Brain-specific dopaminergic activity involving dihydropyridine carboxamides, dihydroquinoline and isoquinoline carboxamides
AssigneeUniversity of Florida
InventorNicholas S. Bodor
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AssigneeUniversity of Florida
InventorNicholas S. Bodor
Estimating the term…
A brain-specific dopaminergic response is elicited in a patient in need of such treatment, e.g., a patient afflicted with Parkinson's disease of hyperprolactinemia, by administering thereto a therapeutically effective amount of preferably catechol protected dopamine tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g., 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type dopamine/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained brain-specific dopaminergic activity.
A compound having the formula ##STR42## or a non-toxic pharmaceutically acceptable salt thereof, wherein each R is independently hydrogen or an acyl radical selected from the group consisting of alkanoyl having 2 to 8 carbon atoms;
A compound having the formula ##STR58## wherein each R is independently hydrogen or an acyl radical selected from the group consisting of alkanoyl having 2 to 8 carbon atoms;
Dependencies are inferred from the claim text.