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某些麦角衍生物的神经化学效应:其抗帕金森作用的基础。

Neurochemical effects of some ergot derivatives: a basis for their antiparkinson actions.

作者信息

Markstein R

出版信息

J Neural Transm. 1981;51(1-2):39-59. doi: 10.1007/BF01664004.

Abstract

Bromocriptine and the two ergoline derivatives, CQ 32-084 and CM 29-712, exert dopamine-like effects in experimental models and have been shown to possess antiparkinsonian activity. Biochemical investigations indicate that they differ in their specificity towards the different dopamine receptor types and, in addition, interact with other neurotransmitter receptors. Bromocriptine appears to be a potent agonist at D2-receptors. Furthermore, it blocks adenylate cyclase coupled serotonin receptors and antagonizes central alpha-adrenergic receptors. The two ergoline derivatives are multiple agonists. CQ 32-084 stimulates both D1- and D2-, and CM 29-712 only D1-receptors. In addition, both compounds stimulate adenylate cyclase coupled serotonin receptors and antagonize central alpha-adrenergic receptors.

摘要

溴隐亭以及两种麦角林衍生物CQ 32 - 084和CM 29 - 712在实验模型中发挥类似多巴胺的作用,并且已被证明具有抗帕金森病活性。生化研究表明,它们对不同类型多巴胺受体的特异性不同,此外,还与其他神经递质受体相互作用。溴隐亭似乎是D2受体的强效激动剂。此外,它能阻断与腺苷酸环化酶偶联的5-羟色胺受体,并拮抗中枢α-肾上腺素能受体。这两种麦角林衍生物是多种激动剂。CQ 32 - 084能刺激D1和D2受体,而CM 29 - 712仅刺激D1受体。此外,这两种化合物都能刺激与腺苷酸环化酶偶联的5-羟色胺受体,并拮抗中枢α-肾上腺素能受体。

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