Preparation and biodistribution of copper‐67 complexes with tetradentate schiff‐base ligands

Elizabeth K. John, Amy J. Bott, Mark A. Green

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

Abstract

Uncharged, lipophilic, low molecular weight copper complexes labeled with generator‐produced copper‐62 are of interest as potential radiopharmaceutials for imaging the brain with positron emission tomography (PET). We report here the synthesis and biodistribution of a series of [67Cu]copper(II) complexes with tetradentate N2O 22‐Schiff‐base ligands. The compounds studied varied in lipophilicity from log P = 1.7 to log P = 3.6, where P is the octanol/water partition coefficient. In rat biodistribution studies the tracers were generally found to penetrate the blood‐brain barrier following intravenous injection, but some far better than others. For closely related compounds brain uptake at 1 min postinjection increased with increasing lipophilicity, although log P was clearly not the sole determinant of high brain uptake. Substantial variations were also observed in the rate at which these various compounds are cleared from brain, with a few exhibiting the prolonged cerebral retention of tracer that would be desired for imaging with 62Cu and PET.

Original languageEnglish (US)
Pages (from-to)587-590
Number of pages4
JournalJournal of Pharmaceutical Sciences
Volume83
Issue number4
DOIs
StatePublished - Apr 1994
Externally publishedYes

ASJC Scopus subject areas

  • Pharmaceutical Science

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