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

SD-282 的药理特性 - p38 MAP 激酶的 α 同工型选择性抑制剂

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作者:Bruce 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, Li

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.

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