Tracazolate metabolites in rat tissue.

Tracazolate (4-n-butylamino-1-ethyl-6-methyl-1H-pyrazolo[3,4-b] pyridine-5-carboxylic acid ethyl ester) undergoes extensive biotransformation to lipophilic metabolites following oral dosage to male rats. Twenty-one metabolites were identified in a plasma hexane extract by mass spectrometry. Coadministration of unlabeled tracazolate with its stable carbon-13 isotope expedited the isolation and identification of 11 biotransformation products.

Metabolism, disposition, and pharmacokinetics of tracazolate in rat and dog.

The metabolism, disposition, and pharmacokinetics of tracazolate, (4-butylamino-1-ethyl-6-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl ester), a novel anxiolytic agent, were studied in rat and dog following single oral and iv doses. Although tracazolate exhibits very good absorption (greater than 80%) in both species, it is extensively metabolized, accounting for low bioavailability. Excretion of 14C was rapid, with the kidney being the major organ of excretion.

Determination of ethinyl estradiol in human urine by radiochemical GLC.

A radiochemical GLC analysis was developed for 3H-labeled ethinyl estradiol in human urine. The technique was applied to the unconjugated and aglycone fractions of urine collected from women who were dosed orally with: (a) single capsules containing 2.0 mg of 3H-quinestrol (900 muCi) and 2.

Radiochemical GLC assay for nortriptyline in human plasma.

A novel method was developed for the assay of nortriptyline in plasma. After nortriptyline was extracted, it was acetylated with 3H-acetic anhydride; the quantity of 3H-acetylnortriptyline in the extract was determined by radiochemical GLC. The method is capable of assaying 5 ng of nortriptyline/ml of plasma.

Assay of human plasma for nortriptyline by radioacetylation and thin-layer chromatography.

A highly specific and sensitive thin-layer chromatographic method for determining nortriptyline levels in plasma is presented. The procedure involves extracting nortriptyline, acetylating it with radioactive acetic anhydride, resolving acetylnortriptyline by thin-layer chromatography, and measuring its radioactivity.