抗精神病药物与从大鼠脑纹状体制备的多巴胺刺激的腺苷酸环化酶。
Antipsychotic drugs and dopamine-stimulated adenylate cyclase prepared from corpus striatum of rat brain.
作者信息
Karobath M, Leitich H
出版信息
Proc Natl Acad Sci U S A. 1974 Jul;71(7):2915-8. doi: 10.1073/pnas.71.7.2915.
Abstract
Antipsychotic drugs and their clinically impotent congeners were examined as inhibitors of dopamine-sensitive adenylate cyclase (EC 4.6.1.1) in cell-free membrane preparations of the caudate-putamen of rat brain. Of 12 neuroleptic drugs with reported antipsychotic efficacy, all inhibit stimulation of adenylate cyclase by 40 muM dopamine at micromolar concentrations. Among 14 other structurally related drugs that are not clinically effective as antipsychotic agents, 12 were almost ineffective while two drugs were moderate inhibitors of dopamine-sensitive adenylate cyclase.
摘要
研究了抗精神病药物及其临床上无活性的类似物对大鼠脑尾状核-壳核无细胞膜制剂中多巴胺敏感腺苷酸环化酶（EC 4.6.1.1）的抑制作用。在12种已报道具有抗精神病疗效的神经安定药物中，所有药物在微摩尔浓度下均能抑制40μM多巴胺对腺苷酸环化酶的刺激。在另外14种结构相关但临床上无抗精神病作用的药物中，12种几乎无效，而有两种药物是多巴胺敏感腺苷酸环化酶的中度抑制剂。
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