Saji H, Yokoyama A, Tanaka H, Odori T, Morita R, Torizuka K
Radioisotopes. 1979 Mar;28(3):145-50. doi: 10.3769/radioisotopes.28.3_145.
Labeling of 2-mercaptopropionylglycine (2-MPG) with 99mTc, was studied and its chemical characteristics were examined. Further, biliary excretion behavior of this complex was comparatively estimated in mice, rats, and rabbits. 99mTc-2-MPG was rapidly excreted in large quantities into the bile in mice and rats: within 1 hr after injection, 51% of the injected dose was recovered from the bile in rats. On the other hand, the ligand exchange reaction between this complex and penicillamine indicates that a low hydrolyzed 99mTc species is coordinated with 2-MPG. These results suggest that a low hydrolyzed 99mTc is an effective feature in biliary excretion behavior of 99mTc compounds. Another interesting in vivo behavior of 99mTc-2-MPG is the difference observed in mice and rabbits: in mice, very high 99mTc activity is concentrated in the gallbladder and the clearance from tissues other than the gallbladder is rapid, whereas in rabbits, although a rapid and high excretion into the gallbladder is observed, a considerable high 99mTc activity is retained in the liver and the kidney. One reasons for this different in vivo behavior is the low stability of this complex at high dilution: a big animal has the large dilution volume which lead to higher decomposition estimated by the higher liver and kidney retention or the lower bile excretion. In conclusion, studies carried on 99mTc-2-MPG showed a good biliary excretion behavior but an in vivo unstableness in big animals.
研究了用99mTc标记2-巯基丙酰甘氨酸(2-MPG)的方法,并检测了其化学特性。此外,还比较评估了该配合物在小鼠、大鼠和兔子体内的胆汁排泄行为。99mTc-2-MPG在小鼠和大鼠体内迅速大量排泄到胆汁中:注射后1小时内,大鼠胆汁中回收了51%的注射剂量。另一方面,该配合物与青霉胺之间的配体交换反应表明,低水解的99mTc物种与2-MPG配位。这些结果表明,低水解的99mTc是99mTc化合物胆汁排泄行为的一个有效特征。99mTc-2-MPG另一个有趣的体内行为是在小鼠和兔子身上观察到的差异:在小鼠中,非常高的99mTc活性集中在胆囊中,从胆囊以外的组织清除速度很快,而在兔子中,虽然观察到快速且大量排泄到胆囊中,但肝脏和肾脏中仍保留相当高的99mTc活性。这种不同体内行为的一个原因是该配合物在高稀释度下稳定性较低:大型动物的稀释体积大,这导致根据肝脏和肾脏中较高的保留率或较低的胆汁排泄率估计的分解程度更高。总之,对99mTc-2-MPG进行的研究表明其具有良好的胆汁排泄行为,但在大型动物体内不稳定。