塩化 アセチルコリン 化学特性,用途語,生産方法
外観
白色, 結晶性粉末又は塊
溶解性
水, エタノールに易溶。エーテル, ベンゼンに不溶。水に極めて溶けやすく、エタノールに溶けやすい。
用途
薬理研究用(副交感神経興奮作用)、神経伝達研究用。
効能
縮瞳薬, 末梢血管拡張薬, コリン受容体作動薬
商品名
オビソート (第一三共)
使用上の注意
吸湿性がある。
説明
Acetylcholine is a neurotransmitter that binds to nicotinic and muscarinic acetylcholine receptors (AChRs) in the central and peripheral nervous systems. It mediates motor function at the neuromuscular junction but also has functions in the parasympathetic and sympathetic nervous systems. It is involved in learning and memory through actions at nicotinic AChRs in the CNS. The actions of acetylcholine are terminated primarily
via the action of acetylcholinesterase, which breaks it down into acetate and choline. Acetylcholine (chloride) mimics the effects of acetylcholine and has been used to determine the function of acetylcholine in various biological processes. Acetylcholine (chloride) inhibits peptide aggregation of p53 mutants
in vitro at micromolar concentrations. It increases alveolar fluid clearance in a dose-dependent manner and enhances Na
+/K
+-ATPase activity, effects which are blocked by atropine , in a mouse model of pulmonary edema.
化学的特性
White or almost white crystalline powder or colourless crystals, very hygroscopic.
使用
Acetylcholine Chloride is a cholinergic.
定義
ChEBI: The chloride salt of acetylcholine, and a parasympatomimetic drug.
一般的な説明
ACh chloride exerts a powerfulstimulant effect on the parasympathetic nervous system.Attempts have been made to use it as a cholinergic agent,but its duration of action is too short for sustained effects,because of rapid hydrolysis by esterases and lack of specificitywhen administered for systemic effects. It is a cardiacdepressant and an effective vasodilator. Stimulation of thevagus and the parasympathetic nervous system produces atonic action on smooth muscle and induces a flow from thesalivary and lacrimal glands. Its cardiac-depressant effectresults from (a) a negative chronotropic effect that causes adecrease in heart rate and (b) a negative inotropic action onheart muscle that produces a decrease in the force of myocardialcontractions.
生物活性
Endogenous neurotransmitter. Acts at nicotinic and muscarinic acetylcholine receptors.
臨床応用
Atropine blocks the depressant effect of ACh on cardiacmuscle and its production of peripheral vasodilation (i.e.,muscarinic effects) but does not affect the skeletal musclecontraction (i.e., nicotinic effect) produced.ACh chloride is a hygroscopic powder that is available inan admixture with mannitol to be dissolved in sterile waterfor injection shortly before use. It is a short-acting mioticwhen introduced into the anterior chamber of the eye and isespecially useful after cataract surgery during the placementof sutures. When applied topically to the eye, it has littletherapeutic value because of poor corneal penetration andrapid hydrolysis by AChE.
安全性プロファイル
Poison by subcutaneous, intravenous, and parenteral routes. Moderately toxic by ingestion. When heated to decomposition it emits very toxic fumes of NOx, and Cl-. A cholinergic agent. See also CHOLINE ACETATE (ESTER).
純化方法
It is very soluble in H2O (>10%), and is very hygroscopic. If pasty, dry it in a vacuum desiccator over H2SO4 until a solid residue is obtained. Dissolve this in absolute EtOH, filter it and add dry Et2O, when the hydrochloride separates. Collect by filtration and store it under very dry conditions. [Jones & Major J Am Chem Soc 52 307 1930.] The chloroplatinate crystallises from hot H2O in yellow needles and can be recrystallised from 50% EtOH, m 242-244o [Dudley Biochem J 23 1069 1929]; other m given is 256-257o. The perchlorate crystallises from EtOH as prisms m 116-117o. [J Am Pharm Assocn 36 272 1947, Beilstein 4 IV 1446.]
塩化 アセチルコリン 上流と下流の製品情報
原材料
準備製品