一种M3样毒蕈碱自身受体调节大鼠纹状体内乙酰胆碱的体内释放。

An M3-like muscarinic autoreceptor regulates the in vivo release of acetylcholine in rat striatum.

作者信息

De Boer P, Westerink B H, Rollema H, Zaagsma J, Horn A S

机构信息

Department of Medicinal Chemistry, University of Groningen, The Netherlands.

出版信息

Eur J Pharmacol. 1990 Apr 10;179(1-2):167-72. doi: 10.1016/0014-2999(90)90414-2.

DOI:10.1016/0014-2999(90)90414-2

PMID:2364978

Abstract

Selective muscarinic antagonists were used in an attempt to characterize the muscarinic autoreceptor modulating the release of acetylcholine in the striatum of the rat. In vivo microdialysis was applied to infuse atropine, 4-DAMP (4-diphenylacetoxy-N-methylpiperidine), pirenzepine or AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5, 11-dihydro[2,3-b][1,4]benzodiazepine-6-one), leading to a dose-dependent increase in the overflow of acetylcholine, the order of potency being: atropine greater than 4-DAMP greater than pirenzepine greater than AF-DX 116. We conclude from these data that the muscarinic receptor modulating release in the striatum is of the M3 type.

摘要

使用选择性毒蕈碱拮抗剂试图对调节大鼠纹状体中乙酰胆碱释放的毒蕈碱自身受体进行表征。采用体内微透析法注入阿托品、4-二苯乙酰氧基-N-甲基哌啶（4-DAMP）、哌仑西平或AF-DX 116（11-[[2-[(二乙氨基)甲基]-1-哌啶基]乙酰基]-5,11-二氢[2,3-b][1,4]苯并二氮杂䓬-6-酮），导致乙酰胆碱溢出呈剂量依赖性增加，效力顺序为：阿托品＞4-DAMP＞哌仑西平＞AF-DX 116。从这些数据我们得出结论，调节纹状体释放的毒蕈碱受体为M3型。