Formulation: A solid
Formal Name: (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-(methyl-13C-d3)-3,7-dihydro-1H-purine-2,6-dione
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C19[13C]H21D3N4O4
Formula Weight: 388,5
Shelf life (days): 1460
Notes: Istradefylline-13C-d3 is intended for use as an internal standard for the quantification of istradefylline (Item No. 22958) by GC- or LC-MS. Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay).{37122} In vivo, istradefylline inhibits catalepsy induced by haloperidol (Item No. 12014) with an ED50 value of 0.23 mg/kg in rats. Oral administration of istradefylline alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson's disease.{37123} It also decreases bradykinesias induced by L-DOPA (Item No. 13248) and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease.{37124} Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.
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