Protective effects of N-methyl-D-aspartate receptor antagonism on VX-induced neuronal cell death in cultured rat cortical neurons

Neurotox Res. 2008 May-Jun;13(3-4):163-72. doi: 10.1007/BF03033500.

Abstract

Exposure of the central nervous system to organophosphorus (OP) nerve agents induces seizures and neuronal cell death. Here we report that the OP nerve agent, VX, induces apoptotic-like cell death in cultured rat cortical neurons. The VX effects on neurons were concentration-dependent, with an IC(50) of approximately 30 microM. Blockade of N-methyl-D-aspartate receptors (NMDAR) with 50 microM. D-2-amino-5-phosphonovalerate (APV) diminished 30 microM VX-induced total cell death, as assessed by alamarBlue assay and Hoechst staining. In contrast, neither antagonists of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors (AMPARs) nor metabotropic glutamate receptors (mGluRs) had any effect on VX-induced neurotoxicity. VX-induced neuronal cell death could not be solely attributed to acetylcholinesterase (AChE) inhibition, since neither the reversible pharmacological cholinesterase inhibitor, physostigmine, nor the muscarinic receptor antagonist, atropine, affected VX-induced cell death. Importantly, APV was found to be therapeutically effective against VX-induced cell death up to 2 h post VX exposure. These results suggest that NMDARs, but not AMPARs or mGluRs, play important roles in VX-induced cell death in cultured rat cortical neurons. Based on their therapeutic effects, NMDAR antagonists may be beneficial in the treatment of VX-induced neurotoxicities.

MeSH terms

  • 2-Amino-5-phosphonovalerate / pharmacology
  • Analysis of Variance
  • Animals
  • Cell Death / drug effects
  • Cells, Cultured
  • Cerebral Cortex / cytology*
  • Chemical Warfare Agents / toxicity*
  • Cholinergic Agonists / pharmacology
  • Dose-Response Relationship, Drug
  • Embryo, Mammalian
  • Excitatory Amino Acid Antagonists / pharmacology
  • Female
  • Glutamic Acid / pharmacology
  • Neurons / drug effects*
  • Neurons / pathology
  • Organothiophosphorus Compounds / toxicity*
  • Pregnancy
  • Propidium
  • Quinoxalines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Receptors, N-Methyl-D-Aspartate / physiology*
  • Time Factors

Substances

  • Chemical Warfare Agents
  • Cholinergic Agonists
  • Excitatory Amino Acid Antagonists
  • Organothiophosphorus Compounds
  • Quinoxalines
  • Receptors, N-Methyl-D-Aspartate
  • 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline
  • Propidium
  • Glutamic Acid
  • 2-Amino-5-phosphonovalerate
  • VX