S1RA
S1RA(E-52862) is a potent and selective sigma-1 receptor(1R, Ki=17 nM) antagonist, showed good selectivity against 2R (Ki > 1000 nM).
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | S1RA |
|---|---|
| Iupac 化学名称 | 4-(2-((5-Methyl-1-(naphthalen-2-yl)-1h-pyrazol-3-yl)oxy)ethyl)morpholine |
| 同义词 | E-52862; E 52862; E52862; S1RA; E-52862; E-52862; |
| 英文同义词 | E-52862; E 52862; E52862; S1RA; E-52862; E-52862; |
| 分子式 | C20H23N3O2 |
| 分子量 | 337.42 |
| Smile | CC1=CC(=NN1C1=CC2=CC=CC=C2C=C1)OCCN1CCOCC1 |
| InChiKey | DGPGXHRHNRYVDH-UHFFFAOYSA-N |
| InChi | InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3 |
| Cas号 | 878141-96-9 |
| 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 | 类白色至白色固体 |
|---|---|
| 纯度 | 98% |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO；不溶于水 |
| 处理方式 | |
| 运输条件 | 可在常温下运输 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Paniagua N, Girón R, Goicoechea C, López-Miranda V, Vela JM, Merlos M, Martín Fontelles MI. Blockade of sigma 1 receptors alleviates sensory signs of diabetic neuropathy in rats. Eur J Pain. 2016 Jun 24. doi: 10.1002/ejp.897. [Epub ahead of print] PubMed PMID: 27341510.
2: Gris G, Portillo-Salido E, Aubel B, Darbaky Y, Deseure K, Vela JM, Merlos M, Zamanillo D. The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats. Sci Rep. 2016 Apr 18;6:24591. doi: 10.1038/srep24591. PubMed PMID: 27087602; PubMed Central PMCID: PMC4834548.
3: Romero L, Merlos M, Vela JM. Antinociception by Sigma-1 Receptor Antagonists: Central and Peripheral Effects. Adv Pharmacol. 2016;75:179-215. doi: 10.1016/bs.apha.2015.11.003. Epub 2016 Jan 27. PubMed PMID: 26920013.
4: Täubel J, Ferber G, Lorch U, Wang D, Sust M, Camm AJ. Single Doses up to 800 mg of E-52862 Do Not Prolong the QTc Interval--A Retrospective Validation by Pharmacokinetic-Pharmacodynamic Modelling of Electrocardiography Data Utilising the Effects of a Meal on QTc to Demonstrate ECG Assay Sensitivity. PLoS One. 2015 Aug 20;10(8):e0136369. doi: 10.1371/journal.pone.0136369. eCollection 2015. PubMed PMID: 26291080; PubMed Central PMCID: PMC4546378.
5: Vela JM, Merlos M, Almansa C. Investigational sigma-1 receptor antagonists for the treatment of pain. Expert Opin Investig Drugs. 2015;24(7):883-96. doi: 10.1517/13543784.2015.1048334. Epub 2015 Jun 3. Review. PubMed PMID: 26037209.
6: Ferber G, Wang D, Täubel J. Concentration-effect modeling based on change from baseline to assess the prolonging effect of drugs on QTc together with an estimate of the circadian time course. J Clin Pharmacol. 2014 Dec;54(12):1400-6. doi: 10.1002/jcph.347. Epub 2014 Jun 27. PubMed PMID: 24935561.
7: Gris G, Merlos M, Vela JM, Zamanillo D, Portillo-Salido E. S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in mice. Behav Pharmacol. 2014 Jun;25(3):226-35. doi: 10.1097/FBP.0000000000000038. PubMed PMID: 24776490.
8: Vidal-Torres A, Fernández-Pastor B, Carceller A, Vela JM, Merlos M, Zamanillo D. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 May;129(3):484-94. doi: 10.1111/jnc.12648. Epub 2014 Jan 29. PubMed PMID: 24384038.
9: Sánchez-Fernández C, Montilla-García Á, González-Cano R, Nieto FR, Romero L, Artacho-Cordón A, Montes R, Fernández-Pastor B, Merlos M, Baeyens JM, Entrena JM, Cobos EJ. Modulation of peripheral μ-opioid analgesia by σ1 receptors. J Pharmacol Exp Ther. 2014 Jan;348(1):32-45. doi: 10.1124/jpet.113.208272. Epub 2013 Oct 23. PubMed PMID: 24155346.
10: Vidal-Torres A, de la Puente B, Rocasalbas M, Touriño C, Bura SA, Fernández-Pastor B, Romero L, Codony X, Zamanillo D, Buschmann H, Merlos M, Baeyens JM, Maldonado R, Vela JM. Sigma-1 receptor antagonism as opioid adjuvant strategy: enhancement of opioid antinociception without increasing adverse effects. Eur J Pharmacol. 2013 Jul 5;711(1-3):63-72. doi: 10.1016/j.ejphar.2013.04.018. Epub 2013 Apr 28. PubMed PMID: 23632394.
11: Laurini E, Da Col V, Wünsch B, Pricl S. Analysis of the molecular interactions of the potent analgesic S1RA with the σ1 receptor. Bioorg Med Chem Lett. 2013 May 15;23(10):2868-71. doi: 10.1016/j.bmcl.2013.03.087. Epub 2013 Mar 30. PubMed PMID: 23582276.
12: Collina S, Gaggeri R, Marra A, Bassi A, Negrinotti S, Negri F, Rossi D. Sigma receptor modulators: a patent review. Expert Opin Ther Pat. 2013 May;23(5):597-613. doi: 10.1517/13543776.2013.769522. Epub 2013 Feb 7. Review. PubMed PMID: 23387851.
13: Nieto FR, Cendán CM, Sánchez-Fernández C, Cobos EJ, Entrena JM, Tejada MA, Zamanillo D, Vela JM, Baeyens JM. Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice. J Pain. 2012 Nov;13(11):1107-21. doi: 10.1016/j.jpain.2012.08.006. Epub 2012 Oct 12. PubMed PMID: 23063344.
14: Wünsch B. The σ(1) receptor antagonist S1RA is a promising candidate for the treatment of neurogenic pain. J Med Chem. 2012 Oct 11;55(19):8209-10. doi: 10.1021/jm3011993. Epub 2012 Sep 5. PubMed PMID: 22951043.
15: Díaz JL, Cuberes R, Berrocal J, Contijoch M, Christmann U, Fernández A, Port A, Holenz J, Buschmann H, Laggner C, Serafini MT, Burgueño J, Zamanillo D, Merlos M, Vela JM, Almansa C. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24. doi: 10.1021/jm3007323. Epub 2012 Jul 27. PubMed PMID: 22784008.
16: Abadias M, Escriche M, Vaqué A, Sust M, Encina G. Safety, tolerability and pharmacokinetics of single and multiple doses of a novel sigma-1 receptor antagonist in three randomized phase I studies. Br J Clin Pharmacol. 2013 Jan;75(1):103-17. doi: 10.1111/j.1365-2125.2012.04333.x. PubMed PMID: 22607269; PubMed Central PMCID: PMC3555050.
17: Romero L, Zamanillo D, Nadal X, Sánchez-Arroyos R, Rivera-Arconada I, Dordal A, Montero A, Muro A, Bura A, Segalés C, Laloya M, Hernández E, Portillo-Salido E, Escriche M, Codony X, Encina G, Burgueño J, Merlos M, Baeyens JM, Giraldo J, López-García JA, Maldonado R, Plata-Salamán CR, Vela JM. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. doi: 10.1111/j.1476-5381.2012.01942.x. PubMed PMID: 22404321; PubMed Central PMCID: PMC3448894.
