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6-Mercaptopurine: total body autoradiograms and plasma concentration-time curves of 6MP and metabolites from marmoset monkeys

6-Mercaptopurine: total body autoradiograms and plasma concentration-time curves of 6MP and metabolites from marmoset monkeys. Schouten, T. J.; De Abreu, R. A.; Schretlen, E. D. A. M.; De Vaan, G. A. M.; Van der Kleijn, E. (Cent. Pediatr. Oncol. S.E., Univ. Hosp. Sint Radboud, Nijmegen 6500 HB, Neth.). Pediatr. Hematol. Oncol., 3(2), 159-65 (English) 1986. CODEN: PHONEN. ISSN: 0888-0018. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) To study the body distribution of 6-mercaptopurine (6MP) [50-44-2], [8-14C]6MP was given by infusion to 2 marmoset monkeys at a dose rate of 5 mg/kg body wt./h for 1 and 4 h, resp. Both exptl. animals were sacrificed 2 h after the end of the drug infusion and instantly frozen at -70°. Whole body sagittal sections were made later. Blood samples were obtained regularly during the expts. to quantitate 6MP, 6MP riboside (6MPR) [574-25-4], 6-thioxanthine [2002-59-7], and 6-thiouric acid [2002-60-0] in plasma. The autoradiograms revealed extensive distribution of the 14C label. High levels of radioactivity were seen in liver, bile, and intestinal contents. Labeling of the central nervous system and bone marrow was obvious. The plasma concn.-time curves of 6MP and 6MPR attained steady-state concns. of 30-40 mM and 6-12 mM, resp. After stopping the infusion of the drug, the concns. of 6MP and 6MPR became equal. 6MPR contributes to the biol. effect of 6MP, as degrdn. of 6MPR results in 6MP. In studies on the pharmacokinetics and dynamics one should try to include all relevant metabolites of 6MP, both in plasma and in the cells.

2-Hydroxy-6-mercaptopurine

2-Hydroxy-6-mercaptopurine. Enoki, Kichiji; Genda, Yoshikazu; Hinoki, Yoshiaki (Nippon Soda Co., Ltd., Japan). Japan. Kokai JP 51076294 1 Jul 1976 Showa, 3 pp.Some commonly used reagents like 2002-59-7 and 59397-68-1 are used in this experiment. (Japanese). (Japan). CODEN: JKXXAF. CLASS: IC: C07D473-22. APPLICATION: JP 75-3162 26 Dec 1974. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) 2-Hydroxy-6-mercaptopurine (I) was prepd. by heating 4(5)-thiocarbamoylimidazole-5(4)-carbamic acid esters in org. solvents. Thus, 5 g Me 4(5)-thiocarbamoylimidazole-5(4)-carbamate in DMF was stirred 2 hr at 140-50.degree. to give 93% I. .