Synthesis and evaluation of technetium-99m monocationic mixed ligand complexes of phenyl substituted/condensed tetradentate schiff's bases and trimethylphosphine

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-08-01 DOI:10.1016/0883-2897(92)90102-5

N.C. Goomer, P.V. Kulkarni, A. Constantinescu, P. Antich, R.W. Parkey, J.R. Corbett

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引用次数: 1

Abstract

Tc-99m monocationic mixed ligand complexes of phenyl substituted/condensed Schiff's bases, N,N′-ethylene-bis-(benzoylacetone imine) (L_b) or N,N′-ethylene-bis-(salicylaldehyde imine) (L_c) or N,N′-ethylene-bis-(2-hydroxyacetophenone imine) (L_d) and trimethylphosphine were synthesized to determine the influence of the presence of a phenyl group in these tracers on their heart uptake in rats. A new formulation procedure using aq. β-hydroxypropylcyclodextrin (HPB) solution was developed for intravenous administration of nonpolar ^99mTc complexes. Comparison of biodistribution data for the reference ^99mTc complex from N,N′-ethylene-bis-(acetylacetone imine) and trimethylphosphine using HPB formulation and alternate formulation (0.9% saline) showed the same results. Biodistribution of the title ^99mTc complexes, [^99mTc L_b (PMe₃)₂]⁺, [^99mTc L_c (PMe₃)₂]⁺ and [^99mTc L_d (PMe₃)₂]⁺ showed heart-to-blood activity ratios of 1.7, 2.1 and 1.7, respectively, at 15 min post-injection in rats.

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苯基取代/浓缩四齿席夫碱与三甲基膦的锝-99m单阳离子混合配体配合物的合成与评价

合成了苯基取代/浓缩希夫碱、N,N ' -乙烯-双-(苯甲酰丙酮亚胺)(Lb)或N,N ' -乙烯-双-(水杨醛亚胺)(Lc)或N,N ' -乙烯-双-(2-羟基苯乙酮亚胺)(Ld)和三甲基膦的Tc-99m单阳离子混合配体，以确定这些示踪剂中苯基的存在对大鼠心脏摄取的影响。采用aq β-羟丙基环糊精(HPB)溶液制备非极性99mTc配合物。用HPB配方和替代配方(0.9%生理盐水)比较N,N ' -乙烯-双-(乙酰丙酮亚胺)和三甲基膦的99mTc络合物的生物分布数据，结果相同。99mTc复合物[99mTc Lb (PMe3)2]+、[99mTc Lc (PMe3)2]+和[99mTc Ld (PMe3)2]+在大鼠体内的生物分布显示，注射后15 min心血活性比分别为1.7、2.1和1.7。

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International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology

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