Gabapentin HCl

For research use only.

Licensed by Pfizer Catalog No.S1338

2 publications

Gabapentin HCl Chemical Structure

CAS No. 60142-95-2

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

Selleck's Gabapentin HCl has been cited by 2 publications

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Biological Activity

Description Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
GABA receptor [1]
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]


Solubility (25°C)

In vitro Water 42 mg/mL (202.21 mM)
DMSO Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 207.7


CAS No. 60142-95-2
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(CC1)(CC(=O)O)CN.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04613024 Not yet recruiting Drug: Topamax|Drug: Gabapentin Weight Loss|Pain Postoperative Stanford University May 1 2021 Early Phase 1
NCT04805827 Completed Drug: Gabapentin|Drug: Neurontin Healthy Pharma Guide CRO February 25 2021 Not Applicable
NCT04068506 Completed Drug: Gabapentin 600 mg Tab Hand Injuries Dow University of Health Sciences September 1 2019 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID