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

Authors
Bromidge, SM Davies, S Duckworth, DM Forbes, IT Jones, GE Jones, J King, FD Blackburn, TP Holland, V Kennett, GA Lightowler, S Middlemiss, DN Riley, GJ Trail, B Wood, MD
Citation
Sm. Bromidge et al., 1-[2-[(heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orallyactive 5-HT2C receptor inverse agonists, BIOORG MED, 10(16), 2000, pp. 1867-1870
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
16
Year of publication
2000
Pages
1867 - 1870
Database
ISI
SICI code
0960-894X(20000821)10:16<1867:1ASAO>2.0.ZU;2-6
Abstract
Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity an d 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 pharma codynamic model of 5-HT2C function and their therapeutic potential is curre ntly under further investigation. (C) 2000 Elsevier Science Ltd. All rights reserved.