Istradefylline

Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay). In vivo, istradefylline inhibits catalepsy induced by haloperidol (Cay-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. It also decreases bradykinesias induced by L-DOPA (Cay-13248) and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease. Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.Formal Name: 8-[(1E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione. CAS Number: 155270-99-8. Synonyms: KW 6002. Molecular Formula: C20H24N4O4. Formula Weight: 384.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Acetonitrile: 1 mg/ml. lambdamax: 228, 363 nm. SMILES: CCN(C(N1CC)=O)C2=C(N(C)C(/C=C/C3=CC=C(OC)C(OC)=C3)=N2)C1=O. InChi Code: InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+. InChi Key: IQVRBWUUXZMOPW-PKNBQFBNSA-N.