产品描述:
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.