Perry E K, Smith C J, Perry R H, Whitford C, Johnson M, Birdsall N J
Department of Neuropathology, Newcastle General Hospital, Newcastle upon Tyne, UK.
J Chem Neuroanat. 1989 Jul-Aug;2(4):189-99.
The distribution of nicotinic and muscarinic receptor subtypes was examined in human brain tissue obtained at autopsy from neurologically normal adult (50-60 years) individuals. Membrane preparations from 15 brain regions were examined for nicotinic (L-[3H]nicotine) binding, both M1 and M2 muscarinic receptor binding (distinguished on the basis of pirenzepine affinity) and high (H) and low (L) affinity muscarinic agonist binding (distinguished on the basis of carbachol displacement). Total muscarinic receptor binding sites were relatively high in striatal and cortical areas, where both M1 subtype and agonist binding type L predominated, compared with thalamic, nigral and cerebellar regions and spinal cord, where the M2 subtype and agonist binding type H predominated. Nicotinic receptor binding sites (predominantly high affinity, measured at low ligand concentrations) did not parallel any of the muscarinic subtypes, being concentrated in thalamic, neocortical and striatal regions. Scatchard analysis indicated the presence of both high and low affinity nicotinic sites, the numbers of the latter generally exceeding the former by over one order of magnitude. Neither muscarinic nor nicotinic receptor binding sites were closely related to the distribution of the cholinergic neuronal marker, choline acetyltransferase, suggesting that individual cholinergic pathways may be distinguished by the relative proportion of the different types of cholinergic receptors present.
对从神经功能正常的成年（50 - 60岁）个体尸检获取的人脑组织中烟碱样和毒蕈碱样受体亚型的分布进行了研究。检测了来自15个脑区的膜制剂的烟碱样（L - [³H]尼古丁）结合、M1和M2毒蕈碱样受体结合（根据哌仑西平亲和力区分）以及高（H）和低（L）亲和力毒蕈碱样激动剂结合（根据卡巴胆碱置换区分）。与丘脑、黑质、小脑区域和脊髓相比，纹状体和皮质区域的总毒蕈碱样受体结合位点相对较高，在纹状体和皮质区域M1亚型和激动剂结合类型L占主导，而在丘脑、黑质、小脑区域和脊髓中M2亚型和激动剂结合类型H占主导。烟碱样受体结合位点（主要是高亲和力，在低配体浓度下测量）与任何毒蕈碱样亚型均不平行，集中在丘脑、新皮质和纹状体区域。Scatchard分析表明存在高亲和力和低亲和力烟碱样位点，后者的数量通常比前者超过一个数量级以上。毒蕈碱样和烟碱样受体结合位点均与胆碱能神经元标记物胆碱乙酰转移酶的分布无密切关系，这表明个体胆碱能通路可能由存在的不同类型胆碱能受体的相对比例来区分。
