Gabapentin (hydrochloride)

Gabapentin hydrochloride is a potent, orally active P/Q type Ca²⁺ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca²⁺ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain^[1][2][3]. In Vitro:Gabapentin (0-300 μM) hydrochloride produces a concentration-dependent inhibition of the K⁺-induced [Ca²⁺]_i increase in synaptosomes (IC₅₀=14 μM; maximal inhibition by 36%)^[1]. Gabapentin (100  μM) hydrochloride decreases the K⁺-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively^[1]. Gabapentin (0-1000 μM) hydrochloride reduces the K⁺-evoked [³H]-noradrenaline release in neocortical slices (IC₅₀=48 μM; maximal inhibition of 46%) but not from synaptosomes^[1]. In Vivo:Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) hydrochloride has improving effects on spatial and emotional cognitive performance of naive mice in Morris water maze (MWM), passive avoidance (PA) and modified elevated plus maze (mEPM) tasks^[2].
Gabapentin (1-100 mg/kg; i.p.; once; male mice) hydrochloride has analgesic effect and reduces writhing in a dose-dependent manner^[3].