El Dareer S M, Tillery K F, Lloyd H H, Hill D L
Cancer Treat Rep. 1982 Jan;66(1):183-6.
The disposition of tritium-labeled indicine N-oxide (INO) was evaluated in mice and rhesus monkeys. Disappearance of INO from the serum of BDF1 mice given iv doses of 100 or 500 mg/kg occurred with an initial half-life of about 11 mins followed by a second phase greater than 100 mins. At 2 hrs after iv injection of mice, the highest concentrations of INO were present in kidney, liver, and intestine. In CDF1 mice bearing P388 leukemia cells and injected ip with a dose of 500 mg/kg, INO was found, in equal concentrations, in cells of the parent line, which is resistant to INO, and in cells of a line resistant to cyclophosphamide but sensitive to INO. Serum levels of INO in these mice decreased with an initial half-life of about 20 mins. For monkeys given iv doses of 24, 2.4 of 0.24 mg/kg, INO disappeared from the serum in three phases, with average half-lives of 3, 32, and 180 mins, respectively. Half-lives for the two observed phases of urinary excretion were 40 and 240 mins. In 24 hrs, both mice and monkeys excreted greater than 80% of the doses unchanged.
对氚标记的印度獐牙菜N - 氧化物（INO）在小鼠和恒河猴体内的处置情况进行了评估。给BDF1小鼠静脉注射100或500mg/kg剂量的INO后，血清中INO的消失过程呈现出两个阶段，初始半衰期约为11分钟，随后第二阶段大于100分钟。静脉注射小鼠2小时后，INO在肾脏、肝脏和肠道中的浓度最高。在携带P388白血病细胞并腹腔注射500mg/kg剂量的CDF1小鼠中，在对INO耐药的亲本细胞系和对环磷酰胺耐药但对INO敏感的细胞系中发现INO浓度相等。这些小鼠血清中INO水平下降的初始半衰期约为20分钟。给恒河猴静脉注射24、2.4或0.24mg/kg剂量的INO后，血清中INO分三个阶段消失，平均半衰期分别为3、32和180分钟。观察到的尿排泄两个阶段的半衰期分别为40和240分钟。在24小时内，小鼠和猴子排出的剂量均超过80%且未发生变化。
