Quaternary forms of classical muscarinic antagonists distinguish subpopulations of muscarinic receptors: correlation with gallamine-defined subpopulations.
Quaternary forms of classical muscarinic antagonists distinguish subpopulations of muscarinic receptors: correlation with gallamine-defined subpopulations.
复制标题
经典毒蕈碱拮抗剂的四元形式区分毒蕈碱受体亚群：与没食子胺定义的亚群的相关性。
DOI：
10.1016/0006-291x(85)90319-5
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发表时间：
1985
影响因子：
3.1
通讯作者：
Lenox,RH
中科院分区：
文献类型：
--
作者：
Ellis,J;Lenox,RH
阿托品和东莨菪碱抑制[3 H]奎宁环二苯乙酸酯（QNB）的结合，以一种方式，表明结合位点的同质性的大鼠前脑的毒蕈碱受体。在相同条件下，N-甲基-阿托品（NMA）和N-甲基东莨菪碱（NMS）对[3 H]QNB结合的抑制作用与受体亚群的存在一致，这些亚群对这些四级配体的亲和力差异很大。根据NMA和NMS的亲和力定义的亚群与通过使用加拉胺定义的亚群非常相关。这表明，在NMS的结合的异质性解释了一些NMS和gallamine之间的异常相互作用，以前已报道。
Atropine and scopolamine inhibit the binding of [3H] quinuclidinyl benzilate (QNB) to muscarinic receptors of rat forebrain in a manner that suggests homogeneity of the binding sites. Under the same conditions, the inhibition by N-methyl-atropine (NMA) and N-methylscopolamine (NMS) of the binding of [3H]QNB is consistent with the presence of subpopulations of receptors that differ greatly in affinities toward these quaternary ligands. The subpopulations that are defined according to the affinities of NMA and NMS correlate very well with those that are defined by the use of gallamine. It is suggested that the heterogeneity in the binding of NMS explains some of the anomalous interactions between NMS and gallamine that have been reported previously.