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利苏瑞ide对大鼠纹状体匀浆中多巴胺敏感腺苷酸环化酶的刺激作用。

Stimulatory action of lisuride on dopamine-sensitive adenylate cyclase in the rat striatal homogenate.

作者信息

Azuma H, Oshino N

出版信息

Jpn J Pharmacol. 1980 Oct;30(5):629-39. doi: 10.1254/jjp.30.629.

Abstract

Effect of lisuride, an ergot derivative of isolysergic structure, on dopamine-sensitive adenylate cyclase was studied in the homogenate of rat corpus striatum. Stimulatory action of lisuride, similar to the actions of dopamine and apomorphine, on striatal adenylate cyclase was potentiated significantly by guanosine triphosphate (GTP) and by guanyl-5'-yl imidodiphosphate (GMP-PNP), although with lisuride alone, there was only a slight stimulation. The maximal stimulation attained in the presence of GTP corresponded to about 1.4 times the basal rate of cyclic AMP formation in the homogenate and was abolished by an addition of haloperidol. Lisuride at a concentration about 3 microM inhibited stimulation of cyclic AMP formation by dopamine. The effect of lisuride and the extent of potentiation by the guanyl nucleotides were almost comparable to the effects of apomorphine, under corresponding conditions. Thus, lisuride, like apomorphine, acts as a partial agonist-antagonist, and has the ability to stimulate the dopamine-sensitive adenylate cyclase in the rat corpus striatum.

摘要

在大鼠纹状体匀浆中研究了异麦角酰结构的麦角衍生物利苏瑞对多巴胺敏感的腺苷酸环化酶的作用。利苏瑞对纹状体腺苷酸环化酶的刺激作用,类似于多巴胺和阿扑吗啡的作用,可被三磷酸鸟苷(GTP)和5'-鸟苷酰亚胺二磷酸(GMP-PNP)显著增强,尽管单独使用利苏瑞时,只有轻微的刺激作用。在GTP存在下达到的最大刺激作用相当于匀浆中环磷酸腺苷(cAMP)形成基础速率的约1.4倍,并可被加入氟哌啶醇所消除。浓度约为3 microM的利苏瑞抑制多巴胺对cAMP形成的刺激作用。在相应条件下,利苏瑞的作用及鸟苷酸增强的程度与阿扑吗啡的作用几乎相当。因此,利苏瑞与阿扑吗啡一样,作为部分激动剂-拮抗剂,具有刺激大鼠纹状体中多巴胺敏感的腺苷酸环化酶的能力。

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