title: Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.
abstract: Starting from a series of 2-aminotetralins 1, a novel series of N-[4-(4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D3 receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1.
authors.affiliation: SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
authors.forename: K Y
authors.initials: KY
authors.lastname: Avenell
authors.forename: I
authors.initials: I
authors.lastname: Boyfield
authors.forename: M C
authors.initials: MC
authors.lastname: Coldwell
authors.forename: M S
authors.initials: MS
authors.lastname: Hadley
authors.forename: M A
authors.initials: MA
authors.lastname: Healy
authors.forename: P M
authors.initials: PM
authors.lastname: Jeffrey
authors.forename: C N
authors.initials: CN
authors.lastname: Johnson
authors.forename: D J
authors.initials: DJ
authors.lastname: Nash
authors.forename: G J
authors.initials: GJ
authors.lastname: Riley
authors.forename: E E
authors.initials: EE
authors.lastname: Scott
authors.forename: S A
authors.initials: SA
authors.lastname: Smith
authors.forename: R
authors.initials: R
authors.lastname: Stacey
authors.forename: G
authors.initials: G
authors.lastname: Stemp
authors.forename: K M
authors.initials: KM
authors.lastname: Thewlis
mesh_terms: D000818:Animals; D065127:Dopamine D2 Receptor Antagonists; D008657:Metabolic Clearance Rate; D051381:Rats; D050637:Receptors, Dopamine D3; D013764:Tetrahydronaphthalenes / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D065127:Dopamine D2 Receptor Antagonists; C493595:Drd3 protein, rat; D050637:Receptors, Dopamine D3; D013764:Tetrahydronaphthalenes; C006561:2-aminotetralin