High affinity block of myocardial L-type calcium channels by the spider toxin omega-Aga-toxin IIIA: advantages over 1,4-dihydropyridines

Mol Pharmacol. 1992 Dec;42(6):947-51.

Abstract

The peptide omega-agatoxin IIIA (omega-Aga-IIIA) from venom of the funnel web spider Agelenopsis aperta blocks L-type Ca2+ channels in neurons and myocardial cells with high affinity. We report that omega-Aga-IIIA also blocks whole-cell Ca2+ channel currents in guinea pig atrial myocytes. Although other high affinity blockers of L-type Ca2+ channels are available (such as the 1,4-dihydropyridines), omega-Aga-IIIA is a valuable pharmacological tool; omega-Aga-IIIA is the only known ligand that blocks L-type Ca2+ channels with high affinity at all voltages (IC50 approximately 1 nM) and it causes little or no block of T-type Ca2+ channels, unlike the 1,4-dihydropyridines. We use omega-Aga-IIIA to selectively eliminate L-type Ca2+ currents and we show that felodipine blocks T-type Ca2+ currents. Consequently, the toxin is better than dihydropyridines for separating ionic currents through voltage-dependent Ca2+ channels and defining their physiological function.

MeSH terms

  • Agatoxins
  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Cells, Cultured
  • Dihydropyridines / pharmacology*
  • Felodipine / pharmacology
  • Guinea Pigs
  • Heart Atria / cytology
  • Heart Atria / drug effects
  • In Vitro Techniques
  • Ion Channel Gating / drug effects
  • Male
  • Myocardium / cytology
  • Myocardium / metabolism*
  • Spider Venoms / pharmacology*
  • Substrate Specificity

Substances

  • Agatoxins
  • Calcium Channel Blockers
  • Dihydropyridines
  • Spider Venoms
  • omega-agatoxin III
  • 1,4-dihydropyridine
  • Felodipine