Icotidine, an antagonist of histamine at both H1 and H2 receptors

N Engl Reg Allergy Proc. 1986 Mar-Apr;7(2):126-33. doi: 10.2500/108854186779047762.

Abstract

SK&F 93319 (icotidine), 2-[4-(3-methoxypyrid-2-yl)butylamino]-5-[(6-methylpyrid-3-yl )-methyl]- pyrimidin-4-one trihydrochloride, has been identified as a novel agent which combines into one molecule the ability to antagonize the actions of histamine at H1 and H2 receptors across a similar concentration or dose range. The degree of antagonism of vascular responses to histamine exceeds that possible with either an H1- or H2-receptor histamine antagonist alone. SK&F 93319 may have therapeutic utility in conditions requiring simultaneous antagonism of histamine at H1 and H2 receptors.

MeSH terms

  • Animals
  • Bronchi / drug effects
  • Chemical Phenomena
  • Chemistry
  • Gastric Acid / metabolism
  • Heart / drug effects
  • Histamine H1 Antagonists*
  • Histamine H2 Antagonists*
  • Humans
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Pyridines / metabolism
  • Pyridines / pharmacology*
  • Structure-Activity Relationship
  • Vascular Resistance / drug effects

Substances

  • Histamine H1 Antagonists
  • Histamine H2 Antagonists
  • Imidazoles
  • Pyridines
  • icotidine
  • oxmetidine