A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through σ1 receptors
A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through σ1 receptors
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DOI：
10.1016/j.ejphar.2006.02.026
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发表时间：
2006-04-24
影响因子：
5
通讯作者：
Drago, F
中科院分区：
文献类型：
--
作者：
Bucolo, C;Marrazzo, A;Drago, F
采用大鼠视网膜缺血再灌注损伤模型，观察了新型N-甲基金刚烷-1-胺类化合物[(-)-MR22]对视网膜变性的影响。在缺血损伤之前，药物是在腹膜内注射的。与缺血对照组相比，新的选择性Sigma(1)受体配基可显著抑制视网膜生化改变，即乳酸含量的增加、葡萄糖和ATP的降低。组织学分析证实(-)MR22对缺血视网膜的保护作用。这些发现表明，(-)-MR22作为视网膜神经保护剂和Sigma(1)受体激动剂发挥作用。(C)2006爱思唯尔B.V.保留所有权利。
The effects of a novel N-methyladamantan-1-amine derivative [(-)-MR22] with high sigma(1) receptor affinity were investigated on retinal degeneration using a rat model of ischemia-reperfusion injury The animals were anaesthetized and retinal ischemia was induced by elevating the intraocular pressure to 120 min Hg for 45 min. The drug was injected intraperitoneally before the ischemic damage. Retinal biochemical changes, i.e. increase of lactate content and decrease of glucose and ATP were significantly inhibited by the new and selective sigma(1) receptor ligand compared to the ischemic control group The effect of (-)-MR22 was antagonized by pre-treatment with the a sigma(1) site antagonist. The protective effect of (-)MR22 on ischemic retina was confirmed by the histological analysis. These findings suggest that (-)-MR22 serves as a retinal neuroprotective agent and acts as a sigma(1) receptor agonist. (c) 2006 Elsevier B.V. All rights reserved.