Protective effect of nilvadipine against glutamate neurotoxicity in purified retinal ganglion cells

Brain Res. 2003 Jan 31;961(2):213-9. doi: 10.1016/s0006-8993(02)03951-3.

Abstract

We determined the effect of nilvadipine, a dihydropyridine-type calcium channel blocker, in preventing glutamate neurotoxicity in purified retinal ganglion cells (RGCs). RGCs were purified from dissociated rat retinal cells (postnatal days 6-8), using a modified two-step panning method, and cultured in serum-free medium containing neurotrophic factors and forskolin. RGC survival after exposure to glutamate (25 microM) with nilvadipine or other calcium channel blockers was measured by calcein-acetoxymethyl ester staining after 3 days in culture. Changes in the level of intracellular Ca(2+) ([Ca(2+)](i)) were measured with fura-2 fluorescence. Induction of apoptosis was evaluated using the TDT-dUTP terminal nick-end labeling technique. The neurotoxic effects of low doses of glutamate were blocked by a specific alpha-amino-3-dihydro-5-methylisoxazole-4-propionate-kainate receptor antagonist, 6,7-dinitroquinoxaline-2,3-dione (20 microM). Simultaneous application of nilvadipine (1-100 nM) with glutamate protected against glutamate neurotoxicity in a dose-dependent manner. Calcium-imaging experiments showed that the glutamate-evoked [Ca(2+)](i) increase was significantly blocked by nilvadipine (P<0.001), but not nifedipine and diltiazem, in about 50% of RGCs. In addition, the application of nilvadipine significantly reduced glutamate-induced apoptosis (P<0.001). These findings suggest that nilvadipine may partly inhibit glutamate-induced apoptotic cell death by blocking calcium influx via voltage-dependent calcium channels in purified RGCs.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Calcium / metabolism
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, L-Type / metabolism
  • Cell Culture Techniques
  • Cell Survival / drug effects
  • Diltiazem / pharmacology
  • Dose-Response Relationship, Drug
  • Excitatory Amino Acid Antagonists / pharmacology
  • Glutamic Acid / toxicity*
  • Neuroprotective Agents / pharmacology*
  • Nifedipine / analogs & derivatives*
  • Nifedipine / pharmacology*
  • Quinoxalines / pharmacology
  • Rats
  • Receptors, AMPA / metabolism*
  • Receptors, Kainic Acid / metabolism*
  • Retinal Ganglion Cells / drug effects*
  • Retinal Ganglion Cells / metabolism

Substances

  • Calcium Channel Blockers
  • Calcium Channels, L-Type
  • Excitatory Amino Acid Antagonists
  • Neuroprotective Agents
  • Quinoxalines
  • Receptors, AMPA
  • Receptors, Kainic Acid
  • nilvadipine
  • Glutamic Acid
  • FG 9041
  • Diltiazem
  • Nifedipine
  • Calcium