title: Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
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 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: Psychiatry 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: Christopher N
authors.initials: CN
authors.lastname: Johnson
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Lovell
authors.forename: Claire M
authors.initials: CM
authors.lastname: Scott
authors.forename: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Stemp
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Thewlis
authors.forename: Antonio K
authors.initials: AK
authors.lastname: Vong
authors.forename: Jeannette M
authors.initials: JM
authors.lastname: Watson
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D008024:Ligands; D011985:Receptors, Serotonin / Q000378:metabolism*; D018490:Serotonin Agents / Q000378:metabolism* / Q000493:pharmacokinetics
chemical_list: D008024:Ligands; D011985:Receptors, Serotonin; D018490:Serotonin Agents