Radiopharmaceuticals and chelating agents useful in their prepar

Details Radiopharmaceuticals and chelating agents useful in their prepar Radiopharmaceuticals and chelating agents useful in their prepar

1990-08-02

1992-08-04

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546141, 546147, 546153, 546169, 546172, 546176, 546261, 546263, C07D21700, C07D21514, C07D21118

Patent

active

051360381

ABSTRACT:
A dihydropyridine.revreaction. 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 primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.revreaction. pyridinium salt redox system 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 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 techniques.

REFERENCES:
patent: 3822194 (1974-07-01), Rushmere
patent: 4775763 (1988-10-01), Dalton et al.

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