[抗精神病药物对人壳核中多巴胺D1和D2受体的抑制作用]

[The inhibition of dopamine D1 and D2 receptors in human putamen by antipsychotic drugs].

作者信息

Kobayashi T, Shimizu H, Toru M

机构信息

Department of Psychiatry, Shinshu University School of Medicine, Nagano, Japan.

出版信息

Yakubutsu Seishin Kodo. 1990 Jun;10(2):331-4.

PMID:1979198

Abstract

The inhibition of 3H-SCH 23390 (D1), 3H-spiperone (D2), and 3H-YM-09151 (D2) binding to human putamen membranes by four antipsychotic drugs was studied. Two substituted benzamides, (-)-sulpiride and YM-09151, weakly inhibited specific 3H-SCH 23390 binding to D1 receptor sites. The inhibition of 3H-SCH 23390 binding by haloperidol and chlorpromazine was also weak in the 10(-8)-10(-6) M range. All four drugs potently inhibited 3H-spiperone binding, with the following rank order of potency: haloperidol greater than YM-09151 greater than (-)-sulpiride greater than chlorpromazine. 3H-YM-09151 binding was potently displaced by YM-09151 (10(-9) M) and weakly displaced by (-)-sulpiride (10(-7) M). The potency of inhibition by haloperidol and chlorpromazine was in the 10(-8) M order.

摘要

研究了四种抗精神病药物对3H-SCH 23390（D1）、3H-螺哌隆（D2）和3H-YM-09151（D2）与人壳核膜结合的抑制作用。两种取代苯甲酰胺，（-）-舒必利和YM-09151，对3H-SCH 23390与D1受体位点的特异性结合有微弱抑制作用。在10（-8）-10（-6）M范围内，氟哌啶醇和氯丙嗪对3H-SCH 23390结合的抑制作用也较弱。所有四种药物均能有效抑制3H-螺哌隆结合，其效力顺序如下：氟哌啶醇＞YM-09151＞（-）-舒必利＞氯丙嗪。3H-YM-09151结合被YM-09151（10（-9）M）有效取代，被（-）-舒必利（10（-7）M）微弱取代。氟哌啶醇和氯丙嗪的抑制效力在10（-8）M级别。