Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Ca2+ channel:140 nM

Administering 10-100 mg/kg of Gabapentin orally to rats results in a dose-dependent blockade of both static and dynamic allodynia.

Gabapentin induces alterations in the cytoplasmic and extracellular concentrations of several amino acids (including L-leucine, L-valine, and L-phenylalanine) in rat cortical astrocytes and synaptosomes, suggesting pharmacological significance. In GABA B receptors composed of gb1a-GB2 subunit heterodimers, gabapentin decreases potassium-stimulated calcium influx via voltage-gated calcium channels. It potentiates N-methyl-D-aspartate-evoked currents in GABAergic rat spinal dorsal horn neurons in the presence of protein kinase C, possibly by enhancing the glycine sensitivity of the NMDA receptor complex. Gabapentin causes a delayed enhancement of indeterminate voltage-activated potassium currents in rat dorsal root ganglion neurons. In fura-2-loaded human neocortical synaptosomes, it concentration-dependently inhibits potassium(+)-induced [Ca(2+)] elevations with an IC50 of 17 mM and maximal inhibition of 37%. Gabapentin binds to the α2 delta subunit of calcium channels, selectively attenuating depolarization-induced presynaptic Ca(2+) influx through P/Q-type Ca(2+) channels, resulting in reduced glutamate/aspartate release from excitatory amino acid nerve terminals to AMPA heteroreceptors on noradrenergic nerve endings.