Further investigations into the mechanism of the antihypertensive activity of the angiotensin AT1 receptor antagonist, GR138950

British Journal of Pharmacology
A HilditchG M Drew


1. The angiotensin AT1 receptor antagonist, GR138950, produces a long-lasting antihypertensive effect in conscious renal artery ligated hypertensive (RALH) rats but this effect does not correlate temporally with its antagonist profile against angiotensin II (AII). In the present experiments we have compared the inhibitory profiles of GR138950 and enalapril, against angiotensin I (AI), with their respective antihypertensive activities. 2. GR138950 (1 mg kg-1, i.a.) and enalapril (3 mg kg-1, i.a.) reduced blood pressure in RALH rats to a similar degree. Maximum reductions in blood pressure occurred approximately 5-24 h and 3-5 h after administration, respectively. The antihypertensive effect of GR138950 lasted for 24-48 h. However, the effect of enalapril lasted for only 5-24 h. 3. In conscious normotensive rats, inhibition of AI-induced pressor responses was maximal 1 h after systemic administration of GR138950 and enalapril. Dose-response curves to AI were displaced to the right, in a parallel manner, 1406 and 102 fold by GR138950 (1 mg kg-1, i.a.) and enalapril (3 mg kg-1 i.a.), respectively. The inhibitory effect of enalapril lasted for < 24 h whereas that of GR138950 lasted for up to 48 h. 4. Contractile responses to AI were...Continue Reading


Mar 12, 1976·Science·P R CaldwellR L Soffer
May 1, 1990·Clinical and Experimental Pharmacology & Physiology·D J CampbellA Kladis
Jun 1, 1990·British Journal of Pharmacology·C EglèmeJ M Wood
Jan 27, 1988·European Journal of Pharmacology·C A GruetterD D Schoepp
Jul 4, 1995·European Journal of Pharmacology·K L ClarkG M Drew
Jan 1, 1994·British Journal of Pharmacology·A HilditchM J Robertson

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