Istradefylline(KW-6002) (Synonyms: KW 6002) |
| Katalog-Nr.GC11590 |
Istradefyllin (KW-6002) ist ein sehr potenter, selektiver und oral aktiver Adenosin-A2A-Rezeptorantagonist mit einer Ki von 2,2 nM in experimentellen Modellen der Parkinson-Krankheit.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 155270-99-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *