Moriyasu M, Nasu M, Honda H, Sakamoto T, Yamamura M, Matsuoka Y
Panapharm Laboratories Co., Ltd., Kumamoto, Japan.
Nihon Yakurigaku Zasshi. 1996 Jun;107(6):285-97. doi: 10.1254/fpj.107.285.
The stimulatory effect of TA-0910 on the secretions of thyroid-stimulating hormone (TSH) and thyroid hormones was investigated in male and female rats. Single intravenous administration of TA-0910 at 8.3 nmol/body acutely elevated the plasma TSH level, with delayed and moderate increases of T3 and T4 in plasma. Similar increments of plasma TSH and thyroid hormones were observed when TRH was injected at the dose of 0.83 nmol/body. Oral administration of TA-0910 at 2.75 mumol/body was equally potent or slightly more potent to secrete TSH than TRH at 0.275 mumol/body. The elevated TSH by TA-0910 decreased to the control level within 2 hr after intravenous injection or within 6 hr after oral administration; on the other hand, the higher levels of the thyroid hormones were retained for up to 4 and 6 hr after intravenous and oral administration, respectively. These findings indicate that TA-0910 and TRH stimulate the secretion of TSH and thyroid hormones by a similar manner and that the TSH-secreting activity of TA-0910 is lower by an order of magnitude compared with that of TRH.
在雄性和雌性大鼠中研究了TA - 0910对促甲状腺激素（TSH）和甲状腺激素分泌的刺激作用。以8.3 nmol/只的剂量单次静脉注射TA - 0910可使血浆TSH水平急性升高，血浆中T3和T4出现延迟且中度升高。当以0.83 nmol/只的剂量注射促甲状腺激素释放激素（TRH）时，观察到血浆TSH和甲状腺激素有类似的升高。以2.75 μmol/只的剂量口服TA - 0910在分泌TSH方面与以0.275 μmol/只的剂量口服TRH同样有效或略强。静脉注射TA - 0910后2小时内或口服后6小时内，TA - 0910引起的TSH升高降至对照水平；另一方面，静脉注射和口服后，甲状腺激素的较高水平分别维持长达4小时和6小时。这些发现表明，TA - 0910和TRH以类似方式刺激TSH和甲状腺激素的分泌，并且与TRH相比，TA - 0910的TSH分泌活性低一个数量级。
