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四种麦角衍生物的神经化学和神经药理学研究:溴隐亭、双氢麦角毒碱、CF 25 - 397和CM 29 - 712。

Neurochemical and neuropharmacological investigations with four ergot derivatives: bromocriptine, dihydroergotoxine, CF 25-397 and CM 29-712.

作者信息

Vigouret J M, Bürki H R, Jaton A L, Züger P E, Loew D M

出版信息

Pharmacology. 1978;16 Suppl 1:156-73. doi: 10.1159/000136817.

Abstract

Neurochemical and neuropharmacological investigations with four ergot derivatives reveal differential pharmacodynamic effects of these compounds. Bromocriptine and CM 29-712 showed actions typical of postsynaptic dopamine receptor stimulants, in particular in the extrapyramidal system. CM 29-712 proved to be more potent than bromocriptine, with an early onset of action. CF 25-397 and dihydroergotoxine, while not showing all actions typical of central dopamine agonists, appeared to exert some of their effects by means of a stimulation of central serotoninergic sites. In the rat sleep-wakefulness cycles and in reserpine-induced ponto-geniculooccipital waves in the cat, they mimicked the effects of 5-hydroxytryptophan. In the latter test, CF 25-397 proved to be particularly potent. In addition, bromocriptine, dihydroergotoxine and CM 29-712 showed neurochemical effects consistent with central alpha-adrenergic blockade or an enhanced impulse flow in central noradrenergic neurons.

摘要

对四种麦角衍生物进行的神经化学和神经药理学研究揭示了这些化合物不同的药效学作用。溴隐亭和CM 29 - 712表现出突触后多巴胺受体兴奋剂的典型作用,尤其是在锥体外系。事实证明,CM 29 - 712比溴隐亭更有效,且起效早。CF 25 - 397和双氢麦角毒碱虽然未表现出中枢多巴胺激动剂的所有典型作用,但似乎通过刺激中枢5 -羟色胺能位点发挥了一些作用。在大鼠睡眠 - 觉醒周期以及猫中利血平诱导的脑桥 - 膝状体 - 枕叶波试验中,它们模拟了5 -羟色氨酸的作用。在后者的试验中,CF 25 - 397被证明特别有效。此外,溴隐亭、双氢麦角毒碱和CM 29 - 712表现出与中枢α -肾上腺素能阻断或中枢去甲肾上腺素能神经元冲动流增强一致的神经化学效应。

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