Accumulation of thiourylene antithyroid drugs in mouse salivary gland

[35S]Methimazole and [35S]propylthiouracil were shown to accumulate in mouse submandibular gland in vivo, with maximal tissue: plasma ratios being achieved at the lowest dose of drug studied (0.1 microgram/animal). Autoradiography of submandibular glands showed that the drugs were localized to the intralobular ductal epithelium and within the lumen of the convoluted granular tubule, which was identical to the localization of radiolabelled iodide. Histochemical studies indicated that this was the site of peroxidase activity within the gland. Drug accumulation persisted when iodide trapping was competitively inhibited using perchlorate. These data suggest that antithyroid drug accumulation by this tissue is not dependent on the anion trap; the localization of drug and iodide at the site of peroxidase activity suggest that this may be an important factor in the mechanism of drug accumulation, possibly related to subsequent drug metabolism.