Westgren U, Melander A, Wåhlin E, Lindgren J
Acta Endocrinol (Copenh). 1977 Jun;85(2):345-50. doi: 10.1530/acta.0.0850345.
The effect of 6-propylthiouracil (PTU) on the peripheral conversion of thyroxine (T4) to 3,5,3'-triiodothyronine (T3) and 3,3',5'-triiodothyronine (reverse T3 rT3) was investigated by assessments of the concentrations of T4 T3 and rT3 in peripheral venous blood from T4-treated healthy volunteers given PTU, 4 X 150 mg daily. Within on day of PTU administration, serum T3 concentrations were reduced, and those of rT3 enhanced. These deviations lasted as long as PTU was given (five days), and there was a rapid return towards normal within one day after PTU administration ceased. It seems probable that, in man, PTU can evoke a diversion of T4 monodeiodination, less being converted to the metabolically active T3 and more to the metabolically inactive rT3. It is ppossible that the rapidity whereby PTU can reduce T3 levels can offer an advantage in the treatment of hyperthyroidism.
通过对接受甲状腺素(T4)治疗的健康志愿者外周静脉血中T4、三碘甲状腺原氨酸(T3)和反三碘甲状腺原氨酸(rT3)浓度的评估,研究了6-丙基硫氧嘧啶(PTU)对T4在外周转化为T3以及3,3',5'-三碘甲状腺原氨酸(反T3,rT3)的影响。这些健康志愿者每天服用4次,每次150毫克PTU。在服用PTU的当天,血清T3浓度降低,rT3浓度升高。只要服用PTU(五天),这些偏差就会持续存在,并且在停止服用PTU后的一天内迅速恢复正常。在人类中,PTU似乎可能引起T4单碘化的转移,较少转化为具有代谢活性的T3,而更多地转化为代谢无活性的rT3。PTU降低T3水平的快速性可能在甲状腺功能亢进症的治疗中具有优势。