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| 化学名: | レバミゾール塩酸塩 | | 英語化学名: | Levamisole hydrochloride | | 别名: | 1-b)thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(s)-imidazo(;1-b)thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,l-(-)-imidazo(;1-b]thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(S)-Imidazo[2;decaris;Imidazo[2,1-b]thiazole,2,3,5,6-tetrahydro-6-phenyl-,monohydrochloride,(S)-;kw-2-le-t;L-2,3,5,6-Tetrahydro-6-phenylimidazo-[2,1-6]-thiazole;levomysolhydrochloride | | CAS番号: | 16595-80-5 | | 分子式: | C11H13ClN2S | | 分子量: | 240.75 | | EINECS: | 240-654-6 | | カテゴリ情報: | Other APIs;REZIFILM;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Pharma;Pharmaceutical intermediate;Antibiotic Explorer;Veterinaries;Protein Phosphatase;Asymmetric Synthesis;Synthetic Organic Chemistry;API;16595-80-5 | | Mol File: | 16595-80-5.mol |  |
| 融点 | 266-267 °C(lit.) | | 比旋光度 | -128 º (c=5, H2O) | | 屈折率 | -126 ° (C=1, H2O) | | 闪点 | 9℃ | | 貯蔵温度 | 2-8°C | | 溶解性 | Freely soluble in water, soluble in ethanol (96 per cent), slightly soluble in methylene chloride. | | 外見 | Crystalline Powder | | 色 | White to almost white | | 水溶解度 | 210 g/L (20 ºC) | | Merck | 14,5459 | | BRN | 4358988 | | BCS Class | 3/1 | | 安定性： | Hygroscopic | | InChI | InChI=1/C11H12N2S.ClH/c1-2-4-9(5-3-1)10-8-13-6-7-14-11(13)12-10;/h1-5,10H,6-8H2;1H/t10-;/s3 | | InChIKey | LAZPBGZRMVRFKY-HNCPQSOCSA-N | | SMILES | [C@H]1(N=C2SCCN2C1)C1=CC=CC=C1.Cl |&1:0,r| | | LogP | 1.845 (est) | | CAS データベース | 16595-80-5(CAS DataBase Reference) | | EPAの化学物質情報 | Levamisole hydrochloride (16595-80-5) |
| | レバミゾール塩酸塩 Usage And Synthesis |
| 外観 | 白色〜ほとんど白色, 結晶性粉末〜粉末 | | 溶解性 | 水溶解度は62.5% (20℃)。水に溶ける。 | | 用途 | 残留レバミゾール定量用。 | | 用途 | 薬理・生理作用研究用。 | | 用途 | 動物用駆虫剤、農薬（松枯れ防止剤）、免疫賦活薬。
| | 効能 | 駆虫薬 | | 使用上の注意 | 毒性がありますので、取り扱う場合は、保護眼鏡、保護手袋および保護マスクを用いて下さい。 | | 化学的特性 | White to light yellow crystalline powder, odorless, bitter taste. Melting point 227-229℃. Soluble in water, methanol, ethanol and glycerol, slightly soluble in chloroform and aether; insoluble in acetone. Stable under acidic conditions, but easy to decompose and fail under alkaline conditions. | | Originator | Solaskil,Specia,France,1971 | | 使用 | Levamisole hydrochloride is an anthelmintic. The activity of levamisole is about twice as high as that of abscisicidal, and the toxicity and side effects are lower. Levamisole can cause muscle paralysis of roundworms and then excrete them in the feces. It is mainly used as an anti-worm and anti-hookworm. | | 使用 | Biological response modifier with anthelmintic activity. Anthelmintic (nematodes); immunomodulator. | | 定義 | ChEBI: Levamisole hydrochloride is an organic molecular entity. | | 製造方法 | Levamisole hydrochloride was prepared from racemic tetraimidazole by splitting, alkali analysis and acidification into salt.
Dibenzoyl-D-tartaric acid is boiled in water for 40min, hydrolyzed and neutralized with sodium hydroxide solution to pH 7.5, and then added to racemic tetraimidazole. The levamisole is precipitated by generating salt with bisbenzoyl-tartaric acid. After separation, add sodium hydroxide solution to PH=9 and decompose levamisole. Then dissolved in dilute hydrochloric acid solution, after decolorization by activated carbon, the filtrate was concentrated nearly dry, and crystallized by adding acetone and cooling to 0℃. Filtered and dried to obtain levamisole hydrochloride. | | brand name | Ergamisol (Janssen);Vermisol. | | Therapeutic Function | Antiinflammatory | | Biochem/physiol Actions | Shows both immunostimulant and immunosuppressant effects, depending on several controllable factors. Very effective in treatment of ascariasis (hookworm infestation). Useful in chemotherapy of colorectal cancers, possibly due to its stimulation of IL-1 production and direct activation of macrophages. | | 薬理学 | Levamisole Hydrochloride is the hydrochloride salt of the synthetic imidazothiazole derivative levamisole with anthelminthic and immunomodulating activities. In immunosuppressed states, levamisole may restore immune function by: 1) stimulating antibody formation, 2) stimulating T-cell activation and proliferation, 3) potentiating monocyte and macrophage phagocytosis and chemotaxis and 4) increasing neutrophil mobility, adherence, and chemotaxis. | | 薬物動態学 | Levamisole is rapidly absorbed from all routes of administration, with peak blood levels occurring within an hour followed by rapid metabolism and depletion principally via urinary excretion, with an elimination half-life of approximately 4 h. | | Mode of action | Levamisole is a cholinergic receptor agonist and elicits spastic muscle paralysis due to prolonged activation of the excitatory nicotinic acetylcholine receptors (nAChR) on nematode body wall muscle. | | Toxicity evaluation | Symptoms of levamisole toxicity mimic organophosphate toxicity (salivation, lacrimation, urination and defecation, hyperesthesia, seizures and irritability). There is no antidote for levamisole toxicity.
The World Health Organization reviewed hematological studies in animals and humans and derived acceptable daily intake for levamisole as 0.006 mg/kg body weight. This suggests a person can ingest 0.36 mg of levamisole/day over a lifetime without any appreciable risk.
levamisole |
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