Whole Body Autoradiographic Studies on the Distribution of ^3H-Labeled Penfluridol (^3H-TLP-607) in Mice and Rats

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The distribution of tritium-labeled Penfluridol (^3H-TLP-607), a potent and longacting neuroleptics, was studied in mice and rats by the whole body autoradiographic technique. In mice after intravenous administration the highest concentration of radioactivity was found in the lung, heart muscle, skeletal muscle, kidney and moderate in the central nervous system. In the brain the radioactivity in the cortices of the cerebrum and the cerebellum was higher than in the white matter, and a fair amount of radioactivity was observed also in the hippocampus. In the case of oral administration the highest radioactivity in various organs was observed 2 to 8 hours after the administration. In these periods the highest concentration was found in the lung, kidney and spleen, next to these in the thyroid and blood, and moderate in the central nervous system and sexual organs. In pregnant mice after oral administration, ^3H-TLP-607 and its radioactive metabolites passed through the placenta into the fetuses, but the concentration in the fetuses was lower than in the mother. In rats the distribution pattern after oral administration was similar to that in mice ; highest in the lung, kidney, spleen and moderate in the central nervous system. The distribution in the rat brain also resembled that in the mouse brain, but the uptake into the hippocampus was observed more remarkably. In female rats high radioactivity was found in the ovary, low in the mammary gland in earlier periods, and vice versa 16 hours later.
公益社団法人日本薬学会の論文
1974-09-25

Whole Body Autoradiographic Studies on the Distribution of ^3H-Labeled Penfluridol (^3H-TLP-607) in Mice and Rats

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