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D2拮抗剂舒必利对大鼠脑多巴胺能区域葡萄糖利用的刺激作用。

Stimulatory effect of the D2 antagonist sulpiride on glucose utilization in dopaminergic regions of rat brain.

作者信息

Pizzolato G, Soncrant T T, Larson D M, Rapoport S I

出版信息

J Neurochem. 1987 Aug;49(2):631-8. doi: 10.1111/j.1471-4159.1987.tb02910.x.

DOI:10.1111/j.1471-4159.1987.tb02910.x
PMID:2955080
Abstract

Local cerebral glucose utilization (LCGU) was measured, using the quantitative autoradiographic [14C]2-deoxy-D-glucose method, in 56 brain regions of 3-month-old, awake Fischer-344 rats, after intraperitoneal administration of sulpiride (SULP) 100 mg/kg. SULP, an "atypical" neuroleptic, is a selective antagonist of D2 dopamine receptors. LCGU was reduced in a few nondopaminergic regions at 1 h after drug administration. Thereafter, SULP progressively elevated LCGU in many other regions. At 3 h, LCGU was elevated in 23% of the regions examined, most of which are related to the CNS dopaminergic system (caudate-putamen, nucleus accumbens, olfactory tubercle, lateral habenula, median eminence, paraventricular hypothalamic nucleus). Increases of LCGU were observed also in the suprachiasmatic nucleus, lateral geniculate, and inferior olive. These effects of SULP on LCGU differ from the effects of the "typical" neuroleptic haloperidol, which produces widespread decreases in LCGU in the rat brain. Selective actions on different subpopulations of dopamine receptors may explain the different effects of the two neuroleptics on brain metabolism, which correspond to their different clinical and behavioral actions.

摘要

采用定量放射自显影[14C]2-脱氧-D-葡萄糖法,在腹腔注射100mg/kg舒必利(SULP)后,对3月龄清醒的Fischer-344大鼠的56个脑区进行局部脑葡萄糖利用(LCGU)测定。SULP是一种“非典型”抗精神病药物,是D2多巴胺受体的选择性拮抗剂。给药后1小时,少数非多巴胺能区域的LCGU降低。此后,SULP在许多其他区域逐渐升高LCGU。在3小时时,在所检查的区域中有23%的LCGU升高,其中大多数与中枢神经系统多巴胺能系统有关(尾状核-壳核、伏隔核、嗅结节、外侧缰核、正中隆起、室旁下丘脑核)。在视交叉上核、外侧膝状体和下橄榄核中也观察到LCGU增加。SULP对LCGU的这些作用与“典型”抗精神病药物氟哌啶醇的作用不同,氟哌啶醇会使大鼠脑中的LCGU普遍降低。对不同多巴胺受体亚群的选择性作用可能解释了这两种抗精神病药物对脑代谢的不同作用,这与它们不同的临床和行为作用相对应。

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