A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through σ1 receptors

被引：21
作者：
Bucolo, C
Marrazzo, A
Ronsisvalle, S
Ronsisvalle, G
Cuzzocrea, S
Mazzon, E
Caputi, A
Drago, F
机构：
[1] Univ Catania, Sch Med, Dept Expt & Clin Pharmacol, I-95125 Catania, Italy
[2] Catania Univ, Sch Pharm, Dept Pharmaceut Sci, Catania, Italy
[3] Univ Messina, Dept Pharmacol, Messina, Italy
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 2006年 / 536卷 / 1-2期
关键词：
sigma(1) receptors; retina; neuroprotection; ischemia; adamantane derivative;
D O I：
10.1016/j.ejphar.2006.02.026
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
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.
引用
收藏
页码：200 / 203
页数：4
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