Quantitative analysis of binding parameters of [3H]N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice
Quantitative analysis of binding parameters of [3H]N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice
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DOI：
10.1016/j.molbrainres.2004.09.012
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发表时间：
2005-01-05
期刊：
影响因子：
--
通讯作者：
Yamada, S
中科院分区：
文献类型：
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作者：
Oki, T;Takagi, Y;Yamada, S
我们研究了[H-3] N-甲基东莨菪碱（[H-3]NMS）在野生型（WT）和M-1-M-5亚型毒蕈碱乙酰胆碱受体（mAChR）基因敲除（KO）小鼠不同脑区和脊髓中的结合参数（K-d，B-max）0。在M-1-M-4 KO小鼠中，[3 H]NMS结合位点的数量在整个中枢神经系统（CNS）中减少，具有显著的区域差异。结果表明，M-1受体在大脑皮层和海马中的密度较高，而M-1和M-4受体在纹状体中的密度最高。M-2受体在丘脑、下丘脑、中脑、脑桥-延髓、小脑和脊髓中的分布以M-2受体为主。这些发现不仅有助于进一步了解mAChR亚型在中枢胆碱能功能中的生理作用，而且有助于开发针对特定亚型的选择性治疗药物。(C)2004 Elsevier B. V.保留所有权利。
We have studied binding parameters (K-d, B-max)0 Of [H-3]N-methylscopolamine ([H-3]NMS) in various brain regions and spinal cord of wildtype (WT) and muscarinic acetylcholine receptor (mAChR) subtype M-1-M-5 knockout (KO) mice. In the M-1-M-4 KO mice, the number of [3H]NMS binding sites was decreased throughout the central nervous system (CNS) with significant regional differences. Our results collectively suggest that M-1 receptor was present in a relatively high density in the cerebral cortex and hippocampus, and the densities of M I and M-4 subtypes were highest in the corpus striatum. M-2 receptor appeared to be the major subtype in the thalamus, hypothalamus, midbrain, pons-medulla, cerebellum and spinal cord. These findings may contribute significantly not only to the further understanding of the physiological roles of mAChR subtypes in the central cholinergic functions, but also to the development of selective therapeutic agents targeting specific subtype. (C) 2004 Elsevier B.V. All rights reserved.