The effect of histamine on cultured endothelial cells. A study of the mechanism of increased vascular permeability

Eur J Pharmacol. 1992 Oct 20;221(2-3):325-31. doi: 10.1016/0014-2999(92)90719-k.


The role of endothelial cells in the histamine-induced vascular response was investigated using cultured endothelial cells obtained from human umbilical veins. A single population of histamine H1 receptors was detected in these cells by means of a [3H]mepyramine binding assay. Its Kd was 0.74 +/- 0.07 nM and Bmax was 41.4 +/- 8.68 fmol/mg protein. Actin filaments were distributed as dense bands at the margin of the cells and as sparse microfilament bundles traversing the center of the cells. Histamine caused a decrease in peripheral bands and an increase in longitudinal bands. The changes evoked by histamine were dose-dependent, related to the duration of incubation of the cells with histamine, and blocked by mepyramine, a histamine H1 receptor antagonist. The results suggest that the endothelial cells respond to histamine through the histamine H1 receptor. This may explain one of the mechanisms of histamine-induced vascular response including vascular permeability increase.

MeSH terms

  • Actins / analysis
  • Capillary Permeability / drug effects*
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / metabolism
  • Endothelium, Vascular / ultrastructure
  • Histamine / pharmacology*
  • Humans
  • Pyrilamine / metabolism
  • Pyrilamine / pharmacology


  • Actins
  • Histamine
  • Pyrilamine