N-(substituted-phenyl) piperazines: Antagonists with high binding and functional selectivity for dopamine D-4 receptors

被引：17

作者：

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Healy, MAM ^{[1
]}

Johns, A ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Scott, EE ^{[1
]}

Smith, SA ^{[1
]}

Stemp, G ^{[1
]}

Wilson, K ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,HARLOW CM19 5AW,ESSEX,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 11期

关键词：

D O I：

10.1016/0960-894X(96)00198-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-(substituted-phenyl) piperazine derivatives was prepared as selective antagonists of the dopamine D-4 receptor. Many analogues possessed a binding selectivity of over 100 fold for D-4 over D-2 receptors. In functional studies in the microphysiometer, compound 24 showed a selectivity over dopamine D-2 receptors of greater than 1000 fold. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1227 / 1232

页数：6

共 12 条

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