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超短效β-肾上腺素能受体阻断剂。2. 芳基官能团上含有酯基的(芳氧基)丙醇胺类。

Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function.

作者信息

Erhardt P W, Woo C M, Anderson W G, Gorczynski R J

出版信息

J Med Chem. 1982 Dec;25(12):1408-12. doi: 10.1021/jm00354a003.

Abstract

Several short-acting beta-adrenergic receptor blocking agents have been prepared by incorporating ester functions into the aryl portion of certain (aryloxy)propanolamine systems. In particular, methyl 3-[4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl]propionate hydrochloride (ASL-8052) was found to be a moderately potent, cardioselective compound with a short duration of action when determined in in vivo canine models.

摘要

通过将酯官能团引入某些(芳氧基)丙醇胺体系的芳基部分,已制备出几种短效β-肾上腺素能受体阻断剂。特别地,当在体内犬模型中测定时,发现盐酸3-[4-[2-羟基-3-(异丙基氨基)丙氧基]苯基]丙酸甲酯(ASL-8052)是一种作用持续时间短的中等效力的心脏选择性化合物。

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