首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Anticoccidial activities of 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine and other alpha 2 adrenergic agonists.
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Anticoccidial activities of 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine and other alpha 2 adrenergic agonists.

机译:7-溴-N-(2-咪唑啉亚基)-1H-吲唑-6-胺和其他α2肾上腺素能激动剂的抗球虫活性。

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摘要

Activity against the coccidial pathogen Eimeria tenella in chickens has been discovered among alpha 2 adrenergic agonists. The clonidine analog 7-bromo-N-(2-imidazolidinylidene)-1H-indazol-6-amine was active in feed at 7.5 ppm, a concentration similar to the use levels of potent commercial agents, e.g., maduramicin. Additional alpha 2 agonists were also found to have anticoccidial activity, for example, the catecholamine nordefrin, which is chemically unrelated to clonidine. However, alpha 1 agonists and alpha antagonists were inactive. These observations imply that anticoccidial effects reflect involvement of a receptor with the characteristics of the vertebrate alpha 2 adrenoceptor. alpha 2 agonists that permeate the blood-brain barrier (like clonidine) inhibit feed intake at efficacious levels, whereas those that are restricted to the peripheral compartment (such as catecholamines) do not inhibit feed intake as much. Hence, anticoccidial efficacy may be a peripheral adrenergic effect whereas depression of feed intake is likely centrally mediated.
机译:在α2肾上腺素能激动剂中发现了针对鸡球虫病艾美体球菌的活性。可乐定类似物7-溴-N-(2-咪唑啉亚基)-1H-吲唑-6-胺在饲料中的活性为7.5 ppm,其浓度与有效的商业制剂(例如马杜拉米定)的使用水平相似。还发现另外的α2激动剂具有抗球虫活性,例如儿茶酚胺去氧铁蛋白,其在化学上与可乐定无关。但是,alpha 1激动剂和alpha拮抗剂没有活性。这些观察结果暗示抗球虫作用反映了具有脊椎动物α2肾上腺素受体特征的受体的参与。透过血脑屏障的α2激动剂(如可乐定)以有效的水平抑制采食量,而限制在外周区室的那些(如儿茶酚胺)则不能抑制采食量。因此,抗球虫药功效可能是外周肾上腺素的作用,而采食量的下降可能是中央介导的。

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