当前位置: X-MOL 学术Toxicol. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Disposition and metabolism of N-butylbenzenesulfonamide in Sprague Dawley rats and B6C3F1/N mice and in vitro in hepatocytes from rats, mice, and humans
Toxicology Letters ( IF 2.9 ) Pub Date : 2020-02-01 , DOI: 10.1016/j.toxlet.2019.11.015
Suramya Waidyanatha 1 , Sherry R Black 2 , Purvi R Patel 2 , Cynthia V Rider 1 , Scott L Watson 2 , Rodney W Snyder 2 , Timothy R Fennell 2
Affiliation  

N-Butylbenzenesulfonamide (NBBS) is a plasticizer detected in the environment suggesting potential human exposure. These studies investigated the in vitro hepatic clearance and disposition of [14C]NBBS in rodents following a single gavage (2, 20 or 200 mg/kg) or intravenous (IV) administration (20 mg/kg). NBBS was cleared slower in hepatocytes from humans compared to rodents. [14C]NBBS was well-absorbed in male rats following gavage administration and excreted extensively in urine (70-76%) and feces (11-15%) 72 h following administration. Following a 20 mg/kg gavage dose in male rats, 25% of the dose was excreted in bile by 24 h suggesting that observed fecal excretion was due to biliary excretion. The radioactivity was distributed to tissues with 14% and 8% of the administered dose remaining in tissues at 24 and 72 h, respectively. There was no apparent dose-dependent effect in disposition in male rats. Disposition patterns were similar in female rats (urine, 83%; feces, 14%) and male (urine, 69%; feces, 11%) and female (urine, 72%; feces, 9%) mice following gavage administration of 20 mg/kg. The disposition following IV administration was similar to that of gavage. Urinary radiochemical profiles were similar between doses, routes, species, and sexes. Among numerous metabolites identified, oxidative metabolites of NBBS predominated.

中文翻译:


N-丁基苯磺酰胺在 Sprague Dawley 大鼠和 B6C3F1/N 小鼠以及体外大鼠、小鼠和人类肝细胞中的分布和代谢



N-丁基苯磺酰胺 (NBBS) 是一种在环境中检测到的增塑剂,表明人类可能接触该增塑剂。这些研究调查了啮齿类动物单次灌胃(2、20 或 200 mg/kg)或静脉(IV)给药(20 mg/kg)后 [14C]NBBS 的体外肝脏清除率和处置情况。与啮齿类动物相比,NBBS 在人类肝细胞中的清除速度较慢。 [14C]NBBS在雄性大鼠中灌胃给药后吸收良好,并在给药后72小时通过尿液(70-76%)和粪便(11-15%)大量排泄。雄性大鼠灌胃剂量为 20 mg/kg 后,24 小时内 25% 的剂量通过胆汁排泄,表明观察到的粪便排泄是由于胆汁排泄所致。 24 小时和 72 小时时,放射性分布到组织中,分别有 14% 和 8% 的给药剂量残留在组织中。对雄性大鼠的处置没有明显的剂量依赖性影响。灌胃 20 粒后,雌性大鼠(尿液,83%;粪便,14%)、雄性(尿液,69%;粪便,11%)和雌性(尿液,72%;粪便,9%)小鼠的处置模式相似毫克/公斤。静脉注射后的分布与强饲相似。不同剂量、途径、物种和性别之间的尿液放射化学特征相似。在鉴定的众多代谢物中,NBBS 的氧化代谢物占主导地位。
更新日期:2020-02-01
down
wechat
bug