Koppelman Bruce, Webb Heather K, Medicherla Satyanarayana, Almirez Ramona, Feng Ying, Chavez Jose Carlos, Mao Cheng Ping, Nguyen Aaron, Liu Yu-Wang, Kapoun Ann M, Muiru Gladys, Huang Yuanying Anne, Dugar Sundeep, Mavunkel Babu J, Lim Don W, Chakravarty Sarvajit, Luedtke Gregory, Protter Andrew A, Higgins Linda S
Scios, Inc., Fremont, Calif., USA.
Pharmacology. 2008;81(3):204-20. doi: 10.1159/000112865. Epub 2008 Jan 7.
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.
小分子p38抑制剂在多种不同疾病状态模型中的作用已见诸报道，其中包括吲哚-5-甲酰胺抑制剂SD-282。本研究旨在评估SD-282在体外细胞因子产生以及两种体内炎症模型中的药理活性，以阐明这种特定抑制剂在多种疾病状态中的作用。此处呈现的结果进一步刻画了SD-282的特性，并为解释这种p38抑制剂在关节炎、疼痛、心肌损伤、脓毒症和哮喘模型中的活性提供了背景；所有这些疾病都有炎症成分。SD-282是阐明p38丝裂原活化蛋白激酶在多种炎症模型中作用的宝贵工具。
