H3-receptors control histamine release in human brain

J Neurochem. 1988 Jul;51(1):105-8. doi: 10.1111/j.1471-4159.1988.tb04841.x.


The regulation of histamine release was studied on slices prepared from pieces of human cerebral cortex removed during neurosurgery and labeled with L-[3H]histidine. Depolarization by increased extracellular K+ concentration induced [3H]histamine release, although to a lesser extent than from rat brain slices. Exogenous histamine reduced by up to 60% the K+-evoked release, with an EC50 of 3.5 +/- 0.5 X 10(-8) M. The H3-receptor antagonists impromidine and thioperamide reversed the histamine effect in an apparently competitive manner and enhanced the K+-evoked release, indicating a participation of endogenous histamine in the release control process. The potencies of histamine and the H3-receptor antagonists were similar to those of these agents at presynaptic H3-autoreceptors controlling [3H]histamine release from rat brain slices. It is concluded that H3-receptors control histamine release in the human brain.

MeSH terms

  • Cerebral Cortex / physiology*
  • Histamine / pharmacology
  • Histamine Release* / drug effects
  • Humans
  • Imidazoles / pharmacology
  • Impromidine
  • Piperidines / pharmacology
  • Potassium / pharmacology
  • Receptors, Histamine / drug effects
  • Receptors, Histamine / physiology*
  • Receptors, Histamine H3
  • Tritium


  • Imidazoles
  • Piperidines
  • Receptors, Histamine
  • Receptors, Histamine H3
  • Tritium
  • Histamine
  • Impromidine
  • thioperamide
  • Potassium