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本实验使用我所研制的[2-~(14)C]四氧嘧啶,比度为629kBq/mg,放化纯度>95％。试验动物为ICR小鼠,分别尾静脉注射74kBq/0.2ml,经5、30、60min及24h后处死,各取约20mg内脏、骨及血液,分别用甲酸、H_2O_2消化后,液闪测量其放射性,计算摄取率(D％/g)。使用pH≈6及pH≈3.8两种四氧嘧啶溶液作对比。pH≈6组注射后5min,肾即明显浓集,摄取率达24.34,为血、肝的4.4倍,而其他脏器摄取率均在5以下,其浓集次序为肾、血、肝、肺、胰、肠、骨、肌、心、脾和脑。胰摄取率为2.56,在各脏器中占第五位,与血液之比为0.46。注射后15min,肾的摄取率为12.91,其他脏器均在3以下,而胰仅为1.27,退居第七位。30min后,各脏器摄取率进一步下降:肾3.86、血2.01、胰0.89。胰仍为第七位。60min及24h,各脏器的放射性已接近本底。pH≈3.8组结果与上述相似,也以肾最高,胰也未见明显放射性浓集,但排泄速度稍慢。每鼠注射185kBq/0.2ml后15、60min及24h,作整体放射自显影,结果也与上述相似,即15、60min时肾及膀胱尿液中放射性最强,肝次之,其他脏器的放射性均无突出表现,胰也未显影。24h后的标本上,除骨外,各脏器的放射性基本消失。以上结果表明,四氧嘧啶大部分经肾迅速排出,24h已基本清除。除肾外,各脏器均无特殊浓集。尿液纸层析分析表明
In this experiment, I developed [2- ~ (14) C] alloxan, the ratio of 629kBq / mg, radiochemical purity> 95%. The experimental animals were ICR mice, respectively, tail vein injection of 74kBq / 0.2ml, after 5,30,60min and 24h after sacrifice, each taking about 20mg visceral, bone and blood, were digested with formic acid, H_2O_2, measured by liquid scintillation radioactivity , The uptake rate (D% / g) was calculated. Use pH≈6 and pH≈3.8 two alloxan solution for comparison. In the group of pH≈6, the kidneys were obviously concentrated 5 minutes after the injection, the uptake rate was 24.34, which was 4.4 times that of the blood and liver, while the uptake rates of other organs were all below 5. The order of concentration was kidney, blood, liver and lung , Pancreas, gut, bone, muscle, heart, spleen and brain. The rate of pancreatic uptake was 2.56, which was the fifth highest among all organs and the ratio to blood was 0.46. 15min after injection, the renal uptake rate was 12.91, other organs were below 3, while the pancreas was only 1.27, relegated to the seventh place. After 30min, the organ uptake rate further decreased: 3.86 in kidney, 2.01 in blood and 0.89 in pancreas. Pancreas is still seventh. 60min and 24h, the radioactivity of various organs is close to the background. pH ≈ 3.8 group results similar to the above, but also the highest renal, pancreatic no significant radioactive concentration, but the drainage rate slower. Each rat injected 185kBq / 0.2ml after 15,60min and 24h, for the whole autoradiography, the results also similar to the above, that is, 15,60min when the most radioactive renal and bladder urine, followed by the liver, the other organs of radioactivity No outstanding performance, pancreatic did not develop. After 24h samples, in addition to bone, the radioactivity of various organs disappeared. The above results show that most of the alloxan rapidly excreted by the kidneys, 24h has been basically cleared. In addition to the kidneys, no special concentration of the organs. Urine paper chromatography analysis showed