Selective alkylatation of dopamine D2 and D4 receptors in rat brain by N-(p-isothiocyanatophenethyl)spiperone

被引：2
作者：
Zhang, KH
Tarazi, FI
Kula, NS
Baldessarini, RJ
Neumeyer, JL
机构：
[1] Massachusetts Gen Hosp, McLean Div, Mailman Res Ctr, Neuropharmacol Lab, Belmont, MA 02478 USA
[2] Harvard Univ, Sch Med, Dept Psychiat, Boston, MA 02115 USA
[3] Harvard Univ, Sch Med, Neurosci Program, Boston, MA 02115 USA
来源：
NEUROSCIENCE LETTERS | 1999年 / 274卷 / 03期
关键词：
alkylation; autoradiography; dopamine receptors; 1-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline; N-(p-isothiocyanatophenethyl)spiperone;
D O I：
10.1016/S0304-3940(99)00700-4
中图分类号：
Q189 [神经科学];
学科分类号：
071006 ;
摘要：
Effects of the D-2-like receptor alkylating agent NIPS (N-[p-isothiocyanatophenethyl]spiperone) on dopamine receptors in rat brain were characterized by radioreceptor assays and quantitative autoradiography. NIPS alkylated D-2 and D-4 receptors concentration-dependently in brain sections and transfected cells. NIPS also alkylated both receptors dose-dependently in vivo, with no effect on dopamine D-1-like or serotonin 5-HT2 receptors at a dose that occluded 75% of D-2 and D-4 receptors. Pretreatment with D-2-like receptor selective antagonist haloperidol completely blocked the effects of NIPS. The findings demonstrate that NIPS selectively alkylates D-2 and D-4 receptors, indicating its potential utility for studies of these receptors. (C) 1999 Elsevier Science Ireland Ltd. Atl rights reserved.
引用
收藏
页码：155 / 158
页数：4
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