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[卤代苯乙醇胺和苯氧丙醇胺的构效关系]

[Structure-activity relationships of halogenated phenylethanolamine and phenoxypropanolamine].

作者信息

Bercher H, Grisk A

出版信息

Acta Biol Med Ger. 1976;35(1):79-85.

PMID:10706
Abstract

12 compounds from the series of halogenated phenylethanolamines and phenoxypropanolamines were tested at the isolated rabbit jejunum, and the pD2-and pA2-values were determined. All the substances act beta-adrenolytically. Except for 3,4-dichloronoradrenaline, which stimulates the alpha-receptors, all the compounds still have pronounced beta-mimetic effects. The 2,5-dihalogenated phenylethanolamines and phenoxypropanolamines block the beta-receptors at lower concentrations than 2,4-dihalogen derivatives. The weakest beta-adrenolytic effects at the intestine were found with compounds halogenated at the 3,4-position.

摘要

在离体兔空肠上对12种卤代苯乙醇胺和苯氧丙醇胺系列化合物进行了测试,并测定了pD2和pA2值。所有物质均具有β-肾上腺素能阻断作用。除了刺激α受体的3,4-二氯去甲肾上腺素外,所有化合物仍具有明显的拟β效应。2,5-二卤代苯乙醇胺和苯氧丙醇胺比2,4-二卤代衍生物在更低浓度下就能阻断β受体。在肠道中发现3,4-位卤代的化合物β-肾上腺素能阻断作用最弱。

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