Naftazone reduces glutamate cerebro spinal fluid levels in rats and glutamate release from mouse cerebellum synaptosomes

It is well known that an excessive release of glutamate in the mammalian br ain plays a major role in several neurological diseases. Naftazone (Etioven (R)) is a currently used vasoprotectant drug that is metabolized in humans by reduction and glucuronidation. In the present study naftazone was found to decrease glutamate levels in the cerebro spinal fluid (CSF) of rats trea ted for 15 days, as determined by a chemiluminescent glutamate assay reacti on. Naftazone and its glucuronide derivative also reduced respectively spon taneous and high K+-evoked glutamate release from mouse cerebellum synaptos omes. It is likely that naftazone and its glucuronide metabolite contribute in vivo to decrease glutamate levels in the CSF through their inhibitory a ctions on glutamate release. (C) 1999 Elsevier Science ireland Ltd. All rig hts reserved.