1.
Bioorg Med Chem Lett
; 20(11): 3436-40, 2010 Jun 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20434910
RESUMEN
A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism.