Pharmacology
Gabapentin was initially synthesized to mimic the chemical structure of the neurotransmitter gamma-aminobutyric acid (GABA), but is not believed to act on the same brain receptors. The mechanism of action that leads to its rapid analgesic effect is simply unknown.
Some of its activity may involve interaction with voltage-gated calcium channels. Gabapentin binds to the α2δ subunit (1 and 2) and has been found to reduce calcium currents after chronic but not acute application via an effect on trafficking of voltage-dependent calcium channels in the central nervous system. Another possible mechanism of action, reported by Ben Barres and colleagues in Cell in 2009, is that gabapentin halts the formation of new synapses.
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