Home Neuronal Signaling GABA Receptor agonist Gabapentin HCl

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Gabapentin HCl GABA Receptor agonist

Cat.No.S1338

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

Chemical Structure

Molecular Weight: 207.7

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

Water : 42 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 207.7 Formula

C9H17NO2.HCl

 Storage (From the date of receipt)
CAS No. 60142-95-2 Download SDF Storage of Stock Solutions

Synonyms Neurontin HCl SMILES C1CCC(CC1)(CC(=O)O)CN.Cl

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Mechanism of Action

Targets/IC50/Ki
GABA receptor
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. 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. 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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-24)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07158476 RECRUITING
ACL Surgery; Pain Management
St. Louis University
 2025-10-21 PHASE4
NCT06992427 RECRUITING
Head and Neck Squamous Cell Carcinoma; Stage I Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8; Stage II Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8; Stage III Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8; Stage IV Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8
Alliance for Clinical Trials in Oncology
 2025-06-05 PHASE3
NCT02219373 NOT_YET_RECRUITING
Pediatric Chronic Neuropathic Pain
Boston Children's Hospital
 2026-06 PHASE3
NCT05827159 RECRUITING
Alcohol Use Disorder
Yale University
 2024-08-17 PHASE3
NCT07308717 RECRUITING
Breast Cancer
Memorial Sloan Kettering Cancer Center
 2025-12-16 PHASE4
NCT07047040 NOT_YET_RECRUITING
Pain, Postoperative; Osteoarthritis, Knee
Assiut University
 2025-08-15 PHASE2; PHASE3

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