Pharmacokinetic investigation on the dehydrodipeptide N-[2-acetylamino-3-(2-thienyl)-2-propenoyl]-tyrosine in the rat.
The dehydrodipeptide N-[2-Acetylamino-3-(2-thienyl)-2-propenoyl]-tyrosine (1) is eliminated from the plasma of the rat after i.v. application with a half-life of 12.3 min, 58.1% via the kidneys (2/3 as the free 1, 1/3 as the glucuronide), 2.8% in the faeces. After oral application, the plasma concentration of 1 is very low and 2% and 53.6% are excreted in the urine and faeces, respectively. In both cases, elimination occurs during the first day after application. Three unidentified metabolites are found in the urine. Degradation of the molecule to tyrosine does not occur as the plasma and urine levels of tyrosine are not increased. The renal elimination following either a single or repeated (90X) oral application is the proportion of the glucuronide derivative. A 50% absorption was calculated on the basis of measurements of residual amounts in the gastrointestinal tract. Fluorimetric determinations were done after TLC separation of the extracts, the analysis of the faeces was done fluorimetrically by derivatisation to the methyl ester of 1.
D000818:Animals; D004151:Dipeptides / Q000378:metabolism*; D005260:Female; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D051381:Rats; D014018:Tissue Distribution
D004151:Dipeptides; C019235:acetyldehydro-3-(2-thienyl)alanyltyrosine