Issue 28, 2011

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

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

Supplementary files

Article information

Article type
Communication
Submitted
14 Dzi 2011
Accepted
25 Mud 2011
First published
13 Kho 2011

Chem. Commun., 2011,47, 7956-7958

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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