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Bioorg Med Chem Lett
; 23(2): 407-11, 2013 Jan 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23253443
RESUMEN
A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK(1)/SERT affinity. Optimization based on NK(1)/SERT binding affinities, and minimization of off-target ion channel activity lead to the discovery of compound 44. In vivo evaluation of 44 in the gerbil forced swim test (a depression model), and ex-vivo NK(1)/SERT receptor occupancy data support the potential of a dual acting compound for the treatment of depression.