IN-VITRO CHARACTERIZATION OF RO-46-8443, THE FIRST NONPEPTIDE ANTAGONIST SELECTIVE FOR THE ENDOTHELIN ET(B) RECEPTOR

Authors
BREU V CLOZEL M BURRI K HIRTH G NEIDHART W RAMUZ H
Citation
V. Breu et al., IN-VITRO CHARACTERIZATION OF RO-46-8443, THE FIRST NONPEPTIDE ANTAGONIST SELECTIVE FOR THE ENDOTHELIN ET(B) RECEPTOR, FEBS letters, 383(1-2), 1996, pp. 37-41
Citations number
32
Categorie Soggetti
Biophysics,Biology
Journal title
FEBS letters → ACNP
ISSN journal
00145793
Volume
383
Issue
1-2
Year of publication
1996
Pages
37 - 41
Database
ISI
SICI code
0014-5793(1996)383:1-2<37:ICORTF>2.0.ZU;2-S
Abstract
We describe here Ro 46-8443, the first non-peptide endothelin ET(B) re ceptor selective antagonist. It displays up to 2000-fold selectivity f or ET(B) receptors both in terms of binding inhibitory potency and fun ctional inhibition. The observed parallel rightward shift of concentra tion-response curves with different antagonist concentrations is consi stent with a competitive binding mode. Since Ro 46-8443 selectively in hibits ET(B) receptor mediated responses, it is a valuable tool for cl arifying the role of ET(B) receptors in pathology.