Preladenant
Preladenant, also known as SCH 420814, is a potent and selective antagonist at the adenosine A2A receptor, which was being researched as a potential treatment for Parkinson's disease. Positive results were reported in Phase II clinical trials in humans, but it did not prove itself to be more effective than a placebo during Phase III trials, and so was discontinued in May 2013.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Preladenant |
|---|---|
| Iupac 化学名称 | 2-(furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine |
| 同义词 | SCH420814; SCH-420814; SCH 420814; MK-3814; MK 3814; MK3814; Preladenant |
| 英文同义词 | SCH420814; SCH-420814; SCH 420814; MK-3814; MK 3814; MK3814; Preladenant |
| 分子式 | C25H29N9O3 |
| 分子量 | 503.567 |
| Smile | NC1=NC(N(CCN2CCN(C3=CC=C(OCCOC)C=C3)CC2)N=C4)=C4C5=NC(C6=CC=CO6)=NN15 |
| InChiKey | DTYWJKSSUANMHD-UHFFFAOYSA-N |
| InChi | InChI=1S/C25H29N9O3/c1-35-15-16-36-19-6-4-18(5-7-19)32-11-8-31(9-12-32)10-13-33-23-20(17-27-33)24-28-22(21-3-2-14-37-21)30-34(24)25(26)29-23/h2-7,14,17H,8-13,15-16H2,1H3,(H2,26,29) |
| Cas号 | 377727-87-2 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Hauser RA, Stocchi F, Rascol O, Huyck SB, Capece R, Ho TW, Sklar P, Lines C, Michelson D, Hewitt D. Preladenant as an Adjunctive Therapy With Levodopa in Parkinson Disease: Two Randomized Clinical Trials and Lessons Learned. JAMA Neurol. 2015 Dec 1;72(12):1491-500. doi: 10.1001/jamaneurol.2015.2268. PubMed PMID: 26523919.
2: Zhou X, Khanapur S, Huizing AP, Zijlma R, Schepers M, Dierckx RA, van Waarde A, de Vries EF, Elsinga PH. Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyr azolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors. J Med Chem. 2014 Nov 13;57(21):9204-10. doi: 10.1021/jm501065t. Epub 2014 Oct 15. PubMed PMID: 25279444.
3: Barret O, Hannestad J, Alagille D, Vala C, Tavares A, Papin C, Morley T, Fowles K, Lee H, Seibyl J, Tytgat D, Laruelle M, Tamagnan G. Adenosine 2A receptor occupancy by tozadenant and preladenant in rhesus monkeys. J Nucl Med. 2014 Oct;55(10):1712-8. doi: 10.2967/jnumed.114.142067. Epub 2014 Jul 31. PubMed PMID: 25082853.
4: Wang Z, Xuan F, Lin WH, Troyer MD, Tendolkar A, Cutler DL. Preladenant, a selective adenosine A₂A receptor antagonist, is not associated with QT/QTc prolongation. Eur J Clin Pharmacol. 2013 Oct;69(10):1761-7. doi: 10.1007/s00228-013-1541-5. Epub 2013 Jul 16. PubMed PMID: 23857248.
5: Factor SA, Wolski K, Togasaki DM, Huyck S, Cantillon M, Ho TW, Hauser RA, Pourcher E. Long-term safety and efficacy of preladenant in subjects with fluctuating Parkinson's disease. Mov Disord. 2013 Jun;28(6):817-20. doi: 10.1002/mds.25395. Epub 2013 Apr 15. PubMed PMID: 23589371.
6: Rosse G. Metabolites of the pyrimidine amine preladenant as adenosine a2a receptor antagonists. ACS Med Chem Lett. 2012 Nov 30;4(1):5-6. doi: 10.1021/ml300397j. eCollection 2013 Jan 10. PubMed PMID: 24900549; PubMed Central PMCID: PMC4027435.
7: Cutler DL, Tendolkar A, Grachev ID. Safety, tolerability and pharmacokinetics after single and multiple doses of preladenant (SCH420814) administered in healthy subjects. J Clin Pharm Ther. 2012 Oct;37(5):578-87. doi: 10.1111/j.1365-2710.2012.01349.x. Epub 2012 Jun 7. PubMed PMID: 22676397.
8: Cutler DL, Tendolkar A, Grachev ID. Evaluation of the effects of a high-fat meal on the oral bioavailability of a single dose of preladenant in healthy subjects. J Clin Pharmacol. 2012 Nov;52(11):1698-703. doi: 10.1177/0091270011428321. Epub 2011 Dec 13. PubMed PMID: 22167566.
9: Hauser RA, Cantillon M, Pourcher E, Micheli F, Mok V, Onofrj M, Huyck S, Wolski K. Preladenant in patients with Parkinson's disease and motor fluctuations: a phase 2, double-blind, randomised trial. Lancet Neurol. 2011 Mar;10(3):221-9. doi: 10.1016/S1474-4422(11)70012-6. PubMed PMID: 21315654.
10: Salamone JD. Preladenant, a novel adenosine A(2A) receptor antagonist for the potential treatment of parkinsonism and other disorders. IDrugs. 2010 Oct;13(10):723-31. Review. PubMed PMID: 20878595.
11: Hodgson RA, Bedard PJ, Varty GB, Kazdoba TM, Di Paolo T, Grzelak ME, Pond AJ, Hadjtahar A, Belanger N, Gregoire L, Dare A, Neustadt BR, Stamford AW, Hunter JC. Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders. Exp Neurol. 2010 Oct;225(2):384-90. doi: 10.1016/j.expneurol.2010.07.011. Epub 2010 Jul 23. PubMed PMID: 20655910.
12: Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, Cohen-Williams ME, Higgins GA, Impagnatiello F, Nicolussi E, Parra LE, Foster C, Zhai Y, Neustadt BR, Stamford AW, Parker EM, Reggiani A, Hunter JC. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e ][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression. J Pharmacol Exp Ther. 2009 Jul;330(1):294-303. doi: 10.1124/jpet.108.149617. Epub 2009 Mar 30. PubMed PMID: 19332567.
