3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2233-6. doi: 10.1016/s0960-894x(99)00353-4.

Abstract

Twenty-four 3-alkyl-(5,5'-diphenyl)imidazolidinediones were synthesized and evaluated as new cannabinoid receptor ligands. Three compounds exhibited a Ki value around 100 nM against [3H]-SR 141716A binding obtained from human CB1 transfected CHO cells membranes. The lack of change of affinity in the presence of a non hydrolyzable GTP analogue seems to indicate they are cannabinoid antagonists.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cannabinoids*
  • Cricetinae
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • Ligands
  • Piperidines / pharmacology
  • Pyrazoles / pharmacology
  • Receptors, Cannabinoid
  • Receptors, Drug / antagonists & inhibitors*
  • Rimonabant
  • Structure-Activity Relationship
  • Transfection

Substances

  • Cannabinoids
  • Imidazoles
  • Ligands
  • Piperidines
  • Pyrazoles
  • Receptors, Cannabinoid
  • Receptors, Drug
  • Rimonabant