Fused aminotetralins:: Novel antagonists with high selectivity for the dopamine D3 receptor

被引：9

作者：

Avenell, KY ^{[1
]}

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Healy, MAM ^{[1
]}

Jeffrey, PM ^{[1
]}

Johnson, CN ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Scott, EE ^{[1
]}

Smith, SA ^{[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 | 1998年 / 8卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(98)00512-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from a series of 2-aminotetralins 1, a novel series of N-[4-(4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine Dg receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2859 / 2864

页数：6

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