Absorption, metabolism, and excretion studies of carbon 14- and tritium-labeled derivatives of a ketomethylene containing tripeptide

Journal Article · Mon Jul 29 00:00:00 EDT 1985 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(85)90499-0· OSTI ID:5520823

Almquist, R G; Steeger, T; Jackson, S; Mitoma, C

Tritium and Carbon 14 analogs of the angiotensin converting enzyme inhibitor ketoACE were synthesized and their oral absorption, metabolism and excretion in rats were investigated. KetoACE, a ketomethylene analog of the tripeptide Bz-Phe-Gly-Pro, was slowly adsorbed at a 35% level upon oral administration. It is rapidly eliminated from the blood with a half-life of about 10 minutes. Its excretion is primarily via the bile duct and it is excreted as 80% unchanged drug. The only identified metabolite consisting of 5-10% of the excreted radioactivity was determined to be the reduced ketoACE in which the ketone group was reduced to a hydroxyl. 5 references, 2 figures, 4 tables.

• Research Organization: SRI International, Menlo Park, CA
• OSTI ID: 5520823
• Journal Information: Life Sci.; (United States), Vol. 37:4
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PEPTIDES
METABOLISM
ABSORPTION
BIOLOGICAL HALF-LIFE
BLOOD-PLASMA CLEARANCE
CARBON 14 COMPOUNDS
EXCRETION
METABOLITES
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
CLEARANCE
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
ORGANIC COMPOUNDS
PROTEINS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques