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某些新型4-苯基哌啶基脲的抗惊厥活性、单胺氧化酶抑制作用及抗溶血特性

Anticonvulsant activity and monoamine oxidase inhibitory and antihemolytic properties of some newer 4-phenylpiperidino carbamides.

作者信息

Pandey B R, Raman K, Barthwal J P, Parmar S S

出版信息

Res Commun Chem Pathol Pharmacol. 1978 Oct;22(1):199-202.

PMID:725317
Abstract

Six 1-[N-acetyl(4-phenylpiperidino)]-3-aryl carbamides were synthesized, characterized and evaluated for their anticonvulsant, monoamine oxidase inhibitory and antihemolytic properties. These compounds (100 mg/kg, i.p.) provided 10--80% protection against pentylenetetrazol-induced seizures in mice. All carbamides (1 mM) inhibited (34--82%) in vitro activity of rat brain monoamine oxidase and provided 18--51% protection against in vitro hypoosmotic hemolysis of human red blood cells at a final concentration of 1 mM. Low toxicity of these carbamides was reflected by their high approximate LD50 values.

摘要

合成了六种1-[N-乙酰基(4-苯基哌啶基)]-3-芳基脲,并对其进行了表征,评估了它们的抗惊厥、单胺氧化酶抑制和抗溶血特性。这些化合物(100毫克/千克,腹腔注射)对小鼠戊四氮诱导的惊厥提供了10%-80%的保护作用。所有的脲(1毫摩尔)在体外抑制(34%-82%)大鼠脑单胺氧化酶的活性,并在终浓度为1毫摩尔时对人红细胞的体外低渗溶血提供了18%-51%的保护作用。这些脲的低毒性通过其较高的近似半数致死量值得以体现。

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