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首页> 外文期刊>Journal of Agricultural and Food Chemistry >ABSORPTION, TISSUE DISTRIBUTION, EXCRETION, AND METABOLISM OF H-3- AND C-14-LABELED EMAMECTIN BENZOATE IN RATS
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ABSORPTION, TISSUE DISTRIBUTION, EXCRETION, AND METABOLISM OF H-3- AND C-14-LABELED EMAMECTIN BENZOATE IN RATS

机译：H-3-和C-14标记的美美汀苯甲酸酯在大鼠中的吸收，组织分布，排泄和代谢

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摘要

Male and female rats were administered a single high (20 mg/kg, oral) or low (0.5 mg/kg, oral or intravenous) dose of radiolabeled 4 ''-deoxy-4 ''-(epi-methylamino)avermectin B-1a (MAB(1a)) benzoate. The bioavailability of MAB(1a) benzoate (low dose) in male and female rats was 43% and 63%, respectively. More than 98% of the total radioactivity was found in feces, with <0.4% in urine and <1.6% in the tissues. The total radioactive residues (TRR) in feces and tissues consisted of MAB(1a) and a single N-demethylated metabolite. The TRR contents (ppb parent equivalent) of kidney, liver, fat, muscle, spinal cord, and brain at day 1 post low oral dose in male rats were 437, 355, 241, 109, 30, and 8 ppb, respectively, and in female rats 260, 244, 192, 90, 11, and 5 ppb, respectively. The TRR contents of these tissues from both male and female rats declined to very low levels (less than or equal to 12 ppb) by day 7. The TRR content of tissues at day 7 post high dose was relatively high (8-2033 ppb). Lung and spleen had higher residue contents in comparison to other tissues. Daily pretreatment with the compound for 14 days had no effect on the tissue residue levels and metabolism.
机译：雄性和雌性大鼠分别接受高剂量（20 mg / kg，口服）或低剂量（0.5 mg / kg，口服或静脉内）放射性标记的4′-脱氧-4′-（表-甲基氨基）阿维菌素B- 1a（MAB（1a））苯甲酸酯。 MAB（1a）苯甲酸酯（低剂量）在雄性和雌性大鼠中的生物利用度分别为43％和63％。粪便中发现总放射性的98％以上，尿中<0.4％，组织中<1.6％。粪便和组织中的总放射性残留（TRR）由MAB（1a）和单个N-去甲基化代谢物组成。低剂量雄性大鼠在第1天，肾脏，肝脏，脂肪，肌肉，脊髓和大脑的TRR含量（ppb母体当量）分别为437、355、241、109、30和8 ppb，并且在雌性大鼠中分别为260、244、192、90、11和5 ppb。到第7天，雄性和雌性大鼠的这些组织的TRR含量均降至非常低的水平（小于或等于12 ppb）。高剂量后第7天的组织的TRR含量相对较高（8-2033 ppb）。 。与其他组织相比，肺和脾脏的残留物含量更高。每天用该化合物预处理14天对组织残留水平和代谢没有影响。

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