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. Author manuscript; available in PMC: 2006 Sep 24.
Published in final edited form as: Epilepsy Res. 2006 Jun;69(3):183–272. doi: 10.1016/j.eplepsyres.2006.03.014

Figure 2.

Figure 2

Relationship between α2-δ binding affinity, system L transporter affinity, and potency for protection against audiogenic seizures in DBA/2 mice for gabapentin, pregabalin and structural analogs. The Y-axis represents the percent protection (out of 5 animals) in the seizure model at a dose of 30 mg/kg, p.o. The Z-axis represents the concentration (μM) producing half-maximal inhibition of [3H]L-leucine uptake by the system L transporter in CHO-K1 cells. The X-axis represents the concentration (μM) producing half-maximal inhibition of specific [3H]gabapentin binding to pig brain membranes. Seizure protection correlates with α2-δ binding only for those compounds that are substrates for the system L transporter, which appears to be required for absorption by the gut and delivery to the brain (D.J. Wustrow and C.P. Taylor, unpublished).