Metabolism of 1-(3-trifluoromethylphenyl)-3-(2-hydroxyethyl) quinazoline-2,4(1H,3H)-dione (H-88). I. Species differences in metabolism.
1. Following oral administration of [14C] H-88 to rat, mouse, quinea-pig and hamster, 40-65% and 5-15% of radioactivity was excreted in urine and faeces respectively during 3 or 4 days. In rabbit, monkey and man, more than 80% of radioactivity was excreted in urine during 2 or 3 days, and faecal excretion was negligible. 2. Rabbit, rat or guinea-pig excreted non-labelled H-88 in urine as unchanged H-88 (M-I), 1-(3-trifluoromethylphenyl) quinazoline-2,4(1H,3H)-dione-3-acetic acid (M-II), H-88 glucuronide (M-III) and 1-(3-trifluoromethylphenyl)-3-(2-hydroxyethyl)-6-hydroxyguinazoline-2,4(1H,3H)-dione (M-IV). 3. The carboxylic acid (M-II) was the major metabolite of H-88 in rat, mouse, guinea-pig and hamster urine and faeces, while the major metabolite in urine of rabbit, monkey and man was H-88 glucuronide (M-III). The 6-hydroxy compound (M-IV) was a major metabolite only in guinea-pig.
D000284:Administration, Oral; D000700:Analgesics / Q000378:metabolism* / Q000652:urine; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000378:metabolism* / Q000652:urine; D055598:Chemical Phenomena; D002621:Chemistry; D002855:Chromatography, Thin Layer; D006224:Cricetinae; D005243:Feces / Q000032:analysis; D006168:Guinea Pigs; D006801:Humans; D008252:Macaca fascicularis; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D011799:Quinazolines / Q000378:metabolism*; D011817:Rabbits; D051381:Rats; D013045:Species Specificity
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011799:Quinazolines; C009027:H-88