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Cationic Tc-99m Complexes as Potential Myocardial Imaging Agents

University of Cincinnati and Nuclear Medicine Laboratory, BRH, FDA, Cincinnati, Ohio

Correspondence: For reprints contact: Edward Deutsch, PhD, Dept. of Chemistry, Univ. of Cincinnati, Cincinnati, OH 45221.

ABSTRACT

Nineteen cationic Tc-99m complexes, based upon four different ligand series, have been synthesized under "no carrier added" conditions and qualitatively evaluated as myocardial imaging agents in a dog model. Of these complexes, the four halogen derivatives of the diars series [diars = o-phenylenebis(dimethylarsine)] successfully concentrate in the myocardium. These Tc-99m diars complexes are shown by thin-layer chromatography to be identical to the Tc-99 analogs that have been fully characterized as trans octahedral complexes of Tc(III) by classical chemical techniques. Tissue distribution studies in rats show a definite difference in the biodistributions of (^99mTc(diars)₂Cl₂]⁺ and [^99mTc(diars)₂Br₂]⁺, despite the similar size, shape, charge, and lipophilicity of these two complexes. A tissue distribution study in resting beagle dogs shows that [^99mTc(diars)₂Br₂]⁺ accumulates in the normal myocardium about half as well as Tl-201 (0.022 compared with 0.038 %dose/g).