Characteristics of histamine H1 receptors on HeLa cells

Eur J Pharmacol. 1993 May 15;245(3):291-5. doi: 10.1016/0922-4106(93)90110-u.


The affinities of antagonists at histamine H1 receptors on HeLa cells have been determined from inhibition of histamine-induced inositol phosphate formation in intact and from inhibition of [3H]mepyramine binding to HeLa cell membranes. The dissociation constants of mepyramine and (+)-chlorpheniramine were similar to values for binding to H1 receptors in other mammalian tissues, but much lower than the values reported in an earlier study with [3H]mepyramine and HeLa cell membranes. Evidence is presented that under conditions employed in the earlier study the binding of [3H]mepyramine is largely to secondary, non-H1 receptor sites.

MeSH terms

  • Binding Sites
  • Cell Membrane / metabolism*
  • Chlorpheniramine / metabolism
  • HeLa Cells
  • Histamine / pharmacology
  • Humans
  • Inositol Phosphates / metabolism
  • Pyrilamine / metabolism
  • Receptors, Histamine H1 / metabolism*


  • Inositol Phosphates
  • Receptors, Histamine H1
  • Chlorpheniramine
  • Histamine
  • Pyrilamine