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Sites of Action of 2-Thiazoline-2-Thiol on Biogenesis of Thyroid Hormones

机译:2-噻唑啉-2-硫醇对甲状腺激素生物发生的作用位点

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References(15) Cited-By(10) 2-Thiazoline-2-thiol is an antithyroid agent that strongly reduces thyroid hormone levels. Synthesis of these hormones is catalyzed in vivo by thyroid peroxidase. The interaction of this drug with molecular iodine and its effect on peroxidase activity were investigated. Iodine and 2-thiazoline-2-thiol form a complex of the charge transfer type of 1:1 stoichiometry characterized by a formation constant of 2, 5271·mole-1 at 20°C. This drug was found to inhibit both horseradish peroxidase and lactoperoxidase (used as a model of thyroid peroxidase) in a competitive manner, giving inhibition constants of 5.7 mM and 0.13 mM, respectively. T3 and T4 levels were reduced significantly after a three-week administration of this drug to a group of 10 rats. Histological examination of the thyroid gland showed the presence of a cylindrical epithelium, which is indicative of hyperactivity of the gland. The results indicated that 2-thiazoline-2-thiol acts on both molecular iodine and thyroid peroxidase.
机译:参考文献(15)Cited-By(10)2-Thiazoline-2-thiol是一种抗甲状腺药,可强烈降低甲状腺激素水平。这些激素的合成在体内被甲状腺过氧化物酶催化。研究了该药物与分子碘的相互作用及其对过氧化物酶活性的影响。碘和2-噻唑啉-2-硫醇形成电荷转移型化学计量比为1:1的络合物,其特征在于在20°C下的形成常数为2、5271·mole-1。发现该药物以竞争性方式抑制辣根过氧化物酶和乳过氧化物酶(用作甲状腺过氧化物酶的模型),抑制常数分别为5.7 mM和0.13 mM。在一组10只大鼠中服用该药物3周后,T3和T4水平显着降低。甲状腺的组织学检查显示圆柱形上皮的存在,这表明该腺过度活跃。结果表明2-噻唑啉-2-硫醇同时作用于分子碘和甲状腺过氧化物酶。

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