Home Neuronal Signaling GABA Receptor agonist Gabapentin HCl For research use only.

Gabapentin HCl

Synonyms: Neurontin HCl

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

Gabapentin HCl Chemical Structure

Gabapentin HCl Chemical Structure

CAS No. 60142-95-2

Purity & Quality Control

Gabapentin HCl Related Products

Signaling Pathway

GABA Receptor Signaling Pathways

GABA Receptor Signaling Pathway

Biological Activity

Description Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.
Targets
GABA receptor [1]
In vitro
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04613024 Not yet recruiting
Weight Loss|Pain Postoperative
Stanford University
 July 1 2023 Early Phase 1
NCT05276089 Not yet recruiting
Opioid Use
Dr Yu Fu|Teesside University|NIHR Applied Research Collaboration for North East and North Cumbria|North East Academic Health Science Network|Newcastle University
 February 1 2023 Not Applicable
NCT05609682 Recruiting
Post Operative Pain
University of Oklahoma
 November 29 2022 Early Phase 1
NCT05750875 Completed
Pruritus|Uremia|Chronic Kidney Diseases
King Edward Medical University
 May 1 2022 Phase 4

Chemical Information & Solubility

Molecular Weight 207.7 Formula

C9H17NO2.HCl
CAS No. 60142-95-2 SDF Download Gabapentin HCl SDF
Smiles C1CCC(CC1)(CC(=O)O)CN.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 42 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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