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Cat. No. Name Size Price Add Cart
KI2076Istradefylline (KW-6002)5 mg$176
Istradefylline (KW-6002)10 mg$316
Istradefylline (KW-6002)25 mg$546
Istradefylline (KW-6002)50 mg$990

Chemical Characteristic

Product NameIstradefylline (KW-6002)
SynonymsKW-6002,KW6002
CAS No.155270-99-8
Molecular Weight 384.4
FormulaC20H24N4O4
Chemical Name?8-[(E)-2-(3,4-dimethoxyphenyl)vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione
Smilesn1(c(nc2n(c(=O)n(c(=O)c12)CC)CC)/C=C/c1cc(c(cc1)OC)OC)C
Chemical Structure

Biological activities

Istradefylline is a potent and selective adenosine A2A receptor antagonist with a Ki value of 2.2 nM.[1] Oral administration of istradefylline protects against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats. In addition, istradefylline treatment also prevents the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) in mice.[2] In vivo, istradefylline working with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys.[3]

Protocols

In vivo: Prior to use, istradefylline is suspended in 0.3% Tween-80 and 10% sucrose solution.[4]

References

[1] Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001, 21(10): RC143.
[2] Ikeda K, et al. Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's disease. J Neurochem. 2002, 80(2): 262-270.
[3] Kanda T, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol. 2000, 162(2): 321-327.
[4] Shiozaki S, et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999, 147(1): 90-95.

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