Efficacy of the Inflammatory Cell Infiltration Inhibitor IS-741 on Colitis Induced by Dextran Sulfate Sodium in the Rat

The Japanese Journal of Pharmacology

Shuichi Yotsuya¹  Masashi Imamura¹  Hiroshi Shikama¹ 

[1] Central Research Institute, Ishihara Sangyo Kaisha, Ltd.

关键词: IS-741;    Inhibition of cell adhesion;    Inhibition of leukocyte infiltration;    Inflammatory bowel disease;    Ulcerative colitis;   

DOI  :  10.1254/jjp.87.151

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(39)Cited-By(5)We examined the therapeutic effects of the inflammatory cell infiltration inhibitor IS-741 (N-(2-((ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)-cyclohexanecarboxamide monosodium salt monohydrate) on a rat colitis model. As a result of its effects on leukocyte infiltration, IS-741 inhibits cell adhesion, alleviates symptoms and signs of pancreatitis and multiple organ failure and demonstrates a life-saving effect in a model of severe acute pancreatitis. A rat model was prepared by inducing colitis with 3% dextran sodium sulfate (DSS) and maintaining pathology with 1% DSS. Repeated oral administration of IS-741 at 1, 10 or 100 mg/kg per day was conducted for 2 weeks (during treatment with 1% DSS). IS-741 at each dose decreased the area of erosion in the large intestine, thickening of the wall of the large intestine and anemia caused by melena. Some effects of IS-741 were nearly equivalent to those of the control compound salazosulfapyridine. Furthermore, IS-741 markedly alleviated inflammatory cell infiltration into the intestinal wall. IS-741 improved lesions in a rat DSS model by inhibiting leukocyte infiltration, suggesting the possibility of clinical application of this drug for IBD.

【 授权许可】

Unknown