PMID: 8012689Jan 1, 1994Paper

Cardiovascular effects of GR117289, a novel angiotensin AT1 receptor antagonist

British Journal of Pharmacology
A HilditchM J Robertson

Abstract

1. The effect of GR117289, an angiotensin AT1 receptor antagonist, on diastolic blood pressure (DBP) was determined in angiotensin-dependent and angiotensin-independent models of hypertension in rats. In addition, the antagonist profile of GR117289 at angiotensin AT1 receptors was determined in conscious renal hypertensive rats and conscious normotensive rats, dogs and marmosets. 2. Intra-arterial and oral administration of GR117289 (0.3-3 mg kg-1, i.a.; 1-10 mg kg-1, p.o.) to 6-day left renal artery ligated hypertensive (RALH) rats (DBP > 140 mmHg) produced significant, dose-related reductions in DBP with little apparent effect on heart rate (< 15%). The antihypertensive effect of GR117289 developed progressively over several hours and with some doses persisted for 24-48 h after administration. 3. Administration of GR117289 (1 mg kg-1, i.a.) on 5 consecutive days to RALH rats reduced DBP on each day. The antihypertensive effect of GR117289 was not cumulative as DBP had almost returned to base-line values, 24 h after administration of each dose. 4. A dose of GR117289 (3 mg kg-1, i.a.), which produced a substantial reduction in DBP (about 70 mmHg) in RALH rats, was administered to rats in which blood pressure was elevated either...Continue Reading

References

Apr 1, 1979·Clinical Science·J D Swales
Jun 11, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·D P BrooksM Gellai
Apr 1, 1987·Hypertension·R C VariR H Freeman
Apr 1, 1987·Hypertension·G D FinkM L Mangiapane
Jan 1, 1971·Journal of Applied Physiology·D J O'BrienJ W McRoberts
Mar 1, 1963·Japanese Circulation Journal·K OKAMOTO, K AOKI
Jul 1, 1960·Journal of Applied Physiology·V POPOVIC, P POPOVIC

❮ Previous
Next ❯

Citations

Nov 1, 1996·British Journal of Pharmacology·L ZhaoM R Wilkins
Dec 5, 1997·Journal of Cardiovascular Pharmacology·K TamuraK Hashimoto
Mar 9, 1999·Journal of Cardiovascular Pharmacology·B H LeeH S Shin
Feb 2, 1996·Journal of Medicinal Chemistry·R R WexlerP B Timmermans

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.