STUDIES ON MUSCARINIC BINDING-SITES IN HUMAN-BRAIN IDENTIFIED WITH [H-3] PIRENZEPINE
STUDIES ON MUSCARINIC BINDING-SITES IN HUMAN-BRAIN IDENTIFIED WITH [H-3] PIRENZEPINE
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DOI：
10.1111/j.1471-4159.1986.tb12958.x
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发表时间：
1986-01-01
影响因子：
4.7
通讯作者：
RICHELSON, E
中科院分区：
文献类型：
--
作者：
LIN, SC;OLSON, KC;RICHELSON, E
吡renzepine是一种有效的抗毒蕈碱剂，对毒蕈碱受体亚型（M1）具有明显的选择性，以氚化形式用于表征其与人脑组织的结合。特异的[3H]吡仑西平结合表现出快速的结合和解离。通过动力学和竞争结合实验，其skd分别为5.5 nM和9 nM。[3H]匹伦塞平结合与[3H]喹喹啉苄基苯甲酸结合（一种非选择性毒蕈碱拮抗剂）的区域分布表明，这两种放射性配体在13个脑区中最大结合位点的数量显著相关，两者在壳核的结合量最高，在小脑的结合量最少。[3H]匹伦西平的结合率平均为[3H]苯基喹啉酯的57%，范围为20%（小脑）至77%（额叶皮质）。大多数抗抑郁药和抗精神病药对[3H]匹伦西平结合位点的亲和力与先前报道的使用[3H]苯基喹啉酯获得的值没有显著差异。
Pirenzepine, a potent antimuscarinic agent with apparent selectivity for a subtype (M1) of muscarinic receptors, was used in tritiated form to characterize its binding to human brain tissue. Specific [3H]pirenzepine binding showed rapid association and dissociation. From kinetic and competitive binding experiments, itsKDwas 5.5 nMand 9 nM, respectively. Regional distribution of [3H]pirenzepine binding determined in parallel with [3H]quinuclidinyl benzilate binding, a nonselective muscarinic antagonist, indicated a significant correlation for the maximum number of binding sites for the two radioligands in 13 brain regions, with the highest amount of binding for each in the putamen and the least in the cerebellum. Binding for [3H]pirenzepine averaged 57% of that for [3H]quinuclidinyl benzilate, with a range of 20% (cerebellum) to 77% (frontal cortex). Most antidepressants and neuroleptics tested had affinities for [3H]pirenzepine binding sites that were not significantly different from their previously reported values obtained with the use of [3H]quinuclidinyl benzilate.