Gabapentin

Catalog No.S2133

For research use only.

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

Gabapentin  Chemical Structure

CAS No. 60142-96-3

Selleck's Gabapentin has been cited by 4 Publications

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Biological Activity

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

Gabapentin produces concentration-dependent inhibitions of the K(+)-induced [Ca(2+)](i) increase in fura-2-loaded human neocortical synaptosomes with IC50 of 17 mM and maximal inhibition of 37%. Gabapentin may bind to the Ca(2+) channel alpha 2 delta subunit to selectively attenuate depolarization-induced Ca(2+) influx of presynaptic P/Q-type Ca(2+) channels; this results in decreased glutamate/aspartate release from excitatory amino acid nerve terminals leading to a reduced activation of AMPA heteroreceptors on noradrenergic nerve terminals. [1] Gabapentin produces alterations in the cytosolic and extracellular concentrations of several amino acids, including L-leucine, L-valine and L-phenylalanine, in rat cortical astrocytes and synaptosomes, effects that are postulated to be of pharmacological significance. Gabapentin reduces potassium-evoked calcium influx via voltage-gated calcium channels in a mouse pituitary cell line that constitutively expresses GABAB receptors comprising the functional gb1a–gb2 subunit heterodimer. Gabapentin can increase N-methyl-d-aspartate (NMDA)-evoked currents in GABA-positive rat dorsal horn neurones in the presence of protein kinase C, possibly by increasing the glycine sensitivity of the NMDA receptor complex. Gabapentin produces a delayed allosteric enhancement of an unspecified voltage-activated potassium current in rat dorsal root ganglion neurons. [2]

In vivo Gabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 171.24
Formula

C9H17NO2

CAS No. 60142-96-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCC(CC1)(CC(=O)O)CN

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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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