Rebello L H, Da Silva J R, Gutfilen B, Bernardo-Filho M
Universidade do Estado do Rio de Janeiro, Instituto de Biofísica e Biometria, Rio de Janeiro, Brasil.
J Nucl Biol Med (1991). 1994 Dec;38(4 Suppl 1):109-12.
Oxamniquine (OXY), a tetrahydroquinoline derivative, is used as an antischistosomal drug and generally has been labeled with carbon-14 and tritium. We decided instead to label it with technetium-99 (99mTc). In order to determine the optimal conditions, different concentrations of this drug were incubated with various stannous chloride solutions. We then added 99mTc, and chromatography was performed using 0.9% NaCl solution, acetone and 1.2N HCl as the mobile phase. Using a solution of 1.0 mg/mL stannous chloride and 0.5 mg/mL oxamniquine, over 94% of the radioactivity bound to oxamniquine (99mTc-OXY). In the biodistribution study, 99mTc-OXY was administered in mice intramuscularly, orally and intravenously. When the intramuscular route was used, the main uptake (after 30 minutes) of the labeled drug was in the kidneys, liver and intestines; after 240 minutes the labeled drug was still found in the liver and kidneys, but at increased levels in the intestines. It was also present in the faeces. When the oral route was employed, labeled OXY was mainly found in the stomach after 30 minutes, but there was a decrease after 240 minutes. During this period radioactivity increased in the intestines. When the intravenous route was employed the labeled OXY was found in the liver and spleen. The radioactivity decreased with time in these organs. Using infected animals, radioactivity was found in isolated worms.
奥沙尼喹（OXY）是一种四氢喹啉衍生物，用作抗血吸虫药物，通常用碳-14和氚进行标记。我们决定改用锝-99（99mTc）对其进行标记。为了确定最佳条件，将不同浓度的该药物与各种氯化亚锡溶液孵育。然后加入99mTc，并以0.9%氯化钠溶液、丙酮和1.2N盐酸作为流动相进行色谱分析。使用1.0mg/mL氯化亚锡和0.5mg/mL奥沙尼喹的溶液时，超过94%的放射性与奥沙尼喹结合（99mTc-OXY）。在生物分布研究中，99mTc-OXY通过肌肉注射、口服和静脉注射的方式给予小鼠。当采用肌肉注射途径时，标记药物的主要摄取部位（30分钟后）是肾脏、肝脏和肠道；240分钟后，标记药物仍可在肝脏和肾脏中发现，但在肠道中的含量增加。它也存在于粪便中。当采用口服途径时，标记的奥沙尼喹在30分钟后主要存在于胃中，但240分钟后含量下降。在此期间，肠道中的放射性增加。当采用静脉注射途径时，标记的奥沙尼喹存在于肝脏和脾脏中。这些器官中的放射性随时间下降。在感染动物中，在分离出的蠕虫中发现了放射性。
