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[3H]N-丙基去甲阿扑吗啡在小鼠脑内的区域活体结合。中枢多巴胺受体标记的证据。

Regional in vivo binding of [3H]N-propylnorapomorphine in the mouse brain. Evidence for labelling of central dopamine receptors.

作者信息

Köhler C, Fuxe K, Ross S B

出版信息

Eur J Pharmacol. 1981 Jul 10;72(4):397-402. doi: 10.1016/0014-2999(81)90584-7.

DOI:10.1016/0014-2999(81)90584-7
PMID:7274333
Abstract

Tail vein injections of [3H]N-propylnorapomorphine ([3H]NPA) in male mice resulted in a dose-related accumulaton of radioactivity in the following brain regions: striatum (max), olfactory tubercle and cerebellum (min). The specific binding was saturable with increasing concentrations of the drug and stereospecifically displaced by (+) butaclamol. Dopamine agonist (apomorphine, NPA and bromocriptine) and antagonists (spiperone, haloperidol, (+) butaclamol and I-sulpiride) all caused dose-dependent prevention of [3H]NPA binding. Mianserin, phenoxybenzamine and propranolol did not prevent the in vivo [3H]NPA binding suggesting that [3H]NPA binds specifically to dopamine receptors in the striatum and the olfactory tubercle of the mouse.

摘要

对雄性小鼠进行尾静脉注射[3H]N-丙基去甲阿朴吗啡([3H]NPA)后,在以下脑区会出现与剂量相关的放射性蓄积:纹状体(最高)、嗅结节和小脑(最低)。随着药物浓度增加,特异性结合具有饱和性,且可被(+)布他拉莫立体特异性取代。多巴胺激动剂(阿朴吗啡、NPA和溴隐亭)和拮抗剂(螺哌隆、氟哌啶醇、(+)布他拉莫和I-舒必利)均导致[3H]NPA结合呈剂量依赖性减少。米安色林、酚苄明和普萘洛尔不能阻止体内[3H]NPA结合,这表明[3H]NPA在小鼠纹状体和嗅结节中特异性结合多巴胺受体。

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