Wong C C, Döhler K D, von zur Mühlen A
J Endocrinol. 1980 Nov;87(2):255-63. doi: 10.1677/joe.0.0870255.
Replacement of the 3'-halogen of the tri-iodothyronine (T3) molecule by a propyl-group produces a thyromimetic analogue, 3'-isopropyl-3,5-di-iodo-L-thyronine (T2iPr), with high biological potency. A serum thyroid-stimulating hormone (TSH) suppression test with one single intraperitoneal injection of 3 or 30 nM-T3 or T2iPr or with 30 or 300 nM-thyroxine (T4) per kg body weight was performed on 56 adult male Lewis rats which were maintained for 3 weeks on an iodine-deficient diet containing 0.2% 6n-propyl-2-thiouracil (PTU). Blood was withdrawn from each rat by cardiac puncture 24 h before and 3, 7, 24 and 48 h after application of the iodothyronines. Raised serum levels of TSH, due to the treatment with PTU, were significantly reduced within 3 h of treatment with 30 nM-T3, 300 nM-T4, 3 or 30 nM-T2iPr and they remained low throughout the observation period. Treatment with 3 nM-T3, or 30 nM-T4 per kg body weight was less effective. Pituitary concentrations of growth hormone, TSH, prolactin and FSH were significantly reduced by the treatment with PTU. There was also a slight, but insignificant reduction of pituitary concentrations of LH. Treatment with T3, T4 or T2iPr stimulated the reaccumulation of growth hormone, TSH, prolactin, LH and FSH in the pituitary gland.
将三碘甲状腺原氨酸（T3）分子的3'-卤素用丙基取代可产生一种甲状腺模拟类似物，即3'-异丙基-3,5-二碘-L-甲状腺原氨酸（T2iPr），其具有很高的生物活性。对56只成年雄性Lewis大鼠进行了血清促甲状腺激素（TSH）抑制试验，这些大鼠在含0.2% 6-丙基-2-硫脲嘧啶（PTU）的缺碘饮食中饲养3周，试验中每千克体重单次腹腔注射3或30 nM-T3或T2iPr或30或300 nM-甲状腺素（T4）。在注射碘甲状腺原氨酸前24小时以及注射后3、7、24和48小时，通过心脏穿刺从每只大鼠采集血液。由于PTU治疗导致血清TSH水平升高，在用30 nM-T3、300 nM-T4、3或30 nM-T2iPr治疗后3小时内显著降低，并且在整个观察期内一直保持较低水平。每千克体重用3 nM-T3或30 nM-T4治疗效果较差。PTU治疗使垂体中生长激素、TSH、催乳素和促卵泡激素的浓度显著降低。垂体中促黄体生成素的浓度也有轻微但不显著的降低。用T3、T4或T2iPr治疗可刺激垂体中生长激素、TSH、催乳素、促黄体生成素和促卵泡激素的重新蓄积。
