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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.

DOI:10.1007/BF01664004
PMID:6267192
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。

相似文献

1
Neurochemical effects of some ergot derivatives: a basis for their antiparkinson actions.某些麦角衍生物的神经化学效应:其抗帕金森作用的基础。
J Neural Transm. 1981;51(1-2):39-59. doi: 10.1007/BF01664004.
2
Bromocriptine and lisuride stimulate the accumulation of cyclic AMP in intact slices but not in homogenates of rat neostriatum.溴隐亭和麦角乙脲能刺激完整切片中环磷酸腺苷(cAMP)的积累,但对大鼠新纹状体匀浆却无此作用。
Neurosci Lett. 1979 Sep;14(1):31-6. doi: 10.1016/0304-3940(79)95339-4.
3
Effects of bromocriptine on central dopaminergic receptors.溴隐亭对中枢多巴胺能受体的影响。
Life Sci. 1976 Jul 15;19(2):225-31. doi: 10.1016/0024-3205(76)90394-5.
4
Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors.美舒麦角及其1,20-N,N-双去甲基代谢物直接与D1和D2受体相互作用。
Eur J Pharmacol. 1983 Nov 11;95(1-2):101-7. doi: 10.1016/0014-2999(83)90272-8.
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D2 dopamine receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in rat striatum.D2多巴胺受体介导的对大鼠纹状体中福斯高林刺激的腺苷酸环化酶活性的抑制作用。
Neurosci Lett. 1985 Aug 30;59(2):177-82. doi: 10.1016/0304-3940(85)90196-x.

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In Vitro Cell Dev Biol Anim. 2009 Sep;45(8):483-9. doi: 10.1007/s11626-009-9191-8. Epub 2009 May 19.
2
Clinical pharmacology of dopamine agonists in Parkinson's disease.帕金森病中多巴胺激动剂的临床药理学
Drugs Aging. 1998 Nov;13(5):381-9. doi: 10.2165/00002512-199813050-00004.
3
Bromocriptine enhancement of responding for conditioned reward depends on intact D1 receptor function.溴隐亭增强对条件性奖励的反应取决于完整的D1受体功能。

本文引用的文献

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pAx and competitive drug antagonism.pAx与竞争性药物拮抗作用。
Br J Pharmacol Chemother. 1949 Sep;4(3):277-80. doi: 10.1111/j.1476-5381.1949.tb00548.x.
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Clinical pharmacokinetics of anti-parkinsonian drugs.抗帕金森病药物的临床药代动力学
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Bromocriptine self-administration and bromocriptine-reinstatement of cocaine-trained and heroin-trained lever pressing in rats.溴隐亭自我给药以及可卡因训练和海洛因训练大鼠按压杠杆行为的溴隐亭复吸实验
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Locomotor-activating effects of the D2 agonist bromocriptine show environment-specific sensitization following repeated injections.D2激动剂溴隐亭的运动激活作用在重复注射后表现出环境特异性致敏。
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Iontophoretically applied dopamine depolarizes and hyperpolarizes the membrane of cat caudate neurons.经离子电渗法施加的多巴胺可使猫尾状核神经元的膜发生去极化和超极化。
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On the mechanism of the antiparkinsonian action of 1-DOPA and bromocriptine: a theoretical and experimental analysis of dopamine receptor sub- and supersensitivity.关于左旋多巴和溴隐亭抗帕金森病作用的机制:多巴胺受体亚敏感性和超敏感性的理论与实验分析
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Aromatic amino acids and modification of parkinsonism.芳香族氨基酸与帕金森病的修饰
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Bromocriptine in Parkinsonism.帕金森病中的溴隐亭
Br Med J. 1974 Nov 23;4(5942):442-4. doi: 10.1136/bmj.4.5942.442.
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Dopamine-sensitive adenylate cyclase in caudate nucleus of rat brain, and its similarity to the "dopamine receptor".大鼠脑尾状核中对多巴胺敏感的腺苷酸环化酶及其与“多巴胺受体”的相似性。
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5-Hydroxydopamine 'tagged' neuronal boutons in rabbit neostriatum: interrelationship between vesicles and axonal membrane.5-羟多巴胺“标记”的兔新纹状体神经元终扣:囊泡与轴突膜之间的相互关系
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Effect of ergot drugs on central catecholamine neurons: evidence for a stimulation of central dopamine neurons.麦角药物对中枢儿茶酚胺能神经元的作用:刺激中枢多巴胺能神经元的证据。
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