o-Chloro-α-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride(C-78)の生体内運命-2-ラットにおける代謝物  [in Japanese] The Metabolic Fate of ο-Chloro-α-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride (C-78). II. Metabolic Products in the Rat  [in Japanese]

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Author(s)

Abstract

The metabolic fate of ο-chloro-α-(tert-butylaminomethyl)-benzyl alcohol hydrochloride (C-78) in the rat was studied by oral administration of 14C-C-78, and the bronchodilating activities of the metabolites were also examined. The major metabolites in the urine, bile, and feces were unchanged C-78 (I) and 4-hydroxy- (II), 3-hydroxy- (III), and 4-hydroxy-5-methoxy-C-78 (IV), and their corresponding conjugates. As the minor metabolites, ο-chlorobenzoic acid, ο-chloromandelic acid, and 1-(ο-Chlorophenyl)-1, 2-ethanediol were detected by gas chromatography. These results suggested that the major metabolic pathway of C-78 in the rat is hydroxylation of the benzene ring. Although IV had no activity, II had a stronger bronchodilating activity than C-78, and III was as effective as C-78, suggesting the participation of the metabolites in the bronchodilating action and durability of C-78.

Journal

  • Journal of the Pharmaceutical Society of Japan

    Journal of the Pharmaceutical Society of Japan 97(3), p244-250, 1977-03

    The Pharmaceutical Society of Japan

Cited by:  1

Codes

  • NII Article ID (NAID)
    110003652519
  • NII NACSIS-CAT ID (NCID)
    AN00284903
  • Text Lang
    JPN
  • Article Type
    Journal Article
  • ISSN
    00316903
  • NDL Article ID
    1819059
  • NDL Source Classification
    SD0(薬学)
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z19-411
  • Data Source
    CJPref  NDL  NII-ELS  IR 
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