Gabapentin
Based on 15 publication(s) in Google Scholar
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.
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- Pureza: 99.99%
- No. CAS: 60142-96-3
- Fòrmula: C9H17NO2
- Peso molecular:171.24
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Almacenamiento:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Gabapentin
More- Free Radic Biol Med. 2026 Jun:249:292-307. [Abstract]
- Sci Total Environ. 2022 Jul 10;829:154437. [Abstract]
- Br J Pharmacol. 2025 Aug 9. [Abstract]
- Cell Rep. 2019 Dec 17;29(12):3847-3858.e5. [Abstract]
- Neuropharmacology. 2024 Dec 21:110276. [Abstract]
- iScience. 2023 Jul 3;26(8):107264. [Abstract]
- J Pain. 2019 May;20(5):577-591. [Abstract]
- ACS Pharmacol Transl Sci. 2023 Mar 6;6(4):519-525. [Abstract]
- Cell Tissue Res. 2026 Jun 24;405(1):3.
- Mol Biol Rep. 2025 Sep 3;52(1):859. [Abstract]
- J Nat Med. 2022 Jan;76(1):268-275. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2022 Sep;47(5):639-652. [Abstract]
- Pharmacol Res Perspect. 2021 Oct;9(5):e00879. [Abstract]
- Turk J Biochem. 2025 Dec 23.
- bioRxiv. 2026 Feb 16.
Ver todos los productos específicos de isoformas Calcium Channel
More
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
30 μM
Compound: 1
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Inhibition of [3H]leucine uptake into CHO cells by L-amino acid transporters
Inhibition of [3H]leucine uptake into CHO cells by L-amino acid transporters
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[PMID: 15801823] |
| CHO | IC50 |
30 μM
Compound: 2
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Displacement of [3H]leucine from Large neutral amino acids transporter system L in CHO cells
Displacement of [3H]leucine from Large neutral amino acids transporter system L in CHO cells
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[PMID: 19010672] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Gabapentin (1-100 mg/kg; i.p.; once; male mice) has analgesic effect and reduces writhing in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (35-45 g)[2]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Increased the time spent in target quadrant and decreased the distance to platform in MWM test
. Decreased the transfer latency on second day in mEPM test
. Prolonged retention latency in PA test
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Animal Model:Male mice (26-30 g)[3]
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Dosage:1, 5, 10, 50 and 100 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Produced 45-70% inhibition of writhing.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 60142-96-3
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Appearance Solid
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Peso molecular 171.24
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Fòrmula C9H17NO2
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Color White to off-white
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SMILES
O=C(O)CC1(CN)CCCCC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Free Radic Biol Med
Cornuside alleviates microglia-mediated neuroinflammation to ameliorate chronic neuropathic pain-induced cognitive impairment via the Nrf2/Sirt3 signaling pathway. [Abstract]2026 Jun:249:292-307. PMID: 41831801 -
Sci Total Environ
Maternal DBP exposure promotes synaptic formation in offspring by activating astrocytes via the AKT/NF-κB/IL-6/JAK2/STAT3 signaling pathway. [Abstract]2022 Jul 10;829:154437. PMID: 35278568 -
Br J Pharmacol
Synthesis and evaluation of a novel inhibitor for the α5-GABAA receptor in the treatment of peripheral neuralgia: Evidence from MD simulation and in vivo studies. [Abstract]2025 Aug 9. PMID: 40782001 -
Cell Rep
A Central Amygdala Input to the Parafascicular Nucleus Controls Comorbid Pain in Depression. [Abstract]2019 Dec 17;29(12):3847-3858.e5. PMID: 31851918 -
Neuropharmacology
Hyperoside ameliorates neuropathic pain by modulating the astroglial reactivity in the vlPAG. [Abstract]2024 Dec 21:110276. PMID: 39716641 -
iScience
SnRNA-seq reveals the heterogeneity of spinal ventral horn and mechanism of motor neuron axon regeneration. [Abstract]2023 Jul 3;26(8):107264. PMID: 37502257 -
J Pain
Alleviation of Mechanical Allodynia by 14,15-Epoxyeicosatrienoic Acid in a Central Poststroke Pain Model: Possible Role of Allopregnanolone and δ-Subunit-Containing Gamma-Aminobutyric Acid A Receptors. [Abstract]2019 May;20(5):577-591. PMID: 30500366 -
ACS Pharmacol Transl Sci
Effects of Gabapentinoids on Heroin-Induced Ventilatory Depression and Reversal by Naloxone. [Abstract]2023 Mar 6;6(4):519-525. PMID: 37082751 -
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Mol Biol Rep
Curcumin suppresses NLRP3 inflammasome activation by inducing autophagy to alleviate neuropathic pain in rats. [Abstract]2025 Sep 3;52(1):859. PMID: 40900270 -
J Nat Med
Celastrol attenuates chronic constrictive injury-induced neuropathic pain and inhibits the TLR4/NF-κB signaling pathway in the spinal cord. [Abstract]2022 Jan;76(1):268-275. PMID: 34510370 -
Eur J Drug Metab Pharmacokinet
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans. [Abstract]2022 Sep;47(5):639-652. PMID: 35733077 -
Pharmacol Res Perspect
Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]2021 Oct;9(5):e00879. PMID: 34628723 -
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Solvente y solubilidad
H2O : 50 mg/mL (291.99 mM; Need ultrasonic)
DMSO : 1 mg/mL (5.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (145.99 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL | 145.9939 mL |
| 5 mM | 1.1680 mL | 5.8398 mL | 11.6795 mL | 29.1988 mL | |
| H2O | 10 mM | 0.5840 mL | 2.9199 mL | 5.8398 mL | 14.5994 mL |
| 15 mM | 0.3893 mL | 1.9466 mL | 3.8932 mL | 9.7329 mL | |
| 20 mM | 0.2920 mL | 1.4599 mL | 2.9199 mL | 7.2997 mL | |
| 25 mM | 0.2336 mL | 1.1680 mL | 2.3359 mL | 5.8398 mL | |
| 30 mM | 0.1947 mL | 0.9733 mL | 1.9466 mL | 4.8665 mL | |
| 40 mM | 0.1460 mL | 0.7300 mL | 1.4599 mL | 3.6498 mL | |
| 50 mM | 0.1168 mL | 0.5840 mL | 1.1680 mL | 2.9199 mL | |
| 60 mM | 0.0973 mL | 0.4866 mL | 0.9733 mL | 2.4332 mL | |
| 80 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8249 mL | |
| 100 mM | 0.0584 mL | 0.2920 mL | 0.5840 mL | 1.4599 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Gabapentin Related Classifications
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