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KI1354Pregabalin100 mg$2560

Chemical Characteristic

Product NamePregabalin
SynonymsLyrica
CAS No.148553-50-8
Molecular Weight 159.23
FormulaC8H17NO2
Chemical Name3-(Aminomethyl)-5-methyl-hexanoic acid
SmilesC(=O)(CC(CC(C)C)CN)O
Chemical Structure

Biological activities

Pregabalin is an anticonvulsant drug used for treating a variety of disorders, including partial seizures, neuropathic pain, generalized anxiety disorder, and fibromyalgia. Pregabalin competively binds to the α2δ (alpha2delta) subunit-1 and α2δ (alpha2delta) subunit-2 of the voltage-dependent calcium channel with IC50 values of 52 and 55 nM, respectively. Pregabalin, at the concentrations up to 100 µM, does not displace radioligands from 38 widely studied receptor sites including adenosine A, α-adrenoceptor, β-adrenoceptor, histamine H1, and muscarinic M.[1] Pregabalin decreases the release of neurotransmitters including glutamate, noradrenaline, substance P and calcitonin gene-related peptide.[2] Pregabalin produces concentration-dependent inhibitions of the K(+)-induced [Ca(2+)](i) increases in fura-2-loaded human neocortical synaptosomes with an IC50 of 17 µM.[3] Intravenous injection of 10-30 mg/kg pregabalin in vivo dose-dependently attenuates tactile allodyniaand thermal hyperalgesia. Furthermore, intravenous injection of pregabalin (30 mg/kg) significantly inhibits the ectopic discharges from injured afferents in a dose-dependent manner.[4]

Protocols

In vivo: Pregabalin is dissolved in sterile saline.[4]

References

[1] Li Z, et al. Pregabalin is a potent and selective ligand for α(2)δ-1 and α(2)δ-2 calcium channel subunits. Eur J Pharmacol. 2011, 667(1-3): 80-90.
[2] Micheva KD, et al. Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol. 2006, 70(2): 467-476.
[3] Fink K, et al. Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex. Neuropharmacology. 2002, 42(2): 229-236.
[4] Chen SR, et al. Stereospecific effect of pregabalin on ectopic afferent discharges and neuropathic pain induced by sciatic nerve ligation in rats. Anesthesiology. 2001, 95(6): 1473-1479.

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