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R(+)-8-羟基二丙胺四乙酸,一种5-羟色胺1A受体激动剂,可抑制苯丙胺诱导的大鼠纹状体和伏隔核中的多巴胺释放。

R(+)-8-OH-DPAT, a 5-HT1A receptor agonist, inhibits amphetamine-induced dopamine release in rat striatum and nucleus accumbens.

作者信息

Ichikawa J, Kuroki T, Kitchen M T, Meltzer H Y

机构信息

Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH 44106-5000, USA.

出版信息

Eur J Pharmacol. 1995 Dec 12;287(2):179-84. doi: 10.1016/0014-2999(95)00624-9.

DOI:10.1016/0014-2999(95)00624-9
PMID:8749033
Abstract

Systemic administration of R(+)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), a selective serotonin (5-hydroxy-tryptamine, 5-HT)1A receptor agonist (25, 50, and 100 mu g/kg s.c.), administered 30 min prior to d-amphetamine, significantly inhibited the d-amphetamine sulfate (1.0 mg/kg s.c.)-induced increase in extracellular dopamine levels in the striatum and nucleus accumbens of freely moving rats, as determined by in vivo microdialysis. The ability of R(+)-8-OH-DPAT (50 mu g/kg s.c.) to inhibit d-amphetamine sulfate (1.0 mg/kg s.c.)-induced increase in extracellular dopamine levels was abolished by WAY 100,635 (n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride), a selective 5-HT1A receptor antagonist (100 mu g/kg s.c.), administered 5 min prior to R(+)-8-OH-DPAT in both regions. These results indicate that the 5-HT1A receptor may exert an inhibitory effect on amphetamine-induced dopamine release.

摘要

在自由活动的大鼠中,通过体内微透析测定发现,在给予硫酸右苯丙胺(1.0mg/kg,皮下注射)前30分钟,系统性给予R(+)-8-OH-DPAT(8-羟基-2-(二正丙基氨基)四氢萘),一种选择性5-羟色胺(5-羟色胺,5-HT)1A受体激动剂(25、50和100μg/kg,皮下注射),可显著抑制硫酸右苯丙胺诱导的纹状体和伏隔核细胞外多巴胺水平的升高。在两个区域中,在给予R(+)-8-OH-DPAT(50μg/kg,皮下注射)前5分钟给予WAY 100,635(n-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-n-(2-吡啶基)环己烷甲酰胺三盐酸盐),一种选择性5-HT1A受体拮抗剂(100μg/kg,皮下注射),可消除R(+)-8-OH-DPAT抑制硫酸右苯丙胺(1.0mg/kg,皮下注射)诱导的细胞外多巴胺水平升高的能力。这些结果表明,5-HT1A受体可能对苯丙胺诱导的多巴胺释放发挥抑制作用。

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