Blockade of neuronal tryptamine receptors by metoclopramide

Eur J Pharmacol. 1978 May 1;49(1):109-12. doi: 10.1016/0014-2999(78)90228-5.

Abstract

Metoclopramide (0.13, 0.51, 2.0 and 8.1 X 10(-6) M) caused parallel, rightward, shifts in the dose response curves to 5-HT on the isolated rabbit heart. A significant straight line relationship was found between log (5-HT dr--1) and log [metoclopramide] (molar) with a slope of 1.08 +/- 0.13 and giving a pA2 value of 7.20. Metoclopramide did not significantly alter responses to noradrenaline and was 575 times less effective as an inhibitor of DMPP than of 5-HT. The results indicate that metoclopramide is a potent, surmountable and selective antagonist of tryptamine receptors on rabbit cardiac sympathetic nerves.

MeSH terms

  • Animals
  • Dimethylphenylpiperazinium Iodide / pharmacology
  • Female
  • Heart / innervation
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Male
  • Metoclopramide / pharmacology*
  • Myocardial Contraction / drug effects
  • Neurons / drug effects
  • Rabbits
  • Receptors, Serotonin / drug effects*
  • Serotonin / pharmacology
  • Sympathetic Nervous System / drug effects*

Substances

  • Receptors, Serotonin
  • Serotonin
  • Dimethylphenylpiperazinium Iodide
  • Metoclopramide