title: N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
abstract: A new class of N-(indol-3-ylglyoxylyl)piperidines are high affinity agonists at the benzodiazepine binding site of human GABA-A receptor ion-channels, with modest selectivity for receptors containing the alpha1 subunit over alpha2 and alpha3. All three receptor subtypes discriminate substantially between the two enantiomers of the chiral ligand 10.
authors.affiliation: Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. ian_collins@merck.com
authors.forename: I
authors.initials: I
authors.lastname: Collins
authors.forename: W B
authors.initials: WB
authors.lastname: Davey
authors.forename: M
authors.initials: M
authors.lastname: Rowley
authors.forename: K
authors.initials: K
authors.lastname: Quirk
authors.forename: F A
authors.initials: FA
authors.lastname: Bromidge
authors.forename: R M
authors.initials: RM
authors.lastname: McKernan
authors.forename: S A
authors.initials: SA
authors.lastname: Thompson
authors.forename: K A
authors.initials: KA
authors.lastname: Wafford
mesh_terms: D058785:GABA-A Receptor Agonists; D006801:Humans; D007211:Indoles / Q000737:chemistry; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000737:chemistry
chemical_list: D058785:GABA-A Receptor Agonists; D007211:Indoles; D010880:Piperidines; D011963:Receptors, GABA-A