Absorption, metabolism, and excretion studies of carbon 14- and tritium-labeled derivatives of a ketomethylene containing tripeptide.
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 absorbed 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.
Almquist
R G
RG
Steeger
T
T
Jackson
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S
Mitoma
C
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D000806:Angiotensin-Converting Enzyme Inhibitors; D000818:Animals; D001646:Bile / Q000378:metabolism; D002250:Carbon Radioisotopes; D004151:Dipeptides / Q000378:metabolism*; D006207:Half-Life; D008297:Male; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D014316:Tritium
D000806:Angiotensin-Converting Enzyme Inhibitors; D002250:Carbon Radioisotopes; D004151:Dipeptides; D014316:Tritium; C028342:compound 20