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ID: ALA1133278

Journal: Bioorg Med Chem Lett

Title: 1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 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.

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.

CiteXplore: 10969987

DOI: 10.1016/s0960-894x(00)00365-6