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塞吲哚对脑5-羟色胺2、多巴胺2及α1受体的急性效应(离体放射受体结合研究)

The acute effect of sertindole on brain 5-HT2, D2 and alpha 1 receptors (ex vivo radioreceptor binding studies).

作者信息

Hyttel J, Nielsen J B, Nowak G

机构信息

H. Lundbeck A/S, Copenhagen, Denmark.

出版信息

J Neural Transm Gen Sect. 1992;89(1-2):61-9. doi: 10.1007/BF01245352.

DOI:10.1007/BF01245352
PMID:1329856
Abstract

The ability of sertindole to influence the ex vivo binding of 3H-ketanserin, 3H-prazosin and 3H-spiperone to 5-HT2 receptors, alpha 1-adrenoceptors and DA D2 receptors, respectively, in rat brain has been studied after acute treatment. Sertindole is a potent, long acting compound which readily passes the blood-brain barrier. It dose-dependently binds to all three receptors types. In line with in vivo behavioural experiments sertindole has the most pronounced effect on 5-HT2 receptors, lower effect on alpha 1-adrenoceptors and the lowest effect on striatal D2 receptors.

摘要

急性给药后,已对塞汀多在大鼠脑中分别影响3H-酮色林、3H-哌唑嗪和3H-螺哌啶与5-HT2受体、α1-肾上腺素能受体和多巴胺D2受体的体外结合能力进行了研究。塞汀多是一种强效、长效化合物,能轻易透过血脑屏障。它对所有三种受体类型均呈剂量依赖性结合。与体内行为实验一致,塞汀多对5-HT2受体的作用最为显著,对α1-肾上腺素能受体的作用较小,对纹状体D2受体的作用最小。

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