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左旋甲状腺素

左旋甲状腺素用途

L-Thyroxine (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)。

左旋甲状腺素名称

[ CAS 号 ]:
51-48-9

[ 中文名 ]:
L-甲状腺素

[ 英文名 ]:
L-thyroxine

[中文别名 ]:

[英文别名 ]:

Thyroxine (VAN)
Thyroxine, L- (8CI)
EINECS 200-101-1
3,3’,5,5‘’-Tetraiodo-L-thyronine
Thyroxine
L-3,5,3',5'-Tetraiodothyronine
thyroxine-binding globulin
(-)-Thyroxine
Thryroxine, l-
thyroxin

左旋甲状腺素生物活性

[ 描述 ]:

L-Thyroxine (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)。

[ 相关类别 ]:

信号通路 >> 其他 >> 甲状腺激素受体

研究领域 >> 内分泌

天然产物 >> 其他

[ 靶点 ]

Human Endogenous Metabolite

[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]

左旋甲状腺素物理化学性质

[ 密度 ]:
2.6±0.1 g/cm3

[ 沸点 ]:
576.3±50.0 °C at 760 mmHg

[ 熔点 ]:
235 °C

[ 分子式 ]:
C₁₅H₁₁I₄NO₄

[ 分子量 ]:
776.870

[ 闪点 ]:
302.3±30.1 °C

[ 精确质量 ]:
776.686646

[ PSA ]:
92.78000

[ LogP ]:
5.93

[ 外观性状 ]:
米色粉末

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.795

[ 储存条件 ]:
2~8°C

[ 水溶解性 ]:
insoluble

左旋甲状腺素MSDS

详细MSDS(安全技术说明书)

左旋甲状腺素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YP2833500

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

CAS REGISTRY NUMBER :: 51-48-9

BEILSTEIN REFERENCE NO. :: 2228515

LAST UPDATED :: 199709

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C15-H11-I4-N-O4

MOLECULAR WEIGHT :: 776.87

WISWESSER LINE NOTATION :: QVYZ1R CI EI DOR DQ CI EI

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 63 ug/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Cardiac - pulse rate increase, without fall in BP

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 400 ug/kg/2D-I

TOXIC EFFECTS :: Behavioral - coma Cardiac - arrhythmias (including changes in conduction)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2 mg/kg/10D-I

TOXIC EFFECTS :: Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - monoamine oxidase Biochemical - Metabolism (Intermediary) - effect on mitochondrial function

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 26250 ug/kg

SEX/DURATION :: female 1-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1400 ug/kg

SEX/DURATION :: female 16-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 410 mg/kg

SEX/DURATION :: female 3 week(s) pre-mating female 1-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 450 ug/kg

SEX/DURATION :: female 7-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 8160 ug/kg

SEX/DURATION :: female 7 day(s) pre-mating - 5 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - postpartum

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 600 ug/kg

SEX/DURATION :: female 19-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 12 mg/kg

SEX/DURATION :: male 6 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 12 mg/kg

SEX/DURATION :: female 9-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TEST SYSTEM :: Rodent - rat

DOSE/DURATION :: 6250 ug/kg/2D (Continuous)

REFERENCE :: BEXBAN Bulletin of Experimental Biology and Medicine (English Translation). Translation of BEBMAE. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.41- 1956- Volume(issue)/page/year: 72,942,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M0234 No. of Facilities: 68 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 2770 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M0234 No. of Facilities: 717 (estimated) No. of Industries: 4 No. of Occupations: 9 No. of Employees: 10666 (estimated) No. of Female Employees: 7298 (estimated)

左旋甲状腺素安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310 + P330-P302 + P352 + P312-P370 + P378

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
2811.0

[ WGK德国 ]:
3

[ RTECS号 ]:
YP2833500

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2942000000

左旋甲状腺素合成路线

详细合成路线

左旋甲状腺素上下游产品

左旋甲状腺素上游产品

左旋甲状腺素下游产品

左旋甲状腺素制备

可从动物甲状腺中提取。可由3,5-二碘-L-酪氨酸为原料制取。

甲状腺素的形成经过合成、贮存、碘化、重吸收、分解和释放六个过程：1. 滤泡上皮细胞从血液中摄取氨基酸，在粗面内质网合成甲状腺球蛋白的前体，继而在高尔基复合体加糖并浓缩形成分泌颗粒，再以胞吐方式排放到滤泡腔内贮存。2. 滤泡上皮细胞能从血液中摄取I-，I-经过过氧化物酶的作用而活化。3. 活化后的I-进入滤泡腔与甲状腺球蛋白结合，形成碘化的甲状腺球蛋白。4. 滤泡上皮细胞在腺垂体分泌的促甲状腺激素的作用下，胞吞滤泡腔内的碘化甲状腺球蛋白，成为胶质小泡。5. 胶质小泡与溶酶体融合，碘化甲状腺球蛋白被水解酶分解形成大量四碘甲状腺原氨酸（T4）和少量三碘甲状腺原氨酸（T3），即甲状腺素。6. T3和T4于细胞基底部释放入血。

左旋甲状腺素海关

[ 海关编码 ]: 2922509090

[ 中文概述 ]:
2922509090. 其他氨基醇酚、氨基酸酚及其他含氧基氨基化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件：AB. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

左旋甲状腺素文献

Inducible, tightly regulated and growth condition-independent transcription factor in Saccharomyces cerevisiae.

Nucleic Acids Res. 42(17) , e130, (2014)

The precise control of gene expression is essential in basic biological research as well as in biotechnological applications. Most regulated systems available in yeast enable only the overexpression o...

Replisome-mediated translesion synthesis and leading strand template lesion skipping are competing bypass mechanisms.

J. Biol. Chem. 289(47) , 32811-23, (2014)

A number of different enzymatic pathways have evolved to ensure that DNA replication can proceed past template base damage. These pathways include lesion skipping by the replisome, replication fork re...

Levothyroxine replacement in hypothyroid humans reduces myocardial lipid load and improves cardiac function.

J. Clin. Endocrinol. Metab. 99(11) , E2341-6, (2014)

Hypothyroidism is a common endocrine disorder frequently accompanied by alterations in lipid metabolism, such as hypercholesterolemia and high circulating triglycerides, both risk factors for nonische...

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