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

Gabapentin

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

Gabapentin Chemical Structure

Gabapentin Chemical Structure

CAS: 60142-96-3

Selleck's Gabapentin has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 100.0%
100.0

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

Molecular Weight 171.24 Formula

C9H17NO2
CAS No. 60142-96-3 SDF Download Gabapentin SDF
Smiles C1CCC(CC1)(CC(=O)O)CN
Storage (From the date of receipt)

In vitro
Batch:

Water : 34 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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