| 货号 | 15771-25g |
| 描述 | Metamizole (sodium salt) is a nonopioid prodrug that is rapidly hydrolyzed to the metabolites 4-methylaminoantipyrine (MAA) and 4-aminoantipyrine (AA), which have analgesic and antipyretic effects.1 MAA has been shown to inhibit COX activity 8-9-fold more potently than AA (COX-1: IC50s = 2.6 and 20.8 µM, respectively, and COX-2: IC50s = 4.7 and 41.8 µM, respectively).2 These metabolites can be further acylated with arachidonic acid (Item No. 90010) to form compounds that can bind to central and peripheral cannabinoid (CB1 and CB2) receptors and TRPV1 receptors at low micromolar concentrations.1,3 Metamizole is associated with a risk of agranulocytosis and has been banned against using in clinical and pharmacological settings in the United States since 1977.4,5 |
| 别名 | Dipirona;Metamizol; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rogosch, T.,Sinning, C.,Podlewski, A., et al. Novel bioactive metabolites of dipyrone (metamizol). Bioorganic & Medicinal Chemistry 20(1), 101-107 (2012). 2.Hinz, B.,Cheremina, O.,Bachmakov, J., et al. Dipyrone elicits substantial inhibition of peripheral cyclooxygenases in humans: New insights into the pharmacology of an old analgesic. The FASEB Journal 21(10), 2343-2351 (2007). 3.Schlosburg, J.E.,Radanova, L.,Di Marzo, V., et al. Evaluation of the endogenous cannabinoid system in mediating the behavioral effects of dipyrone (metamizol) in mice. Behav.Pharmacol. 23(7), 722-726 (2012). 4.Taylor, L.,Abarca, S.,Henry, B., et al. Use of Neo-melubrina, a banned antipyretic drug, in San Diego, California: A survey of patients and providers. West.J.Med. 175(3), 159-163 (2001). 5.Hamerschlak, N. and Cavalcanti, A.B. Neutropenia, agranulocytosis and dipyrone. Sao Paulo Med.J. 123(5), 247-249 (2005). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 333.3 |
| 分子式 | C13H16N3O4S • Na |
| CAS号 | 68-89-3 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |