Page last updated: 2024-12-05

glyburide

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Description

Glyburide is an oral antidiabetic medication that is used to treat type 2 diabetes. It is a sulfonylurea drug that works by stimulating the release of insulin from the pancreas. Glyburide is typically prescribed when lifestyle changes and other medications, such as metformin, have not been effective in controlling blood sugar levels. Glyburide is synthesized through a multi-step process involving the reaction of a sulfonyl chloride with an appropriate amine derivative. It is highly effective in lowering blood sugar levels and is generally well-tolerated by patients. It has been widely studied for its safety, efficacy, and potential side effects. Glyburide is important for managing type 2 diabetes because it helps to improve glycemic control and reduce the risk of long-term complications. It is a commonly prescribed medication for this condition and has a long history of use. Research on glyburide continues to focus on understanding its mechanisms of action, optimizing its use, and developing new formulations. Glyburide remains a significant therapeutic agent in the management of type 2 diabetes. '

Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. [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 CID3488
CHEMBL ID472
CHEBI ID5441
SCHEMBL ID22009
MeSH IDM0009265

Synonyms (366)

Synonym
BIDD:GT0239
CBIOL_001790
MLS001077262
5-chloro-n-[2-(4-{[(cyclohexylcarbamoyl)amino]sulfonyl}phenyl)ethyl]-2-methoxybenzamide
HMS3267A15
AB00051949-17
AB00051949-16
BRD-K36927236-001-06-0
amglidia
gtpl2414
glybenclamide
DIVK1C_000481
KBIO1_000481
EU-0100499
SPECTRUM_000250
BSPBIO_001351
BPBIO1_000344
IDI1_033821
LOPAC0_000499
PRESTWICK3_000316
glibenclamida
5-chloro-n-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxybenzamide
micronase
diabeta
1-(p-(2-(5-chloro-2-methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexylurea
1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea
benzamide, 5-chloro-n-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-
CHEBI:5441 ,
PRESTWICK_569
glibenclamidum
5-chloro-n-(2-{4-[n-(n-cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide
glynase
cas-10238-21-8
NCGC00023447-02
tocris-0911
BIO1_000076
NCGC00016689-01
NCGC00015467-01
lopac-g-0639
BIO2_000551
BIO2_000071
BIO1_000565
BIO1_001054
NCGC00023447-11
OPREA1_764617
SPECTRUM5_001631
PROBES2_000378
BSPBIO_000312
IDI1_000481
PROBES1_000431
PRESTWICK2_000316
UPCMLD-DP006:001
AB00051949
5-chloro-n-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide
STK362992
10238-21-8
glyburide
glibenclamide
C07022
glyburide, meets usp testing specifications
UPCMLD-DP006
DB01016
glynase (tn)
micronase (tn)
D00336
diabeta (tn)
glyburide (usp)
glibenclamide (jp17/inn)
NCGC00023447-05
NCGC00023447-09
NCGC00023447-07
NCGC00023447-06
gen-glybe
glimel
glibil
hb 419
glibenclamid-ratiopharm
glubate
miglucan
euclamin
gliben
semi-euglucon
orabetic
gbn 5
euglucon 5
humedia
glyben
glycomin
pira
gliboral
hb-419
glibet
n-(4-(beta-(2-methoxy-5-chlorbenzamido)-aethyl)-benzolsulfonyl)-n'-cyclohexyl-harnstoff
glucomid
glibens
praeciglucon
glibenclamidum [inn-latin]
ur 606
glibenclamid heumann
glucobene
hexaglucon
glucolon
glybenzcyclamide
daonil
med-glionil
renabetic
n-(4-(2-(5-chloro-2-methoxybenzamido)ethyl)phenylsulfonyl)-n'-cyclohexylurea
glimide
neogluconin
glitisol
c23h28cln3o5s
hemi-daonil
lisaglucon
gluben
glibetic
gliban
cytagon
gewaglucon
duraglucon
dibelet
glyburide [usan]
urea, 1-((p-(2-(chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexyl-
prodiabet
glisulin
glibenil
glamide
glibenclamid fabra
glucoven
gilemal
glibenclamid-cophar
glibenclamid genericon
euglucon
adiab
brn 2230085
glibesyn
einecs 233-570-6
novo-glyburide
apo-glibenclamide
melix
glucohexal
glibenbeta
glyburide (micronized)
azuglucon
glibenclamida [inn-spanish]
betanese 5
lederglib
calabren
normoglucon
tiabet
benzamide, 5-chloro-n-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxy-
maninil
bastiverit
benclamin
glibenclamid basics
euglykon
urea, 1-(p-(2-(5-chloro-2-methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexyl-
sugril
suraben
glicem
yuglucon
norglicem 5
semi-gliben-puren n
semi-daonil
glucoremed
nadib
glidiabet
euglucan
libanil
betanase
debtan
u 26452
glibenclamid al
MLS000069721 ,
smr000058229
KBIOGR_000071
KBIO2_000071
KBIO2_002639
KBIO2_003298
KBIOSS_000071
KBIO3_000141
KBIO3_002273
KBIOGR_001897
KBIO3_000142
KBIO2_000730
KBIOSS_000730
KBIO2_005866
KBIO2_005207
SPBIO_002531
SPECTRUM2_001816
NINDS_000481
PRESTWICK1_000316
SPECTRUM3_001327
SPBIO_001831
PRESTWICK0_000316
SPECTRUM4_001199
SPECTRUM2300229
SR-01000000196-5
BSPBIO_003053
NCGC00015467-02
NCGC00023447-04
NCGC00023447-10
NCGC00023447-08
NCGC00023447-12
glybenclamide, >=99% (hplc)
NCGC00015467-06
G 0639 ,
HMS1989D13
HMS2089L06
HMS2093P04
NCGC00015467-16
AKOS001487495
u-26,45
nsc-759618
u-26452
cirara
CHEMBL472 ,
u-26,452
HMS1791D13
HMS501I03
HMS1361D13
HMS1922L08
HMS1568P14
5-chloro-n-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
bdbm50012957
NCGC00015467-11
A19539
HMS3261D19
HMS3259O12
HMS2095P14
5-chloro-n-[4-(3-cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide
G0382
rp-1127
micronized glyburide
nsc 759618
glibenclamid riker m.
sx6k58tvwc ,
unii-sx6k58tvwc
glibenclamide [inn]
glyburide [usan:usp]
tox21_300758
NCGC00254662-01
pharmakon1600-02300229
nsc759618
dtxsid0037237 ,
dtxcid8017237
tox21_110158
5-chloro-n-(4-(n-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide
CCG-39618
NCGC00015467-10
NCGC00015467-04
NCGC00015467-09
NCGC00015467-07
NCGC00015467-17
NCGC00015467-14
NCGC00015467-12
NCGC00015467-08
NCGC00015467-15
NCGC00015467-18
NCGC00015467-03
NCGC00015467-13
NCGC00015467-05
BCP9000729
abbenclamide
glibadone
diabiphage
glycron
HY-15206
CS-1075
FT-0601608
LP00499
glyburide [who-ip]
glyburide component of glucovance
glibenclamide [ep monograph]
glyburide [orange book]
glucovance component glyburide
glibenclamide [who-dd]
glyburide [vandf]
glibenclamide [who-ip]
glibenclamidum [who-ip latin]
glibenclamide [jan]
glyburide [mi]
glyburide [usp monograph]
glibenclamide [mart.]
glyburide [usp-rs]
NC00566
SCHEMBL22009
NCGC00015467-20
tox21_110158_1
KS-5326
tox21_500499
NCGC00261184-01
ZNNLBTZKUZBEKO-UHFFFAOYSA-N
5-chloro-n-(2-[4-(([(cyclohexylamino)carbonyl]amino)sulfonyl)phenyl]ethyl)-2-methoxybenzamide #
hd 419
n-(4-(.beta.-(2-methoxy-5-chlorbenzamido)-aethyl)-benzolsulfonyl)-n'-cyclohexyl-harnstoff
1-[[p-[2-(5-chloro-o-anisamido)ethyl]phenyl]sulfonyl]-3-cyclohexylurea
1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexyl urea
5-chloro-n-[2-[4-[[[(cylcohexylamino)carbonyl]amino]sulphonyl]phenyl]ethyl]-2-methoxybenzamide
5-chloro-n-[4-(cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide
W-108874
GBM ,
HMS3402D13
HMS3428D15
glyburide (glibenclamide)
AB00051949_19
AB00051949_18
OPERA_ID_801
n-p-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl-n'-cyclohexylurea
mfcd00056625
glybenzcyclamide, 99%
sr-01000000196
SR-01000000196-2
glyburide, united states pharmacopeia (usp) reference standard
glybenclamide, european pharmacopoeia (ep) reference standard
HMS3651E17
glibenclamide for peak identification, european pharmacopoeia (ep) reference standard
glyburide (glibenclamide), pharmaceutical secondary standard; certified reference material
glibenclamide 1.0 mg/ml in acetonitrile
SR-01000000196-8
SR-01000000196-6
SR-01000000196-4
SBI-0050483.P003
HMS3712P14
NCGC00015467-36
Z277540138
SW195828-5
1-{4-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl}-3-cyclohexylurea;1-{4-[2-(5-chloro-2-methoxybenzamido)ethyl]benzenesulfonyl}-3-cyclohexylurea
'glibenclamide; glyburide'
n1-[4-({[(cyclohexylamino)carbonyl]amino}sulfonyl)phenethyl]-5-chloro-2-methoxybenzamide
BCP05327
Q420626
5-chloro-n-(4-[n-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-methoxybenzamide
glyburide - cas 10238-21-8
M01823
nsc-813214
nsc813214
S1716
delmide
HMS3675F16
5-chloro-n-(4-(n-(cyclohexylcarbamoyl)sulfamoyl)-phenethyl)-2-methoxybenzamide
glibenclamide,(s)
HMS3411F16
BRD-K36927236-001-17-7
SB17414
SDCCGSBI-0050483.P004
NCGC00015467-37
5-chloro-n-[2-[4-[[[(cyclohexylamino)carbonyl]-amino]sulfonyl]phenyl]-ethyl]-2-methoxybenzamide
5-chloro-n-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide.
G-150
D81733
NCGC00015467-21
EN300-117270
glibenclamide for peak identification
BG166164
glibenclamide - bio-x
SY057080
glibenclamide (mart.)
glyburide (usan:usp)
glibenclamide (ep monograph)
5-chloro-n-(2-(4-(n-(n-cyclohexylcarbamoyl)sulfamoyl)phenyl)ethyl)-2-methoxybenzamide
4-(2-(5-chloro-2-methoxybenzoylamino)ethyl)-n-(cyclohexylcarbamoyl)benzenesulfonamide
glyburide (usp-rs)
a10bb01
glyburide (usp monograph)
glibenclamida (inn-spanish)
glibenclamidum (inn-latin)

Research Excerpts

Overview

Glyburide (GLB) is an oral sulfonylurea, commonly used for the treatment of gestational diabetes mellitus. Glyburide is an effective treatment for reaching glycaemic goals during pregnancy in women with GDM.

ExcerptReferenceRelevance
"Glyburide is a classic antidiabetic drug that is dominant in inflammation regulation, but its specific role in ozone-induced lung inflammation and injury remains unclear. "( Glyburide attenuates ozone-induced pulmonary inflammation and injury by blocking the NLRP3 inflammasome.
Ba, Y; Chen, X; Duan, S; Feng, F; Gao, M; Huang, L; Li, C; Liu, H; Shao, H; Wang, J; Wang, W; Wang, X; Wang, Z; Wu, W; Yang, Z; Zhang, Q; Zhang, R; Zhu, J; Zhu, Y, 2020
)
3.44
"Glyburide is an effective treatment for reaching glycaemic goals during pregnancy in women with GDM. "( Glyburide therapy for gestational diabetes: Glycaemic control, maternal hypoglycaemia, and treatment failure.
Affres, H; Bouchghoul, H; Bouyer, J; Coustols-Valat, M; Deruelle, P; Letourneau, A; Senat, MV, 2021
)
3.51
"Glyburide is a safe, inexpensive, and efficacious alternative to dexamethasone for the treatment of cerebral metastasis-related vasogenic edema."( Inhibition of SUR1 decreases the vascular permeability of cerebral metastases.
Muldoon, LL; Neuwelt, EA; Pishko, GL; Thompson, EM, 2013
)
1.11
"Glyburide (GLB) is a widely used oral sulfonylurea for the treatment of gestational diabetes. "( Contributions of human cytochrome P450 enzymes to glyburide metabolism.
Hebert, MF; Isoherranen, N; Lin, YS; Liu, L; Mao, Q; Naraharisetti, SB; Unadkat, JD; Wang, H; Zhou, L, 2010
)
2.06
"Glyburide (GLB) is an oral sulfonylurea, commonly used for the treatment of gestational diabetes mellitus. "( Increased glyburide clearance in the pregnant mouse model.
Hebert, MF; Mao, Q; Unadkat, JD; Zhang, Y; Zhou, L, 2010
)
2.21
"Glyburide is an oral hypoglycemic agent used to treat diabetes mellitus."( Glyburide is anti-inflammatory and associated with reduced mortality in melioidosis.
Chaowagul, W; Chierakul, W; Day, NP; Dougan, G; Koh, GC; Lee, SJ; Limmathurotsakul, D; Mahavanakul, W; Maude, RR; Peacock, SJ; Schreiber, MF; van der Poll, T; White, NJ; Wiersinga, WJ; Wuthiekanun, V, 2011
)
2.53
"Glyburide is a prescribed hypoglycemic drug for the treatment of type 2 diabetic patients. "( Synthesis and evaluation of fluorine-18 labeled glyburide analogs as beta-cell imaging agents.
Alavi, AA; Deng, S; Doliba, N; Feng, Q; Matschinsky, F; Naji, A; Pourdehnad, MT; Rösch, F; Schirrmacher, R; Schmitz, A; Shiue, CY; Shiue, GG; Vatamaniuk, M; Wolf, B, 2004
)
2.02
"Glyburide is a poorly water-soluble oral hypoglycemic agent, with problems of variable bioavailability and bio-inequivalence related to its poor water-solubility. "( Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique.
Ballerini, R; Cirri, M; Maestrelli, F; Mura, P; Valleri, M, 2004
)
2.05
"Glyburide is a second-generation sulfonylurea hypoglycemic drug used for the treatment of select women with pregestational and gestational diabetes mellitus (GDM). "( Effect of human serum albumin on transplacental transfer of glyburide.
Ahmed, MS; Hankins, GD; Nanovskaya, TN; Nekhayeva, I, 2006
)
2.02
"Glyburide (GLB) is an antidiabetic drug routinely used to treat gestational diabetes."( The breast cancer resistance protein (Bcrp1/Abcg2) limits fetal distribution of glyburide in the pregnant mouse: an Obstetric-Fetal Pharmacology Research Unit Network and University of Washington Specialized Center of Research Study.
Hebert, MF; Mao, Q; Naraharisetti, SB; Unadkat, JD; Wang, H; Zhou, L, 2008
)
1.29
"Glyburide is an improved drug for the management of non-insulin-dependent diabetes mellitus (NIDDM). "( Glyburide (DiaBeta): a new second-generation hypoglycemic agent.
Krall, LP, 1984
)
3.15
"Glyburide is an effective hypoglycemic agent in patients with type II diabetes even after the loss of its ability to increase insulin secretion. "( Low-dose oral glyburide reduces fasting blood glucose by decreasing hepatic glucose production in healthy volunteers without increasing carbohydrate oxidation.
Tayek, JA, 1995
)
2.09
"Glyburide is an effective, long-acting, second-generation oral sulfonylurea introduced in the United States in 1984."( Glyburide in non-insulin-dependent diabetes: an update.
Kolterman, OG,
)
2.3
"Glyburide is a useful and rational addition to therapy in properly selected patients with type II diabetes mellitus."( Review of glyburide after one year on the market.
Feldman, JM, 1985
)
1.39

Effects

Glyburide and metformin have been shown to be as effective as insulin for the treatment of gestational diabetes. Glyburide has replaced insulin as the more common pharmacotherapy for GDM over the past decade among those privately insured.

ExcerptReferenceRelevance
"Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects."( Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects.
Feldman, JM,
)
2.3
"Glyburide has been shown as an effective neuroprotective agent in preclinical tSCI models and in the treatment of ischaemic stroke with the additional risk of a hypoglycaemic response. "( SCING-Spinal Cord Injury Neuroprotection with Glyburide: a pilot, open-label, multicentre, prospective evaluation of oral glyburide in patients with acute traumatic spinal cord injury in the USA.
Boling, WW; Farhadi, HF; Mehta, A; Minnema, AJ; Schwab, J; Simard, JM, 2019
)
2.21
"Glyburide has been associated with increased neonatal hypoglycemia."( The Use of Non-insulin Agents in Gestational Diabetes: Clinical Considerations in Tailoring Therapy.
Blair, RA; Palermo, NE; Rosenberg, EA, 2019
)
1.24
"Glyburide has good efficacy and short-term data but it also crosses the placenta and may be associated with increased rates of large-for-gestational-age (LGA) infants and neonatal hypoglycaemia when compared with insulin."( Pharmacological Management of Gestational Diabetes Mellitus.
Feig, DS; Mukerji, G, 2017
)
1.18
"Glyburide has been used for managing gestational diabetes mellitus (GDM) in a number of countries. "( The use of glyburide in the management of gestational diabetes mellitus: a meta-analysis.
Chen, Y; Jiang, L; Li, BY; Li, MJ; Mo, XL; Wang, SM; Zeng, YC, 2014
)
2.23
"Glyburide has replaced insulin as the more common pharmacotherapy for GDM over the past decade among those privately insured. "( Trends in glyburide compared with insulin use for gestational diabetes treatment in the United States, 2000-2011.
Benjamin, DK; Boggess, K; Brookhart, MA; Camelo Castillo, W; Jonsson Funk, M; Stürmer, T, 2014
)
2.25
"Glyburide and metformin have been shown to be as effective as insulin for the treatment of gestational diabetes."( Oral hypoglycemic agents in pregnancy.
Refuerzo, JS, 2011
)
1.09
"Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects."( Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects.
Feldman, JM,
)
2.3

Actions

Glyburide (Gly) could inhibit NLRP3 inflammasome, as well as could be treated with Type 2 diabetes as a common medication. Glyburide can produce an acute hepatitis-like illness in some persons.

ExcerptReferenceRelevance
"Glyburide (Gly) could inhibit NLRP3 inflammasome, as well as could be treated with Type 2 diabetes as a common medication. "( Glyburide attenuates B(a)p and LPS-induced inflammation-related lung tumorigenesis in mice.
Feng, F; Gao, M; Huang, L; Li, M; Liu, H; Shang, P; Shao, H; Wang, W; Zhang, P; Zhang, Q, 2021
)
3.51
"Glyburide analogues inhibit ATP- but not hypothermia-induced IL-1beta secretion from human monocytes expressing familial cold-associated autoinflammatory syndrome-associated Cryopyrin mutations, thus suggesting that inhibition occurs upstream of Cryopyrin."( Glyburide inhibits the Cryopyrin/Nalp3 inflammasome.
Deshayes, K; Dixit, VM; Fedorova, A; Hoffman, HM; Lamkanfi, M; Lee, WP; Misaghi, S; Mueller, JL; Vitari, AC, 2009
)
2.52
"Glyburide did not lower DPP-IV activity or glycosylated hemoglobin."( Reduced serum dipeptidyl peptidase-IV after metformin and pioglitazone treatments.
Croom, DK; Lenhard, JM; Minnick, DT, 2004
)
1.04
"Glyburide did not increase basal or insulin-stimulated DNA synthesis."( Pioglitazone: in vitro effects on rat hepatoma cells and in vivo liver hypertrophy in KKAy mice.
Diani, A; Messina, JL; Murray, FT; Sangani, GA; Wachowski, MB; Weinstock, RS, 1997
)
1.02
"Glyburide can produce an acute hepatitis-like illness in some persons."( Glyburide-induced hepatitis.
Dean, PJ; Goodman, RC; Kitabchi, AE; Radparvar, A, 1987
)
2.44

Treatment

Glyburide or quercetin treatment significantly attenuated hepatic steatosis, associated with mitigated expression of the lipogenic markers in liver. Glyburide treatment of diabetes decreased CRP and did so even though body weight increased.

ExcerptReferenceRelevance
"Both glyburide or quercetin treatment significantly attenuated hepatic steatosis, associated with mitigated expression of the lipogenic markers in liver."( Convergence of Fructose-Induced NLRP3 Activation with Oxidative Stress and ER Stress Leading to Hepatic Steatosis.
Ahmad, I; Ahmad, S; Gulzar, F; Guru, B; Kumar, P; Sharma, A; Singh, S; Tamrakar, AK, 2023
)
1.37
"Glyburide treatment decreased the total cells in BALF, the inflammatory score, and the mean linear intercept induced by ozone in lung tissues."( Glyburide attenuates ozone-induced pulmonary inflammation and injury by blocking the NLRP3 inflammasome.
Ba, Y; Chen, X; Duan, S; Feng, F; Gao, M; Huang, L; Li, C; Liu, H; Shao, H; Wang, J; Wang, W; Wang, X; Wang, Z; Wu, W; Yang, Z; Zhang, Q; Zhang, R; Zhu, J; Zhu, Y, 2020
)
2.72
"Glyburide treatment did not affect glucose levels but was associated with reduced pulmonary cellular influx, reduced bacterial dissemination to both liver and spleen and reduced IL1β production when compared to untreated controls."( Glyburide reduces bacterial dissemination in a mouse model of melioidosis.
Bast, A; Breitbach, K; de Jong, HK; Hoogendijk, AJ; Kager, LM; Koh, GC; Krause, K; Peacock, SJ; Steinmetz, I; van der Poll, T; Weehuizen, TA; Wiersinga, WJ, 2013
)
2.55
"Glyburide treatment of diabetes decreased CRP and did so even though body weight increased."( Adiponectin and C-reactive protein in obesity, type 2 diabetes, and monodrug therapy.
Bar, RS; Goldner, WS; Haynes, WG; Putz, DM; Sivitz, WI, 2004
)
1.04
"Glyburide treatment of diabetic rats for 4 weeks corrected the changes observed in diabetic heart."( The effects of the sulfonylurea glyburide on glutathione peroxidase, superoxide dismutase and catalase activities in the heart tissue of streptozotocin-induced diabetic rat.
Altan, N; Bilgihan, A; Buğdayci, G; Bukan, N; Kosova, F; Sancak, B, 2004
)
1.33
"In glyburide/metformin-treated patients, mean A1C was 8.3% at baseline and 6.8% at week 104 (P < 0.0001 vs."( PRESERVE-beta: two-year efficacy and safety of initial combination therapy with nateglinide or glyburide plus metformin.
Baron, MA; Gerich, J; Jean-Louis, L; Purkayastha, D; Raskin, P, 2005
)
1.06
"Glyburide treatment (10-300 microM) had no effect on basal RR, which measured approximately 10% or 30% of the total cellular renin activity after 4 or 24 h, respectively."( Glyburide attenuates calmodulin antagonist-stimulated renin release from isolated mouse juxtaglomerular cells.
Jones, DA; Lawson, JA; Linseman, DA; Ludens, JH, 1995
)
2.46
"3. Glyburide treatment of diabetic rats for 4 weeks corrected the changes on the glutathione levels observed in diabetic liver."( Effect of the sulfonylurea glyburide on glutathione and glutathione peroxidase activity in alloxan-induced diabetic rat hepatocytes.
Altan, N; Cayci, B; Elmali, E; Kiliç, N; Ongun, CO; Yavuz, O, 1994
)
1.1
"3. Glyburide treatment alone for 3 weeks also reversed the changes in the gastro-intestinal beta-adrenergic responses of non-insulin-dependent diabetic rats."( The effects of glyburide and insulin on the decreased beta-adrenergic responsiveness of the gastrointestinal tract in rats with non-insulin-dependent diabetes.
Altan, VM; Oztürk, Y; Ozüari, A; Yildizoğlu-Ari, N, 1994
)
1.16
"Glyburide treatment of diabetic rats for 4 weeks corrected the changes observed in diabetic liver."( Effect of the sulfonylurea glyburide on superoxide dismutase activity in alloxan-induced diabetic rat hepatocytes.
Altan, N; Engin, A; Hasanoğlu, E; Ongun, CO; Sindel, S; Tuncer, C, 1994
)
1.31
"6. Glyburide treatment (5 mg/kg/day per os) for 3 weeks was able to improve the reduced responsiveness of rat atria due to non-insulin-dependent diabetes as well."( The effects of glyburide and insulin on the cardiac performance in rats with non-insulin-dependent diabetes mellitus.
Altan, VM; Ozçelkay, AT; Oztürk, Y; Ozüari, A; Yildizoğlu-Ari, N, 1993
)
1.15
"When glyburide-treated islets were stimulated with glyburide or tolbutamide, insulin release was also impaired compared to that in control islets (P < 0.05)."( Glyburide and tolbutamide induce desensitization of insulin release in rat pancreatic islets by different mechanisms.
Buscema, M; Caltabiano, V; Forte, F; Purrello, F; Rabuazzo, AM; Vetri, M; Vigneri, R; Vinci, C, 1992
)
2.18
"Treatment with glyburide led to significantly reduced relative pancreatic mass and water content and less pancreatic damage and cell death in genetically obese ob/ob mice with SAP compared with vehicle-treated obese SAP mice."( Inhibition of the nucleotide-binding domain, leucine-rich containing family, pyrin-domain containing 3 inflammasome reduces the severity of experimentally induced acute pancreatitis in obese mice.
Cabay, RJ; Castellanos, KJ; Fantuzzi, G; York, JM, 2014
)
0.74
"Treatment with glyburide or insulin during pregnancy within 150 days before delivery."( Association of Adverse Pregnancy Outcomes With Glyburide vs Insulin in Women With Gestational Diabetes.
Benjamin, DK; Boggess, K; Brookhart, MA; Camelo Castillo, W; Jonsson Funk, M; Stürmer, T, 2015
)
1.03
"Treatment with glyburide is associated with increased all-cause and cardiovascular mortality in patients with T2DM."( All-Cause and Cardiovascular Mortality following Treatment with Metformin or Glyburide in Patients with Type 2 Diabetes Mellitus.
Esteghamati, A; Heidari, B; Larry, M; Mansournia, MA; Nakhjavani, M; Nargesi, AA; Rabizadeh, S; Raee, MR; Zarifkar, M, 2017
)
1.04
"Treatment with glyburide, but not rosiglitazone, resulted in a significant deterioration in both resting and stress MBF."( Impact of rosiglitazone and glyburide on nitrosative stress and myocardial blood flow regulation in type 2 diabetes mellitus.
Bajirovic, V; Byun, J; Kellogg, A; Oral, E; Pennathur, S; Pop-Busui, R; Raffel, D; Stevens, MJ; Vivekanandan-Giri, A, 2009
)
0.99
"Treatment with glyburide and metformin significantly decreased plasma glucose concentrations from 207 (76) to 134 (52) mg/dl (p<0.001)."( Improvement in coronary vascular dysfunction produced with euglycaemic control in patients with type 2 diabetes.
Cadenas, J; Facta, AD; Hsueh, WA; Prior, JO; Quinones, MJ; Schelbert, HR; Schindler, TH, 2007
)
0.68
"Treatment with glyburide significantly reduced aggregation in response to 10 microM of epinephrine and collagen at 750 microgram/ml."( Sulfonylureas and platelet function.
Jackson, WP; Jacobs, P; Kernoff, L; Klaff, LJ; Vinik, AI, 1981
)
0.6
"Pretreatment with glyburide (an ATP-dependent K+ channel blocker) preserved ERP response to SNS (9 +/- 1% shortening of ERP vs."( Transient depression of responses to sympathetic nerve stimulation overlying a subendocardial infarct.
Cable, DG; Hingtgen, L; Horn, M; Lund, DD; Martins, JB; Rath, TE, 1993
)
0.61
"Pretreatment with glyburide (10-500 nM) produced a dose-dependent inhibition of the PCO relaxation time course."( Vascular pharmacology of ATP-sensitive K+ channels: interactions between glyburide and K+ channel openers.
Khan, SA; Martin, JL; Meisheri, KD,
)
0.69
"Treatment with glyburide, pinacidil or hydralazine did not alter L-type calcium channels, assessed by [3H]PN 200 110 binding, in cardiac and brain membranes or small size Ca(2+)-activated K+ channels in brain assessed by [125I]apamin binding."( Regulation of ATP-sensitive K+ channels by chronic glyburide and pinacidil administration.
Gopalakrishnan, M; Triggle, DJ, 1992
)
0.88
"Treatment with glyburide, 20 mg/d (plus insulin), compared with placebo (plus insulin) resulted in a significant reduction in mean basal glucose (232 +/- 12 vs 262 +/- 11 mg/dL [12.8 vs 14.4 mmol/L]) and hemoglobin A1C (10.2% +/- 0.5% vs 10.9% +/- 03%) concentrations."( Addition of sulfonylurea to insulin treatment in poorly controlled type II diabetes. A double-blind, randomized clinical trial.
Griego, G; Mitchell, WJ; Schade, DS, 1987
)
0.61
"When treated with glyburide, the severity of the mechanical defect was significantly less."( Effect of chronic sulfonylurea treatment on the myocardium of insulin-dependent diabetic rats.
Mozaffari, MS; Schaffer, SW; Wilson, GL, 1988
)
0.6

Toxicity

Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; it has a lower frequency of adverse effects. A recent human study has shown glyburide to minimally cross the placenta, allowing a safe new treatment for gestational diabetes.

ExcerptReferenceRelevance
" In Sweden, the combined use of spontaneous adverse drug reaction (ADR) reporting data and different registers has yielded much valuable information on safety problems with different drugs."( Regulatory decisions. Emphasis on safety issues.
Strandberg, K; Wiholm, BE, 1986
)
0.27
" Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects."( Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects.
Feldman, JM,
)
2.48
" At the same time about 1/3 of these serious adverse drug reactions (ADR) was found to have been reported to the ADR-register."( Drug utilization and morbidity statistics for the evaluation of drug safety in Sweden.
Westerholm, B; Wiholm, BE, 1984
)
0.27
" At the same time, about 1/3 of these serious adverse drug reactions (ADRs) had been reported to the ADR register."( Drug utilization and morbidity statistics for the evaluation of drug safety in Sweden.
Westerholm, B; Wiholm, BE, 1984
)
0.27
" In conclusion, the cardiovascular toxicity of MNX in dogs is not caused by a direct toxic effect of MNX on the heart but apparently is related to the exaggerated pharmacologic/profound hemodynamic effects it elicits in the dog."( The pharmacologic basis of the cardiovascular toxicity of minoxidil in the dog.
DuCharme, DW; Higgins, MJ; Mesfin, GM; Robinson, FG; Zhong, WZ,
)
0.13
"Miglitol monotherapy is effective and safe in NIDDM patients."( The efficacy and safety of miglitol therapy compared with glibenclamide in patients with NIDDM inadequately controlled by diet alone.
Berlin, C; Feig, PU; Petzinna, D; Ratzmann, KP; Rybka, J; Schernthaner, G; Segal, P, 1997
)
0.3
"A retrospective analysis was conducted to determine the effects of metformin on glycosylated hemoglobin (HbA1c), body weight, and adverse events in an African-American population."( A retrospective analysis of the efficacy and safety of metformin in the African-American patient.
Anderson, D; Briscoe, TA; Cooper, GS; Usifo, OS, 1997
)
0.3
" A recent human study has shown glyburide to minimally cross the placenta, allowing a safe new treatment for gestational diabetes."( Glyburide and fetal safety; transplacental pharmacokinetic considerations.
Koren, G,
)
1.86
" Adverse events (AEs) were recorded and summarized by treatment group."( Glyburide/metformin combination product is safe and efficacious in patients with type 2 diabetes failing sulphonylurea therapy.
Blonde, L; Henry, D; Mooradian, AD; Piper, BA; Rosenstock, J, 2002
)
1.76
" LD50 was found to be 1690 mg/kg."( Effect of potassium channel modulators on toxicity of Cleistanthus collinus.
Anand, KN; Ernest, K; Jeyaseelan, L; Jose, VM; Kuruvilla, A, 2004
)
0.32
" Adverse events were carefully monitored during the study."( [Efficacy and safety of glimepiride plus metformin in a single presentation, as combined therapy, in patients with type 2 diabetes mellitus and secondary failure to glibenclamide, as monotherapy].
González-Ortiz, M; Martínez-Abundis, E,
)
0.13
" The frequency of adverse events was similar for all the groups."( [Efficacy and safety of glimepiride plus metformin in a single presentation, as combined therapy, in patients with type 2 diabetes mellitus and secondary failure to glibenclamide, as monotherapy].
González-Ortiz, M; Martínez-Abundis, E,
)
0.13
"The combined use of glimepiride plus metformin in a single presentation for 3 months showed to be efficacious and safe in patients with DM2 and secondary failure to glibenclamide."( [Efficacy and safety of glimepiride plus metformin in a single presentation, as combined therapy, in patients with type 2 diabetes mellitus and secondary failure to glibenclamide, as monotherapy].
González-Ortiz, M; Martínez-Abundis, E,
)
0.13
" In addition, the oral LD50 of the butanol extract in mice was 3820 mg/kg, while that of glibenclamide was 3160 mg/kg."( Antidiabetic activity and toxicity of Zizyphus spina-christi leaves.
Abdel-Hady, RH; Abdel-Zaher, AO; Assaf, MH; Salim, SY, 2005
)
0.33
" Fasting and mean 7- and 8-point blood glucose profiles, blood lipid levels, plasminogen activator inhibitor levels, adverse events, and hypoglycemia frequency were also compared."( Efficacy and safety of biphasic insulin aspart 30 combined with pioglitazone in type 2 diabetes poorly controlled on glibenclamide (glyburide) monotherapy or combination therapy: an 18-week, randomized, open-label study.
Chow, CC; Filipczak, R; Joshi, P; Lertoft, B; Rastam, J; Raz, I; Shaban, J; Stranks, S, 2005
)
0.53
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Other adverse events, except increased cough in the INH group, were similar."( An open, randomized, parallel-group study to compare the efficacy and safety profile of inhaled human insulin (Exubera) with glibenclamide as adjunctive therapy in patients with type 2 diabetes poorly controlled on metformin.
Barnett, AH; Dreyer, M; Lange, P; Serdarevic-Pehar, M, 2006
)
0.33
" Withdrawal due to lack of efficacy or adverse events occurred more frequently with glyburide (20."( Long-term safety of pioglitazone versus glyburide in patients with recently diagnosed type 2 diabetes mellitus.
Jain, R; Kupfer, S; Osei, K; Perez, AT; Zhang, J, 2006
)
0.83
"With long-term treatment, both glyburide and pioglitazone resulted in comparable glycemic control; however, pioglitazone was associated with less hypoglycemia and fewer withdrawals due to lack of efficacy or adverse events."( Long-term safety of pioglitazone versus glyburide in patients with recently diagnosed type 2 diabetes mellitus.
Jain, R; Kupfer, S; Osei, K; Perez, AT; Zhang, J, 2006
)
0.89
" During combined treatment with olmesartan plus glibenclamide, no adverse event occurred, and the medications were well tolerated."( Pharmacokinetics and safety of olmesartan medoxomil in combination with glibenclamide in healthy volunteers.
Bolbrinker, J; Huber, M; Kreutz, R, 2006
)
0.33
"Nine studies met the inclusion criteria, including a total of 745 glyburideexposed pregnancies and 637 insulin-exposed pregnancies, with each adverse perinatal outcome reported by 4-7 studies."( Safety of glyburide for gestational diabetes: a meta-analysis of pregnancy outcomes.
Koren, G; Moretti, ME; Rezvani, M, 2008
)
0.99
"OBJECTIVE To assess if tooth discoloration is a novel side effect of sulfonylurea therapy in patients with permanent neonatal diabetes due to mutations in KCNJ11."( Tooth discoloration in patients with neonatal diabetes after transfer onto glibenclamide: a previously unreported side effect.
Flanagan, SE; Greeley, SA; Hattersley, AT; Kumaraguru, J; Nuboer, R; Philipson, LH; Rubio-Cabezas, O; Støy, J, 2009
)
0.35
" Over the years, adverse events associated with the consumption of natural health products for sexual enhancement and the treatment of erectile dysfunction have been reported."( Safety and quality assessment of 175 illegal sexual enhancement products seized in red-light districts in Singapore.
Bloodworth, BC; Ge, XW; Koh, HL; Lee, R; Li, L; Low, MY; Zeng, Y, 2009
)
0.35
" In this review, our objectives were to (1) summarise the available evidence on the efficacy these medications, (2) review available data on adverse effect, (3) discuss current gaps in research, outlining limitations in current study designs that deserve attention and (4) summarise key points for the practicing clinician."( Oral hypoglycaemic agents during pregnancy: The evidence for effectiveness and safety.
Baptiste-Roberts, K; Nicholson, W, 2011
)
0.37
" Adverse event frequency was similar in all treatment groups; reported hypoglycaemia event rates were 24."( Safety and efficacy of saxagliptin in combination with submaximal sulphonylurea versus up-titrated sulphonylurea over 76 weeks.
Chacra, AR; Chen, R; List, J; Ravichandran, S; Tan, GH, 2011
)
0.37
" Adverse events for the US cohort were consistent with previously reported data from the 3 trials."( Efficacy and safety of saxagliptin combination therapy in US patients with type 2 diabetes.
Allen, E; Chen, R; Donovan, M; Fleming, D; Karyekar, C; Ravichandran, S, 2011
)
0.37
"5 or 5 mg as add-on therapy to OADs results in improvement across key glycemic parameters compared with placebo add-on and was generally safe and well tolerated."( Efficacy and safety of saxagliptin combination therapy in US patients with type 2 diabetes.
Allen, E; Chen, R; Donovan, M; Fleming, D; Karyekar, C; Ravichandran, S, 2011
)
0.37
" Its use is limited by a major side effect of cardiotoxicity."( Cardioprotective effects of nicorandil, a mitochondrial potassium channel opener against doxorubicin-induced cardiotoxicity in rats.
Abdel-Raheem, IT; Abouzied, MM; Taye, A, 2013
)
0.39
" This study was designed to investigate the toxic effect of MET and GB in the Liver, kidney and testis of rats."( Evaluation of toxic effects of metformin hydrochloride and glibenclamide on some organs of male rats.
Adaramoye, O; Adesanoye, O; Akanni, O; Labo-Popoola, O; Olaremi, O, 2012
)
0.38
" The reduction of prescribed sulfonylurea dose in DPP-4 patients following the safety alert coincided with a decrease of adverse event reports."( Effects of a sitagliptin safety alert on prescription behaviour for oral antihyperglycaemic drugs: a propensity score-matched cohort study of prescription receipt data in Japan.
Kimura, H; Masuda, S; Sato, D; Sato, Y, 2013
)
0.39
" Safety was assessed by adverse events, hypoglycemia, and body weight."( Saxagliptin efficacy and safety in patients with type 2 diabetes mellitus and cardiovascular disease history or cardiovascular risk factors: results of a pooled analysis of phase 3 clinical trials.
Allen, E; Bryzinski, B; Cook, W; Frederich, R; Slater, J, 2013
)
0.39
" Saxagliptin was well tolerated, with similar adverse event rates and types compared with placebo."( Saxagliptin efficacy and safety in patients with type 2 diabetes mellitus and cardiovascular disease history or cardiovascular risk factors: results of a pooled analysis of phase 3 clinical trials.
Allen, E; Bryzinski, B; Cook, W; Frederich, R; Slater, J, 2013
)
0.39
" Other oral medications have not been shown to be safe in pregnancy."( Safety considerations with pharmacological treatment of gestational diabetes mellitus.
Simmons, D, 2015
)
0.42
" reticulata extract did not cause mortality or produce any remarkable haematological, biochemical and histopathological adverse effects in rats."( Antioxidant, α-glucosidase inhibitory activity and sub-chronic toxicity of Derris reticulata extract: its antidiabetic potential.
Chudapongse, N; Kumkrai, P; Weeranantanapan, O, 2015
)
0.42
" The aim of this work was to evaluate antidiabetic activity in Streptozotocin (STZ)-induced diabetic rats and the antioxidant effects of 3',4'-Di-O-acetyl-cis-khellactone (DOAcK), as well as its toxic potential."( Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
Burgueño-Tapia, E; Cornejo-Garrido, J; Domínguez-Mendoza, EA; Ordaz-Pichardo, C, 2016
)
0.43
" Ten (23%) of 44 participants in the intravenous glyburide group and ten (26%) of 39 participants in the placebo group had cardiac events (p=0·76), and four of 20 had serious adverse events (two in the intravenous glyburide group and two in the placebo group, p=1·00)."( Safety and efficacy of intravenous glyburide on brain swelling after large hemispheric infarction (GAMES-RP): a randomised, double-blind, placebo-controlled phase 2 trial.
Beslow, LA; Del Zoppo, GJ; Elm, JJ; Hinson, H; Jacobson, S; Kimberly, WT; Molyneaux, BJ; Ostwaldt, AC; Sheth, KN; Simard, JM; Sze, GK, 2016
)
0.97
" Compared to the high risk of TAK-875 induced liver toxicity, there was no significant adverse effects such as hepatic and renal toxicity were observed in the chronic toxicity studies of compound 20 even at the higher dose."( Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
Dai, Y; Huang, W; Li, H; Li, Z; Liao, C; Liu, C; Pan, M; Qian, H; Qiu, Q; Shi, W; Su, X; Xu, X; Yang, J, 2017
)
0.46
"However, glyburide is the optimumtreatment regarding the rate of glucose control, but withmore adverse outcomes."( Comparative efficacy and safety of oral antidiabetic drugs and insulin in treating gestational diabetes mellitus: An updated PRISMA-compliant network meta-analysis.
Liang, HL; Ma, SJ; Tan, HZ; Xiao, YN, 2017
)
0.87
" In comparison to systemic application, metformin displayed the most adverse effects in vitro in nearly all analyses, interestingly at serum equivalent concentrations."( Side effects of frequently used oral antidiabetics on wound healing in vitro.
Bachmann, HS; Besser, M; Koester, V; Severing, AL; Stuermer, EK; Terberger, N, 2019
)
0.51
"Chronic exposure to n-hexane, a widely used solvent in industry, causes sensorimotor neuropathy, which is mainly mediated by its toxic metabolite, 2,5-hexanedione (HD)."( Glibenclamide attenuates 2,5-hexanedione-induced neurotoxicity in the spinal cord of rats through mitigation of NLRP3 inflammasome activation, neuroinflammation and oxidative stress.
Hou, L; Huang, R; Li, S; Wang, Q; Yang, J; Zhang, D; Zhao, J, 2020
)
0.56
" Safety outcomes are all-cause 30-day mortality and early neurological deterioration, with a focus on cardiac- and glucose-related serious adverse events."( Safety and efficacy of glibenclamide combined with rtPA in acute cerebral ischemia with occlusion/stenosis of anterior circulation (SE-GRACE): study protocol for a randomized controlled trial.
Chen, P; Huang, K; Huang, W; Huang, Y; Ji, Z; Li, G; Pan, S; Weng, G; Wu, Y; Yang, G; Yang, Z; Zhou, S, 2020
)
0.56
"Currently, whether nod-like receptor family pyrin domain-containing 3 (NLRP3) inflammasome activation contributes to neuropathy induced by 2,5-Hexanedione (HD), the toxic metabolite of n-hexane, remains unknown."( NLRP3 inflammasome mediates 2,5-hexanedione-induced neurotoxicity through regulation of macrophage infiltration in rats.
Hou, L; Huang, R; Ruan, Z; Sun, W; Wang, Q; Zhang, D, 2020
)
0.56
" We compared the effects of three SU medications and initial SU doses on adverse glycemic and cardiovascular events among NH residents."( Comparative safety of sulfonylureas among U.S. nursing home residents.
Berry, SD; Hayes, KN; Munshi, MN; Riester, MR; Zullo, AR, 2023
)
0.91
"Unmetabolized human pharmaceuticals may enter aquatic environments, and potentially exert adverse effects on the survival of non-target organisms."( Exposure to low levels of antidiabetic glibenclamide had no evident adverse effects on intestinal microbial composition and metabolic profiles in amphibian larvae.
Chen, Y; Gao, JF; Liu, JH; Lu, HL; Meng, QY; Yang, JM, 2023
)
0.91

Pharmacokinetics

All pharmacokinetic parameters assessed for glyburide were statistically comparable between the two age groups with the exception of a shorter time to peak concentration in the elderly at weeks 0 and 12. No significant pharmacokinetics or pharmacodynamic interactions were observed between memantine and Glyburide/metformin.

ExcerptReferenceRelevance
"Complex pharmacokinetic perturbations follow kidney failure."( [Pharmacokinetic perturbations in kidney failure. Anomalies of metabolites and tissue diffusion (author's transl)].
Balant, L; Blanchard, P; Fabre, J; Rudhardt, M,
)
0.13
" The pharmacokinetic and pharmacodynamic properties of oral glibenclamide have been studied in 31 hospitalised in-patients and 79 ambulant out-patients with diabetes mellitus."( Pharmacokinetic and pharmacodynamic studies of glibenclamide in non-insulin dependent diabetes mellitus.
Coppack, SW; Lant, AF; McIntosh, CS; Rodgers, AV, 1990
)
0.28
"This investigation was carried out to evaluate the in vitro dissolution as well as the pharmacokinetic and pharmacodynamic properties of two tablet oral dosage forms of glibenclamide, Daonil (product A) and Glucomid (product B)."( Comparison of the pharmacokinetics and pharmacodynamics of two commercial products containing glibenclamide.
Abdel-Hamid, ME; el-Sayed, YM; Hasan, MM; Najib, NM; Sallam, ES; Shubair, MS; Suleiman, MS, 1989
)
0.28
" It is concluded that there is no consistent pharmacokinetic interaction between glibenclamide and trimethoprim-sulphamethoxazole in NIDDM patients."( Lack of pharmacokinetic interaction between glibenclamide and trimethoprim-sulphamethoxazole.
Christenson, I; Emilsson, H; Gunnarsson, R; Ostman, J; Sjöberg, S; Thunberg, E; Wiholm, BE,
)
0.13
" Both pharmacokinetic and pharmacodynamic factors may contribute to these differences."( Comparison of pharmacokinetics, metabolic effects and mechanisms of action of glyburide and glipizide during long-term treatment.
Fyhrquist, F; Groop, L; Groop, PH; Melander, A; Saloranta, C; Stenman, S; Tötterman, KJ,
)
0.36
"A system approach to the analysis of pharmacodynamic systems is applied to the relationship between the glyburide serum concentration (Cd) and a resulting pharmacologic effect response, that is, the C-peptide serum concentration (Cc) in patients with non-insulin dependent diabetes mellitus (NIDDM)."( A system approach to pharmacodynamics. II: Glyburide pharmacodynamics and estimation of optimal drug delivery.
Antal, EJ; Gillespie, WR; Phillips, JP; Veng-Pedersen, P, 1988
)
0.75
" In addition, the pharmacokinetic properties, spectrum and severity of side effects and metabolism of this agent are somewhat different from those of first-generation sulfonylureas."( Glipizide: a second-generation sulfonylurea hypoglycemic agent. Pharmacology, pharmacokinetics and clinical use.
Lebovitz, HE,
)
0.13
" The biologic half-life of glyburide is not significantly correlated with renal function in subjects with creatinine clearances of 30 ml/minute/1."( Pharmacokinetics of glyburide.
Pearson, JG, 1985
)
0.89
" For glucose, only Cmin values were found to be significantly lower following Euglucon."( Bioavailability and pharmacodynamics of a sustained-release glibenclamide product (Deroctyl) in comparison to a standard tablet formulation (Euglucon, Daonil).
Ayanoglu, G; Badian, M; Witte, PU, 1983
)
0.27
" Values of Cmax and AUC of glyburide showed an equality of the two treatments by the analysis of variance."( The influence of orlistat on the pharmacokinetics and pharmacodynamics of glyburide in healthy volunteers.
Freundlich, NL; Guerciolini, R; Koss-Twardy, SG; Melia, AT; Milla, G; Min, B; Patel, IH; Zhi, J, 1995
)
0.82
" Regression analysis between the pharmacokinetic variables and body weight status revealed statistically significant correlations between volume or clearance and body weight."( The pharmacokinetics and pharmacodynamics of 12 weeks of glyburide therapy in obese diabetics.
Antal, EJ; Jaber, LA; Slaughter, RL; Welshman, IR, 1993
)
0.53
"The aim of the study presented here was to determine possible pharmacokinetic interactions of moxonidine and glibenclamide at steady state in 18 healthy male volunteers."( Steady state investigation of possible pharmacokinetic interactions of moxonidine and glibenclamide.
Achtert, G; Dilger, C; Eden, G; Michaelis, K; Müller, M; Weber, W; Weimann, HJ,
)
0.13
" Cmax for RG was 212 +/- 41 ng."( Pharmacokinetics and relative bioavailability of tablet of micronized glibenclamide in 4 Chinese healthy men.
Cui, HD; Guo, Y; Jiang, WD; Karras, HO; Zhu, XX, 1993
)
0.29
" During 24-h pharmacokinetic determinations at weeks 0, 6, and 12, serial blood samples were obtained for glyburide determination with HPLC."( Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus.
Antal, EJ; Jaber, LA; Welshman, IR, 1996
)
0.77
"All pharmacokinetic parameters assessed for glyburide were statistically comparable between the two age groups with the exception of a shorter time to peak concentration in the elderly at weeks 0 and 12."( Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus.
Antal, EJ; Jaber, LA; Welshman, IR, 1996
)
0.82
" Observed pharmacodynamic differences indicate the necessity for dosage titration to a specified therapeutic response regardless of patient age."( Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus.
Antal, EJ; Jaber, LA; Welshman, IR, 1996
)
0.56
" Ibuprofen administration resulted in a slight increase in mean glyburide free fraction, but no significant changes in glyburide pharmacokinetic parameters were observed."( Effects of aspirin and ibuprofen on the pharmacokinetics and pharmacodynamics of glyburide in healthy subjects.
Antal, EJ; Juhl, RP; Kubacka, RT; Welshman, IR, 1996
)
0.76
" In conclusion, isolated mesenteric arteries from obese Zucker rats do not show relevant structural changes, and the pharmacodynamic behaviour of such vessels appears to be the same as that of control preparations."( Pharmacodynamic behaviour of isolated resistance vessels obtained from hypertensive-diabetic rats.
Kam, KL; Pfaffendorf, M; van Zwieten, PA, 1996
)
0.29
" An effect compartment was linked to appropriate pharmacokinetic models and pharmacokinetic and pharmacodynamic modelling was used to fit the pharmacokinetics of Gb by both routes and the metabolites for each individual."( Concentration-effect relations of glibenclamide and its active metabolites in man: modelling of pharmacokinetics and pharmacodynamics.
Jönsson, A; Karlsson, MO; Melander, A; Rydberg, T, 1997
)
0.3
" Pharmacokinetic analysis was performed with noncompartmental techniques."( The influence of bromfenac on the pharmacokinetics and pharmacodynamic responses to glyburide in diabetic subjects.
Boni, JP; Cevallos, WH; DeCleene, S; Korth-Bradley, JM,
)
0.36
"The aim of this series of studies was to determine the potential for pharmacokinetic interaction between candesartan (administered orally as the prodrug candesartan cilexetil) and hydrochlorothiazide (HCTZ), nifedipine, glibenclamide, warfarin, digoxin or the components of an oral contraceptive formulation."( Pharmacokinetic drug interaction studies with candesartan cilexetil.
Högemann, A; Jonkman, JH; Lins, R; Sennewald, R; van Heiningen, PN; van Lier, JJ, 1997
)
0.3
" Blood samples were taken to determine the pharmacokinetic characteristics of glibenclamide and the test/reference ratios were evaluated according to bioequivalence criteria."( Concomitant administration of the alpha-glucosidase inhibitor voglibose (AO-128) does not alter the pharmacokinetics of glibenclamide.
Ehrlich, A; Fuder, H; Kleist, P; Lücker, PW; Suzuki, Y; Timmer, W; Wetzelsberger, N, 1997
)
0.3
"Voglibose did not interact with glibenclamide on a pharmacokinetic level."( Concomitant administration of the alpha-glucosidase inhibitor voglibose (AO-128) does not alter the pharmacokinetics of glibenclamide.
Ehrlich, A; Fuder, H; Kleist, P; Lücker, PW; Suzuki, Y; Timmer, W; Wetzelsberger, N, 1997
)
0.3
" We have demonstrated Gb to have a terminal elimination half-life of 15 h, and the main metabolites have a hypoglycaemic effect."( Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function.
Jönsson, A; Melander, A; Rydberg, T; Sterner, G, 1998
)
0.3
" AUC and Cmax of Gb were lower and the clearance to bioavailability ratio (CL/f) was higher in the IRF group."( Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function.
Jönsson, A; Melander, A; Rydberg, T; Sterner, G, 1998
)
0.3
"The differences in AUC, Cmax and CL/f of Gb may be explained by a higher free fraction in the IRF group which would increase Gb metabolic clearance."( Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function.
Jönsson, A; Melander, A; Rydberg, T; Sterner, G, 1998
)
0.3
" The half-life of gliclazide was higher than that of the other three hypoglycemic agents in middle-aged subjects and was the sole to be significantly increased in aged subjects."( Pharmacokinetics of gliquidone, glibenclamide, gliclazide and glipizide in middle-aged and aged subjects.
Courtois, P; Herbaut, C; Malaisse, WJ; Sener, A; Turc, A, 1999
)
0.3
" Important interethnic pharmacodynamic and pharmacokinetic differences have been reported for several drugs."( Pharmacodynamics and pharmacokinetics of intravenous glibenclamide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" Pharmacodynamic results were calculated using net areas under the curves, with basal values set as zero."( Pharmacodynamics and pharmacokinetics of intravenous glibenclamide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" There were no interethnic differences in any of the pharmacokinetic parameters."( Pharmacodynamics and pharmacokinetics of intravenous glibenclamide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" In conclusion, minor pharmacodynamic but no pharmacokinetic differences were found between the two groups."( Pharmacodynamics and pharmacokinetics of intravenous glibenclamide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" Glucodynamic and pharmacokinetic parameters were determined over 6 h after insulin injection using clamp techniques."( Intramuscular injection of insulin lispro or soluble human insulin: pharmacokinetics and glucodynamics in Type 2 diabetes.
Bates, P; Kaliterna, D; Metelko, Z; Milicevic, Z; Profozic, V; Ristic, S; Seger, M; Woodworth, JR; Wyatt, J, 2001
)
0.31
" This study was conducted to investigate a possible pharmacokinetic interaction between bosentan and glyburide."( In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide.
Bodin, F; Clozel, M; Dingemanse, J; Treiber, A; van Giersbergen, PL, 2002
)
0.73
" The observed pharmacodynamic interaction between bosentan and glyburide in patients with chronic heart failure cannot be explained by a pharmacokinetic interaction."( In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide.
Bodin, F; Clozel, M; Dingemanse, J; Treiber, A; van Giersbergen, PL, 2002
)
0.76
"We conducted CYP2C9 genotyping for 29 healthy volunteers who had participated in our previous pharmacokinetic studies on glyburide or glimepiride."( Glyburide and glimepiride pharmacokinetics in subjects with different CYP2C9 genotypes.
Cascorbi, I; Kivistö, KT; Kroemer, HK; Neuvonen, PJ; Niemi, M; Timm, R, 2002
)
1.97
" Patients consumed standardised meals on the days when pharmacokinetic and pharmacodynamic evaluations were performed."( Pharmacokinetics and pharmacodynamics of glyburide/metformin tablets (Glucovance) versus equivalent doses of glyburide and metformin in patients with type 2 diabetes.
Donahue, SR; Patel, S; Turner, KC, 2002
)
0.58
" The mean glibenclamide peak concentration (C(max)) was significantly greater (approximately 16%) after glibenclamide/metformin treatment on both days 1 and 14."( Pharmacokinetics and pharmacodynamics of glyburide/metformin tablets (Glucovance) versus equivalent doses of glyburide and metformin in patients with type 2 diabetes.
Donahue, SR; Patel, S; Turner, KC, 2002
)
0.58
" The patches were subjected to skin irritation test (by both visual observation and histopathological evaluation), oral glucose tolerance test and pharmacokinetic evaluation in mice."( Glibenclamide transdermal patches: physicochemical, pharmacodynamic, and pharmacokinetic evaluations.
Mutalik, S; Udupa, N, 2004
)
0.32
" Given the renal tubular transport and extensive urinary excretion of memantine and metformin, it was of interest to assess the pharmacokinetic and pharmacodynamic interaction with glyburide/metformin."( Investigation of the pharmacokinetic and pharmacodynamic interactions between memantine and glyburide/metformin in healthy young subjects: a single-center, multiple-dose, open-label study.
Abramowitz, W; Chou, T; Rao, N; Ventura, D, 2005
)
0.74
"The primary goal of this study was to determine whether an in vivo pharmacokinetic or pharmacodynamic interaction exists between memantine (an uncompetitive, moderate-affinity, N-methyl-D-aspartate receptor antagonist with fast blocking/unblocking kinetics that is available in the United States for moderate to severe AD) and glyburide/metformin (a combination pharmacotherapy formulation approved for glycemic control in patients with type 2 diabetes mellitus)."( Investigation of the pharmacokinetic and pharmacodynamic interactions between memantine and glyburide/metformin in healthy young subjects: a single-center, multiple-dose, open-label study.
Abramowitz, W; Chou, T; Rao, N; Ventura, D, 2005
)
0.72
" Assessments included determination of pharmacokinetic parameters for memantine and the antidiabetic agents when administered alone and in combination, pharmacodynamic measurements of blood glucose levels, and analyses of tolerability."( Investigation of the pharmacokinetic and pharmacodynamic interactions between memantine and glyburide/metformin in healthy young subjects: a single-center, multiple-dose, open-label study.
Abramowitz, W; Chou, T; Rao, N; Ventura, D, 2005
)
0.55
" No significant pharmacokinetic or pharmacodynamic interactions were observed between memantine and glyburide/metformin."( Investigation of the pharmacokinetic and pharmacodynamic interactions between memantine and glyburide/metformin in healthy young subjects: a single-center, multiple-dose, open-label study.
Abramowitz, W; Chou, T; Rao, N; Ventura, D, 2005
)
0.76
"No pharmacokinetic interactions between memantine and glyburide/metformin were detected in this study of healthy young volunteers."( Investigation of the pharmacokinetic and pharmacodynamic interactions between memantine and glyburide/metformin in healthy young subjects: a single-center, multiple-dose, open-label study.
Abramowitz, W; Chou, T; Rao, N; Ventura, D, 2005
)
0.8
"CYP2C9 * 3 greatly affects both the pharmacokinetic profiles of glibenclamide and lornoxicam."( [Impact of cytochrome P450 CYP2C9 variant allele CYP2C9 * 3 on the pharmacokinetics of glibenclamide and lornoxicam in Chinese subjects].
Chen, XY; Guo, YJ; Si, DY; Zhang, YF; Zhong, DF; Zhou, H, 2005
)
0.33
"To investigate the pharmacokinetic interactions, safety, and tolerability of the combination of olmesartan medoxomil with glibenclamide."( Pharmacokinetics and safety of olmesartan medoxomil in combination with glibenclamide in healthy volunteers.
Bolbrinker, J; Huber, M; Kreutz, R, 2006
)
0.33
"With the exception of a slight shift of tmax values for glibenclamide, the concomitant administration of olmesartan medoxomil with glibenclamide had no significant effects on the steady-state pharmacokinetics of either agent."( Pharmacokinetics and safety of olmesartan medoxomil in combination with glibenclamide in healthy volunteers.
Bolbrinker, J; Huber, M; Kreutz, R, 2006
)
0.33
"To compare the performance of the standard lag time model (LAG model) with the performance of an analytical solution of the transit compartment model (TRANSIT model) in the evaluation of four pharmacokinetic studies with four different compounds."( Implementation of a transit compartment model for describing drug absorption in pharmacokinetic studies.
Jonker, DM; Karlsson, MO; Kerbusch, T; Savic, RM, 2007
)
0.34
"The population pharmacokinetic analyses were performed using NONMEM on concentration-time data of glibenclamide, furosemide, amiloride, and moxonidine."( Implementation of a transit compartment model for describing drug absorption in pharmacokinetic studies.
Jonker, DM; Karlsson, MO; Kerbusch, T; Savic, RM, 2007
)
0.34
" The parameter estimates related to the absorption differed between the two models while the estimates of the pharmacokinetic disposition parameters were similar."( Implementation of a transit compartment model for describing drug absorption in pharmacokinetic studies.
Jonker, DM; Karlsson, MO; Kerbusch, T; Savic, RM, 2007
)
0.34
" 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
" Meanwhile, in co-treated group, elimination rate constant (Ke) of glibenclamide was reduced while peak plasma concentration (C(max)), area under the plasma concentration vs time curve (AUC(0-14 h)) and elimination half-life (T(1/2Ke)) were increased significantly vs glibenclamide alone administered rats."( Effects of 18alpha-glycyrrhizin on the pharmacodynamics and pharmacokinetics of glibenclamide in alloxan-induced diabetic rats.
Ao, Y; Chen, J; Peng, RX; Yue, J, 2008
)
0.35
" Two studies were performed to determine the potential for pharmacokinetic and pharmacodynamic interactions between vildagliptin and the sulfonylurea, glyburide, or pioglitazone in patients with Type 2 diabetes."( Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with Type 2 diabetes.
Balez, S; Bullock, J; Dole, WP; He, YL; Jarugula, V; Ligueros-Saylan, M; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2008
)
0.75
" Changes in AUC and Cmax during combination treatment were small ( pound 15%), and 90% confidence intervals for the geometric mean ratios (drug coadministration/monotherapy) were generally contained within the acceptance range for bioequivalence (0."( Evaluation of pharmacokinetic and pharmacodynamic interaction between the dipeptidyl peptidase IV inhibitor vildagliptin, glyburide and pioglitazone in patients with Type 2 diabetes.
Balez, S; Bullock, J; Dole, WP; He, YL; Jarugula, V; Ligueros-Saylan, M; Riviere, GJ; Schwartz, S; Serra, D; Wang, Y, 2008
)
0.55
" The purpose of this work was to examine in the rat if such interaction involves pharmacokinetic mechanisms or is solely limited to the pharmacodynamic level."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.35
" To evaluate the possibility of a pharmacokinetic interaction, the oral bioavailability of diclofenac (18 mg/kg) was studied in presence and the absence of glibenclamide (10 mg/kg)."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.35
" Notwithstanding, the interaction does no appear to involve pharmacokinetic mechanisms, as oral glibenclamide failed to produce any significant alteration in oral diclofenac bioavailability."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.35
" This interaction, however, appears due solely to a pharmacodynamic mechanisms as diclofenac pharmacokinetics are not altered."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.35
" Potential pharmacokinetic (PK) drug-drug interactions of alogliptin with pioglitazone or glyburide were evaluated in healthy adults."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.85
" However, by means of pharmacokinetic modeling we describe the inverse correlation between lipid solubility of a molecule and its active transport by placental ABC efflux transporters."( Transplacental pharmacokinetics of glyburide, rhodamine 123, and BODIPY FL prazosin: effect of drug efflux transporters and lipid solubility.
Ceckova, M; Cygalova, LH; Hofman, J; Staud, F, 2009
)
0.63
" Therefore, in view of the vast clinical uses and interactions of NSAIDs with commonly used therapeutic agents, the interaction of the NSAID diclofenac and glibenclamide was investigated about pharmacokinetic profile and antinociceptive effect in rats."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.35
" In pharmacokinetic interaction study, no significant (P>0."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.35
" Likewise, the validated assay had sufficient accuracy and precision for pharmacokinetic determination of diclofenac in the rat."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.35
" The half-life of GLB depletion in hepatic S-9 fractions of pregnant mice was significantly shorter than that of nonpregnant mice."( Increased glyburide clearance in the pregnant mouse model.
Hebert, MF; Mao, Q; Unadkat, JD; Zhang, Y; Zhou, L, 2010
)
0.76
" However, this was not seen as clinically relevant due to the absence of a reliable dose-response relationship and the known large pharmacokinetic interindividual variability of glyburide."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.77
" In co-treated group, the pharmacokinetic parameters like clearance (27."( Influence of atorvastatin on the pharmacokinetics and pharmacodynamics of glyburide in normal and diabetic rats.
Gade, J; Neerati, P, 2011
)
0.6
"To evaluate the pharmacokinetic interactions of the potent, selective, dipeptidyl peptidase-4 inhibitor, saxagliptin, in combination with metformin, glyburide or pioglitazone."( Saxagliptin, a potent, selective inhibitor of DPP-4, does not alter the pharmacokinetics of three oral antidiabetic drugs (metformin, glyburide or pioglitazone) in healthy subjects.
Boulton, DW; Brenner, E; Handschuh del Corral, M; Komoroski, B; Kornhauser, D; Li, L; Patel, CG; Vachharajani, N, 2011
)
0.77
" LC-MS/MS was utilized to determine the concentration of glibenclamide in rat plasma and to calculate the corresponding pharmacokinetic parameters."( Effects of HuangKui capsules on glibenclamide pharmacokinetics in rats.
Gao, X; Ju, W; Liu, S; Liu, Z; Tan, H; Yang, C; Zhou, L, 2012
)
0.38
" The novel compound linagliptin has important different pharmacokinetic (PK) properties, when compared with previously commercialized DPP-4 inhibitors, which may offer some advantages in clinical practice."( Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation).
Scheen, AJ, 2011
)
0.37
" In contrast, there were no significant differences in any of the pharmacokinetic parameters for warfarin between the two genotypes."( Pharmacogenomic/pharmacokinetic assessment of a four-probe cocktail for CYPs and OATPs following oral microdosing.
Ando, Y; Deguchi, M; Fukae, M; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kanda, E; Kimura, M; Maeda, K; Matsuguma, K; Matsuki, S; Nakamura, T; Sugiyama, Y, 2012
)
0.38
"The present study suggests that 1) the sampling strategy should be optimized according to pharmacokinetic profiles of the test drugs following oral microdosing, and 2) microdosing can be applied to the pharmacogenomic study of CYP-specific drugs."( Pharmacogenomic/pharmacokinetic assessment of a four-probe cocktail for CYPs and OATPs following oral microdosing.
Ando, Y; Deguchi, M; Fukae, M; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kanda, E; Kimura, M; Maeda, K; Matsuguma, K; Matsuki, S; Nakamura, T; Sugiyama, Y, 2012
)
0.38
" An ultra performance liquid chromatography-tandem mass spectrometry method was developed to determine the concentrations of glibenclamide and puerarin in rat plasma for the study of pharmacokinetic interaction between them."( Determination of glibenclamide and puerarin in rat plasma by UPLC-MS/MS: application to their pharmacokinetic interaction study.
Deng, Y; Li, F; Li, N; Qiao, Y; Wang, D, 2013
)
0.39
"We studied if the clinical pharmacokinetics and drug-drug interactions (DDIs) of the sulfonylurea-derivative glibenclamide can be simulated via a physiologically-based pharmacokinetic modeling approach."( Semi-mechanistic physiologically-based pharmacokinetic modeling of clinical glibenclamide pharmacokinetics and drug-drug-interactions.
Benne, MS; Greupink, R; Huisman, MT; Russel, FG; Schreurs, M, 2013
)
0.39
" Pharmacokinetic parameters were estimated by model-independent methods."( An open-label drug-drug interaction study of the steady-state pharmacokinetics of topiramate and glyburide in patients with type 2 diabetes mellitus.
Curtin, CR; Ford, L; Heald, DL; Manitpisitkul, P; Shalayda, K; Wang, SS, 2013
)
0.61
"The study was aimed to evaluate various pharmacokinetic parameters of a commercially available fixed dose combination of oral antidiabetics (Metformin/Glibenclamide 500/5mg tablets) in plasma sample of normal healthy adult male volunteers by applying an accurate, selective, and reproducible HPLC-UV analytical method for quantification of Metformin HCL and Glibenclamide simultaneously in a single chromatographic run."( Pharmacokinetic studies of metformin and glibenclamide in normal human volunteers.
Ahmad, M; Hassan, IJ; Malik, MZ; Minhas, MU; Rashid, A, 2014
)
0.4
"The purpose of this study is to characterize the involvement of hepato-biliary transport and cytochrome-P450 (CYP)-mediated metabolism in the disposition of glyburide and predict its pharmacokinetic variability due to drug interactions and genetic variations."( Mechanism-based pharmacokinetic modeling to evaluate transporter-enzyme interplay in drug interactions and pharmacogenetics of glyburide.
Bi, YA; Goosen, TC; Lin, J; Rotter, CJ; Scialis, RJ; Varma, MV; Yang, X, 2014
)
0.81
" Niosomal gels were prepared by incorporating the optimized niosomes into a gel base containing Carbopol 934 and evaluated for viscosity, in-vitro diffusion and in-vivo pharmacodynamic activity."( Formulation and pharmacodynamic evaluation of glibenclamide incorporated niosomal gel.
Gutta, TC; Satyanarayana, RP; Vadlamudi, HC; Vandana, K; Vulava, J; Yalavarthi, PR, 2014
)
0.4
"The niosomal gel of glibenclamide had released the drug in well controlled manner which is supported by pharmacodynamic activity with evidence of consistent lowering of blood glucose levels."( Formulation and pharmacodynamic evaluation of glibenclamide incorporated niosomal gel.
Gutta, TC; Satyanarayana, RP; Vadlamudi, HC; Vandana, K; Vulava, J; Yalavarthi, PR, 2014
)
0.4
"Glibenclamide and thymoquinone plasma concentrations were analysed using a sensitive RP-HPLC method, and non-compartmental model pharmacokinetic parameters were calculated."( Effects of Thymoquinone on the Pharmacokinetics and Pharmacodynamics of Glibenclamide in a Rat Model.
Ahmad, A; Al-Jenoobi, FI; Al-Mohizea, AM; Alkharfy, KM; Khan, RM; Raish, M, 2015
)
0.42
"01) all the pharmacokinetic parameters, such as Cmax, AUC0-n, AUCtotal, t1/2, and mean residence time, and decreased the clearance, Vd, markedly as compared with the control group."( Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling.
Samala, S; Veeresham, C, 2016
)
0.65
" Pharmacokinetic parameters were assessed at prespecified intervals."( Effect of canagliflozin on the pharmacokinetics of glyburide, metformin, and simvastatin in healthy participants.
Devineni, D; Mamidi, RN; Manitpisitkul, P; Murphy, J; Skee, D; Stieltjes, H; Tian, H; Usiskin, K; Vandebosch, A; Verhaeghe, T; Wajs, E; Wang, SS,
)
0.38
" This clinical pharmacology study was designed to investigate the potential glucose-lowering effect or pharmacodynamic (PD), pharmacokinetic (PK), and safety/tolerability interactions between piragliatin and glyburide in T2D patients already taking glyburide but not adequately controlled."( Pharmacokinetic and Pharmacodynamic Drug Interaction Study of Piragliatin, a Glucokinase Activator, and Glyburide, a Sulfonylurea, in Type 2 Diabetic Patients.
Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016
)
0.84
" We studied the mechanisms involved in the disposition of glyburide and its pharmacologically active hydroxy metabolites M1 and M2b and evaluated their clinical pharmacokinetics and the potential role in glyburide-induced cholestasis employing physiologically based pharmacokinetic (PBPK) modeling."( Transporter-Mediated Disposition, Clinical Pharmacokinetics and Cholestatic Potential of Glyburide and Its Primary Active Metabolites.
Bi, YA; Li, R; Lin, J; Marroquin, LD; Mathialagan, S; Scialis, RJ; Varma, MVS; Vildhede, A; Yang, X, 2017
)
0.92
" This study aims to investigate the implications of type 2 diabetes (T2DM) on the pharmacokinetics of carvedilol enantiomers using an integrated population pharmacokinetic modelling approach."( Population pharmacokinetics of carvedilol enantiomers and their metabolites in healthy subjects and type-2 diabetes patients.
Coelho, EB; Della Pasqua, O; Lanchote, VL; Nardotto, GHB, 2017
)
0.46
" TCE was co- administered in three different groups (0, 100 and 400 mg/kg) with Glibenclamide at 1 mg/kg dose to observe the alteration in pharmacokinetic parameters of Glibenclamide."( Effect of Tinospora cordifolia aqua-alcoholic extract on pharmacokinetic of Glibenclamide in rat: An herb-drug interaction study.
Ahmed, T; Punde, R; Sahu, R; Sangana, R; Subudhi, BB, 2018
)
0.48
" In addition, the pharmacodynamic and pharmacokinetic studies in New Zealand rabbits were performed using the optimized mini-tablet formulation."( Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance.
Abdellatif, AAH; El Hamd, MA; Roberts, M; Tawfeek, HM; Younis, MA, 2018
)
0.48
" The previously reported compound 2 is a highly potent FFA1 agonist, but it might be suffered from poor pharmacokinetic properties because the phenylpropanoic acid is vulnerable to β-oxidation."( Design, synthesis and biological activity of deuterium-based FFA1 agonists with improved pharmacokinetic profiles.
Chen, H; Deng, F; Deng, L; Li, Y; Li, Z; Liao, R; Liu, B; Zeng, X; Zhang, L, 2019
)
0.51
" This study evaluates the anti-diabetic effect of cumin and glyburide in the streptozotocin induced diabetes model in rats, and investigates their pharmacodynamic interactions and its implication in diabetes."( Pharmacodynamic interaction of cumin seeds (Cuminum cyminum L.) with glyburide in diabetes.
Invally, M; Kaur, G; Tharappel, LJP; Upadhyay, N, 2019
)
0.99
" We previously constructed a physiologically-based pharmacokinetic (PBPK) model of rifampicin accounting for the components for the induction of cytochrome P450 (CYP) 3A/CYP2C9 and the inhibition of organic anion transporting polypeptide 1B (OATP1B)."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
0.51
" Data are limited regarding the pharmacodynamic effects of metformin and glyburide during pregnancy."( Pharmacodynamics of Glyburide, Metformin, and Glyburide/Metformin Combination Therapy in the Treatment of Gestational Diabetes Mellitus.
Ahmed, MS; Brown, LM; Brown, Z; Caritis, S; Clark, S; Easterling, TR; Flood Nichols, SK; Haas, DM; Haneline, LS; Hebert, MF; Ma, X; Manuck, TA; Quinney, SK; Ren, Z; Shen, DD; Shireman, LM; Shuster, DL; Thummel, KE; Tita, AT; Venkataramanan, R, 2020
)
1.11
"This study is conducted to compare the pharmacokinetic profiles of two fixed dose combination of metformin/glibenclamide tablets (500mg/5 mg per tablet)."( Bioequivalence and pharmacokinetic comparison of two fixed dose combination of Metformin/ Glibenclamide formulations in healthy subjects under fed condition.
Ang, JY; Chang, CT; Chin, SK; Lim, AB; Tan, SS; Tan, WH; Wong, JM; Yuen, KH, 2020
)
0.56
" In silico analysis of the pharmacokinetic and toxicity properties of the compound was also performed."( Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one.
Adongo, DW; Amponsah, IK; Baah, MK; Ben, IO; Fleischer, TC; Harley, BK; Mensah, AY; Mireku-Gyimah, NA, 2021
)
0.62
" Here, we seek to identify pharmacodynamic markers of edema that are modified by intravenous (i."( Hypoxanthine is a pharmacodynamic marker of ischemic brain edema modified by glibenclamide.
Acharjee, A; Ament, Z; Hinson, HE; Irvine, HJ; Kimberly, WT; Molyneaux, BJ; Sheth, KN; Simard, JM; Wolcott, Z, 2022
)
0.72
" Blood samples were collected from 24 blood collection sites per cycle for pharmacokinetic analysis until 36 hours after oral administration."( Pharmacokinetic and Bioequivalence Studies of 2 Metformin Glibenclamide Tablets in Healthy Chinese Subjects Under Fasting and Fed Conditions.
Chen, L; Huang, J; Huang, X; Li, X, 2023
)
0.91

Compound-Compound Interactions

Study 2 was a 104-week, multicentre, randomized, double blind and active-controlled study of nateglinide (120 mg, before meals) or glyburide (up to 5 mg bid) in combination with metformin. Study 2 involved 69 treatment-naïve patients with T2DM aged >or=65 years.

ExcerptReferenceRelevance
"To compare the effect of morning and bedtime NPH insulin combined with daytime sulfonylurea on glycemic control in non-insulin-dependent diabetes mellitus (NIDDM) patients no longer responding to treatment with sulfonylureas alone."( Morning or bedtime NPH insulin combined with sulfonylurea in treatment of NIDDM.
Ekstrand, A; Eriksson, JG; Franssila-Kallunki, A; Groop, LC; Saloranta, C; Schalin-Jäntti, C; Widén, E, 1992
)
0.28
"Morning and bedtime NPH insulin combined with glibenclamide are equipotent in the treatment of NIDDM patients with secondary failure to sulfonylurea."( Morning or bedtime NPH insulin combined with sulfonylurea in treatment of NIDDM.
Ekstrand, A; Eriksson, JG; Franssila-Kallunki, A; Groop, LC; Saloranta, C; Schalin-Jäntti, C; Widén, E, 1992
)
0.28
"To compare the effect of bedtime NPH insulin or preprandial regular insulin combined with glibenclamide on metabolic control in non-insulin-dependent diabetes mellitus (NIDDM) patients with secondary failure to sulfonylurea therapy."( Comparison of bedtime NPH or preprandial regular insulin combined with glibenclamide in secondary sulfonylurea failure.
Adamson, U; Arner, P; Bolinder, J; Landstedt-Hallin, L; Lins, PE, 1995
)
0.29
"Eighty NIDDM patients were randomized to treatment with either three preprandial doses of regular insulin (daytime group D) or a bedtime dose of NPH insulin (nocturnal insulinization, group N), both regimens being combined with 10."( Comparison of bedtime NPH or preprandial regular insulin combined with glibenclamide in secondary sulfonylurea failure.
Adamson, U; Arner, P; Bolinder, J; Landstedt-Hallin, L; Lins, PE, 1995
)
0.29
" Candesartan cilexetil was well tolerated both alone and in combination with the other agents."( Pharmacokinetic drug interaction studies with candesartan cilexetil.
Högemann, A; Jonkman, JH; Lins, R; Sennewald, R; van Heiningen, PN; van Lier, JJ, 1997
)
0.3
"Glibenclamide in combination with Kelening in the treatment of NIDDM is more effective and less toxic, and the combination may reduce the dosage of glibenclamide in NIDDM."( [Clinical study of glibenclamide in combination with kelening treatment in non-insulin dependent diabetes mellitus].
Zhou, P, 1997
)
0.3
"To compare the effects of bedtime NPH Insulin vs Metformin combined with Glibenclamide in patients who are obese and had secondary failure to sulphonylurea treatment."( Comparison of bedtime NPH insulin or metformin combined with glibenclamide in secondary sulphonylurea failure in obese type II (NIDDM) patients.
Muzaffar, Z; Niazi, R, 1998
)
0.3
"Many hospital admissions of elderly patients for drug toxicity occur after administration of a drug known to cause drug-drug interactions."( Drug-drug interactions among elderly patients hospitalized for drug toxicity.
Juurlink, DN; Kopp, A; Laupacis, A; Mamdani, M; Redelmeier, DA, 2003
)
0.32
" Data have been lacking on their use in combination with both sulfonylurea and metformin among patients of type 2 diabetes who are on insulin therapy secondary to failure of routine oral hypoglycemic drugs in controlling their diabetes."( Beneficial effects of triple drug combination of pioglitazone with glibenclamide and metformin in type 2 diabetes mellitus patients on insulin therapy.
Chandalia, HB; Fafadia, A; Joshi, SR; Panikar, V; Santvana, C, 2003
)
0.32
"To determine the effects of pioglitazone in combination with sulphonylurea and metformin on diabetes control in patients being treated with insulin due to secondary failure of oral hypoglycemic agents."( Beneficial effects of triple drug combination of pioglitazone with glibenclamide and metformin in type 2 diabetes mellitus patients on insulin therapy.
Chandalia, HB; Fafadia, A; Joshi, SR; Panikar, V; Santvana, C, 2003
)
0.32
" They were switched on to triple drug combination of glibenclamide 5 mg, metformin 500 mg and pioglitazone 15 mg along with insulin."( Beneficial effects of triple drug combination of pioglitazone with glibenclamide and metformin in type 2 diabetes mellitus patients on insulin therapy.
Chandalia, HB; Fafadia, A; Joshi, SR; Panikar, V; Santvana, C, 2003
)
0.32
"7 ng h/ml in combination with glibenclamide; the corresponding Css,max values were 479."( Pharmacokinetics and safety of olmesartan medoxomil in combination with glibenclamide in healthy volunteers.
Bolbrinker, J; Huber, M; Kreutz, R, 2006
)
0.33
"Metformin is widely used in the management of type 2 diabetes, either as monotherapy or in combination with other oral antihyperglycemic agents such as sulfonylureas and thiazolidinediones."( Comparison of extended-release metformin in combination with a sulfonylurea (glyburide) to sulfonylurea monotherapy in adult patients with type 2 diabetes: a multicenter, double-blind, randomized, controlled, phase III study.
Lewin, A; Lipetz, R; Schwartz, S; Wu, J, 2007
)
0.57
"The purpose for this study was to compare the efficacy and tolerability of extended-release metformin (MER) administered with a sulfonylurea (glyburide) to sulfonylurea monotherapy in patients with type 2 diabetes."( Comparison of extended-release metformin in combination with a sulfonylurea (glyburide) to sulfonylurea monotherapy in adult patients with type 2 diabetes: a multicenter, double-blind, randomized, controlled, phase III study.
Lewin, A; Lipetz, R; Schwartz, S; Wu, J, 2007
)
0.77
"The aim of this work was to assess the efficacy and tolerability of nateglinide alone or in combination with metformin in elderly patients with type 2 diabetes (T2DM)."( Nateglinide, alone or in combination with metformin, is effective and well tolerated in treatment-naïve elderly patients with type 2 diabetes.
Baron, MA; Gerich, JE; Jean-Louis, L; Marcellari, A; Purkayastha, D; Schwarz, SL, 2008
)
0.35
" Study 2 was a 104-week, multicentre, randomized, double blind and active-controlled study of nateglinide (120 mg, before meals) or glyburide (up to 5 mg bid) in combination with metformin (up to 1000 mg bid) in 69 treatment-naïve patients with T2DM aged >or=65 years."( Nateglinide, alone or in combination with metformin, is effective and well tolerated in treatment-naïve elderly patients with type 2 diabetes.
Baron, MA; Gerich, JE; Jean-Louis, L; Marcellari, A; Purkayastha, D; Schwarz, SL, 2008
)
0.55
"Initial drug treatment with nateglinide, alone or in combination with metformin, is well tolerated and produces clinically meaningful improvements in glycaemic control in elderly patients with T2DM."( Nateglinide, alone or in combination with metformin, is effective and well tolerated in treatment-naïve elderly patients with type 2 diabetes.
Baron, MA; Gerich, JE; Jean-Louis, L; Marcellari, A; Purkayastha, D; Schwarz, SL, 2008
)
0.35
" Potential pharmacokinetic (PK) drug-drug interactions of alogliptin with pioglitazone or glyburide were evaluated in healthy adults."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.85
" As a result, OATP1B1 and OATP1B3 represent sites for potential drug-drug interactions."( Fluorescence-based assays for the assessment of drug interaction with the human transporters OATP1B1 and OATP1B3.
Bednarczyk, D, 2010
)
0.36
" This study investigated the hypothesis that the common antidiabetic drugs glibenclamide and metformin, in combination with tualang honey, offer additional protection for the pancreas of streptozotocin (STZ)-induced diabetic rats against oxidative stress and damage."( Antioxidant protective effect of glibenclamide and metformin in combination with honey in pancreas of streptozotocin-induced diabetic rats.
Erejuwa, OO; Gurtu, S; Salam, SK; Salleh, MS; Sulaiman, SA; Wahab, MS, 2010
)
0.36
" Based on laboratory findings, we determined the clinical significance of potential CYP2C9-mediated drug-drug interactions in hospitalized patients receiving glibenclamide, glimepiride or glipizide, all of which are metabolized by CYP2C9, together with a CYP2C9 inhibitor."( Potential CYP2C9-mediated drug-drug interactions in hospitalized type 2 diabetes mellitus patients treated with the sulphonylureas glibenclamide, glimepiride or glipizide.
Heikkilä, P; Huupponen, R; Laine, K; Tirkkonen, T, 2010
)
0.36
"Almost 20% of patients were exposed to a potential drug-drug interaction with a CYP2C9 inhibitor during sulphonylurea treatment."( Potential CYP2C9-mediated drug-drug interactions in hospitalized type 2 diabetes mellitus patients treated with the sulphonylureas glibenclamide, glimepiride or glipizide.
Heikkilä, P; Huupponen, R; Laine, K; Tirkkonen, T, 2010
)
0.36
"05) reduced hyperglycemia, glibenclamide or metformin combined with honey produced significantly much lower blood glucose (8."( Glibenclamide or metformin combined with honey improves glycemic control in streptozotocin-induced diabetic rats.
Erejuwa, OO; Gurtu, S; Salleh, MS; Sirajudeen, KN; Sulaiman, SA; Wahab, MS, 2011
)
0.37
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"To compare pioglitazone or glibenclamide alone and in combination with rosuvastatin on hepatic steatosis in type 2 diabetic patients."( Ultrasonography modifications of visceral and subcutaneous adipose tissue after pioglitazone or glibenclamide therapy combined with rosuvastatin in type 2 diabetic patients not well controlled by metformin.
D'Angelo, A; Derosa, G; Fogari, E; Maffioli, P; Perrone, T, 2013
)
0.39
"The objective was to study the of drug-drug interaction between voriconazole and oral hypoglycemic agents in normal and alloxan induced diabetic rats."( Drug-drug interaction between voriconazole and oral hypoglycemic agents in diabetic rats.
Diwan, PV; Joshi, B; Kumar, BH; Singh, JC,
)
0.13
"We studied if the clinical pharmacokinetics and drug-drug interactions (DDIs) of the sulfonylurea-derivative glibenclamide can be simulated via a physiologically-based pharmacokinetic modeling approach."( Semi-mechanistic physiologically-based pharmacokinetic modeling of clinical glibenclamide pharmacokinetics and drug-drug-interactions.
Benne, MS; Greupink, R; Huisman, MT; Russel, FG; Schreurs, M, 2013
)
0.39
" Because topiramate and antidiabetic drugs may be co-administered, the potential drug-drug interactions between topiramate and glyburide (glibenclamide), a commonly used sulfonylurea antidiabetic agent, was evaluated at steady state in patients with type 2 diabetes mellitus (T2DM)."( An open-label drug-drug interaction study of the steady-state pharmacokinetics of topiramate and glyburide in patients with type 2 diabetes mellitus.
Curtin, CR; Ford, L; Heald, DL; Manitpisitkul, P; Shalayda, K; Wang, SS, 2013
)
0.81
" We aimed to compare mortality and cardiovascular risk among users of metformin in combination with pharmacologically different ISs."( Metformin in combination with various insulin secretagogues in type 2 diabetes and associated risk of cardiovascular morbidity and mortality--a retrospective nationwide study.
Andersson, C; Fosbøl, EL; Gislason, G; Køber, L; Mogensen, UM; Scheller, NM; Schramm, TK; Torp-Pedersen, C; Vaag, A, 2015
)
0.42
"Most ISs in combination with metformin were associated with similar mortality and cardiovascular risk."( Metformin in combination with various insulin secretagogues in type 2 diabetes and associated risk of cardiovascular morbidity and mortality--a retrospective nationwide study.
Andersson, C; Fosbøl, EL; Gislason, G; Køber, L; Mogensen, UM; Scheller, NM; Schramm, TK; Torp-Pedersen, C; Vaag, A, 2015
)
0.42
" We aimed to systematically screen for drugs that interact with the five most commonly used secretagogues-glipizide, glyburide, glimepiride, repaglinide, and nateglinide-to cause serious hypoglycemia."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.66
" We first predicted the drug-drug interaction potential based on the pharmacokinetics of each secretagogue-precipitant pair."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
"We predicted 34 pharmacokinetic drug-drug interactions with the secretagogues, nine moderate and 25 weak."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
"The self-controlled case series design has the potential to be widely applicable to screening for drug-drug interactions that lead to adverse outcomes identifiable in healthcare databases."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
"We compared the individual effects of mitiglinide and glibenclamide administered in combination with the dipeptidyl peptidase-IV (DPP-IV) inhibitor sitagliptin on plasma DPP-IV activity and blood glucose levels in rats with streptozotocin-nicotinamide-induced type 2 diabetes (STZ-NA rats)."( Comparison of the Effects of Mitiglinide and Glibenclamide Administered in Combination with the Dipeptidyl Peptidase-IV Inhibitor Sitagliptin in Rats with Streptozotocin-Nicotinamide-Induced Type 2 Diabetes.
Akahane, K; Inoue, T; Kiguchi, S; Kobayashi, M; Ojima, K; Takeda, H; Tatemichi, S; Yokoyama, A, 2017
)
0.46
"This study aimed to construct a physiologically based pharmacokinetic (PBPK) model of rifampicin that can accurately and quantitatively predict complex drug-drug interactions (DDIs) involving its saturable hepatic uptake and auto-induction."( Comprehensive PBPK Model of Rifampicin for Quantitative Prediction of Complex Drug-Drug Interactions: CYP3A/2C9 Induction and OATP Inhibition Effects.
Asaumi, R; Hashizume, K; Imawaka, H; Lee, W; Nunoya, KI; Sugiyama, Y; Tobe, Y; Toshimoto, K, 2018
)
0.48
"d for 14 days and on the 14th day all three groups were administered with 1 mg/kg Glibenclamide."( Effect of Tinospora cordifolia aqua-alcoholic extract on pharmacokinetic of Glibenclamide in rat: An herb-drug interaction study.
Ahmed, T; Punde, R; Sahu, R; Sangana, R; Subudhi, BB, 2018
)
0.48
" Resveratrol alone and its combination with glibenclamide decreased the arrhythmia score, the arrhythmic period and the incidence of other types of arrhythmias during the reperfusion period."( The protection of resveratrol and its combination with glibenclamide, but not berberine on the diabetic hearts against reperfusion-induced arrhythmias: the role of myocardial K
Bozdogan, O; Eksioglu, D; Erim, F; Firat, T; Kaya, ST; Ozarslan, TO; Taskin, E; Yasar, S, 2019
)
0.51
"to investigate possible beneficial effects of hydroalcoholic extract of SecurigeraSecuridaca seed (HESS) on antioxidant capacity, fibroblast growth factor 21 (FGF21) and insulin resistance in Streptozotocin (STZ)-induced diabetic rats, alone and in combination with glibenclamide."( Effects of Securigera Securidaca seed extract in combination with glibenclamide on antioxidant capacity, fibroblast growth factor 21 and insulin resistance in hyperglycemic rats.
Alizadeh-Fanalou, S; Azadi, N; Babaei, M; Bahreini, E; Borji, M; Hosseini, A; Malekinejad, H; Nazarizadeh, A; Shojaii, A, 2020
)
0.56
"Forty male Wistar rats were randomly divided in to eight equal groups including healthy and diabetic controls and six treated groups with a various doses of HESS alone and in combination with glibenclamide, for 35 consecutive days."( Effects of Securigera Securidaca seed extract in combination with glibenclamide on antioxidant capacity, fibroblast growth factor 21 and insulin resistance in hyperglycemic rats.
Alizadeh-Fanalou, S; Azadi, N; Babaei, M; Bahreini, E; Borji, M; Hosseini, A; Malekinejad, H; Nazarizadeh, A; Shojaii, A, 2020
)
0.56
" This study investigates the safety and efficacy of glibenclamide combined with rtPA in treating AIS patients."( Safety and efficacy of glibenclamide combined with rtPA in acute cerebral ischemia with occlusion/stenosis of anterior circulation (SE-GRACE): study protocol for a randomized controlled trial.
Chen, P; Huang, K; Huang, W; Huang, Y; Ji, Z; Li, G; Pan, S; Weng, G; Wu, Y; Yang, G; Yang, Z; Zhou, S, 2020
)
0.56

Bioavailability

Glyburide is a poorly water-soluble oral hypoglycemic agent, with problems of variable bioavailability and bio-inequivalence. Complexation with HBenBCD may be an effective way to increase the bioavailability of glyburide.

ExcerptReferenceRelevance
" The method should be of interest in the quality control of drugs that may cause bioavailability problems because of dissolution rate-limited absorption."( New method for characterizing dissolution properties of drug powders.
Pedersen, PV, 1977
)
0.26
" A 33% increase in bioavailability of glibenclamide emerged, as seen from the respective AUC values, but no clinically remarkable effect was observed in the subjects."( Influence of antacids on the bioavailability of glibenclamide.
Avico, U; Federzoni, G; Pacifici, R; Pichini, S; Pini, LA; Sternieri, E; Zuccaro, P, 1989
)
0.28
" The bioavailability and pharmacodynamic studies were carried out on 16 healthy male adult volunteers who received a single dose of each product in a double-blind crossover design."( Comparison of the pharmacokinetics and pharmacodynamics of two commercial products containing glibenclamide.
Abdel-Hamid, ME; el-Sayed, YM; Hasan, MM; Najib, NM; Sallam, ES; Shubair, MS; Suleiman, MS, 1989
)
0.28
" Time point comparisons were employed to exclude clinically relevant changes of glibenclamide bioavailability and kinetics."( Glibenclamide steady state plasma levels during concomitant vinpocetine administration in type II diabetic patients.
Braun, W; Frercks, HJ; Grandt, R; Lührmann, B; Schulz, HU, 1989
)
0.28
" The two dissolution methods yielded different rank orders of ease of dissolution of the drug from the various preparations; the findings of neither dissolution method correlated adequately with the results of the in vivo bioavailability studies, which correctly predicted the abilities of the preparations to reduce plasma glucose concentrations."( Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide.
Chalk, JB; Eadie, MJ; Patterson, M; Smith, MT, 1986
)
0.27
" Additionally, glyburide does not appear to interact with other medications and is well absorbed from the gastrointestinal tract."( Review of glyburide after one year on the market.
Feldman, JM, 1985
)
1.02
" Post-dose glipizide concentrations were three times higher than those of glibenclamide, due to the incomplete bioavailability of the latter."( Pharmacokinetics and metabolic effects of glibenclamide and glipizide in type 2 diabetics.
Fyhrqvist, F; Groop, L; Groop, PH; Melander, A; Tolppanen, EM; Tötterman, KJ; Wåhlin-Boll, E, 1985
)
0.27
"Pharmacodynamics and tolerance, as well as the bioavailability of two oral dosage forms of 5 mg glibenclamide were determined in eight healthy male volunteers in a double-blind crossover study."( Bioavailability and pharmacodynamics of a sustained-release glibenclamide product (Deroctyl) in comparison to a standard tablet formulation (Euglucon, Daonil).
Ayanoglu, G; Badian, M; Witte, PU, 1983
)
0.27
" Glyburide and glipizide are well absorbed after oral administration."( Glyburide and glipizide, second-generation oral sulfonylurea hypoglycemic agents.
Prendergast, BD,
)
2.48
" Peak concentrations, times-to-peak concentration, elimination half-lives and the extent of bioavailability of the drug were not significantly modified by acarbose."( Glibenclamide pharmacokinetics in acarbose-treated type 2 diabetics.
Gerard, J; Lefebvre, PJ; Luyckx, AS, 1984
)
0.27
" Food intake did not influence the bioavailability of a 5 mg dose of glibenclamide."( Serum glibenclamide in diabetic patients, and influence of food on the kinetics and effects of glibenclamide.
Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1980
)
0.26
" Food did not affect the bioavailability of any of the four drugs, but delayed Gz absorption."( Kinetics-effect relations of glipizide and other sulfonylureas.
Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1980
)
0.26
" The bioavailability of glipizide was apparently greater than that of glibenclamide."( Comparative single-dose kinetics and effects of four sulfonylureas in healthy volunteers.
Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1980
)
0.26
"For glibenclamide bioavailability studies in serum, high-performance liquid column and thin-layer chromatographic methods were introduced."( High-performance liquid column and thin-layer chromatographic determination of human serum glibenclamide at therapeutic levels.
Sistovaris, N; Uihlein, M, 1982
)
0.26
" In the presence of moxonidine, a minor decrease of bioavailability of glibenclamide was detectable, as could be derived from the AUC and clearance data."( Steady state investigation of possible pharmacokinetic interactions of moxonidine and glibenclamide.
Achtert, G; Dilger, C; Eden, G; Michaelis, K; Müller, M; Weber, W; Weimann, HJ,
)
0.13
"Pharmacokinetic characteristics and relative bioavailability of the regular preparation (RG) and micronized preparation (MG) of glibenclamide (Gli) were studied in 4 Chinese healthy men."( Pharmacokinetics and relative bioavailability of tablet of micronized glibenclamide in 4 Chinese healthy men.
Cui, HD; Guo, Y; Jiang, WD; Karras, HO; Zhu, XX, 1993
)
0.29
"0 g of sodium bicarbonate and non-micronized glibenclamide greatly increased the early bioavailability of glibenclamide."( The effects of different doses of sodium bicarbonate on the absorption and activity of non-micronized glibenclamide.
Kivistö, KT; Lehto, P; Neuvonen, PJ, 1993
)
0.29
" There was no significant difference in total metabolite urine recovery between intravenous or oral administration of Gb, suggesting almost complete oral bioavailability of the micronized glibenclamide formulation."( Comparison of the kinetics of glyburide and its active metabolites in humans.
Jönsson, A; Melander, A; Rydberg, T, 1995
)
0.58
" The effect of food on their bioavailability is similar."( Modulation of insulin secretion in non-insulin-dependent diabetes mellitus by two novel oral hypoglycaemic agents, NN623 and A4166.
Kikuchi, M, 1996
)
0.29
" With its good oral bioavailability (47%) and plasma elimination half-life (3 h) in rats, compound 3 offers an excellent candidate to investigate the role of residual vasorelaxant potency of 2 toward its cardioprotective activity in vivo."( Cardioselective antiischemic ATP-sensitive potassium channel (KATP) openers. 5. Identification of 4-(N-aryl)-substituted benzopyran derivatives with high selectivity.
Ahmed, SZ; Atwal, KS; Baird, AJ; Ding, CZ; Dzwonczyk, S; Ferrara, FN; Grover, GJ; Humphreys, WG; McLaughlin, LG; Normandin, DE; Rovnyak, GC; Santafianos, D; Sleph, PG; Traeger, SC, 1997
)
0.3
" Co-administration of candesartan cilexetil with HCTZ produced a statistically significant increase in the bioavailability and Cmax values for candesartan (18% and 25%, respectively)."( Pharmacokinetic drug interaction studies with candesartan cilexetil.
Högemann, A; Jonkman, JH; Lins, R; Sennewald, R; van Heiningen, PN; van Lier, JJ, 1997
)
0.3
" Therefore, one possible mechanism accounting for the more rapid and short-lived hypoglycemic action of A-4166 in vivo, as compared with tolbutamide, may involve the reported differences in the bioavailability of A-4166."( Insulin secretion from isolated rat islets induced by the novel hypoglycemic agent A-4166, a derivative of D-phenylalanine.
Kikuchi, M; Niki, I; Oka, Y; Sakurada, M; Tsukuda, K, 1998
)
0.3
" AUC and Cmax of Gb were lower and the clearance to bioavailability ratio (CL/f) was higher in the IRF group."( Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function.
Jönsson, A; Melander, A; Rydberg, T; Sterner, G, 1998
)
0.3
"The aim of this study was to investigate the effect of cyclodextrins (beta-CD, HP-beta-CD and (SBE)7m-beta-CD), and co-administration of a water-soluble polymer (HPMC) and cyclodextrins, on the oral bioavailability of glibenclamide in dogs."( Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms.
Jarho, P; Järvinen, K; Järvinen, T; Loftsson, T; Savolainen, J; Taipale, H, 1998
)
0.3
" Orally administered glibenclamide and its physical mixture with HP-beta-CD showed poor absolute bioavailability, while orally administered glibenclamide/cyclodextrin-complexes significantly enhanced the absolute bioavailability of glibenclamide."( Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms.
Jarho, P; Järvinen, K; Järvinen, T; Loftsson, T; Savolainen, J; Taipale, H, 1998
)
0.3
"The oral bioavailability of glibenclamide was significantly increased by cyclodextrin complexation."( Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms.
Jarho, P; Järvinen, K; Järvinen, T; Loftsson, T; Savolainen, J; Taipale, H, 1998
)
0.3
" Changes in the bioavailability of the drug and activation of sympathetic nervous system and the hypothalamic-pituitary-adrenocortical axis are potential candidates."( The effect of stress on the pharmacokinetics and pharmacodynamics of glibenclamide in diabetic rats.
Abd Elaziz, MA; Al-Dhawailie, AA; Tekle, A,
)
0.13
" Formation of the new crystal form is considered as reason of reduction in dissolution and bioavailability of tablets."( Preparation and characterisation of a new insoluble polymorphic form of glibenclamide.
Malamataris, S; Panagopoulou-Kaplani, A, 2000
)
0.31
"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
" The absorption rate of glibenclamide and tolbutamide was not affected by food."( [Timing of administration of sulfonyl urea derivatives].
de Smet, PA; Fischer, HR, 2000
)
0.31
" Pharmacokinetics and bioavailability of two strengths (500 mg/2."( Pharmacokinetics and bioavailability of a metformin/glyburide tablet administered alone and with food.
Arnold, ME; Barbhaiya, RH; Greene, DS; Marathe, PH; Meeker, J, 2000
)
0.56
"This simple, rapid and sensitive method is suitable for pharmacokinetic, bioavailability and biequivalence studies."( A novel extractionless hplc fluorescence method for the determination of glyburide in the human plasma: application to a bioequivalence study.
Abed, O; Abraham, B; Al-Lami, A; Khatri, J; Masood, S; Qassim, S,
)
0.36
"Glyburide is a poorly water-soluble oral hypoglycemic agent, with problems of variable bioavailability and bio-inequivalence related to its poor water-solubility."( Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique.
Ballerini, R; Cirri, M; Maestrelli, F; Mura, P; Valleri, M, 2004
)
2.05
"The purpose of this work is to improve the dissolution and bioavailability characteristics of glibenclamide as compared to Daonil tablets (Hoechst)."( In vitro and in vivo evaluation of glibenclamide in solid dispersion systems.
Al-Qashi, ZS; Najib, NM; Tashtoush, BM, 2004
)
0.32
" In particular, the pyrazolyl derivative 35 showed good oral bioavailability and brain penetration associated with high potency and selectivity in vitro."( 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.
Andreoli, M; Ashby, CR; Bifone, A; Blaney, FE; Bonanomi, G; Braggio, S; Capelli, AM; Checchia, A; Curcuruto, O; Damiani, F; Donati, D; Fabio, RD; Gentile, G; Gozzi, A; Gribble, A; Griffante, C; Hagan, JJ; Hamprecht, D; Heidbreder, C; Lacroix, L; Lightfoot, A; Macdonald, G; Micheli, F; Mugnaini, M; Pecoraro, M; Perini, O; Petrone, M; Pilla, M; Piner, J; Rossi, T; Schwarz, A; Scott, C; Smith, A; Stemp, G; Tarsi, L; Tedesco, G; Terreni, S; Valerio, E; Wood, M; Worby, A, 2007
)
0.34
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" It is proposed that these effects are in part related to improved kidney function resulting in increased Hct and blood viscosity which increases vascular wall shear stress and NO bioavailability leading to a vasodilator effect."( Increased hematocrit and reduced blood pressure following control of glycemia in diabetes.
Cabrales, P; Díaz, JS; Intaglietta, M; Negrete, AC; Salazar Vázquez, BY; Salazar Vázquez, MA; Venzor, VC, 2008
)
0.35
" The purpose of this study was to compare the bioavailability of two formulations of glyburide used in Mexico, Daonil and Gen-Glybe."( Bioequivalence of two oral formulations of glyburide (glibenclamide).
Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Herrera, JE; Medina-Santillán, R; Reyes-García, G, 2007
)
0.83
" To evaluate the possibility of a pharmacokinetic interaction, the oral bioavailability of diclofenac (18 mg/kg) was studied in presence and the absence of glibenclamide (10 mg/kg)."( Pharmacokinetics and pharmacodynamics of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2008
)
0.35
"Complexation with HBenBCD may be an effective way to increase the bioavailability of glyburide."( Improving glyburide solubility and dissolution by complexation with hydroxybutenyl-beta-cyclodextrin.
Buchanan, CM; Buchanan, NL; Edgar, KJ; Klein, S; Lambert, JL; Ramsey, MG; Wempe, MF; Zoeller, T, 2009
)
0.98
" In-vivo results of the optimized gel (2% CP: 2% HPMC) revealed that the gel successfully prevented severe hypoglycemia, showed sustained action, and enhanced relative bioavailability with and without penetration enhancers as compared to the marketed formulation."( Buccoadhesive gels of glibenclamide: a means for achieving enhanced bioavailability.
Pathak, K; Philip, AK; Srivastava, M, 2009
)
0.35
"3 ng ml(-1) h(-1)) also indicate increased bioavailability of the drug from these systems compared to the oral route (829."( Microcapsules and transdermal patch: a comparative approach for improved delivery of antidiabetic drug.
Barik, BB; Mishra, MK; Ray, D, 2009
)
0.35
" Besides, this antagonism was not produced by diminution in the bioavailability of diclofenac."( Pharmacokinetic of diclofenac in the presence and absence of glibenclamide in the rat.
Castañeda-Hernández, G; León-Reyes, MR; Ortiz, MI, 2009
)
0.35
"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
" Developed NPs revealed a decreased t(min) and enhanced bioavailability and hence superior activity as compared to plain GB in alloxan-induced diabetic rabbit model."( Development and characterization of nanoparticles of glibenclamide by solvent displacement method.
Datusalia, AK; Deep, A; Dora, CP; Kumar, S; Singh, SK,
)
0.13
" Finally, we discuss the possible effects of tautomerism on basic pharmaceutical parameters such as biological activity or bioavailability in the case of the glibenclamide drug."( On the kinetics of tautomerism in drugs: New application of broadband dielectric spectroscopy.
Grzybowska, K; Hawelek, L; Kaminski, K; Paluch, M; Wlodarczyk, P; Wojnarowska, Z, 2010
)
0.36
"75 mg/day × 1 day) on the relative bioavailability of either compound in healthy subjects (n = 20, age 18-55 years)."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.58
" Tryptanthrin was well absorbed across the Caco-2 monolayers, and its transepithelial transports were dominated by passive diffusion."( Transport characteristics of tryptanthrin and its inhibitory effect on P-gp and MRP2 in Caco-2 cells.
Ma, G; Wang, H; Yan, J; Yang, Q; Zhang, X; Zhu, X, 2011
)
0.37
"Particle size reduction is a suitable method to enhance the bioavailability of poorly soluble drugs."( Process optimization of a novel production method for nanosuspensions using design of experiments (DoE).
Heinzerling, O; Möschwitzer, JP; Müller, RH; Salazar, J, 2011
)
0.37
"Nanosizing is a non-specific approach to improve the oral bioavailability of poorly soluble drugs."( Nanocrystals: comparison of the size reduction effectiveness of a novel combinative method with conventional top-down approaches.
Ghanem, A; Möschwitzer, JP; Müller, RH; Salazar, J, 2012
)
0.38
"Over the last decades the poor solubility of new drugs has become an important issue, with one of the main challenges being to develop oral dosage forms with acceptable bioavailability for such compounds."( Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions.
Dressman, JB; Klein, S; Zoeller, T, 2012
)
0.38
" It was reported that doxorubicin-induced cardiotoxicity is mediated through oxidative stress coupled with impaired NO bioavailability and NF-κB activation."( Cardioprotective effects of nicorandil, a mitochondrial potassium channel opener against doxorubicin-induced cardiotoxicity in rats.
Abdel-Raheem, IT; Abouzied, MM; Taye, A, 2013
)
0.39
"The present study aimed at the development and characterisation of self-nanoemulsifying drug delivery system (SNEDDS) to improve the oral bioavailability of poorly soluble glyburide."( Improved oral bioavailability of glyburide by a self-nanoemulsifying drug delivery system.
Kong, Y; Leng, D; Li, R; Liu, H; Liu, W; Shang, K; Zhang, T, 2014
)
0.88
"These results indicated that SNEDDS is a promising drug delivery system for increasing the oral bioavailability of glyburide."( Improved oral bioavailability of glyburide by a self-nanoemulsifying drug delivery system.
Kong, Y; Leng, D; Li, R; Liu, H; Liu, W; Shang, K; Zhang, T, 2014
)
0.89
" Potential inhibitors of MMPs have been tested for almost 30 years, but none have reached clinical utility due to bioavailability issues and adverse effects."( In vitro biological evaluation of glyburide as potential inhibitor of collagenases.
Bodiga, S; Bodiga, VL; Chavali, S; Eda, SR; Revur, NN; Thokala, S; Zhang, A, 2014
)
0.68
"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 results revealed that BA and AD led to the PK/PD changes because of glyburide-increased bioavailability and because of the inhibition of CYP3A4 enzyme."( Pharmacokinetic and Pharmacodynamic Interaction of Boswellic Acids and Andrographolide with Glyburide in Diabetic Rats: Including Its PK/PD Modeling.
Samala, S; Veeresham, C, 2016
)
0.89
"A solid lipid nanoparticle (SLN) formulation was developed with the aim of improving the oral bioavailability and the therapeutic effectiveness of glibenclamide (GLI), a poorly water-soluble drug used in the treatment of type 2 diabetes."( Development of solid lipid nanoparticles as carriers for improving oral bioavailability of glibenclamide.
Almeida, AJ; Di Cesare Mannelli, L; Ghelardini, C; Gonçalves, LM; Maestrelli, F; Mura, P, 2016
)
0.43
" All of these efforts led to the identification of compound 11 as a potent and orally bioavailable FFA1 agonist without the risk of hypoglycemia."( Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
Cai, X; Dai, Y; Fu, M; Huang, W; Li, Z; Pan, M; Qian, H; Shi, W; Su, X, 2016
)
0.43
"Glibenclamide is an antidiabetic drug showing low bioavailability as consequence of its low solubility."( Supramolecular structure of glibenclamide and β-cyclodextrins complexes.
Font, M; Irache, JM; Lucio, D; Martínez-Ohárriz, MC, 2017
)
0.46
"Drug nanosuspension is one of the established methods to improve the bioavailability of poorly soluble drugs."( Production of drug nanosuspensions: effect of drug physical properties on nanosizing efficiency.
Liu, T; Möschwitzer, JP; Müller, RH, 2018
)
0.48
"In an attempt to decrease the dose, anticipated side effects, and the cost of production of glibenclamide, GLC, a potent oral hypoglycemic drug, the enhancement of the dissolution and hence the oral bioavailability were investigated."( Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance.
Abdellatif, AAH; El Hamd, MA; Roberts, M; Tawfeek, HM; Younis, MA, 2018
)
0.48
"Supersaturating formulations are widely used to improve the oral bioavailability of poorly soluble drugs."( Calculation of drug-polymer mixing enthalpy as a new screening method of precipitation inhibitors for supersaturating pharmaceutical formulations.
Dressman, J; Kuentz, M; Nair, A; Price, DJ; Saal, C, 2019
)
0.51
"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
" Friedelan-3-one was shown to be non-carcinogenic, non-hepatotoxic, has decent oral bioavailability and a good compound for optimisation into a drug candidate."( Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one.
Adongo, DW; Amponsah, IK; Baah, MK; Ben, IO; Fleischer, TC; Harley, BK; Mensah, AY; Mireku-Gyimah, NA, 2021
)
0.62
" To date, using a variety of methods, only the bioavailability time of tritiated thymidine and 5-bromo-2'-deoxyuridine (BrdU) have been evaluated."( The bioavailability time of commonly used thymidine analogues after intraperitoneal delivery in mice: labeling kinetics in vivo and clearance from blood serum.
Belousov, VV; Enikolopov, GN; Maltsev, DI; Mellanson, KA; Podgorny, OV, 2022
)
0.72
" Both the drugs possess dissolution rate-limited oral bioavailability leading to poor therapeutic efficacy."( Polymeric micelles loaded with glyburide and vanillic acid: I. Formulation development, in-vitro characterization and bioavailability studies.
Adams, J; Arshad, MF; Awasthi, A; Bettada, VG; Chellappan, DK; Corrie, L; Dua, K; Famta, P; Gowthamarajan, K; Gulati, M; Gupta, G; Hansbro, PM; Kaur, J; Khatik, GL; Madhunapantula, SV; Paudel, KR; Saini, S; Singh, SK, 2022
)
1.01
" Nanoparticles (NP) of GB and organophilized Layered Double Hydroxide (LDH) were developed to improve oral bioavailability and tested in streptozotocin-induced diabetic rats to evaluate therapeutic efficacy and safety."( Efficacy and safety of nanoparticles of glibenclamide and organomodified layered double hydroxides in diabetics rats.
Alvarez-Lorenzo, C; da Costa Silva Neto, J; Dal Santo, G; Damasceno Leão, A; Duarte Vieira, L; Fontana Agostini, J; Gonçalves da Silva, T; Gonçalves Wanderley, A; Lamartine Soares-Sobrinho, J; Ribeiro da Silva, J; Rodrigues de Lima Porto Ramos, K, 2023
)
0.91

Dosage Studied

Glyburide can be used to treat non-insulin-dependent diabetes mellitus (NIDDM) patients. In the beta cell of aged rats, the following abnormalities were found: right shift of the dose-response curve (depressed sensitivity) of glucose-induced insulin release.

ExcerptRelevanceReference
" The maximal values of both phases of secretion in the dose-response curve elicited by different glucose concentrations shift to the left when glibenclamide is added to the perfusate."( Studies on the dynamics and mechanism of glibenclamide-induced insulin secretion.
Basabe, JC; Chieri, RA; Farina, JM, 1976
)
0.26
" Addition of sulphonylurea induced a left shift in the dose-response relationships in controls and low insulin responders; under these conditions the effect of glibenclamide was more pronounced than that of gliquidone."( Effect of two sulphonylureas on the dose kinetics of glucose-induced insulin release in normal and diabetic subjects.
Cerasi, E; Efendic, S; Luft, R; Thornqvist, C, 1979
)
0.26
" Glibenclamide, Gliquidone, Glusoxepide and placebo were administered in random order with degree dosage adjusted according to degree of severity of diabetes."( [Comparison of glibenclamide, gliquidone, glisoxepide and placebo in maturity onset diabetics of differing degrees of severity (author's transl)].
Brändle, J; Irsigler, K; Ogris, E; Regal, H; Steinhardt, T; Zdolsek, I, 1979
)
0.26
" Due to the high frequency of side effects it does not seem to be worthwhile to further investigate the therapeutic effect of MPC in a larger number of patients with different dosage regimens."( [Effect of methylpyrazole-carboxylic acid on carbohydrate and lipid metabolisms in patients with diabetes mellitus].
Hassalacher, Ch; Lang, PD; Vollmar, J; Wahl, P, 1975
)
0.25
" The dose-response pattern for insulin release (first phase) following two chemically unrelated insulin secretagogues, the potent sulphonyl-urea derivative, glibenclamide, and the beta-adrenegic agonist L-isopropylnoradrenaline, (L-IPNA), was tested with and without vinblastine pretreatment."( Effect of vinblastine in vivo on ultrastructure and insulin releasing capacity of the B-cell following sulphonylurea and isopropyl-noradrenaline.
Ericson, LE; Lundquist, I, 1975
)
0.25
" The changes in weight were similar and both drugs were devoid of serious toxic effects in the dosage prescribed."( Comparative study of glibenclamide & chlorpropamide in newly diagnosed maturity onset diabetics.
Haider, Z; Obaidullah, S, 1976
)
0.26
" It was impossible to demonstrate neither a direct effect nor an enhancement of insulin secretion during drug administration; in another experiment (treatment F) a higher dosage of BL-191 (100 mg as a priming dose + 200 mg as infusion dose) was likely ineffective."( Effects of a xanthine derivative (BL 191) on insulin secretion in normal man.
Angotzi, G; Diana, A; Lenti, G; Pagano, G; Sani, AB, 1975
)
0.25
" Seventy-five percent of patients receiving glyburide were controlled with once-daily dosing compared with 29."( Glyburide versus glipizide in the treatment of patients with non-insulin-dependent diabetes mellitus.
Bloomgarden, Z; Kilo, C; Meenan, A,
)
1.84
" The dosage of hypoglycemic drugs was maintained at a constant level throughout the study."( A high-monounsaturated-fat/low-carbohydrate diet improves peripheral insulin sensitivity in non-insulin-dependent diabetic patients.
Capaldo, B; Ciardullo, AV; Genovese, S; Giacco, A; Parillo, M; Riccardi, G; Rivellese, AA, 1992
)
0.28
"Randomized (between agents and in order of dosing regimens), prospective, open, crossover study among 14 NIDDM patients to compare glucose, insulin, and C-peptide responses to a standard diet and to 10 mg of oral GP or GB taken without food 1) after 2 wk without therapy, 2) after 4 wk of either GP (n = 7) or GB (n = 7) treatment OD, and 3) after 4 wk of TD therapy with the same agent."( Chronic sulfonylurea therapy augments basal and meal-stimulated insulin secretion while attenuating insulin responses to sulfonylurea per se.
Bird, DM; Cameron, DP; Ma, A; McIntyre, HD; Patterson, CA, 1992
)
0.28
"Therapeutic equivalence of OD and TD dosing with GP and GB during chronic therapy."( Chronic sulfonylurea therapy augments basal and meal-stimulated insulin secretion while attenuating insulin responses to sulfonylurea per se.
Bird, DM; Cameron, DP; Ma, A; McIntyre, HD; Patterson, CA, 1992
)
0.28
") dose-response curves for decrease in MBP due to YT-146 underwent parallel rightward shifts."( Vasodepressor mechanisms of 2-(1-octynyl)-adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels.
Satoh, K; Taira, N; Yamada, H; Yoneyama, F, 1992
)
0.28
"TO investigate the effects of the addition of glyburide to the regimen of insulin-treated non-insulin-dependent diabetes mellitus (NIDDM) patients with regard to their overall insulin requirement and dosage schedule and to assess persistence of these effects."( Combination therapy for NIDDM with biosynthetic human insulin and glyburide.
Bailey, TS; Costa, R; Heshka, S; Mezitis, NH; Pi-Sunyer, FX; Saitas, V, 1992
)
0.78
" After a baseline period of satisfactory diabetes control on biosynthetic human insulin alone, insulin dosage was halved, and patients were placed on a combination with either glyburide or placebo."( Combination therapy for NIDDM with biosynthetic human insulin and glyburide.
Bailey, TS; Costa, R; Heshka, S; Mezitis, NH; Pi-Sunyer, FX; Saitas, V, 1992
)
0.71
" The adenosine dose-response curve in these hearts was shifted 20-fold to the right by 1 microM glyburide."( Coronary reactive hyperemia and adenosine-induced vasodilation are mediated partially by a glyburide-sensitive mechanism.
Clayton, FC; Grover, GJ; Hess, TA; Smith, MA, 1992
)
0.72
" Premixed 70% NPH/30% Regular insulin was taken before supper, and the dosage was adjusted weekly by an algorithm seeking nearly normal fasting glycemia."( Combined therapy for obese type 2 diabetes: suppertime mixed insulin with daytime sulfonylurea.
Bingham, P; Garrison, C; Hart, J; McDaniel, P; Riddle, M, 1992
)
0.28
" Gluburide, as adjunctive therapy, may reduce the daily dosage needed by those who require insulin."( Glyburide in non-insulin-dependent diabetes: an update.
Kolterman, OG,
)
1.57
" The dose-response curves for inhibition of I-KATP at different pHo's were found to coincide when plotted for the unionized concentrations of the drugs."( Effects of pH upon the inhibition by sulphonylurea drugs of ATP-sensitive K+ channels in cardiac muscle.
Findlay, I, 1992
)
0.28
" Cells were held at 0 mV and BRL 38227 was added cumulatively to construct a dose-response relationship."( Effects of BRL 38227 on potassium currents in smooth muscle cells isolated from rabbit portal vein and human mesenteric artery.
Aaronson, PI; Russell, SN; Smirnov, SV, 1992
)
0.28
"Despite extensive clinical experience with second-generation oral hypoglycemic agents, the relative dosing equivalence of glyburide and glipizide remains controversial."( Conversion from glipizide to glyburide: a prospective cost-impact survey.
Alexis, G; Henault, R; Sparr, HB,
)
0.63
" In the present investigation we studied the pH dependency and dose-response effects of suramin on islet lysosomal enzyme activities as well as the effect of suramin treatment on the insulin-secretory response to various secretagogues in mice."( Effect of the lysosomotropic drug suramin on islet lysosomal enzyme activities and the insulin-secretory response induced by various secretagogues.
Lundquist, I; Panagiotidis, G; Salehi, AA, 1991
)
0.28
" The dosage was adjusted to obtain adequate control or up to the maximum recommended dosage."( Efficacy of gliclazide in comparison with other sulphonylureas in the treatment of NIDDM.
Harrower, AD, 1991
)
0.28
" Insulin dose-response curves demonstrate that glyburide treatment increased both insulin sensitivity and responsiveness."( Glyburide increases insulin sensitivity and responsiveness in peripheral tissues of the rat as determined by the glucose clamp technique.
Hirshman, MF; Horton, ES, 1990
)
1.98
"1 and 1 microM), with a three-fold and eight-fold shift to the right of the dose-response curve, respectively."( The action of a potassium channel activator, BRL 38227 (lemakalim), on human airway smooth muscle.
Alouan, LA; Armour, CL; Barnes, PJ; Black, JL; Johnson, PR, 1990
)
0.28
" Insulin dosage fell in the glipizide group from 36 to 26 U day-1, as 4 patients experienced hypoglycaemic symptoms."( Combination of insulin with glipizide increases peripheral glucose disposal in secondary failure type 2 diabetic patients.
Reckless, JP; Simpson, HC; Stirling, CA; Sturley, R, 1990
)
0.28
" In diabetic patients treated with sulphonylureas and phenformin at low dosage (glibenclamide 5 mg and phenformin 50 mg) it was possible to maintain good glycometabolic control using only the sulphonylurea gliclazide (160 mg/die)."( [Efficacy of sulfonylurea and sulfonylurea-benfluorex therapy in patients with type 2 diabetes treated with commercial sulfonylurea-biguanide combinations].
Benzi, L; Cecchetti, P; Ciccarone, AM; Di Cianni, G; Giannarelli, R; Navalesi, R; Penno, G,
)
0.13
" Dose-response curves for the increase in coronary blood flow produced by nicorandil or cromakalim were shifted to the right in a parallel manner and to similar extents by glibenclamide given intravenously to support dogs."( Nicorandil increases coronary blood flow predominantly by K-channel opening mechanism.
Satoh, K; Taira, N; Yoneyama, F, 1990
)
0.28
" 68% of all SH-cases did with a dosage of 1-3 mg glibenclamide a day, 28% with 1 mg a day."( [Treatment of newly diagnosed type II diabetic patients with special reference to prescribing glibenclamide in low doses].
Bothe, E; Dempe, A; Hanisch, R; Häntzschel, U; Wurlitzer, M, 1989
)
0.28
" Neogluconin showed an improved absorption and comparable blood sugar levels at a dosage reduced by 25%."( [Clinical study comparing the effectiveness and tolerance of 2 current and one new glibenclamide formulation].
Haushofer, A; Lingg, G, 1989
)
0.28
"This investigation was carried out to evaluate the in vitro dissolution as well as the pharmacokinetic and pharmacodynamic properties of two tablet oral dosage forms of glibenclamide, Daonil (product A) and Glucomid (product B)."( Comparison of the pharmacokinetics and pharmacodynamics of two commercial products containing glibenclamide.
Abdel-Hamid, ME; el-Sayed, YM; Hasan, MM; Najib, NM; Sallam, ES; Shubair, MS; Suleiman, MS, 1989
)
0.28
" Insulin secretory dose-response curves utilizing static incubations fit a single binding site model and established that glyburide (ED50 = 112 +/- 18 nM) is a more potent secretagogue than tolbutamide (ED50 = 15 +/- 3 microM)."( Increased cytosolic calcium. A signal for sulfonylurea-stimulated insulin release from beta cells.
Berg, M; Boyd, AE; Gaines, KL; Nelson, TY; Rajan, AS, 1987
)
0.48
" Since maintained contraction induced by oxytocin in a Ca-free solution could be repeated after making a relaxation dose-response curve to sulfonylurea, the most likely mechanism of sulfonylurea-induced uterine relaxation is not an increase in the efflux of Ca but an increase in the Ca-uptake by intracellular organelles."( Relaxant effects of sulfonylureas on induced contractions of rat uterine smooth muscle: role of intracellular calcium.
Anselmi, E; D'Ocon, MP; Villar, A, 1986
)
0.27
" Compared with the control treatment, cimetidine increased the glibenclamide AUC (973 vs 710 ng ml-1 h), but during ranitidine dosing glibenclamide AUC (726 ng ml-1 h) was not significantly different from the control."( The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics.
Antal, EJ; Juhl, RP; Kubacka, RT, 1987
)
0.27
" Glyburide increased sensitivity to insulin (ie, shifted the dose-response curve to the left) without affecting either responsiveness or insulin binding."( Effect of glyburide on glycogen metabolism in cultured rat hepatocytes.
Davidson, MB; Sladen, G, 1987
)
1.59
" 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
" The required insulin dosage was thus reduced by more than a third."( [Effectiveness of combined treatment with glibenclamide and insulin in secondary sulfonylurea failure. A controlled multicenter double-blind clinical trial].
Bachmann, W; Lotz, N; Mehnert, H; Rosak, C; Schöffling, K, 1988
)
0.27
" To determine an optimal glyburide dosage schedule, the effects of glyburide once (every morning) or twice daily and chlorpropamide once daily (every morning) were compared in 18 men with non-insulin-dependent diabetes mellitus in a randomized, double-blind fashion."( Once-daily use of glyburide.
Fajardo, F; Ginier, P; Levin, SR; Madan, S, 1985
)
0.91
" Its absorption is determined by the rate of emptying of the dose form from the stomach with the lag time between dosing and the start of gastric emptying (and hence absorption of the dose) largely dependent on the in-vivo disintegration time."( The effect of in-vivo dispersion and gastric emptying on glibenclamide absorption from a novel, rapidly dissolving capsule formulation.
Barker, MC; Calvert, RT; Ganley, JA; McEwen, J, 1984
)
0.27
" The dosage of sulfinpyrazone used in this trial was well tolerated by all patients and no side effects were observed."( [Interaction of sulfinpyrazone (Anturan) and glibenclamide (Euglucon) in type II diabetic patients].
Irsigler, K; Kritz, H; Najemnik, C, 1983
)
0.27
"Pharmacodynamics and tolerance, as well as the bioavailability of two oral dosage forms of 5 mg glibenclamide were determined in eight healthy male volunteers in a double-blind crossover study."( Bioavailability and pharmacodynamics of a sustained-release glibenclamide product (Deroctyl) in comparison to a standard tablet formulation (Euglucon, Daonil).
Ayanoglu, G; Badian, M; Witte, PU, 1983
)
0.27
" The study examined the tailoring of drug dosage to the patients needs and found that in the majority of patients it was necessary to give both glibenclamide and gliquidone thrice daily."( Diabetic control with gliquidone--a short acting sulphonylurea.
Borthwick, LJ; Wilson, S, 1984
)
0.27
"The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of glyburide and glipizide, two second-generation oral sulfonylurea hypoglycemic agents, are reviewed."( Glyburide and glipizide, second-generation oral sulfonylurea hypoglycemic agents.
Prendergast, BD,
)
1.79
" The interindividual variation in glibenclamide concentrations was extremely large (0 to 1520 nmol/l), greatly exceeding the variation in dosage (2."( Serum glibenclamide in diabetic patients, and influence of food on the kinetics and effects of glibenclamide.
Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1980
)
0.26
" For each of the four drugs, the steady state concentrations showed very large between-patient variations, not attributable to dosage or weight differences but to individual differences in drug kinetics and to insufficient compliance."( Kinetics-effect relations of glipizide and other sulfonylureas.
Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1980
)
0.26
" In accordance with the augmented physiologic insulin release in the morning, a single morning dose of sulfonylureas may be the preferable dosage regimen in the treatment of elderly insulin-independent diabetics of moderate degree."( Diurnal pattern of plasma insulin and blood glucose during glibenclamide and glipizide therapy in elderly diabetics.
Groop, L; Harno, K, 1980
)
0.26
" Irrespective of dosage and mode of administration, addition of glibenclamide to a standardized breakfast, lunch and dinner enhanced plasma IRI concentrations and reduced blood glucose concentrations as compared to administration of meals without the drug."( Improved effect of glibenclamide on administration before breakfast.
Lundquist, I; Melander, A; Sartor, G; Scherstén, B; Wåhlin-Boll, E, 1982
)
0.26
" A wide interindividual variation in chlorpropamide levels was observed and thus, the prediction of drug concentration was difficult from the dosage alone, despite a statistically significant correlation between the dose per body weight and the serum drug level."( Chlorpropamide and glibenclamide serum concentrations in hospitalized patients.
Huupponen, R; Saarimaa, H; Viikari, J, 1982
)
0.26
" Old age, maximum dosage of glibenclamide (15 mg/day) and multimorbidity were characteristic of these patients."( [Incidence of severe hypoglycemia in relation to metabolic control and patient knowledge].
Ratzmann, KP; Schimke, E, 1995
)
0.29
" A third group of 5 dogs received glyburide alone in the same dosing regimen as in the combination group."( The pharmacologic basis of the cardiovascular toxicity of minoxidil in the dog.
DuCharme, DW; Higgins, MJ; Mesfin, GM; Robinson, FG; Zhong, WZ,
)
0.41
"5 microM) had no significant effect on relaxation dose-response curves (DRCs) to ACh, NTG or NO."( Role of calcium-activated K+ channels in vasodilation induced by nitroglycerine, acetylcholine and nitric oxide.
Khan, SA; Mathews, WR; Meisheri, KD, 1993
)
0.29
"Continuous nitroglycerin (NTG) administration causes pharmacologic tolerance in humans and animals, whereas intermittent dosing is capable of avoiding or reducing tolerance development."( Continuous versus intermittent nitroglycerin administration in experimental heart failure: vascular relaxation and radioligand binding to adrenoceptors and ion channels.
Bauer, JA; Fung, HL; Gopalakrishnan, M; Kwon, YW; Triggle, DJ; Zheng, W, 1993
)
0.29
" Dose-response curves to PGE2, PGD2, and iloprost, a PGI2 analogue, were performed before and during KATP channel blockade with glibenclamide."( Evidence that prostaglandins I2, E2, and D2 may activate ATP sensitive potassium channels in the isolated rat heart.
Bouchard, JF; Dumont, E; Lamontagne, D, 1994
)
0.29
"Pressor dose-response curves to endothelin 1 (0."( Vascular hyporesponsiveness to endothelin 1 in rats with cirrhosis.
Cailmail, S; Gaudin, C; Hartleb, M; Lebrec, D; Moreau, R, 1994
)
0.29
") produced a significant rightward shift of the dose-response curve of morphine, levorphanol, methadone, pilocarpine, clonidine and tizanidine; a modest, but not statistically significant, rightward shift of the dose-response curves of the mu-selective peptides DAMGO ([D-Ala2,N-Me-Phe4,Gly-ol5]-enkephalin) and PL017 ([N-Me-Phe3,D-Pro4]-morphiceptin); and no shift of the dose-response curves of alfentanil, carfentanil, fentanyl, sufentanil, or beta-endorphin."( The 'glibenclamide-shift' of centrally-acting antinociceptive agents in mice.
Martinez, RP; Raffa, RB, 1995
)
0.29
" Bladder activity and selectivity after oral dosing were studied in conscious, normotensive rats and dogs by monitoring cystometric and cardiovascular (CV) parameters."( ZENECA ZD6169: a novel KATP channel opener with in vivo selectivity for urinary bladder.
Do, ML; Empfield, JR; Halterman, TJ; Howe, BB; Ohnmacht, CJ; Pettinger, SJ; Russell, K; Stow, RB; Trainor, DA; Yochim, CL, 1995
)
0.29
" Hydrochlorothiazide (10 microM) and cicletanine (10 microM) were weak calcium antagonists shifting the calcium dose-response curve half a log unit to the right."( Ion channel involvement in the acute vascular effects of thiazide diuretics and related compounds.
Calder, JA; Schachter, M; Sever, PS, 1993
)
0.29
"A Leucodelphinidin derivative isolated from the bark of Ficus bengalensis Linn demonstrated hypoglycemic action at a dosage of 250 mg/kg given both in normal and alloxan diabetic rats."( Hypoglycemic effects of leucodelphinidin derivative isolated from Ficus bengalensis (Linn).
Augusti, KT; Geetha, BS; Mathew, BC, 1994
)
0.29
" These differences support the need for careful dosage titration of glyburide to achieve a desired therapeutic response in patients with type II diabetes."( Comparison of pharmacokinetics and pharmacodynamics of short- and long-term glyburide therapy in NIDDM.
Antal, EJ; Jaber, LA; Slaughter, RL; Welshman, IR, 1994
)
0.75
" The dose-response curve of the effects of levcromakalim on coronary perfusion pressure was shifted to the right in the presence of 20 nM to 1 microM glibenclamide."( The sensitivity of coronary vascular tone to glibenclamide: a study on the isolated perfused guinea pig heart.
Cyrys, S; Daut, J, 1994
)
0.29
" In the beta cell of aged rats, the following abnormalities were found: (a) right shift of the dose-response curve (depressed sensitivity) of glucose-induced insulin release, (b) no increase of the maximum response to glucose in the face of increased insulin content of the islets (reduced responsiveness), (c) no response to forskolin and normal response to the phorbol ester and glyburide, and (d) increased sensitivity to nifedipine."( Insulin secretion by the pancreatic beta cell of aged rats.
Aizawa, T; Hashizume, K; Ishihara, F; Komatsu, M; Nishii, N; Sato, Y; Suzuki, N; Yamada, T, 1994
)
0.46
" In this article, the authors compare the effectiveness of dosing glyburide at bedtime versus in the morning on glycemic control in patients with NIDDM under suboptimal control."( Bedtime dosing of glyburide and the treatment of type II diabetes mellitus.
Bustamante, MA; Hennessey, JV; Markert, RJ; McDonald, SD; Teter, ML, 1994
)
0.86
" Although glibenclamide is a functional antagonist that acts at the level of an effector rather than at a receptor, it caused parallel rightward shifts of agonist dose-response curves."( Glibenclamide reduces the coronary vasoactivity of adenosine receptor agonists.
Niiya, K; Olsson, RA; Tsuji, T; Uchida, S, 1994
)
0.29
" The dosages of glyburide were titrated to achieve specified therapeutic goals based upon serum glucose concentrations or to a maximum dosage of 20 mg per day."( The pharmacokinetics and pharmacodynamics of 12 weeks of glyburide therapy in obese diabetics.
Antal, EJ; Jaber, LA; Slaughter, RL; Welshman, IR, 1993
)
0.88
" The long half-life adds support to the use of a once-daily dosage of glyburide."( Slow elimination of glyburide in NIDDM subjects.
Ekberg, G; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T, 1994
)
0.85
"1 ml), and dose-response curves to levcromakalim (a KATP channel opener) or isoproterenol were constructed."( Role of potassium channels in hypoxic relaxation of porcine bronchi in vitro.
Croxton, TL; Fernandes, LB; Hirshman, CA; Lindeman, KS, 1994
)
0.29
" In three of the five patients treated with deferoxamine, the level of serum ferritin was normalized, but no patient had an appreciable change in dosage of medication for diabetes or glycemic control."( Non-insulin-dependent diabetes mellitus and elevated serum ferritin level.
Guay, AT; Kaye, TB; Simonson, DC,
)
0.13
" A dose-response relationship revealed that I5-HT was activated with an ED50 of 30 nM."( Whole-cell recordings of inwardly rectifying K+ currents activated by 5-HT1A receptors on dorsal raphe neurones of the adult rat.
Fox, AP; Kelly, JS; Penington, NJ, 1993
)
0.29
"The appropriate use of second-generation oral hypoglycemic agents is limited by the lack of definitive guidelines for their use in elderly diabetic patients and controversy over relative dosing equivalence."( Conversion from glipizide to glyburide: long-term follow-up of a cost-impact survey focusing on the elderly.
Alexis, G; Henault, R; Sparr, HB,
)
0.42
"A patient with noninsulin-dependent diabetes mellitus (NIDDM) who had previously developed secondary failure while taking a maximal dosage of glipizide was switched to glyburide 5 mg/d."( Inappropriate use of high-dose glyburide to treat uncontrolled type 2 diabetes mellitus.
Cook, DD; Ewing, RC; Rae, CE, 1993
)
0.77
" In SHR cells, the maximal slope conductance of the levcromakalim-evoked current, normalized by cell capacitance, was decreased, and the dose-response curve was shifted to the right compared with WKY cells."( Impaired action of levcromakalim on ATP-sensitive K+ channels in mesenteric artery cells from spontaneously hypertensive rats.
Abe, I; Fujii, K; Fujishima, M; Nagao, T; Ohya, Y; Setoguchi, M, 1996
)
0.29
"05) rightward shift of the dose-response curve for the depressor effects of adenosine (ED50 = 13."( The involvement of ATP-sensitive potassium channels and adenosine in the regulation of coronary flow in the isolated perfused rat heart.
Randall, MD, 1995
)
0.29
"To determine the influence of age on the pharmacokinetics and pharmacodynamics of glyburide after acute and chronic dosing in young and elderly subjects with non-insulin-dependent diabetes mellitus."( Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus.
Antal, EJ; Jaber, LA; Welshman, IR, 1996
)
0.79
" Observed pharmacodynamic differences indicate the necessity for dosage titration to a specified therapeutic response regardless of patient age."( Pharmacokinetics and pharmacodynamics of glyburide in young and elderly patients with non-insulin-dependent diabetes mellitus.
Antal, EJ; Jaber, LA; Welshman, IR, 1996
)
0.56
" Therefore, it is apparent that the addition of glibenclamide to insulin reduces daily insulin dosage and renders a greater uniformity to diurnal blood glucose control, most probably secondary to enhancement of insulin sensitivity."( More uniform diurnal blood glucose control and a reduction in daily insulin dosage on addition of glibenclamide to insulin in type 1 diabetes mellitus: role of enhanced insulin sensitivity.
Birkenholz, M; Kabadi, M; Kabadi, UM; McCoy, S, 1995
)
0.29
" The long-term follow-up (457 patients) confirmed that glimepiride (1-8 mg) once daily provides equivalent metabolic control to a higher dosage (2."( Long-term treatment of type 2 diabetic patients with the new oral antidiabetic agent glimepiride (Amaryl): a double-blind comparison with glibenclamide.
Draeger, KE; Lomp, HJ; Rosskamp, R; Schüler, E; Wernicke-Panten, K, 1996
)
0.29
"Studies were undertaken to establish the regional hemodynamic profile and dose-response relation of the adenosine triphosphate (ATP)-dependent potassium channel activator lemakalim in anesthetized rats."( Regional hemodynamic dose-response of lemakalim and glybenclamide in anesthetized rats.
Cox, BF; Perrone, MH; Smits, GJ, 1997
)
0.3
" After preconstriction with the thromboxane analog, U46619 (9,11-dideoxy-11 alpha, 9 alpha-epoxymethano-prostaglandin F2 alpha), the pulmonary vascular dose-response relationship for the k+ATP agonist lemakalim was assessed in the conscious and halothane-anesthetized states and also in the conscious and enflurane-anesthetized states."( Halothane and enflurane attenuate pulmonary vasodilation mediated by adenosine triphosphate-sensitive potassium channels compared to the conscious state.
Murray, PA; Nakayama, M; Sato, K; Seki, S, 1997
)
0.3
"05) in the lemakalim dose-response relationship."( Halothane and enflurane attenuate pulmonary vasodilation mediated by adenosine triphosphate-sensitive potassium channels compared to the conscious state.
Murray, PA; Nakayama, M; Sato, K; Seki, S, 1997
)
0.3
" On day 3, multiple dosing on 3 mg glyburide daily began."( Pharmacokinetics of oral glyburide in subjects with non-insulin-dependent diabetes mellitus and renal failure.
Aronoff, GR; Bays, H; Brier, ME; Sloan, R; Stalker, DJ; Welshman, I, 1997
)
0.88
" Moreover adding a bed-time dosage to the standard administration at meal times seems to be an effective therapeutical strategy."( Meformin, plasma glucose and free fatty acids in type II diabetic out-patients: results of a clinical study.
Ambrosi, F; Filipponi, P; Gregorio, F; Manfrini, S; Santucci, A, 1997
)
0.3
" 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
)
0.3
" Defibrillation thresholds were determined from a total of 180 fibrillation and defibrillation sequences, conducted in each preparation, and the results were fitted to a sigmoid dose-response curve by logistic regression analysis."( Reducing electrical defibrillation thresholds with glibenclamide in an isolated rabbit heart preparation.
Holley, LK; Xiao, XH, 1997
)
0.3
" Recognizing patients who may require dosage changes, and educating them on the signs and symptoms of hypoglycemia, may help prevent hospitalizations resulting from this complication associated with glyburide."( Prolonged hypoglycemic crisis associated with glyburide.
Maxa, J; Ogu, CC; Sills, MN,
)
0.58
" Therefore, for the improvement of the compliance of the patients, the development of a transdermal dosage form of sulfonylureas was attempted in this study."( [Trial for transdermal administration of sulfonylureas].
Furuya, K; Iwata, M; Machida, Y; Onishi, H; Shirotake, S; Takahashi, Y, 1997
)
0.3
" To determine the responsiveness of coronary resistance vessels to KATP stimulation and NO, dose-response curves (DRC) for KATP opener, pinacidil-, and NO-donor, 3-morpholino-syndomine-hydrochloride (SIN-1)-induced increase in coronary flow were constructed, respectively."( Inhibitors of nitric oxide synthesis and ischemia/reperfusion attenuate coronary vasodilator response to pinacidil in isolated rat heart.
Beresewicz, A; Maczewski, M, 1997
)
0.3
" However, the inhibition of the combined CPA and CCh response was reduced and the dose-response curve of SIN-1 shifted to the right."( Involvement of intracellular Ca2+ stores in inhibitory effects of NO donor SIN-1 and cGMP.
Allescher, HD; Franck, H; Puschmann, A; Schusdziarra, V; Storr, M, 1998
)
0.3
"Glibenclamide in combination with Kelening in the treatment of NIDDM is more effective and less toxic, and the combination may reduce the dosage of glibenclamide in NIDDM."( [Clinical study of glibenclamide in combination with kelening treatment in non-insulin dependent diabetes mellitus].
Zhou, P, 1997
)
0.3
" HPMC increased the solubilising effect of cyclodextrins and, therefore, the amount of cyclodextrin needed in the solid dosage form was significantly reduced by their co-administration."( Co-administration of a water-soluble polymer increases the usefulness of cyclodextrins in solid oral dosage forms.
Jarho, P; Järvinen, K; Järvinen, T; Loftsson, T; Savolainen, J; Taipale, H, 1998
)
0.3
" Dose-response relationships to the KATP channel agonist nicorandil were established in each dog using doses (25, 50, and 100 microg/min) previously shown to increase coronary collateral blood flow."( Sevoflurane selectively increases coronary collateral blood flow independent of KATP channels in vivo.
Hettrick, DA; Kersten, JR; Pagel, PS; Schmeling, T; Tessmer, J; Warltier, DC, 1999
)
0.3
" Glibenclamide enhanced spontaneous alternation performance in an inverted-U dose-response manner."( ATP-sensitive potassium channel blockade enhances spontaneous alternation performance in the rat: a potential mechanism for glucose-mediated memory enhancement.
Gold, PE; Nicholson, GM; Stefani, MR, 1999
)
0.3
" The initial dosage of glibenclamide was 5 mg/day taken half an hour before meal; this was increased to 5 mg per week and was adjusted according to the patient's tolerance to the drug and their glycemic control."( The effects of glibenclamide on serum lipids and lipoproteins in type II non-insulin dependent diabetes mellitus.
Aamir, K; Ali, M; Jan, M; Maheri, WM; Mughal, MA, 1999
)
0.3
" The bell-shaped dose-response relationship for ZD6169 activation of I(K(ATP)) has also been seen in bladder myocytes, albeit at a lower concentration, and it has been proposed to contribute to the reported lack of in vivo cardiovascular side effects."( The effects of ZD6169 on the ATP-dependent K(+) current (I(K)(ATP)) in isolated cat ventricular myocytes.
Jow, B; Numann, R, 1999
)
0.3
" It was successfully applied to the analysis of clinical samples from patients dosed with glyburide."( Application of liquid chromatography atmospheric pressure chemical ionization tandem mass spectrometry in the quantitative analysis of glyburide (glibenclamide) in human plasma.
Bakhtiar, R; Ramos, L; Tse, F, 1999
)
0.73
" Thus, the age-related dissolution problems of GB can be overcome by utilizing the GB/CD complex in the tablet dosage form."( Effect of aging on the dissolution stability of glibenclamide/beta-cyclodextrin complex.
Babu, RJ; Pandit, JK, 1999
)
0.3
" Diazoxide (2 microg/mouse) shifted morphine's dose-response curve 47-fold, while levcromakalim (0."( ATP-gated K(+) channel openers enhance opioid antinociception: indirect evidence for the release of endogenous opioid peptides.
Lohmann, AB; Welch, SP, 1999
)
0.3
" Patients were randomly assigned to sulphonylurea increased up to its maximum dosage (1st group) or to addition of metformin (2nd group)."( Poorly controlled elderly Type 2 diabetic patients: the effects of increasing sulphonylurea dosages or adding metformin.
Ambrosi, F; Carle, F; Filipponi, P; Gregorio, F; Manfrini, S; Merante, D; Testa, R; Velussi, M, 1999
)
0.3
" It seems appropriate to employ the same dosage principles when using Gb in Caucasians and Chinese."( Pharmacodynamics and pharmacokinetics of intravenous glibenclamide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" These symptoms are usually dose dependent, mild to moderate in severity, occur at the onset of treatment, decline with time and resolve promptly on discontinuation of the drug or with dosage adjustment."( Miglitol: a review of its therapeutic potential in type 2 diabetes mellitus.
Scott, LJ; Spencer, CM, 2000
)
0.31
" Competition experiments showed that taurine shifted the dose-response inhibition curve of glybenclamide to the left on the log-dose axis without significantly affecting those of ATP or Ca(2+) ion."( Taurine blocks ATP-sensitive potassium channels of rat skeletal muscle fibres interfering with the sulphonylurea receptor.
Barbieri, M; Camerino, DC; Tricarico, D, 2000
)
0.31
" In isolated pulmonary arterial rings, 4-AP increased resting tension and caused a leftward shift in the KCl dose-response curve."( K(+) channel inhibition, calcium signaling, and vasomotor tone in canine pulmonary artery smooth muscle.
Damron, DS; Doi, S; Horibe, M; Murray, PA; Ogawa, K; Tanaka, S, 2000
)
0.31
" Estimated interstitial adenosine concentration with glibenclamide was not different from control vehicle and was well below the level necessary to overcome the 10-fold shift in the adenosine dose-response curve due to glibenclamide."( Role of K(ATP)(+) channels and adenosine in the control of coronary blood flow during exercise.
Feigl, EO; Gorman, MW; Richmond, KN; Tune, JD, 2000
)
0.31
" It is thus appropriate to consider dosing it less frequently."( Efficacy and safety of single versus multiple daily doses of glibenclamide in type 2 diabetes mellitus.
Ismail, RB; Mafauzy, M; Tun Fizi, A; Wan Mohamad, WB, 2000
)
0.31
" For the evaluation of Cushing's syndrome, all potential sources and doses of corticosteroids, as well as the patient's compliance with dosing instructions, must be examined."( Cushing's syndrome from Klack's solution.
Lankford, HV,
)
0.13
" It appears that the same dosage principles could be used for Caucasian and Chinese patients with type-2 diabetes when Gb or Gz are prescribed."( Effects and pharmacokinetics of oral glibenclamide and glipizide in Caucasian and Chinese patients with type-2 diabetes.
Chan, JC; Cockram, CS; Critchley, JA; Hallengren, B; Jönsson, A; Melander, A; Rydberg, T; Vaaler, S, 2000
)
0.31
" We investigated The enhancing effect of switching iontophoresis on the transdermal absorption and reduction of skin irritation to develop a transdermal dosage form of GLI."( [Enhancing effect of switching iontophoresis on transdermal absorption of glibenclamide].
Iwata, M; Machida, Y; Takahashi, Y, 2001
)
0.31
"To compare prescribing, dosage and blood glucose levels in patients with type 2 diabetes in two communities with differences in anti-hyperglycaemic drug utilization."( Differences in pharmacotherapy and in glucose control of type 2 diabetes patients in two neighbouring towns: a longitudinal population-based study.
Gottsäter, M; Lindberg, G; Lindwall, K; Melander, A; Olsson, J; Tisell, A, 2001
)
0.31
" However, there were pronounced between-town differences in dosage and glucose control."( Differences in pharmacotherapy and in glucose control of type 2 diabetes patients in two neighbouring towns: a longitudinal population-based study.
Gottsäter, M; Lindberg, G; Lindwall, K; Melander, A; Olsson, J; Tisell, A, 2001
)
0.31
" The dose-response curve of insulin secretion showed a markedly reduced maximum response, but almost normal glucose sensitivity in NSY islets."( Insulin secretion to glucose as well as nonglucose stimuli is impaired in spontaneously diabetic Nagoya-Shibata-Yasuda mice.
Babaya, N; Hamada, Y; Ikegami, H; Kawaguchi, Y; Nojima, K; Ogihara, T; Shibata, M; Ueda, H; Yamada, K; Yamato, E, 2001
)
0.31
" The effect was more pronounced in patients on a low Gb dose, either because of less impaired beta-cells in those receiving low doses, or due to reduced sulphonylurea sensitivity in those on high dosage (down-regulation)."( Effects and serum levels of glibenclamide and its active metabolites in patients with type 2 diabetes.
Hallengren, B; Jönsson, A; Melander, A; Rydberg, T, 2001
)
0.31
" Dose-response curves were recorded by means of an video-electronic arteriograph system."( Human chorionic gonadotropin attenuates the vascular response to angiotensin II.
Hermsteiner, M; Künzel, W; Zoltan, DR, 2002
)
0.31
"To evaluate the efficacy and safety of two dosage strengths of a single-tablet metformin-glibenclamide (glyburide) combination, compared with the respective monotherapies, in patients with Type 2 diabetes mellitus (DM) inadequately controlled by metformin monotherapy."( Improved glycaemic control with metformin-glibenclamide combined tablet therapy (Glucovance) in Type 2 diabetic patients inadequately controlled on metformin.
Allavoine, T; Howlett, H; Lehert, P; Marre, M, 2002
)
0.53
" After Ramadan, patients resumed their regular meal pattern and treatment dosage for 4 weeks."( Repaglinide versus glibenclamide treatment of Type 2 diabetes during Ramadan fasting.
Mafauzy, M, 2002
)
0.31
" Glibenclamide caused a downward displacement of the isoflurane dose-response curve, reducing isoflurane-mediated dilation by an average of 36%."( Isoflurane-induced dilation of porcine coronary microvessels is endothelium dependent and inhibited by glibenclamide.
Cason, BA; Gamperl, AK; Hein, TW; Kuo, L, 2002
)
0.31
" Dose-response relationships of both blockers follow a simple Michaelis-Menten function with K(d) values that differ by three orders of magnitude."( Probing an open CFTR pore with organic anion blockers.
Hu, S; Hwang, TC; Zhou, Z, 2002
)
0.31
"In this study, we determined whether repeated brief isoflurane (Iso) anesthesia induces ischemic tolerance to focal cerebral ischemia in a dose-response manner and whether the effect is dependent on adenosine triphosphate-regulated potassium channels."( Preconditioning with isoflurane produces dose-dependent neuroprotection via activation of adenosine triphosphate-regulated potassium channels after focal cerebral ischemia in rats.
Hou, L; Lu, Z; Wu, M; Xiong, L; Zhang, X; Zheng, Y; Zhu, Z, 2003
)
0.32
" In conclusion, combination treatment with metformin and sulfonylurea is more effective than these drugs alone in improving glycemic control in type 2 diabetes, while also allowing a reduction of the dosage of each drug."( Combination treatment with metformin and glibenclamide versus single-drug therapies in type 2 diabetes mellitus: a randomized, double-blind, comparative study.
Brun, E; Coppini, A; Gori, M; Moghetti, P; Muggeo, M; Perobelli, L; Spiazzi, G; Tosi, F; Zanolin, E, 2003
)
0.32
" The objective was to compare glucose, insulin and C-peptide 24 h profiles in patients with type 2 diabetes mellitus after dosing with nateglinide (given preprandially before three test meals), glibenclamide (administered once before breakfast) or placebo (given before three test meals)."( A placebo-controlled crossover study comparing the effects of nateglinide and glibenclamide on postprandial hyperglycaemia and hyperinsulinaemia in patients with type 2 diabetes.
Anderson, DM; Barnett, AH; Morgan, R; Owens, DR; Shelley, S, 2004
)
0.32
" Dosing followed a six-sequence balanced, two 3 x 3-replicated Latin square."( A placebo-controlled crossover study comparing the effects of nateglinide and glibenclamide on postprandial hyperglycaemia and hyperinsulinaemia in patients with type 2 diabetes.
Anderson, DM; Barnett, AH; Morgan, R; Owens, DR; Shelley, S, 2004
)
0.32
"This review examines the pharmacology, pharmacokinetics, drug-interaction potential, adverse effects, and dosing guidelines for metformin hydrochloride, a biguanide agent for the treatment of type 2 diabetes."( Metformin hydrochloride in the treatment of type 2 diabetes mellitus: a clinical review with a focus on dual therapy.
Campbell, RK; Iltz, JL; Setter, SM; Thams, J, 2003
)
0.32
"Following an open-label, lead-in phase to optimize the dosing of glyburide/metformin tablets, 365 patients randomly received additive therapy comprising rosiglitazone (4 mg once daily) or placebo for 24 weeks."( Glycemic control with glyburide/metformin tablets in combination with rosiglitazone in patients with type 2 diabetes: a randomized, double-blind trial.
Bruce, S; Dailey, GE; Fiedorek, FT; Noor, MA; Park, JS, 2004
)
0.88
" Eighty-eight patients were randomly assigned to receive repaglinide and 87 patients to glyburide, with a titration period of 6 to 8 weeks for optimization of drug dosage and a subsequent 12-month treatment period."( Regression of carotid atherosclerosis by control of postprandial hyperglycemia in type 2 diabetes mellitus.
Esposito, K; Giugliano, D; Marfella, R; Nappo, F, 2004
)
0.55
"A systematic analysis of the influence of different proportions of excipients on the stability of a solid dosage form was carried out."( Optimization of glibenclamide tablet composition through the combined use of differential scanning calorimetry and D-optimal mixture experimental design.
Cirri, M; Furlanetto, S; Maestrelli, F; Marras, AM; Mura, P; Pinzauti, S, 2005
)
0.33
" The simultaneous determination of these analytes is important for the routine monitoring of diabetic patients who take combination medications and for studying the pharmacokinetics of the combined dosage forms."( The development and validation of liquid chromatography method for the simultaneous determination of metformin and glipizide, gliclazide, glibenclamide or glimperide in plasma.
Aburuz, S; McElnay, J; Millership, J, 2005
)
0.33
" The dose-response effect of gliclazide and glibenclamide on ischaemic preconditioning and the action of glibenclamide on signal transduction in human myocardium were investigated using right atrial appendages from cardiac surgery patients."( The effect of gliclazide and glibenclamide on preconditioning of the human myocardium.
Fowler, A; Galiñanes, M; Loubani, M; Standen, NB, 2005
)
0.33
" 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
" In a separate study, five women were given a daily dosage (5 mg/day) of glyburide or glipizide, starting on the first postpartum day."( Transfer of glyburide and glipizide into breast milk.
Ambrose, PJ; Briggs, GG; Donat, DJ; Feig, DS; Klein, J; Koren, G; Kraemer, JM; Moskovitz, DN; Nageotte, M; Padilla, G; Wan, S, 2005
)
0.94
" Blood glucose reductions at 2 hours after dosing were 41."( CYP2C9, but not CYP2C19, polymorphisms affect the pharmacokinetics and pharmacodynamics of glyburide in Chinese subjects.
Chow, MS; Tomlinson, B; Yin, OQ, 2005
)
0.55
" Further studies in diabetic patients with long-term dosing are warranted to confirm these findings."( CYP2C9, but not CYP2C19, polymorphisms affect the pharmacokinetics and pharmacodynamics of glyburide in Chinese subjects.
Chow, MS; Tomlinson, B; Yin, OQ, 2005
)
0.55
" The objective of the DIACOM (effect of DosIng frequency of oral Antidiabetic agents on the COMpliance and biochemical control of type 2 diabetes) study was to compare the compliance of patients treated with once-daily (od) or twice-daily (bid) sulphonylureas."( The DIACOM study (effect of DosIng frequency of oral Antidiabetic agents on the COMpliance and biochemical control of type 2 diabetes).
Kardas, P, 2005
)
0.33
" Incubation with CGRP8-37 (10(-6) M) specifically during the 90-minute desensitization period with nitroglycerin resulted in even greater impairment in the response to nitroglycerin in tolerant rings, even though the calcitonin gene-related peptide antagonist had been washed out before completion of the nitroglycerin dose-response curve."( Nitroglycerin-induced release of calcitonin gene-related peptide from sensory nerves attenuates the development of nitrate tolerance.
Ghatta, S; O'Rourke, ST, 2006
)
0.33
" For therapeutic study, test articles were orally dosed once a day from 21 d after STZ-dosing at 100, 200 and 500 mg/kg/5 ml dosage levels for 4 weeks."( Anti-diabetic activity of SMK001, a poly herbal formula in streptozotocin induced diabetic rats: therapeutic study.
Choi, HS; Choi, HY; Kang, SM; Kim, JD; Ku, SK; Seo, BI, 2006
)
0.33
" In Group MNG, the dose-response curve shifted back to the right and the ED50 for inducing paraparesis was 11."( Intrathecal nicorandil and small-dose morphine can induce spastic paraparesis after a noninjurious interval of spinal cord ischemia in the rat.
Fuchigami, T; Kakinohana, M; Murata, K; Nakamura, S; Sugahara, K, 2006
)
0.33
"The combination of olmesartan with glibenclamide did not influence the bioequivalence of the area under the plasma-concentration time curve at steady state during one dosing interval 0 to tau = 24 hours (AUCss,tau) or the maximum steady-state concentration (Css,max) of both substances."( Pharmacokinetics and safety of olmesartan medoxomil in combination with glibenclamide in healthy volunteers.
Bolbrinker, J; Huber, M; Kreutz, R, 2006
)
0.33
"The effects of tramadol (racemic, R(-) and S(+): 10(-6), 10(-5), 5 x 10(-5) M), and glibenclamide on the levcromakalim dose-response curve were assessed in aortic rings that had been pre-contracted with phenylephrine."( Inhibitory effect of tramadol on vasorelaxation mediated by ATP-sensitive K+ channels in rat aorta.
Chang, KC; Cho, HC; Chung, YK; Lee, HK; Lee, JW; Park, KE; Shin, IW; Sohn, JT, 2007
)
0.34
" Dosing of glyburide three times daily was critical for her successful transition."( Transition from insulin to glyburide in a 4-month-old girl with neonatal diabetes mellitus caused by a mutation in KCNJ11.
Chan, YM; Laffel, LM, 2007
)
1.03
" Treatment was the combined administration of glibenclamide and metformin dosed to obtain a reduction of glucose levels."( Increased hematocrit and reduced blood pressure following control of glycemia in diabetes.
Cabrales, P; Díaz, JS; Intaglietta, M; Negrete, AC; Salazar Vázquez, BY; Salazar Vázquez, MA; Venzor, VC, 2008
)
0.35
" However, glibenclamide, regardless of the dosage schedule, tends to lower the plasma glucose values between midnight and early morning."( Daily blood glucose profiles of glibenclamide and gliclazide taken once or twice daily in elderly type 2 diabetic patients.
Futami-Suda, S; Kigawa, Y; Nakano, H; Norose, J; Oba, K; Ouchi, M; Suzuki, K; Suzuki, T; Watanabe, K; Yasuoka, H, 2008
)
0.35
" Blood glucose levels were significantly lower than those observed after dosing with glyburide alone."( Elucidating rifampin's inducing and inhibiting effects on glyburide pharmacokinetics and blood glucose in healthy volunteers: unmasking the differential effects of enzyme induction and transporter inhibition for a drug and its primary metabolite.
Benet, LZ; Frassetto, LA; Huang, Y; Zheng, HX, 2009
)
0.82
" Dosage was increased to a maximum of four pills in order to reach the glycemic control goals (fasting glucose ( Efficacy of glimepiride/metformin combination versus glibenclamide/metformin in patients with uncontrolled type 2 diabetes mellitus.
Aguilar-Salinas, C; Arechavaleta-Granell, R; Beltrán-Jaramillo, TJ; González-Canudas, J; González-Ortiz, M; Guerrero-Romero, JF; Islas-Andrade, S; Martínez-Abundis, E; Metha, R; Ramos-Zavala, MG; Revilla-Monsalve, C; Rodríguez-Morán, M; Violante-Ortiz, R; Wacher-Rodarte, N; Zavala-Suárez, E,
)
0.13
" Subsequently, the effects of a 1-week chronic daily dosing of DPP-IV inhibitors and sulfonylureas were investigated."( Antidiabetic effects of dipeptidyl peptidase-IV inhibitors and sulfonylureas in streptozotocin-nicotinamide-induced mildly diabetic mice.
Hayakawa, M; Matsuyama-Yokono, A; Nakano, R; Shibasaki, M; Shiraki, K; Someya, Y; Tahara, A, 2009
)
0.35
" Women with GDM in whom glyburide treatment has failed may benefit from alternative medication or dosage escalation; however, fetal safety should be kept in mind."( Are we optimizing gestational diabetes treatment with glyburide? The pharmacologic basis for better clinical practice.
Ahmed, MS; Blough, D; Caritis, SN; Carr, DB; Cobelli, C; Easterling, TR; Hankins, GD; Hebert, MF; Kelly, EJ; Krudys, KM; Ma, X; Mattison, DR; Miodovnik, M; Naraharisetti, SB; Snodgrass, WR; Umans, JG; Unadkat, JD; Vicini, P, 2009
)
0.91
" In a nonrandomized, single-sequence study (study II), participants (n = 24 completed) received a single 5-mg dose of the sulfonylurea glyburide, alone and after 8 days of dosing with alogliptin 25 mg qd."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.83
" The buccoadhesive gels could possibly be a means for alternative dosage form in avoiding first pass metabolism and ensuring enhanced bioavailability for glibenclamide."( Buccoadhesive gels of glibenclamide: a means for achieving enhanced bioavailability.
Pathak, K; Philip, AK; Srivastava, M, 2009
)
0.35
"3 x 10(-3) mol/L) produced a significant rightward shift in the phenylephrine dose-response curve, but had no effects on the potassium chloride-induced contraction."( Relaxant effects of matrine on aortic smooth muscles of guinea pigs.
Dai, GD; Fu, XY; Yan, L; Zheng, J; Zheng, P; Zhou, R; Zhou, X, 2009
)
0.35
" Levcromakalim produced concentration-dependent inhibitory effect on myometrial spontaneity and relaxant effect and the dose-response curve (DRC) was shifted towards right in the presence of glybenclamaide."( Cellular coupling of potassium channels with beta2 adrenoceptors in mediating myometrial relaxation in buffaloes (Bubalus bubalis).
Choudhury, S; Garg, SK; Mishra, SK; Singh, TU, 2010
)
0.36
" Three dosage groups were examined: glyburide 5 mg twice daily increased to 10 mg twice daily (GLYB), glipizide 5 mg twice daily increased to 10 mg twice daily (GLIPA), and glipizide 10 mg twice daily increased to 20 mg twice daily (GLIPB)."( Effect of sulfonylurea dose escalation on hemoglobin A1c in Veterans Affairs patients with type 2 diabetes.
Bartley, EP; Hurren, KM; O'Neill, JL; Ronis, DL, 2013
)
0.66
" However, this was not seen as clinically relevant due to the absence of a reliable dose-response relationship and the known large pharmacokinetic interindividual variability of glyburide."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.77
"An adequate drug dissolution behavior is essential for the therapeutic effectiveness of all solid dosage forms."( New solid self-microemulsifying systems to enhance dissolution rate of poorly water soluble drugs.
Cirri, M; Mennini, N; Mura, P; Valleri, M,
)
0.13
" Thus, the proposed method is simple and suitable for the simultaneous analysis of active ingredients in dosage forms and human serum."( Simultaneous determination of gliquidone, pioglitazone hydrochloride, and verapamil in formulation and human serum by RP-HPLC.
Arayne, MS; Mirza, AZ; Sultana, N, 2011
)
0.37
" In each case, the dose-response curve for N(2)O was progressively shifted to the right by increasing the dose of each pretreatment drug."( Involvement of a NO-cyclic GMP-PKG signaling pathway in nitrous oxide-induced antinociception in mice.
Chung, E; Ohgami, Y; Quock, LP; Quock, RM; Zhang, Y, 2011
)
0.37
" In resistance vessels, venous occlusion plethysmography was used to measure the dilator response to acetylcholine (ACh) [area under ACh dose-response curve (ACh AUC)]."( Postconditioning protects against human endothelial ischaemia-reperfusion injury via subtype-specific KATP channel activation and is mimicked by inhibition of the mitochondrial permeability transition pore.
Bhavsar, DD; Charakida, M; Deanfield, JE; Loukogeorgakis, SP; MacAllister, RJ; Okorie, MI; Ridout, D, 2011
)
0.37
"To (a) identify whether hemoglobin A1c remained equivalent in patients converted from glyburide to glipizide, (b) evaluate the prevalence of hypoglycemia during treatment with glyburide or glipizide, (c) compare change in glycemic control for renally impaired versus nonimpaired patients, and (d) analyze dosage conversion ratios selected by providers and measures of patient follow-up after conversion including time until A1c measurement and number of glipizide dose titrations."( Glycemic control and hypoglycemia in Veterans Health Administration patients converted from glyburide to glipizide.
Cantrell, M; Egge, JA; Shaw, RF; Skoff, RA; Waterbury, NV, 2011
)
0.81
"The aim of this study was to investigate the use of liquisolid technique in improving the dissolution of glyburide in a solid dosage form."( Influence of formulation parameters on dissolution rate enhancement of glyburide using liquisolid technique.
Gaikwad, NB; Gowthamarajan, K; Prakash, D; Singare, DS; Singh, SK; Srinivasan, KK, 2012
)
0.83
"Over the last decades the poor solubility of new drugs has become an important issue, with one of the main challenges being to develop oral dosage forms with acceptable bioavailability for such compounds."( Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions.
Dressman, JB; Klein, S; Zoeller, T, 2012
)
0.38
" Three groups of diabetic animals were orally administered daily with seed extract (SME) at a dosage of 50, 100 and 200 mg/kg BW."( Antioxidative and hypolipidemic efficacy of alcoholic seed extract of Swietenia macrophylla in streptozotocin diabetic rats.
Kalpana, K; Pugalendi, KV, 2011
)
0.37
" These developed calcium alginate/gum Arabic beads containing glibenclamide could possibly be advantageous in terms of advanced patient compliance with reduced dosing interval."( Calcium alginate/gum Arabic beads containing glibenclamide: development and in vitro characterization.
Das, B; Maji, R; Nayak, AK, 2012
)
0.38
" These changes could enhance drug efficacy, but could also make drug accumulation to increase adverse effects, so it was suggested that the dosage should be adjusted or the drug concentration in plasma should be monitored if glibenclamide and puerarin were co-administered."( Determination of glibenclamide and puerarin in rat plasma by UPLC-MS/MS: application to their pharmacokinetic interaction study.
Deng, Y; Li, F; Li, N; Qiao, Y; Wang, D, 2013
)
0.39
"Despite widespread use of glyburide to treat pregnancy-related hyperglycemia, the dosing regimen is based in large part on pharmacokinetic and pharmacodynamic studies in men and nonpregnant women."( A pharmacologic approach to the use of glyburide in pregnancy.
Caritis, SN; Hebert, MF, 2013
)
0.96
" We propose this expanded PBPK model can be used to evaluate different dosing scenarios, during pregnancy, of drugs cleared by single or multiple CYP enzymes."( Expansion of a PBPK model to predict disposition in pregnant women of drugs cleared via multiple CYP enzymes, including CYP2B6, CYP2C9 and CYP2C19.
Ke, AB; Nallani, SC; Rostami-Hodjegan, A; Unadkat, JD; Zhao, P, 2014
)
0.4
" Co-administration of topiramate decreased systemic exposure of glyburide and its active metabolites; combined treatment may require dosing adjustments of glyburide as per clinical judgment and glycemic control."( An open-label drug-drug interaction study of the steady-state pharmacokinetics of topiramate and glyburide in patients with type 2 diabetes mellitus.
Curtin, CR; Ford, L; Heald, DL; Manitpisitkul, P; Shalayda, K; Wang, SS, 2013
)
0.85
"To evaluate the antidiabetic drug dosage differences between geriatric and nongeriatric diabetics with reference to duration of disease and creatinine clearance (Crcl)."( Do geriatrics require dose titration for antidiabetic agents?
Adhikari, P; Chowta, M; Kamath, A; Pai, MR; Shastry, R; Ullal, S,
)
0.13
" Glycaemia values returned to normality only after suspension of escitalopram, despite antidiabetic dosage increase."( A case report on escitalopram-induced hyperglycaemia in a diabetic patient.
Brasesco, PC; Fucile, C; Leone, S; Martelli, A; Mattioli, F; Milano, G; Zuccoli, ML, 2013
)
0.39
" In this article, we review the efficacy, safety, and dosage of oral hypoglycemic agents for the treatment of gestational diabetes mellitus."( Gestational diabetes mellitus management with oral hypoglycemic agents.
Hays, KE; Hebert, MF; Ryu, RJ, 2014
)
0.4
"Dissolution testing is a performance test for many dosage forms including tablets and capsules."( Simulation of in vitro dissolution behavior using DDDPlus™.
Almukainzi, M; Löbenberg, R; Okumu, A; Wei, H, 2015
)
0.42
" Drug-CD complexation process is complex and often requires multiple processes to produce solid dosage form."( Evaluation of various processes for simultaneous complexation and granulation to incorporate drug-cyclodextrin complexes into solid dosage forms.
Betageri, GV; Gyanani, V; Siddalingappa, B, 2015
)
0.42
"Our study results showed that oral administration of swertiamarin at a dosage of 15, 25, 50 mg/kg bw for 28 days resulted in a significant (p < 0."( Immunohistochemistry, histopathology, and biomarker studies of swertiamarin, a secoiridoid glycoside, prevents and protects streptozotocin-induced β-cell damage in Wistar rat pancreas.
Dhanavathy, G, 2015
)
0.42
"A fast capillary zone electrophoresis method for the simultaneous analysis of glibenclamide and its impurities (I(A) and I(B)) in pharmaceutical dosage forms was fully developed within a quality by design framework."( Fast analysis of glibenclamide and its impurities: quality by design framework in capillary electrophoresis method development.
Caprini, C; Furlanetto, S; Mura, P; Orlandini, S; Pasquini, B; Pinzauti, S, 2015
)
0.42
"The aim of this study was to determine the impact of initial glyburide dosing on pregnancy outcomes."( Examining the Starting Dose of Glyburide in Gestational Diabetes.
Biggio, JR; Glover, AV; Harper, LM; Tita, A, 2016
)
0.96
"The objective of this study was to determine if there is a dose-response relationship between sulfonylureas and major adverse cardiovascular events (MACE)."( Dose-response relationship between sulfonylureas and major adverse cardiovascular events in elderly patients with type 2 diabetes.
Abdelmoneim, AS; Eurich, DT; Qiu, W; Senthilselvan, A; Simpson, SH, 2016
)
0.43
"Among new users of sulfonylureas, there appears to be a dose-response relationship between glyburide and MACE, but not for gliclazide."( Dose-response relationship between sulfonylureas and major adverse cardiovascular events in elderly patients with type 2 diabetes.
Abdelmoneim, AS; Eurich, DT; Qiu, W; Senthilselvan, A; Simpson, SH, 2016
)
0.65
" In areas of limited resources where the self-monitoring needed for accurate insulin dosing is not possible, where access to refrigeration for insulin storage is not universal, or severe needle phobia then the benefits of glyburide (controlling hyperglycemia) outweighs the harm of NICU admissions and macrosomia."( Pharmacokinetics, efficacy and safety of glyburide for treatment of gestational diabetes mellitus.
Davis, SN; Malek, R, 2016
)
0.88
" Patients were randomly assigned to receive 10 mg oral glibenclamide daily for 10 days (n = 29) or placebo in the same dosage (n = 23)."( Effects of Oral Glibenclamide on Brain Contusion Volume and Functional Outcome of Patients with Moderate and Severe Traumatic Brain Injuries: A Randomized Double-Blind Placebo-Controlled Clinical Trial.
Derakhshan, N; Eshraghian, H; Ghaffarpasand, F; Khalili, H; Niakan, A; Salehi, M; Shakibafard, A; Zahabi, B, 2017
)
0.46
"1) Pinacidil dose-dependently decreased gastric tone at a dosage of 30 (p = 0."( Roles of ATP sensitive potassium channel in modulating gastric tone and accommodation in dogs.
Chen, JD; Lei, Y; Li, S, 2017
)
0.46
" Interspecies dosing differences versus prior studies may play an important role in these findings."( Glibenclamide Produces Region-Dependent Effects on Cerebral Edema in a Combined Injury Model of Traumatic Brain Injury and Hemorrhagic Shock in Mice.
Hoshitsuki, K; Jackson, TC; Janesko-Feldman, KL; Jha, RM; Kochanek, PM; Minnigh, MB; Molyneaux, BJ; Park, SY; Poloyac, S; Vagni, VA; Wallisch, JS, 2018
)
0.48
" The effect of drying conditions on the morphology, moisture content, hardness, dosage uniformity, surface characteristics, and drug release mechanism of glibenclamide from the matrices was systematically investigated."( Controlled release of glibenclamide from monolithic silica subdermal implants produced by the sol-gel process and its use for hyperglycaemia treatment in a murine model.
Espinosa-Contreras, C; Flores-Cabrera, Y; Hernández-Abad, VJ; Marroquín-Segura, R; Mora-Guevara, JLA; Sánchez-González, EG, 2019
)
0.51
" Median frequencies of hypoglycemia and hyperglycemia were less than 5% of routine blood glucose assays and were similar with both dosage forms."( Glibenclamide oral suspension: Suitable and effective in patients with neonatal diabetes.
Baptiste, A; Beltrand, J; Berdugo, M; Bouazza, N; Boucheron, A; Busiah, K; Djerada, Z; Elie, C; Godot, C; Gozalo, C; Polak, M; Tréluyer, JM, 2019
)
0.51
" humilis or 2-hydroxy-destigloyl-6-deoxyswietenine acetate (mexicanolide 1) with glibenclamide resulted in a reduction of the antihyperglycemic effect while a significant increase was observed when they were dosed with metformin."( Multi-target antidiabetic mechanisms of mexicanolides from Swietenia humilis.
Haddad, PS; Mata, R; Navarrete, A; Noriega, LG; Ovalle-Magallanes, B; Tovar, AR; Tovar-Palacio, C, 2019
)
0.51
" Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing."( Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability.
Ali, HSM; Alqurshi, A; Hanafy, AF, 2019
)
0.81
"The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures."( Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability.
Ali, HSM; Alqurshi, A; Hanafy, AF, 2019
)
1
" The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability."( Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability.
Ali, HSM; Alqurshi, A; Hanafy, AF, 2019
)
0.81
" The established PBPK model was capable of accurately predicting complex rifampicin-induced alterations in the profiles of glibenclamide, repaglinide, and coproporphyrin I (an endogenous biomarker of OATP1B activities) with various dosing regimens."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
0.51
"A sensitive, rapid and cost-effective method based on HPTLC with UV detection was developed for the quantitation of Glibenclamide (GLIBEN), Rosiglitazone maleate (ROSI) and Metformin hydrochloride (MET) from a combined dosage form."( A Sensitive HPTLC Method for the Estimation of Glibenclamide, Rosiglitazone Maleate and Metformin Hydrochloride from a Multicomponent Dosage Form.
Abbulu, K; Bhende, SD; Varanasi, MB, 2020
)
0.56
" Total bolus osmotherapy dosing was quantified by "osmolar load"."( Osmotherapy for malignant cerebral edema in a phase 2 prospective, double blind, randomized, placebo-controlled study of IV glibenclamide.
Demchuk, A; Hinson, HE; Molyneaux, BJ; Romero, J; Sheth, KN; Sun, E; Taylor Kimberly, W; von Kummer, R, 2020
)
0.56
"A plethora of dissolution tests exists for oral dosage forms, with variations in selection of the dissolution medium, the hydrodynamics and the dissolution equipment."( Physiologically based pharmacokinetic model outputs depend on dissolution data and their input: Case examples glibenclamide and dipyridamole.
Dressman, J; Klumpp, L, 2020
)
0.56
"The aim of this research was the development and optimization of nanoniosomes for delivery of glibenclamide (Gbn) as hypoglycaemic agent to the lung in an inhaler dosage form."( Design, optimization, and
Abd Allah, FI; Abdel-Rashid, RS; Hashim, FM; Hassan, AA, 2021
)
0.62
" Group I acted as the control, whereas groups II, III, IV, and V were considered experimental groups which received a single dosage (150 mg/kg body weight) of alloxan (ALX) intraperitoneally (i."( Co-administration of
Kar, A; Panda, S; Sharma, N; Yadav, D, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
hypoglycemic agentA drug which lowers the blood glucose level.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
EC 2.7.1.33 (pantothenate kinase) inhibitorAn EC 2.7.1.* (phosphotransferases with an alcohol group as acceptor) inhibitor that interferes with the action of pantothenate kinase (EC 2.7.1.33).
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitorA EC 3.6.3.* (acid anhydride hydrolase catalysing transmembrane movement of substances) inhibitor that interferes with the action of channel-conductance-controlling ATPase (EC 3.6.3.49, also known as cystic fibrosis conductance regulator, CFCR).
[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 (2)

ClassDescription
N-sulfonylureaA urea in which one of the hydrogens attached to a nitrogen of the urea group is replaced by a sulfonyl group. The N-sulfonylurea moiety is a key group in various herbicides, as well as in a number of antidiabetic drugs used in the management of type 2 diabetis mellitus.
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[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 (2)

PathwayProteinsCompounds
Glibenclamide Action Pathway65
Drug induction of bile acid pathway025

Protein Targets (103)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency2.27400.003245.467312,589.2998AID2517
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency19.07280.140911.194039.8107AID2451
LuciferasePhotinus pyralis (common eastern firefly)Potency6.01200.007215.758889.3584AID588342
thioredoxin reductaseRattus norvegicus (Norway rat)Potency2.99350.100020.879379.4328AID488773; AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency30.25620.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency24.65710.173734.304761.8120AID1346859; AID1346924
USP1 protein, partialHomo sapiens (human)Potency70.79460.031637.5844354.8130AID743255
GLS proteinHomo sapiens (human)Potency0.63100.35487.935539.8107AID624146
SMAD family member 3Homo sapiens (human)Potency24.65710.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686979
GLI family zinc finger 3Homo sapiens (human)Potency1.24730.000714.592883.7951AID1259369
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency35.83700.000221.22318,912.5098AID743035; AID743036; AID743053; AID743063
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency18.86990.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.57880.00137.762544.6684AID914; AID915
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.12590.001318.074339.8107AID926
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.84930.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency34.37620.000417.946075.1148AID1346784
regulator of G-protein signaling 4Homo sapiens (human)Potency2.11920.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.60580.01237.983543.2770AID1645841
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency17.78280.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency18.11370.000214.376460.0339AID588532; AID720691; AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency33.27040.000817.505159.3239AID1159527; AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency58.91460.001530.607315,848.9004AID1224848; AID1224849; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency29.77890.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.26260.000229.305416,493.5996AID743069; AID743075; AID743091
GVesicular stomatitis virusPotency8.42300.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency26.83580.00108.379861.1304AID1645840
ParkinHomo sapiens (human)Potency9.20000.819914.830644.6684AID720572
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency13.71870.001024.504861.6448AID588534; AID588535; AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency20.44850.001019.414170.9645AID743094; AID743140; AID743191
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.43440.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency35.48130.016525.307841.3999AID602332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.44830.001723.839378.1014AID743083
Bloom syndrome protein isoform 1Homo sapiens (human)Potency100.00000.540617.639296.1227AID2364; AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency10.00000.00207.533739.8107AID891
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921423.934123.934123.9341AID1967
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.00000.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency4.15020.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency112.20203.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency43.86790.000627.21521,122.0200AID651741; AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency31.62280.00798.23321,122.0200AID2551
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.00230.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.70080.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.38720.00106.000935.4813AID943
lamin isoform A-delta10Homo sapiens (human)Potency11.22020.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Interferon betaHomo sapiens (human)Potency8.42300.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.42300.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency4.15020.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Guanine nucleotide-binding protein GHomo sapiens (human)Potency8.91251.995325.532750.1187AID624288
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency31.62281.000010.475628.1838AID1457
GABA theta subunitRattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.42300.01238.964839.8107AID1645842
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.48581.000012.224831.6228AID885
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.42300.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.16940.060110.745337.9330AID485368
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)33.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)10.50000.20005.677410.0000AID1473741
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki1.60001.60005.744010.0000AID679148
ATP-binding cassette sub-family C member 9Homo sapiens (human)IC50 (µMol)0.22000.22001.56004.3000AID201324
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)9.03330.40002.75008.6000AID1209456; AID679483; AID680335
Bile salt export pumpRattus norvegicus (Norway rat)Ki6.10000.30003.10006.1000AID679145
Bile salt export pumpHomo sapiens (human)IC50 (µMol)54.97500.11007.190310.0000AID1209455; AID1443980; AID1443986; AID1449628; AID1473738; AID1674183; AID681139; AID681155
Bile salt export pumpHomo sapiens (human)Ki27.50007.00008.25009.5000AID680940
Chymotrypsinogen ABos taurus (cattle)IC50 (µMol)360.00000.98004.05607.2000AID52776
Beta-lactamaseEscherichia coli K-12IC50 (µMol)300.00000.01502.46578.0000AID43431
ATP synthase subunit beta, mitochondrialBos taurus (cattle)IC50 (µMol)100.00000.48000.48000.4800AID68758
ATP synthase subunit delta, mitochondrialBos taurus (cattle)IC50 (µMol)100.00000.48000.48000.4800AID68758
ATP synthase subunit gamma, mitochondrialBos taurus (cattle)IC50 (µMol)100.00000.48000.48000.4800AID68758
ATP synthase subunit epsilon, mitochondrialBos taurus (cattle)IC50 (µMol)100.00000.48000.48000.4800AID68758
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)1.60200.00002.800510.0000AID625248
Cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC50 (µMol)15.00000.30000.32670.3800AID598317
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)100.00000.00031.38338.4000AID68758
Cholesteryl ester transfer proteinOryctolagus cuniculus (rabbit)IC50 (µMol)238.60000.02000.02500.0300AID485980
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.66000.00000.37905.6000AID1537172
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC50 (µMol)0.00430.00431.07038.2000AID201322
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)74.06550.00091.901410.0000AID147661; AID386536; AID420668; AID576612
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50 (µMol)0.11210.00431.36868.2000AID201322; AID201324
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Ki12.30001.84001.84001.8400AID682050
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki7.80003.00006.47788.5000AID678859
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC50 (µMol)10.00000.00041.441910.0000AID1527542
NACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)IC50 (µMol)12.00000.00502.180410.0000AID1286175
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)IC50 (µMol)39.10000.73103.79949.0780AID1323834
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)Ki1.67100.03101.20547.2910AID1323835
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)150.00000.00401.966610.0000AID1873199; AID679622
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50 (µMol)8.20000.05002.37979.7000AID1218863; AID1218864; AID1218865
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium channel subfamily K member 2Homo sapiens (human)EC50 (µMol)64.00000.18702.72248.1800AID1802150
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Km6.26000.70005.00608.0900AID680320
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (316)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
defense response to virusATP-binding cassette sub-family C member 9Homo sapiens (human)
action potentialATP-binding cassette sub-family C member 9Homo sapiens (human)
heart morphogenesisATP-binding cassette sub-family C member 9Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 9Homo sapiens (human)
response to ATPATP-binding cassette sub-family C member 9Homo sapiens (human)
negative regulation of blood pressureATP-binding cassette sub-family C member 9Homo sapiens (human)
fibroblast proliferationATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
coronary vasculature developmentATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac conductionATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
cardiac muscle cell contractionATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 9Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
cardiac ventricle developmentPotassium channel subfamily K member 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayPotassium channel subfamily K member 2Homo sapiens (human)
memoryPotassium channel subfamily K member 2Homo sapiens (human)
response to mechanical stimulusPotassium channel subfamily K member 2Homo sapiens (human)
response to axon injuryPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationPotassium channel subfamily K member 2Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 2Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of DNA biosynthetic processPotassium channel subfamily K member 2Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 2Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
digestionChymotrypsinogen ABos taurus (cattle)
antibiotic catabolic processBeta-lactamaseEscherichia coli K-12
response to antibioticBeta-lactamaseEscherichia coli K-12
proton transmembrane transportATP synthase subunit beta, mitochondrialBos taurus (cattle)
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)
proton transmembrane transportATP synthase subunit delta, mitochondrialBos taurus (cattle)
aerobic respirationATP synthase subunit delta, mitochondrialBos taurus (cattle)
mitochondrial proton-transporting ATP synthase complex assemblyATP synthase subunit delta, mitochondrialBos taurus (cattle)
proton transmembrane transportATP synthase subunit gamma, mitochondrialBos taurus (cattle)
proton transmembrane transportATP synthase subunit epsilon, mitochondrialBos taurus (cattle)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
cholesterol biosynthetic processCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
vesicle docking involved in exocytosisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
bicarbonate transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cholesterol transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
response to endoplasmic reticulum stressCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
transepithelial water transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of exocytosisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
sperm capacitationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
multicellular organismal-level water homeostasisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
intracellular pH elevationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
establishment of localization in cellCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
transmembrane transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
membrane hyperpolarizationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of enamel mineralizationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cellular response to cAMPCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
amelogenesisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of cyclic nucleotide-gated ion channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride transmembrane transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of voltage-gated chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cellular response to forskolinCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of cholesterol effluxPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
long-chain fatty acid transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of osteoblast differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of receptor signaling pathway via STATPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of low-density lipoprotein receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of MAP kinase activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adiponectin secretionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of connective tissue replacement involved in inflammatory response wound healingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
placenta developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of blood pressurePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of lipid storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of angiogenesisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
monocyte differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
epithelial cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to lipidPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
glucose homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
mRNA transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipoprotein transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
innate immune responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell fate commitmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell maturationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
rhythmic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
white fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of SMAD protein signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cholesterol transporter activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to hypoxiaPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of mitochondrial fissionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of extracellular matrix assemblyPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cellular response to transforming growth factor beta stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adipose tissue developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular endothelial cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
gluconeogenesisMalate dehydrogenase, cytoplasmicHomo sapiens (human)
NADH metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
NADP metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
malate metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
oxaloacetate metabolic processMalate dehydrogenase, cytoplasmicHomo sapiens (human)
tricarboxylic acid cycleMalate dehydrogenase, cytoplasmicHomo sapiens (human)
malate-aspartate shuttleMalate dehydrogenase, cytoplasmicHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
intracellular glucose homeostasisATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
female pregnancyATP-binding cassette sub-family C member 8Homo sapiens (human)
memoryATP-binding cassette sub-family C member 8Homo sapiens (human)
visual learningATP-binding cassette sub-family C member 8Homo sapiens (human)
response to pHATP-binding cassette sub-family C member 8Homo sapiens (human)
response to xenobiotic stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
response to zinc ionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of low-density lipoprotein particle clearanceATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of angiogenesisATP-binding cassette sub-family C member 8Homo sapiens (human)
response to lipopolysaccharideATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tumor necrosis factor productionATP-binding cassette sub-family C member 8Homo sapiens (human)
response to insulinATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of potassium ion transportATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of insulin secretionATP-binding cassette sub-family C member 8Homo sapiens (human)
neuromuscular processATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of glial cell proliferationATP-binding cassette sub-family C member 8Homo sapiens (human)
glutamate secretion, neurotransmissionATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of neuroblast migrationATP-binding cassette sub-family C member 8Homo sapiens (human)
cellular response to organic substanceATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
inorganic cation transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of uterine smooth muscle relaxationATP-binding cassette sub-family C member 8Homo sapiens (human)
positive regulation of tight junction disassemblyATP-binding cassette sub-family C member 8Homo sapiens (human)
negative regulation of blood-brain barrier permeabilityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion import across plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 8Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
action potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to hypoxiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ischemiaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ventricular cardiac muscle tissue developmentATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glucose metabolic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
apoptotic processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
determination of adult lifespanATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to xenobiotic stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to estradiolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to ATPATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to testosteroneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
negative regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of insulin secretionATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nervous system processATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
CAMKK-AMPK signaling cascadeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to nicotineATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to glucose stimulusATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cellular response to tumor necrosis factorATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inorganic cation transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
positive regulation of protein localization to plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
response to resveratrolATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion import across plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
regulation of monoatomic ion transmembrane transportATP-sensitive inward rectifier potassium channel 11Homo 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)
pattern recognition receptor signaling pathwayNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
negative regulation of acute inflammatory responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of type 2 immune responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
apoptotic processNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
defense responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
inflammatory responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
signal transductionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
osmosensory signaling pathwayNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
detection of biotic stimulusNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
negative regulation of interleukin-1 beta productionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of interleukin-1 beta productionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of interleukin-4 productionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
NLRP3 inflammasome complex assemblyNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
innate immune responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of T-helper 2 cell differentiationNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
negative regulation of inflammatory responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of inflammatory responseNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
protein homooligomerizationNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
protein maturationNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
pyroptosisNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cellular response to lipopolysaccharideNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cellular response to virusNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of T-helper 2 cell cytokine productionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
regulation of autophagyCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
regulation of cellular respirationCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
protein maturation by [2Fe-2S] cluster transferCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (142)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic cation channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium channel regulator activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 9Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 9Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 2Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingChymotrypsinogen ABos taurus (cattle)
serpin family protein bindingChymotrypsinogen ABos taurus (cattle)
beta-lactamase activityBeta-lactamaseEscherichia coli K-12
hydrolase activityBeta-lactamaseEscherichia coli K-12
protein bindingATP synthase subunit beta, mitochondrialBos taurus (cattle)
ATP bindingATP synthase subunit beta, mitochondrialBos taurus (cattle)
ATP hydrolysis activityATP synthase subunit beta, mitochondrialBos taurus (cattle)
proton-transporting ATPase activity, rotational mechanismATP synthase subunit beta, mitochondrialBos taurus (cattle)
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)
proton transmembrane transporter activityATP synthase subunit delta, mitochondrialBos taurus (cattle)
protein bindingATP synthase subunit gamma, mitochondrialBos taurus (cattle)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
intracellularly ATP-gated chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATP bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
bicarbonate transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
isomerase activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATP hydrolysis activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel regulator activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel inhibitor activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
enzyme bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
PDZ domain bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein-folding chaperone bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
Sec61 translocon complex bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ABC-type transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATPase-coupled transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
transcription cis-regulatory region bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
transcription coregulator bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
double-stranded DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
prostaglandin receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
enzyme bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peptide bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
identical protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear retinoid X receptor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
arachidonic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA binding domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
LBD domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
alpha-actinin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
R-SMAD bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
E-box bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
STAT family protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
malic enzyme activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
protein bindingMalate dehydrogenase, cytoplasmicHomo sapiens (human)
L-malate dehydrogenase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
diiodophenylpyruvate reductase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
hydroxyphenylpyruvate reductase activityMalate dehydrogenase, cytoplasmicHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
sulfonylurea receptor activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ADP bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
transmembrane transporter bindingATP-binding cassette sub-family C member 8Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 8Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATP-activated inward rectifier potassium channel activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activityATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
ankyrin bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
potassium ion bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
heat shock protein bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
transmembrane transporter bindingATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialATP-sensitive inward rectifier potassium channel 11Homo 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)
protein bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
ATP bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
ATP hydrolysis activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
protein-macromolecule adaptor activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
signaling adaptor activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
identical protein bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
peptidoglycan bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
ADP bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
sequence-specific DNA bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
molecular adaptor activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
phosphatidylinositol-4-phosphate bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
DNA-binding transcription factor bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
small molecule sensor activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cysteine-type endopeptidase activator activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
molecular condensate scaffold activityNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
phosphatidylinositol phosphate bindingNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
pyridoxal phosphate bindingCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
identical protein bindingCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
protein homodimerization activityCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
metal ion bindingCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
L-cysteine transaminase activityCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
2 iron, 2 sulfur cluster bindingCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (79)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
sarcomereATP-binding cassette sub-family C member 9Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 9Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 9Homo sapiens (human)
membraneATP-binding cassette sub-family C member 9Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
endoplasmic reticulum membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
cell surfacePotassium channel subfamily K member 2Homo sapiens (human)
apical plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
neuronal cell bodyPotassium channel subfamily K member 2Homo sapiens (human)
calyx of HeldPotassium channel subfamily K member 2Homo sapiens (human)
astrocyte projectionPotassium channel subfamily K member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionChymotrypsinogen ABos taurus (cattle)
serine protease inhibitor complexChymotrypsinogen ABos taurus (cattle)
outer membrane-bounded periplasmic spaceBeta-lactamaseEscherichia coli K-12
periplasmic spaceBeta-lactamaseEscherichia coli K-12
mitochondrial proton-transporting ATP synthase complexATP synthase subunit beta, mitochondrialBos taurus (cattle)
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)
mitochondrial envelopeATP synthase subunit delta, mitochondrialBos taurus (cattle)
mitochondrial proton-transporting ATP synthase complexATP synthase subunit delta, mitochondrialBos taurus (cattle)
proton-transporting ATP synthase complexATP synthase subunit delta, mitochondrialBos taurus (cattle)
mitochondrial proton-transporting ATP synthase complexATP synthase subunit gamma, mitochondrialBos taurus (cattle)
mitochondrial proton-transporting ATP synthase complex, catalytic sector F(1)ATP synthase subunit epsilon, mitochondrialBos taurus (cattle)
mitochondrial proton-transporting ATP synthase complexATP synthase subunit epsilon, mitochondrialBos taurus (cattle)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
nucleusCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytoplasmCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
lysosomal membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
early endosomeCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
endoplasmic reticulum membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytosolCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cell surfaceCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
apical plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
Golgi-associated vesicle membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
early endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
recycling endosomeCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
recycling endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein-containing complexCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel complexCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytosolCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
apical plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cytosolPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
intracellular membrane-bounded organellePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II transcription regulator complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
receptor complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
extracellular spaceMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytoplasmMalate dehydrogenase, cytoplasmicHomo sapiens (human)
centrosomeMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytosolMalate dehydrogenase, cytoplasmicHomo sapiens (human)
extracellular exosomeMalate dehydrogenase, cytoplasmicHomo sapiens (human)
cytosolMalate dehydrogenase, cytoplasmicHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
inward rectifying potassium channelATP-binding cassette sub-family C member 8Homo sapiens (human)
synaptic vesicle membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
sarcolemmaATP-binding cassette sub-family C member 8Homo sapiens (human)
potassium ion-transporting ATPase complexATP-binding cassette sub-family C member 8Homo sapiens (human)
membraneATP-binding cassette sub-family C member 8Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
acrosomal vesicleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
nuclear envelopeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
endosomeATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
inward rectifying potassium channelATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
intercalated discATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
T-tubuleATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
axolemmaATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
presynaptic membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
neuronal cell bodyATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cell body fiberATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
glutamatergic synapseATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
plasma membraneATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)
cytosolNACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)
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)
cytoplasmNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cytosolNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
membraneNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
Golgi membraneNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
extracellular regionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
nucleusNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cytoplasmNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
mitochondrionNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
endoplasmic reticulumNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
microtubule organizing centerNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
cytosolNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
interphase microtubule organizing centerNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
NLRP3 inflammasome complexNACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)
mitochondrionCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
mitochondrial outer membraneCDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (585)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID487898Antidiabetic activity in STZ-induced Wistar rat assessed as reduction in blood glucose level at 50 mg/kg, ig after 3 day relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID1377944Hypoglycemic effect in fasting Sprague-Dawley rat at 10 mg/kg, po measured up to 180 mins post dose2017European journal of medicinal chemistry, Sep-29, Volume: 138Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1636305Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as effect on hepatocytes surrounding central vein architecture at 2.5 mg/kg, po administered for 15 days by hematoxylin/eosin staining based microscopy2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID106801Inhibition of malate dehydrogenase (MDH)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1220020Drug absorption in streptozotocin-induced diabetes mellitus Sprague-Dawley rat jejunum at 10 ug/ml after 120 mins of in situ single-pass perfusion relative to normal rat2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID613542Antihyperlipidemic activity in in streptozotocin-induced diabetic rat model assessed as serum triglyceride level at 10 mg/kg/day, po dosed via gavage for 14 days administered 3 days after streptozotocin challenge by UV-spectrophotometry2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents.
AID223565Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 1 nM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID588215FDA HLAED, alkaline phosphatase increase2004Current 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.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current 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.
AID1220060Apparent hepatic clearance in normal Sprague-Dawley rat liver microsomes assessed per mg protein at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1251342Toxicity in STZ-induced diabetic Wistar rat model assessed as increase in body weight at 30 mg/kg, po repeated for 15 days by GOD-POD method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID201322Inhibition of human SUR1/Kir6.2 expressed in CHO cells2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1220053Drug metabolism in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as compound level at 4 uM after 60 mins (Rvb = 2.06 +/- 0.27 ug/ml)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID462815Antihyperglycemic activity against Han Wistar rat assessed as blood glucose level at 1 mg/kg, po after 45 mins by OGTT2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.
AID681155TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID588995Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, BSEP2010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID331895Antidiabetic effect in streptozo-nicotinamide rat model of diabetes assessed as change in blood glucose level at 100 mg/kg, po after 3 hrs relative to control2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID467613Volume of distribution at steady state in human2009European 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.
AID302758Solubility by shake flask method2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Poorly soluble marketed drugs display solvation limited solubility.
AID604743Displacement of radiolabeled warfarin from fatty acid containing human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID331897Antidiabetic effect in streptozo-nicotinamide rat model of diabetes assessed as change in blood glucose level at 100 mg/kg, po after 7 hrs relative to control2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1636279Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as change in fasting blood glucose level at 2.5 mg/kg, po administered on day 7 post STZ challenge measured immediately post dosage by glucometry (Rvb = 63.75 +/- 7.3 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1163351Antihyperglycemic activity in fasted hyperglycemic Wistar rat assessed as serum glucose level at 10 mg/kg, po measured 60 mins post dose by oral glucose tolerance test (Rvb = 182.55 +/- 6.95 mg/dL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1218864Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID749470Induction of adipogenesis in human bone marrow MSC assessed as AOC2 up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID764283Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of fasting blood glucose level at 20 mg/kg, po qd measured on day 15 (Rvb = 404.2 +/- 29.15 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1220066Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 10 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
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).
AID337873Hypoglycemic activity in fasted po dosed streptozotocin-induced diabetic ddY mouse assessed as decrease in blood glucose level after 6 hrs by glucose oxidase method1993Journal of natural products, Mar, Volume: 56, Issue:3
Isolation of pseudoprototimosaponin AIII from rhizomes of Anemarrhena asphodeloides and its hypoglycemic activity in streptozotocin-induced diabetic mice.
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.
AID218693Fold increase in IC50 vs beta-lactamaase with 1 mg/mL saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
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]
AID386536Inhibition of human ERG potassium channel2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
A binary QSAR model for classification of hERG potassium channel blockers.
AID1698008Hepatic clearance in Wistar Hannover rat at 1 mg/kg, iv
AID1230501Antidiabetic activity against IDX medium-treated human bone marrow mesenchymal stem cells assessed as induction of adiponectin production during adipogenesis after 6 days by ELISA2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Suncheonosides A-D, Benzothioate Glycosides from a Marine-Derived Streptomyces sp.
AID1220054AUC (0 to 60 mins) in normal Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220036Apparent oral volume of distribution in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID161275Binding affinity towards potassium channel of rat aorta using [3H]15 as radioligand1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Synthesis of and radioligand binding studies with a tritiated pinacidil analogue: receptor interactions of structurally different classes of potassium channel openers and blockers.
AID131965Plasma glucose after treatment in obese ob/ob mice at 5 mg/kg (po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1688197Solubility of compound in PBS at pH 7.4 by shake flask method2020European journal of medicinal chemistry, Feb-15, Volume: 188Minor chemical modifications of the aminosteroid derivative RM-581 lead to major impact on its anticancer activity, metabolic stability and aqueous solubility.
AID1220067Drug metabolism in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 10 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID485559Antihyperglycemic activity in Charles Foster-Wistar albino rat sucrose loaded model assessed as decrease of blood glucose level at 100 mg/kg, po administered 30 mins before glucose challenge measured up to 120 mins by glucometer2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
AID722840Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 4 hrs (Rvb = 291 +/- 6.40 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
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).
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID680335TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from male rat2001Toxicology, Oct-05, Volume: 167, Issue:1
Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt
AID1292312Antidiabetic activity in streptozotocin/nicotinamide-induced Wistar rat model of diabetes assessed as plasma glucose variation at 50 mg/kg, ig measured at 1 hr post dose by glucometric analysis (Rvb = 17 +/- 8%)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and molecular docking of N'-arylidene-5-(4-chlorophenyl)-1-(3,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carbohydrazides as novel hypoglycemic and antioxidant dual agents.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1163356Insulin secretagogue activity in fasted hyperglycemic Wistar rat assessed as insulinogenic index ratio at 10 mg/kg, po by ELISA method (Rvb = 0.66 ng/mg)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1870358Induction of adipogenesis in human differentiated BMMSC cells assessed as fold increase in adiponectin production at 10 uM measured on 5 day in presence of IDX induction medium by ELISA2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.
AID687530Antidiabetic activity in STZ-nicotinamide diabetic Wistar rat T2DM model assessed as decrease in blood glucose level at 5 mg/kg, po after 3 hrs by enzymatic glucose oxidase method relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP-1B: in vitro, in silico, and in vivo approaches.
AID681665TP_TRANSPORTER: inhibition of Taurochenodeoxycholate-stimulated ATPase activity (Glibenclamide: 60 uM) in membrane vesicles from Bsep-expressing Sf9 cells2001Hepatology (Baltimore, Md.), May, Volume: 33, Issue:5
Characterization of the mouse bile salt export pump overexpressed in the baculovirus system.
AID1211796Intrinsic clearance in cryopreserved human HepaRG cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID681861TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation in the presence of glyburide at a concentration of 200uM in MRP1-expressing HeLa cells
AID764237Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 3 hrs (Rvb = 384.33 +/- 17.33 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1220034Apparent oral volume of distribution in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID179723Plasma glucose levels of nondiabetic rats after 4 hour of drug administration (25 mg/Kg, po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID592337Antidiabetic activity in streptozotocin-induced diabetic ICR mouse assessed as change in blood glucose level at 10 mg/kg after 2 hrs by oral glucose tolerance test (RVb= -12.9 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID764282Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of fasting blood glucose level at 20 mg/kg, po qd measured on day 30 relative to control2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID679483TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from female rat2001Toxicology, Oct-05, Volume: 167, Issue:1
Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt
AID1211792Hepatic clearance in human2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID131963Plasma glucose after treatment in obese ob/ob mice at 20 mg/kg (po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID764269Antihyperlipidemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as increase of serum HDL-cholesterol level at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1873199Inhibition of ABCG2 (unknown origin) expressed in human MCF7/MX cells mediated mitoxantrone efflux assessed as intracellular mitoxantrone level preincubated with mitoxantrone followed by compound addition and measured upto 90 mins by FACSflow cytometry an2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID604747Aqueous solubility of the compound in phosphate buffer solution of pH 7.4 after 24 hrs by LC-UV analysis2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID1172785Antidiabetic activity in overnight fasted Wistar rat assessed as reduction in plasma glucose level at 30 mg/kg, po by oral glucose tolerance test2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID764262Renalprotective activity in Wistar albino rat assessed as protection against streptozotocin-induced increase in urea level in blood at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1636281Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as change in fasting blood glucose level at 2.5 mg/kg, po administered for 7 days post STZ challenge measured on day 14 by glucometry (Rvb = 63.75 +/- 7.3 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID478234Antidiabetic activity in Wistar albino rat assessed as reduction of fasting blood glucose level administered qd for 9 days by oral glucose tolerance test (RVb = 83.33 +/- 1.54 mg/dl)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Derivatives of benzimidazole pharmacophore: synthesis, anticonvulsant, antidiabetic and DNA cleavage studies.
AID1066947Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose relative to IBMX2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
The insulin secretory action of novel polycyclic guanidines: discovery through open innovation phenotypic screening, and exploration of structure-activity relationships.
AID487896Antidiabetic activity in STZ-induced Wistar rat assessed as reduction in blood glucose level at 50 mg/kg, ig after 1 day relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID722842Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 2 hrs (Rvb = 251 +/- 2.91 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
AID604742Displacement of radiolabeled dansylsarcosine from fatty acid-free human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID764239Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 1 hr (Rvb = 389.16 +/- 19 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID68762Inhibitory concentration towards rat mitochondrial F1F0-ATP synthase using a hexokinase / glucose-6-phosphate dehydrogenase coupled assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
AID1204822In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 4 hrs by glucometer analysis (Rvb = 385.2 +/- 8.94 mg/dl)2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
AID485980Inhibition of CETP in rabbit serum after 1 hr by fluorescent cholesteryl esters transfer assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
AID1220041Tmax in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220040Tmax in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
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]
AID1473740Inhibition 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 assay2013Toxicological 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.
AID654716Antidiabetic activity in normal ICR mouse assessed as increase in plasma insulin level at 5 mg/kg, ip after 60 mins by ELISA (Rvb = 52.5 +/- 4.6 pmol/L)2012Journal of natural products, Feb-24, Volume: 75, Issue:2
Hypoglycemic diterpenoids from Tinospora crispa.
AID680474TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.1 uM, Glibenclamide: 1000 uM) in Oatp1-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID1220038Cmax in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1486864Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose level at 10 mg/kg, po pretreated for 1 hr followed by glucose challenge by OGTT
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID396649Antihyperglycemic activity against sucrose-challenged streptozotocin-induced fasted Sprague-Dawley rat assessed as reduction in blood glucose at 100 mg/kg, po administered 30 mins before sucrose challenge measured after 5 hrs post sucrose dose relative to2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
AID1220013Terminal elimination half life in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1537172Binding affinity to PPARgamma (unknown origin) by TR-FRET assay2019Journal of natural products, 02-22, Volume: 82, Issue:2
Adiponectin-Secretion-Promoting Phenylethylchromones from the Agarwood of Aquilaria malaccensis.
AID487733Hypoglycemic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 7 hrs (RVb = -3.59 +/- 2.65 %)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID1473741Inhibition 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 assay2013Toxicological 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.
AID1556965Antidiabetic activity in Sprague-Dawley rat assessed as change in blood glucose level in fasting state at 10 mg/kg, po pretreated for 1 hr followed by glucose challenge and measured up to 120 mins by OGTT2019European journal of medicinal chemistry, Oct-01, Volume: 179Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID422006Hypoglycemic activity in normal Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route after 3 hrs by glucose oxidase method relative to control2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID1451040Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD at 10 uM by TR-FRET assay relative to control2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Polypharmacology of N
AID317692Antidiabetic activity in sucrose challenged streptozotocin-induced diabetic albino Sprague-Dawley rat model assessed as decrease in blood glucose level at 100 mg/kg, po2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID422010Antihyperglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route 7 days after streptozotocin challenge measured after 1.5 hrs of compound administration by glucose o2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
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
AID540209Volume of distribution at steady state in human after iv administration2008Drug 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.
AID179720Plasma glucose levels of nondiabetic rats after 0 hour of drug administration (25 mg/Kg, po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID592250Antihyperglycemic activity in ICR mouse assessed as change in blood glucose level at 10 mg/kg after 2 hrs by oral glucose tolerance test (RVb= -12 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID422013Antihyperglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route 7 days after streptozotocin challenge measured after 7 hrs of compound administration by glucose oxi2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID52778Fold decrease in IC50 vs chymotrypsinogen on pre-incubation2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID422012Antihyperglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route 7 days after streptozotocin challenge measured after 5 hrs of compound administration by glucose oxi2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID161273Inhibition of [125I]-I binding to ATP-inhibited Potassium channel receptor of Rat brain homogenate1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Expedient synthesis and biochemical properties of an [125I]-labeled analogue of glyburide, a radioligand for ATP-inhibited potassium channels.
AID714669Antihyperglycemic activity against sucrose loaded Charles Foster/Wistar albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge by glucometer2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice.
AID106799Fold increase in IC50 vs malate dehydrogenase (MDH) with 1 mg/ml saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID487734Antidiabetic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 1 hr (RVb = 20.18 % +/- 8.49%)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current 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.
AID1527542Inhibition of NLRP3 inflammasome activation in LPS-primed mouse bone marrow derived macrophages preincubated for 15 mins followed by addition of ATP and measured after 30 mins by immunoblotting analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases.
AID1636291Antidiabetic activity in STZ-induced diabetic Wistar rat blood assessed as HDL level at 2.5 mg/kg, po administered for 15 days (Rvb = 36.31 +/- 0.51 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID680595TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation by glyburide at a concentration of 200uM in MRP3-expressing MDCK cells
AID1451035Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as adiponectin level at 4 uM measured on day 7 after 48 hrs by ELISA2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Polypharmacology of N
AID681139TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID764261Renalprotective activity in Wistar albino rat assessed as protection against streptozotocin-induced increase in creatinine level in blood at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1220021Apparent effective permeability in streptozotocin-induced diabetes mellitus Sprague-Dawley rat jejunum at 10 ug/ml after 30 to 90 mins of in situ single-pass perfusion relative to normal rat2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID613541Antihyperlipidemic activity in in streptozotocin-induced diabetic rat model assessed as serum cholesterol level at 10 mg/kg/day, po dosed via gavage for 14 days administered 3 days after streptozotocin challenge by UV-spectrophotometry2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents.
AID679622TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells
AID1220055AUC (0 to 60 mins) in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID679851TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT1-expressing LLC-PK1 cells1999British journal of pharmacology, Nov, Volume: 128, Issue:6
Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2.
AID699541Inhibition 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 counting2012Journal 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.
AID1220046Drug excretion in urine of Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220044Drug excretion in bile of insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID599101Antihyperglycemic activity against sucrose challenged streptozotocin-induced diabetic Sprague-Dawley albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge measured after 5 hrs2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Design and synthesis of 3,5-diarylisoxazole derivatives as novel class of anti-hyperglycemic and lipid lowering agents.
AID764272Antihyperlipidemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of serum total cholesterol level at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID604744Displacement of radiolabeled dansylsarcosine from fatty acid containing human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID1292315Antidiabetic activity in streptozotocin/nicotinamide-induced Wistar rat model of diabetes assessed as plasma glucose variation at 50 mg/kg, ig measured at 7 hrs post dose by glucometric analysis (Rvb = -5 +/- 8%)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and molecular docking of N'-arylidene-5-(4-chlorophenyl)-1-(3,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carbohydrazides as novel hypoglycemic and antioxidant dual agents.
AID669735Induction of hypoglycemia in fasted Sprague-Dawley rat assessed as decrease in plasma glucose level below normal fasting level at 10 mg/kg, po2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
AID1636354Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as increase in fasting blood glucose level at 2.5 mg/kg, po administered for 15 days post STZ challenge measured on day 21 by glucometry2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID749472Induction of adipogenesis in human bone marrow MSC assessed as formation of intracellular lipid droplets at 10 uM after 15 days by oil red O staining in IDX condition relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID409942Inhibition of human recombinant MAOA by fluorimetric method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID669730Insulinotropic activity in rat INS1(833/15) cells assessed as increase in insulin secretion at 30 uM after 2 hrs by competitive enzyme immunoassay in the presence of 11 mM glucose2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
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.
AID764238Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 2 hrs (Rvb = 386.66 +/- 17.5 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID592328Antidiabetic activity in streptozotocin-induced diabetic ICR mouse assessed as change in blood glucose level at 10 mg/kg after 0.5 hr by oral glucose tolerance test (RVb= 51.9 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1281978Hypoglycemic effect in Kunming mouse assessed as reduction in fasting blood glucose level at 10 mg/kg, po measured at 1.5 to 9 hrs post dose by glucometry analysis2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
α-Glucosidase inhibition and antihyperglycemic activity of flavonoids from Ampelopsis grossedentata and the flavonoid derivatives.
AID1220032Oral clearance in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID540211Fraction unbound in human after iv administration2008Drug 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.
AID687532Antidiabetic activity in STZ-nicotinamide diabetic Wistar rat T2DM model assessed as decrease in blood glucose level at 5 mg/kg, po after 7 hrs by enzymatic glucose oxidase method relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP-1B: in vitro, in silico, and in vivo approaches.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal 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.
AID680809TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation by glyburide at a concentration of 200uM in MRP2-expressing MDCK cells
AID722843Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 1 hr (Rvb = 274 +/- 4.73 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
AID1188218Antidiabetic activity in streptozotocin-nicotinamide-induced NIDDM Wistar rat model assessed as reduction in blood glucose level at 5 mg/kg administered intragastrically measured at 5 hrs post dose relative to control2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect.
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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).
AID173800Compound evaluated for hypoglycemic activity by lowering blood glucose in streptozotocin-diabetic rats by 20% after oral administration; Inactive(less than 10% blood sugar decrease)1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID1220037Cmax in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID437026Induction of NO release in Wistar rat liver homogenate at 200 uM by amperometric detection method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
AID1220065Drug metabolism in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 40 uM sulfaphenazole (Rvb = 18%)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID106802Fold decrease in IC50 vs malate dehydrogenase (MDH) on pre-incubation2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
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).
AID331894Antidiabetic effect in streptozo-nicotinamide rat model of diabetes assessed as change in blood glucose level at 100 mg/kg, po after 1 hr relative to control2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.
AID305297Antihyperglycemic activity in sucrose loaded model of Sprague-Dawley albino rat assessed as reduction in blood glucose by AUC method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Chalcone based aryloxypropanolamines as potential antihyperglycemic agents.
AID722838Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 6 hrs (Rvb = 285 +/- 8.66 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
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).
AID223564Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 10 nM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID194737Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.3 mg/kg dose to fasted adult female rats versus a control group1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1220039Tmax in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID751721Displacement of [3H]Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 cells at 10 uM after 2 hrs relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1449628Inhibition 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 method2012Drug 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.
AID1636283Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as decrease in blood glucose level at 2.5 mg/kg, po administered for 15 days post STZ challenge measured on day 21 by glucometry relative to control2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1220028Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in absence of 40 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220057Half life in normal Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID764270Antihyperlipidemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of serum VLDL-cholesterol level at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1220061Apparent hepatic clearance in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed per mg protein at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID667956Growth inhibition of human U373 cells after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54N-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis.
AID80016Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 0.02 uM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1220064Drug metabolism in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 40 uM sulfaphenazole (Rvb = 38%)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID350897Antihyperglycemic activity against STZ-nicotinamide-induced diabetes in overnight fasted Wistar rat assessed as decrease in glycemia at 100 mg/kg, administered intragastrically after 5 to 7 hrs by glucose oxidase method2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Synthesis, in vitro and computational studies of protein tyrosine phosphatase 1B inhibition of a small library of 2-arylsulfonylaminobenzothiazoles with antihyperglycemic activity.
AID437025Induction of 20 mM glucose-stimulated insulin secretion in human pancreatic islet cells assessed as insulin stimulation index at 100 uM by immunoradiometric assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
AID1525556Inhibition of human TASK3 expressed in Xenopus oocytes at 100 uM by whole cell patch clamp assay relative to control2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
TASK Channels Pharmacology: New Challenges in Drug Design.
AID305298Antihyperglycemic activity in streptozotocin induced diabetic model of Sprague-Dawley albino rat assessed as reduction in blood glucose by AUC method2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Chalcone based aryloxypropanolamines as potential antihyperglycemic agents.
AID1204826In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 8 hrs by glucometer analysis (Rvb = 385.2 +/- 8.94 mg/dl)2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
AID1918192Inhibition of human OAT2 tv.1 variant expressed in HEK293 cells assessed as inhibition of [3H]cGMP uptake by scintillation analysis2022Journal 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.
AID1879483Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA2022Journal of natural products, 03-25, Volume: 85, Issue:3
Adiponectin-Secretion-Promoting Cyclic Peptide-Polyketide Hybrids from a Halophyte-Associated Fungus,
AID1473934Ratio of drug concentration at steady state in human at 1.25 to 25 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological 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.
AID1556096Hypoglycemic activity in diabetic rat assessed as decrease in blood glucose level at 150 mg/kg after 24 hrs relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Andrographolide: A natural product template for the generation of structurally and biologically diverse diterpenes.
AID613540Hypoglycemic activity in streptozotocin-induced diabetic rat model assessed as decrease in serum glucose level at 10 mg/kg/day, po dosed via gavage for 14 days administered 3 days after streptozotocin challenge by UV-spectrophotometry2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents.
AID678859TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT2-expressing LLC-PK1 cells1999British journal of pharmacology, Nov, Volume: 128, Issue:6
Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2.
AID1220014Mean residence time in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID422007Hypoglycemic activity in normal Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route after 5 hrs by glucose oxidase method relative to control2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1220025Drug absorption in normal Sprague-Dawley rat jejunum assessed as 200 uM BCRP inhibitor novobiocin-mediated increase in apparent effective permeability at 10 ug/ml measured at 45 mins of perfusion2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1636285Antidiabetic activity in STZ-induced diabetic Wistar rat blood assessed as creatinine level at 2.5 mg/kg, po administered for 15 days (Rvb = 0.56 +/- 0.03 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID194592Maximum % decrease of blood glucose (deltaBG) was observed within 1 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; NS =' not significant'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1220023Drug absorption in normal Sprague-Dawley rat jejunum at 10 ug/ml in presence of 50 to 200 uM BCRP inhibitor novobiocin2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID467612Fraction unbound in human plasma2009European 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.
AID1473935Ratio of drug concentration at steady state in human at 1.25 to 25 mg, po QD after 24 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells2013Toxicological 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.
AID226482Hill Coefficient calculated by curve fitting of data to a single binding site model1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.
AID1698010Hepatic clearance in human administered through iv dosing
AID1636277Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as body weight at 2.5 mg/kg, po administered for 15 days post STZ challenge measured on day 21 (Rvb = 330.7 +/- 9.2 g)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID654728Antidiabetic activity in diet-induced ICR mouse T2DM model assessed as increase in plasma insulin level at 5 mg/kg, ip after 60 mins by ELISA (Rvb = 123.5 +/- 10.2 pmol/L)2012Journal of natural products, Feb-24, Volume: 75, Issue:2
Hypoglycemic diterpenoids from Tinospora crispa.
AID654710Antidiabetic activity in normal ICR mouse assessed as reduction in plasma glucose level at 5 mg/kg, ip after 60 mins (Rvb = 102 +/- 3.7 mg/dL)2012Journal of natural products, Feb-24, Volume: 75, Issue:2
Hypoglycemic diterpenoids from Tinospora crispa.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID1674184Toxicity in po dosed human assessed as maximum daily dose2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID52776Compound was tested for the inhibition of Chymotrypsinogen2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1281979Hypoglycemic effect in Kunming mouse model of STZ-induced diabetes assessed as reduction in fasting blood glucose level at 10 mg/kg, po measured at 1.5 to 9 hrs post dose by glucometry analysis2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
α-Glucosidase inhibition and antihyperglycemic activity of flavonoids from Ampelopsis grossedentata and the flavonoid derivatives.
AID422008Hypoglycemic activity in normal Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route after 7 hrs by glucose oxidase method relative to control2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID487736Antidiabetic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 7 hrs (RVb = -10.51% +/- 5.53%)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID1443980Inhibition 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]-tauroch2010Toxicological 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.
AID485979Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
AID1220030Drug metabolism in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in absence of 40 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID680596TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation by glyburide at a concentration of 10uM in MRP3-expressing MDCK cells
AID764234Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 6 hrs (Rvb = 372.5 +/- 15.6 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID764235Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 5 hrs (Rvb = 372.2 +/- 16.6 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current 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.
AID1220027Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in absence of CYP2C11 antibody2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID315112Antihyperglycemic activity in sucrose loaded diabetic Sprague-Dawley rat model assessed as reduction of plasma glucose levels at 100 mg/kg, po2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines.
AID669738Induction of hypoglycemia in fasted Sprague-Dawley rat assessed as increase in insulin secretion level at 30 mg/kg, po after 30 mins2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
AID598317Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
An expeditious access to 5-pyrimidinol derivatives from cyclic methylglyoxal diadducts, formation of argpyrimidines under physiological conditions and discovery of new CFTR inhibitors.
AID1220005AUC (0 to infinity) in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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).
AID764236Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 20 mg/kg, po after 4 hrs (Rvb = 373.5 +/- 15.6 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1754624Inhibition of ATP-sensitive K+ channel in LPS-activated human monocytes assessed as inhibition of NLRP3 inflammasome activation-mediated IL-1beta release2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46Discovery of dronedarone and its analogues as NLRP3 inflammasome inhibitors with potent anti-inflammation activity.
AID1220022Drug efflux in streptozotocin-induced diabetes mellitus Sprague-Dawley rat jejunum at 1 mg/kg, iv after 60 mins of in situ single-pass perfusion relative to normal rat2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1163349Antihyperglycemic activity in fasted hyperglycemic Wistar rat assessed as serum glucose level at 10 mg/kg, po measured 15 mins post dose by oral glucose tolerance test (Rvb = 177.46 +/- 5.95 mg/dL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID681293TP_TRANSPORTER: inhibition of Calcein efflux (Calcein: 0.5 micro;M, Glibenclamide: 50-100 uM, increase intercellular calcein level by ca 4 fold ) in GLC4/Sb30 cells2001British journal of pharmacology, Feb, Volume: 132, Issue:3
The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells.
AID1688194Solubility of compound in PBS at pH 7.4 at 300 uM after 24 hrs by HPLC-UV analysis2020European journal of medicinal chemistry, Feb-15, Volume: 188Minor chemical modifications of the aminosteroid derivative RM-581 lead to major impact on its anticancer activity, metabolic stability and aqueous solubility.
AID1918193Dissociation constant, pKa of the compound2022Journal 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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1566638Increase in insulin secretion in high glucose-treated rat INS-1 cells at 0.15 uM preincubated with compound and 40 mM glucose for 48 hrs followed by stimulation with KRB buffer containing 5 to 30 mM glucose for 60 mins and measured by ELISA2019European journal of medicinal chemistry, Sep-15, Volume: 178New insights into the biological activities of Chrysanthemum morifolium: Natural flavonoids alleviate diabetes by targeting α-glucosidase and the PTP-1B signaling pathway.
AID1163353Insulin secretagogue activity in fasted hyperglycemic Wistar rat assessed as insulin level at 10 mg/kg, po measured 15 mins post dose by ELISA method (Rvb = 2.84 +/- 0.002 ng/mL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1211791Fraction unbound in human hepatocytes2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1066948Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
The insulin secretory action of novel polycyclic guanidines: discovery through open innovation phenotypic screening, and exploration of structure-activity relationships.
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1698003Fraction unbound in rat plasma
AID1220059Half life in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220029Drug metabolism in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in absence of 40 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID179722Plasma glucose levels of nondiabetic rats after 2 hour of drug administration (25 mg/Kg, po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID592249Antihyperglycemic activity in ICR mouse assessed as change in blood glucose level at 10 mg/kg after 1.5 hrs by oral glucose tolerance test (RVb= 2.5 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID592331Antidiabetic activity in streptozotocin-induced diabetic ICR mouse assessed as change in blood glucose level at 10 mg/kg after 1 hr by oral glucose tolerance test (RVb= 10.3 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID194171Effect of the compound (50 mg/kg, po) on rat blood sugar level which was given an oral glucose load (1 g/kg) 1 hr after the administration of compound1984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids.
AID1172794Increase in PPARgamma gene expression in mouse 3T3L1 cells at 10 uM incubated for 24 hrs by RT-PCR method2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current 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.
AID1172787Antidiabetic activity in Wistar rat model of streptozotocin-induced diabetes assessed as reduction in plasma glucose level at 30 mg/kg, po and dosage repeated for 15 days by GOD-POD method2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID173791Hypoglycemic activity by lowering blood glucose in normal rats by 20% after oral administration.1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID540212Mean residence time in human after iv administration2008Drug 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.
AID681862TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation in the presence of glyburide at a concentration of 10uM in MRP1-expressing HeLa cells
AID422005Hypoglycemic activity in normal Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route after 1.5 hrs by glucose oxidase method relative to control2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID1220012Terminal elimination half life in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID487730Hypoglycemic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 1 hr (RVb = 10.96 +/- 3.67 %)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID604741Displacement of radiolabeled warfarin from fatty acid-free human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID1172791Increase in body weight in Wistar rat model of streptozotocin-induced diabetes at 30 mg/kg, po measured over 15 days2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID478236Antidiabetic activity in Wistar albino rat assessed as reduction of blood glucose level administered qd for 9 days measured after 90 mins last post dose by oral glucose tolerance test (RVb = 135.7 +/- 2.9 mg/dl)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Derivatives of benzimidazole pharmacophore: synthesis, anticonvulsant, antidiabetic and DNA cleavage studies.
AID487900Antidiabetic activity in STZ-induced Wistar rat assessed as reduction in blood glucose level at 50 mg/kg, ig after 5 day relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID764279Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as increase of body weight at 20 mg/kg, po qd measured on day 15 (Rvb = -30.3%)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID1220006AUC (0 to infinity) in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID751656Displacement of [3H]Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 cells after 2 hrs2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1473738Inhibition 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 assay2013Toxicological 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.
AID194735Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; NS =' not significant'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
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).
AID1220052Drug metabolism in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as compound level at 4 uM after 60 mins (Rvb = 2.0 +/- 0.13 ug/ml)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1220008AUC (0 to t) in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1066945Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose relative to IBMX2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
The insulin secretory action of novel polycyclic guanidines: discovery through open innovation phenotypic screening, and exploration of structure-activity relationships.
AID1220018Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of CYP2C11 antibody (Rvb = 15%)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID179721Plasma glucose levels of nondiabetic rats after 1 hour of drug administration (25 mg/Kg, po)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antihyperglycemic activity of novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides.
AID1636289Antidiabetic activity in STZ-induced diabetic Wistar rat blood assessed as cholesterol level at 2.5 mg/kg, po administered for 15 days (Rvb = 80.09 +/- 9.35 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1251341Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID669731Insulinotropic activity in rat INS1(833/15) cells assessed as increase in insulin secretion at 30 uM after 2 hrs by competitive enzyme immunoassay in the presence of 16 mM glucose2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
AID749463Induction of adipogenesis in human bone marrow MSC assessed as adiponectin up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID1674183Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID437029Inhibition of ADP-induced platelet aggregation in human platelet-rich plasma at 100 uM treated 2 mins before ADP challenge by turbidimetric method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
AID1220031Oral clearance in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID478233Antidiabetic activity in Wistar albino rat assessed as reduction of blood glucose level administered qd for 9 days by glucose oxidation method (RVb = 79.17 +/- 0.48 mg/dl)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Derivatives of benzimidazole pharmacophore: synthesis, anticonvulsant, antidiabetic and DNA cleavage studies.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1292313Antidiabetic activity in streptozotocin/nicotinamide-induced Wistar rat model of diabetes assessed as plasma glucose variation at 50 mg/kg, ig measured at 3 hrs post dose by glucometric analysis (Rvb = -13 +/- 10%)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and molecular docking of N'-arylidene-5-(4-chlorophenyl)-1-(3,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carbohydrazides as novel hypoglycemic and antioxidant dual agents.
AID1636287Antidiabetic activity in STZ-induced diabetic Wistar rat blood assessed as urea level at 2.5 mg/kg, po administered for 15 days (Rvb = 62.98 +/- 6.21 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID194728Maximum % decrease of blood glucose (deltaBG) was observed within 3 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; NS =' not significant'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID681093TP_TRANSPORTER: inhibition of Sb(III) accumulation in the presence of glibenclamid at a concentration of 10uM in MRP1-expressing MCP cells2006FEBS letters, Dec-22, Volume: 580, Issue:30
Transport of antimony salts by Arabidopsis thaliana protoplasts over-expressing the human multidrug resistance-associated protein 1 (MRP1/ABCC1).
AID48985Binding affinity was determined by displacement of [3H]P1075 from its binding sites in canine cardiac membranes1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.
AID43431Compound was tested for the inhibition of beta-lactamase2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1220026Drug absorption in normal Sprague-Dawley rat jejunum assessed as 200 uM BCRP inhibitor novobiocin-mediated increase in apparent effective permeability at 10 ug/ml measured at 90 mins of perfusion2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID487732Hypoglycemic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 5 hrs (RVb = 1.21+/- 3.64 %)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID52774Fold increase in IC50 vs chymotrypsinogen with 1.0 mg/ml saponin2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID487735Antidiabetic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 3 hrs (RVb = -9.83 % +/- 5.67%)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID722837Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 7 hrs (Rvb = 280 +/- 6.51 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
AID1220016Mean residence time in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1188216Antidiabetic activity in streptozotocin-nicotinamide-induced NIDDM Wistar rat model assessed as reduction in blood glucose level at 5 mg/kg administered intragastrically measured at 1 hr post dose relative to control2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect.
AID1220049Drug excretion in feces of Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1163354Insulin secretagogue activity in fasted hyperglycemic Wistar rat assessed as insulin level at 10 mg/kg, po measured 30 mins post dose by ELISA method (Rvb = 0.75 +/- 0.007 ng/mL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1194039Hypoglycemic effect in Wistar albino rat assessed as effect on blood glucose at 0.25 mg/kg, po2015Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
Design and synthesis of new potassium channel activators derived from the ring opening of diazoxide: study of their vasodilatory effect, stimulation of elastin synthesis and inhibitory effect on insulin release.
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).
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).
AID1473932AUC in human at 1.25 to 25 mg, po QD after 24 hrs2013Toxicological 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.
AID409958Inhibition of bovine brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID764284Antihyperglycemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of fasting blood glucose level at 20 mg/kg, po qd measured on day 1 (Rvb = 416.4 +/- 24.2 mg/dl)2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID478235Antidiabetic activity in Wistar albino rat assessed as reduction of blood glucose level administered qd for 9 days measured after 30 mins last post dose by oral glucose tolerance test (RVb = 183.2 +/- 3.68 mg/dl)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Derivatives of benzimidazole pharmacophore: synthesis, anticonvulsant, antidiabetic and DNA cleavage studies.
AID1286175Inhibition of NLRP3 in LPS activated human monocytes after 30 mins by ELISA analysis in presence of ATP2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Inhibiting the Inflammasome: A Chemical Perspective.
AID749468Induction of adipogenesis in human bone marrow MSC assessed as AOC3 up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
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).
AID1218865Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
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).
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.
AID1918194Lipophilicity, log D of the compound2022Journal 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.
AID176492Hypoglycemic activity by lowering blood glucose in normal rats by 50% after oral administration.1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1220033Oral clearance in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1254061Toxicity in overnight fasted ICR mouse assessed as hypoglycemia at 15 mg/kg, po measured at 30 to 180 mins2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1636303Antidiabetic activity in STZ-induced diabetic Wistar rat liver assessed as effect on central vein architecture at 2.5 mg/kg, po administered for 15 days by hematoxylin/eosin staining based microscopy2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID764271Antihyperlipidemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of serum LDL level at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID599100Antihyperglycemic activity in Charles Foster/Wistar albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Design and synthesis of 3,5-diarylisoxazole derivatives as novel class of anti-hyperglycemic and lipid lowering agents.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1679374Anti-glycemic activity in C57 mouse assessed as reduction in blood glucose excursion measured for 120 mins by IPGTT2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Discovery of a novel potent GPR40 full agonist.
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).
AID1163358Effect on glycogen content in liver of fasted hyperglycemic Wistar rat assessed per gram of tissue at 10 mg/kg, po measured 3 hrs post dose (Rvb = 14.6 +/- 1.27 mg/g of tissue)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1220010AUC (0 to t) in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1220048Drug excretion in normal Sprague-Dawley rat feces at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID687531Antidiabetic activity in STZ-nicotinamide diabetic Wistar rat T2DM model assessed as decrease in blood glucose level at 5 mg/kg, po after 5 hrs by enzymatic glucose oxidase method relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP-1B: in vitro, in silico, and in vivo approaches.
AID1373882Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production at 10 uM measured on day 5 in presence of IDX by ELISA2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPARγ partial agonism.
AID680807TP_TRANSPORTER: inhibition of 5-carboxyfluorescein accumulation in MRP2-expressing MDCK cells
AID437022Hypoglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as reduction in blood glucose AUC level at 10 mg/kg, ip measured for 2 hrs (Rvb= 45318 mg/dl/2 h)2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
AID1636275Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as body weight at 2.5 mg/kg, po administered on day 7 post STZ challenge measured immediately post dosage (Rvb = 330.7 +/- 9.2 g)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID749469Induction of adipogenesis in human bone marrow MSC assessed as MAO-B up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID1251337Antidiabetic activity in Wistar rat assessed as reduction in blood glucose level at 30 mg/kg, po dosed 30 mins before glucose challenge and measured 30 and 60 mins post glucose challenge by OGTT method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID669726Insulinotropic activity in rat INS1(833/15) cells assessed as increase in insulin secretion at 30 uM after 2 hrs by competitive enzyme immunoassay in the presence of low concentration of glucose2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1220050Drug excretion in feces of insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1211798Intrinsic clearance in human using well stirred liver model by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1451041Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD at 10 uM by TR-FRET assay relative to control2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Polypharmacology of N
AID315113Antihyperglycemic activity in streptozotocin-induced diabetic mouse model assessed as reduction of plasma glucose levels at 100 mg/kg, po after 5 hrs2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines.
AID1220042Drug excretion in normal Sprague-Dawley rat bile at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1698009Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
AID1220045Drug excretion in normal Sprague-Dawley rat urine at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
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.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID331896Antidiabetic effect in streptozo-nicotinamide rat model of diabetes assessed as change in blood glucose level at 100 mg/kg, po after 5 hrs relative to control2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.
AID764258Antiatherosclerosis activity in Wistar albino rat streptozotocin-induced diabetic model assessed as protection from atherogenicity at 20 mg/kg, po qd for 30 days relative to control2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID43563Fold decrease in IC50 vs beta-lactamase on pre-incubation2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID667965Cell cycle arrest in human U373 cells assessed as accumulation at G0/G1 phase at 10 to 30 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis2012European journal of medicinal chemistry, Aug, Volume: 54N-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis.
AID1163359Toxicity in fasted hyperglycemic Wistar rat assessed as LDH level at 10 mg/kg, po by spectrophotometry based LDH release assay (Rvb = 75.63 +/- 7.08 IU/L)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1288104Toxicity in overnight fasted ICR mouse assessed as hypoglycemic effect at 15 mg/kg, po after 30 to 120 mins by OGTT method2016European journal of medicinal chemistry, May-04, Volume: 113Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID485558Antihyperglycemic activity in Sprague-Dawley albino rat streptozotocin-induced beta-cell damaged diabetic model assessed as decrease of blood glucose level at 100 mg/kg, po administered 30 mins before glucose challenge measured after 5 hrs by glucometer2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1204820In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 2 hrs by glucometer analysis (Rvb = 385.2 +/- 8.94 mg/dl)2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
AID80017Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 0.2 uM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID1473835Stimulation 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 assay2013Toxicological 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.
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]
AID1188219Antidiabetic activity in streptozotocin-nicotinamide-induced NIDDM Wistar rat model assessed as reduction in blood glucose level at 5 mg/kg administered intragastrically measured at 7 hrs post dose relative to control2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect.
AID1451034Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as adiponectin level at 20 uM measured on day 7 after 48 hrs by ELISA2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Polypharmacology of N
AID540210Clearance in human after iv administration2008Drug 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.
AID223566Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 3 nM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID80019Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 2 uM2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas.
AID1220051Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as compound level at 4 uM after 60 mins (Rvb = 2.06 +/- 0.12 ug/ml)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID76398The inhibitory concentration was measured on guinea pig cardiomyocytes2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID176587Half-maximal effective dose was measured on rat blood glucose after administrating at 4 hr1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1918890Induction of adipogenesis in differentiated human BMMSC cells assessed as fold increase in adiponectin level at 5 uM in presence of IDX by ELISA relative to control2022Journal of natural products, 12-23, Volume: 85, Issue:12
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus,
AID1220004Cmax in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1636350Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as increase in body weight at 2.5 mg/kg, po administered for 15 days post STZ challenge measured on day 212016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1188217Antidiabetic activity in streptozotocin-nicotinamide-induced NIDDM Wistar rat model assessed as reduction in blood glucose level at 5 mg/kg administered intragastrically measured at 3 hrs post dose relative to control2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect.
AID1218863Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID588968Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP2B12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID681473TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.035 uM, Glibenclamide: 100 uM) in CC531mdr+ cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
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]
AID422011Antihyperglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route 7 days after streptozotocin challenge measured after 3 hrs of compound administration by glucose oxi2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID1323835Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID764273Antihyperlipidemic activity in Wistar albino rat streptozotocin-induced diabetic model assessed as reduction of serum triglyceride level at 20 mg/kg, po qd for 30 days2013European journal of medicinal chemistry, Aug, Volume: 66Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.
AID665545Hypoglycemic activity in glucose-fed normoglycemic Wistar rat assessed as decrease in rise of blood glucose at 5 to 10 mg/kg, po single dose measured up to 4 hrs post dose by oral glucose tolerance test2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors.
AID409943Inhibition of human recombinant MAOB by fluorimetric method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID218694Fold increase in IC50 vs beta-lactamase with 10x increased enzyme2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1220024Drug absorption in normal Sprague-Dawley rat jejunum assessed as 50 to 200 uM BCRP inhibitor novobiocin-mediated increase in apparent effective permeability at 10 ug/ml2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1698011Fraction unbound in human plasma
AID687529Antidiabetic activity in STZ-nicotinamide diabetic Wistar rat T2DM model assessed as decrease in blood glucose level at 5 mg/kg, po after 1 hr by enzymatic glucose oxidase method relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Antidiabetic activity of some pentacyclic acid triterpenoids, role of PTP-1B: in vitro, in silico, and in vivo approaches.
AID749045Hypoglycemic activity in STZ-nicotinamide-induced Wistar rat diabetic model at 5 mg/kg, po after 1 to 7 hrs2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Discovery, synthesis and in combo studies of a tetrazole analogue of clofibric acid as a potent hypoglycemic agent.
AID1220009AUC (0 to t) in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1486865Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as increase in insulin secretion at 10 mg/kg, po pretreated for 1 hr followed by glucose challenge by OGTT
AID1636301Antioxidant activity in STZ-induced diabetic Wistar rat liver assessed as SOD level measured per mg of protein at 2.5 mg/kg, po administered for 15 days by NBT reduction test (Rvb = 0.22 +/- 0.06 microM/min)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID201324Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID1542893Induction of hypoglycemia in fasting normal ICR mouse assessed as reduction in blood glucose level at 15 mg/kg, po measured up to 3 hrs post dose2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Design, synthesis and biological activity of deuterium-based FFA1 agonists with improved pharmacokinetic profiles.
AID1163350Antihyperglycemic activity in fasted hyperglycemic Wistar rat assessed as serum glucose level at 10 mg/kg, po measured 30 mins post dose by oral glucose tolerance test (Rvb = 190.15 +/- 1.77 mg/dL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1220056AUC (0 to 60 mins) in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID680320TP_TRANSPORTER: uptake in OATP2B1-expressing HEK293 cells2005Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 33, Issue:4
Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B.
AID576612Inhibition of human ERG2011European 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.
AID1163355Insulin secretagogue activity in fasted hyperglycemic Wistar rat assessed as insulin level at 10 mg/kg, po measured 60 mins post dose by ELISA method (Rvb = 0.59 +/- 0.004 ng/mL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1636352Antidiabetic activity in STZ-induced diabetic Wistar rat assessed as change in fasting blood glucose level at 2.5 mg/kg, po administered for 15 days post STZ challenge measured on day 21 by glucometry (Rvb = 63.75 +/- 7.3 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID161279Mean maximal plasma concentration2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID264867Antihyperglycemic activity in sucrose-loaded Sprague-Dawley rat at 100 mg/kg2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Novel substituted naphthalen-1-yl-methanone derivatives as anti-hyperglycemic agents.
AID1220015Mean residence time in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID180678The inhibitory concentration was measured on the rat insulinoma cell line RIN-m5F2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID599103Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in blood glucose level measured after 3 days relative to control2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Design and synthesis of 3,5-diarylisoxazole derivatives as novel class of anti-hyperglycemic and lipid lowering agents.
AID1698005Ratio of drug level in Wistar Hannover rat blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID487737Antidiabetic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 5 hrs (RVb = -1.17% +/- 8.77%)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID422009Hypoglycemic activity in normal Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route after 9 hrs by glucose oxidase method relative to control2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID1211794Fraction unbound in blood (not specified)2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1220011Terminal elimination half life in normal Sprague-Dawley rat at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1537168Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production measured on day 5 in presence of IDX by ELISA2019Journal of natural products, 02-22, Volume: 82, Issue:2
Adiponectin-Secretion-Promoting Phenylethylchromones from the Agarwood of Aquilaria malaccensis.
AID705946Antidiabetic activity in overnight fasted Wister Han rat assessed as reduction in blood glucose level at 1 mg/kg body weight, po administered 30 mins prior to glucose challenge within 45 mins (Rvb = 155 mg/dl)2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
AID1220043Drug excretion in bile of Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID315114Antihyperglycemic activity in streptozotocin-induced diabetic mouse model assessed as reduction of plasma glucose levels at 100 mg/kg, po after 24 hrs2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines.
AID654709Antidiabetic activity in diet-induced ICR mouse T2DM model assessed as reduction in plasma glucose level at 5 mg/kg, ip after 60 mins (Rvb = 170 +/- 2.8 mg/dL)2012Journal of natural products, Feb-24, Volume: 75, Issue:2
Hypoglycemic diterpenoids from Tinospora crispa.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID422014Antihyperglycemic activity in streptozotocin-induced diabetic Wistar rat assessed as variation in glycemia at 10 mg/kg administered via intragastric route 7 days after streptozotocin challenge measured after 9 hrs of compound administration by glucose oxi2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Hypoglycemic activity of extracts and compounds from the leaves of Hintonia standleyana and H. latiflora: potential alternatives to the use of the stem bark of these species.
AID1637020Induction of insulin secretion in human pancreatic islets at 1 uM in presence of glucose2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.
AID1486866Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose AUC at 10 mg/kg, po pretreated for 1 hr followed by glucose challenge after 1 hr of compound dosing measured up to 120 mins post glucose challenge by OGTT
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).
AID682039TP_TRANSPORTER: inhibition of Carboxy-2',7'-dichlorofluorescein efflux (Calcein: 0.5 micro;M, Glibenclamide, 50-100 uM, increase intercellular CF level by ~2 fold) in isolated rat hepatocytes2001British journal of pharmacology, Feb, Volume: 132, Issue:3
The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells.
AID1066946Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
The insulin secretory action of novel polycyclic guanidines: discovery through open innovation phenotypic screening, and exploration of structure-activity relationships.
AID540213Half life in human after iv administration2008Drug 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.
AID396648Antihyperglycemic activity against sucrose-loaded Charles-Foster Wistar albino rat assessed as reduction in blood glucose at 100 mg/kg, po administered 30 mins before sucrose challenge relative to control2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1204828In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 8 hrs by glucometer analysis2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
AID437024Induction of 20 mM glucose-stimulated insulin secretion in human pancreatic islet cells assessed as insulin stimulation index at 10 uM by immunoradiometric assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
AID400352Antihyperglycemic effect in STZ-diabetic ddY mouse assessed as reduction in blood glucose level at 30 umol/kg, ip after 6 hrs by glucose oxidase method1998Journal of natural products, Mar, Volume: 61, Issue:3
Antihyperglycemic effects of N-containing sugars from Xanthocercis zambesiaca, Morus bombycis, Aglaonema treubii, and Castanospermum australe in streptozotocin-diabetic mice.
AID1636299Antioxidant activity in STZ-induced diabetic Wistar rat liver assessed as glutathione peroxidase level measured as NADPH consumption per mg of protein at 2.5 mg/kg, po administered for 15 days (Rvb = 10 +/- 0.6 microM/min)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID487899Antidiabetic activity in STZ-induced Wistar rat assessed as reduction in blood glucose level at 50 mg/kg, ig after 4 day relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
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]
AID679148TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes2000European journal of pharmacology, Jun-16, Volume: 398, Issue:2
Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1636293Antidiabetic activity in STZ-induced diabetic Wistar rat blood assessed as LDL level at 2.5 mg/kg, po administered for 15 days (Rvb = 23.11 +/- 9.82 mg/dl)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID749464Induction of adipogenesis in human bone marrow MSC assessed as PPARgamma up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID1220063Drug metabolism in normal Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 40 uM sulfaphenazole (Rvb = 8%)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID487731Hypoglycemic activity in Wistar rat assessed as change in blood glucose level at 50 mg/kg, ig after 3 hrs (RVb = 1.39 +/- 5.895 %)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID1163352Antihyperglycemic activity in fasted hyperglycemic Wistar rat assessed as serum glucose level at 10 mg/kg, po measured 180 mins post dose by oral glucose tolerance test (Rvb = 141.15 +/- 4.47 mg/dL)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID1473936Ratio of drug concentration at steady state in human at 1.25 to 25 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological 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.
AID1323834Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID317690Antidiabetic activity in sucrose loaded albino Sprague-Dawley rat model assessed as decrease in blood glucose level at 100 mg/kg, po2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID749471Induction of adipogenesis in human bone marrow MSC assessed as MAO-A up-regulation by RT-PCR analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
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.
AID592247Antihyperglycemic activity in ICR mouse assessed as change in blood glucose level at 10 mg/kg after 0.5 hr by oral glucose tolerance test (RVb= 59 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID613543Antihyperlipidemic activity in high-cholesterol diet-induced hypercholesterolemia Swiss albino rat model assessed as reduction in serum cholesterol level at 10 mg/kg/day, po administered via gavage simultaneously with diet cocktail for 14 days by UV-spect2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1163357Effect on glycogen content in skeletal muscle of fasted hyperglycemic Wistar rat assessed per gram of tissue at 10 mg/kg, po measured 3 hrs post dose (Rvb = 8.6 +/- 1 mg/g of tissue)2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel sulfonyl(thio)urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds.
AID679745TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.0175 uM, Glibenclamide: 100 uM) in CEM/VBL600 cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID1233699Hypoglycemic effect in Wistar rat model of streptozotocin-induced type-2 diabetes mellitus assessed as reduction in blood glucose level at 5 mg/kg, ig after 7 hrs2015European journal of medicinal chemistry, Jul-15, Volume: 1001,5-Diarylpyrazole and vanillin hybrids: Synthesis, biological activity and DFT studies.
AID592334Antidiabetic activity in streptozotocin-induced diabetic ICR mouse assessed as change in blood glucose level at 10 mg/kg after 1.5 hrs by oral glucose tolerance test (RVb= 0.005 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID264868Antihyperglycemic activity in sucrose charged streptozotocin-induced beta cell damaged diabetic Sprague-Dawley rat at 100 mg/kg2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Novel substituted naphthalen-1-yl-methanone derivatives as anti-hyperglycemic agents.
AID1220047Drug excretion in urine of insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID194589Maximum % decrease of blood glucose (deltaBG) was observed within 0.5 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; NS =' not significant'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1473933Drug concentration at steady state in human at 1.25 to 25 mg, po QD after 24 hrs2013Toxicological 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.
AID1220062Apparent hepatic clearance in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed per mg protein at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID566349Inhibition of rat K+ATP channel2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID344048Insulinotropic activity in rat INS1 cells assessed as glucose-mediated insulin release at 1 ug/ml by radioimmunoassay relative to glucose2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Synthesis and biological activity of some new flavonyl-2,4-thiazolidinediones.
AID1292314Antidiabetic activity in streptozotocin/nicotinamide-induced Wistar rat model of diabetes assessed as plasma glucose variation at 50 mg/kg, ig measured at 5 hrs post dose by glucometric analysis (Rvb = -2 +/- 6%)2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and molecular docking of N'-arylidene-5-(4-chlorophenyl)-1-(3,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carbohydrazides as novel hypoglycemic and antioxidant dual agents.
AID1204824In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 6 hrs by glucometer analysis (Rvb = 385.2 +/- 8.94 mg/dl)2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
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).
AID1211797Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs.
AID679145TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells2000Gastroenterology, Feb, Volume: 118, Issue:2
Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.
AID680940TP_TRANSPORTER: inhibition of Taurocholate uptake(Glibenclamide 30uM, 50 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus2002Gastroenterology, Nov, Volume: 123, Issue:5
The human bile salt export pump: characterization of substrate specificity and identification of inhibitors.
AID722841Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 3 hrs (Rvb = 263 +/- 10.67 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
AID681852TP_TRANSPORTER: inhibition of Digoxin uptake (Digoxin: 0.05 uM, Glibenclamide: 1000 uM) in Oatp2-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID1062234Hypoglycemic activity in STZ-nicotinamide Wistar rat model of diabetes at 50 mg/kg administered intragastrically as single dose measured after 7 hrs relative to control2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, hypoglycemic activity and molecular modeling studies of pyrazole-3-carbohydrazides designed by a CoMFA model.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID665546Hypoglycemic activity in normoglycemic Wistar rat at 10 mg/kg, po administered as single dose measured up to 3 hrs post dose2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors.
AID467611Dissociation constant, pKa of the compound2009European 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.
AID1486862Toxicity in HFD-fed C57BL/6J mouse assessed as induction of hypoglycemia at 10 mg/kg, po after 1 hr
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID396651Antihyperglycemic activity against C57BL/KsBom db/db type 2 diabetic mouse model assessed as decrease in postprandial blood glucose level on day 3 by OGTT relative to control2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
AID485557Antihyperglycemic activity in Sprague-Dawley albino rat streptozotocin-induced beta-cell damaged diabetic model assessed as decrease of blood glucose level at 100 mg/kg, po administered 30 mins before glucose challenge measured after 24 hrs by glucometer2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
AID1220017Drug metabolism in insulin treated streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes assessed as remaining parent compound level at 4 uM after 60 mins in presence of 10 uM sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID592248Antihyperglycemic activity in ICR mouse assessed as change in blood glucose level at 10 mg/kg after 1 hr by oral glucose tolerance test (RVb= 1.5 %)2011Journal of natural products, Mar-25, Volume: 74, Issue:3
(Z)-3-butylidenephthalide from Ligusticum porteri , an α-glucosidase inhibitor.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID699540Inhibition 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 counting2012Journal 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.
AID1172790Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay relative to rosiglitazone2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1251339Antidiabetic activity in STZ-induced diabetic Wistar rat model assessed as reduction in blood glucose level at 30 mg/kg, po repeated for 15 days by GOD-POD method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1251344Increase in PPARgamma mRNA expression in mouse 3T3L1 cells at 10 uM incubated for 24 hrs by RT-PCR method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID722839Antidiabetic activity in albino rat diabetic model assessed as plasma glucose level measured after 5 hrs (Rvb = 275 +/- 3.53 mg/dl)2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Dual action spirobicycloimidazolidine-2,4-diones: antidiabetic agents and inhibitors of aldose reductase-an enzyme involved in diabetic complications.
AID1220019Drug absorption in streptozotocin-induced diabetes mellitus Sprague-Dawley rat jejunum at 10 ug/ml after 30 mins of in situ single-pass perfusion relative to normal rat2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID194734Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; ND ='not determined'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1636297Antioxidant activity in STZ-induced diabetic Wistar rat liver assessed as catalase level measured as H2O2 consumption per mg of protein at 2.5 mg/kg, po administered for 15 days (Rvb = 68.9 +/- 11.1 microM/min)2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antidiabetic effect, antioxidant activity, and toxicity of 3',4'-Di-O-acetyl-cis-khellactone in Streptozotocin-induced diabetic rats.
AID1251345Solubility of the compound2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1220007AUC (0 to infinity) in insulin treated Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1220058Half life in streptozotocin-induced diabetes mellitus Sprague-Dawley rat liver microsomes at 4 uM after 60 mins2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID1288420Toxicity in ICR mouse assessed as hypoglycemic effect at 15 mg/kg, po measured up to 180 mins2016Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID487897Antidiabetic activity in STZ-induced Wistar rat assessed as reduction in blood glucose level at 50 mg/kg, ig after 2 day relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal 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).
AID1698006Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
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.
AID194596Maximum % decrease of blood glucose (deltaBG) was observed within 2 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; NS =' not significant'1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Repaglinide and related hypoglycemic benzoic acid derivatives.
AID317691Antidiabetic activity in streptozotocin-induced diabetic albino Sprague-Dawley rat model assessed as decrease in blood glucose level at 100 mg/kg, po2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID1220035Apparent oral volume of distribution in Sprague-Dawley rat model of streptozotocin-induced diabetes mellitus at 10 mg/kg, po by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Combined contributions of impaired hepatic CYP2C11 and intestinal breast cancer resistance protein activities and expression to increased oral glibenclamide exposure in rats with streptozotocin-induced diabetes mellitus.
AID68758Inhibitory concentration towards rat mitochondrial F1F0 ATP hydrolase using a pyruvate kinase / lactate dehydrogenase system2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
AID147661K+ channel blocking activity in neuroblastoma cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & 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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The 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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346573Mouse Kir6.2 (Inwardly rectifying potassium channels)1995Science (New York, N.Y.), Nov-17, Volume: 270, Issue:5239
Reconstitution of IKATP: an inward rectifier subunit plus the sulfonylurea receptor.
AID1346885Human CFTR (CFTR)1992The Journal of general physiology, Oct, Volume: 100, Issue:4
Effect of ATP-sensitive K+ channel regulators on cystic fibrosis transmembrane conductance regulator chloride currents.
AID1346630Rat Kir6.2 (Inwardly rectifying potassium channels)1996The Journal of biological chemistry, Oct-04, Volume: 271, Issue:40
A novel sulfonylurea receptor forms with BIR (Kir6.2) a smooth muscle type ATP-sensitive K+ channel.
AID1346573Mouse Kir6.2 (Inwardly rectifying potassium channels)1996Neuron, May, Volume: 16, Issue:5
A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K+ channels.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID493017Wombat Data for BeliefDocking2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS 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.
AID1802150TREK1 Assay from Article 10.1111/cbdd.12810: \\Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.\\2016Chemical biology & drug design, Dec, Volume: 88, Issue:6
Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,243)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990930 (14.90)18.7374
1990's1993 (31.92)18.2507
2000's1819 (29.14)29.6817
2010's1244 (19.93)24.3611
2020's257 (4.12)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 84.69

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.

MetricThis Compound (vs All)
Research Demand Index84.69 (24.57)
Research Supply Index8.88 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index156.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (84.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials620 (9.46%)5.53%
Reviews250 (3.81%)6.00%
Case Studies274 (4.18%)4.05%
Observational4 (0.06%)0.25%
Other5,406 (82.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (102)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 1 Study for Testing Efficacy of Cissus Verticillata L Infusion in Controlling Glucose Concentration [NCT01145534]Phase 1/Phase 215 participants (Actual)Interventional2009-01-31Completed
A Multicenter, Randomized, Double-Blind Placebo-Controlled Phase 3 Trial to Evaluate the Efficacy and Safety of Saxagliptin in Combination With Glyburide in Subjects With Type 2 Diabetes Who Have Inadequate Glycemic Control With Glyburide Alone [NCT00313313]Phase 3768 participants (Actual)Interventional2006-04-30Completed
A Phase 1, Open-Label, Parallel, Sequential, Multi-part Study to Evaluate the Effect of IW-3718 on the Pharmacokinetics of an Oral Contraceptive, Levothyroxine, Glyburide, and Digoxin in Healthy Adult Volunteers [NCT03856970]Phase 187 participants (Actual)Interventional2019-03-11Completed
Phase 1 Study of Randomized Clinical Trial Comparing Vitamin C Supplementation Plus Oral Hypoglycemic Drugs Versus Hypoglycemic Drugs Alone on Serum Selenium, Zinc, Copper and Malondialdehyde Levels in Type 2 Diabetes Mellitus and Its Microvascular Compli [NCT01319734]Phase 150 participants (Anticipated)Interventional2011-02-28Recruiting
Comparative Open-label,Randomized, Fasting, Single Dose, Two-way Crossover Bioequivalence Study of Glibenclamide From Glibesyn 5 mg Tablets (Medochemie LTD Cyprus) and Daonil 5 mg Tablets (Sanofi-Aventis Cyprus Ltd. ) [NCT03855306]Phase 127 participants (Actual)Interventional2018-06-30Completed
A Multi-center, Double-blind, Placebo-controlled, Randomized Study to Compare the Effect of a Subcutaneous Canakinumab Administration to Placebo in Patients With Impaired Glucose Tolerance or Patients With Type 2 Diabetes Treated With Differing Baseline D [NCT01068860]Phase 2246 participants (Actual)Interventional2010-02-28Completed
Glibenclamide in Aneurysmatic Subarachnoid Hemorrhage: A Prospective and Randomized Study [NCT03569540]Phase 450 participants (Anticipated)Interventional2018-07-03Recruiting
Investigation Into Cardioprotective Effect of Glucagon-like Peptide-1 and it's Mechanism of Action During Myocardial Ischaemia [NCT02128022]Phase 132 participants (Actual)Interventional2014-07-31Completed
Effect of Acupuncture to Endothelial Dysfunction Induced by Ischemia-reperfusion Injury Via Adenosine Triphosphate-sensitive Potassium Channels or Prostaglandin Pathway [NCT02255006]36 participants (Anticipated)Interventional2014-05-31Recruiting
Tolerance and Acceptability of Glibentek in Patients With Neonatale Diabetes Secondary to Mutations in K+-ATP Channels [NCT02375828]Phase 310 participants (Actual)Interventional2015-03-20Completed
Comparative Study of Dapagliflozin Versus Glibenclamide Effect on Endothelial Function of Coronary Artery Disease Patients [NCT02919345]Phase 498 participants (Actual)Interventional2017-01-31Completed
Oral Antidiabetic Agents on Gestational Diabetes: Modulating Effect on Fetal Growth - a Clinical Randomized Trial [NCT02091336]Phase 480 participants (Anticipated)Interventional2014-01-31Recruiting
A Four-part, Single-center, Open-label, Phase I Clinical Study to Evaluate the Drug-Drug Pharmacokinetic Interaction Between DBPR108 at Steady-state and Metformin Hydrochloride/Glibenclamide/Valsartan/ Simvastatin in Healthy Subjects [NCT04859452]Phase 156 participants (Actual)Interventional2021-05-26Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Glyburide/Metformin 5 mg/500 mg Film-Coated Tablets and Glucovance® 5 mg/500 mg Film-Coated Tablets in Healthy Subjects Under Fasting Conditions [NCT00836472]Phase 160 participants (Actual)Interventional2003-04-30Completed
A Feasibility Study Looking at the Use of Glibenclamide and metfoRmin Versus stAndard Care in gEstational diabeteS [NCT02080377]Phase 323 participants (Actual)Interventional2014-07-31Completed
[NCT00035568]Phase 40 participants Interventional2002-02-28Completed
Glyburide and Metformin for Gestational Diabetes Mellitus [NCT01329016]Phase 1/Phase 2360 participants (Anticipated)Interventional2011-07-31Active, not recruiting
Relative Bioavailability of BI 1356 and Glyburide After Concomitant Administration of Multiple Oral Doses of BI 1356 5 mg Once Daily and a Single Oral Dose of Glyburide 1.75 mg Compared With the Bioavailability of BI 1356 and Glyburide After Each Treatmen [NCT02183428]Phase 120 participants (Actual)Interventional2008-05-31Completed
Sulphonylurea Receptor Mutation and Responsiveness to Gliclazide - a Pilot Proof of Concept, Randomised Cross-over Study [NCT02201602]Phase 48 participants (Actual)Interventional2014-08-31Completed
[NCT00035542]Phase 30 participants Interventional2001-12-31Completed
Gestational Diabetes Mellitus: Insulin or Oral Hypoglycemic Agents? [NCT01215331]Phase 373 participants (Actual)Interventional2010-08-31Completed
The Safety and Effectiveness of Glibenclamide in the Treatment of Aneurysm Subarachnoid Hemorrhage(aSAH): a Randomized Controlled Clinical Study [NCT05137678]Phase 4110 participants (Anticipated)Interventional2021-10-19Recruiting
A Phase I Randomized, Double-Blind, Placebo-Controlled Study to Assess the Safety, Tolerability, and Pharmacokinetics of Escalating Doses of RP-1127 (Glyburide for Injection) in Healthy Male and Female Volunteers [NCT01132703]Phase 134 participants (Actual)Interventional2010-01-07Completed
A 12-week Study to Compare the Effects of Vildagliptin Versus Glibenclamide on Glycemic Variability After a Sub Maximal Exercise Test in Patients With Type 2 Diabetes Inadequately Controlled With Metformin. [NCT01867502]Phase 420 participants (Anticipated)Interventional2014-04-30Recruiting
12-week Randomized Study to Compare the Effect of Vildagliptin vs. Glibenclamide Associated to Metformin in Endothelial Function in Patients With Type 2 Diabetes and Hypertension [NCT02145611]Phase 450 participants (Actual)Interventional2013-07-31Completed
Risk of Hypoglycemia in Type 2 Diabetes - Effects of Glibenclamide and Exercise on Cardiovascular, Hormonal, and Metabolic Parameters [NCT00734669]12 participants (Actual)Observational2008-07-31Completed
[NCT01563120]Phase 4108 participants (Actual)Interventional2012-01-31Completed
Effect of Liraglutide on Glycaemic Control in Subjects With Type 2 Diabetes [NCT00393718]Phase 3400 participants (Actual)Interventional2006-11-30Completed
Long-term Sulfonylurea Response and Glucose Control After Switching From Insulin in Children With Diabetes Due to ABCC8 (SUR1) Mutations [NCT02624830]Phase 430 participants (Anticipated)Interventional2019-02-15Recruiting
Glyburide vs Glucovance in the Treatment of Gestational Diabetes [NCT02726490]Early Phase 17 participants (Actual)Interventional2016-07-31Terminated(stopped due to Lack of Recruitment)
A Single Randomized, Open, Cross-over, Phase Ie Study to Access the Drug-drug Interaction of SP2086 and Glyburide [NCT02815787]Phase 116 participants (Actual)Interventional2014-03-31Completed
Long-term Sulfonylurea Response and Glucose Control After Switching From Insulin in Children With Diabetes Due to KCNJ11 (KIR6.2) Mutations [NCT02624817]Phase 490 participants (Actual)Interventional2015-12-31Completed
A Relative Bioavailability Study of 5 mg Glyburide/500 mg Metformin HCl Tablets Under Fasting Conditions [NCT00865241]Phase 136 participants (Actual)Interventional2002-11-30Completed
[NCT00935363]Phase 10 participants (Actual)Interventional2010-02-28Withdrawn
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Determine the Efficacy and Safety of SYR110322 (SYR-322) When Used in Combination With a Sulfonylurea in Subjects With Type 2 Diabetes [NCT00286468]Phase 3500 participants (Actual)Interventional2006-04-30Completed
[NCT00472875]Phase 410 participants (Anticipated)Interventional2007-05-31Recruiting
Effects of Pioglitazone on Endothelial Progenitor Cells in Type 2 Diabetic Patients With Vascular Complications - The SPLENDOR Study. [NCT00770835]Phase 439 participants (Actual)Interventional2009-03-31Completed
Oral Glibenclamide in Preterm Infants With Hyperglycaemia (GALOP) [NCT05687500]Phase 245 participants (Anticipated)Interventional2023-05-20Recruiting
Switching From Insulin to Sulfonylurea in Childhood and Adult Diabetes Due to Variants in the HNF1A, HNF4A, or HNF1B Genes [NCT04239586]Phase 430 participants (Anticipated)Interventional2017-04-18Enrolling by invitation
Effect of a Sulfonylurea Compound on the Glucagon Response to Insulin-induced Hypoglycemia in Type 1 Diabetes Mellitus [NCT00515801]Phase 2/Phase 318 participants (Actual)Interventional2007-06-30Completed
A Multicenter, Double-Blind, Randomized, Placebo-Controlled, Parallel Study of the Safety and Efficacy of a Combination of TAK-559 and Glyburide Compared to Placebo and Glyburide in the Treatment of Patients With Type 2 Diabetes Mellitus [NCT00759720]Phase 3447 participants (Actual)Interventional2003-11-30Terminated(stopped due to Potential hepatic safety signal)
A Relative Bioavailability Study of 5 mg Glyburide/500 mg Metformin HCl Tablets Under Fasting Conditions [NCT00865436]Phase 136 participants (Actual)Interventional2004-04-30Completed
A Relative Bioavailability Study of 5 mg Glyburide/500 mg Metformin HCl Tablets Under Non-Fasting Conditions [NCT00864734]Phase 124 participants (Actual)Interventional2002-11-30Completed
The Effect of Sitagliptin on Hypertension, Arterial Stiffness, Oxidative Stress and Inflammation [NCT00696982]60 participants (Anticipated)Interventional2008-06-30Recruiting
Sulfonylureas in Neonatal Diabetes Mellitus With Mutations of 2 Type of Subunits Kir6.2 and SUR1 of the Pancreatic Beta-cell ATP-sensitive K+ Channel. [NCT00610038]Phase 219 participants (Actual)Interventional2006-07-31Completed
The Hemodynamic Effects of CGRP After Glibenclamide Administration in a Randomized Double-blind Cross-over Placebo-controlled Study With Healthy Volunteers [NCT04231617]20 participants (Actual)Interventional2020-01-20Completed
A Randomized Prospective Trial of Metformin Compared to Glyburide in Gestational Diabetes [NCT00965991]149 participants (Actual)Interventional2003-07-31Completed
An Open-Label Drug-Drug Interaction Study in Healthy Subjects to Explore the Effects of Multiple Doses of JNJ-28431754 on the Pharmacokinetics and Safety of Single Doses of Glyburide [NCT01733108]Phase 129 participants (Actual)Interventional2008-07-31Completed
An Open-label, Crossover Study to Investigate the Potential Pharmacodynamic and Potential Pharmacokinetic Interaction Between Glyburide and GK Activator(2) in Type 2 Diabetes Patients Inadequately Controlled With Glyburide as Standard Prescribed Therapy. [NCT00388986]Phase 118 participants (Actual)Interventional2006-10-31Completed
Metabolic Analysis for Treatment Choice in Gestational Diabetes Mellitus [NCT03029702]Phase 454 participants (Actual)Interventional2018-02-28Completed
A Randomized Clinical Trial of Glyburide (RP-1127) for TBI [NCT01454154]Phase 229 participants (Actual)Interventional2011-12-17Completed
[NCT01947699]Phase 40 participants (Actual)Interventional2013-09-30Withdrawn(stopped due to PI decided to withdrawal study before recruitment started)
A 24-Week Randomised, Double-Blind, Parallel-Group, Multi-Centre, Placebo-Controlled Study to Evaluate the Efficacy, Safety and Tolerability of Tesaglitazar Therapy When Added to the Therapy of Patients With Type 2 Diabetes Poorly Controlled on Sulphonylu [NCT00251940]Phase 3555 participants Interventional2004-07-31Terminated(stopped due to The development program has been terminated)
Glyburide and Metformin for the Treatment of Gestational Diabetes Mellitus. A Systematic Review and Meta-analysis of Randomized Controlled Trials Comparing These Drugs Either vs Insulin or vs Each Other. [NCT01998113]2,509 participants (Actual)Observational2013-03-31Completed
Comparison of Glycaemic and Cardiovascular Treatment Outcomes of Voglibose Versus Glibenclamide Added to Metformin in T2DM Patients in Zambia: An Open-label Randomised Clinical Trial [NCT05688332]Phase 3118 participants (Anticipated)Interventional2023-08-31Not yet recruiting
A Multicenter, Double-Blind, Multidose, Placebo-Controlled, Randomized, Parallel-Group, Phase 2 Study to Evaluate the Efficacy and Safety of Intravenous BIIB093 for Patients With Brain Contusion [NCT03954041]Phase 292 participants (Actual)Interventional2019-10-06Terminated(stopped due to Early completed due to strategic considerations, not for efficacy or safety reasons.)
Glimepiride Induced Insulin Secretion Will be Inhibited by Hypoglycemia [NCT00608179]32 participants (Actual)Interventional2002-08-31Completed
Repaglinide Versus Glyburide: Comparitive Effect on Postprandial Lipemia: An Open-labeled, Randomized, Parallel Group Study in Patients With Type 2 Diabetes [NCT01605773]Phase 451 participants (Actual)Interventional2001-11-08Completed
ANALYSIS OF THE EFFECTIVENESS OF A STAGED MANAGEMENT PROGRAM AIMED AT CONTROLLING BLOOD PRESSURE AND BLOOD GLUCOSE OF TYPE 2 DIABETIC PATIENTS USING EXCLUSIVELY THE RESOURCES AVAILABLE IN A PRIMARY CARE SETTING IN BRAZIL [NCT00935805]124 participants (Anticipated)Observational2006-07-31Active, not recruiting
A 12-Week, Phase 2, Randomized, Double-Blind, Active-Controlled Study of LY2599506 Given as Monotherapy or in Combination With Metformin in Patients With Type 2 Diabetes Mellitus [NCT01029795]Phase 238 participants (Actual)Interventional2010-02-28Terminated(stopped due to Terminated due to nonclinical safety findings)
Low-dose Glibenclamide in Type 2 Diabetes Mellitus - Part A [NCT02830048]Phase 216 participants (Actual)Interventional2016-07-31Completed
Durability of Early Initial Combination Therapy With Exenatide/Pioglitazone/Metformin vs Conventional Therapy in New Onset Type 2 Diabetes [NCT01107717]Phase 4521 participants (Actual)Interventional2009-01-31Active, not recruiting
Effect of GlucoNorm vs Glyburide on Post-Prandial Hyperglycemia in Elderly Subjects With Type 2 Diabetes [NCT00451620]Phase 230 participants (Actual)Interventional2003-11-30Completed
A Randomized, Double-Blind, Comparator-Controlled Study of Pioglitazone HCl vs Glyburide in the Treatment of Patients With Type 2 (Non-Insulin-Dependent) Diabetes Mellitus and Mild Cardiac Disease (NYHA I) [NCT00521742]Phase 3300 participants (Actual)Interventional2001-03-31Completed
Glibenclamide Advantage in Treating Edema After Intracerebral Hemorrhage (GATE-ICH): a Multi-center Randomized, Controlled, Assessor-blinded Trial [NCT03741530]220 participants (Actual)Interventional2018-12-15Completed
A Multi-Center, Prospective, Open Label, Phase IIa Trial of RP-1127 (Glyburide for Injection) in Patients With a Severe Anterior Circulation Ischemic Stroke Who Are Likely to Experience Clinically Significant Brain Swelling. [NCT01268683]Phase 1/Phase 210 participants (Actual)Interventional2011-05-26Completed
A 52-Week Randomized, Double-Blind, Parallel-Group, Multi-Centre, Active-Controlled (Glibenclamide) Study to Evaluate the Efficacy, Safety and Tolerability of Tesaglitazar Therapy When Administered to Patients With Type 2 Diabetes [NCT00255541]Phase 3580 participants Interventional2004-09-30Terminated(stopped due to The development program has been terminated)
Efficacy of Repaglinide Compared to Glyburide and Placebo on Hepatic Glucose Metabolism in Type 2 Diabetic Subjects Treated With Diet or With Antidiabetic Oral Agents. A Randomized, Open, Cross-over Single-centre Placebo-controlled Trial [NCT01698931]Phase 49 participants (Actual)Interventional2002-04-26Completed
Glyburide Compared to Insulin in the Management of White's Classification A2 Gestational Diabetes [NCT00160485]Phase 40 participants (Actual)Interventional2004-06-30Withdrawn(stopped due to Active Duty principle investigator currently deployed)
Evaluation of Safety and Efficacy of Glibenclamide in the Treatment of Severe Traumatic Brain Injury [NCT05148403]Phase 1/Phase 276 participants (Anticipated)Interventional2021-10-22Recruiting
A Randomized, Multi-Center, Prospective, Double Blind, Phase II Trial of RP- 1127 (Glyburide for Injection) in Patients With a Severe Anterior Circulation Ischemic Stroke Who Are Likely to Develop Malignant Edema [NCT01794182]Phase 286 participants (Actual)Interventional2013-06-13Completed
A Clinical Trial to Study the Efficacy and Safety of Insulin Aspart Three Times Per Day Compared to Glibenclamide Once or Twice Daily in Type 2 Diabetes by Comparison of Ability to Control Blood Glucose [NCT00267683]Phase 39 participants (Actual)Interventional2005-12-31Terminated(stopped due to This trial was terminated due to low recruitment)
Acute Local Ischemic Preconditioning in Patients With Type 1 Diabetes in Vivo [NCT00184821]20 participants Observational2004-06-30Completed
Effect of Rosiglitazone on Myocardial Blood Flow Regulation in Type 2 Diabetes [NCT00549874]27 participants (Actual)Interventional2002-02-28Completed
A Phase III Study to Assess the Efficacy, Safety and Tolerability of ASP1941 in Combination With Sulfonylurea in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Sulfonylurea Alone [NCT01242215]Phase 3243 participants (Actual)Interventional2010-09-17Completed
A Randomized, Comparator Controlled, Double-Blind Study of the Liver Safety of Pioglitazone HCl vs Glyburide With Metformin and Insulin as Part of Step Therapy in Subjects With Type 2 (Non-Insulin Dependent) Diabetes [NCT00494312]Phase 42,120 participants (Actual)Interventional2000-10-31Completed
A Randomized, Double-Blind, Comparator-Controlled Study of Pioglitazone HCl vs Glyburide in the Treatment of Subjects With Type 2 (Non-Insulin Dependent) Diabetes Mellitus and Mild to Moderate Congestive Heart Failure [NCT00521820]Phase 3518 participants (Actual)Interventional2000-06-30Terminated(stopped due to Higher incidence of hospitalization for congestive heart failure in pioglitazone-treated subjects compared to glyburide treated subjects.)
Substituting Lantus®(Insulin Glargine[rDNAorigin]Inj) for a Thiazolidinedione vs. a 3rd Oral Agent as add-on Therapy in Patients Failing a Thiazolidinedione & Sulfonylurea or Metformin Combination [NCT00046462]Phase 3240 participants Interventional2001-11-30Completed
Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study [NCT05220917]781,430 participants (Anticipated)Observational2021-08-01Active, not recruiting
A Randomized Controlled Clinical Trial of Treatment of Mild Gestational Diabetes With Glyburide Versus Placebo [NCT00744965]Phase 4395 participants (Actual)Interventional2008-09-16Completed
Spinal Cord Injury Neuroprotection With Glyburide (SCING): Pilot Study: An Open-Label Prospective Evaluation of the Feasibility, Safety, Pharmacokinetics, and Preliminary Efficacy of Oral Glyburide (DiaBeta) in Patients With Acute Traumatic Spinal Cord In [NCT05426681]Phase 112 participants (Anticipated)Interventional2022-07-07Recruiting
Randomized, Open Label, Two Parallel Arms, Intervention Trial Comparing the Effect of DPP-IV Inhibitor Vildagliptin vs. Glibenclamide on Circulating Endothelial Progenitor Cell Number in Patients With Type 2 Diabetes in Metformin Failure [NCT01822548]Phase 364 participants (Actual)Interventional2010-10-31Completed
A Randomized, Double-Blind Study to Compare the Durability of Glucose Lowering and Preservation of Pancreatic Beta-Cell Function of Rosiglitazone Monotherapy Compared to Metformin or Glyburide/Glibenclamide in Patients With Drug-Naive, Recently Diagnosed [NCT00279045]Phase 34,426 participants (Actual)Interventional2000-01-03Completed
Phase 4 Study Evaluation of the Effects of Acarbose Versus Glibenclamide on Mean Amplitude of Glycemic Excursions and Oxidative Stress in Patients With Type 2 Diabetes Insufficiently Controlled by Metformin [NCT00417729]Phase 451 participants (Actual)Interventional2007-01-31Completed
Glyburide Healthy Volunteer Study [NCT01716338]Phase 121 participants (Actual)Interventional2013-01-31Completed
Multicenter Randomized Trial of Non-inferiority Between Glyburide and Insulin for the Treatment of Gestational Diabetes [NCT01731431]Phase 3914 participants (Actual)Interventional2012-05-18Completed
Rosiglitazone Intervention Study in Patients With Type 1.5 Diabetes [NCT00194896]64 participants (Actual)Interventional2000-02-29Completed
Effect of the R230C Variant of the ATP-binding Cassette Transporter A1 (ABCA1) Gene on the Response to Treatment With Glibenclamide in Patients With Type 2 Diabetes Mellitus [NCT01456650]Phase 485 participants (Actual)Interventional2011-03-31Completed
Investigation of the Efficacy of Metformin Therapy on Pulmonary Sarcoidosis Phase II Randomized, Double-blind, Placebo-controlled Trial [NCT05910554]Phase 240 participants (Anticipated)Interventional2023-08-01Not yet recruiting
Effects of Dapagliflozin, an SGLT2 Inhibitor, on Hemodynamic Parameters, Target Organ Damage and Obesity Profile in Resistant Hypertensive Subjects [NCT03089333]Phase 416 participants (Actual)Interventional2016-07-31Completed
Comparison of Rosiglitazone Versus Glyburide on Vascular Structure and Function in Type 2 Diabetic Patients [NCT00123643]Phase 436 participants (Actual)Interventional2003-05-31Completed
Preservation of Beta-cell Function in Type 2 Diabetes Mellitus [NCT00232583]58 participants (Actual)Interventional2003-11-30Completed
The Hemodynamic Effects of PACAP38 After Glibenclamide Administration in Healthy Volunteers [NCT04960657]22 participants (Actual)Interventional2020-10-20Completed
Treatment of Early Insulinization With Glargine in Type 2 Diabetes Patients Uncontrolled on Sulfonylurea or Metformin Monotherapy [NCT00347100]Phase 4387 participants (Actual)Interventional2006-06-30Completed
A Comparison of Glucovance (Glyburide and Metformin) to Insulin Therapy for the Treatment of Gestational Diabetes and Adult Onset Diabetes in Pregnancy [NCT00371306]200 participants Interventional2002-09-30Recruiting
Safety and Efficacy of Glibenclamide Combined With Rt-PA in Treating Acute Ischemic Stroke: a Prospective, Randomized, Double-blind, Placebo-control, Multi-center Study [NCT03284463]Phase 2/Phase 3306 participants (Actual)Interventional2018-01-01Completed
Failure Rate of GLyburide And Metformin Among Gestational Diabetics [NCT03078725]Phase 40 participants (Actual)Interventional2017-06-20Withdrawn(stopped due to Research was competing with other projects in the department, and no patients were recruited.)
A Pilot Study and Phase II Double Blind Placebo Controlled Randomized Trial Examining the Safety and Efficacy of Glyburide as Prophylaxis Against Cerebral Edema in Patients Receiving Radiosurgery for Brain Metastases [NCT02460874]Phase 1/Phase 21 participants (Actual)Interventional2017-08-16Terminated(stopped due to Slow accrual)
Randomized, 2-Way Crossover, Bioequivalence Study of Glyburide/Metformin 5 mg/500 mg Film-Coated Tablets and Glucovance® 5 mg/500 mg Film-Coated Tablets in Healthy Subjects Under Fed Conditions [NCT00835991]Phase 160 participants (Actual)Interventional2003-02-28Completed
Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter, Phase 3 Study to Evaluate the Efficacy and Safety of Intravenous BIIB093 (Glibenclamide) for Severe Cerebral Edema Following Large Hemispheric Infarction [NCT02864953]Phase 3537 participants (Actual)Interventional2018-08-29Terminated(stopped due to Early completed to operational challenges and other strategic considerations, not for efficacy or safety reasons)
Spinal Cord Injury Neuroprotection With Glyburide; Pilot Study: An Open-Label Prospective Evaluation of the Feasibility, Safety, Pharmacokinetics, and Preliminary Efficacy of Oral Glyburide (DiaBeta) in Patients With Acute Traumatic Spinal Cord Injury [NCT02524379]Phase 1/Phase 23 participants (Actual)Interventional2017-02-14Terminated(stopped due to Principal investigator has left the university; there were not enough participants to analyze the data.)
A Randomized, Open-label, Comparative Clinical Trial to Study the Efficacy of Sitagliptin and Glibenclamide in a Short Term Treatment on the Daily Glucose Variability Using Continuous Glucose Monitoring (CGM) in Japanese Patients With Type 2 Diabetes Mell [NCT02318693]Phase 453 participants (Actual)Interventional2015-02-04Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00123643 (1) [back to overview]Flow Mediated Dilation
NCT00194896 (2) [back to overview]Changes in Beta Cell Function Assessed by Fasting and Stimulated C-peptide Measured at 36 Months.
NCT00194896 (2) [back to overview]Patients Positive for T Cell Responses to Islet Proteins at 36 Months.
NCT00232583 (17) [back to overview]Weight
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Social Stigma
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Social or Vocational Worry
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Satisfaction With Insulin Treatment
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Lifestyle Flexibility
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Hypoglycemia Fear
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Glycemia Control Perception
NCT00232583 (17) [back to overview]Insulin Sensitivity as Measure be Matsuda Index
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Current Health Perception
NCT00232583 (17) [back to overview]Inflammatory Markers -Fibrinogen
NCT00232583 (17) [back to overview]Inflammatory Markers - PAI-1
NCT00232583 (17) [back to overview]Inflammatory Markers - hsCRP
NCT00232583 (17) [back to overview]Beta-cell Function - C-peptide AUC (Area Under the Curve)
NCT00232583 (17) [back to overview]Bet-cell Function Measured by Disposition Index
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Treatment Satisfaction
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Treatment Impact
NCT00232583 (17) [back to overview]Quality of Life Survey (QoL) - Willingness to Continue Insulin Treatment
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 26).
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 16).
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 8).
NCT00286468 (51) [back to overview]Number of Participants Requiring Rescue.
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin ≤ 6.5%.
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin ≤ 7.0%.
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin ≤ 7.5%.
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 0.5%.
NCT00286468 (51) [back to overview]Change From Baseline in Proinsulin/Insulin Ratio (Week 26).
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 1.0%.
NCT00286468 (51) [back to overview]Change From Baseline in Body Weight (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 20).
NCT00286468 (51) [back to overview]Number of Participants With Marked Hyperglycemia (Fasting Plasma Glucose ≥ 200 mg Per dL).
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 2.0%.
NCT00286468 (51) [back to overview]Change From Baseline in Body Weight (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Body Weight (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in Body Weight (Week 26).
NCT00286468 (51) [back to overview]Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 1.5%.
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 16).
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 26).
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in C-peptide (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 1).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 16).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 2).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 26).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Plasma Glucose (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 16).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 26).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in Fasting Proinsulin (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 26.
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (Week 16).
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (Week 20).
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (Week 4).
NCT00286468 (51) [back to overview]Change From Baseline in Glycosylated Hemoglobin (Week 8).
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 12).
NCT00286468 (51) [back to overview]Change From Baseline in Insulin (Week 16).
NCT00313313 (4) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24
NCT00313313 (4) [back to overview]Change From Baseline in Hemoglobin A1c (A1C) at Week 24
NCT00313313 (4) [back to overview]Changes From Baseline in Postprandial Glucose (PPG) Area Under the Curve (AUC) Response to an Oral Glucose Tolerance Test (OGTT) at Week 24
NCT00313313 (4) [back to overview]Percentage of Participants Achieving A1C < 7% at Week 24
NCT00393718 (13) [back to overview]Mean Postprandial PG Increment in 7-point Plasma Glucose Profile After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Mean PG in 7-point Plasma Glucose Profile After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Mean Postprandial PG Increment in 7-point Plasma Glucose Profile After 52 Weeks of Treatment
NCT00393718 (13) [back to overview]Postprandial Glucose AUC After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Hypoglycaemic Episodes
NCT00393718 (13) [back to overview]Postprandial Glucose AUC After 52 Weeks of Treatment
NCT00393718 (13) [back to overview]Body Weight After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Body Weight After 52 Weeks of Treatment
NCT00393718 (13) [back to overview]Fasting Plasma Glucose After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Fasting Plasma Glucose After 52 Weeks of Treatment
NCT00393718 (13) [back to overview]Glycosylated Haemoglobin A1c (HbA1c) After 24 Weeks of Treatment
NCT00393718 (13) [back to overview]Glycosylated Haemoglobin A1c (HbA1c) After 52 Weeks of Treatment
NCT00393718 (13) [back to overview]Mean PG in 7-point Plasma Glucose Profile After 52 Weeks of Treatment
NCT00744965 (11) [back to overview]Rate of Cesarean Delivery
NCT00744965 (11) [back to overview]Number of Participants With Large for Gestational Age Infants
NCT00744965 (11) [back to overview]Neonatal Intensive Care Unit Admissions
NCT00744965 (11) [back to overview]Need for Insulin Treatment
NCT00744965 (11) [back to overview]Need for Insulin Therapy
NCT00744965 (11) [back to overview]3rd or 4th Degree Perineal Laceration
NCT00744965 (11) [back to overview]Chorioamnionitis
NCT00744965 (11) [back to overview]Diagnosis of Pregnancy-induced Hypertension
NCT00744965 (11) [back to overview]Mean Fetal Weight at Birth
NCT00744965 (11) [back to overview]Shoulder Dystocia
NCT00744965 (11) [back to overview]Macrosomia
NCT00835991 (6) [back to overview]Cmax (Maximum Observed Concentration) - Glyburide
NCT00835991 (6) [back to overview]AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Metformin
NCT00835991 (6) [back to overview]AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Glyburide
NCT00835991 (6) [back to overview]AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Glyburide
NCT00835991 (6) [back to overview]AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Metformin
NCT00835991 (6) [back to overview]Cmax (Maximum Observed Concentration) - Metformin
NCT00836472 (6) [back to overview]AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Glyburide
NCT00836472 (6) [back to overview]AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Metformin
NCT00836472 (6) [back to overview]AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Glyburide
NCT00836472 (6) [back to overview]Cmax (Maximum Observed Concentration) - Glyburide
NCT00836472 (6) [back to overview]Cmax (Maximum Observed Concentration) - Metformin
NCT00836472 (6) [back to overview]AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Metformin
NCT00965991 (1) [back to overview]Number of Participants Assessed for Glucose Control
NCT01029795 (1) [back to overview]Percentage of Participants With Clinically-Significant Elevations of Alanine Aminotransferase/Serum Glutamate Pyruvate Transaminase (ALT/SGPT) During the 12-week Treatment Period
NCT01068860 (16) [back to overview]Mean Change in C-peptide Area Under the Curve (AUC), 0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Plasma Glucose, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Plasma Insulin, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fructosamine, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Insulin Area Under the Curve (AUC) 0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-2 Hours, From Baseline to 4 Weeks.
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-4 Hours, From Baseline to 4 Weeks.
NCT01068860 (16) [back to overview]Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 2-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma C-peptide Level, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma Glucose, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Peak Plasma Insulin, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Post-prandial Glucose Area Under the Curve (AUC)0-4 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Fasting Glucose Disposition Index(GDI)1 and Index 2, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Absolute Glucose Level at 2 Hours, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Mean Change in Quantitative Insulin Sensitivity Check Index (QUICKI) Score, From Baseline to 4 Weeks
NCT01068860 (16) [back to overview]Number of Participants Reporting Death, Serious Adverse Events (SAEs) and Adverse Events (AEs) Above 5% Frequency, From Baseline to 4 Weeks
NCT01268683 (20) [back to overview]Number of Participants With a Modified Rankin Scale (mRS) Score ≤ 4
NCT01268683 (20) [back to overview]National Institute of Health Stroke Scale (NIHSS) Score
NCT01268683 (20) [back to overview]Midline Shift
NCT01268683 (20) [back to overview]Ipsilateral Ventricle Volume
NCT01268683 (20) [back to overview]Infarcted Hemisphere Volume
NCT01268683 (20) [back to overview]Glasgow Coma Scale (GCS) Score
NCT01268683 (20) [back to overview]Frequency of Hemorrhagic Events
NCT01268683 (20) [back to overview]Absolute Diffusion Weighted Imaging (DWI) Lesion Volume
NCT01268683 (20) [back to overview]Rate of Enrollment
NCT01268683 (20) [back to overview]Percentage of Participants With Pre-specified Adverse Events Associated With Glyburide According to Protocol
NCT01268683 (20) [back to overview]Percentage of Participants With All Four MRI Assessments Per Protocol
NCT01268683 (20) [back to overview]Percentage of Participants Requiring One or More Hypoglycemia Treatments
NCT01268683 (20) [back to overview]Percentage of Participants Completing 90-Day Follow-Up
NCT01268683 (20) [back to overview]Percentage of Enrolled Participants to Screened Participants
NCT01268683 (20) [back to overview]Full Outline of UnResponsiveness (FOUR) Score
NCT01268683 (20) [back to overview]Number of Participants Requiring Decompressive Craniectomy (DC)
NCT01268683 (20) [back to overview]Number of MRI Assessments Per Participant
NCT01268683 (20) [back to overview]Change From Baseline in DWI Lesion Volume
NCT01268683 (20) [back to overview]Percentage of Dose Reductions/ Dose Suspensions
NCT01268683 (20) [back to overview]Number of Participants With Adverse Events and Serious Adverse Events
NCT01822548 (2) [back to overview]Absolute Change in HbA1C Compared to Baseline
NCT01822548 (2) [back to overview]Absolute Change in the Endothelial Progenitor Cell (EPC) Number
NCT02318693 (5) [back to overview]Change From Baseline in Percentage of Hypoglycemic Values (Glucose Sensor Readings: < 70, <60, <50 mg/dL)
NCT02318693 (5) [back to overview]Change From Baseline in 24-hour Mean Glucose Level
NCT02318693 (5) [back to overview]Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) at Day 13
NCT02318693 (5) [back to overview]Change From Baseline in the Standard Deviation of Blood Glucose Levels
NCT02318693 (5) [back to overview]Change From Baseline in Maximum Incremental Postprandial Glucose Levels in Each Meal
NCT02460874 (6) [back to overview]Number of Participants Administered Dexamethasone (or Any Corticosteroid Administration With the Purpose of Treating Cerebral Edema)
NCT02460874 (6) [back to overview]Number of Participants With Absolute Volume Change of Index Tumor(s)
NCT02460874 (6) [back to overview]Number of Participants With Cerebral Edema Increase as Measured on FLAIR Volumetric Imaging
NCT02460874 (6) [back to overview]Number of Participants With CTCAE Version 4.0 Reportable Toxicities of Grades 1-2 Cardiac Disorders or Hepatobiliary Disorders.
NCT02460874 (6) [back to overview]Number of Participants With CTCAE Version 4.0 Reportable Toxicities of Grades 2-5.
NCT02460874 (6) [back to overview]Number of Participants With Dose Limiting Toxicities (DLTs)
NCT02524379 (3) [back to overview]Number of Participants With Neurologic Recovery Following tSCI
NCT02524379 (3) [back to overview]Number of Participants With tSCI Recruited Within the Specified Time Window
NCT02524379 (3) [back to overview]Number of Drug Related Adverse Events
NCT03954041 (8) [back to overview]Percentage of Participants With Glasgow Outcome Scale - Extended (GOS-E) Score at Day 180
NCT03954041 (8) [back to overview]Percentage of Participants Requiring Delayed Intubation
NCT03954041 (8) [back to overview]Change From Baseline in Mean Total Contusion Volume (Hematoma Plus Perihematomal Edema) at 96 Hours as Measured by Brain Imaging
NCT03954041 (8) [back to overview]Percentage of Participants With Modified Rankin Scale (mRS) Score at Day 90
NCT03954041 (8) [back to overview]Change From Baseline in Mean Total Contusion Volume (Hematoma Plus Perihematomal Edema) at 24 Hours as Measured by Brain Imaging
NCT03954041 (8) [back to overview]Change From Baseline in Absolute Hematoma Volume at 24 Hours
NCT03954041 (8) [back to overview]Change From Baseline in Absolute Edema Volume at 96 Hours
NCT03954041 (8) [back to overview]Time to All-Cause Death Through Day 90

Flow Mediated Dilation

Measure of endothelial function (NCT00123643)
Timeframe: change from baseline to 6 months

Interventionpercent change (Mean)
Rosiglitazone6.8
Glyburide5.5

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Changes in Beta Cell Function Assessed by Fasting and Stimulated C-peptide Measured at 36 Months.

Changes in beta cell function assessed by fasting and stimulated C-peptide measured at 36 months. (NCT00194896)
Timeframe: 36 months

,,,
Interventionng per ml (Mean)
Fasting C-peptideGlucagon Stimulated C-peptide
Glyburide Autoantibody Negative0.30.3
Glyburide Autoantibody Positive0.13.1
Rosiglitazone Autoantibody Negative-1.4-2.8
Rosiglitazone Autoantibody Positive-0.4-0.6

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Patients Positive for T Cell Responses to Islet Proteins at 36 Months.

Number of participants positive for T cell reactivity to islet proteins at 36 months. (NCT00194896)
Timeframe: 36 months

Interventionparticipants (Number)
Rosiglitazone Autoantibody Positive1
Rosiglitazone Autoantibody Negative2
Glyburide Autoantibody Positive2
Glyburide Autoantibody Negative3

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Weight

Body Weight (NCT00232583)
Timeframe: 72 months

Interventionkg (Mean)
Metfomin and Insulin107.7
Metformin, Pioglitazone and Glyburide107.9

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Quality of Life Survey (QoL) - Social Stigma

Social stigma was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1 to 5, where 1- strongly agree; 2 - somewhat agree; 3 - neither agree nor disagree; 4 - somewhat disagree; 5 - strongly disagree. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin2.2
Metfomin, Pioglitazone & Glyburide2.2

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Quality of Life Survey (QoL) - Social or Vocational Worry

Social or vocational worry was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 0-5, where 0 - does not apply; 1 - never; 2 - seldom; 3 - sometimes; 4 - often; 5 - all of the time. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin1.8
Metfomin, Pioglitazone & Glyburide1.7

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Quality of Life Survey (QoL) - Satisfaction With Insulin Treatment

Satisfaction with insulin treatment was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a scale score of 1 to 7, where 1 extremely satisfied to 7 - not at all satisfied. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin1.2

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Quality of Life Survey (QoL) - Lifestyle Flexibility

Lifestyle flexibility was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1 to 5, where 1 - a great deal of choice; 2 - a lot of choice; 3 - some choice; 4 - a little choice; 5 - no choice. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin2.1
Metfomin, Pioglitazone & Glyburide2.0

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Quality of Life Survey (QoL) - Hypoglycemia Fear

Hypoglycemia fear was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1-5, where 1 - never worry; 2 - rarely water; 3 - sometimes worry; 4 - often worry; 5 - very often worry (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin1.8
Metfomin, Pioglitazone & Glyburide1.8

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Quality of Life Survey (QoL) - Glycemia Control Perception

Glycemia control perception was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a scale score of 1-7, where 1 - extremely controlled and 7 - not at all controlled. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin2.8
Metfomin, Pioglitazone & Glyburide2.0

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Insulin Sensitivity as Measure be Matsuda Index

C-peptide-based Matsuda index using following formula: Matsuda index = 500,00 / root square [(fasting c-peptide x fasting glucose x 333) x (average c-peptide 0-120 mins x average glucose 0-120 mins x 333). Higher the Matsuda index, better the insulin sensitivity. (NCT00232583)
Timeframe: 72 months

Interventionindex (Mean)
Metfomin & Insulin3.12
Metfomin, Pioglitazone & Glyburide2.45

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Quality of Life Survey (QoL) - Current Health Perception

Current health perception was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1-5, where 1 = much better than 3 months ago; 2 - Somewhat better now than 3 months ago; 3 - About the same; 4 - Somewhat worse now than 3 months ago; 5 Much worse now than 3 months ago. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin2.7
Metfomin, Pioglitazone & Glyburide2.9

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Inflammatory Markers -Fibrinogen

Inflammatory markers - Fibrinogen (NCT00232583)
Timeframe: 72 months

Interventionmg/dL (Mean)
Metfomin & Insulin399.0
Metfomin, Pioglitazone & Glyburide395.4

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Inflammatory Markers - PAI-1

Inflammatory markers - PAI-1 (Plasminogen activator inhibitor type 1) (NCT00232583)
Timeframe: 72 months

InterventionIU/L (Mean)
Metfomin & Insulin13.9
Metfomin, Pioglitazone & Glyburide16.7

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Inflammatory Markers - hsCRP

Inflammatory markers - hsCRP (C reactive protein) (NCT00232583)
Timeframe: 72 months

Interventionmg/L (Mean)
Metfomin & Insulin6.9
Metfomin, Pioglitazone & Glyburide6.1

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Beta-cell Function - C-peptide AUC (Area Under the Curve)

C-peptide AUC during a 3-hours mixed meal challenge testing (NCT00232583)
Timeframe: 72 months

Interventionng*min/mL (Mean)
Metformin & Insulin2096
Metformin, GLyburide & Pioglitazone1725

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Bet-cell Function Measured by Disposition Index

Disposition index was measured by multiplying the insulin secretion (C-peptide AUC/C-peptide AUC glucose) by the Matsuda index. Disposition index reflects the beta-cell function adjusted for total body insulin sensitivity (NCT00232583)
Timeframe: 72 months

Interventionindex (Mean)
Metfomin & Insulin0.12
Metfomin, Pioglitazone & Glyburide0.16

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Quality of Life Survey (QoL) - Treatment Satisfaction

Treatment satisfaction was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1-5, where 1 - very satisfied; 2 - moderately satisfied; 3 - neither satisfied nor dissatisfied; 4 - moderately dissatisfied; 5 - very dissatisfied. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin1.7
Metfomin, Pioglitazone & Glyburide2.1

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Quality of Life Survey (QoL) - Treatment Impact

Treatment impact was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a Likert scale score of 1-5, where 1 - very satisfied; 2 - moderately satisfied; 3 - neither satisfied nor dissatisfied; 4 - moderately dissatisfied; 5 - very dissatisfied. (NCT00232583)
Timeframe: 72 months

Interventionscore on a sale (Mean)
Metfomin & Insulin1.7
Metfomin, Pioglitazone & Glyburide1.8

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Quality of Life Survey (QoL) - Willingness to Continue Insulin Treatment

Willingness to continue insulin treatment was measured at randomization and 72 months later using the modified Diabetes Quality of Life Clinical Trial Questionnaire. This questionnaire addresses several areas with respect to diabetes QoL. Answers are in the form of a scale score of 1 to 7, where 1 extremely willing to 7 - not at all willing. (NCT00232583)
Timeframe: 72 months

Interventionscore on a scale (Mean)
Metfomin & Insulin1.4

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Change From Baseline in Insulin (Week 26).

The change between the value of insulin collected at week 26 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

InterventionmcIU/mL (Least Squares Mean)
Placebo-1.89
Alogliptin 12.5 mg QD-0.85
Alogliptin 25 mg QD0.14

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Change From Baseline in Insulin (Week 4).

The change between the value of insulin collected at week 4 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

InterventionmcIU/mL (Least Squares Mean)
Placebo-0.62
Alogliptin 12.5 mg QD0.64
Alogliptin 25 mg QD0.89

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Change From Baseline in Insulin (Week 8).

The change between the value of insulin collected at week 8 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

InterventionmcIU/mL (Least Squares Mean)
Placebo-0.81
Alogliptin 12.5 mg QD-0.62
Alogliptin 25 mg QD0.38

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Change From Baseline in Proinsulin/Insulin Ratio (Week 12).

The change between the ratio value of proinsulin and insulin collected at week 12 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionratio (Least Squares Mean)
Placebo-0.002
Alogliptin 12.5 mg QD-0.030
Alogliptin 25 mg QD-0.040

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Change From Baseline in Proinsulin/Insulin Ratio (Week 16).

The change between the ratio value of proinsulin and insulin collected at week 16 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

Interventionratio (Least Squares Mean)
Placebo0.003
Alogliptin 12.5 mg QD-0.037
Alogliptin 25 mg QD-0.041

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Change From Baseline in Proinsulin/Insulin Ratio (Week 20).

The change between the ratio value of proinsulin and insulin collected at week 20 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionratio (Least Squares Mean)
Placebo-0.005
Alogliptin 12.5 mg QD-0.035
Alogliptin 25 mg QD-0.036

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Change From Baseline in Proinsulin/Insulin Ratio (Week 4).

The change between the ratio value of proinsulin and insulin collected at week 4 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

Interventionratio (Least Squares Mean)
Placebo-0.008
Alogliptin 12.5 mg QD-0.064
Alogliptin 25 mg QD-0.043

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Change From Baseline in Proinsulin/Insulin Ratio (Week 8).

The change between the ratio value of proinsulin and insulin collected at week 8 and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionratio (Least Squares Mean)
Placebo-0.009
Alogliptin 12.5 mg QD-0.052
Alogliptin 25 mg QD-0.045

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Number of Participants Requiring Rescue.

The number of participants requiring rescue for failing to achieve pre-specified glycemic targets during the 26 week study. (NCT00286468)
Timeframe: 26 Weeks.

Interventionparticipants (Number)
Placebo28
Alogliptin 12.5 mg QD30
Alogliptin 25 mg QD31

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Number of Participants With Glycosylated Hemoglobin ≤ 6.5%.

The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 6.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo7
Alogliptin 12.5 mg QD19
Alogliptin 25 mg QD28

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Number of Participants With Glycosylated Hemoglobin ≤ 7.0%.

The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo18
Alogliptin 12.5 mg QD60
Alogliptin 25 mg QD69

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Number of Participants With Glycosylated Hemoglobin ≤ 7.5%.

The number of participants with a value for the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) less than or equal to 7.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo33
Alogliptin 12.5 mg QD94
Alogliptin 25 mg QD112

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Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 0.5%.

The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 0.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo26
Alogliptin 12.5 mg QD96
Alogliptin 25 mg QD100

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Change From Baseline in Proinsulin/Insulin Ratio (Week 26).

The change between the ratio value of proinsulin and insulin collected at week 26 or final visit and the ratio value of proinsulin and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionratio (Least Squares Mean)
Placebo-0.008
Alogliptin 12.5 mg QD-0.034
Alogliptin 25 mg QD-0.034

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Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 1.0%.

The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo13
Alogliptin 12.5 mg QD38
Alogliptin 25 mg QD59

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Change From Baseline in Body Weight (Week 8).

The change between Body Weight measured at week 8 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionkg (Least Squares Mean)
Placebo-0.27
Alogliptin 12.5 mg QD0.47
Alogliptin 25 mg QD0.33

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Change From Baseline in Insulin (Week 20).

The change between the value of insulin collected at week 20 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

InterventionmcIU/mL (Least Squares Mean)
Placebo-0.07
Alogliptin 12.5 mg QD1.18
Alogliptin 25 mg QD0.93

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Number of Participants With Marked Hyperglycemia (Fasting Plasma Glucose ≥ 200 mg Per dL).

The number of participants with a fasting plasma glucose value greater than or equal to 200 mg per dL during the 26 week study. (NCT00286468)
Timeframe: 26 Weeks.

Interventionparticipants (Number)
Placebo53
Alogliptin 12.5 mg QD94
Alogliptin 25 mg QD79

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Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 2.0%.

The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 2.0% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo4
Alogliptin 12.5 mg QD5
Alogliptin 25 mg QD12

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Change From Baseline in Body Weight (Week 12).

The change between Body Weight measured at week 12 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionkg (Least Squares Mean)
Placebo-0.12
Alogliptin 12.5 mg QD0.58
Alogliptin 25 mg QD0.40

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Change From Baseline in Body Weight (Week 20).

The change between Body Weight measured at week 20 and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionkg (Least Squares Mean)
Placebo-0.30
Alogliptin 12.5 mg QD0.79
Alogliptin 25 mg QD0.61

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Change From Baseline in Body Weight (Week 26).

The change between Body Weight measured at week 26 or final visit and Body Weight measured at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionkg (Least Squares Mean)
Placebo-0.20
Alogliptin 12.5 mg QD0.60
Alogliptin 25 mg QD0.68

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Number of Participants With Glycosylated Hemoglobin Decrease From Baseline ≥ 1.5%.

The number of participants with a decrease from baseline in the percentage of glycosylated hemoglobin (the percentage of hemoglobin that is bound to glucose) greater than or equal to 1.5% during the 26 week study. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionparticipants (Number)
Placebo7
Alogliptin 12.5 mg QD13
Alogliptin 25 mg QD24

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Change From Baseline in C-peptide (Week 12).

The change between the value of C-peptide collected at week 12 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionng/mL (Least Squares Mean)
Placebo-0.020
Alogliptin 12.5 mg QD0.162
Alogliptin 25 mg QD0.206

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Change From Baseline in C-peptide (Week 16).

The change between the value of C-peptide collected at week 16 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

Interventionng/mL (Least Squares Mean)
Placebo-0.007
Alogliptin 12.5 mg QD0.222
Alogliptin 25 mg QD0.153

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Change From Baseline in C-peptide (Week 20).

The change between the value of C-peptide collected at week 20 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionng/mL (Least Squares Mean)
Placebo-0.016
Alogliptin 12.5 mg QD-0.001
Alogliptin 25 mg QD0.122

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Change From Baseline in C-peptide (Week 26).

The change between the value of C-peptide collected at week 26 or final visit and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionng/mL (Least Squares Mean)
Placebo-0.215
Alogliptin 12.5 mg QD-0.140
Alogliptin 25 mg QD-0.153

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Change From Baseline in C-peptide (Week 4).

The change between the value of C-peptide collected at week 4 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

Interventionng/mL (Least Squares Mean)
Placebo-0.041
Alogliptin 12.5 mg QD0.122
Alogliptin 25 mg QD0.136

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Change From Baseline in C-peptide (Week 8).

The change between the value of C-peptide collected at week 8 and C-peptide collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionng/mL (Least Squares Mean)
Placebo-0.176
Alogliptin 12.5 mg QD0.092
Alogliptin 25 mg QD0.173

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Change From Baseline in Fasting Plasma Glucose (Week 1).

The change between the value of fasting plasma glucose collected at final visit or week 1 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 1.

Interventionmg/dL (Least Squares Mean)
Placebo0.3
Alogliptin 12.5 mg QD-11.8
Alogliptin 25 mg QD-19.0

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Change From Baseline in Fasting Plasma Glucose (Week 12).

The change between the value of fasting plasma glucose collected at week 12 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionmg/dL (Least Squares Mean)
Placebo-3.4
Alogliptin 12.5 mg QD-13.5
Alogliptin 25 mg QD-15.0

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Change From Baseline in Fasting Plasma Glucose (Week 16).

The change between the value of fasting plasma glucose collected at week 16 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

Interventionmg/dL (Least Squares Mean)
Placebo-7.1
Alogliptin 12.5 mg QD-9.0
Alogliptin 25 mg QD-13.0

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Change From Baseline in Fasting Plasma Glucose (Week 2).

The change between the value of fasting plasma glucose collected at week 2 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 2.

Interventionmg/dL (Least Squares Mean)
Placebo-1.8
Alogliptin 12.5 mg QD-16.7
Alogliptin 25 mg QD-21.8

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Change From Baseline in Fasting Plasma Glucose (Week 20).

The change between the value of fasting plasma glucose collected at week 20 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionmg/dL (Least Squares Mean)
Placebo-0.4
Alogliptin 12.5 mg QD-9.3
Alogliptin 25 mg QD-13.6

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Change From Baseline in Fasting Plasma Glucose (Week 26).

The change between the value of fasting plasma glucose collected at week 26 or final visit and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionmg/dL (Least Squares Mean)
Placebo2.2
Alogliptin 12.5 mg QD-4.7
Alogliptin 25 mg QD-8.4

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Change From Baseline in Fasting Plasma Glucose (Week 4).

The change between the value of fasting plasma glucose collected at week 4 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

Interventionmg/dL (Least Squares Mean)
Placebo-3.7
Alogliptin 12.5 mg QD-14.6
Alogliptin 25 mg QD-21.1

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Change From Baseline in Fasting Plasma Glucose (Week 8).

The change between the value of fasting plasma glucose collected at week 8 and fasting plasma glucose collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionmg/dL (Least Squares Mean)
Placebo-3.2
Alogliptin 12.5 mg QD-19.9
Alogliptin 25 mg QD-18.6

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Change From Baseline in Fasting Proinsulin (Week 12).

The change between the value of fasting proinsulin collected at week 12 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionpmol/L (Least Squares Mean)
Placebo-0.5
Alogliptin 12.5 mg QD-0.7
Alogliptin 25 mg QD-0.7

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Change From Baseline in Fasting Proinsulin (Week 16).

The change between the value of fasting proinsulin collected at week 16 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

Interventionpmol/L (Least Squares Mean)
Placebo-1.8
Alogliptin 12.5 mg QD-1.5
Alogliptin 25 mg QD-1.1

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Change From Baseline in Fasting Proinsulin (Week 20).

The change between the value of fasting proinsulin collected at week 20 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionpmol/L (Least Squares Mean)
Placebo-2.5
Alogliptin 12.5 mg QD-2.1
Alogliptin 25 mg QD0.0

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Change From Baseline in Fasting Proinsulin (Week 26).

The change between the value of fasting proinsulin collected at week 26 or final visit and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionpmol/L (Least Squares Mean)
Placebo-2.0
Alogliptin 12.5 mg QD-3.9
Alogliptin 25 mg QD-2.1

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Change From Baseline in Fasting Proinsulin (Week 4).

The change between the value of fasting proinsulin collected at week 4 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

Interventionpmol/L (Least Squares Mean)
Placebo-3.0
Alogliptin 12.5 mg QD-2.6
Alogliptin 25 mg QD0.7

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Change From Baseline in Fasting Proinsulin (Week 8).

The change between the value of fasting proinsulin collected at week 8 and fasting proinsulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionpmol/L (Least Squares Mean)
Placebo-4.2
Alogliptin 12.5 mg QD-4.5
Alogliptin 25 mg QD-0.9

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Change From Baseline in Glycosylated Hemoglobin (HbA1c) at Week 26.

The change in the value of glycosylated hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 26 or final visit and glycosylated hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 26.

Interventionmg/dL (Least Squares Mean)
Placebo0.01
Alogliptin 12.5 mg QD-0.38
Alogliptin 25 mg QD-0.52

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Change From Baseline in Glycosylated Hemoglobin (Week 12).

The change in the value of Glycosylated Hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 12 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

Interventionmg/dL (Least Squares Mean)
Placebo-0.17
Alogliptin 12.5 mg QD-0.58
Alogliptin 25 mg QD-0.69

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Change From Baseline in Glycosylated Hemoglobin (Week 16).

The change in the value of Glycosylated Hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 16 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

Interventionmg/dL (Least Squares Mean)
Placebo-0.16
Alogliptin 12.5 mg QD-0.53
Alogliptin 25 mg QD-0.66

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Change From Baseline in Glycosylated Hemoglobin (Week 20).

The change in the value of Glycosylated Hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 20 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 20.

Interventionmg/dL (Least Squares Mean)
Placebo-0.08
Alogliptin 12.5 mg QD-0.43
Alogliptin 25 mg QD-0.60

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Change From Baseline in Glycosylated Hemoglobin (Week 4).

The change in the value of Glycosylated Hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 4 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 4.

Interventionmg/dL (Least Squares Mean)
Placebo-0.18
Alogliptin 12.5 mg QD-0.40
Alogliptin 25 mg QD-0.46

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Change From Baseline in Glycosylated Hemoglobin (Week 8).

The change in the value of Glycosylated Hemoglobin (the concentration of glucose bound to hemoglobin as a percent of the absolute maximum that can be bound) collected at week 8 and Glycosylated Hemoglobin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 8.

Interventionmg/dL (Least Squares Mean)
Placebo-0.18
Alogliptin 12.5 mg QD-0.57
Alogliptin 25 mg QD-0.65

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Change From Baseline in Insulin (Week 12).

The change between the value of insulin collected at week 12 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 12.

InterventionmcIU/mL (Least Squares Mean)
Placebo-0.02
Alogliptin 12.5 mg QD1.33
Alogliptin 25 mg QD1.00

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Change From Baseline in Insulin (Week 16).

The change between the value of insulin collected at week 16 and insulin collected at baseline. (NCT00286468)
Timeframe: Baseline and Week 16.

InterventionmcIU/mL (Least Squares Mean)
Placebo-1.21
Alogliptin 12.5 mg QD1.74
Alogliptin 25 mg QD0.51

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Change From Baseline in Fasting Plasma Glucose (FPG) at Week 24

Mean change from baseline in FPG at Week 24, adjusted for baseline value. (NCT00313313)
Timeframe: Baseline, Week 24

,,
Interventionmg/dL (Mean)
Baseline MeanWeek 24 MeanAdjusted Mean Change from Baseline
Placebo + Glyburide 7.5 mg174.4174.60.7
Saxagliptin 2.5 mg + Glyburide 7.5 mg170.1164.4-7.1
Saxagliptin 5 mg + Glyburide 7.5 mg175.0164.6-9.7

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Change From Baseline in Hemoglobin A1c (A1C) at Week 24

Mean change from baseline in A1C at Week 24, adjusted for baseline value. (NCT00313313)
Timeframe: Baseline, Week 24

,,
Interventionpercent (Mean)
Baseline MeanWeek 24 MeanAdjusted Mean Change from Baseline
Placebo + Glyburide 7.5 mg8.448.520.08
Saxagliptin 2.5 mg + Glyburide 7.5 mg8.367.83-0.54
Saxagliptin 5 mg + Glyburide 7.5 mg8.487.83-0.64

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Changes From Baseline in Postprandial Glucose (PPG) Area Under the Curve (AUC) Response to an Oral Glucose Tolerance Test (OGTT) at Week 24

Mean change from baseline for 0 to 180 minutes PPG AUC at Week 24, adjusted for baseline values. (NCT00313313)
Timeframe: Baseline, Week 24

,,
Interventionmg*min/dL (Mean)
Baseline MeanWeek 24 MeanAdjusted Mean Change from Baseline
Placebo + Glyburide 7.5 mg51801524161196
Saxagliptin 2.5 mg + Glyburide 7.5 mg4912445402-4296
Saxagliptin 5 mg + Glyburide 7.5 mg5034245391-5000

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Percentage of Participants Achieving A1C < 7% at Week 24

Percentage of participants achieving A1C < 7%, the American Diabetes Association's defined goal for glycemia, at each dose of saxagliptin plus glyburide versus placebo plus upward titrated glyburide at Week 24. (NCT00313313)
Timeframe: Week 24

InterventionPercentage of participants (Number)
Saxagliptin 2.5 mg + Glyburide 7.5 mg22.4
Saxagliptin 5 mg + Glyburide 7.5 mg22.8
Placebo + Glyburide 7.5 mg9.1

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Mean Postprandial PG Increment in 7-point Plasma Glucose Profile After 24 Weeks of Treatment

Mean postprandial plasma glucose (PG) increment in 7-point plasma glucose profile, ie the mean of the difference of plasma glucose measured before and after a meal, after 24 weeks of treatment. The 7 time points during the day were: Before breakfast, 120 minutes after start of breakfast, before lunch, 120 minutes after start of lunch, before dinner, 120 minutes after start of dinner, and at bedtime. (NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide59.69
Glibenclamide79.66

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Mean PG in 7-point Plasma Glucose Profile After 24 Weeks of Treatment

Plasma glucose (PG) profile measured after 24 weeks of treatment. The time points during the day were: Before breakfast, 120 minutes after start of breakfast, before lunch, 120 minutes after start of lunch, before dinner, 120 minutes after start of dinner, and at bedtime. (NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide155.98
Glibenclamide173.61

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Mean Postprandial PG Increment in 7-point Plasma Glucose Profile After 52 Weeks of Treatment

Mean postprandial plasma glucose (PG) increment in 7-point plasma glucose profile, ie the mean of the difference of plasma glucose measured before and after a meal, after 52 weeks of treatment. The 7 time points during the day were: Before breakfast, 120 minutes after start of breakfast, before lunch, 120 minutes after start of lunch, before dinner, 120 minutes after start of dinner, and at bedtime. (NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide63.56
Glibenclamide76.59

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Postprandial Glucose AUC After 24 Weeks of Treatment

Postprandial glucose AUC measured 0-3 hours after a meal after 24 weeks of treatment (NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionmg/dL *h (Least Squares Mean)
Liraglutide557.54
Glibenclamide670.60

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Hypoglycaemic Episodes

Hypoglycaemic episodes measured over 52 weeks of treatment. Hypoglycaemic episodes were defined as major, minor, or symptoms only. Major if the subject was unable to treat her/himself. Minor if subject was able to treat her/himself and plasma glucose was below 3.1 mmol/L. Symptoms only if subject was able to treat her/himself and with no plasma glucose measurement or plasma glucose higher than or equal to 3.1 mmol/L. (NCT00393718)
Timeframe: over 52 weeks of treatment

,
Interventionnumber of events per year of exposure (Number)
All hypoglycaemic episodesMajorMinorSymptoms only
Glibenclamide3.8430.0001.1032.740
Liraglutide0.6940.0000.1870.507

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Postprandial Glucose AUC After 52 Weeks of Treatment

Postprandial glucose AUC measured 0-3 hours after a meal after 52 weeks of treatment (NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionmg/dL *h (Least Squares Mean)
Liraglutide608.66
Glibenclamide683.17

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Body Weight After 24 Weeks of Treatment

(NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionkg (Least Squares Mean)
Liraglutide64.06
Glibenclamide65.97

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Body Weight After 52 Weeks of Treatment

(NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionkg (Least Squares Mean)
Liraglutide64.30
Glibenclamide66.01

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Fasting Plasma Glucose After 24 Weeks of Treatment

(NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide137.2
Glibenclamide150.1

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Fasting Plasma Glucose After 52 Weeks of Treatment

(NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide145.8
Glibenclamide157.5

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Glycosylated Haemoglobin A1c (HbA1c) After 24 Weeks of Treatment

(NCT00393718)
Timeframe: after 24 weeks of treatment

Interventionpercentage of total haemoglobin (Least Squares Mean)
Liraglutide6.99
Glibenclamide7.50

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Glycosylated Haemoglobin A1c (HbA1c) After 52 Weeks of Treatment

(NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionpercentage of total haemoglobin (Least Squares Mean)
Liraglutide7.31
Glibenclamide7.80

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Mean PG in 7-point Plasma Glucose Profile After 52 Weeks of Treatment

Mean plasma glucose(PG) in 7-point plasma glucose profile measured after 52 weeks of treatment. The 7 time points during the day were: Before breakfast, 120 minutes after start of breakfast, before lunch, 120 minutes after start of lunch, before dinner, 120 minutes after start of dinner, and at bedtime. (NCT00393718)
Timeframe: after 52 weeks of treatment

Interventionmg/dL (Least Squares Mean)
Liraglutide167.39
Glibenclamide184.60

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Rate of Cesarean Delivery

(NCT00744965)
Timeframe: After delivery

InterventionParticipants (Count of Participants)
Placebo67
Glyburide70

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Number of Participants With Large for Gestational Age Infants

Birth weight exceeding the 90th percentile for the gestational age at delivery. (NCT00744965)
Timeframe: After delivery

InterventionParticipants (Count of Participants)
Placebo22
Glyburide20

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Neonatal Intensive Care Unit Admissions

(NCT00744965)
Timeframe: Until hospital discharge

InterventionParticipants (Count of Participants)
Placebo11
Glyburide13

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Need for Insulin Treatment

(NCT00744965)
Timeframe: after delivery

InterventionParticipants (Count of Participants)
Placebo4
Glyburide4

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Need for Insulin Therapy

(NCT00744965)
Timeframe: throughout pregnancy and delivery

InterventionParticipants (Count of Participants)
Placebo4
Glyburide4

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3rd or 4th Degree Perineal Laceration

(NCT00744965)
Timeframe: at delivery

InterventionParticipants (Count of Participants)
Placebo5
Glyburide1

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Chorioamnionitis

Maternal fever >=38.0°C (NCT00744965)
Timeframe: intrapartum

InterventionParticipants (Count of Participants)
Placebo12
Glyburide15

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Diagnosis of Pregnancy-induced Hypertension

(NCT00744965)
Timeframe: until hospital discharge

InterventionParticipants (Count of Participants)
Placebo12
Glyburide15

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Mean Fetal Weight at Birth

(NCT00744965)
Timeframe: Immediately after delivery of fetus

Interventiongrams (Mean)
Placebo3355
Glyburide3322

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Shoulder Dystocia

(NCT00744965)
Timeframe: at delivery

InterventionParticipants (Count of Participants)
Placebo1
Glyburide0

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Macrosomia

birth weight 4,000 g or greater (NCT00744965)
Timeframe: After delivery

InterventionParticipants (Count of Participants)
Placebo18
Glyburide13

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Cmax (Maximum Observed Concentration) - Glyburide

Bioequivalence based on Cmax (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Glyburide Metformin190.17
Glucovance®166.48

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AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Metformin

Bioequivalence based on AUC0-t (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin6203.57
Glucovance®6448.34

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AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Glyburide

Bioequivalence based on AUC0-t (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin942.94
Glucovance®943.45

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AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Glyburide

Bioequivalence based on AUC0-inf (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin970.22
Glucovance®977.28

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AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Metformin

Bioequivalence based on AUC0-inf (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin6308.12
Glucovance®6552.79

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Cmax (Maximum Observed Concentration) - Metformin

Bioequivalence based on Cmax (NCT00835991)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Glyburide Metformin755.10
Glucovance®766.30

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AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Glyburide

Bioequivalence based on AUC0-inf (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin805.92
Glucovance®806.89

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AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Metformin

Bioequivalence based on AUC0-t (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin5798.89
Glucovance®5942.99

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AUC0-t [Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)] - Glyburide

Bioequivalence based on AUC0-t (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin773.84
Glucovance®781.35

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Cmax (Maximum Observed Concentration) - Glyburide

Bioequivalence based on Cmax (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Glyburide Metformin106.46
Glucovance®116.53

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Cmax (Maximum Observed Concentration) - Metformin

Bioequivalence based on Cmax (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Glyburide Metformin840.23
Glucovance®889.45

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AUC0-inf [Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)] - Metformin

Bioequivalence based on AUC0-inf (NCT00836472)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Glyburide Metformin5915.32
Glucovance®6047.23

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Number of Participants Assessed for Glucose Control

The importance of exercise in the management of blood glucose was emphasized, and 30 minutes of walking per day was recommended. Patients received instruction from a nurse educator or a certified diabetes educator regarding diet and the use of the glucometer. Number of participants with a glucose level <100 mg/dL. (NCT00965991)
Timeframe: fasting and 2 hour postprandial blood glucose

InterventionParticipants (Count of Participants)
Metformin50
Glyburide50

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Percentage of Participants With Clinically-Significant Elevations of Alanine Aminotransferase/Serum Glutamate Pyruvate Transaminase (ALT/SGPT) During the 12-week Treatment Period

Clinically significant elevations of ALT/SGPT were considered ≥3 times the upper limit of normal (ULN). The percentage of participants above 2- and 5-fold ULN was not analyzed due to the early termination of the trial. The percentage of participants with ALT 3-fold ULN or higher is presented. (NCT01029795)
Timeframe: Baseline through 12 weeks

Interventionpercentage of participants (Number)
LY259950618.8
Glyburide0

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Mean Change in C-peptide Area Under the Curve (AUC), 0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnmol*hour/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.18
Placebo + Metformin-0.18
Canakinumab 150 mg + Metformin + Sulfonylurea-0.21
Placebo + Metformin + Sulfonylurea0.12
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.61
Placebo + Met + Sulfonyl + Thiaz0.02
Canakinumab 150 mg + Insulin0.16
Placebo + Insulin-0.29
Canakinumab 150 mg in Participants With IGT-0.43
Placebo in Participants With IGT-0.40

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Mean Change in Fasting Plasma Glucose, From Baseline to 4 Weeks

"Change in Fasting Glucose Level measured from plasma taken at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.32
Placebo + Metformin0.33
Canakinumab 150 mg + Metformin + Sulfonylurea-0.20
Placebo + Metformin + Sulfonylurea-0.23
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.33
Placebo + Met + Sulfonyl + Thiaz-0.36
Canakinumab 150 mg + Insulin-0.26
Placebo + Insulin-0.80
Canakinumab 150 mg in Participants With IGT-0.06
Placebo in Participants With IGT0.10

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Mean Change in Fasting Plasma Insulin, From Baseline to 4 Weeks

"Change in Fasting Insulin level taken from plasma, measured at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-3.58
Placebo + Metformin10.73
Canakinumab 150 mg + Metformin + Sulfonylurea-16.07
Placebo + Metformin + Sulfonylurea-9.40
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.77
Placebo + Met + Sulfonyl + Thiaz2.31
Canakinumab 150 mg + Insulin21.27
Placebo + Insulin25.67
Canakinumab 150 mg in Participants With IGT-.021
Placebo in Participants With IGT-3.43

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Mean Change in Fructosamine, From Baseline to 4 Weeks

"Change in Fructosamine Level taken from plasma, measured at Baseline and after 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population" (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-5.30
Placebo + Metformin-0.75
Canakinumab 150 mg + Metformin + Sulfonylurea-3.45
Placebo + Metformin + Sulfonylurea-7.50
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-1.81
Placebo + Met + Sulfonyl + Thiaz-3.07
Canakinumab 150 mg + Insulin-3.00
Placebo + Insulin-19.73
Canakinumab 150 mg in Participants With IGT-6.36
Placebo in Participants With IGT1.39

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Mean Change in Insulin Area Under the Curve (AUC) 0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol*hour/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-9.37
Placebo + Metformin1.21
Canakinumab 150 mg + Metformin + Sulfonylurea-73.25
Placebo + Metformin + Sulfonylurea-38.32
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-36.96
Placebo + Met + Sulfonyl + Thiaz8.46
Canakinumab 150 mg + Insulin163.87
Placebo + Insulin139.24
Canakinumab 150 mg in Participants With IGT44.27
Placebo in Participants With IGT-106.68

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Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-2 Hours, From Baseline to 4 Weeks.

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge. Blood samples were taken prior to and after meal for glucose and insulin at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal.A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include patients from the IGT population (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.06
Placebo + Metformin-0.23
Canakinumab 150 mg + Metformin + Sulfonylurea0.04
Placebo + Metformin + Sulfonylurea0.45
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.79
Placebo + Met + Sulfonyl + Thiaz1.16
Canakinumab 150 mg + Insulin1.23
Placebo + Insulin-0.49
Canakinumab 150 mg in Participants With IGT-1.50
Placebo in Participants With IGT-1.93

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Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 0-4 Hours, From Baseline to 4 Weeks.

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge. Blood samples were taken prior to and after meal for glucose, insulin and C-peptide at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin0.44
Placebo + Metformin-0.99
Canakinumab 150 mg + Metformin + Sulfonylurea-0.32
Placebo + Metformin + Sulfonylurea1.22
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.63
Placebo + Met + Sulfonyl + Thiaz1.24
Canakinumab 150 mg + Insulin0.53
Placebo + Insulin-0.49
Canakinumab 150 mg in Participants With IGT-1.38
Placebo in Participants With IGT-1.35

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Mean Change in Meal Stimulated Insulin Secretion Rate (ISR) Relative to Glucose 2-4 Hours, From Baseline to 4 Weeks

Change in Insulin Secretion Rate stimulated by Liquid mixed-meal challenge Blood samples were taken prior to and after meal for glucose and insulin at sample times: -20, -10, -1 and 10, 20, 30, 60, 90, 120, 180, and 240 minutes relative to the start of the meal. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/min/m^2/mmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin0.21
Placebo + Metformin-2.15
Canakinumab 150 mg + Metformin + Sulfonylurea-2.98
Placebo + Metformin + Sulfonylurea2.02
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.15
Placebo + Met + Sulfonyl + Thiaz1.19
Canakinumab 150 mg + Insulin-0.43
Placebo + Insulin-0.51
Canakinumab 150 mg in Participants With IGT-0.71
Placebo in Participants With IGT-1.00

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Mean Change in Peak Plasma C-peptide Level, From Baseline to 4 Weeks

"Change in mean peak plasma C-peptide level measured from Baseline to 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.04
Placebo + Metformin-0.04
Canakinumab 150 mg + Metformin + Sulfonylurea-0.10
Placebo + Metformin + Sulfonylurea0.16
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.21
Placebo + Met + Sulfonyl + Thiaz0.05
Canakinumab 150 mg + Insulin0.07
Placebo + Insulin-0.14
Canakinumab 150 mg in Participants With IGT-0.18
Placebo in Participants With IGT-0.18

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Mean Change in Peak Plasma Glucose, From Baseline to 4 Weeks

"Change in peak plasma glucose level as measured from Baseline to 4 weeks of treatment.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.41
Placebo + Metformin0.21
Canakinumab 150 mg + Metformin + Sulfonylurea-0.43
Placebo + Metformin + Sulfonylurea-0.03
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-0.82
Placebo + Met + Sulfonyl + Thiaz-0.77
Canakinumab 150 mg + Insulin-0.15
Placebo + Insulin-0.60
Canakinumab 150 mg in Participants With IGT-0.34
Placebo in Participants With IGT-0.04

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Mean Change in Peak Plasma Insulin, From Baseline to 4 Weeks

Change in mean peak plasma Insulin level as measured from Baseline to 4 weeks of treatment. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionpmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin8.09
Placebo + Metformin44.56
Canakinumab 150 mg + Metformin + Sulfonylurea-55.07
Placebo + Metformin + Sulfonylurea11.33
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia5.13
Placebo + Met + Sulfonyl + Thiaz-5.15
Canakinumab 150 mg + Insulin91.74
Placebo + Insulin36.87
Canakinumab 150 mg in Participants With IGT56.21
Placebo in Participants With IGT-26.43

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Mean Change in Post-prandial Glucose Area Under the Curve (AUC)0-4 Hours, From Baseline to 4 Weeks

Blood samples were drawn after a test meal at 0, 15, 30, 45, 60, 90, 120, 180 and 240 min. Insulin levels over 4 hrs were shown as Area Under the Curve,(AUC). AUC was calculated as: x=1 AUC ΣAx n Where Ax = AUC for the 240 min.interval, and X = 1 for the 1st interval. A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab vs placebo within each T2DM group. The mixed model didn't include the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol*hr/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.59
Placebo + Metformin0.46
Canakinumab 150 mg + Metformin + Sulfonylurea-1.37
Placebo + Metformin + Sulfonylurea-1.24
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-3.58
Placebo + Met + Sulfonyl + Thiaz-2.88
Canakinumab 150 mg + Insulin-1.49
Placebo + Insulin-1.76
Canakinumab 150 mg in Participants With IGT-0.71
Placebo in Participants With IGT-0.10

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Mean Change in Fasting Glucose Disposition Index(GDI)1 and Index 2, From Baseline to 4 Weeks

GDI 1 is the product of insulin sensitivity index (Si)during the 1st phase of insulin secretion and β-cell function as measured by the acute insulin response (AIR).GDI 2 is the product of (Si)during the 2nd phase of insulin secretion and β-cell function as measured by the acute insulin response (AIR). A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT group. (NCT01068860)
Timeframe: Baseline, 4 weeks

,,,,,,,,,
Interventionnumber (Least Squares Mean)
Index 1Index 2 (n= 32,15, 29,15, 30,13, 25, 15, 20, 26)
Canakinumab 150 mg + Insulin0.25-0.21
Canakinumab 150 mg + Metformin0.060.14
Canakinumab 150 mg + Metformin + Sulfonylurea0.06-0.94
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.240.62
Canakinumab 150 mg in Participants With IGT-0.51-0.16
Placebo + Insulin-0.27-0.25
Placebo + Met + Sulfonyl + Thiaz0.330.49
Placebo + Metformin-0.29-0.81
Placebo + Metformin + Sulfonylurea0.370.81
Placebo in Participants With IGT-0.64-0.31

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Mean Change in Absolute Glucose Level at 2 Hours, From Baseline to 4 Weeks

"Change in glucose level measured after 2 hours of fasting. Blood sample was drawn at 0 minutes and at 240 minutes.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionmmol/L (Least Squares Mean)
Canakinumab 150 mg + Metformin-0.53
Placebo + Metformin0.13
Canakinumab 150 mg + Metformin + Sulfonylurea-0.60
Placebo + Metformin + Sulfonylurea0.18
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia-1.08
Placebo + Met + Sulfonyl + Thiaz-0.56
Canakinumab 150 mg + Insulin-0.56
Placebo + Insulin-0.16
Canakinumab 150 mg in Participants With IGT-0.26
Placebo in Participants With IGT-0.25

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Mean Change in Quantitative Insulin Sensitivity Check Index (QUICKI) Score, From Baseline to 4 Weeks

"The Quantitative Insulin Sensitivity Check Index (QUICKI) score, measures insulin sensitivity which is the inverse of insulin resistance. The score is calculated by the equation: 1 /(log(fasting insulin µU/mL) + log(fasting glucose mg/dL)). In normal subjects the mean score ± SE is 0.366 ± 0.029.~A mixed model with treatment fitted as fixed effect, and population and the interaction of population and treatment fitted as random effects were used for the comparison of Canakinumab versus placebo within each T2DM population. The mixed model did not include participants from the IGT population." (NCT01068860)
Timeframe: Baseline, 4 weeks

Interventionnumber (Least Squares Mean)
Canakinumab 150 mg + Metformin0.004
Placebo + Metformin-0.000
Canakinumab 150 mg + Metformin + Sulfonylurea0.002
Placebo + Metformin + Sulfonylurea0.009
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia0.018
Placebo + Met + Sulfonyl + Thiaz-0.001
Canakinumab 150 mg + Insulin-0.003
Placebo + Insulin0.005
Canakinumab 150 mg in Participants With IGT-0.001
Placebo in Participants With IGT0.001

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Number of Participants Reporting Death, Serious Adverse Events (SAEs) and Adverse Events (AEs) Above 5% Frequency, From Baseline to 4 Weeks

An adverse event is any unwanted event, whether related to study drug or not occuring during the study period. A Serious Adverse Event (SAE) is an event resulting in death, requiring or prolonging hospitalization, a congenital anomaly or other important medical event. AEs and SAEs were recorded at each visit. (NCT01068860)
Timeframe: Baseline, 4 weeks

,,,,,,,,,
Interventionparticipants (Number)
Number of Participants with Serious Adverse EventsNumber of Participants with Non-serious AEs > 5%
Canakinumab 150 mg + Insulin06
Canakinumab 150 mg + Metformin00
Canakinumab 150 mg + Metformin + Sulfonylurea06
Canakinumab 150 mg Canakinumab 150 mg + Met + Sulfonyl + Thia04
Canakinumab 150 mg in Participants With IGT00
Placebo + Insulin03
Placebo + Met + Sulfonyl + Thiaz03
Placebo + Metformin04
Placebo + Metformin + Sulfonylurea03
Placebo in Participants With IGT00

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Number of Participants With a Modified Rankin Scale (mRS) Score ≤ 4

The mRS scale runs from 0-6, the scoring is as follows: 0 - No symptoms, 1 - No significant disability, 2 - Slight disability, 3 - Moderate disability, 4 - Moderately severe disability, 5 - Severe disability, 6 - Dead (NCT01268683)
Timeframe: Day 30, Day 90

InterventionNumber of Participants (Number)
Day 30Day 90
RP-1127 (Glyburide for Injection)98

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National Institute of Health Stroke Scale (NIHSS) Score

The NIHSS is composed of 11 categories, each of which is scored between 0 and 4. A score of 0 indicates normal function, a higher score indicates more impairment. Category scores are summed to generate the total NIHSS score (possibles scores range from 0-42). (NCT01268683)
Timeframe: Baseline, Day 1, Day 2, Day 3, and Day 7

InterventionScore on a Scale (Mean)
BaselineDay 1Day 2Day 3Day 7
RP-1127 (Glyburide for Injection)17.818.415.616.213.9

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Midline Shift

(NCT01268683)
Timeframe: Baseline, Day 1, Day 2, and Day 3

InterventionMillimeters (mm) (Mean)
BaselineDay 1Day 2Day 3
RP-1127 (Glyburide for Injection)0.562.002.632.50

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Ipsilateral Ventricle Volume

(NCT01268683)
Timeframe: Baseline, Day 1, Day 2, and Day 3

InterventionCm^3 (Mean)
BaselineDay 1Day 2Day 3
RP-1127 (Glyburide for Injection)11.789.258.9210.07

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Infarcted Hemisphere Volume

(NCT01268683)
Timeframe: Baseline, Day 1, Day 2, and Day 3

InterventionCentimeters cubed (cm^3) (Mean)
BaselineDay 1Day 2Day 3
RP-1127 (Glyburide for Injection)135.20156.78165.38181.71

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Glasgow Coma Scale (GCS) Score

The GCS is scored on a scale between 3 and 15 (3 = the worst, and 15 = best). It is composed of three parameters : Best Eye Response (scored on a scale of 1-4), Best Verbal Response (scored on a scale of 1-5), Best Motor Response (scored on a scale of 1-6) (NCT01268683)
Timeframe: Baseline, Day 1, Day 2, Day 3, and Day 7

InterventionScore on a scale (Mean)
BaselineDay 1Day 2Day 3Day 7
RP-1127 (Glyburide for Injection)12.511.912.512.813.5

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Frequency of Hemorrhagic Events

(NCT01268683)
Timeframe: Day 1, Day 2, and Day 3

InterventionNumber of Events (Number)
Hemorrhagic Infarction Type 1Hemorrhagic Infarction Type 2Parenchymal Hematoma Type 1Parenchymal Hematoma Type 2
RP-1127 (Glyburide for Injection)3800

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Absolute Diffusion Weighted Imaging (DWI) Lesion Volume

(NCT01268683)
Timeframe: Baseline, Day 1, Day 2, and Day 3

InterventionCm^3 (Mean)
BaselineDay 1Day 2Day 3
RP-1127 (Glyburide for Injection)101.76141.62152.31169.73

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Rate of Enrollment

The number of months to enroll 10 participants. (NCT01268683)
Timeframe: Day 1

InterventionMonths (Number)
RP-1127 (Glyburide for Injection)9.6

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Percentage of Participants With Pre-specified Adverse Events Associated With Glyburide According to Protocol

(NCT01268683)
Timeframe: Up to Day 4

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)0

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Percentage of Participants With All Four MRI Assessments Per Protocol

(NCT01268683)
Timeframe: Up to Day 3

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)90

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Percentage of Participants Requiring One or More Hypoglycemia Treatments

(NCT01268683)
Timeframe: Up to Day 4

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)0

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Percentage of Participants Completing 90-Day Follow-Up

(NCT01268683)
Timeframe: Day 90

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)80

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Percentage of Enrolled Participants to Screened Participants

(NCT01268683)
Timeframe: Day 1

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)5.7

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Full Outline of UnResponsiveness (FOUR) Score

The FOUR Score is a 17-point scale (with potential scores ranging from 0 - 16). Decreasing FOUR Score is associated with worsening level of consciousness. The FOUR Score assesses four domains of neurological function: eye responses, motor responses, brainstem reflexes, and breathing pattern. (NCT01268683)
Timeframe: Baseline, Day 1, Day 2, Day 3, and Day 7

InterventionScore on a Scale (Mean)
BaselineDay 1Day 2Day 3Day 7
RP-1127 (Glyburide for Injection)15.114.514.614.614.8

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Number of Participants Requiring Decompressive Craniectomy (DC)

(NCT01268683)
Timeframe: Up to Day 90

InterventionNumber of Participants (Number)
RP-1127 (Glyburide for Injection)2

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Number of MRI Assessments Per Participant

(NCT01268683)
Timeframe: Up to Day 3

InterventionNumber of MRIs (Mean)
RP-1127 (Glyburide for Injection)3.9

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Change From Baseline in DWI Lesion Volume

(NCT01268683)
Timeframe: Baseline, Day 1, Day 2, and Day 3 (Day 3 reported)

InterventionCm^3 (Mean)
RP-1127 (Glyburide for Injection)60.30

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Percentage of Dose Reductions/ Dose Suspensions

(NCT01268683)
Timeframe: Up to Day 3

InterventionPercentage of Participants (Number)
RP-1127 (Glyburide for Injection)0

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Number of Participants With Adverse Events and Serious Adverse Events

Adverse Events (AE's) of special interest (cardiac events, difficulty controlling blood sugar, liver problems, and blood disorders, including anemia) will be followed for 30 days and all Severe Adverse Events (SAE's) will be followed for 90 days. SAE's and AE's were reviewed, and the number of participants with unanticipated adverse events, or drug-related SAE's were assessed. (NCT01268683)
Timeframe: Up to Day 90

InterventionNumber of Participants (Number)
Adverse EventsSerious Adverse Events
RP-1127 (Glyburide for Injection)103

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Absolute Change in HbA1C Compared to Baseline

The secondary endpoint was the change from baseline values of HbA1C in the Vildagliptin vs Glibenclamide arm at 4 and 12 months (NCT01822548)
Timeframe: V0 (randomization), V2 (month4), V4 (month 12).

,
Interventionpercentage (Median)
V2 (4 month)V4 (12 month)
Glibenclamide & Metformin6.87.1
Vildagliptin & Metformin6.87.0

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Absolute Change in the Endothelial Progenitor Cell (EPC) Number

The study primary endpoint was the change from baseline values of the EPC number in the Vildagliptin vs Glibenclamide arm at 4 and 12 months. (NCT01822548)
Timeframe: V0, V2 (month 4), V4 (12 month)

,
InterventionEPC/10^6 cells (Median)
V2 (4 month)V4 (12 month)
Glibenclamide & Metformin3632
Vildagliptin & Metformin3745

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Change From Baseline in Percentage of Hypoglycemic Values (Glucose Sensor Readings: < 70, <60, <50 mg/dL)

Hypoglycemia, defined as low blood glucose, is a common side effect of medications used to treat diabetes mellitus type 2. The percentage of hypoglycemic corrected CGM readings (sensor glucose <70, <60, <50 mg/dL) over a 24-hour period were determined at baseline and Day 13. CGM values were corrected using a participant-administered finger-stick test for blood glucose. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from baseline to Day 13 indicates improvement in occurrence of hypoglycemia. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

,
InterventionPercent change (Least Squares Mean)
<70 mg/dL<60 mg/dL<50 mg/dL
Glibenclamide 2.50 mg TDD0.80.2-0.3
Sitagliptin 50 mg-0.3-0.4-0.3

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Change From Baseline in 24-hour Mean Glucose Level

The mean glucose level over 24-hours at Baseline and Day 13 was determined using CGM values corrected for participant-administered finger-stick values. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-19.1
Glibenclamide 2.50 mg TDD-34.8

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Change From Baseline in Mean Amplitude of Glycemic Excursions (MAGE) at Day 13

MAGE is a popular metric for assessment of major (e.g., postprandial) glucose swings. MAGE is calculated as the average of differences between consecutive glucose peaks and nadirs greater than 1 standard deviation (SD) of 24-hour mean glucose. In this assessment, glucose levels were determined using continuous glucose monitoring (CGM) over 24 hours at Baseline and Day 13; CGM values were further corrected for blood glucose values obtained via participant-administered finger-stick. Least squares (LS) means values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-18.5
Glibenclamide 2.50 mg TDD-9.7

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Change From Baseline in the Standard Deviation of Blood Glucose Levels

SD is a popular metric for assessment of postprandial glucose swings. The SD of all glycemic excursions over 24 hours (i.e., total of 288 glucose values over 24 hours) was determined for Baseline and Day 13. Original values were obtained using CGM and corrected for blood glucose values obtained via participant-administered finger-stick. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from Baseline to Day 13 indicates improvement of the assessed outcome. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

Interventionmg/dL (Least Squares Mean)
Sitagliptin 50 mg-10.2
Glibenclamide 2.50 mg TDD-4.2

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Change From Baseline in Maximum Incremental Postprandial Glucose Levels in Each Meal

The peak postprandial glucose level during the 3 hours post meal minus the preprandial glucose level 1 hour before meal was determined for corrected CGM values at Baseline and Day 13 for breakfast, lunch, and dinner. Meals were standardized with respect to total calories, and protein, fat, and carbohydrate composition as well as timing of administration. CGM values were corrected using a participant-administered finger-stick test for blood glucose. LS mean values were derived from a constrained longitudinal analysis model. A negative (-) change from baseline to Day 13 indicates better control of postprandial glucose. (NCT02318693)
Timeframe: Baseline (Day -2) and Day 13

,
Interventionmg/dL (Least Squares Mean)
BreakfastLunchDinner
Glibenclamide 2.50 mg TDD-12.01.2-14.1
Sitagliptin 50 mg-24.8-13.2-9.0

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Number of Participants Administered Dexamethasone (or Any Corticosteroid Administration With the Purpose of Treating Cerebral Edema)

Measured between the time of SRS and the time of the one and three month post SRS MRI scans. (NCT02460874)
Timeframe: 4 months

InterventionParticipants (Count of Participants)
Pilot Portion0
Randomized Portion0

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Number of Participants With Absolute Volume Change of Index Tumor(s)

Absolute volume change of index tumor(s) that received radiosurgery as manually contoured by the radiation oncologist defined from T1 post gadolinium sequences at the time of SRS and the time of the one and three month post SRS MRI scans. (NCT02460874)
Timeframe: 4 months

InterventionParticipants (Count of Participants)
Pilot Portion0
Randomized Portion0

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Number of Participants With Cerebral Edema Increase as Measured on FLAIR Volumetric Imaging

Defined from MRI taken at the time of SRS and the time of the one and three month post SRS MRI scans. (NCT02460874)
Timeframe: 4 months

InterventionParticipants (Count of Participants)
Pilot Portion1
Randomized Portion0

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Number of Participants With CTCAE Version 4.0 Reportable Toxicities of Grades 1-2 Cardiac Disorders or Hepatobiliary Disorders.

Incidence of CTCAE version 4.0 reportable toxicities of grades 1-2 Cardiac Disorders or Hepatobiliary Disorders. (NCT02460874)
Timeframe: Up to 4 months

InterventionParticipants (Count of Participants)
Pilot Portion0
Randomized Portion0

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Number of Participants With CTCAE Version 4.0 Reportable Toxicities of Grades 2-5.

Incidence of CTCAE version 4.0 reportable toxicities of grades 2-5. (NCT02460874)
Timeframe: 4 months

InterventionParticipants (Count of Participants)
Pilot Portion0
Randomized Portion0

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Number of Participants With Dose Limiting Toxicities (DLTs)

Assessed between the time of glyburide initiation and the time of the one month follow-up MRI. (NCT02460874)
Timeframe: 4 months

InterventionParticipants (Count of Participants)
Pilot Portion0
Randomized Portion0

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Number of Participants With Neurologic Recovery Following tSCI

The neurologic status of patients will be assessed using the American Spinal Injury Association (ASIA) Impairment Scale (AIS) as assessed by International Standards for Neurological Classification of SCI (ISNCSCI) criteria. (NCT02524379)
Timeframe: One year post enrollment

InterventionParticipants (Count of Participants)
Glyburide Treatment Arm2

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Number of Participants With tSCI Recruited Within the Specified Time Window

A measure of feasibility of undertaking a larger phase II study among this population of patients where treatment must begin within a short injury-to-drug time window. (NCT02524379)
Timeframe: Enrollment Period (within 8 hours of tSCI)

InterventionParticipants (Count of Participants)
Glyburide Treatment Arm3

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Percentage of Participants With Glasgow Outcome Scale - Extended (GOS-E) Score at Day 180

The GOS-E is a global disability scale used to assess recovery after traumatic brain injury. For this study, the 8 point ordinal scale was condensed to the following 7-categories: 1 and 2 combined: Dead and Vegetative State, 3: Lower Severe disability, 4: Upper Severe disability, 5: Lower Moderate disability, 6: Upper Moderate disability, 7 : Lower Good recovery, and 8: Upper Good Recovery. Lower scores indicate death and higher scores indicate recovery. (NCT03954041)
Timeframe: Day 180

,,
InterventionPercentage of participants (Number)
Score: 1/2Score: 3Score: 4Score: 5Score: 6Score: 7Score: 8
BIIB093 3 mg/Day013.326.76.7013.340.0
BIIB093 5 mg/Day027.39.10027.336.4
Placebo013.3013.326.76.740.0

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Percentage of Participants Requiring Delayed Intubation

Delayed intubation is defined as participants requiring intubation (for neurologic deterioration only) at any time between 24 hours and 96 hours post-injury. (NCT03954041)
Timeframe: Day 1 (24 hours) up to Day 4 (96 hours) post-injury

InterventionPercentage of participants (Number)
Placebo2.3
BIIB093 3 mg/Day4.8
BIIB093 5 mg/Day0

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Change From Baseline in Mean Total Contusion Volume (Hematoma Plus Perihematomal Edema) at 96 Hours as Measured by Brain Imaging

Total contusion volume including hematoma and perihematomal edema volumes reported in milliliters (mL) was assessed by the central imaging core laboratory on baseline non-contrast computed tomography (NCCT), 24-hour NCCT, and the 96-hour scan (Magnetic resonance imaging [MRI] and/or NCCT) and the scans obtained prior to decompressive craniectomy (DC), intraparenchymal hematoma (IPH) evacuation, or comfort measures only (CMO). (NCT03954041)
Timeframe: Baseline up to 96 hours (Day 4)

,,
InterventionmL (Mean)
BaselineChange From Baseline at 96 Hours
BIIB093 3 mg/Day21.2130.07
BIIB093 5 mg/Day21.3318.78
Placebo29.4518.91

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Percentage of Participants With Modified Rankin Scale (mRS) Score at Day 90

The mRS measures the degree of functional independence following stroke. In this study, the 7-category ordinal mRS scale was condensed to the following 5-categories: 0/1, 2, 3, 4, 5/6 where 0 and 1 reflect no disability and near-normal functioning while 5 and 6 represent severe disability and death, respectively. (NCT03954041)
Timeframe: Day 90

,,
InterventionPercentage of participants (Number)
Score: 0/1Score: 2Score: 3Score: 4Score: 5/6
BIIB093 3 mg/Day31.626.321.115.85.3
BIIB093 5 mg/Day57.17.1021.414.3
Placebo38.525.612.810.312.8

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Change From Baseline in Mean Total Contusion Volume (Hematoma Plus Perihematomal Edema) at 24 Hours as Measured by Brain Imaging

Total contusion volume including hematoma and perihematomal edema volumes reported in mL was assessed by the central imaging core laboratory on baseline NCCT and 24-hour NCCT. (NCT03954041)
Timeframe: Baseline up to 24 hours (Day 1)

,,
InterventionmL (Mean)
BaselineChange From Baseline at 24 Hours
BIIB093 3 mg/Day21.2111.24
BIIB093 5 mg/Day21.336.67
Placebo29.458.16

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Change From Baseline in Absolute Hematoma Volume at 24 Hours

Hematoma volume reported in mL was assessed by the central imaging core laboratory on baseline NCCT, 24-hour NCCT, and the scans obtained prior to DC, IPH evacuation, or CMO. (NCT03954041)
Timeframe: Baseline up to 24 hours (Day 1)

,,
InterventionmL (Mean)
BaselineChange From Baseline at 24 Hours
BIIB093 3 mg/Day6.112.13
BIIB093 5 mg/Day3.622.23
Placebo6.722.07

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Change From Baseline in Absolute Edema Volume at 96 Hours

Edema volume reported in mL was assessed by the central imaging core laboratory on baseline NCCT, 24-hour NCCT, and the 96-hour scan (MRI and/or NCCT) and the scans obtained prior to DC, IPH evacuation, or CMO. (NCT03954041)
Timeframe: Baseline up to 96 hours (Day 4)

,,
InterventionmL (Mean)
BaselineChange From Baseline at 96 Hours
BIIB093 3 mg/Day15.1025.87
BIIB093 5 mg/Day17.5214.98
Placebo22.4116.13

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Time to All-Cause Death Through Day 90

Time to all-cause death is defined as the time from randomization to the time of death and includes all-cause death along with neurological death. (NCT03954041)
Timeframe: Randomization up to Day 90

Interventiondays (Median)
PlaceboNA
BIIB093 5 mg/DayNA

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