Pharmacological properties of KT3-671, a novel nonpeptide angiotensin II receptor antagonist

Journal of Cardiovascular Pharmacology
S MochizukiA Tomiyama


We examined pharmacological profiles of KT3-671, 2-propyl-8-oxo-1-[(2'-(1H-tetrazole-5-yl) biphenyl-4-yl)methyl]- 4,5,6,7-tetrahydro-cycloheptimidazole, a newly synthesized nonpeptide angiotensin II (AII) receptor antagonist in various in vitro and in vivo studies. KT3-671 displaced specific binding of [125I]Sar1 Ile8-AII to AT1 receptor with a Ki value of 0.71 +/- 0.14 x 10(-9) M in rat liver membranes, but had no affinity for AT2 receptor in bovine cerebellar membranes (Ki > 10(-5) M). In isolated rabbit aorta, KT3-671 produced a parallel rightward shift in the concentration-response curve for AII with a pA2 value of 10.04 +/- 0.12, but had no effect on KCl-, norepinephrine (NE)-, and serotonin (5-HT)-induced contractions. In conscious normotensive rats, KT3-671 (0.3-10 mg/kg, p.o.) inhibited the AII-induced pressor response dose dependently. In renal artery-ligated hypertensive rats, KT3-671 (0.1-3 mg/kg, p.o.) decreased arterial blood pressure (BP) dose dependently. The hypotensive action of 3 mg/kg KT3-671 was maintained for at least 24 h. These results suggest that KT3-671 is a potent AT1 subtype-selective and competitive nonpeptide AII receptor antagonist and has an orally active antihypertensive effect without agonistic...Continue Reading


Apr 27, 2001·Biochemical Pharmacology·F L FierensaG Vauquelin
Sep 18, 2002·Biochemical Pharmacology·Ilse VerheijenGeorges Vauquelin
Jul 8, 1999·European Journal of Pharmacology·F L FierensG Vauquelin
Mar 25, 2008·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Toshio OgiharaHiromi Rakugi
Jul 16, 2008·Molecular and Cellular Endocrinology·I Van Liefde, G Vauquelin
Dec 4, 2003·British Journal of Clinical Pharmacology·D PattersonT MacDonald
Mar 1, 2001·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Georges VauquelinPatrick Ml Vanderheyden
Apr 23, 2002·Journal of the Renin-angiotensin-aldosterone System : JRAAS·P M VanderheydenG Vauquelin
Apr 8, 2006·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·Georges VauquelinIsabelle Van Liefde
Aug 17, 2002·The Journal of Pharmacology and Experimental Therapeutics·Marc P MaillardMichel Burnier
Jun 17, 2003·Biological & Pharmaceutical Bulletin·Tadashi NagamatsuYoshio Suzuki
Jan 22, 2005·Fundamental & Clinical Pharmacology·G Vauquelin, I Van Liefde

❮ 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.