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In vitro characterization of Ro 46‐2005, a novel synthetic non‐peptide endothelin antagonist of ET A and ET B receptors
Author(s) -
Breu Volker,
Löffler Bernd-Michael,
Clozel Martine
Publication year - 1993
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(93)81713-a
Subject(s) - antagonist , receptor , peptide , endothelin receptor , in vitro , chemistry , receptor antagonist , arachidonic acid , endothelin 1 , competitive antagonist , stimulation , stereochemistry , pharmacology , endocrinology , medicine , biochemistry , biology , enzyme
Ro 46‐2005 is a new synthetic non‐peptide endothelin (ET) receptor antagonist. In binding experiments, Ro 46‐2005 proved to be equipotent (IC 50 200–500 nM) for inhibition of [ 125 I]ET‐1 binding on the two known ET receptor subtypes (ET A and ET B ). Scatchard analysis was consistent with a competitive binding mode. Ro 46‐2005 also inhibited the functional consequences of ET‐1 stimulation: the ET‐1‐induced release of arachidonic acid from rat mesangial cells was inhibited with an IC 50 of 1.8 μM.