Issue 28, 2011
From the journal:

Chemical Communications

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

Izumi Yamamoto,a   Gildas P. Deniau,b   Navnath Gavande,a   Mary Chebib,a   Graham A. R. Johnstonc  and  David O'Hagan*b  

* Corresponding authors

a Faculty of Pharmacy, University of Sydney, NSW, Australia

b University of St Andrews, EASTChem School of Chemistry and Centre for Biomolecular Sciences, North Haugh, St Andrews, Fife, UK
E-mail: do1@st-andrews.ac.uk
Fax: (+44)1334 463800
Tel: (+44)1334 467171

c Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology DO6, University of Sydney, NSW, Australia

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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Article information

DOI
https://doi.org/10.1039/C1CC12141C
Article type
Communication
Submitted
10 جمادى الأولى 1432
Accepted
22 جمادى الثانية 1432
First published
11 رجب 1432

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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