首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Further investigation of anticoccidial activity of 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine.
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Further investigation of anticoccidial activity of 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine.

机译:进一步研究7-溴-N-(2-咪唑啉亚基)-1H-吲唑-6-胺的抗球虫活性。

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摘要

The clonidine analog 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine exhibits potent activity against Eimeria tenella infections in chickens. Disease control was abrogated by a selective alpha 2 antagonist, which is consistent with the dependence of such activity upon binding to receptors with characteristics of the vertebrate alpha 2 adrenoceptor. Lack of significant activity against the parasite in tissue culture and our inability to detect significant binding of alpha 2 adrenergic ligands to E. tenella imply that the anticoccidial action may be an indirect effect mediated by the host. Efficacy varied, depending upon the Eimeria species, being greatest for the cecal species E. tenella and less for the intestinal species. The effects described differ substantially from previous accounts of adrenergic actions on parasitic protozoa. The evidence suggests that we have observed a new mechanism of action for antiparasitic drugs.
机译:可乐定类似物7-溴-N-(2-咪唑啉亚基)-1H-吲唑-6-胺对鸡的艾美尔球虫感染具有有效的活性。选择性α2拮抗剂废除了疾病控制,这与这种活性对结合具有脊椎动物α2肾上腺素受体特征的受体的依赖性是一致的。缺乏对组织培养物中的寄生虫的显着活性,以及​​我们无法检测到α2肾上腺素能配体与天疱性大肠杆菌的显着结合,这表明抗球虫作用可能是宿主介导的间接作用。功效随艾美球虫种类的不同而变化,对盲肠大肠埃希氏菌而言最大,而对于肠道菌种则较小。所描述的效果与以前对寄生虫原生动物的肾上腺素能作用的描述大不相同。有证据表明,我们已经观察到抗寄生虫药物的新作用机理。

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