Agonist responses of (R)- and (S)-3-fluoro-gamma-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABA(C) receptors

Izumi Yamamoto, Gildas P. Deniau, Navnath Gavande, Mary Chebib, Graham A. R. Johnston, David O'Hagan*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

31 Citations (Scopus)

Abstract

The enantiomers of 3F-GABA were evaluated on GABA(C) receptors. Both enantiomers were agonists, with the (R)-enantiomer being an order of magnitude more potent. This result is consistent with a folded binding mode for GABA, a conclusion which suggests a different binding mode to that found in the related but pharmacologically distinct GABA(A) receptors.

Original languageEnglish
Pages (from-to)7956-7958
Number of pages3
JournalChemical Communications
Volume47
Issue number28
DOIs
Publication statusPublished - 2011

Keywords

  • ANTAGONISTS
  • PHARMACOLOGY
  • LIGAND
  • X-RAY-STRUCTURE
  • CYCLOPENTENE
  • CONFORMATION
  • ANALOGS
  • MEDICINAL CHEMISTRY
  • FLUORINE
  • GATED ION-CHANNEL

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