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[多巴胺受体激动剂与拮抗剂在多巴胺合成及代谢方面的相互作用]

[Interactions of dopamine receptor agonists and antagonists with regard to dopamine synthesis and metabolism].

作者信息

Kehr W

出版信息

Arzneimittelforschung. 1976;26(6):1086-8.

PMID:9107
Abstract

Intraperitioneal injection of d-amphetamine sulfate, 0.3-3 mg/kg, led to a marked rise in dopa formation in the dopamine rich areas c. striatum and mesolibbic cortex of the rat brain inhibiton of the aromatic amino acid decarboxylase with 3-hydroxybenzylhydrazine HCL (NSD 1015). However, amphetamine given in a dose of 10 mg/kg decreased the tyrosine hydroxylation rate in the mesolimbic cortex as well as the norepinephrine containing neocortex. In combination with haloperidol the stimulating effect of the neuroleptic on dopa formation was markedly potentiated by amphetamine in rat forebrain. Also, amphetamine potentiated the haloperidol induced increase in dopamine release in vivo measured as 3-methoxytyramine formation. The functional antagonists haloperidol and d-amphetamine appear to have synergistic effects on dopaminergic neurons.

摘要

腹腔注射0.3 - 3毫克/千克硫酸右苯丙胺,会使大鼠脑中富含多巴胺的区域(尾状核和中脑边缘皮质)的多巴形成显著增加,而用盐酸3 - 羟基苄肼(NSD 1015)抑制芳香族氨基酸脱羧酶后则不然。然而,10毫克/千克剂量的苯丙胺会降低中脑边缘皮质以及含去甲肾上腺素的新皮质中的酪氨酸羟化率。在大鼠前脑中,苯丙胺与氟哌啶醇联合使用时,该抗精神病药物对多巴形成的刺激作用会被显著增强。此外,苯丙胺增强了氟哌啶醇诱导的体内多巴胺释放增加,这是以3 - 甲氧基酪胺的形成为指标来衡量的。功能性拮抗剂氟哌啶醇和右苯丙胺似乎对多巴胺能神经元具有协同作用。

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