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Agents and Actions

, Volume 16, Issue 3–4, pp 179–182 | Cite as

Characterization of vascular histamine H1-receptors: Multiple affinity states of aortic histamine H1-receptor

  • Marija Čarman-Kržan
Histamine Receptors

Abstract

We have shown that [3H]mepyramine labels histamine H1-receptor-binding sites in bovine aortic membranes. Further characterization of H1-receptors in this tissue was done by the interaction of an unlabelled histamine receptor agonist or antagonist, with the radioantagonist [3H]mepyramine-binding sites. The competition-binding assays have uncovered differences in the characteristics of the agonist/receptor interaction not shared by antagonists. Agonists interact in the heterogeneous manner with the radioantagonist-labelled sites, showing shallow competition curves with thenH 0.50–0.72, whereas antagonists were devoid of this effect (steeper slopes of the inhibition curvesnH≈1). The results suggest the presence in this tissue of multiple affinity states of histamine H1-receptor, differentiated by high and low affinity for agonists and the same affinity for antagonists.

Keywords

Histamine Receptor Agonist Steep Slope Histamine Receptor Mepyramine 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Birkhäuser Verlag 1985

Authors and Affiliations

  • Marija Čarman-Kržan
    • 1
  1. 1.Department of Pharmacology, Medical FacultyUniversity of LjubljanaLjubljanaYugoslavia

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