title: Pyrazolopyridinones as functionally selective GABAA ligands.
abstract: 2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimize this functional selectivity are described.
authors.affiliation: Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. Wesley_Blackaby@Merck.com
authors.forename: Wesley P
authors.initials: WP
authors.lastname: Blackaby
authors.forename: John R
authors.initials: JR
authors.lastname: Atack
authors.forename: Frances
authors.initials: F
authors.lastname: Bromidge
authors.forename: Richard
authors.initials: R
authors.lastname: Lewis
authors.forename: Michael G N
authors.initials: MG
authors.lastname: Russell
authors.forename: Alison
authors.initials: A
authors.lastname: Smith
authors.forename: Keith
authors.initials: K
authors.lastname: Wafford
authors.forename: Ruth M
authors.initials: RM
authors.lastname: McKernan
authors.forename: Leslie J
authors.initials: LJ
authors.lastname: Street
authors.forename: José L
authors.initials: JL
authors.lastname: Castro
mesh_terms: D001391:Azo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D001391:Azo Compounds; D008024:Ligands; D011725:Pyridines; D011963:Receptors, GABA-A; C023666:pyridine