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Membrane Transport of Tc-99m-Labeled Radiopharmaceuticals. I. Brain Uptake by Passive Transport

University of Maryland, Baltimore, Maryland

Correspondence: For reprints contact: Michael D. Loberg, E. R. Squibb & Sons, Georges Rd., New Brunswick, NJ 08903.

ABSTRACT

The membrane transport properties of twelve Tc-99m complexes were studied by determining each complex's brain uptake index (BUI), extent of protein binding, and octanol-to-saline partition coefficient. The chelating agents used were classified as either N-substituted carbamoylmethyliminodiacetates, substituted oxines, N.N'-diesters of EDTA, or N-substituted derivatives of DTPA. The Tc-99m complexes were found to cross the blood-brain barrier in proportion to their lipophilicity. Of the four types of chelating agents tested, substituted oxines appear to be most suitable for the development of diffusible Tc-99m-labeled compounds for imaging nonexcretory organs.

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