血管舒张剂/β-肾上腺素能阻滞剂的应用：二氢卢替啶类示例。

Approaches to vasodilating/beta-adrenergic blocking agents: examples of the dihydrolutidine type.

作者信息

Baldwin J J, Hirschmann R, Engelhardt E L, Ponticello G S, Sweet C S, Scriabine A

出版信息

J Med Chem. 1981 May;24(5):628-31. doi: 10.1021/jm00137a028.

Abstract

The aminohydroxypropoxy moiety has been incorporated into the dihydrolutidine class of vasodilators. In the spontaneously hypertensive rat, one of these, (S)-4-[2-methyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-3,5-dicarboethoxy-1,4-dihydrolutidine (4c), exhibited antihypertensive activity on the order of the standard 4-[2-(trifluoromethyl)phenyl]-3,5-dicarboethoxy-1,4-dihydrolutidine (2a). This antihypertensive activity could not be explained in terms of a vasodilating effect, as determined in the dog. In this latter model, 2a decreased both mean arterial and hindlimb perfusion pressures.

摘要

氨基羟基丙氧基部分已被引入二氢卢替啶类血管扩张剂中。在自发性高血压大鼠中，其中一种化合物，即(S)-4-[2-甲基-4-[3-(叔丁基氨基)-2-羟基丙氧基]苯基]-3,5-二乙氧羰基-1,4-二氢卢替啶(4c)，表现出与标准的4-[2-(三氟甲基)苯基]-3,5-二乙氧羰基-1,4-二氢卢替啶(2a)相当的降压活性。如在犬模型中所测定的，这种降压活性不能用血管舒张作用来解释。在犬模型中，2a可降低平均动脉压和后肢灌注压。