For research use only. Not for therapeutic Use.
Istradefylline（Cat No.:I001965）is an adenosine A2A receptor antagonist used as an adjunctive therapy for Parkinson’s disease to reduce “off” episodes in patients on levodopa/carbidopa. By selectively blocking the A2A receptors in the brain, istradefylline modulates the dopamine pathways involved in motor control, helping to improve movement and reduce symptoms like stiffness and slowness. Unlike traditional dopaminergic therapies, it works through a non-dopaminergic mechanism, offering a complementary approach to managing Parkinson’s disease and enhancing the effectiveness of existing treatments with fewer side effects.
| Catalog Number | I001965 |
| CAS Number | 155270-99-8 |
| Synonyms | 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione |
| Molecular Formula | C20H24N4O4 |
| Purity | 98% |
| Target | Adenosine Receptor |
| Target Protein | P29274 |
| Solubility | DMSO: ＜ 6 mg/mL |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | Ki: 2.2 nM (adenosine A2A receptor) |
| IUPAC Name | 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione |
| InChI | InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+ |
| InChIKey | IQVRBWUUXZMOPW-PKNBQFBNSA-N |
| SMILES | CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)/C=C/C3=CC(=C(C=C3)OC)OC)C |
| Reference | </br>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 </br>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 </br>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 </br>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 </br>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 </br>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 </br>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 Article</br>8: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 </br>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 </br>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 |
