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Istradefylline(KW-6002)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Istradefylline(KW-6002)图片
CAS NO:155270-99-8
规格:98%
分子量:384.43
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Selective A2A receptor antagonist
CAS:155270-99-8
分子式:C20H24N4O4
分子量:384.43
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.