多巴胺能化合物与胆碱能化合物对脑内多巴胺激活的腺苷酸环化酶的相反作用。

Opposing effects of dopaminergic to cholinergic compounds on a cerebral dopamine-activated adenylate cyclase.

作者信息

Tang L C, Cotzias G C

出版信息

Proc Natl Acad Sci U S A. 1977 Feb;74(2):769-73. doi: 10.1073/pnas.74.2.769.

DOI:10.1073/pnas.74.2.769

PMID:265541

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC392375/

Abstract

In contrast to antipsychosis drugs which inhibit the dopamine-activated adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] of caudate nucleus, dopaminergic drugs for treatment of Parkinson's disease stimulate this cyclase. Stimulants and inhibitors of cholinergic neurons inhibited this adenylate cyclase activity competitively and specifically. Thus, the mechanism by which dopaminergic medications ameliorate the effects of Parkinson's disease includes activation of the dopamine-sensitive adenylate cyclase. Excessive activation might be present during the psychotic episodes seen in patients with parkinsonism who are overtreated. The enzymatic effects of the drugs that affect cholinergic mechanisms seem to be generally in keeping with the pharmacological reciprocity between psychoses and extrapyramidal function, except for the anticholinergic ones which inhibited this cyclase although they can be hallucinogenic.

摘要

与抑制尾状核中多巴胺激活的腺苷酸环化酶[ATP焦磷酸裂解酶（环化），EC 4.6.1.1]的抗精神病药物相反，用于治疗帕金森病的多巴胺能药物会刺激这种环化酶。胆碱能神经元的兴奋剂和抑制剂竞争性且特异性地抑制这种腺苷酸环化酶活性。因此，多巴胺能药物改善帕金森病症状的机制包括激活对多巴胺敏感的腺苷酸环化酶。在接受过度治疗的帕金森病患者出现的精神病发作期间，可能存在过度激活的情况。影响胆碱能机制的药物的酶促作用似乎总体上与精神病和锥体外系功能之间的药理学相互关系相符，但抗胆碱能药物除外，尽管它们可能会导致幻觉，但却抑制了这种环化酶。