Inhibition of calcium channels in rat central and peripheral neurons by omega-conotoxin MVIIC

J Neurosci. 1996 Apr 15;16(8):2612-23. doi: 10.1523/JNEUROSCI.16-08-02612.1996.

Abstract

Inhibition of voltage-dependent calcium channels by omega-conotoxin MVIIC (omega-CTx-MVIIC) was studied in various types of rat neurons. When studied with 5 mM Ba2+ as charge carrier, omega-CTx-MVIIC block of N-type calcium channels in sympathetic neurons was potent, with half-block at 18 nM. Block of N-type channels had a rapid onset (tau approximately 1 sec at 1 microM omega-CTx-MVIIC) and quick reversibility (tau approximately 30 sec). The rate of block was proportional to toxin concentration, consistent with 1:1 binding of toxin to channels, with a rate constant (k on) of approximately 1 X 10(6) M-1. sec-1. Both potency and rate of block were reduced dramatically with increasing concentrations of extracellular Ba2+ omega-CTx-MVIIC also blocked P-type calcium channels in cerebellar Purkinje neurons, but both development and reversal of block were far slower than for N-type channels. The rate of block was proportional to toxin concentration, with k on -1.5 x 10(3) M-1. sec-1 at 5 mM Ba2+. From this value and an unblocking time constant of approximately 200 min, a dissociation constant of approximately 50 nM was estimated. Thus, block of P-type channels is potent but very slow. In hippocampal CA3 pyramidal neurons, omega-CTx-MVIIC blocked approximately 50% of the high-threshold calcium channel current; one component (approximately 20%) was blocked with the rapid kinetics expected for N-type channels, whereas the other component was blocked slowly. The component blocked slowly was reduced but not eliminated by preexposure to 200 nM or 1 microM omega-Aga-IVA.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects*
  • Dose-Response Relationship, Drug
  • Ganglia, Sympathetic / drug effects*
  • Hippocampus / drug effects*
  • Neurons / drug effects
  • Nimodipine / pharmacology
  • Peptides / pharmacology*
  • Pyramidal Cells / drug effects*
  • Rats
  • omega-Conotoxins*

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Peptides
  • omega-Conotoxins
  • omega-conotoxin-MVIIC
  • Nimodipine