ネオスチグミン ブロミド 化学特性,用途語,生産方法
外観
白色～ほとんど白色, 結晶性粉末～粉末
溶解性
水, エタノールに易溶、エーテルに不溶。水及びエタノールに溶けやすく、アセトンにほとんど溶けない。
解説
C12H19BrN2O2(303.19)．m-ヒドロキシ-N,N-ジメチルアニリンにホスゲンを作用させ，ついでジメチルアミンを縮合し，さらにN-四級化してつくる．
"融点167 ℃．水，エタノールに可溶．機能減退を伴う消化器障害，筋無力症などの運動障害の治療薬として使用される．LD50 0.165 mg/kg(マウス，静注)，7449 mg/kg(ネコ，経口)．[CAS 114-80-7]
森北出版「化学辞典（第2版）
用途
コリンエステラーゼ阻害剤。
効能
副交感神経刺激薬, アセチルコリンエステラーゼ阻害薬
商品名
ワゴスチグミン (塩野義製薬)
化学的特性
Crystalline Solid
使用
Neostigmine bromide has been used as an acetyl cholinesterase (AChE) inhibitor:
- to control reaction specificity of acetylcholinesterase in coronal organ of Botryllus schlosseri.
- to study its effects on abnormal contraction of pyloric circular smooth muscle strips (PCSMS).
- to study its effects on depolarization of bag cell neurons.
一般的な説明
Neostigmine bromide, (m-hydroxyphenyl)trimethylammonium bromide dimethylcarbamateor the dimethylcarbamic ester of 3-hydroxyphenyltrimethylammoniumbromide (Prostigmin bromide), is usedas an antidote to nondepolarizing neuromuscular blockingdrugs and in the treatment of myasthenia gravis. It occurs asa bitter, odorless, white, crystalline powder. It is soluble inwater and alcohol. The crystals are much less hygroscopicthan those of neostigmine methylsulfate and thus may beused in tablets. Solutions are stable and may be sterilized byboiling. Aqueous solutions are neutral to litmus.
臨床応用
Use of physostigmine, as a prototype of an indirect-actingparasympathomimetic drug, facilitated the development ofstigmine, in which a trimethylamine group was placed para toa dimethylcarbamate group in benzene. Better inhibition ofcholinesterase was observed when these groups were placedmeta to each other as in neostigmine, a more active and usefulagent. Although physostigmine contains a methylcarbamatefunctional group, greater chemical stability towardhydrolysis was obtained with the dimethylcarbamyl group inneostigmine.
安全性プロファイル
Poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. When heated to decomposition it emits very toxic fumes of Br-, NH3, and NOx. See also CARBAMATES and BROMIDES.
純化方法
Crystallise neostigmine bromide from EtOH/diethyl ether. Its solubility in H2O is ~50%. [Beilstein 13 III 939.] (It is cholinergic and highly TOXIC.) The starting material 3-dimethylcarbamoyl-N,N-dimethylaniline [59-99-4] has b 195o/20mm [Beilstein 13 III 936], and its picrate has m 138o (from EtOH).
ネオスチグミン ブロミド 上流と下流の製品情報
原材料
準備製品