title: Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
abstract: Imidazo[1,2-a]pyrimidines are GABA(A) receptor benzodiazepine binding site ligands which can exhibit functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimize this functional selectivity are described.
authors.affiliation: Neuroscience Research Centre, Merck Sharp and 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: José L
authors.initials: JL
authors.lastname: Castro
authors.forename: Simon C
authors.initials: SC
authors.lastname: Goodacre
authors.forename: David J
authors.initials: DJ
authors.lastname: Hallett
authors.forename: Richard T
authors.initials: RT
authors.lastname: Lewis
authors.forename: George R
authors.initials: GR
authors.lastname: Marshall
authors.forename: Andrew
authors.initials: A
authors.lastname: Pike
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Smith
authors.forename: Leslie J
authors.initials: LJ
authors.lastname: Street
authors.forename: David F D
authors.initials: DF
authors.lastname: Tattersall
authors.forename: Keith A
authors.initials: KA
authors.lastname: Wafford
mesh_terms: D007093:Imidazoles / Q000737:chemistry* / Q000378:metabolism*; D008024:Ligands; D015394:Molecular Structure; D011743:Pyrimidines / 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: D007093:Imidazoles; D008024:Ligands; D011743:Pyrimidines; D011963:Receptors, GABA-A; C029899:imidazole