An internal standard for the quantification of paraxanthine
货号:ajcx23238
CAS:117490-41-2
分子式:C7H2D6N4O2
分子量：186.2
溶解度:DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Paraxanthine-d₆is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine .¹It is formedviaN3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A₁and A₂receptor antagonist (K_is = 35 and 22 µM, respectively).²In vivo, paraxanthine (30 mg/kg) increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A₁agonist CPA or the adenosine A₂receptor agonist CGS 21680 in rats not habituated to caffeine.³It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.⁴

1.Tassaneeyakul, W., Birkett, D.J., McManus, M.E., et al.Caffeine metabolism by human hepatic cytochromes P450: contributions of 1A2, 2E1 and 3A isoformsBiochem. Pharmacol.47(10)1767-1776(1994) 2.Chou, C.-C., and Vickroy, T.W.Antagonism of adenosine receptors by caffeine and caffeine metabolites in equine forebrain tissuesAm. J. Vet. Res.64(2)216-224(2003) 3.OrrÚ, M., Guitart, X., Karcz-Kubicha, M., et al.Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humansNeuropharmacology67476-484(2013) 4.Okuro, M., Fujiki, N., Kotorii, N., et al.Effects of paraxanthine and caffeine on sleep, locomotor activity, and body temperature in orexin/ataxin-3 transgenic narcoleptic miceSleep33(7)930-942(2010)