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 N2O2(2-)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.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
John EK,Bott AJ,Green MAdoi
10.1002/jps.2600830429subject
Has Abstractpub_date
1994-04-01 00:00:00pages
587-90issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49441-9journal_volume
83pub_type
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