DISTRIBUTION OF MUSCARINIC RECEPTOR SUBTYPES IN RAT-BRAIN AS DETERMINED IN BINDING-STUDIES WITH AF-DX 116 AND PIRENZEPINE
DISTRIBUTION OF MUSCARINIC RECEPTOR SUBTYPES IN RAT-BRAIN AS DETERMINED IN BINDING-STUDIES WITH AF-DX 116 AND PIRENZEPINE
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DOI：
10.1016/0024-3205(87)90031-2
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发表时间：
1987-03-02
期刊：
影响因子：
6.1
通讯作者：
LADINSKY, H
中科院分区：
文献类型：
--
作者：
GIRALDO, E;HAMMER, R;LADINSKY, H
选择性毒蕈碱受体拮抗剂AF DX 116和哌仑西平（PZ）与~ 3 H-N-甲基东莨菪碱（3 H-N-methylscopolamine，3 H-N-methylscopolamine）的体外竞争结合实验表明，毒蕈碱受体亚型在大鼠脑的不同区域有特征性分布。基于非线性最小二乘分析，结合数据与三种不同亚型的存在相容：M1受体（对PZ的高亲和力）、心脏M2受体（对AF-DX 116的高亲和力）和颗粒M2受体（对PZ和AF-DX 116的低亲和力）。海马中M1受体的比例最高，而小脑和下丘脑分别是心脏M2和腺体M2受体比例最大的区域。在某些脑区，根据亚型的相对比例，观察到AF-DX 116和PZ的平坦结合曲线。基于这些数据，在不同的大脑区域的亚型的近似分布模式。
In vitro competition binding experiments with the selective muscarinic antagonists AF-DX 116 and pirenzepine (PZ) vs 3H-N-methylscopolamine as radioligand revealed a characteristic distribution of muscarinic receptor subtypes in different regions of rat brain. Based on non linear least squares analysis, the binding data were compatible with the presence of three different subtypes: the M1 receptor (high affinity for PZ), the cardiac M2 receptor (high affinity for AF-DX 116) and the grandular M2 receptor (low affinity for PZ and AF-DX 116). The highest proportion of M1 receptors was found in the hippocampus, whilst the cerebellum and the hypothalamus were the regions with the largest fraction of the cardiac M2 and glandular M2 receptors, respectively. In certain brain areas, depending on the relative proportions of the subtypes, flat binding curves were seen for AF-DX 116 and PZ. Based on these data, an approximate distribution pattern of the subtypes in the various brain regions is presented.