|溶解性||Soluble in DMSO (23 mg/ml at 25 °C), ethanol (23 mg/ml at 25 °C), chloroform (~222.22 mg/ml), water (~200 mg/ml), and methanol.|
|产品介绍||A JAK/STAT signaling pathway inhibitor|
|别名||甲巯咪唑;1-甲基咪唑-2-硫醇;甲硫咪唑;1-Methyl-2-imidazolethiol; Methimazole; 1-Methylimidazole-2-thiol; Thiamazole; 2H-Imidazole-2-thione; 1,3-Dihydro-1-methyl-2H-imidazole-2-thione|
|生化机理||Methimazole is an antithyroid compound found to have antioxidant properties. Methimazole inhibits activation of the IFN-g-induced Janus kinase (JAK)/STAT signaling pathway in FRTL-5 thyroid cells, which may account for its immunodolulatory effects. Additionally, methimazole is an inhibitor of thyroperoxidase.|
|个人防护设备||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|
Antithyroid medications are the preferred therapy for the treatment of Graves' disease during pregnancy. Propylthiouracil (PTU) is favored over methimazole (MMI) due to potential teratogenic conc...Read More
The relationship between bone marrow characteristics and the clinical prognosis of antithyroid drug-induced agranulocytosis.
This study is aimed to explore the relationship between bone marrow characteristics and clinical prognosis of antithyroid drug (ATD) induced agranulocytosis. A retrospective study was conducted in the...Read More
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...Read More
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic ...Read More
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...Read More
Melasma is an acquired hyperpigmentation skin disorder in sun-exposed areas. It occurs almost exclusively over the face, and is most commonly seen in women. Several depigmenting agents have been used ...Read More
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...Read More
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
The liver-specific organic cation transport protein (OCT1; SLC22A1) transports several cationic drugs including the antidiabetic drug metformin and the anticancer agents oxaliplatin and imatinib. In t...Read More
Drug-induced liver injury (DILI) is a leading cause of drugs failing during clinical trials and being withdrawn from the market. Comparative analysis of drugs based on their DILI potential is an effec...Read More
CYP51 fulfills an essential requirement for all cells, by catalyzing three sequential mono-oxidations within the cholesterol biosynthesis cascade. Inhibition of fungal CYP51 is used as a therapy for t...Read More
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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...Read More
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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...Read More
[Sex difference of functional and structural alterations in the myocardium of rats with hypothyroidism].
In experiments on sexually mature rats we studied specific cholinergic regulations of the heart and the degree of its structural damage in hypothyroidism, depending on gender and hormone-productive ac...Read More
The inhibition of human cytochrome P450s (CYPs) is one of the most common mechanisms which can lead to drug-drug interactions. The inhibition of CYPs can be reversible (competitive or non-competitive)...Read More
Agranulocytosis is a rare but dreaded side-effect of thiamazole. A 61-year-old woman presented at the emergency department with fever and dyspnoea. Because she had recently started therapy with thiama...Read More
Methimazole (MMI) is an anti-thyroid drug used in the treatment of chronic hyperthyroidism. There is, however, some debate about its use during pregnancy as MMI is known to cross the mammalian placent...Read More
Higher dose of methimazole causes frequent adverse effects in the management of Graves' disease in children and adolescents.
Methimazole (MMI) is used as a first-line antithyroid drug in children and adolescents with Graves' disease (GD). The aim of this study was to evaluate the correlation between the initial dose of...Read More
The long-term regulation of food intake and body weight depends on the availability of thyroid hormones in the brain.
OBJECTIVES: We evaluated the contribution of the thyroid hormones to the long-term maintenance of feeding behavior and body weight, while distiguishing their direct central effects from those resultin...Read More
Thyrotoxicosis is mainly caused by autonomous adenomas of the thyroid gland and by Graves' disease. A less frequent cause for thyrotoxicosis is Hashimoto's thyroiditis. Thyrotoxicosis in aut...Read More
Regulation of gonadal sex ratios and pubertal development by the thyroid endocrine system in zebrafish (Danio rerio).
We examined associations between thyroid condition, gonadal sex and pubertal development in zebrafish. Seventy-two-hour postfertilization larvae were reared in untreated medium or in the presence of g...Read More
Abstract The Mayer-Rokitansky-Küster-Hauser (MRKH) syndrome is a congenital disorder characterized by aplasia of the uterus and the upper part of the vagina in an XX individual with normal developmen...Read More
A 15-year-old girl presented with chorea as a first sign of Graves' hyperthyroidism. Chorea abated with antithyroid drug treatment and reappeared when hyperthyroidism recurred but not when thyrot...Read More
The effect of chronic hyperthyroidism and restored euthyroid state by methimazole therapy in rat small mesenteric arteries.
Not much has been reported about the effects of hyperthyroidism and its correction on resistance vessels, and just two inconsistent studies have investigated the impacts of restored euthyroidism on va...Read More
Hypothyroidism and hyperthyroidism are associated with maternal and neonatal pregnancy complications. Hypothyroidism should be treated with levothyroxine. Hyperthyroidism requires treatment with propy...Read More
In the treatment of pregnant patients with Graves' disease, propylthiouracil is preferred over methimazole in early pregnancy because of a possible teratogenicity of methimazole. Methimazole is p...Read More
To assess the influence of thyroid function on natriuretic peptide concentration in hyperthyroid cats before and after treatment.Serum natriuretic peptide concentration was measured in 61 hyperthyroid...Read More
Jaundice related to thyrotoxicosis and not as an effect of antithyroid drugs is a rare complication that usually occurs in the presence of heart failure (HF) or hepatitis. We report a case of a 54-yea...Read More
Treadmill exercise ameliorates symptoms of methimazole-induced hypothyroidism through enhancing neurogenesis and suppressing apoptosis in the hippocampus of rat pups.
Thyroid hormones play a crucial role in new neuron production and maturation during brain development. Physical exercise is known to promote cell survival and functional recovery after brain injuries....Read More
Thyrotoxic periodic paralysis with graves' disease leading to the discovery of a hidden nonclassic 11β hydroxylase deficiency.
11β hydroxylase deficiency (OHD) is one of the main causes of congenital adrenal hyperplasia. There have been only a few reported cases of nonclassic 11β OHD, a milder form of the disease. It is dif...Read More
A 78 year old white male on methimazole due to Grave's thyroiditis presented with acute renal failure after a short term history of progressive shortness of breath, malaise, myalgias, arthralgias...Read More
To elucidate whether incidence of malformation related to 'methimazole (MMI) embryopathy' is increasing associated with exposure to MMI in the first 12 gestational weeks, Graves' women(...Read More
Development of a CD-MEKC method for investigating the metabolism of tamoxifen by flavin-containing monooxygenases and the inhibitory effects of methimazole, nicotine and DMXAA.
A selective and low-cost CD-MEKC method under acidic conditions was developed for investigating the N-oxygenation of tamoxifen (TAM) by flavin-containing monooxygenases (FMOs). The inhibitory effects ...Read More
ANCA-associated vasculitis with central retinal artery occlusion developing during treatment with methimazole.
A 63-year-old woman suddenly developed central retinal artery occlusion following a slight fever while being treated with methimazole (MMI) for hyperthyroidism. She was diagnosed to have anti-neutroph...Read More
Duration of t4 suppression in hyperthyroid cats treated once and twice daily with transdermal methimazole.
Transdermal methimazole is an acceptable alternative to oral treatment for hyperthyroid cats. There are, however, no studies evaluating the duration of T4 suppression after transdermal methimazole app...Read More
The aim of this study was to examine whether the relative gene expression of AdipoR1 and AdipoR2 in rat adipose tissue is altered by thyroid hormones, and whether this might relate to their circulatin...Read More
Interaction of methimazole with I2: X-ray crystal structure of the charge transfer complex methimazole-I2. implications for the mechanism of action of methimazole-based antithyroid drugs.
The antithyroid drug methimazole (MMI) reacts with molecular iodine to form, in a multistep process, 1-methylimidazole as final product. In this process, the charge transfer complex MMI-I 2 and the io...Read More
Antithyroid drug carbimazole and its analogues: synthesis and inhibition of peroxidase-catalyzed iodination of L-tyrosine.
Synthesis and biological activity of the antithyroid drug carbimazole (CBZ) and its analogues are described. The introduction of an ethoxycarbonyl group in methimazole and its selenium analogue not on...Read More
Mitochondrial biotransformation of omega-(phenoxy)alkanoic acids, 3-(phenoxy)acrylic acids, and omega-(1-methyl-1H-imidazol-2-ylthio)alkanoic acids: a prodrug strategy for targeting cytoprotective antioxidants to mitochondria.
Mitochondrial reactive oxygen species (ROS) generation and the attendant mitochondrial dysfunction are implicated in a range of disease states. The objective of the present studies was to test the hyp...Read More
Comparative studies on the effect of noxythiolin and other thioureas on the thyroid using in vitro and in vivo models of thyroid function.
Noxythiolin (Noxyflex-S) inhibited iodide organification (thyroid hormone synthesis) by cultured porcine thyrocytes in vitro after 5 hr (IC50 approx. 9.0 microM). The positive control, the anti-thyroi...Read More
Inhibition of iodine organification and regulation of follicular size in rat thyroid tissue in vitro.
The factors mediating the accumulation of thyroglobulin are of great importance to the understanding of the pathogenesis of human and experimentally induced colloid goiters. To elucidate further the u...Read More
The thioamides methimazole and thiourea inhibit growth of M. avium Subspecies paratuberculosis in culture.
Thyrotoxicosis is conceptualized as an "autoimmune" disease with no accepted infectious etiology. There are increasingly compelling data that another "autoimmune" affliction, Crohn...Read More