Синтез метаболитов бета2-агонистов 2-(4-амино-3,5-дихлорфенил)-2-(алкиламино)этанолов и их выведение с мочой в сравнении с исходными соединениями

Metabolites of β2-agonists of 2-(4-amino-3,5-dichlorophenyl)-2-(alkylamino)ethanols, derivatives of hippuric and mandelic acids, have been synthesized. In experiments on laboratory animals, the excretion profile of target compounds and metabolites with urine was studied. After single oral administration of drugs in doses of 270 and 540 mg/kg, 9.7% of 2-(4-amino-3,5-dichlorophenyl)-2-(isopropylamino)ethanol and 0,7 % of 2-(4-amino-3,5-dichlorophenyl)-2-( tert -amylamino)ethanol from the administered dose were isolated in unchanged form. The times for determination of target components and metabolites in the urine of laboratory animals at the method sensitivity of 0.1 ng/mL has been established: 2-(4-amino-3,5-dichlorophenyl)-2-(isopropylamino)ethanol is identified for more than 120 h after drug taking and 2-(4-amino-3,5-dichlorophenyl)-2-( tert -amylamino)ethanol is identified for 96 h. Metabolite of 2-(4-amino-3,5-dichlorophenyl)-2-( tert -amylamino)ethanol (derivative of hippuric acid) is detected in urine longer than the initial compound – for more than 120 h.