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取代哌啶的中枢神经系统抑制、镇痛及单胺氧化酶抑制特性

Central nervous system depressant, analgesic and monoamine oxidase inhibitory properties of substituted piperidines.

作者信息

Pandey B R, Agrawal D K, Parmar S S, Willson W W, Mayer G G

出版信息

Res Commun Chem Pathol Pharmacol. 1984 Jan;43(1):173-6.

PMID:6701401
Abstract

Eight 1-(arylaminothiocarbonyl)-4-hydroxy-4-phenyl piperidines were evaluated for their central nervous system depressant, analgesic, and monoamine oxidase inhibitory properties. The central nervous system depressant property of these substituted piperidines was reflected by their ability to potentiate pentobarbital-induced sleep in mice ranging from 18.3 to 58.5 minutes. The analgesic activity possessed by these substituted piperidines, with the exception of one compound, was shown by their ability to provide 16.7 to 50 percent protection against tail pinch response in mice. All substituted piperidines (1 mM) inhibited in vitro activity of rat brain monoamine oxidase with the degree of inhibition ranging from 17.2 to 18.3 percent.

摘要

对8种1-(芳基氨基甲酰基)-4-羟基-4-苯基哌啶进行了中枢神经系统抑制、镇痛和单胺氧化酶抑制特性的评估。这些取代哌啶的中枢神经系统抑制特性表现为,它们能使小鼠戊巴比妥诱导的睡眠时间延长18.3至58.5分钟。除一种化合物外,这些取代哌啶均具有镇痛活性,表现为能使小鼠对夹尾反应的保护率达到16.7%至50%。所有取代哌啶(1 mM)均能抑制大鼠脑单胺氧化酶的体外活性,抑制程度在17.2%至18.3%之间。

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Res Commun Chem Pathol Pharmacol. 1984 Jan;43(1):173-6.
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