title: In search of potent 5-HT6 receptor inverse agonists.
abstract: A series of non-sulfonamide/non-sulfone derived potent 5-HT6 receptor inverse agonists has been disclosed. Representative compound 9 (Ki  = 14 nm) displayed selectivity against a set of family members as well as brain permeability 6 h post-oral administration. In addition, the separated enantiomers of compound 9 displayed difference in activity indicating the influence of chirality on potency.
authors.affiliation: Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA, 19380-4245, USA.
authors.forename: Greg
authors.initials: G
authors.lastname: Hostetler
authors.forename: Derek
authors.initials: D
authors.lastname: Dunn
authors.forename: Beth Ann
authors.initials: BA
authors.lastname: McKenna
authors.forename: Karla
authors.initials: K
authors.lastname: Kopec
authors.forename: Sankar
authors.initials: S
authors.lastname: Chatterjee
mesh_terms: D001552:Benzazepines / Q000737:chemistry / Q000494:pharmacology; D001681:Biological Assay; D054314:Drug Inverse Agonism; D006801:Humans; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D011985:Receptors, Serotonin / Q000737:chemistry*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D013450:Sulfones / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001552:Benzazepines; D011985:Receptors, Serotonin; D013449:Sulfonamides; D013450:Sulfones; C097216:serotonin 6 receptor
keywords: 5-HT6 receptor; CNS disorders; benzazepine