一种作用时间显著延长的血管紧张素II拮抗剂。
An angiotensin II antagonist with strongly prolonged action.
作者信息
Holck M, Bossé R, Fischli W, Gerold H, Escher E
机构信息
Hoffmann La Roche A.G., Basel, Switzerland.
出版信息
Biochem Biophys Res Commun. 1989 May 15;160(3):1350-6. doi: 10.1016/s0006-291x(89)80152-4.
A highly hydrophobic analogue of angiotensin II (AT), [Sar1,(2',3',4',5',6'-Br5)Phe8]AT exhibited strong and persistent specific antagonism against AT, both in vitro and in vivo. This peptide exhibited 32% of the binding affinity of [Sar1]AT towards membranes of bovine adrenal cortex, it was a specific AT antagonist of irreversible character on smooth muscle assays, and it also suppressed for over 120 min at 7.10(-8) M/kg the blood pressure response towards AT in the rat blood pressure assay. This compound harbours therefore the potential of a new class of AT-specific antihypotensive drugs.
血管紧张素II（AT）的一种高度疏水类似物，[Sar1,(2',3',4',5',6'-Br5)Phe8]AT在体外和体内均表现出对AT的强烈且持久的特异性拮抗作用。该肽对牛肾上腺皮质膜表现出[Sar1]AT结合亲和力的32%，在平滑肌试验中它是一种具有不可逆特性的特异性AT拮抗剂，并且在大鼠血压试验中，以7.10(-8) M/kg的剂量它还能在超过120分钟的时间里抑制对AT的血压反应。因此，这种化合物具有成为一类新型AT特异性抗高血压药物的潜力。
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