Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors

Naunyn Schmiedebergs Arch Pharmacol. 1990 Nov;342(5):619-22. doi: 10.1007/BF00169055.

Abstract

5-Hydroxytryptamine (5-HT), 5-carboxamidotryptamine (5-CT) and the gastrointestinal kinetic benzamides renzapride and cisapride caused tachycardia in spontaneously beating right atria of piglet in the presence of 400 nmol/l (+/-)-propranolol and 6 mumol/l cocaine. The maximum tachycardia caused by agonists, compared to that evoked by 200 mumol/l (-)-isoprenaline, was 63% for 5-HT, 50% for 5-CT, 50% for renzapride and 28% for cisapride. The rank order of potency was 5-HT greater than renzapride greater than cisapride greater than 5-CT. The effects of the agonists, but not those of (-)-isoprenaline, were antagonised by 3 alpha-tropanyl-1H-indole-3-carboxylic acid (ICS 205930); the pKB of ICS 205930 (vs 5-HT) was 6.9. These characteristics suggest that piglet sinoatrial 5-HT receptors are similar to "so-called" 5-HT4 receptors previously described in mouse colliculi neurons. Piglet sinoatrial 5-HT4-like receptors resemble the human atrial 5-HT receptors that mediate positive inotropic effects of 5-HT.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Benzamides / pharmacology
  • Bridged Bicyclo Compounds / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic*
  • Cardiotonic Agents / pharmacology
  • Cisapride
  • Female
  • Heart / drug effects*
  • Heart Atria / drug effects
  • Humans
  • In Vitro Techniques
  • Indoles / pharmacology
  • Male
  • Piperidines / pharmacology
  • Receptors, Serotonin / classification*
  • Receptors, Serotonin / drug effects
  • Serotonin / analogs & derivatives
  • Serotonin / pharmacology
  • Serotonin Antagonists / pharmacology
  • Sinoatrial Node / drug effects*
  • Swine
  • Tropisetron

Substances

  • Benzamides
  • Bridged Bicyclo Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Cardiotonic Agents
  • Indoles
  • Piperidines
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin
  • Tropisetron
  • renzapride
  • 5-carboxamidotryptamine
  • Cisapride