title: 1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.
abstract: Bisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their potential as novel non-sedating anxiolytic and antidepressants is under investigation.
authors.affiliation: SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com
authors.forename: S M
authors.initials: SM
authors.lastname: Bromidge
authors.forename: S
authors.initials: S
authors.lastname: Dabbs
authors.forename: S
authors.initials: S
authors.lastname: Davies
authors.forename: D M
authors.initials: DM
authors.lastname: Duckworth
authors.forename: I T
authors.initials: IT
authors.lastname: Forbes
authors.forename: G E
authors.initials: GE
authors.lastname: Jones
authors.forename: J
authors.initials: J
authors.lastname: Jones
authors.forename: F D
authors.initials: FD
authors.lastname: King
authors.forename: D V
authors.initials: DV
authors.lastname: Saunders
authors.forename: T P
authors.initials: TP
authors.lastname: Blackburn
authors.forename: V
authors.initials: V
authors.lastname: Holland
authors.forename: G A
authors.initials: GA
authors.lastname: Kennett
authors.forename: S
authors.initials: S
authors.lastname: Lightowler
authors.forename: D N
authors.initials: DN
authors.lastname: Middlemiss
authors.forename: G J
authors.initials: GJ
authors.lastname: Riley
authors.forename: B
authors.initials: B
authors.lastname: Trail
authors.forename: M D
authors.initials: MD
authors.lastname: Wood
mesh_terms: D000284:Administration, Oral; D000631:Aminopyridines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000928:Antidepressive Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000737:chemistry / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000631:Aminopyridines; D014151:Anti-Anxiety Agents; D000928:Antidepressive Agents; D007211:Indoles; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists