A potential copper radiopharmaceutical for imaging the heart and brain: Copper-labeled pyruvaldehyde bis(N4-methylthiosemicarbazone)

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Abstract

An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis(N4-methylthiosemicarbazone), [64Cu]Cu-PTSM, was prepared and found to be lipophilic (octanol/saline partition coefficient, log p = 1.97 ± 0.03). Biodistribution studies following i.v. injection of [64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7% of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.

Original languageEnglish (US)
Pages (from-to)59-61
Number of pages3
JournalNuclear Medicine and Biology
Volume14
Issue number1
StatePublished - 1987
Externally publishedYes

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Pyruvaldehyde
Radiopharmaceuticals
Neuroimaging
Copper
Brain
Octanols
Injections
Half-Life
copper pyruvaldehyde bis(N(4)-methylthiosemicarbazone) complex

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

Cite this

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title = "A potential copper radiopharmaceutical for imaging the heart and brain: Copper-labeled pyruvaldehyde bis(N4-methylthiosemicarbazone)",
abstract = "An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis(N4-methylthiosemicarbazone), [64Cu]Cu-PTSM, was prepared and found to be lipophilic (octanol/saline partition coefficient, log p = 1.97 ± 0.03). Biodistribution studies following i.v. injection of [64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7{\%} of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.",
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AU - Green, Mark

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N2 - An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis(N4-methylthiosemicarbazone), [64Cu]Cu-PTSM, was prepared and found to be lipophilic (octanol/saline partition coefficient, log p = 1.97 ± 0.03). Biodistribution studies following i.v. injection of [64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7% of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.

AB - An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis(N4-methylthiosemicarbazone), [64Cu]Cu-PTSM, was prepared and found to be lipophilic (octanol/saline partition coefficient, log p = 1.97 ± 0.03). Biodistribution studies following i.v. injection of [64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7% of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.

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