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Bioorg Med Chem Lett. 2000 Jun 19;10(12):1381-4.

N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.

Author information

1
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. ian_collins@merck.com

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.

PMID:
10890169
DOI:
10.1016/s0960-894x(00)00245-6
[Indexed for MEDLINE]

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