A novel series of 2-aminotetralins with high affinity and selectivity for the dopamine D-3 receptor

被引：18

作者：

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Johnson, CN ^{[1
]}

Riley, GJ ^{[1
]}

Scott, EE ^{[1
]}

Stacey, R ^{[1
]}

Stemp, G ^{[1
]}

Thewlis, KM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(97)00350-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of N-[4-(4-Phenylbenzoylamino)butyl]-1,2,3,4-tetrahydro-2-naphthylamines with high affinity and selectivity for the dopamine D-3 receptor has been prepared. The 5-cyclopropylmethyloxy 3j, methanesulfonyloxy 3k and trifluoromethanesulfonyloxy 3l derivatives represent some of the highest affinity (pKi's 8.6-8.9) and most selective (200-320-fold) dopamine D-3 receptor antagonists reported to date. (C) 1997 Elsevier Science Ltd.

引用

页码：1995 / 1998

页数：4

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