Open AccessSTUDIES ON CAERULEIN (FI6934). ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF CAERULEIN
Author(s) -
Tomonobu Tokiwa,
Ieaki Uemura,
Hironori Murakami,
Sonoko Tsuruoka,
Masami Kaneko,
Kazuko Ogawa,
Tomoko Manzai
Publication year - 1975
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.25.747
Subject(s) - urine , metabolite , chemistry , metabolism , endocrinology , medicine , kidney , absorption (acoustics) , excretion , paper chromatography , pancreas , chromatography , biochemistry , biology , physics , acoustics
35S-Caerulein (35S-FI6934) was administered intramuscularly into rats (280 mug/kg), rabbits (380 mug/kg) and mice (3.3 mg/kg). Blood level of radioactivity in rats and rabbits reached the maximum at 5 and 15 min after administration, respectively, and then decreased rapidly. In both rats and rabbits, the radioactivities were excreted mainly into the urine. The physiological activity of FI6934 was detected in the blood of rats and rabbits collected within 15 and 30 min after injection respectively, and in the bile of rats collected within the first 2 hr. In rats, the radioactivities were densely distributed in kidney, liver, pancreas, and intestine. Four metabolites of 35S-FI6934 were isolated by paper chromatography from rat urine (i.m., 500 mug/kg). The main metabolites, F-I and F-II, were negative to nynhydrin and to the Ehrlich reagent and carried no physiological activity. 35S-Chym-I, which was prepared by digesting 35S-FI6934 with chymotrypsin, was injected to rats (i.m. 16 or 8 mg/kg/. The metabolite, C-I, isolated from the urine was considered to have a very similar structure to F-I from the results of paper chromatography and paper electrophoresis. By amino acid analysis, the structure of C-I was estimated to be as follows: Pyr-Gln (or Glu)-Asp-Tyr-Thr-Gly. (see article).