title: Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.
abstract: Starting from the dopamine D3 receptor antagonist SB-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinity for the dopamine D3 receptor and selectivity over the D2 receptor. The 3-acetamido-2-fluorocinnamide derivative 20 gave high D3 receptor affinity (pKi 8.4) with 130-fold selectivity over the 2, receptor.
authors.affiliation: SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
authors.forename: N E
authors.initials: NE
authors.lastname: Austin
authors.forename: K Y
authors.initials: KY
authors.lastname: Avenell
authors.forename: I
authors.initials: I
authors.lastname: Boyfield
authors.forename: C L
authors.initials: CL
authors.lastname: Branch
authors.forename: M S
authors.initials: MS
authors.lastname: Hadley
authors.forename: P
authors.initials: P
authors.lastname: Jeffrey
authors.forename: C N
authors.initials: CN
authors.lastname: Johnson
authors.forename: G J
authors.initials: GJ
authors.lastname: Macdonald
authors.forename: D J
authors.initials: DJ
authors.lastname: Nash
authors.forename: G J
authors.initials: GJ
authors.lastname: Riley
authors.forename: A B
authors.initials: AB
authors.lastname: Smith
authors.forename: G
authors.initials: G
authors.lastname: Stemp
authors.forename: K M
authors.initials: KM
authors.lastname: Thewlis
authors.forename: A K
authors.initials: AK
authors.lastname: Vong
authors.forename: M
authors.initials: M
authors.lastname: Wood
mesh_terms: D000818:Animals; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000187:drug effects*; D050637:Receptors, Dopamine D3; D044005:Tetrahydroisoquinolines
chemical_list: C493595:Drd3 protein, rat; D009570:Nitriles; D011804:Quinolines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; C409982:SB 277011; D044005:Tetrahydroisoquinolines