Document Detail

The mechanism of action of synthetic antithyroid drugs: iodine complexation during oxidation of iodide.
MedLine Citation:
PMID:  1689656     Owner:  NLM     Status:  MEDLINE    
A number of compounds of pharmaceutical importance from a variety of chemical families, including thiocyanates, isothiocyanates, thiourea and derivatives, imidazoles, and various amines, were found to form charge transfer complexes with iodine. Parallel studies were carried out to investigate the actions of these drugs on lactoperoxidase and thyroid activity in vivo in the rat (assays of T3 and T4 and histology of the thyroid gland). The results showed that there was a good correlation between the value of Kc (the formation constant of the iodinated complex) and antithyroid activity in vivo. The higher the electron donor power of the compound, the higher the Kc value and the stronger the action on the thyroid. The results indicated that a number of drugs could have secondary antithyroid activity. Some compounds, such as levamisole, tetramethylthiourea, tetrahydrozoline, phenothiazines, and imipramines, with no action on peroxidase had high Kc values (tetramethylthiourea, 13,825 liters/M) and had strong antithyroid activity in the rat. These results suggest that synthetic antithyroid agents may act either on peroxidase and/or the molecular iodine which may be produced by oxidation of iodides (2I(-)----I2----2I+). It has been shown that oxidation of I- can occur in the absence of thyroglobulin. In the absence of a suitable receptor, significant amounts of I2 may, thus, accumulate. The action of such drugs on molecular iodine may have considerable pharmacological significance.
C Raby; J F Lagorce; A C Jambut-Absil; J Buxeraud; G Catanzano
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Endocrinology     Volume:  126     ISSN:  0013-7227     ISO Abbreviation:  Endocrinology     Publication Date:  1990 Mar 
Date Detail:
Created Date:  1990-04-05     Completed Date:  1990-04-05     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0375040     Medline TA:  Endocrinology     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1683-91     Citation Subset:  AIM; IM    
Department of Chemical Pharmacy, Faculty of Pharmacy, Limoges, France.
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MeSH Terms
Antithyroid Agents / chemical synthesis,  metabolism,  pharmacology*
Chemical Phenomena
Enzyme Activation
Iodides / metabolism*
Iodine / metabolism*
Lactoperoxidase / metabolism
Thiourea / analogs & derivatives,  pharmacology
Thyroxine / blood
Triiodothyronine / blood
Ultraviolet Rays
Reg. No./Substance:
0/Antithyroid Agents; 0/Iodides; 2782-91-4/tetramethylthiourea; 62-56-6/Thiourea; 6893-02-3/Triiodothyronine; 7488-70-2/Thyroxine; 7553-56-2/Iodine; EC 1.11.1.-/Lactoperoxidase

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