1-[2-[(heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists

被引：13

作者：

Bromidge, SM ^{[1
]}

Davies, S ^{[1
]}

Duckworth, DM ^{[1
]}

Forbes, IT ^{[1
]}

Jones, GE ^{[1
]}

Jones, J ^{[1
]}

King, FD ^{[1
]}

Blackburn, TP ^{[1
]}

Holland, V ^{[1
]}

Kennett, GA ^{[1
]}

Lightowler, S ^{[1
]}

Middlemiss, DN ^{[1
]}

Riley, GJ ^{[1
]}

Trail, B ^{[1
]}

Wood, MD ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(00)00365-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 1, 2, 8, 12, 14 and 18 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their therapeutic potential is currently under further investigation. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1867 / 1870

页数：4

共 6 条

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