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 brain plays a major role in several neurological diseases. Naftazone (Etioven) 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 treated for 15 days, as determined by a chemiluminescent glutamate assay reaction. Naftazone and its glucuronide derivative also reduced respectively spontaneous and high K+-evoked glutamate release from mouse cerebellum synaptosomes. It is likely that naftazone and its glucuronide metabolite contribute in vivo to decrease glutamate levels in the CSF through their inhibitory actions on glutamate release.
Mattei
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C
Laboratoire de Neurobiologie Cellulaire et Moléculaire (UPR 9040), CNRS, Gif sur Yvette, France. mattei@nbcm.cnrs-gif.fr
Molgó
J
J
Joseph
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Israel
M
M
Bloy
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C
D000818:Animals; D002531:Cerebellum / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D002555:Cerebrospinal Fluid / Q000187:drug effects; D005260:Female; D018698:Glutamic Acid / Q000134:cerebrospinal fluid*; D008163:Luminescent Measurements; D008297:Male; D051379:Mice; D008854:Microscopy, Electron; D009285:Naphthoquinones / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D009412:Nerve Fibers / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D011188:Potassium / Q000494:pharmacology; D017729:Presynaptic Terminals / Q000648:ultrastructure; D051381:Rats; D017207:Rats, Sprague-Dawley; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism*
D009285:Naphthoquinones; C005272:naftazone; D018698:Glutamic Acid; D011188:Potassium