Licensed by Pfizer Catalog No.S2133
Molecular Weight(MW): 171.24
Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
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Choose Selective GABA Receptor Inhibitors
|Description||Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.|
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.  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. 
|In vivo||Gabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats. |
|In vitro||Water||34 mg/mL (198.55 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03275012||Not yet recruiting||Chronic Pain||Pharmaceutical Research Management srl|European Commission||October 2019||Phase 2|
|NCT03668041||Not yet recruiting||Insomnia||VA Office of Research and Development||August 1 2019||Phase 3|
|NCT03472521||Not yet recruiting||Opioid Use|Postpartum Disorder|Chronic Pain Syndrome||Stanford University||April 1 2019||Phase 4|
|NCT03689114||Not yet recruiting||Epilepsies Partial||Mario Negri Institute for Pharmacological Research|Azienda Ospedaliera San Gerardo di Monza|Ministry of Health Italy||January 2019||Phase 4|
|NCT02219373||Not yet recruiting||Pediatric Chronic Neuropathic Pain||Boston Children’s Hospital||January 2019||Phase 3|
|NCT03682367||Not yet recruiting||Cancer of Head and Neck|Narcotic Use||University of California Davis||December 1 2018||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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