N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
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.
Collins
I
I
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. ian_collins@merck.com
Davey
W B
WB
Rowley
M
M
Quirk
K
K
Bromidge
F A
FA
McKernan
R M
RM
Thompson
S A
SA
Wafford
K A
KA
D058785:GABA-A Receptor Agonists; D006801:Humans; D007211:Indoles / Q000737:chemistry; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000737:chemistry
D058785:GABA-A Receptor Agonists; D007211:Indoles; D010880:Piperidines; D011963:Receptors, GABA-A