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[在(3-氨基-2-羟基丙氧基)苯氧基甲基异恶唑衍生物中寻找新型β-肾上腺素能阻滞剂]

[Search for new beta-adrenoblockaders among derivatives of (3-amino-2-hydroxypropoxy) phenoxymethyl isoxazole].

作者信息

Iuzhakov S D, Sokolov S D, Vinogradova S M

出版信息

Farmakol Toksikol. 1988 Jul-Aug;51(4):47-52.

PMID:2903834
Abstract

In experiments on anesthetized rats it was found that some derivatives of 2-(3-isopropylamino-2-hydroxypropoxy) phenoxymethyl isoxazole possess marked beta-adrenoblocking activity associated with alpha-adrenoblocking properties. The most active compound is 3-methyl-4-chloro-5-(3-isopropylamino-2-hydroxypropoxy) phenoxymethyl isoxazole hydrochloride (compound II) which by its beta-adrenoblocking activity is superior to propranolol, oxprenolol and especially labetalol. By its alpha-adrenoblocking activity the compound does not differ significantly from labetalol but it is inferior to phentolamine. Compound II has partial agonistic activity, exerts nonspecific membrane-stabilizing action and exhibits antifibrillatory and antiarrhythmic activity.

摘要

在对麻醉大鼠的实验中发现,2-(3-异丙基氨基-2-羟基丙氧基)苯氧基甲基异恶唑的一些衍生物具有明显的β-肾上腺素能阻断活性,并伴有α-肾上腺素能阻断特性。最具活性的化合物是3-甲基-4-氯-5-(3-异丙基氨基-2-羟基丙氧基)苯氧基甲基异恶唑盐酸盐(化合物II),其β-肾上腺素能阻断活性优于普萘洛尔、氧烯洛尔,尤其优于拉贝洛尔。就其α-肾上腺素能阻断活性而言,该化合物与拉贝洛尔无显著差异,但不如酚妥拉明。化合物II具有部分激动活性,发挥非特异性膜稳定作用,并表现出抗纤颤和抗心律失常活性。

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