Preparation and biodistribution of copper-67 complexes with tetradentate Schiff-base ligands

E. K. John, A. J. Bott, Mark Green

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

Uncharged, lipophilic, low molecular weight copper complexes labeled with generator-produced copper-62 are of interest as potential radiopharmaceuticals for imaging the brain with positron omission tomography (PET). We report here the synthesis and biodistribution of a series of [67Cu]copper(II) complexes with tetradentate N2O22 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 - 1994
Externally publishedYes

Fingerprint

Schiff Bases
Copper
Brain
Ligands
Octanols
Radiopharmaceuticals
Blood-Brain Barrier
Imaging techniques
Neuroimaging
Intravenous Injections
Positrons
Molecular Weight
Tomography
Electrons
Rats
Water
Molecular weight

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

Cite this

Preparation and biodistribution of copper-67 complexes with tetradentate Schiff-base ligands. / John, E. K.; Bott, A. J.; Green, Mark.

In: Journal of Pharmaceutical Sciences, Vol. 83, No. 4, 1994, p. 587-590.

Research output: Contribution to journalArticle

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