毒性动力学和生物转化3 - (4-methylbenzylidene)樟脑口服后在老鼠身上。
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Schauer Volkel W, Colnot T,嗯,Broschard TH, Dekant W
毒性动力学和生物转化3 - (4-methylbenzylidene)樟脑口服后在老鼠身上。
Toxicol:杂志。2006年10月15日,216 (2):331 - 8。doi: 10.1016 / j.taap.2006.05.012。2006年5月23日Epub。
- PubMed ID
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16806338 (在PubMed]
- 文摘
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(3)- 4-Methylbenzylidene樟脑(4-MBC)是一个防晒霜中的紫外线空气净化常用剂和化妆品。模棱两可的结果在某些筛查荷尔蒙活动发起讨论可能的弱4-MBC求偶性。在这项研究中,毒性动力学和生物转化4-MBC口服后在大鼠表征。男性和女性Sprague-Dawley老鼠每组(n = 3)管理单一口服剂量的25个或250毫克/公斤bw 4-MBC玉米油。代谢物形成的动力学特征和消除4-MBC及其血液和尿液的代谢物。代谢物4-MBC的特点是(1)H核磁共振波谱和质/女士3 - (4-carboxybenzylidene)樟脑和四个异构体3 - (4-carboxybenzylidene) hydroxycamphor包含羟基位于樟脑环系统与3 - (4-carboxybenzylidene) 6-hydroxycamphor主要代谢物。4-MBC口服后,只有非常低的浓度4-MBC存在于血液和峰值浓度的3 - (4-carboxybenzylidene)樟脑大约500倍高于4-MBC;3 - (4-carboxybenzylidene) 6-hydroxycamphor血药浓度的检测极限以下。4-MBC血药浓度和3 - (4-carboxybenzylidene)樟脑4-MBC 10 h后政府内部达到顶峰,然后减少的半衰期大约15 h。没有重大差异在雄性和雌性大鼠血浓度峰值。在尿液中,一个异构体3 - (4-carboxybenzylidene) hydroxycamphor主要代谢物[3 - (4-carboxybenzylidene) 6-hydroxycamphor],其他同分异构体和3 - (4-carboxybenzylidene)樟脑只有轻微的代谢物排出尿液。 However, urinary excretion of 4-MBC-metabolites represents only a minor pathway of elimination for 4-MBC, since most of the applied dose was recovered in feces as 3-(4-carboxybenzylidene)camphor and, to a smaller extent, as 3-(4-carboxybenzylidene)-6-hydroxycamphor. Glucuronides of both metabolites were also present in feces, but partly decomposed during sample workup and were thus not quantified. The results show that absorbed 4-MBC undergoes extensive first-pass biotransformation in rat liver resulting in very low blood levels of the parent 4-MBC. Enterohepatic circulation of glucuronides derived from the two major 4-MBC metabolites may explain the slow excretion of 4-MBC metabolites with urine and the small percentage of the administered doses recovered in urine.
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