Gabapentin HCl

Catalog No.S1338 Synonyms: Neurontin HCl

For research use only.

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

Gabapentin HCl Chemical Structure

CAS No. 60142-95-2

Selleck's Gabapentin HCl has been cited by 3 Publications

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Biological Activity

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

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 207.7
Formula

C9H17NO2.HCl

CAS No. 60142-95-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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
NCT05100160 Not yet recruiting Drug: Gabapentin|Other: Placebo Thoracic|Pulmonary Disease M.D. Anderson Cancer Center July 31 2023 Phase 3
NCT05276089 Not yet recruiting Behavioral: Video message 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 Not yet recruiting Drug: Gabapentin|Drug: Placebo Post Operative Pain University of Oklahoma November 7 2022 Early Phase 1
NCT04613024 Not yet recruiting Drug: Topamax|Drug: Gabapentin Weight Loss|Pain Postoperative Stanford University July 1 2022 Early Phase 1
NCT05156060 Recruiting Drug: Gabapentin|Drug: Ketamine Head and Neck Cancer|Locally Advanced Head and Neck Carcinoma Natalie Lockney|Vanderbilt-Ingram Cancer Center January 24 2022 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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