Edwards D S, Liu S, Lyster D M, Poirier M J, Vo C, Webb G A, Zhang Z, Orvig C
Du Pont Merck Pharmaceutical Company, Radiopharmaceutical Division, N. Billerica, MA 01862.
Nucl Med Biol. 1993 Oct;20(7):857-63. doi: 10.1016/0969-8051(93)90152-k.
A series of monocationic complexes of N-substituted-3-hydroxy-2-methyl-4-pyridinones labeled with technetium(IV)-99m have been evaluated in vivo as potential radiopharmaceuticals. The pyridinones have different substituents at the ring nitrogen atom: ethyl, i-propyl, i-butyl, benzyl, phenyl, p-methoxyphenyl, 3-butoxypropyl and cyclohexyl. Biodistribution studies of the 99mTc complexes have been carried out in rabbits and mice. High kidney uptake and retention of the radionuclide has been shown in rabbits and mice with the cationic complexes of 3-hydroxy-1-(p-methoxyphenyl)-2-methyl-4-pyridinone and 1-(cyclohexyl)-3-hydroxy-2-methyl-4-pyridinone. These 99mTcL3+ compounds appear to be morphologic renal agents.
一系列用99m锝（IV）标记的N-取代-3-羟基-2-甲基-4-吡啶酮的单阳离子配合物已作为潜在的放射性药物在体内进行了评估。吡啶酮在环氮原子上有不同的取代基：乙基、异丙基、异丁基、苄基、苯基、对甲氧基苯基、3-丁氧基丙基和环己基。已在兔子和小鼠身上进行了99mTc配合物的生物分布研究。3-羟基-1-（对甲氧基苯基）-2-甲基-4-吡啶酮和1-（环己基）-3-羟基-2-甲基-4-吡啶酮的阳离子配合物在兔子和小鼠体内显示出高肾脏摄取和放射性核素滞留。这些99mTcL3+化合物似乎是形态学肾脏显像剂。
