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

Autor:	Werner Neidhart, Martine Clozel, Volker Breu, Georges Hirth, Henri Ramuz, Kaspar Burri
Jazyk:	angličtina
Předmět:	Endothelin Receptor Antagonists Endothelin receptor type A Non peptide antagonist Receptors Peptide Biophysics CHO Cells Viper Venoms Pharmacology In Vitro Techniques Endothelin ETA receptor Biochemistry Binding Competitive Endothelin Endothelin antagonist Structural Biology Cricetinae Microsomes Genetics Animals Humans Vasoconstrictor Agents Molecular Biology Etb receptor Sulfonamides Arachidonic Acid Molecular Structure Chemistry Receptors Endothelin Rightward shift Cell Membrane Antagonist Cell Biology respiratory system musculoskeletal system Endothelin 1 Receptor Endothelin B In vitro Recombinant Proteins Rats Pyrimidines Vasoconstriction cardiovascular system Endothelin receptor Endothelin ETB receptor Muscle Contraction Protein Binding circulatory and respiratory physiology
Zdroj:	FEBS Letters. (1-2):37-41
ISSN:	0014-5793
DOI:	10.1016/0014-5793(96)00213-X
Popis:	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 Ro 46-8443 selectively inhibits ETB receptor mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.
Databáze:	OpenAIRE
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