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Correlation of lipophilicity to biodistribution of 99mTc-labelled aminothiols
M Papadopoulos1, E Chiotellis, A Varvarigou
1Radiopharmaceuticals Laboratory, Institute of Radioisotopes and Radiodiagnostics, NCSR Demokritos, Attiki, Greece.
Nuclear Medicine and Biology
|January 1, 1993
Abstract:
A series of 99mTc-DADT complexes substituted with heterocyclic amines were synthesized and tested for their ability to cross the BBB. Each 99mTc-DADT complex analysed by HPLC was found to consist of two epimers. The more lipophilic epimers were biodistributed in mice. The data demonstrated a significant brain uptake (3-12% dose/g whole brain) and a high lung accumulation (11-85% dose/g) at 2 min p.i. Between the partition coefficients of the technetium complexes, a linear correlation for lung accumulation was observed, while a parabolic curve for brain uptake was found.