Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex

Nature. 1983 Jul 7-13;304(5921):65-7. doi: 10.1038/304065a0.

Abstract

Although the H2 subclass of histamine receptor has been revealed by classical pharmacological approaches, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using 3H-metiamide and 3H-histamine and, subsequently, work from our own laboratory and others using 3H-cimetidine and 3H-ranitidine in various tissues, has shown the unsuitability of these ligands for labelling the H2 receptor. We report here our results using 3H-tiotidine, a more potent H2-antagonist than either cimetidine or ranitidine, and show that this ligand meets the criteria for labeling the H2 receptor in guinea pig cerebral cortex membranes.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cerebral Cortex / metabolism*
  • Cimetidine* / analogs & derivatives*
  • Guanidines / metabolism*
  • Guinea Pigs
  • Histamine H2 Antagonists / metabolism*
  • Kinetics
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H2 / metabolism*
  • Structure-Activity Relationship
  • Thiazoles / metabolism*

Substances

  • Guanidines
  • Histamine H2 Antagonists
  • Receptors, Histamine
  • Receptors, Histamine H2
  • Thiazoles
  • Cimetidine
  • tiotidine