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Hypothetical mechanisms of action of gabapentin (GBP). The effect of GBP may be to displace an endogenous ligand (L-leucine) and impair the ability of the auxiliary CaVα2δ subunit to increase the number of functional channels at the plasma membrane. GBP may be entering the cells using the system-L transporter protein LAT4 and might be exerting its effect on intracellular CaVα2δ subunits during assembly and trafficking of the CaV channel complex to the cell surface.
