Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro

被引：18
|
作者：
Lahti, R. A.
Tamminga, C. A.
Carlsson, A.
机构：
[1] Univ Gothenburg, Dept Pharmacol, Sahlgrenska Acad, S-41319 Gothenburg, Sweden
[2] Univ Maryland, Maryland Psychiat Res Ctr, Baltimore, MD USA
[3] UT SW Med Sch, Dept Psychiat, Dallas, TX USA
来源：
JOURNAL OF NEURAL TRANSMISSION | 2007年 / 114卷 / 09期
关键词：
partial dopamine agonist; dopamine; GTPgammaS(35); psychosis;
D O I：
10.1007/s00702-007-0784-7
中图分类号：
R74 [神经病学与精神病学];
学科分类号：
摘要：
The effect of (-)-OSU6162 on the incorporation of GTPgammaS(35) in the membranes of hD(2l)-transfected CHO cells was investigated. In the absence of dopamine the compound exerted a slight but significant stimulating action, suggesting a weak partial agonism. In the presence of dopamine, low concentrations (10 to 100 nM) enhanced the stimulating action of dopamine. This enhancing effect was reversed by higher concentrations of (-)-OSU6162 in a complex biphasic manner. The dopamine-enhancing action is proposed to be mediated by binding to an allosteric site with high affinity and the inhibitory component by a low-affinity binding to the orthosteric site of the dopamine receptor.
引用
收藏
页码：1143 / 1146
页数：4
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