Tsuji R F, Magae J, Nagai K, Yamasaki M
Noda Institute for Scientific Research, Chiba, Japan.
Biosci Biotechnol Biochem. 1992 Dec;56(12):2034-6. doi: 10.1271/bbb.56.2034.
L-156,602, a C5a receptor antagonist, was found as an immunosuppressant with preferential effects on delayed-type hypersensitivity (DTH) in our screening program and it was shown that L-156,602 suppressed the efferent phase of DTH. Here, we tested its effects on experimental models of inflammation induced in mice. L-156,602 did not suppress serotonin- and carrageenan- induced inflammation while it completely suppressed concanavalin A-induced inflammation 4 h after elicitation. The inflammation appeared 24 h after the elicitation with concanavalin A and it was significantly suppressed by L-156,602. Muramyl dipeptide (MDP)-induced acute joint inflammation was also significantly suppressed by L-156,602. These results demonstrated the unique immunomodulating properties of L-156,602 in mouse experimental models of inflammation.
L-156,602是一种C5a受体拮抗剂，在我们的筛选项目中被发现是一种对迟发型超敏反应（DTH）有优先作用的免疫抑制剂，并且已表明L-156,602可抑制DTH的传出相。在此，我们测试了其对小鼠诱导的炎症实验模型的作用。L-156,602不抑制血清素和角叉菜胶诱导的炎症，而在激发后4小时它完全抑制伴刀豆球蛋白A诱导的炎症。伴刀豆球蛋白A激发后24小时出现炎症，L-156,602可显著抑制该炎症。L-156,602也显著抑制了胞壁酰二肽（MDP）诱导的急性关节炎症。这些结果证明了L-156,602在小鼠炎症实验模型中具有独特的免疫调节特性。
