exp3174 profile

losartan carboxylic acid: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	108185
CHEMBL ID	907
CHEBI ID	74125
SCHEMBL ID	179
MeSH ID	M0181329

Synonym
gtpl586
PDSP1_000581
exp-3174
carboxylosartan
124750-92-1
exp 3174
l-158641
1h-imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
e-3174
PDSP2_001437
PDSP2_000578
PDSP1_000580
PDSP1_001453
exp3174
AKOS000280957
chebi:74125 ,
CHEMBL907 ,
L001184
1h-imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-((2'-(2h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
losartan carboxylic acid
FT-0668447
e 3174
bdbm50006909
2-butyl-5-chloro-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid
2-butyl-5-chloro-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid (exp3174)
2-butyl-5-chloro-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid (exp3174)
2-butyl-5-chloro-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-imidazole-4-carboxylic acid
carboxylic acid metabolite (e-3174)
2-butyl-5-chloro-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
2-butyl-4-chloro-1-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-1h-imidazole-5-carboxylic acid
AKOS015917819
FT-0670858
FT-0670859
l 158641
unii-gd76och73x
gd76och73x ,
S5980
e3174
ZEUXAIYYDDCIRX-UHFFFAOYSA-N
SCHEMBL179
allisartan [who-dd]
2-butyl-4-chloro-1-[(2'-(1-h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl)methyl]-1-h-imidazole-5-carboxylic acid
DTXSID80154474
J-005163
EX-A803
1-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1h-imidazole-5-carboxylic acid
2-butyl-4-chloro-1-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-carboxylic acid
mfcd00871928
losartan carboxylic acid [exp3174]
1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-4-chloro-1h-imidazole-5-carboxylic acid
BCP08038
CS-0012367
HY-12765
Q27077270
losartancarboxylicacid
carboxylic acid metabolite
bdbm50230882
1h-imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
losartan carboxylic acid (exp-3174)
1-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1h-imidazole-5-carboxylic acid
A890363
2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-carboxylic acid (losartan carboxylic acid)
2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-carboxylic acid; e 3174; exp 3174; losartan acid; 2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-carboxylic acid
2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-carboxylic acid

Excerpt	Reference	Relevance
"EXP3174 is an active metabolite, which contributes to the overall activity of losartan."	( Simultaneous determination of losartan and EXP3174 in human plasma and urine utilizing liquid chromatography/tandem mass spectrometry. Lo, MW; Polinko, M; Riffel, K; Song, H, 2003)	1.3
"EXP3174 is a metabolite of losartan (previous name DuP753), which is a non-peptide angiotensin II receptor antagonist."	( EXP3174, a metabolite of losartan (MK 954, DuP 753) is more potent than losartan in blocking the angiotensin II-induced responses in vascular smooth muscle cells. Christian, R; Düsing, R; Ko, Y; Meyer zu Brickwedde, MK; Sachinidis, A; Vetter, H; Weisser, P; Wieczorek, AJ, 1993)	3.17
"EXP3174 is a major metabolite generated after the oral dosing of 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H- tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole, potassium salt in rats."	( Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent. Carini, DJ; Chiu, AT; Duncia, JV; Johnson, AL; Price, WA; Timmermans, PB; Wexler, RR; Wong, PC, 1990)	1.24

Excerpt	Reference	Relevance
" The acute pharmacodynamic actions of intravenous (i."	( Pharmacodynamic activity of intravenous E-3174, an angiotensin II antagonist, in patients with essential hypertension. Berman, RS; Bradstreet, DC; Jallard, N; Saenz, A; Sweet, CS; Weidler, DJ, 1994)	0.29
" The mean values of Cmax and AUC0-infinity increased in a dose-dependent manner."	( Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Nakashima, M; Ohtawa, M; Saitoh, K; Takayama, F; Yoshinaga, T, 1993)	0.29
" for 6 days) on the pharmacokinetics and pharmacodynamic effects of the angiotensin II receptor antagonist, losartan (100 mg)."	( Effects of cimetidine on pharmacokinetics and pharmacodynamics of losartan, an AT1-selective non-peptide angiotensin II receptor antagonist. Bradstreet, TE; Goldberg, MR; Höglund, P; Lo, MW; Ritter, MA, 1995)	0.29
" This study indicates a predictable plasma concentration-effect relationship of EXP3174 in rats which would be helpful in designing more rational dosing schemes for pharmacodynamic studies."	( Nonpeptide angiotensin II receptor antagonist: pharmacokinetics and pharmacodynamics in rats of EXP3174, an active metabolite of losartan. Christ, DD; Lam, GN; Wong, PC; Wong, YN, 1996)	0.74
" After concomitant administration with fluconazole, losartan AUC(0-t) and Cmax were significantly increased 66% and 30%, respectively, compared with those values for losartan alone."	( Effect of fluconazole on the pharmacokinetics of eprosartan and losartan in healthy male volunteers. Blum, RA; Boike, SC; Etheredge, R; Ilson, B; Jorkasky, DK; Kazierad, DJ; Martin, DE; Tenero, DM, 1997)	0.3
" The pharmacodynamic activities of losartan and EXP3174 were determined during constant intravenous infusion as the degree of inhibition of angiotensin II-induced increase in the diastolic pressure."	( Pharmacokinetic-pharmacodynamic relations of losartan and EXP3174 in a porcine animal model. Bai, SA; Christ, DD; Hellyer, P; Lankford, SM; Plummer, D, 1997)	0.8
" Significant differences were observed in some of the pharmacokinetic parameters of losartan and its metabolite E3174 after losartan administration with and without co-administered GJ."	( Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers. Avni, B; Dishi, V; Gips, M; Golik, A; Scapa, E; Soback, S; Weissgarten, Y; Zaidenstein, R, 2001)	0.31
"Single-dose pharmacokinetic study."	( Losartan and E3174 pharmacokinetics in cytochrome P450 2C91/1, 1/2, and 1/3 individuals. Blaisdell, JA; Goldstein, JA; Hinderliter, AL; Lee, CR; Pieper, JA, 2003)	0.32
"Plasma and urine samples were collected for 24 hours, and losartan and E3174 pharmacokinetic data were compared across the three genotypes."	( Losartan and E3174 pharmacokinetics in cytochrome P450 2C91/1, 1/2, and 1/3 individuals. Blaisdell, JA; Goldstein, JA; Hinderliter, AL; Lee, CR; Pieper, JA, 2003)	0.32
" Finally, some relevant pharmacokinetics and metabolic properties of the database of 53 compounds are calculated using the VolSurf and MetaSite software to allow the simultaneous characterization of pharmacodynamic and pharmacokinetics properties of the chemical space of angiotensin II receptor antagonists."	( Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists. Berellini, G; Cruciani, G; Mannhold, R, 2005)	0.33
" Under fed conditions, treatment C had no significant effect on the AUC(0-t) and Cmax of losartan and E-3174."	( The effect of AST-120 on the single-dose pharmacokinetics of losartan and losartan acid (E-3174) in healthy subjects. Guilbaud, R; Kambhampati, SR; Lee, J; Marier, JF; Mathew, P; Moberly, J; Salazar, DE, 2006)	0.33
"The pharmacokinetic parameters for losartan and E3174 changed inconsequentially across the range of renal insufficiency."	( The pharmacokinetics of losartan in renal insufficiency. Furtek, CI; Gehr, TW; Halstenson, CE; Keane, WF; Lipschutz, K; Lo, MW; Ritter, MA; Shahinfar, S; Shaw, WC; Sica, DA, 1995)	0.29
" These pharmacokinetic alterations do not warrant dose adjustment in the face of renal insufficiency."	( The pharmacokinetics of losartan in renal insufficiency. Furtek, CI; Gehr, TW; Halstenson, CE; Keane, WF; Lipschutz, K; Lo, MW; Ritter, MA; Shahinfar, S; Shaw, WC; Sica, DA, 1995)	0.29
"To determine whether, when losartan was used in combination with soy extract, a significant pharmacokinetic interaction would be observed in healthy female volunteers."	( Effect of soy extract administration on losartan pharmacokinetics in healthy female volunteers. Chen, Y; Fan, L; Guo, D; Hu, DL; Li, Z; Peng, XJ; Qian, RH; Wang, G; Xiao, CQ; Zhou, HH, 2009)	0.35
" Meanwhile, the CYP2C91/3 genotype group had significant differences in t(1/2) and Cmax of E3174 compared with the CYP2C91/1 group."	( Effects of the CYP2C9*13 allele on the pharmacokinetics of losartan in healthy male subjects. Chen, BL; Fan, L; Hu, DL; Li, Q; Li, Z; Liu, J; Liu, ZQ; Tan, ZR; Tu, JH; Wang, G; Wang, LS; Zhang, W; Zhou, HH, 2009)	0.35
"The pharmacokinetic parameters of losartan and EXP-3174 were determined after oral administration of losartan (9 mg/kg) to rats in the presence or absence of myricetin (0."	( Effects of myricetin, an antioxidant, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats: possible role of cytochrome P450 3A4, cytochrome P450 2C9 and P-glycoprotein inhibition by myricetin. Choi, DH; Choi, JS; Li, C, 2010)	0.36
" The pharmacokinetic parameters of losartan were significantly altered by myricetin compared with the control."	( Effects of myricetin, an antioxidant, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats: possible role of cytochrome P450 3A4, cytochrome P450 2C9 and P-glycoprotein inhibition by myricetin. Choi, DH; Choi, JS; Li, C, 2010)	0.36
" Pharmacokinetic parameters of losartan and EXP-3174 in rats were determined after oral and intravenous administration of losartan (9 mg/kg) without and with HMG-CoA reductase inhibitors (1 mg/kg)."	( Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of losartan and its main metabolite EXP-3174 in rats: possible role of CYP3A4 and P-gp inhibition by HMG-CoA reductase inhibitors. Choi, DH; Choi, JS; Yang, SH, 2011)	0.37
" After normalization by weight, no ethnicity-based difference was noted in the pharmacokinetic parameters of losartan."	( Pharmacokinetics of losartan and its active carboxylic acid metabolite E-3174 in five ethnic populations of China. Guo, T; Xia, DY; Yang, L; Zhao, LS, 2012)	0.38
" CYP2C9 variants were associated only with losartan pharmacokinetics: the half-life of losartan was higher in CYP2C9*3 allele carriers (3."	( Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers. Abad-Santos, F; Cabaleiro, T; López-Rodríguez, R; Novalbos, J; Ochoa, D; Prieto-Pérez, R; Román, M; Talegón, M; Wojnicz, A, 2013)	0.39
" rosea resulted in a statistically significant increase of the following pharmacokinetic parameters for losartan: the maximum plasma concentration (C(max)), the area under the curve (AUC) and the apparent total body clearance (CL/F)."	( Pharmacokinetic interaction between losartan and Rhodiola rosea in rabbits. Batzias, G; Niopas, I; Spanakis, M; Vizirianakis, IS, 2013)	0.39
" rosea significantly alters the pharmacokinetic properties of losartan after concurrent oral administration to rabbits."	( Pharmacokinetic interaction between losartan and Rhodiola rosea in rabbits. Batzias, G; Niopas, I; Spanakis, M; Vizirianakis, IS, 2013)	0.39
" Plasma concentrations of losartan and EXP3174 were determined by LC-MS at designated points after drug administration, and the main pharmacokinetic parameters were estimated."	( Influence of compound danshen tablet on the pharmacokinetics of losartan and its metabolite EXP3174 by liquid chromatography coupled with mass spectrometry. Chai, Y; Ma, W; Sun, S; Wang, B; Yuan, Y; Zhang, G; Zhang, H; Zhao, L, 2013)	0.88
" Meanwhile, the Cmax of amlodipine, losartan and EXP3174 were reduced by 11."	( The influence of food on the pharmacokinetics of amlodipine and losartan after single-dose of its compound tablets in healthy chinese subjects. Guo, R; Li, R; Lv, C; Wang, B; Wang, X; Wei, C; Yao, H, 2014)	0.66
" Pharmacokinetic parameters of losartan and EXP-3174 were determined after oral administration of losartan (9 mg/kg) to rats in the presence or absence of licochalcon A (0."	( Effects of licochalcon A on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats. Choi, DH; Choi, JS, 2013)	0.39
" In this study, the pharmacokinetic (PK) interaction between RG and losartan, an antihypertensive drug, was examined."	( Negligible Pharmacokinetic Interaction of Red Ginseng and Losartan, an Antihypertensive Agent, in Sprague-Dawley Rats. Jang, HJ; Kim, KB; Kim, YS; Ryu, SH, 2015)	0.42
" Male Sprague-Dawley rats were randomly assigned to 3 groups: LST, LST+SA-B and LST+Tan IIA, and the main pharmacokinetic parameters were estimated after oral administration of LST, LST+SA-B and LST+Tan IIA."	( Effects of salvianolic acid B and tanshinone IIA on the pharmacokinetics of losartan in rats by regulating the activities and expression of CYP3A4 and CYP2C9. Wang, R; Wang, Y; Yu, X; Yuan, Y; Zhang, H, 2016)	0.43
" The pharmacokinetic parameters of losartan and its metabolite on the background of 4-day afabazole administration 5 mg/kg dose were not significantly different from analogous values calculated for the control group of rats."	( [EVALUATION OF THE PHARMACOKINETIC INTERACTION OF AFOBAZOLE WITH CYP2C9 ENZYME DRUG SUBSTRATE OF CYTOCHROME P450]. Gribakina, OG; Kolyvanov, GB; Litvin, AA; Shevchenko, RV; Smirnov, VV; Zherdev, VP, 2015)	0.42
" The plasma concentrations of losartan and EXP3174 were determined by LC-MS, and the main pharmacokinetic parameters were calculated."	( The effect of tripterygium glucoside tablet on pharmacokinetics of losartan and its metabolite EXP3174 in rats. Hu, Y; Shi, H; Shi, W; Ye, S; Zhang, H; Zhou, X, 2017)	0.94
" The aim of this study was to develop a population pharmacokinetic model for losartan and its active metabolite (EXP-3174) in order to describe the effect of gastric emptying on their disposition."	( Modelling gastric emptying: A pharmacokinetic model simultaneously describing distribution of losartan and its active metabolite EXP-3174. Karalis, V; Karatza, E, 2020)	0.56

Excerpt	Reference	Relevance
" Although 71 was active orally only at a 10-fold higher dose level, good oral bioavailability was demonstrated for a monoacidic analogue 62."	( Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles. Ashton, WT; Cantone, CL; Chang, LL; Chang, RS; Chen, TB; Faust, KA; Hutchins, SM; Lotti, VJ; MacCoss, M; Strelitz, RA, 1993)	0.29
" The oral bioavailability of losartan tablets was 33%."	( Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Bjornsson, TD; Furtek, CI; Goldberg, MR; Lo, MW; Lu, H; McCrea, JB, 1995)	0.51
" The absolute extent of oral bioavailability of losartan, F, (32."	( Pharmacokinetics of losartan and its metabolite, EXP3174, after intravenous and oral administration of losartan to rats with streptozotocin-induced diabetes mellitus. Baik, EJ; Jung, YS; Lee, HJ; Lee, SH; Moon, CH, 1998)	0.55
"The enhanced bioavailability of losartan may be mainly due to inhibition of the CYP3A4- and CYP2C9-mediated metabolism of losartan in the small intestine or in the liver, and the P-glycoprotein efflux pump in the small intestine by myricetin."	( Effects of myricetin, an antioxidant, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats: possible role of cytochrome P450 3A4, cytochrome P450 2C9 and P-glycoprotein inhibition by myricetin. Choi, DH; Choi, JS; Li, C, 2010)	0.36
" A comparable AUC(0-24h), shortened T(max) and a significant increase in the plasma C(max) of EXP3174 were observed following oral administration of EXP3174-pivoxil (as EXP3174, 1 mg/kg) compared with those of losartan (as EXP3174, 5 mg/kg) in rats, suggesting faster absorption and a 5-fold enhancement in the bioavailability of EXP3174."	( The physicochemical properties, in vitro metabolism and pharmacokinetics of a novel ester prodrug of EXP3174. Choi, HG; Kim, HK; Lee, GS; Lee, WS; Seo, KH; Woo, JS; Yan, YD; Yong, CS, 2010)	0.8
" Consequently, the absolute bioavailability (F) of losartan after oral administration with simvastatin was significantly increased by 59."	( Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of losartan and its main metabolite EXP-3174 in rats: possible role of CYP3A4 and P-gp inhibition by HMG-CoA reductase inhibitors. Choi, DH; Choi, JS; Yang, SH, 2011)	0.37
" Consequently, the absolute bioavailability of losartan in the presence of licochalcon A increased significantly (2."	( Effects of licochalcon A on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats. Choi, DH; Choi, JS, 2013)	0.39
" Losartan carboxylic acid (LCA), the potent AT1 blocker metabolite of losartan, suffers from poor bioavailability and brain access."	( Conjugation to Ascorbic Acid Enhances Brain Availability of Losartan Carboxylic Acid and Protects Against Parkinsonism in Rats. Prusty, S; Sahu, PK; Singh, VK; Subudhi, BB, 2018)	0.48

Excerpt	Relevance	Reference
" The inhibitory effect of EXP3174 (1 mg/kg iv) was not overcome by angiotensin II in the range of doses studied, and the shift to the right of the dose-response curve was nonparallel, suggesting that the blockade was noncompetitive."	( Inhibitory effects of DuP 753 and EXP3174 on responses to angiotensin II in pulmonary vascular bed of the cat. Hood, JS; Kadowitz, PJ; Kaye, AD; McMahon, TJ; Minkes, RK; Nossaman, BD, 1992)	0.86
" EXP3174 is a major metabolite generated after the oral dosing of 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H- tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole, potassium salt in rats."	( Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent. Carini, DJ; Chiu, AT; Duncia, JV; Johnson, AL; Price, WA; Timmermans, PB; Wexler, RR; Wong, PC, 1990)	1.42
"The in vitro protein binding characteristics of the prototypical angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite EXP3174 were determined by ultrafiltration with plasma from naive donors, volunteers dosed with losartan, and purified human plasma proteins."	( Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite EXP3174. Christ, DD, 1995)	0.68
", the blockade was overcome and the dose-response curves for angiotensin II were shifted to the right in a parallel manner."	( Analysis of the inhibitory effects of DuP 753 and EXP 3174 on responses to angiotensin II in the feline hindquarters vascular bed. Bellan, JA; Kadowitz, PJ; Minkes, RK; Osei, SY, 1993)	0.29
" This study indicates a predictable plasma concentration-effect relationship of EXP3174 in rats which would be helpful in designing more rational dosing schemes for pharmacodynamic studies."	( Nonpeptide angiotensin II receptor antagonist: pharmacokinetics and pharmacodynamics in rats of EXP3174, an active metabolite of losartan. Christ, DD; Lam, GN; Wong, PC; Wong, YN, 1996)	0.74
" Serial blood samples were collected over one dosing interval on study days 10 and 20 for measurement of plasma concentrations of eprosartan, losartan, and E-3174 (the active metabolite of losartan)."	( Effect of fluconazole on the pharmacokinetics of eprosartan and losartan in healthy male volunteers. Blum, RA; Boike, SC; Etheredge, R; Ilson, B; Jorkasky, DK; Kazierad, DJ; Martin, DE; Tenero, DM, 1997)	0.3
"The U46619-stimulated platelet aggregation was significantly inhibited by losartan in a dose-response manner."	( [Effect of losartan on human platelet activation by thromboxane A2]. Casado, S; Castilla, C; Farré, J; Gómez, J; Guerra, JI; Jiménez, AM; López-Farré, A; Marcos, P; Montón, M; Núñez, A; Rico, L; Rodríguez-Feo, JA; Sánchez De Miguel, L, 2000)	0.31
" While the biphenyltetrazole compound candesartan dissociated slowly and behaved as an insurmountable antagonist for WT-AT(1), it dissociated swiftly and only produced a rightward shift of the angiotensin Ang II- and -IV dose-response curves for inositol phosphate (IP) accumulation in cells expressing N111G."	( Peptide and nonpeptide antagonist interaction with constitutively active human AT1 receptors. Hunyady, L; Kersemans, V; Le, MT; Szaszák, M; Vanderheyden, PM; Vauquelin, G, 2003)	0.32
" Alterations in losartan dosing in CYP2C91/2 and 1/3 individuals does not appear necessary."	( Losartan and E3174 pharmacokinetics in cytochrome P450 2C91/1, 1/2, and 1/3 individuals. Blaisdell, JA; Goldstein, JA; Hinderliter, AL; Lee, CR; Pieper, JA, 2003)	0.32
" Therefore, administration of AST-120 60 minutes after losartan under fed conditions may be preferred over other dosing regimens for CKD patients."	( The effect of AST-120 on the single-dose pharmacokinetics of losartan and losartan acid (E-3174) in healthy subjects. Guilbaud, R; Kambhampati, SR; Lee, J; Marier, JF; Mathew, P; Moberly, J; Salazar, DE, 2006)	0.33
" In vivo absorption was investigated following regional intestinal dosing in rats, and the pharmacokinetics was determined using rats after a single oral administration."	( The physicochemical properties, in vitro metabolism and pharmacokinetics of a novel ester prodrug of EXP3174. Choi, HG; Kim, HK; Lee, GS; Lee, WS; Seo, KH; Woo, JS; Yan, YD; Yong, CS, 2010)	0.58

Role	Description
metabolite	Any intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
biphenylyltetrazole	A member of the class of biphenyls that consists of a biphenyl ring system substituted by a tetrazole ring at an unspecified position.
imidazoles	A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
organochlorine compound	An organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0013	0.0003	1.3833	8.4000	AID37698
Type-1A angiotensin II receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0027	0.0004	0.1555	3.8000	AID37698; AID37830; AID37836; AID37843; AID37969; AID39505
Type-1A angiotensin II receptor	Rattus norvegicus (Norway rat)	Ki	0.0068	0.0002	0.1025	1.7000	AID37973
Type-1B angiotensin II receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0036	0.0004	0.1334	3.8000	AID37685; AID37698; AID37830; AID37836; AID37843; AID37969; AID39504; AID39505
Type-1B angiotensin II receptor	Rattus norvegicus (Norway rat)	Ki	0.0068	0.0002	0.0521	1.1000	AID37973
Type-1 angiotensin II receptor	Homo sapiens (human)	IC50 (µMol)	0.0020	0.0002	0.0932	3.6000	AID1525517
Type-2 angiotensin II receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	33.3358	0.0010	0.3957	3.3000	AID39505; AID39524; AID39631
5-hydroxytryptamine receptor 1A	Mus musculus (house mouse)	IC50 (µMol)	0.0075	0.0021	0.3581	2.0000	AID39505
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Type-1 angiotensin II receptor	Homo sapiens (human)	Affinity	0.0013	0.0005	0.0315	0.2300	AID243379
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
regulation of cell growth	Type-1 angiotensin II receptor	Homo sapiens (human)
kidney development	Type-1 angiotensin II receptor	Homo sapiens (human)
renin-angiotensin regulation of aldosterone production	Type-1 angiotensin II receptor	Homo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensin	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensin	Type-1 angiotensin II receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Type-1 angiotensin II receptor	Homo sapiens (human)
Rho protein signal transduction	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of macrophage derived foam cell differentiation	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of vasoconstriction	Type-1 angiotensin II receptor	Homo sapiens (human)
calcium-mediated signaling	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of phospholipase A2 activity	Type-1 angiotensin II receptor	Homo sapiens (human)
low-density lipoprotein particle remodeling	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of renal sodium excretion	Type-1 angiotensin II receptor	Homo sapiens (human)
angiotensin-activated signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of cell population proliferation	Type-1 angiotensin II receptor	Homo sapiens (human)
symbiont entry into host cell	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of protein metabolic process	Type-1 angiotensin II receptor	Homo sapiens (human)
cell chemotaxis	Type-1 angiotensin II receptor	Homo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
blood vessel diameter maintenance	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesis	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of CoA-transferase activity	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Type-1 angiotensin II receptor	Homo sapiens (human)
inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
angiotensin type I receptor activity	Type-1 angiotensin II receptor	Homo sapiens (human)
angiotensin type II receptor activity	Type-1 angiotensin II receptor	Homo sapiens (human)
protein binding	Type-1 angiotensin II receptor	Homo sapiens (human)
bradykinin receptor binding	Type-1 angiotensin II receptor	Homo sapiens (human)
protein heterodimerization activity	Type-1 angiotensin II receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
plasma membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (124)

Assay ID	Title	Year	Journal	Article
AID183758	Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 6 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID183748	Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 6 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID1214143	Cmax in human plasma expressing CYP2C8*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214146	AUC in human plasma expressing CYP2C8*4 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214145	Tmax in human plasma expressing CYP2C8*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1487375	Antagonist activity at human AT1 receptor expressed in CHO cells assessed as reduction in angiotensin 2-induced inositol phosphate accumulation by measuring residence time constant preincubated with cells followed by compound washout in presence of losart	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID175105	Time to produce onset of action for inhibition of pressor response in conscious, normotensive rats at 0.1 mg/kg iv (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID247113	Maximal effect produced by the drug in human	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
AID1214097	Half life in human plasma expressing CYP2C9*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214148	Half life in human plasma expressing CYP2C8*4 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37843	Inhibitory concentration against binding of [125I]angiotensin II to rat liver expressing Angiotensin II receptor	1993	Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16	Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID568872	Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID39504	Binding affinity against AT1 receptor in the presence of 0.01% BSA	1994	Journal of medicinal chemistry, May-27, Volume: 37, Issue:11	Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID175107	Time to produce onset of action for inhibition of pressor response in conscious, normotensive rats at 0.3 mg/kg po (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID1214141	Tmax in human plasma expressing CYP2C81/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37685	Concentration required to inhibit binding of radioligand [125I]AII to Angiotensin II receptor, type 1 in rat adrenal glomerulosa tissue	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1- yl]phenyl]methyl]imidazole derivatives and their in vitro activity.
AID174246	% decrease in blood pressure after 4 hours at a dose of 10 mg/kg in male rats by using Renal artery hypertensive model	1993	Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18	2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID183757	Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 3 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID568873	Antihypertensive activity in iv dosed renal artery ligated rat model assessed as reduction of means arterial blood pressure by 30 mm Hg	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID1214208	AUC in human plasma expressing CYP2C81/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214215	Cmax in women plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID39641	In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID37542	Potency to antagonize the ability of angiotensin II to contract rabbit aorta	1993	Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18	2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
AID183747	Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 3 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID568874	Antihypertensive activity in po dosed renal artery ligated rat model assessed as reduction of means arterial blood pressure by 30 mm Hg	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID1214218	Tmax in men plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID194619	Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 1 mg/Kg p.o.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID1214216	Half life in men plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID39801	Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID568790	Displacement of radiolabeled angiotensin2 from angiotensin AT1 receptor in rat adrenal cortex membranes	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID182953	In vivo inhibitory activity against angiotensin II induced pressor response in anesthetized normotensive rats	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID183749	Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 1 hr	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID39503	In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta	1994	Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24	A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID239885	pKa value against human Angiotensin II receptor type 1	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
AID177200	Intravenous effective dose required for lowering blood pressure in renal hypertensive rats (RHR)	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID29138	Acid dissociation value was evaluated	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1214219	Tmax in women plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID185598	Percent peak inhibition of pressor response induced by exogenously administered AII at 1 mg/kg in 2 or more pithed rats.	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Synthesis and structure-activity relationship of a new series of potent AT1 selective angiotensin II receptor antagonists: 5-(biphenyl-4-ylmethyl)pyrazoles.
AID1214142	AUC in human plasma expressing CYP2C8*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37698	Inhibitory concentration that gives 50% displacement of specific binding at labeled angiotensin II type 1 receptor in rat adrenal cortical membranes.	2003	Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5	Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.
AID165371	Inhibitory concentration against [125I]angiotensin II(AII) induced contraction in rabbit aorta by 50%	1993	Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16	Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID1216814	Metabolic activation assessed as CYP2C9 activation-induced cytotoxicity in human HepG2 cells transfected with human AdCYP2C9 at MOI 10 for 2 days in presence of siNrf2 at 25 to 100 uM after 24 hrs by WST-8 assay	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	CYP2C9-mediated metabolic activation of losartan detected by a highly sensitive cell-based screening assay.
AID39809	Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID183746	Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 1 hr	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID1214217	Half life in women plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID184384	Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 0.3 mg/kg iv (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID193882	Effect on mean arterial pressure after oral dosing at 10 mg/kg to renal hypertensive rats	1993	Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16	Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID18415	Oral bioavailability in rat	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID263158	Antagonist activity against AT1 receptor after 60 min preincubation	2006	Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8	New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: design, synthesis, and biopharmacological properties.
AID194768	Peak inhibition of A II pressor response in conscious normotensive rats after peroral administration of 0.3 mg/kg of drug (2 animals treated)	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID1214147	Cmax in human plasma expressing CYP2C8*4 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214149	Tmax in human plasma expressing CYP2C8*4 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214079	Cmax in human plasma expressing CYP2C9*2 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID179987	Tested in vivo for effective dose (iv) that produces inhibition of pressor response to Angiotensin II in conscious normotensive rats	1993	Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16	Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID193072	Duration of inhibition of AII pressor response no longer observed in conscious normotensive rats at 0.3 mg/Kg i.v.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID1214144	Half life in human plasma expressing CYP2C8*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214077	Tmax in human plasma expressing CYP2C91/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID193086	Time from onset of action until significant (i.e., >= 30%) inhibition of pressor response no longer observed (0.3 mg/kg intravenous route)	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID184380	Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 0.1 mg/kg iv (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID39505	Binding affinity against AT1 receptor of rat adrenal cortical membranes	1994	Journal of medicinal chemistry, May-27, Volume: 37, Issue:11	Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID243379	Binding affinity for AT1 receptor	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
AID1487363	Antagonist activity at human AT1 receptor expressed in CHO cells assessed as reduction in angiotensin 2-induced inositol phosphate accumulation by measuring dissociation rate constant preincubated with cells followed by compound washout and subsequent add	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID1487365	Displacement of [3H]-candesartan from human AT1 receptor expressed in CHO cells assessed as dissociation rate constant at 5 nM pre-incubated with cells followed by compound washout and subsequent addition of [3H]-candesartan up to 60 mins	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID175106	Time to produce onset of action for inhibition of pressor response in conscious, normotensive rats at 0.3 mg/kg iv (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID1214096	Cmax in human plasma expressing CYP2C9*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1487374	Antagonist activity at human AT1 receptor expressed in CHO cells assessed as reduction in angiotensin 2-induced inositol phosphate accumulation by measuring residence time constant preincubated with cells followed by compound washout and subsequent additi	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID193088	Time from onset of action until significant (i.e., >= 30%) inhibition of pressor response no longer observed (0.3 mg/kg peroral route).	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID39047	Inhibition of Angiotensin II induced contractions in rabbit aortic rings	1994	Journal of medicinal chemistry, May-27, Volume: 37, Issue:11	Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID23693	Partition coefficient (logP)	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1- yl]phenyl]methyl]imidazole derivatives and their in vitro activity.
AID1487377	Displacement of [3H]-candesartan from human AT1 receptor expressed in CHO cells assessed as residence time at 5 nM pre-incubated with cells followed by compound washout and subsequent addition of [3H]-candesartan up to 60 mins	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID263157	Antagonist activity against AT1 receptor after 20 min preincubation	2006	Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8	New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: design, synthesis, and biopharmacological properties.
AID183750	Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 3 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID1214212	AUC in men plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID231453	Ratio between +BSA and -BSA was determined	1994	Journal of medicinal chemistry, May-27, Volume: 37, Issue:11	Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
AID39810	In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID39524	In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain	1994	Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24	A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
AID37830	In vitro binding affinity for rat liver angiotensin II receptor type 1, determined by displacement of the specially bound [3H]AII radioligand	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Synthesis and structure-activity relationship of a new series of potent AT1 selective angiotensin II receptor antagonists: 5-(biphenyl-4-ylmethyl)pyrazoles.
AID183751	Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 6 hour	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID167381	Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID39652	Inhibition against Angiotensin II receptor, type 1	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1214209	Cmax in human plasma expressing CYP2C81/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID167384	pA2 value was determined by the compound's ability to antagonize the AII-induced contraction of rabbit aorta rings.	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1- yl]phenyl]methyl]imidazole derivatives and their in vitro activity.
AID27862	Total clearance value was evaluated	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID39498	In vitro inhibitory activity against angiotensin II rabbit aorta AT1 receptor using radioligand [125I]-Sar Ile-AII	1994	Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17	Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.
AID194618	Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 0.3 mg/Kg i.v.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID183756	Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 1 hr	1996	Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1	Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
AID1214098	Tmax in human plasma expressing CYP2C9*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID169539	Maximum fall in blood pressure in groups of four sodium-depleted rats, after peroral administration; Not tested	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Synthesis and structure-activity relationship of a new series of potent AT1 selective angiotensin II receptor antagonists: 5-(biphenyl-4-ylmethyl)pyrazoles.
AID193073	Duration of inhibition of AII pressor response no longer observed in conscious normotensive rats at 1 mg/Kg p.o.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID184389	Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 0.3 mg/kg po (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID177204	Oral effective dose required for lowering blood pressure in renal hypertensive rats (RHR)	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID1214150	AUC in human plasma expressing CYP2C91/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214213	AUC in women plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214095	AUC in human plasma expressing CYP2C9*3 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID39791	Relative binding affinity of compound to Angiotensin II receptor, type 1 was determined	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID219836	Inhibition of bovine cAMP phosphodiesterase	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID175109	Time to produce onset of action for inhibition of pressor response in conscious, normotensive rats at 1 mg/kg po (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID193093	Time from onset of action until significant (i.e., >= 30%) inhibition of pressor response no longer observed (1 mg/kg peroral route)	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID23918	Renal clearance value was evaluated	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1214225	Half life in human plasma expressing CYP2C81/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214078	AUC in human plasma expressing CYP2C9*2 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214152	Half life in human plasma expressing CYP2C91/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37690	In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta Angiotensin II receptor, type 1	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID647625	Antioxidant activity assessed as trolox equivalent of ABTS radical scavenging activity relative to control	2012	European journal of medicinal chemistry, Apr, Volume: 50	New losartan-hydrocaffeic acid hybrids as antihypertensive-antioxidant dual drugs: Ester, amide and amine linkers.
AID568871	Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response relative to control	2010	Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24	Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID1487362	Antagonist activity at human AT1 receptor expressed in CHO cells assessed as reduction in angiotensin 2-induced inositol phosphate accumulation by measuring dissociation rate constant preincubated with cells followed by compound washout in presence of los	2017	Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16	Influence of the cellular environment on ligand binding kinetics at membrane-bound targets.
AID27037	Half life of compound was determined	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID1525517	Inhibition of ATR1 (unknown origin)	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Hydroxyl Groups in Synthetic and Natural-Product-Derived Therapeutics: A Perspective on a Common Functional Group.
AID28322	Peak concentration of compound was blunted in cAMP-mediated signaling	2003	Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12	Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
AID184394	Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 1 mg/kg po (no. of animals treated)	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
AID194770	Peak inhibition of A II pressor response in conscious normotensive rats after peroral administration of 1 mg/kg of drug (2 animals treated)	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID1214214	Cmax in men plasma treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214151	Cmax in human plasma expressing CYP2C91/1 polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID1214093	Half life in human plasma expressing CYP2C9*2 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37836	Inhibitory activity against Angiotensin II receptor, type 1 in rat adrenal cortical microsomes	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID39631	In vitro inhibitory activity against angiotensin II rat midbrain AT2 receptor using radioligand [125I]-Sar Ile-AII	1994	Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17	Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.
AID237099	Time required for elimination of 50% of the compound	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Pharmacophore, drug metabolism, and pharmacokinetics models on non-peptide AT1, AT2, and AT1/AT2 angiotensin II receptor antagonists.
AID1214094	Tmax in human plasma expressing CYP2C9*2 allele carrier polymorphism treated with losartan at 50 mg by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
AID37969	Tested for inhibitory concentration against AT1 receptor binding affinity in rat liver	1993	Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16	Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoro
AID37973	Displacement of [3H]angiotensin II from Angiotensin II type 1 receptor in rat adrenal cortical membrane	1995	Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24	N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID39812	In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID194762	Peak inhibition of A II pressor response in conscious normotensive rats after intravenous administration of 0.3 mg/kg of drug (2 animals treated)	1993	Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5	Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
AID1346995	Human AT1 receptor (Angiotensin receptors)	1993	Pharmacological reviews, Jun, Volume: 45, Issue:2	Angiotensin II receptors and angiotensin II receptor antagonists.
AID1346995	Human AT1 receptor (Angiotensin receptors)	1999	British journal of pharmacology, Feb, Volume: 126, Issue:4	Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	118 (51.30)	18.2507
2000's	63 (27.39)	29.6817
2010's	40 (17.39)	24.3611
2020's	9 (3.91)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	29 (12.29%)	5.53%
Reviews	14 (5.93%)	6.00%
Case Studies	1 (0.42%)	4.05%
Observational	1 (0.42%)	0.25%
Other	191 (80.93%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
protocatechuic acid protocatechuic acid: RN given refers to parent cpd; structure. 3,4-dihydroxybenzoic acid : A dihydroxybenzoic acid in which the hydroxy groups are located at positions 3 and 4.	2.07	1	0	catechols; dihydroxybenzoic acid	antineoplastic agent; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor; human xenobiotic metabolite; plant metabolite
adenine [no description available]	2.02	1	0	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
quinacrine Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.	1.98	1	0	acridines; aromatic ether; organochlorine compound; tertiary amino compound	antimalarial; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
cytosine [no description available]	2.02	1	0	aminopyrimidine; pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
glycine [no description available]	1.99	1	0	alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid	EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical
histamine [no description available]	1.98	1	0	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
uric acid Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.	4.35	4	1	uric acid	Escherichia coli metabolite; human metabolite; mouse metabolite
urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.	2.46	2	0	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
2,4-dinitrophenol 2,4-Dinitrophenol: A toxic dye, chemically related to trinitrophenol (picric acid), used in biochemical studies of oxidative processes where it uncouples oxidative phosphorylation. It is also used as a metabolic stimulant. (Stedman, 26th ed). dinitrophenol : Members of the class of nitrophenol carrying two nitro substituents.. 2,4-dinitrophenol : A dinitrophenol having the nitro groups at the 2- and 4-positions.	2	1	0	dinitrophenol	allergen; antiseptic drug; bacterial xenobiotic metabolite; geroprotector; oxidative phosphorylation inhibitor
theophylline [no description available]	2.48	2	0	dimethylxanthine	adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent
amlodipine Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.	2.1	1	0	dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound	antihypertensive agent; calcium channel blocker; vasodilator agent
benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.	2.06	1	0	1-benzofurans; aromatic ketone	uricosuric drug
bisindolylmaleimide i bisindolylmaleimide I: a bis(indolyl)maleimide	2.13	1	0
caffeine [no description available]	2.48	2	0	purine alkaloid; trimethylxanthine	adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	1.98	1	0	aromatic ether; nitrile; polyether; tertiary amino compound
candesartan cilexetil candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects	5.59	7	0	biphenyls
candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.	7.05	27	0	benzimidazolecarboxylic acid; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.	3.37	1	1	aliphatic sulfide; guanidines; imidazoles; nitrile	adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor
4-cresol 4-cresol: RN given refers to parent cpd. p-cresol : A cresol that consists of toluene substituted by a hydroxy group at position 4. It is a metabolite of aromatic amino acid metabolism produced by intestinal microflora in humans and animals.	2.05	1	0	cresol	Escherichia coli metabolite; human metabolite; uremic toxin
valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.	3.84	2	1	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent
fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.	3.51	1	1	piperidines; tertiary amine	anti-allergic agent; H1-receptor antagonist
fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.	4.34	2	2	conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug	environmental contaminant; P450 inhibitor; xenobiotic
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	3.41	1	1	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.	2.06	1	0	(trifluoromethyl)benzenes; monocarboxylic acid amide	androgen antagonist; antineoplastic agent
furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.	3.08	5	0	chlorobenzoic acid; furans; sulfonamide	environmental contaminant; loop diuretic; xenobiotic
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	3.66	2	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.	7.03	1	0	benzothiadiazine; organochlorine compound; sulfonamide	antihypertensive agent; diuretic; environmental contaminant; xenobiotic
hydroflumethiazide Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide.	2.05	1	0	benzothiadiazine; thiazide	antihypertensive agent; diuretic
indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.	2.6	1	0	indoles; organochlorine compound; sulfonamide	antihypertensive agent; diuretic
indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.	2.68	3	0	aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole	analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	10.07	22	1	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position	16.3	227	29	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
mecamylamine Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.	1.98	1	0	primary aliphatic amine
midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	2.08	1	0	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	2.48	2	0	aromatic ether; benzimidazoles; pyridines; sulfoxide
1,7-dimethylxanthine 1,7-dimethylxanthine : A dimethylxanthine having the two methyl groups located at positions 1 and 7. It is a metabolite of caffeine and theobromine in animals.	2.48	2	0	dimethylxanthine	central nervous system stimulant; human blood serum metabolite; human xenobiotic metabolite; mouse metabolite
phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.	3.37	1	1	barbiturates	anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative
ono 1078 pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist	2.03	1	0	chromones
propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.	2	1	0	naphthalenes; propanolamine; secondary amine	anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic
ro 31-8220 Ro 31-8220: a protein kinase C inhibitor	1.99	1	0	imidothiocarbamic ester; indoles; maleimides	EC 2.7.11.13 (protein kinase C) inhibitor
spiperone Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.	3.25	1	0	aromatic ketone; azaspiro compound; organofluorine compound; piperidines; tertiary amino compound	alpha-adrenergic antagonist; antipsychotic agent; dopaminergic antagonist; psychotropic drug; serotonergic antagonist
terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.	3.51	1	1	diarylmethane
ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.	7.06	1	0	monochlorobenzenes; thienopyridine	anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor
ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist	2.03	1	0	carbamate ester; indoles; N-sulfonylcarboxamide	anti-asthmatic agent; leukotriene antagonist
zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.	2.06	1	0	imidazopyridine	central nervous system depressant; GABA agonist; sedative
reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.	1.98	1	0	alkaloid ester; methyl ester; yohimban alkaloid	adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.68	3	0	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
aldosterone [no description available]	4.84	4	2	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite
estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.	2.03	1	0	17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols	antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	2.44	2	0	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
aspartic acid Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.	2.01	1	0	aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; mouse metabolite; neurotransmitter
adenosine diphosphate Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.	2	1	0	adenosine 5'-phosphate; purine ribonucleoside 5'-diphosphate	fundamental metabolite; human metabolite
tyrosine Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.	2.39	2	0	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; proteinogenic amino acid; tyrosine	EC 1.3.1.43 (arogenate dehydrogenase) inhibitor; fundamental metabolite; micronutrient; nutraceutical
leucine Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.	1.99	1	0	amino acid zwitterion; L-alpha-amino acid; leucine; proteinogenic amino acid; pyruvate family amino acid	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite
colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.	2.11	1	0	alkaloid; colchicine	anti-inflammatory agent; gout suppressant; mutagen
valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.	7.42	15	0	L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
threonine Threonine: An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.. threonine : An alpha-amino acid in which one of the hydrogens attached to the alpha-carbon of glycine is substituted by a 1-hydroxyethyl group.	2.05	1	0	amino acid zwitterion; aspartate family amino acid; L-alpha-amino acid; proteinogenic amino acid; threonine	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	6.59	9	1	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
vanillic acid Vanillic Acid: A flavoring agent. It is the intermediate product in the two-step bioconversion of ferulic acid to vanillin. (J Biotechnol 1996;50(2-3):107-13).. vanillic acid : A monohydroxybenzoic acid that is 4-hydroxybenzoic acid substituted by a methoxy group at position 3.	2.07	1	0	methoxybenzoic acid; monohydroxybenzoic acid	plant metabolite
thiazoles [no description available]	3.81	2	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
thiazolidines Thiazolidines: Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES.	3.81	2	0	thiazolidine
syringic acid syringic acid: RN given refers to parent cpd; structure in third source. syringic acid : A dimethoxybenzene that is 3,5-dimethyl ether derivative of gallic acid.	2.07	1	0	benzoic acids; dimethoxybenzene; phenols	plant metabolite
alpha-naphthoflavone alpha-naphthoflavone: inhibits P4501A1 and P4501A2; stimulates some activities of P4503A4. alpha-naphthoflavone : An extended flavonoid resulting from the formal fusion of a benzene ring with the h side of flavone. A synthetic compound, it is an inhibitor of aromatase (EC 1.14.14.14).	1.98	1	0	extended flavonoid; naphtho-gamma-pyrone; organic heterotricyclic compound	aryl hydrocarbon receptor agonist; aryl hydrocarbon receptor antagonist; EC 1.14.14.14 (aromatase) inhibitor
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	1.99	1	0	cyclic ketone; erythromycin
3,5-di-tert-butyl-4-hydroxybenzoic acid [no description available]	2.07	1	0
tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.	1.98	1	0	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator
phosphotyrosine Phosphotyrosine: An amino acid that occurs in endogenous proteins. Tyrosine phosphorylation and dephosphorylation plays a role in cellular signal transduction and possibly in cell growth control and carcinogenesis.. O(4)-phospho-L-tyrosine : A non-proteinogenic L-alpha-amino acid that is L-tyrosine phosphorylated at the phenolic hydroxy group.	1.98	1	0	L-tyrosine derivative; non-proteinogenic L-alpha-amino acid; O(4)-phosphotyrosine	Escherichia coli metabolite; immunogen
phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.	2.03	1	0	benzenes; phenyl acetates
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.13	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
substance p [no description available]	1.98	1	0	peptide	neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent
ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis.	2.06	1	0	aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes	antihypertensive agent; hepatotoxic agent; loop diuretic
ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.	2.42	2	0	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor
captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.	3.87	12	0	alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).	2.06	1	0	delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring)	anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug
simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.	2.06	1	0	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug
itraconazole Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.	4.38	2	2	aromatic ether; conazole antifungal drug; cyclic ketal; dichlorobenzene; dioxolane; N-arylpiperazine; triazole antifungal drug; triazoles	EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; Hedgehog signaling pathway inhibitor; P450 inhibitor
cilazapril, anhydrous Cilazapril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.. cilazapril : A pyridazinodiazepine resulting from the formal condensation of the carboxy group of cilazaprilat with ethanol. It is a drug used in the treatment of hypertension and heart failure.	1.98	1	0	dicarboxylic acid monoester; ethyl ester; pyridazinodiazepine	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug
dup 532 DuP 532: angiotensin I receptor antagonist	5.19	6	0
valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.	8.46	23	0	biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
tasosartan tasosartan: angiotensin II antagonist; structure given in first source	4.88	4	0	biphenyls
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	2.15	1	0	D-glucopyranose	epitope; mouse metabolite
terlakiren terlakiren: RN given for (R-(R,S))-isomer	1.99	1	0	peptide
telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.	8.61	12	1	benzimidazoles; biphenyls; carboxybiphenyl	angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic
gr 117289 GR 117289: angiotensin AT1 receptor antagonist; structure given in first source. zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).	4.31	3	0	1-benzofurans; biaryl; imidazolyl carboxylic acid; monocarboxylic acid; organobromine compound; organochlorine compound; tetrazoles	angiotensin receptor antagonist; antihypertensive agent
rosiglitazone [no description available]	3.81	2	0	aminopyridine; thiazolidinediones	EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug
coenzyme a [no description available]	2	1	0	adenosine 3',5'-bisphosphate	coenzyme; Escherichia coli metabolite; mouse metabolite
cp 96345 CP 96345: structure given in first source; potent nonpeptide antagonist of the substance P (NK1) receptor; CP 96344 is enantiomer of CP 96345	1.98	1	0
fpl 55712 FPL 55712: inhibitor of SRS-A and LTC4 and LTD4 receptors	1.98	1	0	aromatic ketone
1-hydroxymethylmidazolam 1-hydroxymethylmidazolam: metabolite of midazolam. 1-hydroxymidazolam : An imidazobenzodiazepine that is midazolam in which one of the hydrogens of the methyl group is substituted by a hydroxy group. It is the major metabolite of the anesthetic, midazolam.	2.08	1	0	aromatic primary alcohol; imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	drug metabolite; human blood serum metabolite; human urinary metabolite
hydroxyitraconazole hydroxyitraconazole: a hydroxylated metabolite of itraconazole; likely contributes importantly to the in vivo activity attributed to itraconazole	3.51	1	1
pd 123177 PD 123177: nonpeptide angiotensin AII-2 inhibitor	3.49	8	0	diarylmethane
tanshinone tanshinone: from root of Salvia miltiorrhiza Bunge; RN given refers to tanshinone I; cardioprotective agent and neuroprotective agent	2.13	1	0	abietane diterpenoid	anticoronaviral agent
5-hydroxymethylomeprazole 5-hydroxymethylomeprazole: metabolite of omeprazole. 5'-hydroxyomeprazole : A sulfoxide that is omeprazole in which one of the methyl hydrogens at position 5 on the pyridine ring is substituted by a hydroxy group.	2.07	1	0	aromatic ether; benzimidazoles; pyridines; sulfoxide	drug metabolite
l 692429 L 692429: stimulates release of growth hormone; RN refers to (R)-isomer; structure given in first source	3.11	1	0
cgp 42112a CGP 42112A: a hexapeptide analog of angiotensin II; activation of Receptor, Angiotensin, Type 2 results in vasodilation. CGP-42112A : A hexapeptide consisting of L-tyrosine, L-lysine, L-histidine, L-proline and L-isoleucine amino acid residues coupled in sequence and in which the amino group of the L-tyrosyl residue is substituted by a (pyridin-3-ylcarbonyl)nitrilo group and in which the L-lysyl side chain amino group is substituted by a {N(2)-[(benzyloxy)carbonyl]-L-arginyl}nitrilo group. It is a potent angiotensin II receptor type 2 (AT2 receptor) agonist.	2.68	3	0	benzyl ester; oligopeptide; pyridinecarboxamide	angiotensin receptor agonist; anti-inflammatory agent; antineoplastic agent; neuroprotective agent; vasodilator agent
angiotensin ii, des-phe(8)- Ile(5)-angiotensin II (1-7) : An angiotensin compound consisting of the linear heptapeptide sequence L-Asp-L-Arg-L-Val-L-Tyr-L-Ile-L-His-L-Pro.	2.7	3	0	amino acid zwitterion; angiotensin	vasodilator agent
wl 19 WL 19: structure given in first source; angiotensin II type 2 receptor antagoinst	1.98	1	0
exp7711 EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source	4.34	6	0
olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.	2.01	1	0	biphenyls
bibs 39 BIBS 39: structure given in first source; angiotensin II receptor antagonist	3.09	1	0
sc 51316 SC 51316: structure given in first source; an angiotensin II receptor antagonist	3.51	2	0
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3h-imidazo(4,5-b)pyridine 3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3H-imidazo(4,5-b)pyridine: a non-peptide angiotensin II-receptor antagonist; structure given in first source	4.03	2	0
a 81988 A 81988: angiotensin II antagonist selective for type 1 receptors	4.3	3	0
bibs 222 BIBS 222: structure given in first source; angiotensin II receptor antagonist	3.09	1	0
ici d8731 ICI D8731: structure given in first source; an angiotensin II receptor antagonist	4.64	3	0
forasartan forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure. forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.	4.64	3	0	benzenes; pyridines; tetrazoles; triazoles	angiotensin receptor antagonist; antihypertensive agent
up 269-6 UP 269-6: structure given in first source; angiotensin receptor antagonist	5.91	4	1
omega-n-methylarginine omega-N-Methylarginine: A competitive inhibitor of nitric oxide synthetase.. N(omega)-methyl-L-arginine : A L-arginine derivative with a N(omega)-methyl substituent.	2	1	0	amino acid zwitterion; arginine derivative; guanidines; L-arginine derivative; non-proteinogenic L-alpha-amino acid
embusartan [no description available]	2	1	0
mk 996 MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source	4.3	3	0
olmesartan olmesartan: an active metabolite of CS 866	4.06	4	0	biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	10.93	98	7	amino acid zwitterion; angiotensin II	human metabolite
me 3221 ME 3221: an angiotensin II receptor antagonist; structure given in first source	4.3	3	0
l 158809 L 158809: RN & structure given in first source; angiotensin receptor antagonist	5.64	10	0
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	2.13	1	0
3,4-dihydroxyphenylpropionic acid 3,4-dihydroxyphenylpropionic acid: metabolite of caffeic acid; RN given refers to parent cpd; structure. 3-(3,4-dihydroxyphenyl)propanoic acid : A monocarboxylic acid that is 3-phenylpropionic acid substituted by hydroxy groups at positions 3 and 4. Also known as dihydrocaffeic acid, it is a metabolite of caffeic acid and exhibits antioxidant activity.	2.07	1	0	(dihydroxyphenyl)propanoic acid	antioxidant; human xenobiotic metabolite
dihydropyridines Dihydropyridines: Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.	2	1	0
bradykinin [no description available]	2.68	3	0	oligopeptide	human blood serum metabolite; vasodilator agent
inositol 1,4,5-trisphosphate Inositol 1,4,5-Trisphosphate: Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin.	2.02	1	0	myo-inositol trisphosphate	mouse metabolite
nitroarginine Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.	1.99	1	0	guanidines; L-arginine derivative; N-nitro compound; non-proteinogenic L-alpha-amino acid
indican [no description available]	2.05	1	0	beta-D-glucoside; exopolysaccharide; indolyl carbohydrate
arachidonic acid icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.	3.39	1	1	icosa-5,8,11,14-tetraenoic acid; long-chain fatty acid; omega-6 fatty acid	Daphnia galeata metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; human metabolite; mouse metabolite
3-hydroxy-3-methylglutaryl-coenzyme a 3-hydroxy-3-methylglutaryl-coenzyme A: RN given refers to cpd without isomeric designation. 3-hydroxy-3-methylglutaryl-CoA : An alpha,omega dicarboxyacyl-CoA that results from the formal condensation of the thiol group of coenzyme A with one of the carboxy groups of 3-hydroxy-3-methylglutaric acid.. (3S)-3-hydroxy-3-methylglutaryl-CoA : A 3-hydroxy-3-methylglutaryl-CoA where the 3-hydroxy-3-methylglutaryl component has (S)-configuration.	2.06	1	0	3-hydroxy-3-methylglutaryl-CoA; 3-hydroxy fatty acyl-CoA	human metabolite; mouse metabolite
thapsigargin Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.	2.02	1	0	butyrate ester; organic heterotricyclic compound; sesquiterpene lactone	calcium channel blocker; EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
caffeic acid trans-caffeic acid : The trans-isomer of caffeic acid.	2.07	1	0	caffeic acid	geroprotector; mouse metabolite
curcumin Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.	7.07	1	0	aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol	anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger
terbinafine [no description available]	2.06	1	0	acetylenic compound; allylamine antifungal drug; enyne; naphthalenes; tertiary amine	EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor; sterol biosynthesis inhibitor
nadp [no description available]	1.98	1	0
estrone sulfate estrone sulfate: sulfoconjugated estrone; RN given refers to parent cpd	2.03	1	0	17-oxo steroid; steroid sulfate	human metabolite; mouse metabolite
cv 11194 CV 11194: structure given in first source; an angiotensin II receptor antagonist	3.15	1	0
raclopride Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.	3.25	1	0	salicylamides
milfasartan milfasartan: angiotensin I receptor antagonist; structure in first source	4.3	3	0
dmp 811 DMP 811: angiotensin II receptor antagonist; structure given in first source	4.31	3	0
sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.	3.25	1	0	triazolopyrazine; trifluorobenzene	EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic
rhodamine 123 Rhodamine 123: A fluorescent probe with low toxicity which is a potent substrate for ATP BINDING CASSETTE TRANSPORTER, SUBFAMILY B, MEMBER 1 and the bacterial multidrug efflux transporter. It is used to assess mitochondrial bioenergetics in living cells and to measure the efflux activity of ATP BINDING CASSETTE TRANSPORTER, SUBFAMILY B, MEMBER 1 in both normal and malignant cells. (Leukemia 1997;11(7):1124-30). rhodamine 123(1+) : A cationic fluorescent dye derived from 9-phenylxanthene.	2.48	2	0	organic cation; xanthene dye	fluorochrome
dinoprost Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.	3.39	1	1	monocarboxylic acid; prostaglandins Falpha	human metabolite; mouse metabolite
arachidonyltrifluoromethane arachidonyltrifluoromethane: structure given in first source; inhibits 85-kDa phospholipase A2. AACOCF3 : A fatty acid derivative that is arachidonic acid in which the OH part of the carboxy group has been replaced by a trifluoromethyl group	2	1	0	fatty acid derivative; ketone; olefinic compound; organofluorine compound	EC 3.1.1.4 (phospholipase A2) inhibitor
11-cis-retinal Rhodopsin: A purplish-red, light-sensitive pigment found in RETINAL ROD CELLS of most vertebrates. It is a complex consisting of a molecule of ROD OPSIN and a molecule of 11-cis retinal (RETINALDEHYDE). Rhodopsin exhibits peak absorption wavelength at about 500 nm.. 11-cis-retinal : A retinal having 2E,4Z,6E,8E-double bond geometry.	2.03	1	0	retinal	chromophore; human metabolite; mouse metabolite
thromboxane a2 Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).. thromboxane A2 : A thromboxane which is produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.	4.49	5	1	epoxy monocarboxylic acid; thromboxanes A	mouse metabolite
6-ketoprostaglandin f1 alpha 6-Ketoprostaglandin F1 alpha: The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.. 6-oxoprostaglandin F1alpha : A prostaglandin Falpha that is prostaglandin F1alpha bearing a keto substituent at the 6-position.	1.99	1	0	prostaglandins Falpha	human metabolite; mouse metabolite
eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.	7.66	12	1	dicarboxylic acid; imidazoles; thiophenes	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
montelukast montelukast: a leukotriene D4 receptor antagonist	2.03	1	0	aliphatic sulfide; monocarboxylic acid; quinolines	anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist
pd 123319 PD123319 : An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectively	8.94	13	0	imidazopyridine	angiotensin receptor antagonist; endothelin receptor antagonist; vasoconstrictor agent
exp 655 [no description available]	3.09	1	0
licochalcone a licochalcone A: has both anti-inflammatory and antineoplastic activities; structure given in first source; isolated from root of Glycyrrhiza inflata; RN given refers to (E)-isomer	2.08	1	0	chalcones
ag-490 [no description available]	1.99	1	0	catechols; enamide; monocarboxylic acid amide; nitrile; secondary carboxamide	anti-inflammatory agent; antioxidant; apoptosis inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector; STAT3 inhibitor
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.	2.06	1	0	dihydroxy monocarboxylic acid; indoles; organofluorine compound
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid: A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)	2.92	4	0
ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.	1.98	1	0	azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester	bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug
enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).	2	1	0	dicarboxylic acid monoester; dipeptide	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug
enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.	3.24	6	0	dicarboxylic acid; dipeptide	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ramiprilat ramiprilat : A dipeptide that is the active metabolite of ramipril. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.	1.98	1	0	azabicycloalkane; cyclopentapyrrole; dicarboxylic acid; dipeptide	bradykinin receptor B2 agonist; cardioprotective agent; drug metabolite; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor
ro 42-5892 remikiren : An L-histidine derivative that is L-histidine in which one of the amino hydrogens is replaced by a (2S)-2-[(2-methylpropane-2-sulfonyl)methyl]-3-phenylpropanoyl group and the carboxy group is replaced by a [(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]amino group. It is a renin inhibitor which was under development for the treatment of hypertension (now discontinued).	1.98	1	0	cyclopropanes; diol; L-histidine derivative; secondary carboxamide; sulfone	antihypertensive agent; EC 3.4.23.15 (renin) inhibitor; peptidomimetic; vasodilator agent
saralasin Saralasin: An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.	3.08	5	0	oligopeptide
1-oleoyl-2-acetylglycerol [no description available]	2.13	1	0	1,2-diglyceride
salvianolic acid B salvianolic acid B: isolated from Salvia miltiorrhiza. salvianolic acid B : A member of the class of 1-benzofurans that is an antioxidant and free radical scavenging compound extracted from S. miltiorrhiza	2.13	1	0	1-benzofurans; catechols; dicarboxylic acid; enoate ester; polyphenol	anti-inflammatory agent; antidepressant; antineoplastic agent; antioxidant; apoptosis inducer; autophagy inhibitor; cardioprotective agent; hepatoprotective agent; hypoglycemic agent; neuroprotective agent; osteogenesis regulator; plant metabolite
l 162313 L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95	3.09	1	0
6 beta-hydroxycortisol 6 beta-hydroxycortisol: RN given refers to the (6beta,11beta)-isomer; see also record for 6 alpha-hydrocortisol. 6beta-hydroxycortisol : A C21-steroid that is cortisol bearing an additional hydroxy substituent at the 6beta-position. In humans, it is produced as a metabolite of cortisol by cytochrome p450-3A4 (CYP3A4, an important enzyme involved in the metabolism of a variety of exogenous and endogenous compounds) and can be used to detect moderate and potent CYP3A4 inhibition in vivo.	3.37	1	1	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; 6beta-hydroxy steroid; C21-steroid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	human metabolite; mammalian metabolite; probe
vapiprost vapiprost: thromboxane receptor antagonist; prostaglandin receptor antagonist	1.98	1	0
vildagliptin [no description available]	3.25	1	0	amino acid amide
exp-3179 [no description available]	3.54	2	0
pratosartan pratosartan: angiotensin II type 1 receptor blocker	4.03	2	0	biphenylyltetrazole	antihypertensive agent
ave 0991 AVE 0991: structure in first source	2.01	1	0
l 163491 L 163491: structure given in first source	3.09	1	0
sm 346 SM 346: 2-mercaptobenzimidazole derivative	2.11	1	0
ema401 [no description available]	3.09	1	0
6-hydroxytaxol 6-hydroxytaxol: structure in first source. 6-hydroxypaclitaxel : A taxane diterpenoid that consists of paclitaxel bearing an additional hydroxy substituent at the 6alpha-position.	2.13	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent
bms 477118 [no description available]	3.25	1	0	adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol	EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent
fonsartan fonsartan: an angiotensin II receptor antagonist; structure given in first source	1.99	1	0
losartan potassium Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.	3.5	2	0
pituitrin Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR).	1.98	1	0
angiotensin ii, sar(1)-me-tyr(4)- angiotensin II, Sar(1)-Me-Tyr(4)-: angiotensin II antagonist	2.69	3	0
icatibant icatibant: a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer. icatibant : A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acute attacks of hereditary angioedema in adult patients.	2.39	2	0
nad NAD(1-) : An anionic form of nicotinamide adenine dinucleotide arising from deprotonation of the two OH groups of the diphosphate moiety.	1.98	1	0	organophosphate oxoanion	cofactor; human metabolite; hydrogen acceptor; Saccharomyces cerevisiae metabolite
angiotensinogen Angiotensinogen: An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver in response to lowered blood pressure and secreted into blood circulation. Angiotensinogen is the inactive precursor of the ANGIOTENSINS produced in the body by successive enzyme cleavages. Cleavage of angiotensinogen by RENIN yields the decapeptide ANGIOTENSIN I. Further cleavage of angiotensin I (by ANGIOTENSIN CONVERTING ENZYME) yields the potent vasoconstrictor octapeptide ANGIOTENSIN II; and then, via other enzymes, other angiotensins also involved in the hemodynamic-regulating RENIN-ANGIOTENSIN SYSTEM.	1.98	1	0
3h-imidazo(4,5-b)pyridine, 2-butyl-3-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, sodium salt 2-butyl-3-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-3H-imidazo(4,5-b)pyridine: an angiotensin II-receptor antagonist; structure in first source	3.08	1	0
allisartan isoproxil allisartan isoproxil: structure in first source	3.01	2	0
cardiovascular agents Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.	2.08	1	0
ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.	2.17	1	0	ascorbic acid; vitamin C	coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent
warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.	2.08	1	0	benzenes; hydroxycoumarin; methyl ketone
transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.	2.15	1	0
angiotensin i Angiotensin I: A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.. angiotensin I : A ten amino acid peptide formed by renin cleavage of angiotensinogen. Angiotensin I has no direct biological function except that high levels can stimulate catecholamine production. It is metabolized to its biologically active byproduct angiotensin II, a potent vasoconstrictor, by angiotensin converting enzyme (ACE) through cleavage of the two terminal amino acids.. angiotensin I dizwitterion : A peptide zwitterion that is the dizwitterionic form of angiotensin I having both carboxy groups deprotonated and the aspartyl amino group and arginine side-chain protonated. It is the major species at pH 7.3.	6.08	16	2	angiotensin; peptide zwitterion	human metabolite; neurotransmitter agent
angiotensin iii Angiotensin III: A heptapeptide formed from ANGIOTENSIN II after the removal of an amino acid at the N-terminal by AMINOPEPTIDASE A. Angiotensin III has the same efficacy as ANGIOTENSIN II in promoting ALDOSTERONE secretion and modifying renal blood flow, but less vasopressor activity (about 40%).	2.89	4	0
guanosine triphosphate Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.	1.98	1	0	guanosine 5'-phosphate; purine ribonucleoside 5'-triphosphate	Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.43	2	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	3.25	1	0	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic
azilsartan azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.	3.15	1	0	1,2,4-oxadiazole; aromatic ether; benzimidazolecarboxylic acid	angiotensin receptor antagonist; antihypertensive agent
concanavalin a Concanavalin A: A MANNOSE/GLUCOSE binding lectin isolated from the jack bean (Canavalia ensiformis). It is a potent mitogen used to stimulate cell proliferation in lymphocytes, primarily T-lymphocyte, cultures.	1.98	1	0
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	2.39	2	0

Condition	Relationship Strength	Studies	Trials
Blood Pressure, High [description not available]	9.88	27	7
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	9.88	27	7
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	3.79	11	0
Hypertension, Renal Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.	3.09	5	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	3.86	12	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	5.01	9	1
Debility [description not available]	3.8	1	1
Chronic Kidney Diseases [description not available]	2.6	1	0
Renal Insufficiency, Chronic Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)	2.6	1	0
Blood Pressure, Low [description not available]	2.6	1	0
Hypotension Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.	2.6	1	0
Hyperuricemia Excessive URIC ACID or urate in blood as defined by its solubility in plasma at 37 degrees C; greater than 0.42mmol per liter (7.0mg/dL) in men or 0.36mmol per liter (6.0mg/dL) in women. This condition is caused by overproduction of uric acid or impaired renal clearance. Hyperuricemia can be acquired, drug-induced or genetically determined (LESCH-NYHAN SYNDROME). It is associated with HYPERTENSION and GOUT.	2.6	1	0
Deep Vein Thrombosis [description not available]	2.46	2	0
Goldblatt Syndrome [description not available]	2.44	2	0
Blood Clot [description not available]	2.21	1	0
Hypertension, Renovascular Hypertension due to RENAL ARTERY OBSTRUCTION or compression.	2.44	2	0
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	2.21	1	0
Venous Thrombosis The formation or presence of a blood clot (THROMBUS) within a vein.	2.46	2	0
Autosomal Dominant Juvenile Parkinson Disease [description not available]	2.17	1	0
Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.	2.17	1	0
Heart Valve Diseases Pathological conditions involving any of the various HEART VALVES and the associated structures (PAPILLARY MUSCLES and CHORDAE TENDINEAE).	2.08	1	0
Adamantiades-Behcet Disease [description not available]	2.11	1	0
Innate Inflammatory Response [description not available]	3.83	2	1
Behcet Syndrome Rare chronic inflammatory disease involving the small blood vessels. It is of unknown etiology and characterized by mucocutaneous ulceration in the mouth and genital region and uveitis with hypopyon. The neuro-ocular form may cause blindness and death. SYNOVITIS; THROMBOPHLEBITIS; gastrointestinal ulcerations; RETINAL VASCULITIS; and OPTIC ATROPHY may occur as well.	2.11	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	3.83	2	1
Left Ventricular Dysfunction [description not available]	2.15	1	0
Cirrhosis [description not available]	2.15	1	0
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	2.15	1	0
Ventricular Dysfunction, Left A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.	2.15	1	0
Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.	3.37	1	1
Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.	3.37	1	1
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	2.41	2	0
Chronic Kidney Failure [description not available]	5	3	1
Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.	5	3	1
Uremia A clinical syndrome associated with the retention of renal waste products or uremic toxins in the blood. It is usually the result of RENAL INSUFFICIENCY. Most uremic toxins are end products of protein or nitrogen CATABOLISM, such as UREA or CREATININE. Severe uremia can lead to multiple organ dysfunctions with a constellation of symptoms.	2.05	1	0
Heart Disease, Ischemic [description not available]	2.91	4	0
Myocardial Ischemia A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).	2.91	4	0
Embolism, Pulmonary [description not available]	2.01	1	0
Pulmonary Embolism Blocking of the PULMONARY ARTERY or one of its branches by an EMBOLUS.	2.01	1	0
Weight Gain Increase in BODY WEIGHT over existing weight.	4.88	4	0
Diabetic Glomerulosclerosis [description not available]	2.93	1	0
Diabetic Nephropathies KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.	2.93	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	2.02	1	0
Cruveilhier-Baumgarten Syndrome Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS.	2.02	1	0
Cirrhosis, Liver [description not available]	2.02	1	0
Hypertension, Portal Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.	2.02	1	0
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	2.02	1	0
Colorectal Cancer [description not available]	3.41	1	1
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	3.41	1	1
Aura [description not available]	3.42	1	1
Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)	3.42	1	1
Cardiovascular Stroke [description not available]	2.68	3	0
Injury, Myocardial Reperfusion [description not available]	1.98	1	0
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	7.68	3	0
Carotid Arteriopathies, Traumatic [description not available]	2.4	2	0
Sclerosis, Systemic [description not available]	1.99	1	0
Scleroderma, Systemic A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.	1.99	1	0
Decerebrate Posturing [description not available]	1.99	1	0
Alloxan Diabetes [description not available]	1.99	1	0
Cardiac Failure [description not available]	3.61	3	0
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	3.61	3	0
Arrhythmia [description not available]	7	1	0
Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.	2	1	0
Recrudescence [description not available]	2	1	0
Coronary Heart Disease [description not available]	2	1	0
Coronary Disease An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.	2	1	0
Hypotension, Postural [description not available]	2	1	0
Hypotension, Orthostatic A significant drop in BLOOD PRESSURE after assuming a standing position. Orthostatic hypotension is a finding, and defined as a 20-mm Hg decrease in systolic pressure or a 10-mm Hg decrease in diastolic pressure 3 minutes after the person has risen from supine to standing. Symptoms generally include DIZZINESS, blurred vision, and SYNCOPE.	2	1	0
Cardiac Diseases [description not available]	2.91	1	0
Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities.	2.91	1	0
Tachyarrhythmia [description not available]	2	1	0
Tachycardia Abnormally rapid heartbeat, usually with a HEART RATE above 100 beats per minute for adults. Tachycardia accompanied by disturbance in the cardiac depolarization (cardiac arrhythmia) is called tachyarrhythmia.	2	1	0
Renal Artery Stenosis [description not available]	6.98	1	0
Renal Artery Obstruction Narrowing or occlusion of the RENAL ARTERY or arteries. It is due usually to ATHEROSCLEROSIS; FIBROMUSCULAR DYSPLASIA; THROMBOSIS; EMBOLISM, or external pressure. The reduced renal perfusion can lead to renovascular hypertension (HYPERTENSION, RENOVASCULAR).	1.98	1	0

exp3174

Description

Cross-References

Synonyms (64)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (1)

Drug Classes (3)

Protein Targets (6)

Inhibition Measurements

Other Measurements

Biological Processes (28)

Molecular Functions (5)

Ceullar Components (2)

Bioassays (124)

Research

Studies (230)

Market Indicators

Research Demand Index: 28.29

Study Types

exp3174

Description

Cross-References

Synonyms (64)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (1)

Drug Classes (3)

Protein Targets (6)

Inhibition Measurements

Other Measurements

Biological Processes (28)

Molecular Functions (5)

Ceullar Components (2)

Bioassays (124)

Research

Studies (230)

Market Indicators

Research Demand Index: 28.29

Study Types

Related Drugs (189)

Related Conditions (74)