Suppr超能文献

中枢神经系统中的麦角生物碱和环核苷酸。

Ergot alkaloids and cyclic nucleotides in the CNS.

作者信息

Trabucchi M, Hofmann M, Montefusco O, Spano P F

出版信息

Pharmacology. 1978;16 Suppl 1:150-55. doi: 10.1159/000136816.

Abstract

Ergotamine and dihydroergotamine show a higher blocking effect towards the dopamine-induced stimulation of adenylate cyclase activity than to the apomorphine-induced stimulation. This could reflect a possible specificity of the compound to dopaminergic receptor. Bromocriptine blocks in a more competitive way the activation of adenylate cyclase induced in vitro by dopamine, but increases the levels of cAMP in rat striatum in vivo. This effect is blocked by haloperidol and reserpine when given together with bromocriptine. On the base of the biochemical observation and various behavioral data the drug has been used in the treatment of parkinsonism with contrasting results and of Huntington's chorea. Moreover, bromocriptine induces a marked decrease of cGMP levels in cerebellum such as haloperidol and chloropromazine while apomorphine and other dopaminergic drugs increase the levels of cGMP. At the dose of 1 mg/kg, bromocriptine as well as DH-ergotoxine markedly reduces the levels of striatal DOPAC.

摘要

麦角胺和二氢麦角胺对多巴胺诱导的腺苷酸环化酶活性刺激的阻断作用比对阿扑吗啡诱导的刺激更强。这可能反映了该化合物对多巴胺能受体的潜在特异性。溴隐亭以更具竞争性的方式阻断多巴胺在体外诱导的腺苷酸环化酶激活,但在体内可增加大鼠纹状体中cAMP的水平。当与溴隐亭一起给药时,氟哌啶醇和利血平可阻断这种作用。基于生化观察和各种行为数据,该药物已用于治疗帕金森病,但结果不一,也用于治疗亨廷顿舞蹈病。此外,溴隐亭可使小脑cGMP水平显著降低,氟哌啶醇和氯丙嗪也有此作用,而阿扑吗啡和其他多巴胺能药物则可增加cGMP水平。在1mg/kg的剂量下,溴隐亭以及二氢麦角毒碱可显著降低纹状体中DOPAC的水平。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验