Formulation: A crystalline solid
Formal Name: 8-[(1E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
Purity: ≥98%
Formula Markup: C20H24N4O4
Formula Weight: 384,4
Shelf life (days): 1460
CAS Number: 155270-99-8
Notes: 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.