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

FEBS Letters
V BreuH Ramuz

Abstract

We describe here Ro 46-8443, the first non-peptide endothelin ETB receptor selective antagonist. It displays up to 2000-fold selectivity for ETB 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 R0 46-8443 selectively inhibits ETB receptor mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.

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Citations

Jan 1, 1997·Life Sciences·T GillerM Clozel
Sep 24, 2002·Pharmacology & Therapeutics·P D'Orléans-JusteJ C Honoré
May 6, 2003·Bioorganic & Medicinal Chemistry Letters·Udo E W LangeGeorg Kettschau
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May 23, 2007·BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy·Joris H Robben, Peter M T Deen
Mar 10, 2016·Pharmacological Reviews·Anthony P DavenportJanet J Maguire
Jun 9, 2016·Journal of Medicinal Chemistry·John-David Aubert, Lucienne Juillerat-Jeanneret
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
Aug 13, 1999·The American Journal of Physiology·E ThorinM Lavallée

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