Bis(3-methylsulfonyloxypropyl)amine p-Toluenesulfonate(864-T)の正常ラットにおける吸収, 排泄, 体内分布および代謝

抄録

Absorption, excretion, distribution and metabolism of bis(3-methylsulfonyloxy-propyl)amine p-toluenesulfonate (864-T), a new alkylating agent, were investigated in normal rats using the tritium-labeled compound. Within 3 days after the oral or intraperitoneal administration of radioactive compound (³H-864-T), 80-90% of the given radioactivity (³H) was excreted in the urine and 1-10% in the feces. In addition, 4% of the given tritium was also recovered in the bile during 24 hr after the oral administration. The blood level of tritium reached the maximum at 2 hr after the oral administration, and then decreased at such a rate that the half-life time was 2 hr. The highest concentration of tritium was observed in the kidney, while relatively low lever were found in other tissues. There was no sign indicating that the given tritium was bound to the serum protein. Two kinds of metabolites were detected in the urine during 24 hr after the oral administration of ³H-864-T. These metabolites were isolated from the urine after the administration of non-labeled compound (864-T). One of them was found to be 2-oxotetrahydro-1, 3-oxazine-3-propanol and the other, 2-oxotetrahydro-1, 3-oxazine-3-propionic acid.