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  • Title: Ester-modified 99mTcO[SN(R)S/S] mixed ligand complexes: synthesis and preliminary evaluation.
    Author: Tsoukalas C, Pirmettis I, Patsis G, Papadopoulos A, Raptopoulou CP, Terzis A, Papadopoulos M, Chiotellis E.
    Journal: Nucl Med Biol; 2001 Nov; 28(8):975-82. PubMed ID: 11711317.
    Abstract:
    Two novel 99mTc-(SNS/S) complexes: a mono-ester compound carrying an ethyl ester group on the tridentate ligand, 99mTcO[C(2)H(5)OOCCH(2)N(CH(2)CH(2)S)(2)][SC(6)H(4)CH(3)], 3, and a diester compound, carrying a second ethyl ester group on the monodentate ligand, 99mTcO[C(2)H(5)OOCCH(2)N(CH(2)CH(2)S)(2)][SC(6)H(4)COOC(2)H(5)], 4, were synthesized. The corresponding oxorhenium(V) complexes, 1 and 2 were also synthesized. Enzymatic hydrolysis demonstrated that 3 remains intact after 10 min incubation while 4 is totally converted to an unidentified hydrophilic complex. Tissue distribution data in mice revealed that both complexes, 3 and 4, exhibit significant initial brain uptake (1.42 and 1.01% of injected dose at 5 minutes post injection respectively) and fast blood clearance.
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