Abstract

Female white rats were dosed orally with pentylenetetrazol-10-14C. Total radioactivity in different tissues was determined at five times after dosing. The kidney and liver showed slightly higher levels of radioactivity than did the blood and other tissues analyzed. During the first 24 hr., approximately 73% of the administered 14C was recovered in the urine; less than 1% was recovered in the feces. TLC of urine followed by autoradiography showed the presence of pentylenetetrazol-10-14C and at least five radioactive metabolites. Acetone extracts of the blood were chromatographed and were found to contain pentylenetetrazol-10-14C and four of the five labeled metabolites detected in the urine. TLC of urine collected from humans dosed orally with pentylenetetrazol-10-14C showed the presence of pentylenetetrazol-10-14C and at least four radioactive metabolites. The metabolites in human urine occurred at the same Rf positions as the labeled metabolites of rat urine when cochromatographed, indicating possible similar metabolism by rats and humans.

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