title: Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
abstract: Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3,4-dihydro-2H-1,4-benzoxazin-3-ones showing high affinities for the 5-HT(1A/1B/1D) receptors coupled with potent 5-HT reuptake inhibitory activity have been discovered. This is the first report describing docking of the lead compound 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2H-1,4-benzoxazin-3(4H)-one 1, into a model of the 5-HT transporter and the 5-HT(1A) receptor model.
authors.affiliation: Neurosciences CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. halina.serafinowska@gsk.com
authors.forename: Halina T
authors.initials: HT
authors.lastname: Serafinowska
authors.forename: Frank E
authors.initials: FE
authors.lastname: Blaney
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Lovell
authors.forename: Giancarlo G
authors.initials: GG
authors.lastname: Merlo
authors.forename: Claire M
authors.initials: CM
authors.lastname: Scott
authors.forename: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Kathryn R
authors.initials: KR
authors.lastname: Starr
authors.forename: Jeannette M
authors.initials: JM
authors.lastname: Watson
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002845:Chromatography / Q000379:methods; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D008297:Male; D008956:Models, Chemical; D008968:Molecular Conformation; D051381:Rats; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors