In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ET(B) receptor

被引：42

作者：

Breu, V

Clozel, M

Burri, K

Hirth, G

Neidhart, W

Ramuz, H

机构：

[1] Pharma Division, Preclinical Research, c/o F. Hoffmann-La Roche Ltd., CH-4070 Basel

来源：

FEBS LETTERS | 1996年 / 383卷 / 1-2期

关键词：

endothelin; endothelin antagonist; endothelin ET(B) receptor; endothelin ET(A) receptor;

D O I：

10.1016/0014-5793(96)00213-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We describe here Ro 46-8443, the first non-peptide endothelin ET(B) receptor selective antagonist. It displays up to 2000-fold selectivity for ET(B) receptors both in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration-response curves with different antagonist concentrations is consistent with a competitive binding mode. Since Ro 46-8443 selectively inhibits ET(B) receptor mediated responses, it is a valuable tool for clarifying the role of ET(B) receptors in pathology.

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页码：37 / 41

页数：5

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