TY - JOUR
T1 - Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes
AU - Simeone, Timothy A.
AU - Otto, James F.
AU - Wilcox, Karen S.
AU - White, H. Steve
N1 - Funding Information:
The authors would like to sincerely thank Dr. Michael McIntosh and associates for supplying Xenopus oocytes. This work was supported by NS-4-2311 (HSW).
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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U2 - 10.1016/j.ejphar.2006.09.002
DO - 10.1016/j.ejphar.2006.09.002
M3 - Article
C2 - 17056029
AN - SCOPUS:33750466915
VL - 552
SP - 31
EP - 35
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1-3
ER -