Inhibition by the tetramine disulphide, benextramine, of cardiac chronotropic histamine H2-receptor-mediated effects

Br J Pharmacol. 1982 Apr;75(4):573-8. doi: 10.1111/j.1476-5381.1982.tb09176.x.

Abstract

1 Benextramine (N,N1-bis[o-methoxybenzylamino)-n-hexyl]cystamine), which irreversibly blocks alpha-adrenoceptors and does not inhibit the H1-receptor-mediated contractile effect of histamine on guinea-pig isolated ileum, also did not inhibit the H1-receptor-mediated inotropic effect of histamine on guinea-pig isolated atrium. 2 Benextramine irreversibly inhibited the H2-receptor-mediated chronotropic effect of histamine on guinea-pig isolated atrium. 3 Since its combination with the competitive H2-receptor blocking drug cimetidine had a additive blocking effect, benextramine appears to act directly on the chronotropic H2-receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Cimetidine / pharmacology
  • Cystamine / analogs & derivatives*
  • Cystamine / pharmacology
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • Heart Rate / drug effects*
  • Histamine / pharmacology
  • Histamine H2 Antagonists*
  • In Vitro Techniques
  • Time Factors

Substances

  • Adrenergic alpha-Antagonists
  • Histamine H2 Antagonists
  • benextramine
  • Cimetidine
  • Histamine
  • Cystamine