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 ... more >> HIV Infections Collapse <<	Phase 1	Completed	-	United States, California ... more >> 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 Collapse <<
  NCT00002027	Cryptosporidiosis ... more >> HIV Infections Collapse <<	Not Applicable	Completed	-	United States, New York ... more >> 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 Collapse <<
  NCT00002278	Cryptosporidiosis ... more >> HIV Infections Collapse <<	Not Applicable	Completed	-	United States, New York ... more >> 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 Collapse <<

• 参考文献

• [1] Rucquoy M, Sorel L. Diclofenamide in the treatment of therapy-resistant epilepsy. Acta Neurol Belg. 1978 May-Jun;78(3):174-82.

  [2] Kanski JJ. Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors. Br J Ophthalmol. 1968 Aug;52(8):642-3.

  [3] Diaferia M, Veronesi F, Morganti G, Nisoli L, Fioretti DP. Efficacy of toltrazuril 5 % suspension (Baycox®, Bayer) and diclazuril (Vecoxan®, Janssen-Cilag) in the control of Eimeria spp. in lambs. Parasitol Res. 2013 Aug;112 Suppl 1:163-8

  [4] El-Ashram S, Aboelhadid SM, Arafa WM, Gadelhaq SM, Abdel-Razik AH. Protective potential of diclazuril-treated oocysts against coccidiosis in layer chicks. Vet Parasitol. 2019 Sep;273:105-111

  [5] Zhou BH, Ding HY, Yang JY, Chai J, Guo HW, Wang HW. Effects of diclazuril on the expression of enolase in second-generation merozoites of Eimeria tenella. Poult Sci. 2020 Dec;99(12):6402-6409

  [6] Oz HS, Tobin T. Diclazuril Protects against Maternal Gastrointestinal Syndrome and Congenital Toxoplasmosis. Int J Clin Med. 2014 Jan 1;5(3):93-101

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