Page last updated: 2024-12-05

tolmetin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug. [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]

Cross-References

ID SourceID
PubMed CID5509
CHEMBL ID1020
CHEBI ID71941
SCHEMBL ID3150
MeSH IDM0021631

Synonyms (114)

Synonym
BIDD:GT0468
tolmetina [dcit]
tolectin
1-methyl-5-(4-methylbenzoyl)-1h-pyrrole-2-acetic acid
brn 0485305
tolmetine
mcn-2559
tolmetine [inn-french]
tolmetinum [inn-latin]
mcn 2559
einecs 247-497-2
acido 1-metil-5-(p-tolnil)-pirrol-2-acetico [spanish]
hsdb 3403
pyrrole-2-acetic acid, 1-methyl-5-p-toluoyl-
tolmetino [inn-spanish]
chebi:71941 ,
CHEMBL1020 ,
BRD-K82562631-236-02-0
BRD-K82562631-325-03-9
1h-pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-
KBIO1_000213
DIVK1C_000213
SPECTRUM_000935
PRESTWICK3_000856
BPBIO1_000959
OPREA1_869397
SPECTRUM5_001194
26171-23-3
tolmetin
C07149
1-methyl-5-(4-methylbenzoyl)-pyrrole-2-acetic acid
DB00500
5-(p-toluoyl)-1-methylpyrrole-2-acetic acid
1-methyl-5-p-toluoylpyrrole-2-acetic acid
tolmetin (usan/inn)
D02355
BSPBIO_002106
KBIO2_001415
KBIO2_003983
KBIOGR_000797
KBIOSS_001415
KBIO2_006551
KBIO3_001606
SPECTRUM4_000359
SPBIO_000990
PRESTWICK1_000856
PRESTWICK0_000856
SPECTRUM2_001205
SPECTRUM3_000603
NINDS_000213
SPBIO_002792
BSPBIO_000871
PRESTWICK2_000856
IDI1_000213
HMS2090D06
[1-methyl-5-(4-methyl-benzoyl)-1h-pyrrol-2-yl]-acetic acid(tolmetin)
2-(1-methyl-5-(4-methylbenzoyl)-1h-pyrrol-2-yl)acetic acid
[1-methyl-5-(4-methyl-benzoyl)-1h-pyrrol-2-yl]-acetic acid
bdbm50295287
2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetic acid
tlt ,
A818238
[1-methyl-5-(4-methylbenzoyl)-1h-pyrrol-2-yl]acetic acid
tolmetino
tolmetin [usan:inn:ban]
d8k2jpn18b ,
tolmetina
5-22-06-00392 (beilstein handbook reference)
acido 1-metil-5-(p-tolnil)-pirrol-2-acetico
tolmetinum
unii-d8k2jpn18b
FT-0649942
tolmetin [mi]
tolmetin [usan]
tolmetin [jan]
tolmetin [hsdb]
tolmetin [vandf]
tolmetin [who-dd]
tolmetin [inn]
AKOS015850645
S4832
gtpl7311
2-[1-methyl-5-(4-methylbenzoyl)-1h-pyrrol-2-yl]acetic acid
SCHEMBL3150
DTXSID2043951 ,
1-methyl-5-p-toluoyl-pyrrole-2-acetic acid
1-methyl-5-(4-methylbenzoyl)pyrrole-2-acetic acid
1-methyl- 5-(p-toluoyl)pyrrole-2-acetic acid
[1-methyl-5-(4-methylbenzoyl)-1h-pyrrol-2-yl]acetic acid #
2-{1-methyl-5-[(4-methylphenyl)carbonyl]-1h-pyrrol-2-yl}acetic acid
mfcd00599595
CS-W008734
GS-6529
J-504975
SBI-0051537.P002
FT-0675272
Q3992411
BCP09085
HMS3886I03
CCG-267033
SB63879
1-methyl-5-p-toluoylpyrrole-2-aceticacid
F6782-4251
NCGC00094796-03
HY-B1799
EN300-6482019
Z1741975772
(1-methyl-5-(4-methylbenzoyl)-1h-pyrrol-2-yl)acetic acid
m02aa21
tolmetino (inn-spanish)
m01ab03
tolmetinum (inn-latin)
tolmetine (inn-french)
dtxcid0023951

Research Excerpts

Overview

Tolmetin is a nonsteroidal anti-inflammatory drug (NSAID) that reduces adhesion formation in several animal models after a single intraperitoneal (i.p.) dose delivered at the time of surgery.

ExcerptReferenceRelevance
"Tolmetin, which is an antiinflammatory agent with a short half-life, can provide adequate, safe therapy in the geriatric population."( Long-term efficacy and safety of tolmetin sodium in treatment of geriatric patients with rheumatoid arthritis and osteoarthritis: a retrospective study.
O'Brien, WM, 1983
)
1.27
"Tolmetin is a nonsteroidal anti-inflammatory drug (NSAID) that reduces adhesion formation in several animal models after a single intraperitoneal (i.p.) dose delivered at the time of surgery. "( Time-dependent effect of tolmetin sodium in a rabbit uterine adhesion model.
Dizerega, GS; Huang, WJ; Johns, DB; Rodgers, KE; Wiseman, DM,
)
1.88

Effects

ExcerptReferenceRelevance
"Tolmetin sodium has been investigated and determined from dosage forms as its Cu(II) complex and method optimized by statistical optimization. "( Statistical optimization applied to the spectrophotometric study of a tolmetin-copper(II) complex.
Agatonović-Kustrin, S; Pećanac, D; Radulović, D; Vasiljević, M; Zivanović, L, 1991
)
1.96

Actions

Tolmetin was shown to increase the number of RBC at one postoperative time point in rabbits, but not in rats. Tolmetin seems to cause an allosteric change in the diazepam binding site in spite of it sharing a primary site with warfarin.

ExcerptReferenceRelevance
"Tolmetin was shown to increase the number of RBC at one postoperative time point in rabbits, but not in rats."( Modulation of postsurgical cell infiltration and fibrinolytic activity by tolmetin in two species.
diZerega, GS; Ellefson, DD; Girgis, W; Rodgers, KE, 1994
)
1.24
"Tolmetin-zinc promotes gain in breaking strength, not by increasing the collagen content, but by favouring better maturation of available collagen at the wound site."( Comparative evaluation of tolmetin & tolmetin-zinc on wound-repair & inflammation.
Bairy, KL; Kulkarni, DR; Ramesh, KV; Rao, CM, 1990
)
1.3
"Tolmetin seems to cause an allosteric change in the diazepam binding site in spite of it sharing a primary site with warfarin."( The effects of pH, calcium and chloride ions on the binding of tolmetin to human serum albumin: circular dichroic, dialysis and fluorometric measurements.
Matsuyama, K; Perrin, JH; Sen, AC, 1987
)
1.23

Treatment

In amtolmetin guacyl-treated rats, 1400W decreased gastric mucosal blood flow, whereas it was inactive in vehicle- and tolmetin-treated animals. Tolmetin treatment significantly reduced the levels of prostaglandin E2 and polymorphonuclear leukocytes.

ExcerptReferenceRelevance
"In amtolmetin guacyl-treated rats, 1400W decreased gastric mucosal blood flow, whereas it was inactive in vehicle- and tolmetin-treated animals."( Gastroprotective effects of amtolmetin guacyl: a new non-steroidal anti-inflammatory drug that activates inducible gastric nitric oxide synthase.
Cavestro, GM; Coppelli, G; Coruzzi, G; Lo Giudice, P; Okolicsanyi, L; Pisano, C; Spaggiari, S; Tepperman, BL, 2002
)
1.06
"Tolmetin treatment significantly reduced the levels of prostaglandin E2, polymorphonuclear leukocytes and protein concentration in aqueous samples obtained from the eyes treated with arachidonate."( Pharmacological evaluation of anti-inflammatory pyrrole-acetic acid derivative eye drops.
Bucolo, C; Spadaro, A, 1997
)
1.02

Toxicity

ExcerptReferenceRelevance
" Significantly fewer patients treated with ketorolac reported adverse events in comparison with those treated with meperidine (17% and 59%, respectively), which suggests that it possesses a better therapeutic index than meperidine."( Comparison of the efficacy and safety of ketorolac and meperidine in the relief of dental pain.
Angelocci, D; Bynum, L; Fox, K; Fricke, JR; McHugh, D; Yee, JP, 1992
)
0.28
" Ketorolac was well tolerated, with rates of adverse events generally lower than those of the opiate comparators."( Analgesic efficacy and safety of single-dose oral and intramuscular ketorolac tromethamine for postoperative pain.
Brown, CR; Bynum, LJ; Clarke, PJ; Dickie, G; Evans, SA; Moodie, JE; Smith, BA; Wild, VM, 1990
)
0.28
" Three patients (one on ketorolac, two on Doleron) withdrew because of adverse events (vomiting)."( Analgesic efficacy and safety comparison of ketorolac tromethamine and Doleron for the alleviation of orthopaedic post-operative pain.
Johansson, S; Josefsson, G; Lindstrand, A; Malstam, J; Stenstroem, A,
)
0.13
" Tolmetin was also found to be safe and well tolerated by the elderly patient population."( Long-term efficacy and safety of tolmetin sodium in treatment of geriatric patients with rheumatoid arthritis and osteoarthritis: a retrospective study.
O'Brien, WM, 1983
)
1.46
" It was found that compounds with polar substituents at the 2 or 3 position of the ring system are less acutely toxic while maintaining antiinflammatory activity."( Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles.
Ariyan, ZS; Fogt, SW; Heilman, RD; Matthews, RJ; Powers, LJ; Rippin, DJ, 1981
)
0.26
" In this long-term safety study, patients treated with zomepirac had significantly fewer adverse reactions and fewer limiting adverse reactions than did patients treated with aspirin."( Long-term safety of zomepirac: a double-blind comparison with aspirin in patients with osteoarthritis.
Andelman, SY; Cannella, JJ; Ruoff, GE,
)
0.13
" The safety profile was also studied by recording all adverse events noted."( Single-blind comparative analgesic and safety study of single doses of intramuscularly administered ketorolac tromethamine and pethidine hydrochloride in patients with pain following orthopaedic surgery.
Chhatwal, V; Kumar, VP; Lai, FO; Pereira, BP; Satku, K, 1994
)
0.29
"The end points analyzed were adverse effects, duration of postoperative ileus, degree of pain control, length of hospitalization, and development of postoperative confusion as measured on serial MMSEs."( Does patient-controlled analgesia achieve better control of pain and fewer adverse effects than intramuscular analgesia? A prospective randomized trial.
Avecilla, CS; Berg, RL; Nitschke, LF; Schlösser, CT; Selthafner, JV; Wengert, TJ, 1996
)
0.29
"Only two patients, both in the PCA group, reported adverse effects; neither required a change in analgesia group."( Does patient-controlled analgesia achieve better control of pain and fewer adverse effects than intramuscular analgesia? A prospective randomized trial.
Avecilla, CS; Berg, RL; Nitschke, LF; Schlösser, CT; Selthafner, JV; Wengert, TJ, 1996
)
0.29
" Most patients should probably be managed with PCA narcotics, but the addition of ketorolac might reduce narcotic dose and resultant adverse effects."( Does patient-controlled analgesia achieve better control of pain and fewer adverse effects than intramuscular analgesia? A prospective randomized trial.
Avecilla, CS; Berg, RL; Nitschke, LF; Schlösser, CT; Selthafner, JV; Wengert, TJ, 1996
)
0.29
"Ketorolac proved safe for short-term intravenous use in children more than 1 year of age when patients with known contraindications to the use of non-steroidal antiinflammatory drugs were excluded."( Safety of intravenous ketorolac therapy in children and cost savings with a unit dosing system.
Berde, CB; Houck, CS; McDermott, JS; Sethna, NF; Wilder, RT, 1996
)
0.29
" In general, the adverse events associated with ketorolac are similar to other NSAIDs."( Side effects of NSAIDs and dosing recommendations for ketorolac.
Camu, F; Lauwers, MH; Vanlersberghe, C, 1996
)
0.29
"Levels of sedation, pain intensity, pain relief, and adverse events were recorded at baseline, at 2, 4, and 6 hours, and at termination."( Evaluation of the safety and efficacy of ketorolac versus morphine by patient-controlled analgesia for postoperative pain.
Bynum, L; Fanciullo, G; Hubbard, L; Maneatis, T; O'Hara, DA; Seuffert, P; Shefrin, A,
)
0.13
" No treatment-related adverse events were reported in the ketorolac group, and only one treatment-related adverse event was reported in the vehicle group."( Analgesic efficacy and safety of nonpreserved ketorolac tromethamine ophthalmic solution following radial keratotomy. Ketorolac Radial Keratotomy Study Group.
Yee, RW, 1998
)
0.3
"5% ophthalmic solution was significantly more effective than, and as safe as, vehicle in the treatment of postoperative pain associated with radial keratotomy."( Analgesic efficacy and safety of nonpreserved ketorolac tromethamine ophthalmic solution following radial keratotomy. Ketorolac Radial Keratotomy Study Group.
Yee, RW, 1998
)
0.3
" Patients treated with ketorolac experienced the same low rate of treatment-related adverse events as those treated with the vehicle and exhibited the same improvement in visual acuity and manifest refraction."( Efficacy and safety of nonpreserved ketorolac ophthalmic solution in postoperative ocular pain following radial keratotomy.
Abel, ML; Brint, SF; Cheetham, JK; DeGryse, R; Rosenthal, A; Thompson, VM, 1999
)
0.3
"5% ophthalmic solution was significantly more effective than, and as safe as, the vehicle in alleviating the postoperative pain associated with RK."( Efficacy and safety of nonpreserved ketorolac ophthalmic solution in postoperative ocular pain following radial keratotomy.
Abel, ML; Brint, SF; Cheetham, JK; DeGryse, R; Rosenthal, A; Thompson, VM, 1999
)
0.3
" No adverse events were reported, and there were no significant changes in intraocular pressure in either group."( Comparison of the efficacy and safety of ketorolac tromethamine 0.5% and prednisolone acetate 1% after cataract surgery.
Jenkins, JE; Pendelton, RA; Simone, JN, 1999
)
0.3
" Adverse symptoms were acceptable with both drugs."( A double-blind evaluation of the analgesic efficacy and toxicity of oral ketorolac and diclofenac in cancer pain. The TD/10 recordati Protocol Study Group.
Camaggi, CM; Pannuti, F; Robustelli della Cuna, G; Strocchi, E; Ventaffrida, V,
)
0.13
" To ensure participant safety, biomicroscopy, ophthalmoscopy, intraocular pressure, adverse events, and preoperative and postoperative visual acuity and refractive error were also monitored."( Efficacy and safety profile of ketorolac 0.5% ophthalmic solution in the prevention of surgically induced miosis during cataract surgery.
Cheetham, JK; Grosserode, R; Rosenthal, A; Stewart, R, 1999
)
0.3
"Both COX inhibitors were toxic to dams in the highest doses evaluated, which caused a significantly greater incidence of intrauterine growth retardation and developmental variations."( Developmental toxicity evaluation of ibuprofen and tolmetin administered in triple daily doses to Wistar CRL:(WI)WUBR rats.
Burdan, F, 2004
)
0.58
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" However, this group of drugs is associated with serious adverse drug reactions."( Differential involvement of mitochondrial dysfunction, cytochrome P450 activity, and active transport in the toxicity of structurally related NSAIDs.
Unlü, B; van Leeuwen, JS; Vermeulen, NP; Vos, JC, 2012
)
0.38
" Clearly, longer acyl glucuronide half-lives were observed for safe drugs compared to drugs that can cause IDT."( Toxicity of Carboxylic Acid-Containing Drugs: The Role of Acyl Migration and CoA Conjugation Investigated.
Aatsinki, SM; Hokkanen, J; Lassila, T; Mattila, S; Tolonen, A; Turpeinen, M, 2015
)
0.42

Pharmacokinetics

Tolmetin half-life significantly prolonged in females compared with males. Plasma concentration-time data in man after oral dosing of the nonsteroidal antiinflammatory agent, tolmetin sodium.

ExcerptReferenceRelevance
"Plasma concentration-time data in man after oral dosing of the nonsteroidal antiinflammatory agent, tolmetin sodium, were fitted to both linear and nonlinear pharmacokinetic equations."( Linear and nonlinear assessment of tolmetin pharmacokinetics.
Ayres, JW; Sakmar, E; Wagner, JG; Weidler, DJ, 1977
)
0.75
" The absorption of ketorolac is rapid, Cmax being attained between 20 to 60 min."( Clinical pharmacokinetics of ketorolac tromethamine.
Brocks, DR; Jamali, F, 1992
)
0.28
" Values of steady-state volume of distribution and plasma clearance were approximately two times higher than those in adults but values of elimination half-life were similar."( The pharmacokinetics of postoperative intravenous ketorolac tromethamine in children.
Maunuksela, EL; Olkkola, KT, 1991
)
0.28
" Ketorolac did not alter the pharmacodynamic profile of racemic warfarin."( Investigations into the potential effects of multiple dose ketorolac on the pharmacokinetics and pharmacodynamics of racemic warfarin.
Aarons, L; Bullingham, R; Holt, BL; Mullins, FG; Rowland, M; Toon, S, 1990
)
0.28
" The elimination of ketorolac was decreased slightly in the elderly following both doses, as evidenced by a prolongation in half-life (4."( Pharmacokinetics of single-dose oral and intramuscular ketorolac tromethamine in the young and elderly.
Garg, DC; Jallad, NS; Martinez, JJ; Mroszczak, EJ; Weidler, DJ, 1990
)
0.28
" The rate of absorption of K and formation of PHK, as determined by Cmax and Tmax values, was significantly slower following the im doses."( Pharmacokinetics of ketorolac and p-hydroxyketorolac following oral and intramuscular administration of ketorolac tromethamine.
Bynum, L; Jung, D; Ling, TL; Mroszczak, EJ; Sevelius, H; Wu, A, 1989
)
0.28
"The relationship between the pharmacokinetic properties and the analgesic effect of ketorolac was evaluated with the pain-induced functional impairment model in the rat."( Relationship between pharmacokinetics and the analgesic effect of ketorolac in the rat.
Flores-Murrieta, FJ; Granados-Soto, V; Hong, E; López-Muñoz, FJ, 1995
)
0.29
" Pharmacokinetic parameters were derived from plasma samples collected after the first and last active doses."( Tolerability, central effects and pharmacokinetics of intravenous ketorolac tromethamine in volunteers.
Bullingham, R; Hooftman, L; Lloyd, J; Lucker, P; Mroszczak, E, 1994
)
0.29
"A pharmacokinetic study has been performed on a new non-steroidal anti-inflammatory drug, AU-8001 (4'-acetamidophenyl-2-(5'-p-toluyl-1'-methylpyrrole)acetate, CAS 82239-77-8) in the rat, following intravenous (10 mg/kg) and oral (50 mg/kg) administrations."( Pharmacokinetic study of 4'-acetamidophenyl-2-(5'-p-toluyl-1'-methylpyrrole)acetate in the rat.
Domenéch, J; Obach, R; Sabater, J, 1993
)
0.29
" Pharmacokinetic data was available for 85 subjects."( Population pharmacodynamic model for ketorolac analgesia.
Mandema, JW; Stanski, DR, 1996
)
0.29
"The pharmacokinetic data was best described by a two-compartment model with first-order absorption."( Population pharmacodynamic model for ketorolac analgesia.
Mandema, JW; Stanski, DR, 1996
)
0.29
" Pharmacokinetic values were estimated by a nonlinear computer program."( Pharmacokinetics of ketorolac in children after abdominal surgery.
González-Martin, G; González-Sotomayor, J; Maggio, L; Zuniga, S, 1997
)
0.3
"5 mg/kg), and racemic KT (5 mg/kg) were administered orally to male Sprague-Dawley rats and plasma samples were collected for 6 h post-dose for pharmacokinetic assessments."( Stereospecific pharmacokinetics and toxicodynamics of ketorolac after oral administration of the racemate and optically pure enantiomers to the rat.
Aberg, G; Corrigan, BW; Davies, NM; Jamali, F; Lovlin, R, 1999
)
0.3
" Pharmacokinetic (PK) and pharmacodynamic (PD) data were simultaneously fitted using nonlinear mixed effects modeling (NONMEM) to the one-compartment model and indirect response model."( Pharmacokinetic-pharmacodynamic modeling of tolmetin antinociceptive effect in the rat using an indirect response model: a population approach.
Castañeda-Hernández, G; Flores-Acevedo, DM; Flores-Murrieta, FJ; Jusko, WJ; Ko, HC; López-Muñoz, FJ; Sale, ME, 1998
)
0.56
" Plasma pharmacokinetic parameters for racemic drug and both enantiomers were determined for each patient."( Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children.
Aravind, MK; Kauffman, RE; Lieh-Lai, MW; Uy, HG, 1999
)
0.3
" Terminal half-life of S(-)-ketorolac was 40% that of the R(+) enantiomer, and the apparent volume of distribution of the S(-) enantiomer was greater than that of the R(+) form."( Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children.
Aravind, MK; Kauffman, RE; Lieh-Lai, MW; Uy, HG, 1999
)
0.3
" Because of the greater clearance and shorter half-life of S(-)-ketorolac, pharmacokinetic predictions based on racemic assays may overestimate the duration of pharmacologic effect."( Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children.
Aravind, MK; Kauffman, RE; Lieh-Lai, MW; Uy, HG, 1999
)
0.3
" Notwithstanding, tolmetin half-life was significantly prolonged in females compared with males."( Influence of sex on the pharmacokinetics of tolmetin in the rat.
Flores-Murrieta, FJ; Jiménez, M; Pérez-Urizar, J, 1999
)
0.9
" 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
" 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

Compound-Compound Interactions

ExcerptReferenceRelevance
"To examine the efficacy of intramuscular (IM) ketorolac used in combination with intravenous (IV) patient-controlled analgesia (PCA) morphine for postoperative pain relief following intra-abdominal gynecologic surgery."( The efficacy of intramuscular ketorolac in combination with intravenous PCA morphine for postoperative pain relief.
Brull, SJ; Ning, T; Paige, D; Sevarino, FB; Silverman, DG; Sinatra, RS,
)
0.13
"Propacetamol and ketorolac, combined with patient-controlled analgesia morphine, show similar analgesic efficacy after gynecologic surgery."( A double-blinded evaluation of propacetamol versus ketorolac in combination with patient-controlled analgesia morphine: analgesic efficacy and tolerability after gynecologic surgery.
Agrò, F; Aloe, L; Ballabio, M; De Cillis, P; De Nicola, A; Giunta, F; Ischia, S; Marinangeli, F; Stefanini, S; Varrassi, G, 1999
)
0.3

Bioavailability

ExcerptReferenceRelevance
" The bioavailability was 96."( Pharmacokinetic study of tolmetin in the rat.
Domenéch, J; Obach, R; Sabater, J, 1992
)
0.59
" Its oral bioavailability is estimated to range from 80 to 100%."( Clinical pharmacokinetics of ketorolac tromethamine.
Brocks, DR; Jamali, F, 1992
)
0.28
" Simultaneously fittings (intravenous and oral curves showed significant statistical differences for bioavailability estimated parameters (AUCev, F and K01)."( Reduction of oral bioavailability of paracetamol by tolmetin in rat.
Domenech, J; Moreno, J; Obach, R; Peraire, C; Sabater, J, 1991
)
0.53
" Ketorolac is well absorbed and has a rapid onset of action."( Ketorolac: a parenteral nonsteroidal antiinflammatory drug.
Resman-Targoff, BH, 1990
)
0.28
" The rate of absorption of K and formation of PHK, as determined by Cmax and Tmax values, was significantly slower following the im doses."( Pharmacokinetics of ketorolac and p-hydroxyketorolac following oral and intramuscular administration of ketorolac tromethamine.
Bynum, L; Jung, D; Ling, TL; Mroszczak, EJ; Sevelius, H; Wu, A, 1989
)
0.28
"9 h, respectively) and the systemic bioavailability was essentially complete."( Pharmacokinetics of ketorolac tromethamine in humans after intravenous, intramuscular and oral administration.
Bynum, L; Jung, D; Mroszczak, E, 1988
)
0.27
" Assessment of Z's absolute bioavailability in monkeys (10 mg/kg, iv vs."( The metabolism of zomepirac sodium. I. Disposition in laboratory animals and man.
Grindel, JM; McKown, LA; Migdalof, BH; O'Neill, PJ; Schwartz, MH; Wu, WN; Yorgey, KA,
)
0.13
" After a single topical application of tolmetin gel to the shaved backs of rats, tolmetin was well absorbed percutaneously into the non-inflamed dorsal muscle."( Tolmetin uptake into inflamed tissue in the rat.
Chasseaud, LF; John, BA; Wood, SG, 1983
)
1.98
" The bioavailability of zomepirac was unaffected by single or repeated doses of antacid."( Review of the pharmacokinetics and metabolism of zomepirac in man and animals.
Grindel, JM; Muschek, LD, 1980
)
0.26
" The drug is well absorbed when given orally."( Evaluation of zomepirac sodium.
McEvoy, GK, 1981
)
0.26
" Bioavailability of zomepirac from the 3 dosage forms was much the same."( Zomepirac kinetics in healthy males.
Gottlieb, S; Nayak, RK; Ng, KT; Plostnieks, J, 1980
)
0.26
" The systemic bioavailability of ketorolac acid from three transdermal formulations was evaluated in nine healthy subjects in a randomized three-way crossover fashion."( Absorption of transdermally delivered ketorolac acid in humans.
Combs, D; Manoukian, E; Roy, SD, 1995
)
0.29
"The bioavailability of ketorolac after administration of two oral formulations containing 10 mg of ketorolac tromethamine, Exodol and Dolac, to 12 healthy Mexican volunteers was compared."( Comparative bioavailability of two oral formulations of ketorolac tromethamine: Dolac and Exodol.
Castañeda-Hernández, G; Flores-Murrieta, FJ; Granados-Soto, V; Herrera, JE; Hong, E, 1994
)
0.29
" Ketorolac applied in this way had a bioavailability greater than 80%."( Nasal formulations of ketorolac tromethamine: technological evaluation--bioavailability and tolerability in rabbits.
Bottoni, G; Canali, S; Peano, S; Rivolta, R; Santus, G; Testa, B, 1993
)
0.29
" The bioavailability of the prodrug is incomplete and, according to the urinary excretion data, a fraction of the dose reaches the blood stream in the form of metabolites."( Pharmacokinetic study of 4'-acetamidophenyl-2-(5'-p-toluyl-1'-methylpyrrole)acetate in the rat.
Domenéch, J; Obach, R; Sabater, J, 1993
)
0.29
" The single-dose mean pharmacokinetic characteristics and relative bioavailability of the four different 10 mg ketorolac tromethamine tablets were evaluated in 12 healthy volunteers in a randomized study of Latin square design."( In vivo/in vitro correlations for four differently dissolving ketorolac tablets.
Chowhan, Z; Gordon, MS, 1996
)
0.29
"This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo."( Effect of benzalkonium chloride/EDTA on the ocular bioavailability of ketorolac tromethamine following ocular instillation to normal and de-epithelialized corneas of rabbits.
Madhu, C; Nguyen, TG; Rix, PJ; Shackleton, MJ; Tang-Liu, DD, 1996
)
0.29
" Furthermore, the bioavailability of the mucoadhesive formulation in the aqueous humor against an aqueous-based solution was compared."( Pharmacological evaluation of anti-inflammatory pyrrole-acetic acid derivative eye drops.
Bucolo, C; Spadaro, A, 1997
)
0.3
" Its oral bioavailability is estimated to be 80%."( Microencapsulation of ketorolac tromethamine by means of a coacervation-phase separation technique induced by the addition of non-solvent.
Demirel, M; Genç, L; Güler, E; Hegazy, N,
)
0.13
"To investigate the bioavailability (extent and rate of absorption) of ketorolac from two cutaneous absorption sources, active electrotransport and passive transdermal, and to examine the enantiomeric selectivity of bioavailability for each source."( Passive versus electrotransport-facilitated transdermal absorption of ketorolac.
Gupta, SK; Park, K; Sheiner, LB; Verotta, D, 1998
)
0.3
"Based on a crossover study in 12 healthy volunteers, the extent and rate of absorption of ketorolac, delivered by a patch, were found by estimating the input rate function of the drug."( Passive versus electrotransport-facilitated transdermal absorption of ketorolac.
Gupta, SK; Park, K; Sheiner, LB; Verotta, D, 1998
)
0.3
"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
"It may be concluded that BCRP plays an important role in the intestinal efflux of MED-5 and limits the bioavailability after oral administration of MED-15."( Evaluation of intestinal absorption of amtolmetin guacyl in rats: breast cancer resistant protein as a primary barrier of oral bioavailability.
Li, X; Liu, D; Rong, Z; Xiang, D; Xu, Y; Zhang, C, 2013
)
0.66

Dosage Studied

The effectiveness of tolmetin sodium in the treatment of rheumatoid arthritis was evaluated by: 1) a 12-week, double-blind study with a dosage range of 800-1600 mg daily; and 2) an open 2-year study.

ExcerptRelevanceReference
"The effectiveness of tolmetin sodium in the treatment of rheumatoid arthritis was evaluated by: 1) a 12-week, double-blind study with a dosage range of 800-1600 mg daily; and 2) an open 2-year study with a dosage range of 400-2400 mg daily."( Tolmetin sodium, a new anti-arthritis drug: double-blind and long-term studies.
Cordrey, LJ, 1976
)
2.02
"Plasma concentration-time data in man after oral dosing of the nonsteroidal antiinflammatory agent, tolmetin sodium, were fitted to both linear and nonlinear pharmacokinetic equations."( Linear and nonlinear assessment of tolmetin pharmacokinetics.
Ayres, JW; Sakmar, E; Wagner, JG; Weidler, DJ, 1977
)
0.75
"Tolmetin sodium has been investigated and determined from dosage forms as its Cu(II) complex and method optimized by statistical optimization."( Statistical optimization applied to the spectrophotometric study of a tolmetin-copper(II) complex.
Agatonović-Kustrin, S; Pećanac, D; Radulović, D; Vasiljević, M; Zivanović, L, 1991
)
1.96
" Flurbiprofen in 50 mg and 100 mg dosages demonstrated effective analgesic activity with the 100 mg dosage being at least as effective as the acetaminophen/codeine combination."( The analgesic efficacy of flurbiprofen compared to acetaminophen with codeine.
Cooper, SA; Kupperman, A, 1991
)
0.28
"04) superior to diflunisal in reducing the pain severity during the first 9 h of treatment; a difference possibly related to the more flexible dosage regimen of ketorolac."( Comparative multiple-dose study of ketorolac tromethamine and diflunisal for pain following orthopaedic surgery.
Fernández-Sabaté, A; Portabella, F,
)
0.13
" With the dosage regimens used, neither drug adequately controlled moderate to severe pain in the immediate postoperative period."( Intravenous ketorolac tromethamine versus morphine sulfate in the treatment of immediate postoperative pain.
Fragen, RJ; Peirce, RJ; Pemberton, DM, 1990
)
0.28
" The present results show that the elderly may need slightly less frequent dosing of ketorolac than young adults to maintain similar plasma levels."( Pharmacokinetics of single-dose oral and intramuscular ketorolac tromethamine in the young and elderly.
Garg, DC; Jallad, NS; Martinez, JJ; Mroszczak, EJ; Weidler, DJ, 1990
)
0.28
" Plasma and milk samples were collected on the two dosing days and on the first day after dosing."( The excretion of ketorolac tromethamine into breast milk after multiple oral dosing.
Bullingham, R; Lloyd, J; Manth, SM; Thompson, JS; Wischnik, A, 1989
)
0.28
" Our results suggested a positive dose-response relationship for ketorolac."( Ketorolac versus aspirin for postpartum uterine pain.
Barden, TP; Bloomfield, SS; Cissell, GB; Mitchell, J; Yee, JP,
)
0.13
" In the multiple dosing phase, zomepirac was statistically better than dihydrocodeine."( Zomepirac, dihydrocodeine and placebo compared in postoperative pain after day-case surgery. The relationship between the effects of single and multiple doses.
Bullingham, RE; Carroll, D; Collin, J; Evans, PJ; Lloyd, JW; McQuay, HJ; Moore, RA; O'Sullivan, G, 1985
)
0.27
" Evaluation of symptoms and signs revealed no statistical difference of effectiveness between the two dosage groups."( [Clinical experiences with 5% Tolectin (tolmetin) gel in patients with degenerative joint and spine diseases and soft tissue rheumatism].
Fellmann, N,
)
0.4
" Dosage adjustments may, therefore, be necessary in patients with cirrhosis of the liver."( Abnormal glucuronidation of zomepirac in patients with cirrhosis of the liver.
Bircher, J; Huguenin, P; Preisig, R; Witassek, F,
)
0.13
" The dosage of tolmetin sodium remained at 1600 mg daily for the 3-month duration of the study but side-effects necessitated the reduction of the dosage of aloxiprin in many patients and after 3-months' treatment the mean dosage was 4 g daily."( Clinical experience with tolmetin sodium.
Balme, HW; Huskisson, EC; Wojtulewski, JA, 1980
)
0.92
" Patients were allocated at random to treatment with either 800 mg tolmetin sodium daily or 500 mg naproxen daily over a period of 12 weeks, both drugs being given in identical capsule form in a dosage of 2 capsules twice daily."( A double-blind comparative evaluation of tolmetin versus naproxen in osteoarthritis.
Bach-Andersen, R; Persson, B; Telhag, H, 1981
)
0.76
" In therapeutic dosage it will adequately control joint symptoms in the majority of patients."( Pharmacotherapy of juvenile rheumatoid arthritis.
Lindsley, CB, 1981
)
0.26
" 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
" Bioavailability of zomepirac from the 3 dosage forms was much the same."( Zomepirac kinetics in healthy males.
Gottlieb, S; Nayak, RK; Ng, KT; Plostnieks, J, 1980
)
0.26
"A spectrophotometric assay for determining tolmetin sodium in pharmaceutical solid dosage forms is described."( Stability-indicating assay for tolmetin sodium in solid dosage forms.
Daly, KF; Janicki, CA, 1980
)
0.81
" Treatment animals were then maintained on a regimen of intramuscular ketorolac using a three times a day dosing schedule for 14 days postoperatively."( Ketorolac (Toradol) and acute random-pattern skin flap survival in rat.
Cohen, JI; Cook, TA; Davis, RE; Robinson, JE; Urben, SL, 1995
)
0.29
"To describe the use of parenteral ketorolac in a large population of children, focusing on dosing patterns, efficacy, and safety."( Clinical experience with ketorolac in children.
Buck, ML, 1994
)
0.29
"Indications for treatment, dose, dosing interval, use of a loading dose, length of therapy, efficacy (subjective response and use of concomitant therapy), and adverse effects (bleeding, gastrointestinal ulceration or vomiting, and renal dysfunction)."( Clinical experience with ketorolac in children.
Buck, ML, 1994
)
0.29
" The time to first administration of rescue analgesic, up to 24 h following dosing with the study medication, was recorded."( A comparison of intramuscular ketorolac and pethidine in the alleviation of renal colic.
Arkell, DG; Fletcher, MS; Iacovou, JW; Kaisary, AV; Philip, NH; Sandhu, DP, 1994
)
0.29
" To determine the effects of withdrawal all subjects were then given further dosing with placebo (4 times daily) for 2 days while maintaining the double-blind nature of the previous drug assignment."( Tolerability, central effects and pharmacokinetics of intravenous ketorolac tromethamine in volunteers.
Bullingham, R; Hooftman, L; Lloyd, J; Lucker, P; Mroszczak, E, 1994
)
0.29
" The administered dosage was 10 mg every 6 h for ketorolac and 50 mg every 8 h for diclofenac sodium."( Ketorolac versus diclofenac sodium in cancer pain.
Corli, O; De Conno, F; Gallucci, M; Piva, L; Speranza, R; Tamburini, M; Toscani, F; Ventafridda, V, 1994
)
0.29
"The pressor response to noxious colorectal distention (80 mmHg, 20 s) was evaluated in 29 male Sprague-Dawley rats and dose-response curves were determined for intravenous morphine, ketorolac and the mixture of morphine and ketorolac."( Ketorolac potentiates morphine antinociception during visceral nociception in the rat.
Gebhart, GF; Maves, TJ; Meller, ST; Pechman, PS, 1994
)
0.29
"Randomized, double-blind, placebo-controlled, dose-response evaluation."( Intravenous ketorolac as an adjunct to patient-controlled analgesia (PCA) for management of postgynecologic surgical pain.
Paige, D; Sevarino, FB; Silverman, DG; Sinatra, RS,
)
0.13
" Finally, since ketorolac is excreted almost entirely by the kidney, either elderly patients or patients with underlying renal insufficiency must have an adjustment of the dosing interval, or this medication should be avoided in such patients altogether."( NSAID nephrotoxicity revisited: acute renal failure due to parenteral ketorolac.
Buller, GK; Perazella, MA, 1993
)
0.29
" 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
" The pharmacist's concurrent interventions improved prescribing for correct dosage and facilitated discontinuation of the agent in high-risk patients."( Ketorolac injection use in a university hospital.
Krstenansky, PM, 1993
)
0.29
"We identified five reports that specifically addressed intravenous dosing of ketorolac."( Pain management with intravenous ketorolac.
Kramer, MA; Miller, LJ, 1993
)
0.29
"Propofol infusion and supplemental fentanyl dosage requirements, oxygen saturation values, respiratory rates, recovery times, and postoperative side effects were recorded."( Use of analgesics during propofol sedation: a comparison of ketorolac, dezocine, and fentanyl.
Ramirez-Ruiz, M; Smith, I; White, PF, 1995
)
0.29
" A dose-response relationship was evident between average daily ketorolac dose and both gastrointestinal bleeding and operative site bleeding (trend test P < ."( Parenteral ketorolac and risk of gastrointestinal and operative site bleeding. A postmarketing surveillance study.
Berlin, JA; Carson, JL; Feldman, H; Hennessy, S; Kimmel, S; Kinman, JL; Spitz, PW; Strom, BL, 1996
)
0.29
" Topical dosing led to relatively low aqueous and undetectable vitreous levels."( Intraocular penetration of periocular ketorolac and efficacy in experimental uveitis.
Fiscella, RG; Rabiah, PK; Tessler, HH, 1996
)
0.29
" In this study, we compared the extent and pattern of covalent adduct formation in plasma and livers of rats dosed with the nonsteroidal anti-inflammatory drugs (NSAIDs) zomepirac (ZP) and diflunisal (DF), the hypolipidemic agent clofibric acid (CA), and the anti-epileptic agent valproic acid (VPA)."( Chemical and immunochemical comparison of protein adduct formation of four carboxylate drugs in rat liver and plasma.
Bailey, MJ; Dickinson, RG,
)
0.13
"To determine the incidence of side effects with the short-term use of intravenously administered ketorolac in children and the overall cost savings with a unit dosing system."( Safety of intravenous ketorolac therapy in children and cost savings with a unit dosing system.
Berde, CB; Houck, CS; McDermott, JS; Sethna, NF; Wilder, RT, 1996
)
0.29
" The relative bioavailabilities of ketorolac in the GCF after dosing with the dentifrice formulations with respect to the rinse were 89."( Evaluation of ketorolac concentrations in plasma and gingival crevicular fluid following topical treatment with oral rinses and dentifrices.
Bapat, NV; Buchanan, W; Collins, JG; Dobrozsi, DJ; Doyle, MJ; Eichhold, TH; Kelm, GR; Mankodi, SM; Meredith, MP; Offenbacher, S; Wehmeyer, KR, 1996
)
0.29
" The incidence of serious or fatal adverse events reported with ketorolac has decreased since revision of dosage guidelines."( Ketorolac. A reappraisal of its pharmacodynamic and pharmacokinetic properties and therapeutic use in pain management.
Brogden, RN; Gillis, JC, 1997
)
0.3
" These pharmacokinetic differences indicate that a higher relative dosage is required in children, but the dosage interval is similar in children and adults."( Ketorolac for postoperative pain management in children.
Forrest, JB; Heitlinger, EL; Revell, S, 1997
)
0.3
"96) or a dose-response relationship (P = ."( Lack of hepatotoxic effects of parenteral ketorolac in the hospital setting.
Berlin, JA; Carson, JL; Farrar, J; Feldman, HI; Harb, G; Hennessy, S; Kimmel, SE; Kinman, JL; Strom, BL, 1997
)
0.3
" Footpad PG levels returned to base line or below within 5 min of dosing with ketorolac, which suggests rapid turnover of PG in the inflamed tissue."( Inhibition of cyclooxygenase-2 rapidly reverses inflammatory hyperalgesia and prostaglandin E2 production.
Isakson, PC; Portanova, J; Seibert, K; Shaffer, A; Zhang, Y, 1997
)
0.3
" In addition, the total daily dose of ketorolac was reduced following a change from intermittent bolus dosing to a continuous infusion."( Prolonged central intravenous ketorolac continuous infusion in a cancer patient with intractable bone pain.
Gordon, RL, 1998
)
0.3
" However, smaller doses provided less effective pain relief, and a linear dose-response relationship was demonstrated."( The dose-response relationship of ketorolac as a component of intravenous regional anesthesia with lidocaine.
Gardner, G; Reuben, SS; Steinberg, RB, 1998
)
0.3
" ZP-modified tubulin was shown to be present in the cytosol of livers from rats dosed twice daily for 3 days with ZP at 50 mg/kg, using a sandwich ELISA with ZP and tubulin antisera."( Zomepirac acyl glucuronide covalently modifies tubulin in vitro and in vivo and inhibits its assembly in an in vitro system.
Bailey, MJ; de Jersey, J; Dickinson, RG; Worrall, S, 1998
)
0.3
" Groups of six rats received either vehicle or analgesic drug and antinociception was evaluated by evaluating the dose-response curves over time."( Antinociceptive effects of S(+)-ketoprofen and other analgesic drugs in a rat model of pain induced by uric acid.
Cabré, F; Díaz, I; Fernández-Guasti, A; López-Muñoz, FJ; Mauleón, D; Tost, D; Ventura, R, 1998
)
0.3
" Adequate stable anesthesia was achieved in reduced dosage of conventional anesthesiological agents."( [Use of nonopiate agents for anesthesia in ENT patients at high surgical-anesthesiological risk].
Akopian, RG; Daĭkhes, NA; Davudov, KhSh; Gur'ianov, VA; Kokliaeva, NV; Kuĭian, SM; Nazhmudinov, II; Pogosov, VS; Riazanov, VB; Tiukov, VL, 1998
)
0.3
" The first is a pharmacist conversion order protocol in which pharmacists are given the responsibility of flagging and monitoring IV to oral dosage conversions of selected medications; the second is a pharmacist screening program for parenteral ketorolac dosing."( Pharmacist empowerment: taking practice guidelines to the next level (Part 2).
Egle, L; Galt, M; Puckett, W, 1994
)
0.29
"Drugs were separately, orally dosed to pregnant rats triple daily 8 hr apart from day 8 to 21 (GD=1-plug day)."( Developmental toxicity evaluation of ibuprofen and tolmetin administered in triple daily doses to Wistar CRL:(WI)WUBR rats.
Burdan, F, 2004
)
0.58
" Piroxicam and DFU were dosed once daily."( Skeletal developmental effects of selective and nonselective cyclooxygenase-2 inhibitors administered through organogenesis and fetogenesis in Wistar CRL:(WI)WUBR rats.
Burdan, F; Dudka, J; Klepacz, R; Marzec, B; Szumilo, J, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
non-steroidal anti-inflammatory drugAn 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) inhibitorA 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.
[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]

Drug Classes (3)

ClassDescription
pyrrolesAn azole that includes only one N atom and no other heteroatom as a part of the aromatic skeleton.
monocarboxylic acidAn oxoacid containing a single carboxy group.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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]

Pathways (1)

PathwayProteinsCompounds
Tolmetin Action Pathway2967

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Interleukin-8Homo sapiens (human)IC50 (µMol)0.09000.00800.04360.0900AID426392
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.04100.00021.557410.0000AID625243
Lactoylglutathione lyaseHomo sapiens (human)Ki396.53330.00122.59479.1400AID568008; AID568009; AID604299
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (92)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
positive regulation of gene expressionInterleukin-8Homo sapiens (human)
negative regulation of gene expressionInterleukin-8Homo sapiens (human)
positive regulation of cellular biosynthetic processInterleukin-8Homo sapiens (human)
negative regulation of cell adhesion molecule productionInterleukin-8Homo sapiens (human)
angiogenesisInterleukin-8Homo sapiens (human)
response to molecule of bacterial originInterleukin-8Homo sapiens (human)
chemotaxisInterleukin-8Homo sapiens (human)
inflammatory responseInterleukin-8Homo sapiens (human)
signal transductionInterleukin-8Homo sapiens (human)
G protein-coupled receptor signaling pathwayInterleukin-8Homo sapiens (human)
negative regulation of cell population proliferationInterleukin-8Homo sapiens (human)
calcium-mediated signalingInterleukin-8Homo sapiens (human)
regulation of cell adhesionInterleukin-8Homo sapiens (human)
neutrophil chemotaxisInterleukin-8Homo sapiens (human)
receptor internalizationInterleukin-8Homo sapiens (human)
response to endoplasmic reticulum stressInterleukin-8Homo sapiens (human)
intracellular signal transductionInterleukin-8Homo sapiens (human)
neutrophil activationInterleukin-8Homo sapiens (human)
cellular response to fibroblast growth factor stimulusInterleukin-8Homo sapiens (human)
regulation of single stranded viral RNA replication via double stranded DNA intermediateInterleukin-8Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayInterleukin-8Homo sapiens (human)
positive regulation of angiogenesisInterleukin-8Homo sapiens (human)
embryonic digestive tract developmentInterleukin-8Homo sapiens (human)
induction of positive chemotaxisInterleukin-8Homo sapiens (human)
cellular response to lipopolysaccharideInterleukin-8Homo sapiens (human)
cellular response to interleukin-1Interleukin-8Homo sapiens (human)
cellular response to tumor necrosis factorInterleukin-8Homo sapiens (human)
positive regulation of neutrophil chemotaxisInterleukin-8Homo sapiens (human)
regulation of entry of bacterium into host cellInterleukin-8Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideInterleukin-8Homo sapiens (human)
chemokine-mediated signaling pathwayInterleukin-8Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
carbohydrate metabolic processLactoylglutathione lyaseHomo sapiens (human)
regulation of transcription by RNA polymerase IILactoylglutathione lyaseHomo sapiens (human)
glutathione metabolic processLactoylglutathione lyaseHomo sapiens (human)
methylglyoxal metabolic processLactoylglutathione lyaseHomo sapiens (human)
osteoclast differentiationLactoylglutathione lyaseHomo sapiens (human)
negative regulation of apoptotic processLactoylglutathione lyaseHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
interleukin-8 receptor bindingInterleukin-8Homo sapiens (human)
protein bindingInterleukin-8Homo sapiens (human)
chemokine activityInterleukin-8Homo sapiens (human)
heparin bindingInterleukin-8Homo sapiens (human)
CXCR chemokine receptor bindingInterleukin-8Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
lactoylglutathione lyase activityLactoylglutathione lyaseHomo sapiens (human)
protein bindingLactoylglutathione lyaseHomo sapiens (human)
zinc ion bindingLactoylglutathione lyaseHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
extracellular regionInterleukin-8Homo sapiens (human)
extracellular spaceInterleukin-8Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nucleoplasmLactoylglutathione lyaseHomo sapiens (human)
cytoplasmLactoylglutathione lyaseHomo sapiens (human)
cytosolLactoylglutathione lyaseHomo sapiens (human)
plasma membraneLactoylglutathione lyaseHomo sapiens (human)
extracellular exosomeLactoylglutathione lyaseHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (74)

Assay IDTitleYearJournalArticle
AID568008Inhibition of human recombinant His-tagged glyoxalase 1 expressed in Escherichia coli BL21 (DE3) preincubated for 20 mins by Dixon plot analysis2011Bioorganic & 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.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID677462Dissociation constant, pKa of the compound2012European journal of medicinal chemistry, Jul, Volume: 53Self-organizing molecular field analysis of NSAIDs: assessment of pharmacokinetic and physicochemical properties using 3D-QSPkR approach.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID93272Percent inhibition of collagen-induced platelet aggregation at a concentration of 100 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1744122Inhibition of human ACMSD assessed as picolinic acid level at 1 mM by HPLC analysis (Rvb = 83.6 +/- 3.1%)2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway.
AID5985271-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug 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.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID190166Ulcerogenic dose that produced gastric lesions, ulcers and/or hemorrhage in 50% of the animals tested1981Journal 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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID93273Percent inhibition of collagen-induced platelet aggregation at a concentration of 20 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID681767TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Tolmetin: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, May, Volume: 55, Issue:5
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1079933Acute 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
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID183692Evaluated for the percentage inhibition by adjuvant arthritis test at a dose of 50 mg/kg administarted perorally1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID1744121Inhibition of human ACMSD assessed as QUIN level at 1 mM by HPLC analysis (Rvb = 16.4 +/- 2.9%)2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway.
AID128889Percent analgesia in phenylquinone writhing assay at 100 mg/kg1981Journal 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.
AID131340Dose giving one-half of average maximal [40%] response in phenylquinone writhing assay1981Journal 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.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079935Cytolytic 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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID129025Percent analgesia in phenylquinone writhing assay at 30 mg/kg1981Journal 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.
AID599064Plasma protein binding in human2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID93279percent inhibition of serotonin release from platelets at a concentration of 20 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID604299Inhibition of human glyoxalase 12011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID568009Inhibition of glyoxalase 12011Bioorganic & 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.
AID24265Ability 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 hydrolysis1987Journal 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.
AID239780Percentage plasma protein binding towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID426392Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID93278percent inhibition of serotonin release from platelets at a concentration of 100 uM1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079931Moderate 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]
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID598525Lipophilicity, log P of the compound2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID5985261-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID131339Dose giving one-half of average maximal [40%] response in carrageenan assay1981Journal 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.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079938Chronic 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]
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID135276Neurotoxic dose that causes minimal recognizable neurotoxicity in 50% of animals tested1981Journal 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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID24263Ability 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 hydrolysis1987Journal 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.
AID426478Cytotoxicity against mouse L1.2 cells assessed as cell viability by trypan blue dye exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID426393Cytotoxicity against of human polymorphonuclear leukocytes assessed as cell viability by trypan blue dye exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
AID243230Binding affinity towards human serum albumin2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079936Choleostatic 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]
AID128888Percent analgesia in phenylquinone writhing assay at 10 mg/kg1981Journal 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,158)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990380 (32.82)18.7374
1990's698 (60.28)18.2507
2000's43 (3.71)29.6817
2010's33 (2.85)24.3611
2020's4 (0.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.85

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.85 (24.57)
Research Supply Index7.47 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index81.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials433 (32.88%)5.53%
Reviews60 (4.56%)6.00%
Case Studies176 (13.36%)4.05%
Observational0 (0.00%)0.25%
Other648 (49.20%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]