(±)-5'-Chloro-5'-deoxy-ENBA

(±)-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.