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Calciseptine, a peptide isolated from black mamba venom, is a specific blocker of the L-type calcium channel

Proc Natl Acad Sci U S A. 1991 Mar 15;88(6):2437-40. doi: 10.1073/pnas.88.6.2437.

Abstract

The venom of the black mamba contains a 60-amino acid peptide called calciseptine. The peptide has been fully sequenced. It is a smooth muscle relaxant and an inhibitor of cardiac contractions. Its physiological action resembles that of drugs, such as the 1,4-dihydropyridines, which are important in the treatment of cardiovascular diseases. Calciseptine, like the 1,4-dihydropyridines, selectively blocks L-type Ca2+ channels and is totally inactive on other voltage-dependent Ca2+ channels such as N-type and T-type channels. To our knowledge, it is the only natural polypeptide that has been shown to be a specific inhibitor of L-type Ca2+ channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects
  • Calcium Channels / physiology*
  • Cell Line
  • Elapid Venoms / chemistry
  • Elapid Venoms / isolation & purification
  • Elapid Venoms / pharmacology*
  • Electric Conductivity
  • Female
  • In Vitro Techniques
  • Membrane Potentials / drug effects
  • Molecular Sequence Data
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / physiology
  • Neurons / drug effects
  • Neurons / physiology*
  • Rats
  • Uterine Contraction / drug effects

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Elapid Venoms
  • calciseptine