How can the differences among AT1-receptor antagonists be explained?

Cell Biochemistry and Biophysics

Volumn 35, Issue 1, 2001, Pages 89-102

  Morsing, Peter ^a   Vauquelin, Georges ^b  

^a ASTRAZENECA R AND D   (Sweden)

^b VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

Author keywords

Candesartan; CHO cells; Dose response relationship; Irbesartan; Losartan; Nonpeptide angiotensin II AT1 receptor antagonists; Pharmacokinetics

Indexed keywords

ANGIOTENSIN 1 RECEPTOR; ANGIOTENSIN RECEPTOR; ANTIHYPERTENSIVE AGENT; BENZIMIDAZOLE DERIVATIVE; CANDESARTAN; LOSARTAN; TETRAZOLE DERIVATIVE;

ANIMAL; BIOLOGICAL MODEL; CHEMICAL MODEL; CHO CELL; DOSE RESPONSE; DRUG ANTAGONISM; HAMSTER; HUMAN; KINETICS; PROTEIN BINDING; REVIEW;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BENZIMIDAZOLES; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; KINETICS; LOSARTAN; MODELS, BIOLOGICAL; MODELS, CHEMICAL; PROTEIN BINDING; RECEPTOR, ANGIOTENSIN, TYPE 1; RECEPTORS, ANGIOTENSIN; TETRAZOLES;

EID: 0035754163     PISSN: 10859195     EISSN: None     Source Type: Journal    
DOI: 10.1385/CBB:35:1:89     Document Type: Review

References (79)

1. Conlin, P. R., Spence, J. D., Williams, B., Ribeiro, A. B., Saito, I., Benedict, C., and Bunt, A. M. (2000) Angiotensin II antagonists for hypertension: are there differences in efficacy? Am. J. Hypertens. 13, 418-426.
2. Andersson, O. K. and Neldam, S. (1998) The antihypertensive effect and tolerability of candesartan cilexetil, a new generation angiotensin II antagonist, in comparison with losartan. Blood Press. 7, 53-59.
3. Lacourciere, Y. and Asmar, R. (1999) A comparison of the efficacy and duration of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients. A placebo-controlled, forced titration study. Am. J. Hypertens. 12, 1181-1187.
4. Koenig, W. (2000) Comparison of the efficacy and tolerability of combination tablets containing candesartan cilexetil and hydrochlorothiazide or losartan and hydrochlorothiazide in patients with moderate to severe hypertension. Results of the CARLOS-Study. Clin. Drug Invest. 19, 239-246.
5. Gradman, A. H., Lewin, A., Bowling, B. T., Tonkon, M., Deedwania, P. C., Kezer, A. E., et al. (1999) Comparative effects of candesartan cilexetil and losartan in patients with systemic hypertension. For the candesartan versus losartan efficacy comparison (CANDLE) study group. Heart. Dis. 1, 52-57.
6. Manolis, A. J., Grossman, E., Jelakovic, B., Jacovides, A., Bernhardi, D. C., Cabrera, W. J., et al. (2000) Losartan and candesartan produce comparable blood pressure reductions but only losartan lowers plasma uric acid in hypertensive patients. For the losartan trial investigators. Clin. Ther. 22, 1186-1203.
7. Fridman, K., Wysocki, M., Friberg, P., and Andersson, O. (1999) A comparison of the inhibitory effects of candesartan cilexetil, losartan and valsartan on the response to angiotensin II infusion in hypertensive patients. Am. J. Hypertens. 12, 135A.
8. Öhman, K. P., Milon, H., and Valnes, K. (2000) Efficacy and tolerability of a combination tablet of candesartan cilexetil and hydrochlorothiazide in insufficiently controlled primary hypertension. Comparison with a combination of losartan and hydrochlorothiazide. Blood Press. 9, 214-220.
9. Mallion, J. M., Siche, J. P., Mouret, S., Quessada, I. L., and Baguet, J. P. (2000) A placebo-controlled comparison between candesartan cilexetil 8mg and losartan 50mg monotherapy in essential hypertension using 36H ambulatory blood pressure monitoring. JRAAS 1, 104.
10. Kassler-Taub, K., Littlejohn, T., Elliot, W., Ruddy, T., and Adler, E. (1998) Comparative efficacy of two angiotensin II receptor antagonists, irbesartan and losartan in mild-to-moderate hypertension. Irbesartan/Losartan study investigators. Am. J. Hypertens. 11, 445-453.
11. Oparil, S., Guthrie, R., Lewin, A. J., Marbury, T., Reilly, K., Triscari, J., and Witcher, J. A. (1998) An elective-titration study of the comparative effectiveness of two angiotensin II-receptor blockers, irbesartan and losartan. Irbesartan/losartan study investigators. Clin. Ther. 20, 398-409.
12. Mallion, J. M., Siche, J. P., Lacourcière, Y., and the Telmisartan Blood Pressure Monitoring Group. (1999) ABPM comparison of the antihypertensive profiles of the selective angiotensin II receptor antagonists telmisartan and losartan in patients with mild-to-moderate hypertension. J. Hum. Hypertens. 13, 657-664.
13. 1 receptors. Am. J. Hypertens. 13, 31S-38S.
14. Timmermans, P. B. M. W. M., Benfield, P., Chiu, A. T., Herblin, W., and Wong, P. C. (1992) Angiotensin II receptors and functional correlates. Am. J. Hypertens. 5, 221S-235S.
15. Lumbers, E. R. (1999) Angiotensin and aldosterone. Regul. Pept. 80, 91-100.
16. 2 subtype receptors: an emerging target for cardiovascular therapy. Ital. Heart. J. 1, 96-103.
17. Kambayashi, Y., Bardhan, S., Takahashi, K., Tsuzuki, S., Inui, H., Hamakubo, T., and Inagami, T. (1993) Molecular cloning of a novel angiotensin II receptor isoform involved in phosphotyrosire phosphatase inhibition. J. Biol. Chem. 268, 24543-24546.
18. Mukoyama, M., Nakajima, M., Horiuchi, M., Sasamura, H., Pratt, R. E., and Dzau, V. J. (1993) Expression cloning of type 2 angiotensin II receptor reveals a unique class of seven-transmembrane receptors. J. Biol. Chem. 268, 24, 539-24,542.
19. Vallotton, M. B. (1987) The renin-angiotensin system. Trends Pharmacol Sci. 8, 69-74.
20. Zhang, J. C., Van Meel, A., Pfaffendorf, M., and Van Zwieten, P. (1993) Different types of angiotensin II receptor antagonism induced by BIBS 222 in the rat portal vein and rabbit aorta; the Influence of receptor reserve. J. Pharmacol. Exp. Ther. 269, 509-514.
21. Robertson, M. J. (1998) Angiotensin antagonists, in Receptor-Based Drug Design (Leff, P., ed.), Marcel Dekker, New York, pp. 207-223.
22. Liu, Y. J., Shankley, N. P., Welsh, N. J., and Black, J. W. (1992) Evidence that the apparent complexity of receptor antagonism by angiotensin II analogues is due to a reversible and synoptic action. Br. J. Pharmacol. 106, 233-241.
23. 1 receptor subtype. Br. J. Pharmacol. 110, 761-771.
24. 1 subtype angiotensin II receptor antagonist. J. Pharmacol. Exp. Ther. 265, 826-834.
25. Noda, M., Shibouta, Y., Inada, Y., Ojima, M., Wada, T., Sanada, T., et al. (1993) Inhibition of rabbit aortic angiotensin II (AII) receptor by CV-11974, a new neuropeptide AII antagonist. Biochem. Pharmacol. 46, 311-318.
26. Mochizuki, S., Sato, T., Furata, K., Hase, K., Ohkura, Y., Fukai, C., et al. (1995) Pharmacological properties of KT3-671, a novel nonpeptide angiotensin II receptor antagonist. J. Cardiovasc. Pharmacol. 25, 22-29.
27. Wienen, W., Mauz, A. B. M., Van Meel, J. C. A., and Entzeroth, M. (1992) Different types of receptor interaction of peptide and nonpeptide angiotensin II antagonists revealed by receptor binding and functional studies. Mol. Pharmacol. 41, 1081-1089.
28. de Chaffoy de Courcelles, D., Leysen, J. E., Roevens, P., and Van Belle, H. (1986) The serotonin-S2 receptor: A receptor, transducer coupling model to explain insurmountable antagonist effects. Drug Dev. Res. 8, 173-178
29. Robertson, M. J., Dougall, I. G., Harper, D., Mckechnie, K. C. W., and Leff, P. (1994) Agonist-antagonist interactions at angiotensin receptors: application of a two-state receptor model. Trends Pharmacol. Sci. 15, 364-369.
30. Dickinson, K. E., Cohen, R. B., Skwish, S., Delaney, C. L., Serafino, R. P., Poss, M. A., et al. (1994) BMS-180560, an insurmountable inhibitor of angiotensin II-stimulated responses: comparison with losartan and EXP3174. Br. J. Pharmacol. 113, 179-189.
31. Wienen, W., Hauel, N., Van Meel, J. C. A., Narr, B., Ries, U., and Entzeroth, M. (1993) Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br. J. Pharmacol. 110, 245-252.
32. Olins, G. M., Chen, S. T., McMahon, E. G., Palomo, M. A., and Reitz, D. B. (1994) Elucidation of the insurmountable nature of an angiotensin receptor antagonist, SC-54629. Mol. Pharmacol. 47, 115-120.
33. 1 receptor antagonist. Eur. J. Pharmacol. 283, 63-72.
34. 1 receptor antagonist. Br. J. Pharmacol. 114, 1117-1124.
35. 1 receptor antagonist, UR-7280. Eur. J. Pharmacol. 318, 341-347.
36. Ojima, M., Inada, Y., Shibouta, Y., Wada, T., Sanada, T., Kubo, K., and Nishikawa, K. (1997) Candesartan (CV-11974) dissociates slowly from the angiotensin ATI receptor. Eur. J. Pharmacol. 319, 137-146.
37. 1 receptor antagonist. Br. J. Pharmacol. 107, 1173-1180.
38. 1 antagonism. J. Pharm. Exp. Ther. 273, 753-761.
39. Zhang, J., Pfaffendorf, M., Zhang, J. S., and Van Zwieten, P. (1993) A non-competitive type of angiotensin receptor antagonism by losartan in renal artery preparations Eur. J. Pharmacol. 252, 337-340.
40. 1 receptors. Br. J. Pharmacol. 126, 1057-1065.
41. 1 receptor antagonists: the role of tight antagonist binding. Eur. J. Pharmacol. 372, 199-206.
42. Pendleton, R. G., Gessner, G., and Horner, E. (1989) Studies on inhibition of angiotensin II receptors in rabbit adrenal and aorta. J. Pharmacol. Exp. Ther. 248, 637-643.
43. Hara, M., Kiyama, R., Nakajima, S., Kawabata, T., Kawakami, M., Ohtani, K., et al. (1995) Kinetic studies on the interaction of nonlabelled antagonists with the angiotensin II receptor. Eur. J. Pharmacol. 289, 267-273
44. Rang, H. P. (1965) The kinetic action of acetylcholine antagonists in smooth muscle. Proc. R. Soc. Lond. 164, 488-510.
45. Rang, H. P. and Dale, M. M. (1987) Mechanisms of drug action, in Pharmacology (Rang, H. P. and Dale, M. M., eds.), Churchill Livingstone, London, pp. 3-34.
46. Kenakin, T. P. (1987) Drug antagonism, in Pharmacological Analysis of Drug-Receptor Interaction (Kenakin, T. P., ed.), Raven Press, New York, pp. 205-244.
47. 1 receptor-rransfected Chinese hamster ovary cells. Eur. J. Pharmacol. 367, 413-422.
48. 1 receptors expressed in CHO-K1 cells. Biochem. Pharmacol. 59, 927-935.
49. 3H]-irbesartan to human recombinant angiotensin II type 1 receptors. J. Renin- Angiotensin- Aldosterone System 1, 159-165.
50. Limbird, L. E. in Limbird L. E. (eds.) (1996) Cell Surface Receptors: A Short Course on Theory and Methods, 2nd ed. Kluwer Academic Publishers Boston, 61-122.
51. 1receptor blockers in isolated vessels of different origin. Hypertension 33, 1406-1413.
52. Delacrétaz, E., Nussberger, J., Biollaz, J., Waeber, B., and Brunner, H. R. (1995) Characterization of the angiotensin II receptor antagonist TCV-116 in healthy volunteers. Hypertension 25, 14-21.
53. Maillard, M. P., Mazzolai, L., Daven, V., Centeno, C., Nussberger, J., Brunner, H. R., and Burnier, M. (1999) Assessment of angiotensin II receptor blockade in humans using a standardized angiotensin II receptor-binding assay. Am. J. Hypertens. 12, 1201-1208.
54. van Lier, J. J., van Heiningen, P. N. M., and Sunzel, M. (1997) Absorption, metabolism and excretion of 14C-candesartan and 14C candesartan-cilexetil in healthy volunteers. J. Human Hypertens. 11(Suppl 2), S27-28.
55. Tamura, K., Okuhira, M., Mikoshiba, I., and Hashimoto, K. (1997) In vitro pharmacological properties of KRH-594, a novel angiotensin II type 1 receptor antagonist. Biol. Pharmacol. Bull. 20, 850-855.
56. Wong, P. C., and Timmermans, P. B. (1991) Nonpeptide angiotensin II receptor antagonists: insurmountable angiotensin II antagonism of EXP3892 is reversed by the surmountable antagonist DuP753. J. Pharmacol. Exp. Ther. 258, 49-57.
57. Inoue, Y., Nakamura, N., and Inagami, T. (1997) A review of mutagenesis studies of angiotensin II type 1 receptor: the three-dimensional receptor model in search of the agonist and antagonist binding site and the hypothesis of a receptor activation mechanism. J. Hypertens. 15, 703-714.
58. Azizi, M., Chatellier, G., Guyene, T. T., and Menard, J. (1999) Pharmacokinetic-pharmacodynamic interactions of candesartan and losartan. J. Hypertens. 17, 561-568.
59. 1 receptors and their non-peptide antagonists. Biochem. Pharmacol. 61, 277-284.
60. Anderson, K. M., Murahashi, T., Dorstal, D. E., and Peach, M. J. (1993) Morphological and biochemical analysis of angiotensin II internalization in cultured rat aortic smooth muscle cells. Am. J. Physiol 264, C179-C188.
61. 2 receptors: evidence for selective sorting of receptor and ligand. Mol. Endocrinol. 11, 1266-1277.
62. Crozat, A., Penhoat, A., and Saez, J. M. (1986) Processing of angiotensin II (A-II) and (sarl,Ala8)A-II by cultured bovine adrenocorti-cal cells. Endocrinology 118, 2312-2318.
63. 1b receptors: pharmacological and functional requirements. FEBS Lett. 349, 365-370.
64. 1 receptors in intact cells is apparently unrelated to receptor internalization. Biochem. Pharmacol. 61, 1227-1235.
65. De Lean, A., Stadel, J. M., and Lefkowitz, R. J. (1980) A ternary complex model explains the agonist-specific properties of the adenylate cyclase-coupled β adrenergic receptor. J. Biol. Chem. 255, 7108-7117.
66. Severne, Y., Ijzerman, A., Nerme, V., Zimmerman, H., and Vauquelin, G. (1986) Shallow agonist competition binding curves for β-adrenergic receptors: the role for tight agonist binding. Mol. Pharmacol. 31, 69-73.
67. Yu, S. S., Lefkowitz, R. J., and Hausdorff, W. P. (1993) β-Adrenergic receptor sequestration: a potential mechanism of receptor resensitization. J. Biol. Chem. 268, 337-341.
68. Cvejic, S. and Devi, L. A. (1997) Dimerization of the δ opioid receptor. J. Biol. Chem. 272, 26,959-26,964.
69. Gürdal, H., Bond, R. A., Johnson, M. D., Friedman, E., and Onaran, H. O. (1997) An efficacy-dependent effect of cardiac overexpression of β2-adrenoceptor on ligand affinity in transgenic mice. Mol. Pharmacol. 52, 187-194.
70. Monnot, C., Bihoreau, C., Conchon, S., Curnow, K. M., Corvol, P., and Clauser, E. (1996) Polar residues in the transmembrane domains of the type 1 angiotensin II receptor are required for binding and coupling. Reconstitution of the binding site by co-expression of two deficient mutants. J. Biol. Chem. 271, 1507-1513.
71. 1 receptor antagonist. J. Cardiovasc. Pharmacol. 25, 354-360.
72. 1 receptor. J. Biol. Chem. 274, 7103-7110.
73. Schambye, H. T., Hjorth, S. A., Bergsma, D. J., Sathe, G., and Schwartz, T. W. (1994) Differentiation between binding sites for angiotensin II and nonpeptide antagonists on the angiotensin II type 1 receptors. Proc. Natl. Acad. Sci. USA 91, 7046-7050.
74. 1 receptor in agonist activation. J. Biol. Chem. 270, 28,511-28,514.
75. 1 receptor differently affects the binding of surmountable and insurmountable non-peptide antagonists. J. Renin. Angiotensin Syst. (submitted).
76. 1). J. Biol. Chem. 270, 14,024-14,030.
77. Vauquelin G, Fierens, F. L. P., Gáborik, Z., Tam Le Minh, T., De Backer, J.-P., Hunyady, L., and Vanderheyden, P. M. L. (2001) Role of basic amino acids of the human angiotensin type 1 receptor in the binding of the non-peptide antagonist candesartan. J. Renin- Angiotensin- Aldostewne System 2 (Suppl. 1), S32-S36.
78. Duncia, J. V., Chiu, A. T., Carini, D. J., Gregory, G. B., Johnson, A. L., Price, W. A., et al. (1990) The discovery of potent nonpeptide angiotensin II receptors antagonists: a new class of potent antihypertensives. J. Med. Chem. 33, 1312-1329.
79. Timmermans, P. B. W. M., Wong, P. C., Chiu, A. T., Herblin, W. F., Benfield, P., Carini, D. J., et al. (1993) Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol. Rev. 45, 205-251.