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Cellular and molecular action of the putative GABA-mimetic, gabapentin

  • Drugs of the Future: Review
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Gabapentin was originally designed as an anticonvulsant γ-aminobutyric acid (GABA) mimetic capable of crossing the blood-brain barrier. In the present review we show that although gabapentin is not a GABA mimetic, it has great utility as an add-on therapy for epilepsy and as a first-line treatment for neuropathic pain. We summarise the studies that have been performed which demonstrate that gabapentin appears to interact with a novel binding site expressed at high density within the central nervous system (CNS), namely the α2δ voltage-dependent calcium channel subunit. The review continues by examining the effects of gabapentin on calcium channel function and neurotransmitter release before, in the latter part of the review, summarising the more recently discovered actions of gabapentin in relation to intracellular signalling.

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Received 13 May 2002; received after revision 31 August 2002 and 21 September 2002; accepted 30 September 2002


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Maneuf, Y., Gonzalez, M., Sutton, K. et al. Cellular and molecular action of the putative GABA-mimetic, gabapentin. CMLS, Cell. Mol. Life Sci. 60, 742–750 (2003).

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