title: 4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands.
abstract: The preparation of a novel class of 4-(2-aminoethoxy)-N-(phenylsulfonyl)indoles which exhibit high affinity towards the 5-HT6 receptor is reported here. Among these compounds, 4-(2-methylaminoethoxy)-N-(phenylsulfonyl)indole 5g showed superior affinity (Ki = 1 nM) towards the 5-HT6 receptor as well as excellent selectivity (> 2000-fold) against the closely related subtype 5-HT7 receptor.
authors.affiliation: Chemical and Screening Science and Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. zhoup@wyeth.com
authors.forename: Ping
authors.initials: P
authors.lastname: Zhou
authors.forename: Yinfa
authors.initials: Y
authors.lastname: Yan
authors.forename: Ronald
authors.initials: R
authors.lastname: Bernotas
authors.forename: Boyd L
authors.initials: BL
authors.lastname: Harrison
authors.forename: Donna
authors.initials: D
authors.lastname: Huryn
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Robichaud
authors.forename: Guo Ming
authors.initials: GM
authors.lastname: Zhang
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
mesh_terms: D001667:Binding, Competitive; D007211:Indoles / Q000138:chemical synthesis / Q000145:classification / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D011985:Receptors, Serotonin / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D008024:Ligands; D011985:Receptors, Serotonin; C097216:serotonin 6 receptor