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具有1,3-氧硫杂环戊烷核的手性毒蕈碱激动剂:对豚鼠回肠、心房及大鼠膀胱离体标本的对映体选择性和组织选择性

Chiral muscarinic agonists possessing a 1,3-oxathiolane nucleus: enantio- and tissue-selectivity on isolated preparations of guinea-pig ileum and atria and of rat urinary bladder.

作者信息

Angeli P, Brasili L, Giannella M, Gualtieri F, Picchio M T, Teodori E

机构信息

Dipartimento di Scienze Chimiche, Universitá di Camerino, Italy.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1988 Mar;337(3):241-5. doi: 10.1007/BF00168833.

Abstract

Racemate and corresponding enantiomers of muscarinic agonists carrying a 1,3-oxathiolane nucleus were studied on isolated preparations of guinea-pig ileum and atria and of rat urinary bladder. The efficacy of these agonists were determined according to the method of Furchgott and Bursztyn (1967) and enantio-selectivity and tissue-selectivity were investigated. The enantio-selectivities of the most potent compounds studied (expressed as the ratio of potencies or affinities of the enantiomers) vary significantly from tissue to tissue, supporting the view that M2 receptors are not homogeneous. In particular, the data all indicate that the ileal receptors are different to the atrial and bladder ones.

摘要

对带有1,3 - 氧硫杂环戊烷核心的毒蕈碱激动剂的外消旋体和相应对映体,在豚鼠回肠、心房以及大鼠膀胱的离体标本上进行了研究。这些激动剂的效能根据Furchgott和Bursztyn(1967年)的方法测定,并研究了对映体选择性和组织选择性。所研究的最有效化合物的对映体选择性(以对映体的效能或亲和力之比表示)在不同组织间有显著差异,这支持了M2受体并非均一的观点。特别是,所有数据均表明回肠受体与心房和膀胱受体不同。

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