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D2多巴胺受体介导的对大鼠纹状体中福斯高林刺激的腺苷酸环化酶活性的抑制作用。

D2 dopamine receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in rat striatum.

作者信息

Battaglia G, Norman A B, Hess E J, Creese I

出版信息

Neurosci Lett. 1985 Aug 30;59(2):177-82. doi: 10.1016/0304-3940(85)90196-x.

Abstract

Forskolin markedly stimulates striatal adenylate cyclase activity in a concentration-dependent manner, and at 10(-4) M produces an approximate 40-fold increase in enzyme activity above basal levels. Dopamine (in the presence of 100 nM SCH 23390), bromocryptine and quinpirole (LY 171555) significantly inhibit both basal and forskolin-stimulated adenylate cyclase activity. There is a significant increase in the absolute but not in the percent inhibition of enzyme activity by dopaminergic agonists as a function of forskolin concentration. This inhibition is agonist-concentration dependent and antagonized by the D2 antagonist, spiperone. These results suggest that forskolin may be used as a tool for amplifying the abolute D2-receptor-mediated inhibition of adenylate cyclase in rat striatal homogenates.

摘要

福司可林以浓度依赖的方式显著刺激纹状体腺苷酸环化酶活性,在10^(-4) M时,酶活性比基础水平增加约40倍。多巴胺(在100 nM SCH 23390存在下)、溴隐亭和喹吡罗(LY 171555)显著抑制基础和福司可林刺激的腺苷酸环化酶活性。多巴胺能激动剂对酶活性的绝对抑制作用显著增加,但抑制百分比没有增加,这是福司可林浓度的函数。这种抑制作用是激动剂浓度依赖性的,并被D2拮抗剂螺哌隆拮抗。这些结果表明,福司可林可作为一种工具,用于放大大鼠纹状体匀浆中绝对的D2受体介导的腺苷酸环化酶抑制作用。

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