Brain levels and metabolism of the dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene after administration of various prodrugs.

doi:10.1021/JM00350A022

Paper

Brain levels and metabolism of the dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene after administration of various prodrugs.

Published Aug 1, 1982 · A. Horn, H. Griever-Kazemier, D. Dijkstra

Journal of medicinal chemistry

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Abstract

The synthesis of four prodrug diesters (diacetyl, diisobutyryl, dipivaloyl, and dibenzoyl) of the potent dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene (6,7-ADTN) is described. The effects of prodrug structure on the levels of 6,7-ADTN in the rat corpus striatum and cerebellum, as well as the levels of the metabolite, 6-hydroxy-7-methoxy-2-aminotetralin, in the corpus striatum, have been determined after intraperitoneal administration. In addition, the striatal levels of 6,7-ADTN after administration of the dibenzoyl analogue via intraperitoneal, subcutaneous, and oral routes have been measured. These prodrugs produce a significant improvement in the penetration and accumulation of 6,7-ADTN in the brain.

Non-RCTAnimal Study

Study Snapshot

Prodrugs of the dopaminergic agonist 6,7-ADTN significantly improve its penetration and accumulation in the brain, with dibenzoyl analogues showing the most significant improvement in brain levels.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Brain levels and metabolism of the dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene after administration of various prodrugs.

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