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1. The metabolism of a new schistosomicide, 2-isopropylaminomethyl-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline, was investigated in the mouse, rat, rabbit and rhesus monkey.2. All the species studied converted the compound to its 6-hydroxymethyl analogue, which showed greater schistosomicidal activity in vivo than the parent drug.3. Several other metabolites were also produced by oxidation at the 2- and/or 6-positions to give carboxylic acid derivatives. None of these metabolites showed biological activity.4. A species difference was apparent, since the 2-carboxylic acid metabolite was not detected in the urine or bile of the rat.

1. 5,7-Dinitroindazole was extensively metabolized in both rats and mice. The principal biotransformations were nitro group reduction and aromatic hydroxylation.2. Selective reduction of the 7-nitro group to yield the 7-amino derivative occurred in both species in vivo. The same specificity of reduction was evident when dinitroindazole was incubated with a mixed culture of rat faecal microorganisms.3. A species difference in conjugation was found. In the mouse the major urinary excretion product was the N-glucuronide of the 7-amino derivative but this was not found in rat urine, acetylation of the 7-amino group being the preferred biosynthetic reaction.4. This 7-acetamido derivative is the probable precursor of two other metabolites in the rat. One of these has been identified as 3-hydroxy-5-nitro-7-acetamidoindazole and the other may be an N-hydroxylated derivative.