Nefopam, an analogue of orphenadrine, protects against both NMDA receptor-dependent and independent veratridine-induced neurotoxicity
| Autor: | Antonello Novelli, M. T. Fernández-Sánchez, Barbara Manfredi, Gabriele Biella, Maria Luisa Sotgiu, Ramón Díaz-Trelles, Antonio Groppetti, Anna T. Brini |
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| Rok vydání: | 2002 |
| Předmět: |
Male
Clinical Biochemistry Analgesic Neurotoxins Excitotoxicity Glutamic Acid Pharmacology medicine.disease_cause Biochemistry Receptors N-Methyl-D-Aspartate Rats Sprague-Dawley chemistry.chemical_compound Nefopam Cerebellum Orphenadrine medicine Animals GABA Agonists Cells Cultured Neurons Veratridine Chemistry Muscimol Organic Chemistry Neurotoxicity Analgesics Non-Narcotic medicine.disease GABA receptor agonist Rats Neuroprotective Agents nervous system NMDA receptor Dizocilpine Maleate medicine.drug |
| Zdroj: | Amino acids (Wien, Print) 23 (2002): 31–36. info:cnr-pdr/source/autori:Fernandez Sanchez M.T., Diaz Trelles R., Groppetti A., Manfredi B., Brini A.T., Biella G., Sotgiu M.L., Novelli A./titolo:Nefopam, an analogue of orphenadrine, protects against both NMDA receptor-dependent and independent veratridine-induced neurotoxicity/doi:/rivista:Amino acids (Wien, Print)/anno:2002/pagina_da:31/pagina_a:36/intervallo_pagine:31–36/volume:23 |
| ISSN: | 0939-4451 |
| Popis: | Nefopam hyghochloride is a potent analgesic compound commercialized in most Western Europe for 20 years, which possesses a profile distinct from that of opioids or anti-inflammatory drugs. Previous evidence suggested a central action of nefopam but the detailed mechanisms remain unclear. While, nefopam structure resembles that of orphenadrine, an uncompetitive NMDA receptor antagonist, here we report that differently from orphenadrine, nefopam (100 microM) failed to protect cultured cerebellar neurons from excitotoxicity following direct exposure of neurons to glutamate. Moreover, nefopam failed to displace MK-801 binding to hippocampal membranes. Nefopam effectively prevented NMDA receptor-mediated early appearance (30 min) of toxicity signs induced by the voltage sensitive sodium channel (VSSC) activator veratridine. The later phase (24 h) of neurotoxicity by veratridine occurring independently from NMDA receptor activation, was also prevented by nefopam. Nefopam effect was not mimicked by the GABA receptor agonist muscimol. |
| Databáze: | OpenAIRE |
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