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  • 3-aminotetralins  (1)
  • Catechol-O-methyl transferase  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 326 (1984), S. 203-209 
    ISSN: 1432-1912
    Keywords: Dopamine analogues ; Catechol-O-methyl transferase ; Brain concentrations ; Partition coefficients ; N,N-dipropyldopamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Concentrations of dopamine (DA) analogues were determined in rat brain regions and serum after peripheral administration of the drugs. The time course of the concentrations of four N,N-dialkylated DA derivatives is reported in relation to the simultaneously measured effects on DA metabolism. Maximum brain concentrations were reached at about 10 min after injection, followed by a rapid elimination of the parent compounds. O-Methylation was found to be of major importance in this early disappearance. The 3-O-methyl metabolite of N,N-dipropyl-DA (DiPr-DA) was very rapidly formed and was eliminated much more slowly than the parent compound. Inhibition of O-methylation as well as subcutaneous, instead of intraperitoneal (ip), administration resulted in higher brain and serum levels of DiPr-DA. Brain concentrations of 11 DA analogues were determined 10 min after ip injection and were compared with their octanol/water (pH 7.4) partition coefficients. Within one group of compounds with a similar metabolic profile the brain concentrations and partition coefficients showed a good correlation.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-5044
    Keywords: 3-aminotetralins ; bioconversions ; catechols ; entrapped plant cells ; mass spectrometry ; Mucuna pruriens L.
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Although alginate-entrapped cells of Mucuna pruriens L. possess a low substrate specificity, only para-substituted monocyclic phenols have been ortho-hydroxylated into catechols so far. In this study, compounds with more complex chemical structures were found to be substrates using entrapped cells of M. pruriens as well as the partially purified Mucuna-phenoloxidase. Thus, 5-, 6- and 7-hydroxylated 2-aminotetralins and a tricyclic compound, 9-hydroxy N-n-propyl hexahydronaphthoxazine, were converted into catechols. After isolation using preparative HPLC, the identity of the products was confirmed by MS. In general, for the entrapped cells and the enzyme preparation identical substrate specificities were found.
    Type of Medium: Electronic Resource
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