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Metabolism and disposition of the dopaminergic agonist 5-hydroxy-6-methyl-2-di-n-propylaminotetralin in the rat

Journal Article · · Drug Metab. Dispos.; (United States)
OSTI ID:6085667
; ;

As part of a program to investigate the metabolism and disposition of putative dopamine receptor agonists, DK-118 (5-hydroxy-6-methyl-2-di-n-propylaminotetralin) was chosen for study in the rat. Following a 3.85 mg/kg (ip) dose of 5-hydroxy(6- UC)methyl-2-di-n-propylaminotetralin, an average of 100.3% was recovered in 67 hr: 77.2% in urine and 23.1% in feces. No excretion of UCO2 was observed. In bile duct-cannulated animals, an average of 31.6% of the dose was recovered in the bile within 6 hr. Highest concentrations of tissue radioactivity, 0.5 hr after ip injection of UC-DK-118, were found in lung, kidney, and liver. Only a small amount of unchanged DK-118 is excreted into urine and bile; HPLC radiochromatography separated five metabolites in urine and at least eight metabolites in bile. The three major metabolites in urine have been identified as 5-hydroxy-6-carboxy-2-di-n-propylaminotetralin, 5-hydroxy-6-carboxy-2-n-propylaminotetralin, and 5-hydroxy-6-methyl-2-n-propylaminotetralin-O-sulfate. The two major biliary metabolites have been identified as 5-hydroxy-6-carboxy-2-n-propylaminotetralin and an acid-labile conjugate of DK-118. Together, these 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.

Research Organization:
Univ. of Iowa, Iowa City
OSTI ID:
6085667
Journal Information:
Drug Metab. Dispos.; (United States), Journal Name: Drug Metab. Dispos.; (United States) Vol. 3; ISSN DMDSA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BILE
BIOLOGICAL MATERIALS
BIOLOGICAL WASTES
BODY
BODY FLUIDS
CARBON 14 COMPOUNDS
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON OXIDES
CARDIOTONICS
CARDIOVASCULAR AGENTS
CHALCOGENIDES
DIGESTIVE SYSTEM
DISTRIBUTION
DOPAMINE
DRUGS
FECES
GLANDS
HYDROCARBONS
HYDROXY COMPOUNDS
KIDNEYS
LABELLED COMPOUNDS
LIVER
LUNGS
MAMMALS
MATERIALS
METABOLISM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
OXIDES
OXYGEN COMPOUNDS
PHENOLS
POLYPHENOLS
RATS
RECEPTORS
RESPIRATORY SYSTEM
RODENTS
SYMPATHOMIMETICS
TETRALIN
TISSUE DISTRIBUTION
URINE
VERTEBRATES
WASTES