Theophylline derivatives as potential histamine H3-receptor antagonists

Pharmazie. 1998 Aug;53(8):518-21.

Abstract

Previous results of histamine H3-receptors investigations allowed to formulate a general structure of H3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and thiourea function) via an alkyl chain linked by a spacer to a lipophilic residue. The common distance between xanthine moiety and lipophilic rest was a six-link-chain. Selected compounds did not show significant H3-receptor antagonist activity and were weak antagonists at histamine H1-receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Guinea Pigs
  • Histamine Antagonists / chemical synthesis*
  • Histamine Antagonists / pharmacology
  • Ileum / drug effects
  • In Vitro Techniques
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • Receptors, Histamine H3 / drug effects*
  • Theophylline / analogs & derivatives*
  • Theophylline / chemical synthesis
  • Theophylline / pharmacology*

Substances

  • Histamine Antagonists
  • Receptors, Histamine H3
  • Theophylline