NCT03473665] | Phase 4 | 9 participants (Actual) | Interventional | 2018-03-01 | Terminated(stopped due to Slow recruitment) | ||
A Phase 3, Randomized, Double-Blind, Multiple-Dose, Parallel-Group, Active- and Placebo-Controlled Study of Indomethacin [Test] Capsules for the Treatment of Acute Postoperative Pain After Bunionectomy [NCT01543685] | Phase 3 | 462 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
Pharmacologic Treatment of Congenital Nephrogenic Diabetes Insipidus [NCT00478335] | 4 participants (Actual) | Interventional | 2007-05-31 | Completed | |||
Prospective Randomized Controlled Trial of Combination Ranibizumab and Indomethacin for Exudative Age-Related Macular Degeneration [NCT03261635] | Phase 4 | 58 participants (Actual) | Interventional | 2016-01-07 | Completed | ||
A Phase 3, Randomized, Double-Blind, Multiple-Dose, Parallel-Group, Placebo-Controlled Study of Indomethacin Nanoformulation Capsules for the Treatment of Acute Postoperative Pain After Bunionectomy [NCT01626118] | Phase 3 | 373 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Non-inferiority Trial Comparing Pharmacological Prevention Alone Versus Pancreatic Stents Plus Pharmacological Prevention to Prevent Post-ERCP Pancreatitis [NCT02368795] | 400 participants (Anticipated) | Interventional | 2015-02-28 | Recruiting | |||
Paracetamol And Ibuprofen/Indomethacin in Closing Patent Ductus Arteriosus of Preterm Infants - Randomised, Placebo-controlled Multicentre Trial [NCT03648437] | Phase 1 | 60 participants (Anticipated) | Interventional | 2018-09-03 | Recruiting | ||
A Phase 2, Open-label Trial of the Safety and Biological Effect of Subcutaneous IRX-2 (With Cyclophosphamide, Indomethacin, and Zinc) in Patients With Resectable Cancer of the Head and Neck [NCT00210470] | Phase 2 | 27 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
A Randomized, Balanced, Open Label, Two Treatment, Two Period, Two Sequence, Single Dose, Crossover, Bioequivalence Study of Indomethacin Extended-Release Capsules 75 mg of Ipca Laboratories Ltd., With Indomethacin Extended-Release Capsules USP 75 mg of E [NCT01722110] | Phase 1 | 32 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
Vitreous pge2 Level Changes After Topical Administration of Diclofenac 0.1%, Nepafenac 0.3%, Indomethacin 0.5% and Bromfenac 0.09% in Vitrectomy Patients [NCT03597867] | Phase 3 | 104 participants (Actual) | Interventional | 2018-04-25 | Completed | ||
A Prospective, Randomized, Controlled Trial of Rectal Indomethacin in the Prevention of Post-ERCP Pancreatitis in High Risk Patients. [NCT00820612] | Phase 4 | 602 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to Stopped by DSMB for overwhelming benefit of indomethacin (unethical to withhold indomethacin from patients)) | ||
A Phase 0 Platform Study Exploring the Use of Challenge Agents in Healthy Volunteers [NCT04821323] | Early Phase 1 | 10 participants (Actual) | Interventional | 2021-03-10 | Completed | ||
Indomethacin and Delayed Umbilical Cord Clamp for Preterm Infant IVH [NCT02221219] | Phase 1/Phase 2 | 256 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
Randomized, Placebo Controlled Trial of Indomethacin for Tocolysis [NCT01869361] | Early Phase 1 | 0 participants (Actual) | Interventional | 2020-08-01 | Withdrawn(stopped due to Due to much lower than expected numbers of eligible patients and lack of PI time, the study was not started.) | ||
Nifedipine Alone or Nifedipine Plus Indomethacin for Treatment of Acute Preterm Labor: An Open Label, Randomized Comparative Effectiveness Controlled Trial [NCT02438371] | Phase 4 | 49 participants (Actual) | Interventional | 2015-05-31 | Terminated(stopped due to Study halted due to slow recruitment) | ||
A Clinical Study to Assess the Efficacy of Pain Relief of Topical Indomethacin Patch Over Placebo in Ankle Sprain Patients [NCT01957215] | Phase 4 | 270 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |