Distribution and excretion of C14-labeled ABBOTT-16612 in experimental animals

Autor: Arthur Alter, Earl V. Cardinal, Ann Dalziel, Preston M. Bauman, Jonathan P. Miller
Rok vydání: 1966
Předmět:
Zdroj: Toxicology and Applied Pharmacology. 8:295-305
ISSN: 0041-008X
DOI: 10.1016/s0041-008x(66)80016-9
Popis: Summary The tissue distribution and excretion of C 14 -labeled ABBOTT-16612, a disubstituted piperazine with schistosomicidal activity, have been studied in the rat, mouse, dog, and monkey. The results of the rate of excretion and tissue distribution studies of C 14 -labeled ABBOTT-16612 or its metabolites do not explain the greater susceptibility of the dog, as opposed to the monkey, to the toxic effects of the drug. The highest concentration of C 14 in all species studied was found in the liver and bile of monkeys and dogs. Only 2–4% of the dose was excreted in the urine over a 4-day period. The gastrointestinal tract and its contents contained a high concentration of C 14 . The estimated biological half-life of C 14 -labeled ABBOTT-16612 after a single oral dose is approximately 5 hours in the mouse, 19 hours in the dog, and 53 hours in the monkey. The serum concentration curves in dogs and monkeys were biphasic, with a short-lived component with a half-life of 3–4 hours, and a longer-lived component with a half-life of 52–92 hours.
Databáze: OpenAIRE