L-159282 (MK 996) 是一种高效的口服活性非肽血管紧张素 II 受体拮抗剂，具有抗高血压活性。
L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.
In the anesthetized chimpanzee, L-159282 (1 mg/kg, iv) produces 100% inhibition of the AII pressor response and is still active (52%) at 24 h. In aortic coarcted (high renin) rats, L-159282 (3 mg/kg, p.o.) reduces blood pressure to normotensive (< 120 mm Hg) levels without reflex tachycardia. This dose of L-159282 reduces blood pressure to approximately the same level as both losartan (3 mg/kg, p.o.) and enalapril (3 mg/kg, p.o.) in this model[1].
[1]. Kivlighn SD, et al. In vivo pharmacology of a novel AT1 selective angiotensin II receptor antagonist, MK-996. Am J Hypertens. 1995 Jan;8(1):58-66.
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