Liothyronine sodium is a potent thyroid hormone receptor TRα and TRβ agonist with Ki values of 2.33nM[1]. Liothyronine sodium is an active form of thyroid hormone that is chemically almost identical to the endogenous thyroid hormone triiodothyronine (T3)[2]. Liothyronine sodium is usually used in the replacement treatment of hypothyroidism[3], and can also be used in the treatment of thyroid cancer and the detection of thyroid function[4]. In addition, Liothyronine sodium is also used in the study of other metabolic related diseases, such as obesity[5].
In vitro, Liothyronine sodium(100µM) treatment of Jurkat hTIGIT cells and CHOK1-hPVR cells for 48h reversed the IL-2 secretion inhibition resulted by TIGIT/PVR ligation without affecting cell viability[6]. Liothyronine sodium(100nM) stimulates the proliferation of hepatocellular carcinoma cells overexpressing TRβ1[1].
In vivo, Liothyronine sodium(25μg/kg; 1h post-tMCAO; intravenously) reduced infarct volumes in a dose-dependent manner, with reduced efficacy at 4.5h post-tMCAO(P = 0.066) and no effect at 8h post-tMCAO(P > 0.999), while demonstrating a persistent protective effect for 72h post-tMCAO (P < 0.01) and accelerating motor function recovery by day 3 (P < 0.05), accompanied by reduced cerebral edema, diminished blood–brain barrier leakage, and decreased aquaporin-4 expression in stroke mice[7].
References:
[1] Lin, K. H., Lin, Y. W., Parkison, C., & Cheng, S. Y. (1994). Stimulation of proliferation by 3,3',5-triiodo-L-thyronine in poorly differentiated human hepatocarcinoma cells overexpressing beta 1 thyroid hormone receptor. Cancer letters, 85(2), 189–194.
[2] MORTON J. H. (1957). Sodium liothyronine in metabolic insufficiency syndrome and associated disorders; preliminary report. Journal of the American Medical Association, 165(2), 124–129.
[3] Escobar-Morreale, H. F., Botella-Carretero, J. I., & Morreale de Escobar, G. (2015). Treatment of hypothyroidism with levothyroxine or a combination of levothyroxine plus L-triiodothyronine. Best practice & research. Clinical endocrinology & metabolism, 29(1), 57–75.
[4] Salas-Lucia, F., & Bianco, A. C. (2022). T3 levels and thyroid hormone signaling. Frontiers in endocrinology, 13, 1044691.
[5] Krotkiewski M. (2000). Thyroid hormones and treatment of obesity. International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity, 24 Suppl 2, S116–S119.
[6] Zhou, X., Du, J., Wang, H., Chen, C., Jiao, L., Cheng, X., Zhou, X., Chen, S., Gou, S., Zhao, W., Zhai, W., Chen, J., & Gao, Y. (2020). Repositioning liothyronine for cancer immunotherapy by blocking the interaction of immune checkpoint TIGIT/PVR. Cell communication and signaling : CCS, 18(1), 142.
[7] Ullrich, D., Führer, D., Heuer, H., Mayerl, S., Haupeltshofer, S., Schmitt, L. I., Leo, M., Szepanowski, R. D., Hagenacker, T., Schwaninger, M., Kleinschnitz, C., & Langhauser, F. (2025). Triiodothyronine treatment in mice improves stroke outcome and reduces blood-brain barrier damage. European thyroid journal, 14(1), e240143.
Liothyronine sodium是一种强效的甲状腺激素受体TRα和TRβ激动剂，其Ki值为 2.33nM[1]。Liothyronine sodium是一种活性形式的甲状腺激素，其化学性质几乎与内源性甲状腺激素三碘甲状腺原氨酸（T3）相同[2]。Liothyronine sodium通常用于甲状腺功能减退症的替代治疗[3]，也可用于甲状腺癌的治疗和甲状腺功能的检测[4]。此外，Liothyronine sodium还用于其他与代谢相关的疾病研究，如肥胖[5]。
在体外实验中，用100µM的Liothyronine sodium 处理Jurkat hTIGIT细胞和CHOK1-hPVR细胞 48小时，可逆转TIGIT/PVR结合导致的IL-2分泌抑制，且不影响细胞活力[6]。100nM的Liothyronine sodium可刺激过表达 TRβ1 的肝癌细胞增殖[1]。
在体内实验中，在中风小鼠模型中，Liothyronine sodium(25μg/kg；短暂性大脑中动脉闭塞（tMCAO）后1小时；静脉注射）以剂量依赖性方式减少梗死体积，在术后4.5小时给药时效性降低（P = 0.066），在 术后8小时给药则无效（P > 0.999），且在tMCAO后 72小时内显示出持续的保护效果（P < 0.01），并在第3天加速运动功能恢复（P < 0.05），同时观察到脑水肿减轻、血脑屏障渗漏减少以及水通道蛋白-4 表达降低[7]。