Istradefylline-13C-d3 is intended for use as an internal standard for the quantification of istradefylline by GC- or LC-MS. Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay).1 In vivo, istradefylline inhibits catalepsy induced by haloperidol 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.2 It also decreases bradykinesias induced by L-DOPA and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease.3 Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.
1.Shimada, J., Nobuaki, K., Nonaka, H., et al.Adenosine A2A antagonists with potent anti-cataleptic activityBioorg. Med. Chem. Lett.7(18)2349-2352(1997) 2.Kanda, T., Jackson, M.J., Smith, L.A., et al.Adenosine A2A antagonist: A novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeysAnn. Neurol.43(4)507-513(1998) 3.Ko, W.K.D., Camus, S.M., Li, Q., et al.An evaluation of istradefylline treatment on Parkinsonian motor and cognitive deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaque modelsNeuropharmacology100(Pt. A)48-58(2016)