TY - JOUR
T1 - A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through σ1 receptors
AU - Bucolo, Claudio
AU - Marrazzo, Agostino
AU - Ronsisvalle, Simone
AU - Ronsisvalle, Giuseppe
AU - Cuzzocrea, Salvatore
AU - Mazzon, Emanuela
AU - Caputi, Achille
AU - Drago, Filippo
PY - 2006/4/24
Y1 - 2006/4/24
N2 - The effects of a novel N-methyladamantan-1-amine derivative [(-)-MR22] with high σ1 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 mm 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 σ1 receptor ligand compared to the ischemic control group. The effect of (-)-MR22 was antagonized by pre-treatment with the σ1 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 σ1 receptor agonist.
AB - The effects of a novel N-methyladamantan-1-amine derivative [(-)-MR22] with high σ1 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 mm 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 σ1 receptor ligand compared to the ischemic control group. The effect of (-)-MR22 was antagonized by pre-treatment with the σ1 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 σ1 receptor agonist.
KW - σ receptors
KW - Adamantane derivative
KW - Ischemia
KW - Neuroprotection
KW - Retina
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U2 - 10.1016/j.ejphar.2006.02.026
DO - 10.1016/j.ejphar.2006.02.026
M3 - Article
C2 - 16580663
AN - SCOPUS:33645813569
VL - 536
SP - 200
EP - 203
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1-2
ER -