PeptideDB

Gabapentin hydrochloride

CAS: 60142-95-2 F: C9H18ClNO2 W: 207.70

Gabapentin hydrochloride is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin hydrochloride inhibits neu
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Bioactivity 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].
Invitro 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]. Animal Model:
Name Gabapentin hydrochloride
CAS 60142-95-2
Formula C9H18ClNO2
Molar Mass 207.70
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [1]. Fink K, et, al. Inhibition of neuronal Ca(2+) influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices. Br J Pharmacol. 2000 Jun;130(4):900-6. [2]. Celikyurt IK, et, al. Gabapentin, A GABA analogue, enhances cognitive performance in mice. Neurosci Lett. 2011 Apr 1;492(2):124-8. [3]. Meymandi MS, et, al. Gabapentin action and interaction on the antinociceptive effect of morphine on visceral pain in mice. Eur J Anaesthesiol. 2008 Feb;25(2):129-34.