title: Metabolism of amosulalol hydrochloride in man: quantitative comparison with laboratory animals.
abstract: The metabolism of amosulalol hydrochloride, (+/-)-5-[1-hydroxy-2-[[2-(o-methoxyphenoxy)ethyl]amino]ethyl]-2- methylbenzenesulphonamide hydrochloride, was studied in man and laboratory animals. Humans excreted 30.1% of dose as unchanged drug, and the sulphate conjugate of a 5-hydroxy metabolite, (+/-)-5-[1-hydroxy-2-[[2-(5-hydroxy-2-methoxyphenoxy)ethyl]-amino] ethyl]-2-methylbenzenesulphonamide, was the major metabolite. Amosulalol hydrochloride was extensively metabolized in animals with 10% or less excreted as unchanged drug. Hydroxylation of the 2-methyl group and O-demethylation of the o-methoxyphenoxy group were preferred in rats, and oxidative C-N cleavage yielding o-methoxyphenoxyacetic acid (M-5) preceded other reactions in dogs. Monkeys excreted almost equal amounts of the 5-hydroxy and 4-hydroxy metabolites as well as M-5.
mesh_terms: D000818:Animals; D001711:Biotransformation; D004285:Dogs / Q000652:urine*; D004983:Ethanolamines / Q000378:metabolism*; D000882:Haplorhini / Q000652:urine*; D006801:Humans; D006900:Hydroxylation; D007700:Kinetics; D051381:Rats / Q000652:urine*; D013045:Species Specificity; D000096926:Benzenesulfonamides
chemical_list: D004983:Ethanolamines; C032473:amosulalol; D000096926:Benzenesulfonamides