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In vitro characterisation of Ro 46‐8443, the first non‐peptide antagonist selective for the endothelin ET B receptor
Author(s) -
Breu Volker,
Clozel Martine,
Burri Kaspar,
Hirth Georges,
Neidhart Werner,
Ramuz Henri
Publication year - 1996
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(96)00213-x
Subject(s) - endothelin receptor , antagonist , receptor , competitive antagonist , chemistry , potency , peptide , receptor antagonist , pharmacology , in vitro , medicine , endocrinology , biochemistry , biology
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.