title: Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.
abstract: The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles. Copyright2000 Elsevier Science Ltd.
authors.affiliation: GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Stafford
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Pacofsky
authors.forename: Richard F
authors.initials: RF
authors.lastname: Cox
authors.forename: Jill R
authors.initials: JR
authors.lastname: Cowan
authors.forename: George F
authors.initials: GF
authors.lastname: Dorsey
authors.forename: Stephen S
authors.initials: SS
authors.lastname: Gonzales
authors.forename: David K
authors.initials: DK
authors.lastname: Jung
authors.forename: George W
authors.initials: GW
authors.lastname: Koszalka
authors.forename: Maggie S
authors.initials: MS
authors.lastname: McIntyre
authors.forename: Jeffrey H
authors.initials: JH
authors.lastname: Tidwell
authors.forename: Robert P
authors.initials: RP
authors.lastname: Wiard
authors.forename: Paul L
authors.initials: PL
authors.lastname: Feldman
mesh_terms: D000818:Animals; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D058785:GABA-A Receptor Agonists; D006801:Humans; D004856:Postural Balance / Q000187:drug effects; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D058785:GABA-A Receptor Agonists; D011963:Receptors, GABA-A; D001569:Benzodiazepines