The disposition, tissue distribution, and cellular transport of N-[[(trimethylamino)boryl]carbonyl]-L-phenylalanine methyl ester in CF1 mice.
The disposition and tissue distribution of 14C-labeled N-[[(trimethylamino)boryl]carbonyl]-L-phenylalanine methyl esther (1) determined in CF1 mice following i.v., p.o., and i.p. administration. Compound 1 was found to undergo rapid and extensive metabolism, and the majority of the radioactivity was found in the skin and carcass regardless of the route of administration. Approximately 55% of the radioactivity was recovered in urine and feces after 78 h; however, excretion via these routes was not complete. Degradation of compound 1 occurred at the amide bond at low pH (0.8) but at the ester bond a physiological pH. This difference in degradation was reflected in elevation of the blood radioactivity levels after p.o. administration compared to i.p. and i.v. administration.
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D001711:Biotransformation; D001896:Boron Compounds / Q000493:pharmacokinetics*; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D004912:Erythrocytes / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D001896:Boron Compounds; C097136:N-(((trimethylamino)boryl)carbonyl)phenylalanine methyl ester; D010649:Phenylalanine