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

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.
AuthorsBruce Koppelman, Heather K Webb, Satyanarayana Medicherla, Ramona Almirez, Ying Feng, Jose Carlos Chavez, Cheng Ping Mao, Aaron Nguyen, Yu-Wang Liu, Ann M Kapoun, Gladys Muiru, Yuanying Anne Huang, Sundeep Dugar, Babu J Mavunkel, Don W Lim, Sarvajit Chakravarty, Gregory Luedtke, Andrew A Protter, Linda S Higgins
JournalPharmacology (Pharmacology) Vol. 81 Issue 3 Pg. 204-20 ( 2008) ISSN: 1423-0313 [Electronic] Switzerland
PMID18176091 (Publication Type: Journal Article)
CopyrightCopyright 2008 S. Karger AG, Basel.
Chemical References
  • Anti-Inflammatory Agents
  • Enzyme Inhibitors
  • Indoles
  • Tumor Necrosis Factor-alpha
  • indole-5-carboxamide
  • Ovalbumin
  • p38 Mitogen-Activated Protein Kinases
Topics
  • Animals
  • Anti-Inflammatory Agents (pharmacology)
  • Disease Models, Animal
  • Enzyme Inhibitors (pharmacokinetics, pharmacology)
  • Female
  • Granulocytes (drug effects, metabolism)
  • Guinea Pigs
  • Humans
  • In Vitro Techniques
  • Indoles (pharmacokinetics, pharmacology)
  • Inflammation (drug therapy)
  • Lung (drug effects, pathology)
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Ovalbumin
  • Sepsis (drug therapy, physiopathology)
  • Tumor Necrosis Factor-alpha (blood, drug effects)
  • p38 Mitogen-Activated Protein Kinases (antagonists & inhibitors)

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