N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2583-8. doi: 10.1016/s0960-894x(98)00461-2.

Abstract

New potent N alpha-alkylated histamine H1-receptor agonists have been prepared and functionally evaluated for partial agonist potency and selectivity. N alpha-Methyl-2-(3-trifluoromethylphenyl)histamine contracts ileal segments and aortic rings of guinea-pig with a relative potency of 174% (95% confid. lim. 161-188%) and 217% (164-287%), respectively (histamine: 100%) and is the most potent H1 receptor agonist described so far.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Animals
  • Aorta / drug effects
  • Guinea Pigs
  • Histamine / analogs & derivatives*
  • Histamine Agonists / chemical synthesis*
  • Histamine Agonists / pharmacology
  • In Vitro Techniques
  • Receptors, Histamine H1 / metabolism*
  • Structure-Activity Relationship
  • Vasoconstriction / drug effects

Substances

  • Histamine Agonists
  • Receptors, Histamine H1
  • Histamine