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Mechanism of action of the anticonvulsant felbamate: Opposing effects on N‐methyl‐D‐aspartate and γ‐aminobutyric acidA receptors
Abstract
Felbamate is a promising new antiepileptic drug whose mechanism of action is unknown. In whole‐cell voltage clamp recordings from cultured rat hippocampal neurons, clinically relevant concentrations of felbamate (0.1–3 mM) inhibited N‐methyl‐D‐aspartate (NMDA) responses and potentiated γ‐aminobutyric acid (GABA) responses. Single‐channel recordings indicated that the effect on NMDA responses occurred via a channel blocking mechanism. Felbamate is the first anticonvulsant drug with dual actions on excitatory (NMDA) and inhibitory (GABA) brain mechanisms. This unique combination of effects could account for felbamate's broad spectrum of anticonvulsant activity in animal seizure models and its distinctive clinical efficacy and safety profile.
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Cited by
Clinical Experience With Excitatory Amino Acid Antagonist Drugs
Muir, K. W., & Lees, K. R. (1995) · Stroke · doi:10.1161/01.str.26.3.503 · Cited by 502
The effect of novel anti-epileptic drugs in rat experimental models of acute and chronic pain
Hunter, J. C., Gogas, K. R., Hedley, L. R., Jacobson, L. O., Kassotakis, L., Thompson, J., & Fontana, D. J. (1997) · European Journal of Pharmacology · doi:10.1016/s0014-2999(97)00070-8 · Cited by 310
The mechanisms of action of commonly used antiepileptic drugs
Kwan, P., Sills, G. J., & Brodie, M. J. (2001) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(01)00122-x · Cited by 289
Update on the Mechanism of Action of Antiepileptic Drugs
Meldrum, B. S. (1996) · Epilepsia · doi:10.1111/j.1528-1157.1996.tb06038.x · Cited by 247
Metadata
- Authors
- Rho, J. M., Donevan, S. D., & Rogawski, M. A.
- Venue
- Annals of Neurology
- Publisher
- Wiley
- Published
- 1994-02
- Volume
- 35
- Issue
- 2
- Pages
- 229-234
- ISSN
- 0364-5134 (ISSN-L)
- 1531-8249
- OpenAlex
- W4319308579
- Cited by
- 187
- References
- 0
- FWCI
- 15.09
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Mechanism of action of the anticonvulsant felbamate: Opposing effects on N‐methyl‐D‐aspartate and γ‐aminobutyric acidA receptors. https://app.cochat.ai/papers/10.1002/ana.410350216
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- Rho, J. M., Donevan, S. D., & Rogawski, M. A. (1994). Mechanism of action of the anticonvulsant felbamate: Opposing effects on N‐methyl‐D‐aspartate and γ‐aminobutyric acidA receptors. Annals of Neurology. https://doi.org/10.1002/ana.410350216
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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