L-甲状腺素钠五水合物(左甲状腺素钠)

L-甲状腺素钠五水合物(左甲状腺素钠)用途

L-Thyroxine sodium salt pentahydrate (Levothyroxine; T4) 是一种合成的甲状腺激素,用于治疗甲状腺功能减退症。DIO 酶将 L-Thyroxine (T4) 转化成具有生物活性的三碘甲状腺氨酸 (T3)。

L-甲状腺素钠五水合物(左甲状腺素钠)名称

[ CAS 号 ]:
6106-07-6

[ 中文名 ]:
L-甲状腺素钠盐五水合物

[ 英文名 ]:
Sodium levothyroxine pentahydrate

[中文别名 ]:

左旋甲状腺素钠五水合物

[英文别名 ]:

MFCD00149110
EINECS 200-221-4
L-Thyroxine (sodium salt pentahydrate)

L-甲状腺素钠五水合物(左甲状腺素钠)生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 甲状腺激素受体

研究领域 >> 内分泌

[ 靶点 ]

Thyroid Hormone Receptor

[体内研究]

催化甲状腺素(前激素)转化为活性甲状腺激素的脱碘酶(DIO)与促甲状腺激素(TSH)水平有关。与DIO3相比,DIO1和DIO2催化甲状腺激素分泌的激活,起到分泌失活的作用。 DIO1和DIO2的活性在垂体TSH分泌的负反馈调节中起关键作用[1]。已知L-甲状腺素(T4)和三碘甲腺原氨酸(T3)激素调节离子通道,泵和调节性收缩蛋白的表达。此外,已显示甲状腺激素影响钙稳态和负责激发和收缩的通量,L-甲状腺素和三碘甲状腺原氨酸调节其药理控制和分泌。在用无碘饮食喂养12周的大鼠中,与用标准饮食喂养的对照组相比,观察到三碘甲腺原氨酸和L-甲状腺素水平的显着降低(p <0.001)。在用低剂量L-甲状腺素治疗的组中,观察到L-甲状腺素水平的增加(p = 0.02),而三碘甲状腺原氨酸水平实际上与对照组相似(p = 0.19)。与未治疗的甲状腺功能减退组相比,用高剂量L-甲状腺素治疗的大鼠显示三碘甲状腺原氨酸和L-甲状腺素循环浓度显着增加(分别为p <0.001和p = 0.004),并且L-甲状腺素水平显着增加与对照值相比(p = 0.03)[2]。

[动物实验]

使用大鼠[2] Sprague-Dawley雌性大鼠（N = 22）。非妊娠大鼠分为四组：1）对照，2）甲状腺功能减退，3）用低剂量L-甲状腺素（20μg/ kg /天）治疗甲状腺功能减退症和4）高剂量L-甲状腺素（100μg） / kg /天）。对照大鼠（组1）用标准饮食喂养，而干预大鼠用无碘饮食喂养12周以诱导甲状腺功能减退（2-4组），持续4周以允许筛查甲状腺功能减退状态和L -Thyroxine处理。随意提供食物和水（无碘饮食）。用低（第3组）或高剂量的L-甲状腺素（第4组）治疗的甲状腺功能减退组每24小时腹膜内注射，分别为20μg/ kg /天和100μg/ kg /天。在开始对照或无碘饮食后，在第12和16周收集血样用于甲状腺功能筛查。在治疗结束时在全身麻醉（异氟醚2％）下进行子宫切除术，并将两个子宫角放置在生理Krebs溶液中，直到等长张力测量不超过1小时。

[参考文献]

[1]. Arici M, et al. Association between genetic polymorphism and levothyroxine bioavailability in hypothyroid patients. Endocr J. 2018 Jan 11.

[2]. Corriveau S, et al. Levothyroxine treatment generates an abnormal uterine contractility patterns in an in vitro animalmodel. J Clin Transl Endocrinol. 2015 Sep 9;2(4):144-149.

[相关活性小分子]

L-甲状腺素钠五水合物(左甲状腺素钠)物理化学性质

[ 密度 ]:
2.381

[ 熔点 ]:
207-210 (dec.)(lit.)

[ 分子式 ]:
C₁₅H₂₀I₄NNaO₉

[ 分子量 ]:
888.928

[ 精确质量 ]:
888.721436

[ PSA ]:
141.76000

[ LogP ]:
3.60140

[ 外观性状 ]:
powder

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
cell culture medium: 0.1 mg/mL

L-甲状腺素钠五水合物(左甲状腺素钠)MSDS

详细MSDS(安全技术说明书)

L-甲状腺素钠五水合物(左甲状腺素钠)毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YP2833760

CHEMICAL NAME :: L-Tyrosine, O-(4-hydroxy-3,5-diiodophenyl)-3,5-diiodo-, sodium salt, pentahydrate

CAS REGISTRY NUMBER :: 6106-07-6

LAST UPDATED :: 199504

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H10-I4-N-O4.Na.5H2-O

MOLECULAR WEIGHT :: 888.95

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1 mg/kg

SEX/DURATION :: female 1-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: JOENAK Journal of Endocrinology. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1939- Volume(issue)/page/year: 139,275,1993 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2466 No. of Facilities: 19 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 399 (estimated) No. of Female Employees: 308 (estimated)

L-甲状腺素钠五水合物(左甲状腺素钠)安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
40

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
YP2833760

L-甲状腺素钠五水合物(左甲状腺素钠)文献

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Biol. Chem. 396(3) , 261-75, (2015)

The genome of Tannerella forsythia, an etiological factor of chronic periodontitis, contains several genes encoding putative proteases. Here, we characterized a subtilisin-like serine protease of T. f...

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