Istradefylline

• CAT Number: I001965
• CAS Number: 155270-99-8
• Molecular Formula: C20H24N4O4
• Molecular Weight: 384.43
• Purity: ≥95%
• Synonyms: 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione
• Target: Adenosine Receptor
• Solubility: DMSO: ＜ 6 mg/mL
• Storage: 3 years -20C powder
• IC50: 2.2 nM (Ki)

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson/’s disease.IC50 value: 2.2 nM (Ki)Target: adenosine A2A receptorIstradefylline reduces dyskinesia resulting from long-term treatment with classical antiparkinson drugs such as levodopa. Istradefylline is an analog of caffeine.

Reference

1: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. Ko WK, Camus SM, Li Q, Yang J, McGuire S, Pioli EY, Bezard E.Neuropharmacology. 2016 Nov;110(Pt A):48-58. doi: 10.1016/j.neuropharm.2016.07.012. Epub 2016 Jul 14. PMID: 27424102 2:Clinical efficacy of istradefylline on lower urinary tract symptoms in Parkinson/’s disease. Kitta T, Yabe I, Takahashi I, Matsushima M, Sasaki H, Shinohara N.Int J Urol. 2016 Oct;23(10):893-894. doi: 10.1111/iju.13160. Epub 2016 Jul 8. No abstract available. PMID: 27388933 3:The efficacy of oral adenosine A(2A) antagonist istradefylline for the treatment of moderate to severe Parkinson/’s disease. Vorovenci RJ, Antonini A.Expert Rev Neurother. 2015;15(12):1383-90. doi: 10.1586/14737175.2015.1113131. PMID: 26630457 4:The adenosine A2A receptor antagonist, istradefylline enhances anti-parkinsonian activity induced by combined treatment with low doses of L-DOPA and dopamine agonists in MPTP-treated common marmosets. Uchida S, Soshiroda K, Okita E, Kawai-Uchida M, Mori A, Jenner P, Kanda T.Eur J Pharmacol. 2015 Nov 5;766:25-30. doi: 10.1016/j.ejphar.2015.09.028. Epub 2015 Sep 28. PMID: 26415982 5:Clinical efficacy of istradefylline versus rTMS on Parkinson/’s disease in a randomized clinical trial. Li ZJ, Wu Q, Yi CJ.Curr Med Res Opin. 2015 Nov;31(11):2055-8. doi: 10.1185/03007995.2015.1086994. Epub 2015 Sep 22. PMID: 26393386 6:A long-term study of istradefylline safety and efficacy in patients with Parkinson disease. Kondo T, Mizuno Y; Japanese Istradefylline Study Group..Clin Neuropharmacol. 2015 Mar-Apr;38(2):41-6. doi: 10.1097/WNF.0000000000000073. PMID: 25768849 7:Istradefylline is recommended for morning use: a report of 4 cases. Matsuura K, Tomimoto H.Intern Med. 2015;54(5):509-11. doi: 10.2169/internalmedicine.54.3522. Epub 2015 Jan 15. PMID: 25758079 Free Article8:The safety of istradefylline for the treatment of Parkinson/’s disease. Müller T.Expert Opin Drug Saf. 2015 May;14(5):769-75. doi: 10.1517/14740338.2015.1014798. Epub 2015 Feb 13. Review. PMID: 25676023 9:The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists in MPTP-treated common marmosets. Uchida S, Soshiroda K, Okita E, Kawai-Uchida M, Mori A, Jenner P, Kanda T.Eur J Pharmacol. 2015 Jan 15;747:160-5. doi: 10.1016/j.ejphar.2014.11.038. Epub 2014 Dec 11. PMID: 25499739 10:Efficacy of adenosine A2A receptor antagonist istradefylline as augmentation for Parkinson/’s disease: a meta-analysis of randomized controlled trials. Tao Y, Liang G.Cell Biochem Biophys. 2015 Jan;71(1):57-62. doi: 10.1007/s12013-014-0162-7. PMID: 25096504