The Metabolic Fate of ο-Chloro-α-(tert-butylaminomethyl)-benzyl Alcohol Hydrochloride (C-78). II. Metabolic Products in the Rat

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Abstract
The metabolic fate of o-choloro-.alpha.-(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 and 4-hydroxy-(II), 3-hydroxy-(III) and 4-hydroxy-5-methoxy-C-78 (IV), and their corresponding conjugates. As the minor metabolites, o-chlorobenzoic acid, o-chloromandelic acid and 1-(o-chlorophenyl)-1,2-ethanediol were detected by gas chromatography. The major metabolic pathway of C-78 in the rat was probably 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.

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