product name Gabapentin
Description: Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain. Gabapentin is a major inhibitory neurotransmitter that functions by binding to the GABA receptors located in the spinal cord. Gabapentin also binds to a novel site on voltage-sensitive Ca2+ channels. Additionally, Gabapentin demonstrates inhibition of dopamine release from caudate nucleus, prevent neuronal cell death, and is antinociceptive. It is structurally similar to GABA and is reported in various research studies to increase GABA concentrations within the brain.
References: Neuropharmacology. 2002 Feb;42(2):229-36; Curr Opin Pharmacol. 2006 Feb;6(1):108-13.
171.24
Formula
C9H17NO2
CAS No.
60142-96-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 34 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19421788
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Gabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats. |
| Animal model | Rats |
| Formulation & Dosage | 10-100 mg/kg; p.o. |
| References | Neuropharmacology. 2002 Feb;42(2):229-36; Curr Opin Pharmacol. 2006 Feb;6(1):108-13. |
