Pharmacological identification of a novel Ca2+ channel in chicken brain synaptosomes

Brain Res. 1994 Apr 18;643(1-2):204-10. doi: 10.1016/0006-8993(94)90026-4.

Abstract

Ca2+ influx was measured in rat and chicken brain synaptosomes in the presence of a number of pharmacological tools which have recently been used to define voltage-sensitive Ca(2+)-channel (VSCC) types. In chicken brain synaptosomes. VSCCs which, because of their sensitivity to inhibition by omega-conotoxin (omega-CgTx), are thought to be exclusively N-type, the P-type VSCC polyamine inhibitor FTX (from Agelenopsis aperta venom; 1 microliters/ml), its synthetic analogue, sFTX (1-5 mM) and the polypeptides AgaIVA (IC50 0.29 microM) and omega-CgTx MVIIC (IC50 0.0022 microM) inhibited 70-100% of the measurable K+ stimulated Ca2+ influx. The prototypical N-channel VSCC inhibitor omega-CgTx GVIA (IC50 0.014 microM), Cd2+ (50 microM) and diluted venom from Hololena curta (1:2,500) also caused complete or almost complete, inhibition of Ca2+ influx. In comparable studies using rat brain synaptosomes, sFTX (1-10 mM) caused a dose-dependent reduction of Ca2+ influx, while FTX (1 microliters/ml) and AgaIVA (IC50 0.02 microM) completely inhibited Ca2+ influx. Similar to the findings in chicken synaptosomes, Cd2+ (50 microM) and H. curta (1:2,500 dilution) both inhibited K+ stimulated influx by > 80% whereas omega-CgTx (1 microM) only caused a maximum 25% inhibition. Both sFTX and its congener spermine, inhibited [125I]omega-CgTx binding to rat and chicken synaptosomal membranes. These results strongly implicate P-type channels as the major VSCC in rat brain. The results also clearly demonstrate a heretofore unrecognized, novel, FTX/AgaIVA/omega-CgTx GVIA/omega-CgTx MVIIC-sensitive VSCC in chicken brain.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Brain / metabolism*
  • Calcium / metabolism*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects
  • Calcium Channels / metabolism*
  • Chickens
  • Dose-Response Relationship, Drug
  • Peptides / pharmacology
  • Polyamines / pharmacology
  • Potassium / pharmacology
  • Rats
  • Spermine / pharmacology
  • Spider Venoms / pharmacology
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism*
  • omega-Agatoxin IVA
  • omega-Conotoxin GVIA

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • FTX, spider toxin
  • Peptides
  • Polyamines
  • Spider Venoms
  • omega-Agatoxin IVA
  • Spermine
  • omega-Conotoxin GVIA
  • Potassium
  • Calcium