title: 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
abstract: 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimise this functional selectivity are described.
authors.affiliation: Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow CM20 2QR, UK. andrew_mitchinson@merck.com
authors.forename: Andrew
authors.initials: A
authors.lastname: Mitchinson
authors.forename: John R
authors.initials: JR
authors.lastname: Atack
authors.forename: Peter
authors.initials: P
authors.lastname: Blurton
authors.forename: Robert W
authors.initials: RW
authors.lastname: Carling
authors.forename: José L
authors.initials: JL
authors.lastname: Castro
authors.forename: Karen S
authors.initials: KS
authors.lastname: Curley
authors.forename: Michael G N
authors.initials: MG
authors.lastname: Russell
authors.forename: George
authors.initials: G
authors.lastname: Marshall
authors.forename: Ruth M
authors.initials: RM
authors.lastname: McKernan
authors.forename: Kevin W
authors.initials: KW
authors.lastname: Moore
authors.forename: Robert
authors.initials: R
authors.lastname: Narquizian
authors.forename: Alison
authors.initials: A
authors.lastname: Smith
authors.forename: Leslie J
authors.initials: LJ
authors.lastname: Street
authors.forename: Sally-Anne
authors.initials: SA
authors.lastname: Thompson
authors.forename: Keith
authors.initials: K
authors.lastname: Wafford
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D006801:Humans; D007700:Kinetics; D008024:Ligands; D015394:Molecular Structure; D018408:Patch-Clamp Techniques; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry / Q000378:metabolism; D011869:Radioligand Assay; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D011720:Pyrazoles; D011725:Pyridines; D011963:Receptors, GABA-A; C054730:CGS 17867A; D001569:Benzodiazepines