| CAS NO: | 103626-26-2 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 379.84 |
| Cas No. | 103626-26-2 |
| Formula | C17H22ClN5O3 |
| Solubility | <37.98mg/ml in DMSO;<37.98mg/ml in ethanol |
| Chemical Name | (2R,3R,4S,5S)-2-(6-((1R,2R,4R)-bicyclo[2.2.1]heptan-2-ylamino)-9H-purin-9-yl)-5-(chloromethyl)tetrahydrofuran-3,4-diol |
| Canonical SMILES | ClC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)N2C(N=CN=C3N[C@H]4[C@H](CC5)C[C@@H]5C4)=C3N=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
(±)-5'-Chloro-5'-deoxy-ENBA是一种选择性的和高亲和性的腺苷A1受体激动剂，Ki值为0.51 nM[1]。
腺苷A1受体介导神经和心脏保护（抗心律失常效应），脂肪组织中脂肪分解的减少和神经性疼痛的减少[1]。
在注射1-2 mg/kg福尔马林的小鼠中，(±)-5'-Chloro-5'-deoxy-ENBA抑制福尔马林诱导的疼痛反应的第一和第二阶段[1]。在神经性疼痛（坐骨神经保留性神经损伤（SNI））小鼠模型中，(±)-5'-Chloro-5'-deoxy-ENBA（0.5 mg/kg）在SNI后的7天和3天时减少热痛觉过敏和机械异常性疼痛，而对运动协调和动脉血压没有显著影响。(±)-5'-Chloro-5'-deoxy-
ENBA慢性治疗也减少活化和增生性的小胶质细胞[2]。在帕金森病（PD）小鼠模型中，(±)-5'-Chloro-5'-deoxy-ENBA阻止SKF诱导的sIPSC频率和eIPSC振幅的增加。在单侧DA去神经的小鼠中，(±)-5'-Chloro-5'-deoxy-ENBA减少L-DOPA诱导的异常不自主运动的发展[3]。
参考文献：
[1]. Franchetti P, Cappellacci L, Vita P, Petrelli R, et al. N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. J Med Chem, 2009, 52(8): 2393-2406.
[2]. Luongo L, Petrelli R, Gatta L, et al. 5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions. Molecules, 2012, 17(12): 13712-13726.
[3]. Mango D, Bonito-Oliva A, Ledonne A, et al. Adenosine A1 receptor stimulation reduces D1 receptor-mediated GABAergic transmission from striato-nigral terminals and attenuates l-DOPA-induced dyskinesia in dopamine-denervated mice. Exp Neurol, 2014, 261: 733-743.
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