α2δ and the mechanism of action of gabapentin in the treatment of pain

Gabapentin is a drug that has been widely used in the treatment of chronic pain states. Despite its widespread usage, it is only recently that light has been shed on the mechanism of action of this agent. In the current review, the authors document the pharmacological, biochemical and molecular information that has led to the identification of the α2δ1 auxilliary subunit of voltage gated calcium channels as the target for this drug's actions.