2. Academic Validation
  3. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors

In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors

  • FEBS Lett. 1993 Nov 15;334(2):210-4. doi: 10.1016/0014-5793(93)81713-a.
V Breu 1,  B M Löffler,  M Clozel
Affiliations

Affiliation

  • 1 Pharma Division, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
PMID: 8224248 DOI: 10.1016/0014-5793(93)81713-a
Abstract

Ro 46-2005 is a new synthetic non-peptide endothelin (ET) receptor antagonist. In binding experiments, Ro 46-2005 proved to be equipotent (IC50 200-500 nM) for inhibition of [125]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Scatchard analysis was consistent with a competitive binding mode. Ro 46-2005 also inhibited the functional consequences of ET-1 stimulation: the ET-1 induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 microM.

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