In vitro characterisation of Ro 46‐8443, the first non‐peptide antagonist selective for the endothelin ETB receptor

FEBS Letters

Clozel, Martine¹  Hirth, Georges¹  Breu, Volker¹  Burri, Kaspar¹  Ramuz, Henri¹  Neidhart, Werner¹ 

[1] Pharma Division, Preclinical Research, c/o F. Hoffmann-La Ltd., Grenzacherstrasse 124, CH-4070 Basel, Switzerland

关键词: Endothelin;    Endothelin antagonist;    Endothelin ETB receptor;    Endothelin ETA receptor;   

DOI  :  10.1016/0014-5793(96)00213-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 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.

【 授权许可】

Unknown