Compounds for site-enhanced delivery of radionuclides and...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/90 (2006.01) C07D 207/404 (2006.01) C07D 213/82 (2006.01) C07D 277/04 (2006.01) C07D 285/00 (2006.01) C07D 401/12 (2006.01) C07F 15/00 (2006.01) C07K 5/06 (2006.01)

Patent

CA 1267899

Abstract of the Disclosure A dihydropyridine ? pyridinium salt type of redox, or chemical, delivery system for the site specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a reactive hydroxyl. carboxyl, amino, amide or imide group is coupled to a carrier moiety comprising a dihydro- pyridine ? pyridinium salt nucleus and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic tech- niques.

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