The peripheral benzodiazepine receptor ligand PK 11195 inhibits arthritis in the MRL-lpr mouse model.

The peripheral benzodiazepine receptor ligand PK 11195 inhibits arthritis in the MRL-lpr mouse model.
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外周苯二氮卓受体配体 PK 11195 可抑制 MRL-lpr 小鼠模型中的关节炎。

DOI:
10.1093/rheumatology/38.11.1068
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发表时间:
1999
期刊:
影响因子:
5.5
通讯作者:
P. Mcgeer
P. Mcgeer
中科院分区:
医学1区
文献类型:
--
作者:
J. Waterfield;E. Mcgeer;P. Mcgeer

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目的 当用完全弗氏佐剂致敏时,MRL-lpr品系的小鼠发展出严重的自身免疫性关节炎病症。病理学与人类类风湿性关节炎相似。我们研究了PK 11195(外周苯二氮卓类受体的强大配体)在该模型中是否具有预防或治疗作用。 方法 在13-14周龄时用完全弗氏佐剂致敏MRL-lpr小鼠。每日PK 11195注射在预充的同一天开始,以检测预防效果。在预充后10天开始每日PK 11195注射,以测试治疗效果。 结果 PK 11195显示出预防和治疗作用。在1 mg/kg/天剂量下,可抑制疾病发作。在3 mg/kg/天剂量下,它抑制了既定的疾病进展。 结论 有证据表明PK 11195可能是一类新的抗炎药的原型。
OBJECTIVE Mice of the MRL-lpr strain develop a severe autoimmune arthritic condition when primed with complete Freund's adjuvant. The pathology is similar to that seen in human rheumatoid arthritis. We investigated whether PK 11195, a powerful ligand for peripheral benzodiazepine receptors, would have preventative or therapeutic effects in this model. METHODS MRL-lpr mice were primed with complete Freund's adjuvant at 13-14 weeks of age. Daily PK 11195 injections were started on the same day as priming to test for preventative effects. Daily PK 11195 injections were started 10 days after priming to test therapeutic effects. RESULTS PK 11195 showed both preventative and therapeutic effects. At 1 mg/kg/day, it inhibited disease onset. At 3 mg/kg/day, it inhibited established disease progression. CONCLUSION The evidence suggests that PK 11195 may be the prototype of a new class of anti-inflammatory agents.
DOI: 10.1002/art.1780280511
发表时间: 1985-01-01
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