| 货号 | 11989-25mg |
| 描述 | Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke.1,2 NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively).3 At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes.3 At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ferraguti, F.,Crepaldi, L., and Nicoletti, F. Metabotropic glutamate 1 receptor: Current concepts and perspectives. Pharmacological Reviews 60(4), 536-581 (2008). 2.Mabire, D.,Coupa, S.,Adelinet, C., et al. Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. Journal of Medicinal Chemistry 48, 2134-2153 (2005). 3.VanWagenen, B.C.,Smith, D.L.,Artman, L.D., et al. Structure-activity relationship studies of NPS 2390: a potent and selective group I metabotropic glutamate receptor antagonist. Society for Neuroscience 1-2 (2000). 4.Lavreysen, H.,Janssen, C.,Bischoff, F., et al. [3H]R214127: A novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. Molecular Pharmacology 63(5), 1082-1093 (2003). | |
| 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 | 307.4 |
| 分子式 | C19H21N3O |
| CAS号 | 226878-01-9 |
| 稳定性 | ≥ 2 years |
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