In vitro pharmacological characterization of a new selective angiotensin AT1 receptor antagonist, UR-7280

European Journal of Pharmacology

Volumn 318, Issue 2-3, 1996, Pages 341-347

  De Arriba, Alberto F ^a   Gómez Casajús, Luis A ^a   Cavalcanti, Fernando ^a   Almansa, Carme ^a   García Rafanell, Julián ^a   Forn, Javier ^a  

^a Grupo Uriach   (Spain)

Author keywords

Angiotensin AT1 receptor; Angiotensin II; Aorta, rabbit; Binding; Losartan; UR 7280

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; 3 TERT BUTYL 1 PROPYL 5 [[2' (1H TETRAZOL 5 YL) 1,1' BIPHENYL 4 YL]METHYL] 1H PYRAZOLE 4 CARBOXYLIC ACID; ANGIOTENSIN; ANGIOTENSIN 1 RECEPTOR; ANGIOTENSIN RECEPTOR ANTAGONIST; BOVINE SERUM ALBUMIN; LOSARTAN; N [[4' [(2 ETHYL 5,7 DIMETHYL 3H IMIDAZO[4,5 B]PYRIDIN 3 YL)METHYL] 2 BIPHENYLYL]SULFONYL]BENZAMIDE; UNCLASSIFIED DRUG; VALSARTAN;

ADRENAL GLAND; ANIMAL TISSUE; AORTA; ARTICLE; CONTROLLED STUDY; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; FEMALE; IN VITRO STUDY; LIVER MEMBRANE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SMOOTH MUSCLE CONTRACTION; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION; TISSUE SPECIFICITY;

ANGIOTENSIN II; ANIMALS; MALE; MUSCLE, SMOOTH, VASCULAR; PYRAZOLES; RABBITS; RATS; RECEPTORS, ANGIOTENSIN; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAZOLES; VASOCONSTRICTION;

EID: 0030607656     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(96)00794-7     Document Type: Article

References (26)

1. 1 receptor antagonist, Eur. J. Pharmacol. 283, 63.
2. Birabeau, M.A., A.M. Capponi and M.B. Vallotton, 1984, Solubilized adrenal angiotensin II receptors and angiotensin II receptor antagonists, Pharmacol. Rev. 45, 205.
3. 1) receptor antagonist, Drug Dev. Res. 32, 161.
4. Chiu, A.T., D.E. McCall, W.A. Price, P.C. Wong, D.J. Carini, J.V. Duncia, A.L. Johnson, R.R. Wexler, S.E. Yoo and P.B.M.W.M. Timmermans, 1990, Nonpeptide angiotensin II receptor antagonists. VII. Cellular and biochemical pharmacology of DuP753, an orally active antihypertensive agent, J. Pharmacol. Exp. Ther. 252, 711.
5. 1-receptor subtype, Br. J. Pharmacol. 110, 761.
6. Dickinson, K.E.J., R.B. Cohen, S. Skwish, C.L. Delaney, R.P. Serafino, M.A. Poss, Z. Gu, D.E. Ryono, S. Moreland and J.R. Powell, 1994, BMS-180560, an insurmountable inhibitor of angiotensin II-stimulated responses: comparison with losartan and EXP3174, Br. J. Pharmacol. 113, 179.
7. Gaddum, J.H., K.A. Hameed, D.E. Hathaway and F.F. Stephens, 1955, Quantitative studies of antagonists for 5-hydroxytryptamine, Q. J. Exp. Physiol. 40, 49.
8. 1, receptor antagonist, 16th Scientific Meeting of the International Society of Hypertension, 23-27 June 1996, Glasgow, UK.
9. Goodfriend, T.L., M.E. Elliott and K.J. Catt, 1996, Angiotensin receptors and their antagonists, New Engl. J. Med. 334, 1649.
10. Hara, M., R. Kiyama, S. Nakajima, T. Kawabata, M. Kawakami, K. Ohtani, K. Itazaki, T. Fujishita and M. Fujimoto, 1995, Kinetic studies on the interaction of nonlabeled antagonists with the angiotensin II receptor, Eur. J. Pharmacol. 289, 267.
11. Ichiki, T., P.A. Labosky, C. Shiota, S. Okuyama, Y. Imagawa, A. Fogo, F. Niimura, I. Ichikawa, B.L.M. Hogan and T. Inagami, 1995, Effects on blood pressure and exploratory behaviour of mice lacking angiotensin II type-2 receptor, Nature 377, 748.
12. Munson, P.J. and D. Rodbard, 1980, LIGAND: a versatile computerized approach for characterization of ligand-binding systems, Anal. Biochem. 107, 220.
13. 2 receptor: searching for signal-transduction pathways and physiological function, Trends Pharmacol. Sci. 16, 223.
14. Noda, K., Y. Saad, A. Kinoshita, T.P. Boyle, R.M. Graham, A. Husain and S.S. Karnik, 1995, Tetrazole and carboxylate groups of angiotensin receptor antagonists bind to the same subsite by different mechanisms, J. Biol. Chem. 270, 2284.
15. Olins, G.M., S.T. Chen, E.G. McMahon, M.A. Palomo and D.B. Reitz, 1995, Elucidation of the insurmountable nature of an angiotensin receptor antagonist, SC-54629, Mol. Pharmacol. 45, 115.
16. 1 antagonism, J. Pharmacol. Exp. Ther. 273, 753.
17. Kenakin, T., 1993, Pharmacologic Analysis of Drug-Receptor Interaction (Raven Press, New York, NY) p. 278.
18. 1-sterically hindered 2 H-imidazol-2-one angiotensin II receptor antagonists: the conversion of surmountable antagonists to insurmountable antagonists, Biorg. Med. Chem. Lett. 3, 1055.
19. 1 receptor antagonist, Br. J. Pharmacol. 107, 1173.
20. Scatchard, G., 1949, The attraction of proteins for small molecules and ions, Ann. NY Acad. Sci. 51, 660.
21. Schambye, H.T., S.A. Hjorth, D.J. Bergsma, G. Sathe and T.W. Schwanz, 1994, Differentiation between binding sites for angiotensin II and nonpeptide antagonists on the angiotensin II type 1 receptors, Proc. Natl. Acad. Sci. USA 91, 7046.
22. Smith, R.D., A.T. Chiu, P.C. Wong, W.F. Herblin and P.B.M.W.M. Timmermans, 1992, Pharmacology of nonpeptide angiotensin II receptor antagonists, Annu. Rev. Pharmacol. Toxicol. 32, 135.
23. Tallarida, R.J. and R.B. Murray, 1981, Manual of Pharmacologic Calculations with Computer Programs (Springer-Verlag, New York, NY) p. 29.
24. Wexler, R.R., W.J. Greenlee, J.D. Irvin, M.R. Goldberg, K. Prendergast R.D. Smith and P.B.M.W.M. Timmermans, 1996, Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy, J. Med. Chem. 39, 625.
25. Wienen, W., A.B.M. Mauz, J.C.A. Van Meel and M. Entzeroth, 1992, Different types of receptor interaction of peptide and nonpeptide angiotensin II antagonists revealed by receptor binding and functional studies, Mol. Pharmacol. 41, 1081.
26. Wong, P.C. and P.B.M.W.M. Timmermans, 1991, Nonpeptide angiotensin II receptor antagonists: insurmountable angiotensin II receptor antagonism of EXP3892 is reversed by the surmountable antagonist DuP 753, J. Pharmacol. Exp. Ther. 258, 49.