Product Details of 61-82-5. In 2020.0 XENOBIOTICA published article about THYROPEROXIDASE INHIBITION; MECHANISM in [Price, Roger J.; Lake, Brian G.] Univ Surrey, Fac Hlth & Med Sci, Guildford GU2 7XH, Surrey, England; [Burch, Rachel] Brunel Univ, Res Support & Dev Off, Uxbridge, Middx, England; [Chatham, Lynsey R.; Higgins, Larry G.] CXR Biosci Ltd, Concept Life Sci, Dundee, Scotland; [Currie, Richard A.] Syngenta Ltd, Jealotts Hill Int Res Ctr, Bracknell, Berks, England in 2020.0, Cited 16.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
1. A number of chemicals have been shown to produce disruption of the thyroid gland, resulting in reduced thyroid hormone synthesis, by a mechanism involving inhibition of thyroid peroxidase (TPO) activity (EC 1.11.1.8). 2. An assay was developed for rat thyroid gland microsomal TPO activity, employing L-tyrosine as the physiological substrate, with analysis of the formation of the 3-iodo-L-tyrosine (3MIT) metabolite by ultra-performance liquid chromatography-mass spectrometry-mass spectrometry. 3. Formation of 3MIT was linear with respect to both rat thyroid gland microsomal protein concentration and incubation time, whereas only small quantities of 3,5-diodo-L-tyrosine were formed. 4. Studies were performed with nine known TPO inhibitors. The most potent inhibitors were 3-amino-1,2,4-triazole, ethylene thiourea, methimazole and 6-propyl-2-thiouracil which had IC50 values (i.e. concentration to produce a 50% inhibition of enzyme activity) of 0.059, 0.791, 1.07 and 1.96 mu M, respectively, whereas the least potent inhibitor was sodium perchlorate which had an IC50 value of 13,800 mu M. 5. For five inhibitors, where literature data were available, the observed IC50 values obtained in this study employing rat thyroid gland microsomes and L-tyrosine as substrate were similar to those previously reported using the spectrophotometric guaiacol oxidation assay.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics