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评估药物对小鼠突触前多巴胺受体刺激作用的简单方法。

Simple method for evaluation of stimulatory effect of drugs on presynaptic dopamine receptors in mice.

作者信息

Watanabe H

出版信息

J Pharmacol Methods. 1985 Aug;14(1):41-7. doi: 10.1016/0160-5402(85)90041-5.

DOI:10.1016/0160-5402(85)90041-5
PMID:3928976
Abstract

In order to clarify the stimulating activity of presynaptic dopamine (DA) receptors, the ability of drugs to inhibit in vivo accumulation of l-dopa produced by gamma-butyrolactone was estimated in the striatum of mouse treated with an amino acid decarboxylase inhibitor. Apomorphine (0.05-0.5 mg/kg, s.c.) significantly suppressed this accumulation in a dose-related manner. Bromocriptine, lisuride, and ergometrine also reduced it. Methamphetamine (5 and 10 mg/kg, s.c.) diminished striatal l-dopa accumulation and the effects of apomorphine, bromocriptine, and methamphetamine were all blocked by 0.1 mg/kg, i.p., of haloperidol. Ephedrine (100 mg/kg, s.c.) caused a slight decrease in the dopa accumulation although the same dose of cocaine did not change it. These results indicate that the estimation of striatal l-dopa from a single mouse brain is feasible, and dopamine receptor agonists, apomorphine, and ergot alkaloids have stimulatory effects on the activity of presynaptic dopamine receptors of the nigrostriatal dopaminergic neurons of the mouse.

摘要

为了阐明突触前多巴胺(DA)受体的刺激活性,在用氨基酸脱羧酶抑制剂处理的小鼠纹状体中,评估了药物抑制γ-丁内酯产生的左旋多巴体内蓄积的能力。阿扑吗啡(0.05 - 0.5毫克/千克,皮下注射)以剂量相关的方式显著抑制了这种蓄积。溴隐亭、利苏瑞ide和麦角新碱也降低了它。甲基苯丙胺(5和10毫克/千克,皮下注射)减少了纹状体左旋多巴的蓄积,阿扑吗啡、溴隐亭和甲基苯丙胺的作用均被腹腔注射0.1毫克/千克的氟哌啶醇阻断。麻黄碱(100毫克/千克,皮下注射)使多巴蓄积略有下降,而相同剂量的可卡因则无此作用。这些结果表明,从单只小鼠脑中估计纹状体左旋多巴是可行的,多巴胺受体激动剂、阿扑吗啡和麦角生物碱对小鼠黑质纹状体多巴胺能神经元的突触前多巴胺受体活性具有刺激作用。

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