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Copper(II) Bis(thiosemicarbazone) Complexes as Potential Tracers for Evaluation of Cerebral and Myocardial Blood Flow with PET

Departments of Radiology and Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota

Correspondence: For reprints contact: Mark A. Green, Dept. of Medicinal Chemistry, School of Pharmacy, Purdue University, West Lafayette, IN 47907.

ABSTRACT

Wider application of position emission tomography would be facilitated by the availability of position-emitting radiopharmaceuticals labeled with nuclides, like ⁶²Cu, that are available from parent/daughter generator systems. Using a longer-lived copper isotope (⁶⁷Cu) we have examined three derivatives of copper(II) pyruvaldehyde bis(thiosemicarbazone) as potential tracers for evaluation of cerebral and myocardial blood flow: Cu(PTS), Cu(PTSM), and Cu(PTSM₂) (where PTS = pyruvaldehyde bis(thiosemicarbazone), PTSM = pyruvaldehyde bis(N⁴-methylthiosemicarbazone), and PTSM₂ = pyruvaldehyde bis(N⁴-dimethylthiosemicarbazone). All three lipophilic radiocopper complexes were obtained in high yield via a procedure that could be adapted to a "kit" formulation. In animal model systems CU(PTSM) and Cu(PTSM₂) show excellent uptake in the brain and heart following i.v. injection. These tracers differ in that Cu(PTSM) exhibits microsphere-like retention in the brain and heart, whereas Cu(PTSM₂) substantially clears from these organs. The relative cerebral pharmacokinetics of [⁶⁷Cu]Cu(PTSM) and [⁶⁷Cu]Cu(PTSM₂) are consistent with their known reactivity towards intracellular sulfhydryl groups.

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