An A2A receptor antagonist
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Labeled Version(s)
31240Istradefylline-13C-d3
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Istradefylline

Item No. 22958

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
Acetonitrile: 1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $134

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    10 mg

    $202

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    25 mg

    $466

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    Product Description

    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 (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.2 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.3 Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shimada, J., Nobuaki, K., Nonaka, H., et al. Adenosine A2A antagonists with potent anti-cataleptic activity. Bioorg. 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 monkeys. Ann. 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 models. Neuropharmacology 100(Pt. A), 48-58 (2016).