ο-Chloro-α-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride(C-78)の生体内運命(第2報<SUP>1)</SUP>)ラットにおける代謝物

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タイトル別名
  • The Metabolic Fate of ο-Chloro-α-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride (C-78). II. Metabolic Products in the Rat
  • 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
  • o Chloro アルファ tert butylaminomethyl ben
  • The Metabolic Fate of &omicron;-Chloro-&alpha;-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride (C-78). II. Metabolic Products in the Rat
  • The metabolic fate of o-chloro-o'-(tert.-butylaminomethyl)-benzyl alcohol hydrochloride (C-78). II.

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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.

収録刊行物

  • 薬学雑誌

    薬学雑誌 97 (3), 244-250, 1977

    公益社団法人 日本薬学会

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