Neurontin; Gabapentin; Neurontin; Gabapentine; Gabapentin HCl; Gabapentin hydrochloride;Aclonium; Convalis; gabapentin; Gabapentin Hexal; Gabapentin Stada
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Purity: ≥98%
Gabapentin HCl (Neurontin; Aclonium; Convalis; Gabapentin Stada), the hydrochloride salt of gabapentin which is a GABA analog, is an orally bioavailable medication that was approved for use in the treatment of seizures and neuropathic pain. Gabapentin is structurally similar to GABA and is reported in various research studies to be able to increase GABA concentrations in the brain.
| ln Vitro |
The concentration-dependent inhibition of the K+-induced [Ca2+]i increase in synaptosomes (IC50=14 μM; maximal inhibition by 36%) is produced by gabapentin (0-300 μM)[1]. In neocortical slices, gabapentin (100 μM) reduces endogenous aspartate and glutamate's K+-evoked release by 16 and 18%, respectively[1]. In neocortical slices, gabapentin (0-1000 μM) decreases the release of [3H]-noradrenaline evoked by K+ (IC50=48 μM; maximal inhibition of 46%), but not from synaptosomes[1].
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| ln Vivo |
The spatial and affective cognitive performance of naive mice in the Morris water maze (MWM), passive avoidance (PA), and modified elevated plus maze (mEPM) tasks is improved by gabapentin (5 and 10 mg/kg; ip; once; male BALB/c mice)[2]. ?In male mice, gabapentin (1–100 mg/kg; intraperitoneally; once) exerts analgesic effect and dose-dependently lowers writhing[3].
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| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (35 -45 g)[2]
Doses: 5 and 10 mg/kg Route of Administration: intraperitoneal (ip)injection; once Experimental Results: Increased the time spent in target quadrant and diminished the distance to platform in MWM test . diminished the transfer latency on second day in mEPM test . Prolonged retention latency in PA test . Animal/Disease Models: Male mice (26-30 g)[3] Doses: 1, 5, 10, 50 and 100 mg/kg Route of Administration: intraperitoneal (ip)injection; once Experimental Results: Produced 45-70% inhibition of writhing. |
| References |
[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. |
| Molecular Formula |
C9H17NO2
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| Molecular Weight |
171.24
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| Exact Mass |
348.1274
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| CAS # |
60142-96-3
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| Related CAS # |
Gabapentin enacarbil;478296-72-9;Gabapentin hydrochloride;60142-95-2;Gabapentin-d4;1185039-20-6
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| SMILES |
O([H])C(C([H])([H])C1(C([H])([H])N([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O
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| Chemical Name |
2-[1-(aminomethyl)cyclohexyl]acetic acid
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (145.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL | |
| 5 mM | 1.1680 mL | 5.8398 mL | 11.6795 mL | |
| 10 mM | 0.5840 mL | 2.9199 mL | 5.8398 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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(a) Trace showing changes in fluorescence ratio produced by changes in KCl in imaging experiments. (b) Graph showing linear correlation between change in fluorescence ratio and membrane potential at varying concentrations of K+. |
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