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五氯茴香醚在F344大鼠和B6C3F1小鼠中的毒代动力学

Toxicokinetics of pentachloroanisole in F344 rats and B6C3F1 mice.

作者信息

Yuan J H, Goehl T J, Murrill E, Moore R, Clark J, Hong L, Irwin R

机构信息

National Institute of Environmental Health Sciences, Research Triangle Park, NC 27709.

出版信息

Xenobiotica. 1993 Apr;23(4):427-38. doi: 10.3109/00498259309057031.

Abstract
  1. Toxicokinetics of pentachloroanisole (PCA) were studied in F344 rat and B6C3F1 mouse of both sexes by gavage at doses of 10, 20 and 40 mg/kg and by i.v. at 10 mg/kg. 2. PCA was rapidly demethylated to pentachlorophenol (PCP) in both rat and mouse and the resulting PCP plasma concentrations were much higher than that of parent PCA due to the much smaller apparent volume of distribution of PCP. 3. Peak plasma concentrations of PCA and PCP increased with dose in both rat and mouse. 4. Bioavailability of PCA was low in both rat and mouse and was sex independent. 5. The high plasma concentrations and relatively long biological half-life of PCP in both species after both i.v. and oral dosing with PCA indicate possible bioaccumulation of PCP upon multiple oral administrations of PCA.
摘要
  1. 采用灌胃法,以10、20和40mg/kg的剂量以及静脉注射10mg/kg的剂量,在F344大鼠和B6C3F1小鼠两性中研究了五氯苯甲醚(PCA)的毒代动力学。2. PCA在大鼠和小鼠体内均迅速脱甲基化为五氯苯酚(PCP),由于PCP的表观分布容积小得多,所产生的PCP血浆浓度远高于母体PCA的血浆浓度。3. 大鼠和小鼠体内PCA和PCP的血浆峰浓度均随剂量增加。4. PCA在大鼠和小鼠中的生物利用度均较低,且与性别无关。5. 在PCA静脉注射和口服给药后,两种物种中PCP的高血浆浓度和相对较长的生物半衰期表明,多次口服PCA后PCP可能会发生生物蓄积。

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