title: 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.
authors.affiliation: Scios, Inc., Fremont, Calif., USA. bruce_koppelman@yahoo.com
authors.forename: Bruce
authors.initials: B
authors.lastname: Koppelman
authors.forename: Heather K
authors.initials: HK
authors.lastname: Webb
authors.forename: Satyanarayana
authors.initials: S
authors.lastname: Medicherla
authors.forename: Ramona
authors.initials: R
authors.lastname: Almirez
authors.forename: Ying
authors.initials: Y
authors.lastname: Feng
authors.forename: Jose Carlos
authors.initials: JC
authors.lastname: Chavez
authors.forename: Cheng Ping
authors.initials: CP
authors.lastname: Mao
authors.forename: Aaron
authors.initials: A
authors.lastname: Nguyen
authors.forename: Yu-Wang
authors.initials: YW
authors.lastname: Liu
authors.forename: Ann M
authors.initials: AM
authors.lastname: Kapoun
authors.forename: Gladys
authors.initials: G
authors.lastname: Muiru
authors.forename: Yuanying Anne
authors.initials: YA
authors.lastname: Huang
authors.forename: Sundeep
authors.initials: S
authors.lastname: Dugar
authors.forename: Babu J
authors.initials: BJ
authors.lastname: Mavunkel
authors.forename: Don W
authors.initials: DW
authors.lastname: Lim
authors.forename: Sarvajit
authors.initials: S
authors.lastname: Chakravarty
authors.forename: Gregory
authors.initials: G
authors.lastname: Luedtke
authors.forename: Andrew A
authors.initials: AA
authors.lastname: Protter
authors.forename: Linda S
authors.initials: LS
authors.lastname: Higgins
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D004195:Disease Models, Animal; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D005260:Female; D006098:Granulocytes / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000493:pharmacokinetics / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy*; D008168:Lung / Q000187:drug effects / Q000473:pathology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010047:Ovalbumin; D018805:Sepsis / Q000188:drug therapy / Q000503:physiopathology; D014409:Tumor Necrosis Factor-alpha / Q000097:blood / Q000187:drug effects; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D007211:Indoles; D014409:Tumor Necrosis Factor-alpha; C514526:indole-5-carboxamide; D010047:Ovalbumin; D048051:p38 Mitogen-Activated Protein Kinases