代谢
一只雄性和一只雌性大鼠通过单次口服灌胃方式接受了25 mg/kg剂量的(14)C-DPX-KJM44(氨基环吡咯甲酸甲酯)。动物被放置在玻璃代谢单元中,以收集14C呼出的挥发性物质和(14)CO2,持续48小时(每隔24小时)。尿液和粪便也在干冰上以24小时为间隔收集,持续168小时。通过液闪计数(LSC)、高效液相色谱(HPLC)和质谱(MS)分析,对尿液、粪便、组织、尸体、笼具清洗液和残余饲料中的放射性进行了量化。在单次25 mg/kg剂量后的48小时内,呼吸气体中未检测到放射性。尿液是放射性排泄的主要途径,168小时内雄性和雌性大鼠分别有80.4%和79.3%的给药剂量被检测到(大部分(78.8%,两个性别)在给药后前24小时内排出)。在168小时内,雄性和雌性大鼠粪便中的放射性分别为6.67%和3.06%,其中大部分在治疗后48小时内排出(雄性5.6%,雌性2.8%)。笼具清洗液和残余饲料中的放射性分别为雄性2.0%和雌性0.1%。168小时后,雄性和雌性的总体物质平衡分别为89.2%和82.6%。组织中的14C残留物通常低于定量限,除了雄性和雌性尸体中分别含有0.144%和0.121%的给药剂量,以及雄性胃肠道和内容物中总共含有0.009%的剂量。DPX-MAT28(氨基环吡咯)是尿液中唯一被识别的代谢物(两个性别均为78.8%的给药剂量)和粪便中(雄性4.57%,雌性1.72%的剂量)。氨基环吡咯甲酸甲酯
1 male and 1 female rat received a single oral gavage dose of (14)C-DPX-KJM44 /aminocyclopyrachlor methyl/ at 25 mg/kg. Animals were placed in glass metabolism units for collection of 14C exhaled volatiles and (14)CO2 for 48 hours (at 24-hour intervals). Urine and feces were also collected at 24-hour intervals over dry ice for 168 hours. Radioactivity was quantified in urine, feces, tissues, carcass, cage wash, and residual feed and urine and feces were also analyzed for metabolites (LSC, HPLC, mass spectrometry (MS)). Radioactivity was not detected in respired breath during 48 hours after a single 25 mg/kg dose. Urine was the main route of excretion of radioactivity with 80.4% (male) and 79.3% (female) of administered dose detected during 168 hours post-dosing (most (78.8% for both sexes) was excreted during the first 24 hours after dosing). 6.67% (male) and 3.06% (female) of administered radioactivity was found in feces during 168 hours with the majority excreted during 48 hours post-treatment (5.6% (male) and 2.8% (female)). Radioactivity detected in cage wash and residual food was 2.0% and 0.1% for the male and female, respectively. The overall material balance was 89.2% (male) and 82.6% (female) after 168 hours. 14C residues in tissues were generally below the limit of quantification except male and female carcasses contained 0.144% and 0.121% of administered dose, respectively, and the male gastrointestinal tract and contents contained 0.009% of dose combined. DPX-MAT28 /aminocyclopyrachlor/ was the only metabolite identified in urine (78.8% of administered dose for both sexes) and feces (4.57% (males) and 1.72% (females) of dose). /Aminocyclopyrachlor-methyl/
来源:Hazardous Substances Data Bank (HSDB)