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Gabapentin

Catalog No. T0702 CAS 60142-96-3

Synonyms: Neurontin, Gabapentine, Aclonium

Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

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Gabapentin, CAS 60142-96-3

Pack Size	Availability	Price/USD
10 mg	In stock	$ 42.00
25 mg	In stock	$ 57.00
50 mg	In stock	$ 70.00
100 mg	In stock	$ 97.00
200 mg	In stock	$ 143.00
500 mg	In stock	$ 243.00
1 mL * 10 mM (in H2O)	In stock	$ 39.00

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Purity: 99.39%

Purity: 98%

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Description	Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.
Targets&IC50	Ca2+ channel:140 nM
In vitro	Administering 10-100 mg/kg of Gabapentin orally to rats results in a dose-dependent blockade of both static and dynamic allodynia.
In vivo	Gabapentin induces alterations in the cytoplasmic and extracellular concentrations of several amino acids (including L-leucine, L-valine, and L-phenylalanine) in rat cortical astrocytes and synaptosomes, suggesting pharmacological significance. In GABA B receptors composed of gb1a-GB2 subunit heterodimers, gabapentin decreases potassium-stimulated calcium influx via voltage-gated calcium channels. It potentiates N-methyl-D-aspartate-evoked currents in GABAergic rat spinal dorsal horn neurons in the presence of protein kinase C, possibly by enhancing the glycine sensitivity of the NMDA receptor complex. Gabapentin causes a delayed enhancement of indeterminate voltage-activated potassium currents in rat dorsal root ganglion neurons. In fura-2-loaded human neocortical synaptosomes, it concentration-dependently inhibits potassium(+)-induced [Ca(2+)] elevations with an IC50 of 17 mM and maximal inhibition of 37%. Gabapentin binds to the α2 delta subunit of calcium channels, selectively attenuating depolarization-induced presynaptic Ca(2+) influx through P/Q-type Ca(2+) channels, resulting in reduced glutamate/aspartate release from excitatory amino acid nerve terminals to AMPA heteroreceptors on noradrenergic nerve endings.

Synonyms	Neurontin, Gabapentine, Aclonium
Molecular Weight	171.24
Formula	C9H17NO2
CAS No.	60142-96-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Insoluble

H2O: 10 mM

References and Literature

1. Fink K, et al. Neuropharmacology, 2002, 42(2), 229-236. 2. Sills GJ, et al. Curr Opin Pharmacol, 2006, 6(1), 108-113. 3. Field MJ, et al. Pain, 1999, 80(1-2), 391-398. 4. Wang H, Li X, Zhangsun D, et al. The α9α10 Nicotinic Acetylcholine Receptor Antagonist αO-Conotoxin GeXIVA[1,2] Alleviates and Reverses Chemotherapy-Induced Neuropathic Pain. Marine drugs. 2019 May 5;17(5).

Citations

1. Wang H, Li X, Zhangsun D, et al. The α9α10 Nicotinic Acetylcholine Receptor Antagonist αO-Conotoxin GeXIVA[1,2] Alleviates and Reverses Chemotherapy-Induced Neuropathic Pain. Marine Drugs. 2019 May 5;17(5) 2. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Anti-Parkinson's Disease Compound Library Pediatric Drug Library Anti-Hypertension Compound Library Anti-Lung Cancer Compound Library Calcium Channel Compound Library

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Keywords

Gabapentin 60142-96-3 Membrane transporter/Ion channel Metabolism Neuroscience GABA Receptor Calcium Channel Inhibitor Neurontin inhibit Ca2+ channels Ca channels Gabapentine Aclonium inhibitor

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