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Gabapentin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gabapentin图片
CAS NO:60142-96-3
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
Gabapentin HCl (Neurontin; Aclonium; Convalis; Gabapentin Stada), the hydrochloride salt of gabapentin which is a GABA analog, is an orally bioavailable medication that was approved for use in the treatment of seizures and neuropathic pain. Gabapentin is structurally similar to GABA and is reported in various research studies to be able to increase GABA concentrations in the brain.
理化性质和储存条件
Molecular Weight (MW)171.24
FormulaC9H17NO2
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
Other info

Chemical Name: 2-[1-(aminomethyl)cyclohexyl]acetic acid

SMILES Code: NCC1(CCCCC1)CC(=O)O

Synonyms

Neurontin; Gabapentin; Neurontin; Gabapentine; Gabapentin HCl; Gabapentin hydrochloride; Aclonium; Convalis; gabapentin; Gabapentin Hexal; Gabapentin Stada

实验参考方法
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.

In VivoGabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats.
Animal modelRats
Formulation & Dosage10-100 mg/kg; p.o.
References

Neuropharmacology. 2002 Feb;42(2):229-36; Curr Opin Pharmacol. 2006 Feb;6(1):108-13.