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Bioorg Med Chem Lett. 2000 Aug 21;10(16):1867-70.

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

Author information

1
SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com

Abstract

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.

PMID:
10969987
DOI:
10.1016/s0960-894x(00)00365-6
[Indexed for MEDLINE]

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