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Issue 28, 2011
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Agonist responses of (R)- and (S)-3-fluoro-γ-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABAC receptors

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Abstract

The enantiomers of 3F-GABA were evaluated on GABAC 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 GABAA receptors.

Graphical abstract: Agonist responses of (R)- and (S)-3-fluoro-γ-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABAC receptors

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Publication details

The article was received on 14 Apr 2011, accepted on 25 May 2011 and first published on 13 Jun 2011


Article type: Communication
DOI: 10.1039/C1CC12141C
Citation: Chem. Commun., 2011,47, 7956-7958
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    Agonist responses of (R)- and (S)-3-fluoro-γ-aminobutyric acids suggest an enantiomeric fold for GABA binding to GABAC receptors

    I. Yamamoto, G. P. Deniau, N. Gavande, M. Chebib, G. A. R. Johnston and D. O'Hagan, Chem. Commun., 2011, 47, 7956
    DOI: 10.1039/C1CC12141C

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