N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides:: Human dopamine D4 ligands with high affinity for the 5-HT2A receptor

被引：11

作者：

Arora, J ^{[1
]}

Bordeleau, M ^{[1
]}

Dube, L ^{[1
]}

Jarvie, K ^{[1
]}

Mazzocco, L ^{[1
]}

Peragine, J ^{[1
]}

Tehim, A ^{[1
]}

Egle, I ^{[1
]}

机构：

[1] NPS Pharmaceut, Mississauga, ON L4V 1V7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 23期

关键词：

dopamine; serotonin; schizophrenia; D4; 5-HT2A;

D O I：

10.1016/j.bmcl.2005.08.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-[(3S)-1-benzylpyrrolidin-3-y1]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D-4 (hD(4)) and 5-HT2A receptors. Several compounds displayed selectivity for these receptors versus hD(2) and alpha(1), adrenergic receptors of over 500-fold. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：5253 / 5256

页数：4

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