Zhang Z D, Zhou C M, Jin G Z, Zhang X, Yang L
Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Zhongguo Yao Li Xue Bao. 1990 Jul;11(4):289-92.
After iv [3H]stepholidine (SPD) 12 MBq/kg, the concentration-time curve in rats was found to be a two-compartment open model. The distribution phase T1/2 alpha = 3.6 min, the elimination phase T1/2 beta = 168 min. The absorbed radioactivities of [3H] SPD in 15-30 min were 80-87%. The amounts of [3H]SPD bound to plasma protein, liver and kidney homogenates were estimated to be 37, 31, and 30%, respectively. During 3 d after ip [3H]SPD 50 MBq/kg, 56% of the radioactivity was excreted in urine and 5% in feces, thus, it suggested that [3H]SPD was mainly excreted by kidneys. After iv a single dose of [14C]SPD in mice, the whole-body autoradiography showed that [14C]SPD was rapidly distributed among various tissues. High radioactivities were found in kidneys, liver, brain, salivary glands, Harder's glands, heart blood and muscle at 2 min and intensively localized in kidneys and stomach mucosa at 30 min. The radioactivities in these tissues disappeared 4 and 8 h later, while that in intestine could not be detected 24 h later.
静脉注射[3H]千金藤啶碱（SPD）12 MBq/kg后，大鼠体内的浓度-时间曲线符合二室开放模型。分布相T1/2α = 3.6分钟，消除相T1/2β = 168分钟。15 - 30分钟内[3H]SPD的吸收放射性为80 - 87%。与血浆蛋白、肝匀浆和肾匀浆结合的[3H]SPD量估计分别为37%、31%和30%。腹腔注射[3H]SPD 50 MBq/kg后3天内，56%的放射性经尿液排出，5%经粪便排出，因此表明[3H]SPD主要经肾脏排泄。小鼠静脉注射单剂量[14C]SPD后，全身放射自显影显示[14C]SPD迅速分布于各组织。2分钟时，肾脏、肝脏、脑、唾液腺、哈德氏腺、心血和肌肉中放射性较高，30分钟时在肾脏和胃黏膜中放射性集中。这些组织中的放射性在4小时和8小时后消失，而24小时后肠道中未检测到放射性。
