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Propylthiouracil


Mechanism of action:

Propylthiouracil is a thioamide derivative. Propylthiouracil inhibits thyroid peroxidase (TPO) within thyroid follicular cells, thereby blocking iodide oxidation (iodide → iodine), iodination of tyrosine residues, and the coupling reactions of iodotyrosines (MIT, DIT → T3, T4), leading to reduced de novo synthesis of T3 and T4. Propylthiouracil also inhibits 5'-deiodinase, reducing the conversion of T4 into the more physiologically active T3 in peripheral tissues such as the liver and kidneys.

Reference(s):

1. Sugawara M et al. (1999). Methimazole and propylthiouracil increase cellular thyroid peroxidase activity and thyroid peroxidase mRNA in cultured porcine thyroid follicles. Thyroid. 


2. Manzon RG et al. (2001). Variable effects of goitrogens in inducing precocious metamorphosis in sea lampreys (Petromyzon marinus). J Exp Zool. 


3. Ferreira AC et al. (2003). Thyroid Ca2+/NADPH-dependent H2O2 generation is partially inhibited by propylthiouracil and methimazole. Eur J Biochem.

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