For research use only.
Licensed by Pfizer Catalog No.S2133
CAS No. 60142-96-3
Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
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|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||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04613024||Not yet recruiting||Drug: Topamax|Drug: Gabapentin||Weight Loss|Pain Postoperative||Stanford University||May 1 2021||Early Phase 1|
|NCT04805827||Completed||Drug: Gabapentin|Drug: Neurontin||Healthy||Pharma Guide CRO||February 25 2021||Not Applicable|
|NCT04068506||Completed||Drug: Gabapentin 600 mg Tab||Hand Injuries||Dow University of Health Sciences||September 1 2019||Phase 4|
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