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三环类抗抑郁药与大鼠脑纹状体中对多巴胺敏感的腺苷酸环化酶

Tricyclic antidepressive drugs and dopamine-sensitive adenylate cyclase from rat brain striatum.

作者信息

Karobath M E

出版信息

Eur J Pharmacol. 1975 Feb;30(2):159-63. doi: 10.1016/0014-2999(75)90095-3.

Abstract

Tricyclic antidepressant drugs were examined as inhibitors of dopamine-sensitive adenylate cyclase in a cell-free homogenate of rat brain striatum. Amitriptyline (Ki 0.17 muM) and doxepin (Ki 0.24 muM) were found to be potent inhibitors of dopamine-sensitive adenylate cyclase, chlorimipramine (Ki 0.59 muM) and nortriptyline (Ki 0.50 muM) were moderate inhibitors and imipramine, desmethylimipramine, protriptyline and melitracene were weak inhibitors with Ki values higher than 1 muM.

摘要

三环类抗抑郁药作为大鼠脑纹状体无细胞匀浆中多巴胺敏感腺苷酸环化酶的抑制剂进行了研究。发现阿米替林(Ki 0.17 μM)和多塞平(Ki 0.24 μM)是多巴胺敏感腺苷酸环化酶的强效抑制剂,氯米帕明(Ki 0.59 μM)和去甲替林(Ki 0.50 μM)是中度抑制剂,而丙咪嗪、去甲丙咪嗪、普罗替林和美利曲辛是弱抑制剂,其Ki值高于1 μM。

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