Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor

被引：17

作者：

Austin, NE ^{[1
]}

Avenell, KY ^{[1
]}

Boyfield, I ^{[1
]}

Branch, CL ^{[1
]}

Hadley, MS ^{[1
]}

Jeffrey, P ^{[1
]}

Johnson, CN ^{[1
]}

Macdonald, GJ ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Smith, AB ^{[1
]}

Stemp, G ^{[1
]}

Thewlis, KM ^{[1
]}

Vong, AKK ^{[1
]}

Wood, M ^{[1
]}

机构：

[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(00)00505-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from the dopamine D-3 receptor antagonist SE-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinity for the dopamine D3 receptor and selectivity over the D-2 receptor. The 3-acetamido-2-fluorocinnamide derivative 20 gave high D-3 receptor affinity (pK(i) 8.4) with 130-fold selectivity over the D-2 receptor. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2553 / 2555

页数：3

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