• Publications
  • Influence
Derivatives of 5-hydroxy-6-methyl-2-aminotetralin.
Three title compounds were designed to provide semirigid congeners of m-tyramine in which the ring position ortho to the phenolic OH is blocked to metabolic hydroxylation and were potent in a cat cardioaccelerator nerve assay, which involves dopamine receptors.
Analysis of cyclodextrins using fast atom bombardment/mass spectrometry and tandem mass spectrometry
The combination of fast atom bombardment/mass spectrometry (FAB/MS) and FAB with tandem mass spectrometry (FAB/MS/MS) was used for the characterization of nearly 30 chemically modified cyclodextrins.
Metabolism and disposition of the dopaminergic agonist 5-hydroxy-6-methyl-2-di-n-propylaminotetralin in the rat.
Data indicate that DK-118 is metabolized in the rat by a combination of N-dealkylation, oxidation of the 6-methyl carbon, and conjugation with sulfate, which indicates enterohepatic circulation of some of the drug/metabolites excreted in bile.
Dopamine receptor stimulating activity of 5-hydroxy-6-methyl-2-aminotetralin derivatives.
The results suggest that DK-121 and DK-118 possess stimulant properties on dopaminergic receptors in the central and peripheral nervous system, however,DK-121 does not appear to stimulate postsynaptic dopamine receptors inThe central nervous system.
Synthesis of 5-hydroxy-[6-14C]-methyl-2-di-n-propylaminotetralin
By an improved synthesis, 5-hydroxy-6-methyl-2-di-n-propylaminotetralin (DK-118), a dopamine agonist, has been obtained in only six steps and in greater than 10% overall yield. This new synthesis has
Effects of metyrapone on the pharmacological activity, plasma levels and urinary excretion of the dopamine receptor agonist DK-118.
Results of this study show that inhibition of DK-118 metabolism reduces certain of its pharmacologic actions, indicating that one or more of the metabolites of the drug may contribute to its effects.