生物活性 | |||
---|---|---|---|
描述 | Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. The good efficacy of toltrazuril administered orally to lambs in the prepatent period in subclinical natural Eimeria infections in housed lambs[3]. G4 and G5 animals immunized with 0.2% diclazuril-treated oocysts showed a significant decrease in bloody diarrhea severity, lesion scores, and oocyst counts in comparison to those immunized with untreated oocysts. Diclazuril is effective in attenuating Eimeria oocysts[4]. The mRNA and protein expression levels of EtENO were decreased by 36.3 and 40.36%, respectively, by diclazuril treatment. With diclazuril treatment, it was significantly reduced in the surface and cytoplasm and even disappeared in the nucleus of the infected/diclazuril group[5]. Diclazuril treatment significantly protected dams from hepatitis, also in tachyzoites dose (100, 300, 600) dependent manner (respectively infected-treated versus infected controls). Colonic tissues were significantly shortened in length, with infiltration of lymphocytes, and macrophages and microabscess formations in the cryptic structures, with significant improvement in diclazuril treated animals. Additionally, the number of fetuses, fetal length and fetal weight were preserved in diclazuril treated dams[6]. |
临床研究 | |||||
---|---|---|---|---|---|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00001018 | Cryptosporidiosis ... 展开 >> HIV Infections 收起 << | Phase 1 | Completed | - | United States, California ... 展开 >> USC School of Medicine Los Angeles, California, United States, 90033 United States, New York Dr Douglas Dieterich New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 << |
NCT00002027 | Cryptosporidiosis ... 展开 >> HIV Infections 收起 << | Not Applicable | Completed | - | United States, New York ... 展开 >> Dr Douglas Dieterich New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 << |
NCT00002278 | Cryptosporidiosis ... 展开 >> HIV Infections 收起 << | Not Applicable | Completed | - | United States, New York ... 展开 >> Bellevue Hosp / New York Univ Med Ctr New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 << |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.25mL |
12.27mL 2.45mL 1.23mL |
24.53mL 4.91mL 2.45mL |
参考文献 |
---|