丙硫氧嘧啶抑制L-甲状腺素转化为L-三碘甲状腺原氨酸。对丙硫氧嘧啶的抗甲状腺素作用的解释以及支持三碘甲状腺原氨酸是活性甲状腺激素这一概念的证据。
Propylthiouracil inhibits the conversion of L-thyroxine to L-triiodothyronine. An explanation of the antithyroxine effect of propylthiouracil and evidence supporting the concept that triiodothyronine is the active thyroid hormone.
作者信息
Oppenheimer J H, Schwartz H L, Surks M I
出版信息
J Clin Invest. 1972 Sep;51(9):2493-7. doi: 10.1172/JCI107063.
Abstract
6-n-propylthiouracil (PTU) administered to male Sprague-Dawley rats maintained on 2 and 5 mug L-thyroxine (T(4))/100 g body weight resulted in a marked reduction in the rate of conversion of L-thyroxine to L-triiodothyronine (T(3)). These effects could not be ascribed to induced hypothyroidism since the group maintained on 5 mug T(4)/day had normal levels of liver mitochondrial alpha glycerophosphate dehydrogenase. In confirmation of previous studies, PTU also reduced the fractional rate of deiodination of T(3). These observations provide a possible explanation of the many published observations indicating that PTU antagonizes the tissue effects of T(4) but not of T(3). The data suggest that monodeiodination of T(4) but not of T(3) is essential before hormonal effects can be manifested at the cellular level.
摘要
给体重100克、每日维持摄入2微克和5微克L-甲状腺素（T4）的雄性斯普拉格-道利大鼠施用6-正丙基硫氧嘧啶（PTU），会导致L-甲状腺素向L-三碘甲状腺原氨酸（T3）的转化率显著降低。这些作用不能归因于诱发的甲状腺功能减退，因为每日维持摄入5微克T4的组肝脏线粒体α甘油磷酸脱氢酶水平正常。正如之前研究所证实的，PTU也降低了T3的脱碘分数率。这些观察结果为许多已发表的观察结果提供了一种可能的解释，这些观察结果表明PTU拮抗T4而非T3的组织效应。数据表明，在细胞水平上表现出激素效应之前，T4而非T3的单脱碘是必不可少的。
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Propylthiouracil inhibits the conversion of L-thyroxine to L-triiodothyronine. An explanation of the antithyroxine effect of propylthiouracil and evidence supporting the concept that triiodothyronine is the active thyroid hormone.丙硫氧嘧啶抑制L-甲状腺素转化为L-三碘甲状腺原氨酸。对丙硫氧嘧啶的抗甲状腺素作用的解释以及支持三碘甲状腺原氨酸是活性甲状腺激素这一概念的证据。
J Clin Invest. 1972 Sep;51(9):2493-7. doi: 10.1172/JCI107063.
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Correlation of serum triiodothyronine (T3) and thyroxine (T4) with biologic effects of thyroid hormone replacement in propylthiouracil-treated rats.丙硫氧嘧啶治疗大鼠血清三碘甲状腺原氨酸（T3）和甲状腺素（T4）与甲状腺激素替代生物效应的相关性
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Metabolic effects of thyroxine injected into normal, thiouracil-treated and thyroidectomized rats.向正常、经硫脲处理及甲状腺切除的大鼠注射甲状腺素后的代谢效应。
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The identification of 3:5:3'-L-triiodothyronine in human plasma.人血浆中3:5:3'-L-三碘甲状腺原氨酸的鉴定。
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ALPHA-GLYCEROPHOSPHATE DEHYDROGENASE RESPONSE TO THYROXINE IN THYROIDECTOMIZED, THIOURACIL-FED AND TEMPERATURE-ADAPTED RATS.甲状腺切除、服用硫脲嘧啶及温度适应大鼠中α-甘油磷酸脱氢酶对甲状腺素的反应
Endocrinology. 1964 Dec;75:908-16. doi: 10.1210/endo-75-6-908.
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Effects of propylthiouracil and thiouracil on the metabolism of thyroxine and several of its derivatives by rat kidney slices in vitro.丙硫氧嘧啶和硫氧嘧啶对大鼠肾切片体外代谢甲状腺素及其几种衍生物的影响。
Endocrinology. 1962 Nov;71:701-12. doi: 10.1210/endo-71-5-701.
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The effects of triiodo-L-thyronine and L-thyroxine on the oxygen consumption and body weights of rats fed on a diet containing 0.05 percent propylthiouracil.三碘-L-甲状腺原氨酸和L-甲状腺素对喂食含0.05%丙基硫氧嘧啶饮食的大鼠耗氧量和体重的影响。
J Endocrinol. 1963 Mar;26:55-63. doi: 10.1677/joe.0.0260055.
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Interference with deiodination of some thyroxine analogues in the rat.对大鼠体内某些甲状腺素类似物脱碘作用的干扰。
Endocrinology. 1961 Dec;69:1085-7. doi: 10.1210/endo-69-6-1085.
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