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Current Neuropharmacology


ISSN (Print): 1570-159X
ISSN (Online): 1875-6190

Gabapentin-Mediated Effects on Voltage- and Ligand-Gated Currents

Author(s): Alessandro Stefani and Atticus Henry Hainsworth

Volume 1, Issue 3, 2003

Page: [237 - 244] Pages: 8

DOI: 10.2174/1570159033477143

Price: $65


Gabapentin ( Neurontin) is currently utilised in the treatment of a range of neurological and psychiatric conditions, including partial epilepsy, neuropathic pain and bipolar disorders. Gabapentin (GBP) mechanisms of action, although extensively investigated, are only partially known. This review examines GBP-mediated effects on voltage- and ligand-gated neuronal ionic currents. GBP binds in vivo to the alpha-2-delta sub-unit of the calcium channel and, in dorsal root ganglia, GBP-induced modulation of calcium conductance plays a central role in the drugs inhibitory effect on pain transmission. Less clear is the relevance of GBP as a calcium current modulator in central neo-cortical neurons and the potential use of GBP as add-on therapy for resistant seizures. GBP is also reported to interact with NMDA receptor currents, inwardly rectifying potassium channels and a subtype of baclofen-sensitive-receptors. The potential utility of GBP in modifying the balance among released endogenous amino-acids, and also in neuroprotection, has been suggested. It is, however, unclear whether - and through which cellular pathways - GBP might give therapeutic benefit in the course of neurodegenerative disorders.

Keywords: gabapentin, ligand-gated currents, neurontin

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