| Bioactivity | 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[1][2][3]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | Gabapentin | ||||||||||||
| CAS | 60142-96-3 | ||||||||||||
| Formula | C9H17NO2 | ||||||||||||
| Molar Mass | 171.24 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |