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Bioorg Med Chem Lett
; 22(4): 1494-8, 2012 Feb 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22290076
RESUMEN
A new series of epiminocyclohepta[b]indoles with potent 5-HT(6) antagonist activity were discovered and optimized using in vitro protocols. One compound from this series was progressed to advanced pharmacokinetic (PK) studies followed by 5-HT(6) receptor occupancy studies. The compound was found to have excellent oral absorption, a highly favorable PK profile and demonstrated pharmacodynamic interaction with the 5-HT(6) receptor as shown by ex vivo autoradiography.