Abstract
Felbamate (2-phenyl-1,3-propanediol dicarbamate) is clinically available for the treatment of refractory epileptic seizures, and is known to modulate several ion channels including γ-aminobutyric acid type A (GABAA) receptors. To determine felbamate subunit selectivity for GABAA receptors we expressed 15 different GABAA receptor combinations in Xenopus laevis oocytes. Felbamate positively modulated GABA-currents of α1β2γ2S, α1β3γ2S, α2β2γ2S and α2β3γ2S, whereas felbamate was either ineffective or negatively modulated the other 11 receptor combinations. Regional distributions of GABAA receptor subunits suggest that felbamate may differentially modulate distinct inhibitory circuits, a possibility that may have relevance to felbamate efficacy in refractory epilepsies.
| Original language | English |
|---|---|
| Pages (from-to) | 31-35 |
| Number of pages | 5 |
| Journal | European Journal of Pharmacology |
| Volume | 552 |
| Issue number | 1-3 |
| DOIs | |
| State | Published - Dec 15 2006 |
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All Science Journal Classification (ASJC) codes
- Cellular and Molecular Neuroscience
- Pharmacology
Cite this
Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes. / Simeone, Timothy; Otto, James F.; Wilcox, Karen S.; White, H. Steve.
In: European Journal of Pharmacology, Vol. 552, No. 1-3, 15.12.2006, p. 31-35.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes
AU - Simeone, Timothy
AU - Otto, James F.
AU - Wilcox, Karen S.
AU - White, H. Steve
PY - 2006/12/15
Y1 - 2006/12/15
N2 - Felbamate (2-phenyl-1,3-propanediol dicarbamate) is clinically available for the treatment of refractory epileptic seizures, and is known to modulate several ion channels including γ-aminobutyric acid type A (GABAA) receptors. To determine felbamate subunit selectivity for GABAA receptors we expressed 15 different GABAA receptor combinations in Xenopus laevis oocytes. Felbamate positively modulated GABA-currents of α1β2γ2S, α1β3γ2S, α2β2γ2S and α2β3γ2S, whereas felbamate was either ineffective or negatively modulated the other 11 receptor combinations. Regional distributions of GABAA receptor subunits suggest that felbamate may differentially modulate distinct inhibitory circuits, a possibility that may have relevance to felbamate efficacy in refractory epilepsies.
AB - Felbamate (2-phenyl-1,3-propanediol dicarbamate) is clinically available for the treatment of refractory epileptic seizures, and is known to modulate several ion channels including γ-aminobutyric acid type A (GABAA) receptors. To determine felbamate subunit selectivity for GABAA receptors we expressed 15 different GABAA receptor combinations in Xenopus laevis oocytes. Felbamate positively modulated GABA-currents of α1β2γ2S, α1β3γ2S, α2β2γ2S and α2β3γ2S, whereas felbamate was either ineffective or negatively modulated the other 11 receptor combinations. Regional distributions of GABAA receptor subunits suggest that felbamate may differentially modulate distinct inhibitory circuits, a possibility that may have relevance to felbamate efficacy in refractory epilepsies.
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UR - http://www.scopus.com/inward/citedby.url?scp=33750466915&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2006.09.002
DO - 10.1016/j.ejphar.2006.09.002
M3 - Article
VL - 552
SP - 31
EP - 35
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1-3
ER -