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成年雄性大鼠体内2-乙氧基乙醇的代谢与排泄

Metabolism and excretion of 2-ethoxyethanol in the adult male rat.

作者信息

Cheever K L, Plotnick H B, Richards D E, Weigel W W

出版信息

Environ Health Perspect. 1984 Aug;57:241-8. doi: 10.1289/ehp.8457241.

Abstract

The routes of 14C excretion following the administration of a single oral 230 mg/kg body weight dose of 2-ethoxyethanol [ethanol-1,2-14C] or 2-ethoxyethanol [ethoxy-1-14C] to male Sprague-Dawley rats were investigated. Elimination of the 14C by the urinary route accounted for 76 to 80% of the dose within 96 hr. The main pathway of biotransformation is oxidation to the corresponding acid, with some subsequent conjugation of the acid metabolite with glycine. The major metabolites, ethoxyacetic acid and N-ethoxy-acetyl glycine, representing 73 to 76% of the administered dose, were eliminated in the urine. The major difference in the metabolic profiles of the two radiochemicals was in the rate and amount of 14CO2 expired via the lung. Of the administered 14C, 11.7% of the ethoxy-labeled and 4.6% of the ethanol-labeled compounds were eliminated as CO2. The biological half-time was 9.9 +/- 1.5 hr for the ethoxy-labeled compound and 12.5 +/- 1.9 hr for the ethanol label. After administration of the ethanol-labeled compound, the only radiolabeled component found in the rat testes was identified as ethoxyacetic acid. Results of this study suggest that the reported testicular effects in the rat may be a result of tissue levels of ethoxyacetic acid.

摘要

研究了给雄性斯普拉格 - 道利大鼠单次口服230mg/kg体重剂量的[乙醇 - 1,2 - ¹⁴C]2 - 乙氧基乙醇或[乙氧基 - 1 - ¹⁴C]2 - 乙氧基乙醇后¹⁴C的排泄途径。在96小时内,经尿液途径排出的¹⁴C占剂量的76%至80%。生物转化的主要途径是氧化为相应的酸,随后该酸代谢物会与甘氨酸进行一些结合。主要代谢物乙氧基乙酸和N - 乙氧基 - 乙酰甘氨酸占给药剂量的73%至76%,通过尿液排出。这两种放射性化学物质代谢谱的主要差异在于经肺呼出的¹⁴CO₂的速率和量。在给药的¹⁴C中,乙氧基标记化合物的11.7%和乙醇标记化合物的4.6%以CO₂形式排出。乙氧基标记化合物的生物半衰期为9.9±1.5小时,乙醇标记物的生物半衰期为12.5±1.9小时。给予乙醇标记化合物后,在大鼠睾丸中发现的唯一放射性标记成分被鉴定为乙氧基乙酸。本研究结果表明,报道的大鼠睾丸效应可能是乙氧基乙酸组织水平的结果。

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