Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes

Timothy A. Simeone; James F. Otto; Karen S. Wilcox; H. Steve White

doi:10.1016/j.ejphar.2006.09.002

Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes

Timothy A. Simeone, James F. Otto, Karen S. Wilcox, H. Steve White

Department of Pharmacology and Neuroscience

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

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 (GABA_A) receptors. To determine felbamate subunit selectivity for GABA_A receptors we expressed 15 different GABA_A receptor combinations in Xenopus laevis oocytes. Felbamate positively modulated GABA-currents of α₁β₂γ_2S, α₁β₃γ_2S, α₂β₂γ_2S and α₂β₃γ_2S, whereas felbamate was either ineffective or negatively modulated the other 11 receptor combinations. Regional distributions of GABA_A 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 (US)
Pages (from-to)	31-35
Number of pages	5
Journal	European Journal of Pharmacology
Volume	552
Issue number	1-3
DOIs	https://doi.org/10.1016/j.ejphar.2006.09.002
State	Published - Dec 15 2006

All Science Journal Classification (ASJC) codes

Pharmacology

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@article{e96811786b744704b6633f90092e87b2,

title = "Felbamate is a subunit selective modulator of recombinant γ-aminobutyric acid type A receptors expressed in Xenopus oocytes",

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.",

author = "Simeone, {Timothy A.} and Otto, {James F.} and Wilcox, {Karen S.} and White, {H. Steve}",

note = "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).",

year = "2006",

month = dec,

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doi = "10.1016/j.ejphar.2006.09.002",

language = "English (US)",

volume = "552",

pages = "31--35",

journal = "European Journal of Pharmacology",

issn = "0014-2999",

publisher = "Elsevier",

number = "1-3",

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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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JO - European Journal of Pharmacology

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