Istradefylline(KW-6002) (Synonyms: KW 6002) |
| Catalog No.GC11590 |
Istradefylline(KW-6002) is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
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Cas No.: 155270-99-8
Sample solution is provided at 25 µL, 10mM.
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KW-6002 is a selective adenosine A2A receptor antagonist, offering a novel mechanistic approach for the treatment of Parkinson’s disease (PD). A2A blockade will increase in GABAergic inhibition on the medium-sized neurons, leading to a net decrease in excessive activation of striatopallidal output.
In vitro: The affinity of KW-6002 for the A2AR is 70-fold greater than that for the A1 receptor. The binding affinities (Ki) of KW-6002 for human A1 receptor and A2A receptor are >287 nM and 9.12 nM, respectively [1].
In vivo: In MPTP neurotoxin model of PD in mice, KW-6002 significantly attenuated striatal dopamine depletion under various conditions. In addition, pretreatment with KW-6002 (3.3 mg/kg, i.p.) before a single dose of MPTP attenuated the partial dopamine and DOPAC depletions 1 week later [2].
Clinical trial: In a clinical study, the authors evaluated the safety and efficacy of KW-6002 40 mg as monotherapy for Parkinson’s disease (PD) in 176 patients. The primary efficacy outcome was changed from baseline to endpoint, while safe and well-tolerated, failed to show a significant improvement from placebo for this endpoint [1].
References:
[1] Park A, Stacy M. Istradefylline for the treatment of Parkinson's disease. Expert Opin Pharmacother. 2012 Jan;13(1):111-4.
[2] Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N Jr, Schwarzschild MA. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001;21(10):RC143.
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