S1RA
货号：
16279-10mg 基本售价：
8190.0 元 规格：
10 mg
产品信息
概述| 货号 | 16279-10mg |
| 描述 | The sigma-1 (σ1) receptor is an intracellular, non-opioid receptor that is abundantly expressed in the central nervous system as well as peripherally. S1RA is a potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM).1 It is active in vivo, dose-dependently inhibiting neuropathic pain in several animal models, including formalin-induced nociception and capsaicin-induced mechanical hypersensitivity.1,2 S1RA enhances peripheral µ-opioid analgesia without affecting opioid-induced constipation.3 |
| 别名 | E-52862; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Romero, L.,Zamanillo, D.,Nadal, X., et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. British Journal of Pharmacology 166(8), 2289-2306 (2012).
2.Abadias, M.,Escriche, M.,Vaqué, A., et al. Safety, tolerability and pharmacokinetics of single and multiple doses of a novel sigma-1 receptor antagonist in three randomized phase I studies. British Journal of Pharmacology 75(1), 103-117 (2013).
3.Sánchez-Fernández, C.,Montilla-García, A.,González-Cano, R., et al. Modulation of peripheral μ-opioid analgesia by σ1 receptors. Journal of Pharmacology and Experimental Therapeutics 348(1), 32-45 (2014).
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| 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 | 337.4 |
| 分子式 | C20H23N3O2 |
| CAS号 | 878141-96-9 |
| 稳定性 | ≥ 2 years |
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