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

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 wit...

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Veröffentlicht in:	FEBS letters 1996-03, Vol.383 (1-2), p.37-41
Hauptverfasser:	Breu, Volker, Clozel, Martine, Burri, Kaspar, Hirth, Georges, Neidhart, Werner, Ramuz, Henri
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arachidonic Acid - metabolism Binding, Competitive Cell Membrane - metabolism CHO Cells Cricetinae Endothelin Endothelin antagonist Endothelin ETA receptor Endothelin ETB receptor Endothelin Receptor Antagonists Humans In Vitro Techniques Microsomes - metabolism Molecular Structure Muscle Contraction - drug effects Protein Binding Pyrimidines - metabolism Pyrimidines - pharmacology Rats Receptor, Endothelin B Receptors, Endothelin - metabolism Receptors, Peptide - antagonists & inhibitors Receptors, Peptide - metabolism Recombinant Proteins - metabolism Sulfonamides - metabolism Sulfonamides - pharmacology Vasoconstriction - drug effects Vasoconstrictor Agents - metabolism Viper Venoms - metabolism
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