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[阿明和尼布芬同系物的毒性和药理学特性]

[Toxic and pharmacological characteristics of armin and nibufin homologs].

作者信息

Leonov V I

出版信息

Farmakol Toksikol. 1979 May-Jun;42(3):299-302.

PMID:446717
Abstract

The experimental studies of alkylesters of phosphonic and phosphinic acids, close homologues of armine and nibufin, showed this series of compounds to have a strongly marked anticholinesterase action. All the substances produce an inhibitory effect on the central nervous system, raise the tone of the smooth muscles on an isolated strip of rabbit small intestine and induce a miotic pupil in the animals. Introduction of butyl radicals into molecules of phosphonic acid derivatives results in diminution of toxicity and a slight decrease in anticholinesterase activity. By their properties butyl paranitrophenyl esters of ethyl- and butylphosphonic acids are closely related to armine and nibufin.

摘要

对膦酸和次膦酸的烷基酯(与阿明和尼布芬结构相近的同系物)进行的实验研究表明,该系列化合物具有显著的抗胆碱酯酶作用。所有这些物质对中枢神经系统均产生抑制作用,能提高兔小肠离体肠段平滑肌的张力,并使动物瞳孔缩小。将丁基引入膦酸衍生物分子中会导致毒性降低以及抗胆碱酯酶活性略有下降。乙基膦酸和丁基膦酸的对硝基苯基丁酯在性质上与阿明和尼布芬密切相关。

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