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高亲和力的3H-血清素与尾状核的结合:致幻剂和血清素能药物的抑制作用。

High-affinity 3H-serotonin binding to caudate: inhibition by hallucinogens and serotoninergic drugs.

作者信息

Whitaker P M, Seeman P

出版信息

Psychopharmacology (Berl). 1978 Sep 15;59(1):1-5. doi: 10.1007/BF00428022.

Abstract

The specific binding of 3H-serotonin to calf caudate homogenate was studied. The dissociation constant was 2nM and the number of specific sites was 14fmoles/mg protein. Of many drugs tested, inhibition of specific 3H-serotonin binding occurred almost exclusively with serotonin agonists and antagonists. The concentrations for 50% inhibition of 3H-serotonin binding by serotonergic agonists follow: bufotenin, 6nM; 5-methoxytryptamine, 12 nM; psilocin, 35nM; dimethyltryptamine, 220 nM; and tryptamine, 270 nM. The concentrations for the antagonists were: LSD 9.5 nM; methysergide 16nM and metergoline 25nM.

摘要

研究了³H-血清素与小牛尾状核匀浆的特异性结合。解离常数为2nM,特异性结合位点的数量为14飞摩尔/毫克蛋白质。在测试的许多药物中,³H-血清素特异性结合的抑制几乎只发生在血清素激动剂和拮抗剂中。血清素能激动剂对³H-血清素结合产生50%抑制的浓度如下:蟾毒色胺,6nM;5-甲氧基色胺,12 nM;裸盖菇素,35nM;二甲基色胺,220 nM;色胺,270 nM。拮抗剂的浓度为:麦角酰二乙胺9.5 nM;美西麦角16nM;麦角乙脲25nM。

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