关于某些毒蕈碱激动剂与竞争性拮抗剂的相互作用位点。
On the site of interaction of some muscarinic agonists and competitive antagonists.
作者信息
Gualtieri F, Romanelli M N, Teodori E
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Firenze.
出版信息
Farmaco. 1989 Oct;44(10):897-909.
The stereochemistry of interaction of several 1,3-oxathiolane muscarinic ligands is considered and discussed. On the basis of the identical absolute configuration of the most affinitive enantiomers of agonists and antagonists it is suggested that the two kinds of ligands interact with an identical binding site, namely the recognition site of Acetylcholine. The hypothesis is extended to other muscarinic antagonists like the bulky esters of choline, 2,2-disubstituted-1,3-dioxolanes and Atropine-like compounds; a model for such an interaction is proposed.
本文对几种1,3-氧硫杂环戊烷类毒蕈碱配体的相互作用立体化学进行了考量和讨论。基于激动剂和拮抗剂最具亲和力对映体相同的绝对构型，提出这两类配体与同一个结合位点相互作用，即乙酰胆碱的识别位点。该假说被扩展至其他毒蕈碱拮抗剂，如胆碱的大分子酯、2,2-二取代-1,3-二氧戊环及阿托品样化合物；并提出了此类相互作用的模型。
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