The in vitro pharmacological profile of KR31080, a nonpeptide AT1 receptor antagonist

Fundamental and Clinical Pharmacology

Volumn 12, Issue 1, 1998, Pages 64-69

  Hong, K W ^a,b   Kim, C D ^a   Lee, S H ^c   Yoo, S E ^c  

^a Pusan National University School of Medicine   (South Korea)

^b Pohang University of Science and Technology (POSTECH)   (South Korea)

^c Korea Research Institute of Chemical Technology   (South Korea)

Author keywords

Angiotensin II; AT receptor; KR31080; Losartan; Rabbit thoracic aorta

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; 2 BUTYL 5 METHYL 6 (1 OXOPYRIDIN 2 YL) 3 [[2 (1H TETRAZOL 5 YL)BIPHENYL 4 YL]METHYL] 3H IMIDAZO[4,5 B]PYRIDINE; ANGIOTENSIN; ANGIOTENSIN 1 RECEPTOR; ANGIOTENSIN RECEPTOR ANTAGONIST; LOSARTAN; NORADRENALIN; RECOMBINANT RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CATTLE; CELL MEMBRANE; CEREBELLUM; CONTROLLED STUDY; DOSE RESPONSE; DRUG RECEPTOR BINDING; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; RABBIT; SCATCHARD PLOT; THORACIC AORTA; VASODILATATION;

EID: 0031950643     PISSN: 07673981     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1472-8206.1998.tb00925.x     Document Type: Article

References (16)

1. 2 receptors do not interact with guanine nucleotide binding proteins. Eur J Pharmacol Mol Pharmacol 1991 ; 207 : 157-63
2. Chang RSL, Siegl PKS, Clineschmidt BV, Mantle NB, Chakravarty PH, Greenlee WJ et al. In vitro pharmacology of highly potent and selective nonpeptide angiotensin II (Ang II) receptor antagonist: L-158,809. Fed Proc 1991 ; 5 : A1575
3. Chang RSL, Siegel PKS, Clineschmidt BV, Mantle NB, Chakravaty PK, Greenlee WJ et al. In vitro pharmacology of L-158,809, a new highly potent and selective angiotensin II receptor antagonist. J Pharmacol Exp Ther 1992 ; 262 : 133-8
4. 50) of an enzymatic reaction. Biochem Pharmacol 1973 ; 22 : 3099-108
5. Chiu AT, McCall DE, Price WA, Wong PC, Carini DJ, Duncia JV et al. Nonpeptide angiotensin II receptor antagonists. VII. Cellular and biochemical pharmacology of DuP753, an orally active antihypertensive agent. J Pharmacol Exp Ther 1990 ; 252 : 711-8
6. De Chaffoy de Courcelles D, Leysen LE, Roevens P, van Belle H. The serotonin-S2 receptor: a receptor transducer coupling model to explain insurmountable antagonist effects. Drug Dev Res 1986 ; 8 : 173-8
7. Ganten D, Paul M, Lang RE. The role of neuropeptides in cardiovascular regulation. Cardiovasc Drugs Ther 1991 ; 5 : 119-30
8. Murphy TJ, Alexander RW, Griendling KK, Runge MS, Bernstein KE. Isolation of a cDNA encoding the vascular type-1 angiotensin II receptor. Nature 1991 ; 351 : 233-6
9. 1 antagonism. J Pharmacol Exp Ther 1995 ; 273 : 753-61
10. Peach MJ, Dostal DE. The angiotensin II receptor and the actions of angiotensin II. J Cardiovasc Pharmacol 1990 ; 16 : S25-30
11. Scatchard G. The attraction of proteins for small molecules and ions. Ann NY Acad Sci 1949 ; 51 : 660-72
12. Shibouta Y, Inada Y, Ojima M, Wada T, Noda M, Sanada T et al. Pharmacological profile of a highly potent and long-acting angiotensin II-receptor antagonist, 2-ethoxy-1-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid (CV-11974), and its prodrug, (±)-1-(cyclohexyloxy carbonyloxy)-ethyl-2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]- methyl]-1H-benzimidazole-7-carboxylate (TCV-116). J Pharmacol Exp Ther 1993 ; 266 : 114-20
13. Stearns RA, Doss GA, Miller RR, Chiu SHL. Synthesis and identification of a novel tetrazole metabolite of the angiotensin II receptor antagonist DuP753. Drug Metab Dispos 1991 ; 19 : 1160-2
14. Weinen W, Mauz ABM, van Meel JCA, Entzeroth M. Different types of receptor interaction of peptide and nonpeptide angiotensin II antagonists revealed by receptor binding and functional studies. Mol Pharmacol 1992 ; 41 : 1081-8
15. Wong PC, Timmermans PBMW. Nonpeptide angiotensin II receptor antagonists: insurmountable angiotensin II antagonism of EXP3892 is reversed by the surmountable antagonist DuP753. J Pharmacol Exp Ther 1991 ; 258 : 49-57
16. Wong PC, Price WA, Chiu AT, Duncia JV, Carini DJ, Wexler RR et al. Nonpeptide angiotensin II receptor antagonists. VIII. Characterization of functional antagonism displayed by DuP753, an orally active antihypertensive agent. J Pharmacol Exp Ther 1990 ; 252 : 719-25