N-(Indol-3-ylglyoxylyl) piperidines: high affinity agonists of human GABA-A receptors containing the α 1 subunit

…, WB Davey, M Rowley, K Quirk, FA Bromidge…

Index: Collins, Ian; Davey, William B.; Rowley, Michael; Quirk, Kathleen; Bromidge, Frances A.; McKernan, Ruth M.; Thompson, Sally-Anne; Wafford, Keith A. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 12 p. 1381 - 1384

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Citation Number: 12

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 α1 subunit over α2 and α3. All three receptor subtypes discriminate substantially between the two enantiomers of the chiral ligand 10.