Pharmacological characterisation of novel kinin B2 receptor ligands

被引：2

作者：

Camarda, V

Rizzi, A

Calò, G

Wirth, K

Regoli, D ^{[1
]}

机构：

[1] Univ Ferrara, Dept Expt & Clin Med, Pharmacol Sect, I-44100 Ferrara, Italy

[2] Aventis Pharma, Cardiovasc Dis Grp, Frankfurt, Germany

来源：

CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY | 2002年 / 80卷 / 04期

关键词：

bradykinin; B-2 receptor ligands; bioassay; isolated vessels;

D O I：

10.1139/Y02-037

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Peptide and nonpeptide compounds have been shown to interact specifically with B-2 receptors of three different species, namely human, rabbit, and pig. Peptide agonists and nonpeptide antagonists show marked differences in potencies and suggest the existence of B-2 receptor subtypes. This conclusion is based on data obtained with the modified agonist peptide LF 150943 whose potency (pEC(50) 9.4) is at least 100-fold higher in rabbit than in humans (7.4) and pig (6.7). The same conclusion can be drawn from data obtained with antagonists that are more potent in humans (LF 160687, pA(2) 9.2) than in rabbit (8.7) and pig (8.2) or with antagonists (S 1567) that show the opposite potency order, being much weaker in humans (pA(2) 6.9) than in rabbit (7.6) and pig (9.4). Two other compounds (FR 173657 and FR 172357) show similar pharmacological spectra as S 1567 and differ from LF 160687.

引用

页码：281 / 286

页数：6

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