Pharmacological properties of SD-282 - an alpha-isoform selective inhibitor for p38 MAP kinase

Pharmacology. 2008;81(3):204-20. doi: 10.1159/000112865. Epub 2008 Jan 7.

Abstract

The effects of small-molecule p38 inhibitors in numerous models of different disease states have been published, including those of SD-282, an indole-5-carboxamide inhibitor. The aim of the present study was to evaluate the pharmacological activity of SD-282 on cytokine production in vitro as well as in 2 in vivo models of inflammation in order to illuminate the role of this particular inhibitor in diverse disease states. The results presented here provide further characterization of SD-282 and provide a context in which to interpret the activity of this p38 inhibitor in models of arthritis, pain, myocardial injury, sepsis and asthma; all of which have an inflammatory component. SD-282 represents a valuable tool to elucidate the role of p38 MAP kinase in multiple models of inflammation.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Disease Models, Animal
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Female
  • Granulocytes / drug effects
  • Granulocytes / metabolism
  • Guinea Pigs
  • Humans
  • In Vitro Techniques
  • Indoles / pharmacokinetics
  • Indoles / pharmacology*
  • Inflammation / drug therapy*
  • Lung / drug effects
  • Lung / pathology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Ovalbumin
  • Sepsis / drug therapy
  • Sepsis / physiopathology
  • Tumor Necrosis Factor-alpha / blood
  • Tumor Necrosis Factor-alpha / drug effects
  • p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*

Substances

  • Anti-Inflammatory Agents
  • Enzyme Inhibitors
  • Indoles
  • Tumor Necrosis Factor-alpha
  • indole-5-carboxamide
  • Ovalbumin
  • p38 Mitogen-Activated Protein Kinases