N-[N-(3-diphenylphosphinopropionyl)glycyl]cysteine and its methyl ester derivative were labeled with (99m)Tc at neutral pH, leading to a single species in high yield (>95%) in 30 min. RP-HPLC comparison with the analogue Re(V)-oxo complexes identified the labeled compounds as the anti isomers of pentacoordinated (99m)TcO[PN(2)S]-OH and (99m)TcO[PN(2)S]-OMe complexes. The compounds are stable from pH 7 to pH 9 when (99m)TcO[PN(2)S]-OH interconverts to related syn isomer, while (99m)TcO[PN(2)S]-OMe undergoes both saponification and interconversion. They exhibit high stability in human plasma and in vivo (mice), and a biodistribution characterized by hepatobiliary excretion.
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