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Gabapentin hydrochloride

Catalog No. T6507 CAS 60142-95-2

Synonyms: Neurontin HCl, Gabapentin HCl

Gabapentin hydrochloride (Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

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Gabapentin hydrochloride Chemical Structure

Gabapentin hydrochloride, CAS 60142-95-2

Pack Size	Availability	Price/USD
25 mg	In stock	$ 34.00
50 mg	In stock	$ 51.00
100 mg	In stock	$ 72.00
200 mg	In stock	$ 105.00
500 mg	In stock	$ 176.00

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Purity: 99.46%

Biological Description

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Description	Gabapentin hydrochloride (Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.
Targets&IC50	α2δ Ca2+ channel:140 nM
In vitro	Gabapentin suppresses ectopic afferent discharge activity generated from injured peripheral nerves. Gabapentin, in a range of 30 to 90 mg/kg, significantly attenuates allodynia in nerve-injured rats. Gabapentin dose-dependently inhibits the ectopic discharge activity of 15 injured sciatic afferent nerve fibers through an action on impulse generation. [1] Gabapentin inhibits KCl (30 mM)-evoked voltage-dependent Ca(2+) influx. Gabapentin potently inhibits the peak whole-cell Ca(2+) channel current (I(Ba)) in a dose-dependent manner with an estimated IC(50) value of 167 nM. Gabapentin inhibition is voltage-dependent, producing an approximately 7 mV hyperpolarizing shift in current voltage properties and reducing a non-inactivating component of whole-cell current activated at relatively depolarized potentials. [2] Gabapentin selectively activates heterodimeric GABAB1a-B2 receptors, but not GABAB1b-B2 or GABAB1c-B2 receptors. Gabapentin selectively activates presynaptic GABAB heteroreceptors on glutamatergic terminals, but not GABAB autoreceptors on GABAergic terminals. Gabapentin is found to inhibit both the excitatory synaptic transmission in vitro and the neuronal response to noxious electrical and mechanical stimulation in vivo mediated by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), but not those mediated by N-methyl-D-asparate (NMDA) receptors. Gabapentin acts as an AMPA-receptor antagonist in the rat spinal cord to exert its spinal antinociceptive effect. Gabapentin depresses, but NMDA enhanced, the presynaptic fiber volley in the CA1 region of rat hippocampal slices. [3]

Synonyms	Neurontin HCl, Gabapentin HCl
Molecular Weight	207.7
Formula	C9H17NO2·HCl
CAS No.	60142-95-2

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. Pan HL, et al. J Pharmacol Exp Ther, 1999, 288(3), 1026-1030. 2. Sutton KG, et al. Br J Pharmacol,2002, 135(1), 257-265. 3. Cheng JK, et al. J Pharmacol Sci, 2006, 100(5), 471-486.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Orally Active Compound Library Ion Channel Inhibitor Library Bioactive Compound Library

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Keywords

Gabapentin hydrochloride 60142-95-2 Membrane transporter/Ion channel Metabolism Neuroscience Calcium Channel GABA Receptor Inhibitor Gabapentin Ca channels inhibit Ca2+ channels Gabapentin Hydrochloride Neurontin HCl Gabapentin HCl inhibitor

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