C-3 Amido-indole cannabinoid receptor modulators

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2399-402. doi: 10.1016/s0960-894x(02)00466-3.

Abstract

C-3 Amido-indoles were found to selectively bind to the CB2 receptor. SAR studies led to optimized compounds with excellent in vivo potency against LPS induced TNF-alpha release in murine models of cytokine production.

MeSH terms

  • Amides
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Humans
  • Immunity, Cellular / drug effects
  • Indoles
  • Inhibitory Concentration 50
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Lipopolysaccharides / pharmacology
  • Mice
  • Protein Binding
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists*
  • Sensitivity and Specificity
  • Structure-Activity Relationship
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Amides
  • Anti-Inflammatory Agents
  • Indoles
  • Lipopolysaccharides
  • Receptors, Cannabinoid
  • Receptors, Drug
  • Tumor Necrosis Factor-alpha