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Uniformly ring-labeled 14C o-chlorotoluene was administered by gavage to rats at a dose of 320 mg/kg bw. Expired air, urine and faeces were examined for metabolites.

The recovery of radioactivity at 48 h averaged 11% in the expired air, 81% in urine, and 4% in feces; radioactivity in expired air was identified as unchanged o-chlorotoluene; urinary metabolites (as % of dose) were: o-chlorohippuric acid (16- 20%), a mercapturic acid conjugate of o-chlorotoluene (20- 24%) and polar metabolites (36-43%); enzymatic hydrolysis of rat urine indicated that the polar metabolites included the glucuronide conjugate of the phenolic hydroxylation product of o-chlorotoluene; unchanged o-chlorotoluene was not present in urine or feces of treated rats.

When male and female Sprague-Dawley rats were given a single oral dose of o-chlorotoluene at 1 mg/kg bw by gavage, 85 - 92% of the applied dose was eliminated in urine, 5 - 8% was excreted in feces and 1 - 4% of the applied dose was exhaled as volatile 14C; at least 84% of the volatile 14C was identified as unmetabolized o-chlorotoluene whereas 14C-carbon dioxide was an insignificant metabolite (< 1% applied dose).
A similar distribution of radioactivity was also seen in female rats given single oral doses of 91 or 102 mg/kg bw. The major urinary and fecal metabolites were o-chlorohippurate, a beta-glucuronide of o-chlorobenzyl alcohol and mercapturic acid; no significant sex-related metabolic differences were noticed between males and females and the same qualitative and quantitative distribution of metabolites was found for doses of 1-102 mg/kg bw.
O-chlorotoluene is quickly absorbed from the gastrointestinal tract into blood as evidenced by exhalation of o-chlorotoluene and the rapid peak in 14C residues at ca. 2 h in blood plasma. Analysis of the 14C residues in plasma showed that the two major radioactive components were mercapturic acid and the beta-glucuronide of o-chlorobenzyl alcohol (38 and 25% of plasma 14C, respectively), while trace levels of o-chlorotoluene, o-chlorobenzoic acid, o-chlorobenzyl alcohol and o-chlorohippurate were detectable also; virtually all of the administered o-chlorotoluene was eliminated within 4 d with < 1% remaining in the carcass.