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胆碱能受体活性位点的分子要求。十六 - 2-或5-烷基或5-苯基-4-甲基-3-氧代-1-二甲基氨基甲基环戊烷甲碘化物的合成及胆碱能活性

Molecular requirements of the active sites of the cholinergic receptors. XVI - Synthesis and cholinergic activity of 2- or 5-alkyl or 5-phenyl-4-methyl-3-oxo-1-dimethylaminomethylcyclopentane methiodide.

作者信息

Pigini M, Brasili L

出版信息

Farmaco Sci. 1981 Feb;36(2):152-8.

PMID:7227502
Abstract

In order to study the cholinergic receptor through affinity chromatography, some derivatives of deoxamuscarone (I a) incorporating alkyl and phenyl substituents at the positions 2 and 5 were synthesized as model compounds. However, the sharp drop in activity and the lack of discrimination between nicotinic and muscarinic receptors exhibited by the compounds discourage their further development as affinity reagents.

摘要

为了通过亲和色谱法研究胆碱能受体,合成了一些在2位和5位带有烷基和苯基取代基的去氧毒扁豆酮(I a)衍生物作为模型化合物。然而,这些化合物所表现出的活性急剧下降以及对烟碱型和毒蕈碱型受体缺乏区分能力,阻碍了它们作为亲和试剂的进一步开发。

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