title: Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
abstract: 5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, which represent a useful set of molecules for further understanding the roles of the 5-HT1 receptor subtypes and providing new approaches for the treatment of depression.
authors.affiliation: Psychiatry Centre of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline, Essex, UK. Simon.E.Ward@gsk.com
authors.forename: Simon E
authors.initials: SE
authors.lastname: Ward
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Eddershaw
authors.forename: Claire M
authors.initials: CM
authors.lastname: Scott
authors.forename: Laurie J
authors.initials: LJ
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: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Kathryn R
authors.initials: KR
authors.lastname: Starr
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Thewlis
authors.forename: Jeannette M
authors.initials: JM
authors.lastname: Watson
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D010879:Piperazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011994:Recombinant Proteins / Q000494:pharmacology; D058829:Serotonin 5-HT1 Receptor Antagonists; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D011804:Quinolines; D011994:Recombinant Proteins; D058829:Serotonin 5-HT1 Receptor Antagonists