Skip to content
2000
Volume 1, Issue 3
  • ISSN: 1570-159X
  • E-ISSN: 1875-6190

Abstract

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 drug's 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.

Loading

Article metrics loading...

/content/journals/cn/10.2174/1570159033477143
2003-09-01
2025-07-11
Loading full text...

Full text loading...

/content/journals/cn/10.2174/1570159033477143
Loading

  • Article Type:
    Review Article
Keyword(s): gabapentin; ligand-gated currents; neurontin
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test