YM-50001: A novel, potent and selective dopamine D4 receptor antagonist

被引：18

作者：

Hidaka, K

Tada, S

Matsumoto, M

Ohmori, J

Maeno, K

Yamaguchi, T

机构：

[1] Neuroscience Research, Inst. for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., Tsukuba, lbaraki, 305

来源：

NEUROREPORT | 1996年 / 7卷 / 15-17期

关键词：

YM-50001; dopamine receptor; D4; receptor; D2-like receptor; antagonist;

D O I：

10.1097/00001756-199611040-00028

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

WE investigated some in vitro pharmacological properties of a novel human dopamine D2-like receptor antagonist, YM-50001 [(R)-5-chloro-4-cyclopropylcarbonylamino-2-methoxy-N-[1-(3-methoxybenzyl)-3-pyrrolidinyl]benzamide monooxalate]. Receptor binding studies revealed that YM-50001 had a potent affinity for human D4 receptors (Ki = 5.62 nM). YM-50001 displayed weak or negligible affinity for other neurotransmitter receptors including human D2 and D3 receptors. YM-50001 shifted the dopamine response curve on each human D2-like receptor subtype-mediated low-Km GTPase activity to the right. YM-50001 also exhibited good D4 selectivity with respect to D2-like receptor antagonism in the functional assay. These results indicate that YM-50001 is a novel, potent and selective D4 receptor antagonist.

引用

页码：2543 / 2546

页数：4

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