Affinities of histamine H1-antagonists in guinea pig brain: similarity of values determined from [3H]mepyramine binding and from inhibition of a functional response

J Neurochem. 1981 Nov;37(5):1357-60. doi: 10.1111/j.1471-4159.1981.tb04692.x.


Affinity constants for five antagonists at histamine H1-receptors in guinea pig brain have been determined from inhibition of the potentiation by histamine of the adenosine-induced accumulation of cyclic AMP in cerebral cortical slices. This action of histamine appeared to be mediated solely through H1-receptors. The affinity constants obtained were similar to those determined on peripheral H1-receptors and from inhibition of high-affinity [3H]mepyramine binding. This provides strong evidence that at least some of the [3H]mepyramine binding sites in guinea pig brain can be identified with functional H1-receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopyridines / metabolism*
  • Animals
  • Binding, Competitive
  • Brain / metabolism*
  • Female
  • Guinea Pigs
  • Histamine H1 Antagonists / pharmacology*
  • Kinetics
  • Male
  • Pyrilamine / metabolism*
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H1 / metabolism*
  • Structure-Activity Relationship


  • Aminopyridines
  • Histamine H1 Antagonists
  • Receptors, Histamine
  • Receptors, Histamine H1
  • Pyrilamine