General construction pattern of histamine H3-receptor antagonists: change of a paradigm

Bioorg Med Chem Lett. 1998 Aug 4;8(15):2011-6. doi: 10.1016/s0960-894x(98)00342-4.

Abstract

Novel omega-phenyl substituted and unsubstituted alkyl and alkenyl imidazole derivatives were prepared and tested for their antagonist activity in vitro and in vivo at histamine H3-receptors. Some compounds showed high in vitro and in vivo H3-receptor activity despite their structure bearing no polar moiety in the centre of the molecule which is a common structural feature of all other antagonists known. Quite probably there are further in vivo effects for some compounds resulting from other receptor interactions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Guinea Pigs
  • Histamine Antagonists / chemical synthesis*
  • Histamine Antagonists / chemistry
  • Histamine Antagonists / pharmacology
  • Histamine Release / drug effects
  • Ileum / drug effects
  • Ileum / physiology
  • In Vitro Techniques
  • Mice
  • Rats
  • Receptors, Histamine H3 / drug effects*
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism

Substances

  • Histamine Antagonists
  • Receptors, Histamine H3