title: Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.
abstract: A series of 5-(piperidinylethyloxy)quinoline 5-HT(1) receptor ligands have been studied by elaboration of the series of dual 5-HT(1)-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.
authors.affiliation: Neuroscience Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. simon.e.ward@gsk.com
authors.forename: Simon E
authors.initials: SE
authors.lastname: Ward
authors.forename: Peter
authors.initials: P
authors.lastname: Eddershaw
authors.forename: Sean T
authors.initials: ST
authors.lastname: Flynn
authors.forename: Laurie
authors.initials: L
authors.lastname: Gordon
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Lovell
authors.forename: Susan H
authors.initials: SH
authors.lastname: Moore
authors.forename: Claire M
authors.initials: CM
authors.lastname: Scott
authors.forename: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Thewlis
authors.forename: Paul A
authors.initials: PA
authors.lastname: Wyman
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D008024:Ligands; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D044263:Receptors, Serotonin, 5-HT1 / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D011804:Quinolines; D044263:Receptors, Serotonin, 5-HT1