GabapentinGabapentin
MedChemExpress (MCE)
HY-A0057
60142-96-3
98.0%
Store at room temperature 3 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain.
Gabapentin (0-300 μM) 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) decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively[1].?Gabapentin (0-1000 μM) reduces the K+-evoked [3H]-noradrenaline release in neocortical slices (IC50=48?μM
maximal inhibition of 46%) but not from synaptosomes[1].
Gabapentin (5 and 10 mg/kg
i.p.
once
male BALB/c mice) 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) has analgesic effect and reduces writhing in a dose-dependent manner[3].
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[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. [Content Brief]
[2]. Celikyurt IK, et, al. Gabapentin, A GABA analogue, enhances cognitive performance in mice. Neurosci Lett. 2011 Apr 1
492(2):124-8. [Content Brief]
[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. [Content Brief]