1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/Anxiolytic agents
2000; Elsevier BV; Volume: 10; Issue: 16 Linguagem: Inglês
10.1016/s0960-894x(00)00364-4
ISSN1464-3405
AutoresSteven M. Bromidge, Steven Dabbs, Susannah Davies, D. Malcolm Duckworth, Ian T. Forbes, Graham E. Jones, Jerome Jones, Frank D. King, Damian V. Saunders, Thomas P. Blackburn, Vicky Holland, G.A. Kennett, Sean Lightowler, Derek N. Middlemiss, Graham J. Riley, Brenda Trail, Martyn Wood,
Tópico(s)Catalytic C–H Functionalization Methods
ResumoBisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their potential as novel non-sedating anxiolytic and antidepressants is under investigation.
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