2. Academic Validation
  3. In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor

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

  • FEBS Lett. 1996 Mar 25;383(1-2):37-41. doi: 10.1016/0014-5793(96)00213-x.
V Breu 1,  M Clozel,  K Burri,  G Hirth,  W Neidhart,  H Ramuz
Affiliations

Affiliation

  • 1 Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
PMID: 8612786 DOI: 10.1016/0014-5793(96)00213-x
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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