Benzofuran based angiotensin II antagonists related to GR117289: Part III; GR138950, a triflamide with high oral bioavailability.☆

Abstract The identification of GR138950, a non-peptide antagonist of angiotensin II with high oral bioavailability, is described. GR138950 is a potent and selective AT 1 receptor antagonist which causes marked falls in blood pressure in renal hypertensive rats after either systemic or oral administration. It has high bioavailability in both rats and dogs and been selected as our second candidate for clinical development.