Homologous histamine H1 receptor desensitization results in reduction of H1 receptor agonist efficacy

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

Prolonged exposure of the guinea-pig intestinal longitudinal smooth muscle to histamine caused homologous desensitization of the H1 receptor, which led to reduced H1 receptor-mediated production of [3H]inositol phosphates as well as to reduced H1 agonist-induced contractions. [3H]Mepyramine binding studies showed that desensitization affected neither the agonist affinity nor the number of H1 receptors. Combining the data from the binding studies and the contraction measurements it was found that desensitization results in a selective reduction of agonist efficacy.

Original languageEnglish
Pages (from-to)319-22
Number of pages4
JournalEuropean Journal of Pharmacology
Volume196
Issue number3
DOIs
Publication statusPublished - 24 Apr 1991

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

  • Animals
  • Guinea Pigs
  • Histamine
  • In Vitro Techniques
  • Inositol Phosphates
  • Jejunum
  • Male
  • Membranes
  • Muscle Contraction
  • Muscle, Smooth
  • Phosphatidylinositols
  • Pyridines
  • Pyrilamine
  • Receptors, Histamine H1
  • Tritium
  • Journal Article

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