Gabapentin HCl (Neurontin)

Alias:
Cat No.:V1284 Purity: ≥98%
Gabapentin HCl (Neurontin),the hydrochloride salt of gabapentin which is a GABA analogue, is an orally bioavailable and approved medication used to treat seizures and neuropathic pain.
Gabapentin HCl (Neurontin) Chemical Structure CAS No.: 60142-95-2
Product category: GABA Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Gabapentin HCl (Neurontin):

  • Gabapentin
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Gabapentin HCl (Neurontin), the hydrochloride salt of gabapentin which is a GABA analogue, is an orally bioavailable and approved medication used to treat seizures and neuropathic pain. Gabapentin is a major inhibitory neurotransmitter that functions by binding to the GABA receptors located in the spinal cord. Gabapentin also binds to a novel site on voltage-sensitive Ca2+ channels. Additionally, Gabapentin demonstrates inhibition of dopamine release from caudate nucleus, prevent neuronal cell death, and is antinociceptive. It is structurally similar to GABA and is reported in various research studies to increase GABA concentrations within the brain.

Biological Activity I Assay Protocols (From Reference)
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) hydrochloride[1]. In neocortical slices, gabapentin hydrochloride (100 μM) reduces endogenous aspartate and glutamate release triggered by K+ by 16 and 18%, respectively[1]. The K+-evoked [3H]-noradrenaline release in neocortical slices is lessened by gabapentin hydrochloride (0-1000 μM; maximal inhibition of 46%), but not from synaptosomes[1].
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 hydrochloride (5 and 10 mg/kg; ip; once; male BALB/c mice)[2]. Gabapentin hydrochloride (1–100 mg/kg; ip; once; male mice) provides a dose-dependent analgesic effect and lessens writhing[3].
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H17NO2.HCL
Molecular Weight
207.7
CAS #
60142-95-2
SMILES
O=C(O)CC1(CN)CCCCC1.[H]Cl
InChi Key
XBUDZAQEMFGLEU-UHFFFAOYSA-N
InChi Code
InChI=1S/C9H17NO2.ClH/c10-7-9(6-8(11)12)4-2-1-3-5-9;/h1-7,10H2,(H,11,12);1H
Chemical Name
1-(Aminomethyl)cyclohexaneacetic acid HCl
Synonyms

Gabapentin hydrochloride;Neurontin

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:<1 mg/mL
Water: 42 mg/mL (202.2 mM)
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.8146 mL 24.0732 mL 48.1464 mL
5 mM 0.9629 mL 4.8146 mL 9.6293 mL
10 mM 0.4815 mL 2.4073 mL 4.8146 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

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Biological Data
  • Gabapentin HCI

    (a) Time-course showing gabapentin inhibition of peak IBa. (b) Whole-cell current trace of peak HVA IBa activated under control conditions (con) and following a 10 min application of gabapentin (GBP). (c) Dose-response of GBP-mediated inhibition of peak HVA IBa.Br J Pharmacol.2002 Jan;135(1):257-65.

  • Gabapentin HCI

    Gabapentin inhibited Ca2+ influx into cultured DRG as measured using fura-2 fluorescence imaging.Br J Pharmacol.2002 Jan;135(1):257-65.
  • Gabapentin HCI

    (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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