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双环胺对豚鼠回肠中的M1和M2毒蕈碱受体具有鉴别作用。

Dicyclomine discriminates between M1- and M2-muscarinic receptors in the guinea-pig ileum.

作者信息

Kilbinger H, Stein A

机构信息

Pharmakologisches Institut Universität, Mainz, F.R.G.

出版信息

Br J Pharmacol. 1988 Aug;94(4):1270-4. doi: 10.1111/j.1476-5381.1988.tb11647.x.

DOI:10.1111/j.1476-5381.1988.tb11647.x
PMID:3207984
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1854096/
Abstract
  1. The affinity of the antagonist dicyclomine for subtypes of muscarinic receptors has been assessed in the myenteric plexus-longitudinal muscle preparation of the guinea-pig. 2. Dicyclomine had a high affinity (pA2 9.13) for the neuronal M1-receptor whose activation by pilocarpine causes an increase in acetylcholine release. Dicyclomine had a low affinity for both the prejunctional M2-receptor (pA2 7.61) mediating inhibition of the electrically-evoked acetylcholine release and the postjunctional M2-receptor (pA2 7.21). 3. It is concluded that dicyclomine distinguishes between M1- and M2-muscarinic receptors in functional experiments.
摘要
  1. 已在豚鼠的肠肌丛-纵行肌制备物中评估了拮抗剂双环维林对毒蕈碱受体亚型的亲和力。2. 双环维林对神经元M1受体具有高亲和力(pA2 9.13),毛果芸香碱激活该受体可导致乙酰胆碱释放增加。双环维林对介导电诱发乙酰胆碱释放抑制的节前M2受体(pA2 7.61)和节后M2受体(pA2 7.21)均具有低亲和力。3. 得出的结论是,在功能实验中双环维林可区分M1和M2毒蕈碱受体。

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Comparison of affinities of muscarinic antagonists to pre- and postjunctional receptors in the guinea-pig ileum.豚鼠回肠中毒蕈碱拮抗剂对节前和节后受体亲和力的比较。
Eur J Pharmacol. 1984 Aug 17;103(3-4):313-20. doi: 10.1016/0014-2999(84)90492-8.
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Muscarinic receptor subtypes: a critique of the current classification and a proposal for a working nomenclature.毒蕈碱受体亚型:对当前分类的批判及实用命名法的建议
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Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine.选择性M1毒蕈碱受体拮抗剂苯海索和双环维林的结合及功能特征
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Antimuscarinic and noncompetitive antagonist properties of dicyclomine hydrochloride in isolated human and rabbit bladder muscle.
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