SB-366791
SB-366791 is a potent and selective TRPV1 antagonist. SB-366791 inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. SB-366791 decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | SB-366791 |
|---|---|
| Iupac 化学名称 | 3-(4-chlorophenyl)-N-(3-methoxyphenyl)-2-propenamide |
| 同义词 | SB-366791; SB 366791; SB366791. |
| 英文同义词 | SB-366791; SB 366791; SB366791. |
| 分子式 | C16H14ClNO2 |
| 分子量 | 287.743 |
| Smile | O=C(NC1=CC=CC(OC)=C1)/C=C/C2=CC=C(Cl)C=C2 |
| InChiKey | RYAMDQKWNKKFHD-JXMROGBWSA-N |
| InChi | InChI=1S/C16H14ClNO2/c1-20-15-4-2-3-14(11-15)18-16(19)10-7-12-5-8-13(17)9-6-12/h2-11H,1H3,(H,18,19)/b10-7+ |
| Cas号 | 472981-92-3 |
| 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: Lappin SC, Randall AD, Gunthorpe MJ, Morisset V. TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Eur J Pharmacol. 2006 Jul 1;540(1-3):73-81. Epub 2006 May 6. PubMed PMID: 16737693.
2: Gunthorpe MJ, Rami HK, Jerman JC, Smart D, Gill CH, Soffin EM, Luis Hannan S, Lappin SC, Egerton J, Smith GD, Worby A, Howett L, Owen D, Nasir S, Davies CH, Thompson M, Wyman PA, Randall AD, Davis JB. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology. 2004 Jan;46(1):133-49. Erratum in: Neuropharmacology. 2004 May;46(6):905. PubMed PMID: 14654105.
3: van Veghel D, Cleynhens J, Pearce LV, Blumberg PM, Van Laere K, Verbruggen A, Bormans G. Synthesis and biological evaluation of [¹¹C]SB366791: a new PET-radioligand for in vivo imaging of the TRPV1 receptor. Nucl Med Biol. 2013 Jan;40(1):141-7. doi: 10.1016/j.nucmedbio.2012.08.011. Epub 2012 Nov 7. PubMed PMID: 23141549.
4: Niiyama Y, Kawamata T, Yamamoto J, Furuse S, Namiki A. SB366791, a TRPV1antagonist, potentiates analgesic effects of systemic morphine in a murine model of bone cancer pain. Br J Anaesth. 2009 Feb;102(2):251-8. doi: 10.1093/bja/aen347. Epub 2008 Nov 26. PubMed PMID: 19038965.
5: Varga A, Németh J, Szabó A, McDougall JJ, Zhang C, Elekes K, Pintér E, Szolcsányi J, Helyes Z. Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat. Neurosci Lett. 2005 Sep 9;385(2):137-42. PubMed PMID: 15950380.
