甲巯咪唑

甲巯咪唑用途

用途一：为抗甲状腺药: 用于各种类型的甲状腺功能亢进症，包括Graves病(伴自身免疫功能紊乱、甲状腺弥漫性肿大、可有突眼)，甲状腺腺瘤，结节性甲状腺肿及甲状腺癌所引起者。
用途二：甲亢平的中间体。

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甲巯咪唑作用

甲巯咪唑为抗甲状腺药物。其作用机制是抑制甲状腺内过氧化物酶，从而阻碍吸聚到甲状腺内碘化物的氧化及酪氨酸的偶联，阻碍甲状腺素（T4）和三碘甲状腺原氨酸（T3）的合成。动物实验观察到可抑制B淋巴细胞合成抗体，降低血循环中甲状腺刺激性抗体的水平，使抑制性T细胞功能恢复正常。甲巯咪唑抗甲状腺药物综述：抗甲状腺药物抑制甲状腺激素的合成，其作用机制是抑制甲状腺内过氧化物酶，从而阻碍吸聚到甲状腺内碘化物的氧化及酪氨酸的偶联，阻碍甲状腺素(T4)和三碘甲状腺原氨酸(T3)的合成。另外，丙硫氧嘧啶在外周组织中抑制T4转变为T3。硫脲类抗甲状腺药除阻碍甲状腺激素合成外，还有轻度的免疫抑制作用。可抑制B淋巴细胞合成抗体，降低血循环中甲状腺刺激性抗体的水平，使抑制性T细胞功能恢复正常。这些作用可能是促使Graves病中免疫紊乱得到缓解的原因。

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甲巯咪唑名称

[ CAS 号 ]:
60-56-0

[ 中文名 ]:
甲巯咪唑

[ 英文名 ]:
Methimazole

[中文别名 ]:

[英文别名 ]:

1-methyl-1H-imidazole-2(3H)-thione
Methimazole
2H-Imidazole-2-thione, 1,3-dihydro-1-methyl-
3-methyl-imidazole-2-thione
methyl-2-mercaptoimidazole
1-methyl-1H-imidazole-2-thiol
Thimazol
Merkastan
Frentirox
2-mercapto-1-methyl-imidazole

甲巯咪唑生物活性

[ 描述 ]:

Methimazole(Tapazole, Northyx)是抗甲状腺化合物。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 内分泌

[参考文献]

[1]. Nakamura H, et al. Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease. J Clin Endocrinol Metab. 2007 Jun;92(6):2157-62. Epub 2007 Mar 27.

[2]. Crescioli C, et al. Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes. J Endocrinol. 2007 Oct;195(1):145-55.

[相关活性小分子]

甲巯咪唑物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
280.0±9.0 °C at 760 mmHg

[ 熔点 ]:
144-147 °C(lit.)

[ 分子式 ]:
C₄H₆N₂S

[ 分子量 ]:
114.169

[ 闪点 ]:
123.1±18.7 °C

[ 精确质量 ]:
114.025169

[ PSA ]:
56.62000

[ LogP ]:
-0.34

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.633

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
soluble

甲巯咪唑MSDS

详细MSDS(安全技术说明书)

甲巯咪唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NI8615000

CHEMICAL NAME :: Imidazole-2-thiol, 1-methyl-

CAS REGISTRY NUMBER :: 60-56-0

LAST UPDATED :: 199710

DATA ITEMS CITED :: 29

MOLECULAR FORMULA :: C4-H6-N2-S

MOLECULAR WEIGHT :: 114.18

WISWESSER LINE NOTATION :: T5N CNJ A BSH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2250 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - somnolence (general depressed activity) Behavioral - tremor

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1050 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 860 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - somnolence (general depressed activity) Behavioral - tremor

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 345 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - somnolence (general depressed activity) Behavioral - tremor

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 580 mg/kg/1W-C

TOXIC EFFECTS :: Endocrine - evidence of thyroid hypofunction Endocrine - changes in thyroid weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2400 mg/kg/12D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1100 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Endocrine - thyroid tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 33 gm/kg/1Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Endocrine - thyroid tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2700 mg/kg/26W-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Endocrine - thyroid tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 145 mg/kg

SEX/DURATION :: female 1-34 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 80 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 600 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 7 day(s) post-birth

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 320 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - endocrine system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1100 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 160 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 567 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1530 ug/kg

SEX/DURATION :: female 18-20 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 320 mg/kg

SEX/DURATION :: female 16-21 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 320 mg/kg

SEX/DURATION :: female 16-21 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1152 mg/kg

SEX/DURATION :: female 16-21 day(s) after conception lactating female 10 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - behavioral

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 28 mg/kg/2W (Continuous)

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 326,193,1995 *** REVIEWS *** TOXICOLOGY REVIEW PCNAA8 Pediatric Clinics of North America. (W.B. Saunders Co., W. Washington Sq., Philadelphia, PA 19105) V.1- 1954- Volume(issue)/page/year: 8,413,1961 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83970 No. of Facilities: 33 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 297 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83970 No. of Facilities: 23 (estimated) No. of Industries: 2 No. of Occupations: 4 No. of Employees: 707 (estimated) No. of Female Employees: 239 (estimated)

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甲巯咪唑安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H317-H361

[ 警示性声明 ]:
P280

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R43;R62;R63

[ 安全声明 (欧洲) ]:
S26-S27-S36-S45-S36/37

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

[ WGK德国 ]:
3

[ RTECS号 ]:
NI8615000

[ 海关编码 ]:
2933290090

甲巯咪唑合成路线

详细合成路线

甲巯咪唑上下游产品

甲巯咪唑上游产品

甲巯咪唑下游产品

甲巯咪唑制备

以氨基乙醛缩二乙醇与异硫氰酸甲酯反应制取。亦可从硫氰酸与N-取代的氨基乙缩醛反应制取。亦可从硫氰酸与N-取代的氨基乙缩醛反应制取。

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甲巯咪唑海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

甲巯咪唑文献

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

The Japanese toxicogenomics project: application of toxicogenomics.

Mol. Nutr. Food. Res. 54 , 218-27, (2010)

Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted appr...

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甲巯咪唑

甲巯咪唑用途

甲巯咪唑作用

甲巯咪唑名称

甲巯咪唑生物活性

甲巯咪唑物理化学性质

甲巯咪唑MSDS

详细MSDS(安全技术说明书)

甲巯咪唑毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

甲巯咪唑安全信息

甲巯咪唑合成路线

详细合成路线

甲巯咪唑上下游产品

甲巯咪唑上游产品

甲巯咪唑下游产品

甲巯咪唑制备

甲巯咪唑海关

甲巯咪唑文献

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