| 货号 | 18398-1mg |
| 描述 | N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents.1 It is selective for NR2B subunit-containing receptors (IC50 = 1 µM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits.2,3 Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 µM, respectively).2 It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion.1 Eliprodil can also have proarrhythmic actions in hearts under normal conditions.4 |
| 别名 | SL 820715; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bath, C.P.,Farrell, L.N.,Gilmore, J., et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. European Journal of Pharmacology 299(1-3), 103-112 (1996). 2.Whittemore, E.R.,Ilyin, V.I. and Woodward, R.M. Antagonism of N-methyl-D-aspartate receptors by σ site ligands: Potency, subtype-selectivity and mechanisms of inhibition. Journal of Pharmacology and Experimental Therapeutics 282(1), 326-338 (1997). 3.Grimwood, S.,Richards, P.,Murray, F., et al. Characterisation of N-methyl-D-aspartate receptor-specific [3H]Ifenprodil binding to recombinant human NR1a/NR2B receptors compared with native receptors in rodent brain membranes. Journal of Neurochemistry 75(6), 2455-2463 (2000). 4.Lengyel, C.,Dézsi, L.,Biliczki, P., et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: Importance of the decreased repolarisation reserve in the development of proarrhythmic risk. British Journal of Pharmacology 143(1), 152-158 (2004). | |
| 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 | 347.9 |
| 分子式 | C20H23ClFNO |
| CAS号 | 119431-25-3 |
| 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。 |