Na+ and high-voltage-activated Ca2+ channel blocking actions of NS-7, a novel neuroprotective agent, in NG108-15 cells

Eur J Pharmacol. 1997 Oct 8;336(2-3):283-90. doi: 10.1016/s0014-2999(97)01261-2.

Abstract

The actions of a novel neuroprotective compound, 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine hydrochloride (NS-7), on voltage-gated Na+, Ca2+ and K+ channels were investigated in a mouse neuroblastoma and rat glioma hybrid cell line, NG108-15, using a whole-cell voltage clamp technique. NG108-15 cells have a tetrodotoxin-sensitive Na+ channel, three types of Ca2+ channel (L, N and T) and voltage-gated K+ channels, all of which were inhibited by NS-7 in a concentration-dependent manner. However, there was a considerable difference in its potency: the IC50 values for the tetrodotoxin-sensitive Na+ channel, L-type Ca2+ channel and N-type Ca2+ channel were similar (7.8, 4.5 and 7.3 microM, respectively), lower than the IC50 value for the T-type Ca2+ channel (17.1 microM), and much lower than the IC50 value for the voltage-gated K+ channel (160.5 microM). NS-7 altered neither the shape nor the reversal potential of the current-voltage curves for Na+, L-type or N-type Ca2+ channels, although the currents were reduced at every potential tested. These results indicate that NS-7 is a Na+ and high-voltage-activated (L- and N-type) Ca2+ channel blocker, and its channel-blocking properties may contribute to its neuroprotective action.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Mice
  • Neurons / drug effects*
  • Neurons / metabolism
  • Neuroprotective Agents / pharmacology*
  • Patch-Clamp Techniques
  • Potassium Channel Blockers
  • Pyrimidines / pharmacology*
  • Rats
  • Sodium Channel Blockers*
  • Tumor Cells, Cultured

Substances

  • 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy)pyrimidine hydrochloride
  • Calcium Channel Blockers
  • Neuroprotective Agents
  • Potassium Channel Blockers
  • Pyrimidines
  • Sodium Channel Blockers