Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. 60-56-0, formula is C4H6N2S, Name is 1-Methyl-1H-imidazole-2(3H)-thione. Their solubility in alcohol is lower than that in water and decreases with increasing molecular weight of the alcohols . HPLC of Formula: 60-56-0.
Busby, Robert W.;Cai, Xiaokun;Yang, Sihyung;Ramos, Luis;Venkatarangan, Lata;Shen, Helen;Wax, Stephen;Sadeque, Abu J. M.;De Colle, Cyril research published 《 Metopimazine is primarily metabolized by a liver amidase in humans》, the research content is summarized as follows. Metopimazine (MPZ) is a peripherally restricted, dopamine D2 receptor antagonist used for four decades to treat acute nausea and vomiting. MPZ is currently under clin. investigation for the treatment of gastroparesis (GP). MPZ undergoes high first-pass metabolism that produces metopimazine acid (MPZA), the major circulating metabolite in humans. Despite a long history of use, the enzymes involved in the metabolism of MPZ have not been identified. Here we report a series of studies designed to identify potential MPZ metabolites in vitro, determine their clin. relevance in humans, and elucidate the enzymes responsible for their formation. The findings demonstrated that the formation of MPZA was primarily catalyzed by human liver microsomal amidase. Addnl., human liver cytosolic aldehyde oxidase (AO) catalyzes the formation of MPZA, in vitro, although to a much lesser extent. Neither cytochrome P 450 enzymes nor flavin-monooxygenases (FMO) were involved in the formation MPZA, although two minor oxidative pathways were catalyzed by CYP3A4 and CYP2D6 in vitro. Anal. of plasma samples from subjects dosed 60 mg of MPZ verified that these oxidative pathways are very minor and that CYP enzyme involvement was negligible compared to microsomal amidase/hydrolase in overall MPZ metabolism in humans. The metabolism by liver amidase, an enzyme family not well defined in small mol. drug metabolism, with minimal metabolism by CYPs, differentiates this drug from current D2 antagonists used or in development for the treatment of GP.
60-56-0, 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.
Methimazole is a thiourea antithyroid agent that prevents iodine organification, thus inhibiting the synthesis of thyroxine. Antihyperthyroid.
Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%.3 It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat. Methimazole has been used to induce hypothyroidism in mice. Formulations containing methimazole have been used in the treatment of hyperthyroidism.
Methimazole is a thyreostatic compound, and an antihormone, which is widely used in medicine for the treatment of hyperthyroidism.
Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO), with antithyroid activity. Upon administration, methimazole inhibits the metabolism of iodide and the iodination of tyrosine residues in the thyroid hormone precursor thyroglobulin by TPO; this prevents the synthesis of the thyroid hormones triiodothyronine (T3) and thyroxine (T4).
Methimazole is an antithyroid medication which is now considered the first line agent for medical therapy of hyperthyroidism and Graves disease. Methimazole has been linked to serum aminotransferase elevations during therapy as well as to a clinically apparent, idiosyncratic liver injury that is typically cholestatic and self-limited in course.
Methimazole, also known as tapazole or danantizol, belongs to the class of organic compounds known as imidazolethiones. These are aromatic compounds containing an imidazole ring which bears a thioketone group. Methimazole is a drug which is used for the treatment of hyperthyroidism, goiter, graves disease and psoriasis. Methimazole is soluble (in water) and a very weakly acidic compound (based on its pKa). Methimazole has been detected in multiple biofluids, such as urine and blood. Methimazole can be converted into methimazole S-oxide., HPLC of Formula: 60-56-0
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem