title: A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
abstract: Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
authors.affiliation: Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithkline Pharmaceuticals, Third Avenue, Harlow, Essex CM19 5AW, UK. Caroline_Goodacre@GSK.com
authors.forename: Caroline J
authors.initials: CJ
authors.lastname: Goodacre
authors.forename: Steven M
authors.initials: SM
authors.lastname: Bromidge
authors.forename: David
authors.initials: D
authors.lastname: Clapham
authors.forename: Frank D
authors.initials: FD
authors.lastname: King
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Lovell
authors.forename: Mike
authors.initials: M
authors.lastname: Allen
authors.forename: Lorraine P
authors.initials: LP
authors.lastname: Campbell
authors.forename: Vicky
authors.initials: V
authors.lastname: Holland
authors.forename: Graham J
authors.initials: GJ
authors.lastname: Riley
authors.forename: Kathryn R
authors.initials: KR
authors.lastname: Starr
authors.forename: Brenda K
authors.initials: BK
authors.lastname: Trail
authors.forename: Martyn D
authors.initials: MD
authors.lastname: Wood
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002460:Cell Line; D006801:Humans; D048289:Imidazolidines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism; D012680:Sensitivity and Specificity; D058830:Serotonin 5-HT2 Receptor Antagonists; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D048289:Imidazolidines; D044402:Receptor, Serotonin, 5-HT2A; D044403:Receptor, Serotonin, 5-HT2B; D044405:Receptor, Serotonin, 5-HT2C; D058830:Serotonin 5-HT2 Receptor Antagonists