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Article

Synthesis of GABAA receptor agonists and evaluation of their alpha-subunit selectivity and orientation in the GABA binding site.

Journal of medicinal chemistry - 14 Aug 2008

Jansen Michaela, Rabe Holger, Strehle Axelle, Dieler Sandra, Debus Fabian, Dannhardt Gerd, Akabas Myles H, Lüddens Hartmut

Abstract excerpt

Drugs used to treat various disorders target GABA A receptors. To develop alpha subunit selective compounds, we synthesized 5-(4-piperidyl)-3-isoxazolol (4-PIOL) derivatives. The 3-isoxazolol moiety was substituted by 1,3,5-oxadiazol-2-one, 1,3,5-oxadiazol-2-thione, and substituted 1,2,4-triazol-3-ol heterocycles with modifications to the basic piperidine substituent as well as substituents without basic...

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Identifiers

PMID: 18651727
DOI: 10.1021/jm701562x
PMCID: PMC2566937

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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