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Edrophonium(chloride)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Edrophonium(chloride)图片
CAS NO:116-38-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
250mg电议
500mg电议
1g电议

产品介绍
依曲溴铵（氯化物）是一种易可逆的乙酰胆碱酯酶抑制剂；防止神经递质乙酰胆碱的分解，并通过竞争性抑制乙酰胆碱酯酶（主要在神经肌肉接头处）起作用。
Cas No.116-38-1
别名依酚氯铵
化学名N-ethyl-3-hydroxy-N,N-dimethyl-benzenaminium, monochloride
Canonical SMILESOC1=CC([N+](C)(C)CC)=CC=C1.[Cl-]
分子式C10H16NO o Cl
分子量201.7
溶解度DMF: 0.5 mg/ml,DMSO: 2 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Store at -20°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Edrophonium is a competitive inhibitor of acetylcholinesterase (AChE) [1]. AChE is an extrinsic membrane-hound enzyme that functions in the central and peripheral nervous systems. AChE rapidly terminates the ACh receptor-mediated signal transmission by hydrolyzing Ach. Inhibition of AChE results in accumulation of ACh in the synaptic cleft and leads to impeded neurotransmission [2].

In vitro: Edrophonium inhibited AChE activity in human red blood cells, purified calf forebrain, and octopus brain with Ki values of 0.2, 0.2, and 0.4 μM, respectively. The IC50s were 0.2, 0.05, and 0.5 μM, respectively [1].

In vivo: In symptomatic patients without coronary artery disease, edrophonium (80 μg/kg, intravenous bolus) induced chest pain [3]. Edrophonium increased esophageal amplitude and repetitive contractions. Edrophonium was useful for provoking esophageal chest pain [3]. In infants and children during N2O-halothane anesthesia, the ED50 for edrophonium is 128 μg/kg for adults [4]. In patients anaesthetized with nitrous oxide and halothane undergoing kidney transplant nephrectomy or transplantation of a live related donor kidney, patients undergoing transplant nephrectomy showed a significant increase in elimination half-life and a significant decrease (67%) in serum clearance when compared with kidney transplant recipients or patients with normal renal function [5].

References:
[1] Boyle N A J, Talesa V, Giovannini E, et al.  Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase[J]. Journal of medicinal chemistry, 1997, 40(19): 3009-3013.
[2] Quinn D M.  Acetylcholinesterase: enzyme structure, reaction dynamics, and virtual transition states[J]. Chemical Reviews, 1987, 87(5): 955-979.
[3] Cronnelly R, Morris R B, Miller R D.  Edrophonium: duration of action and atropine requirement in humans during halothane anesthesia[J]. Anesthesiology, 1982, 57(4): 261-266.
[4] Fisher D M, Cronnelly R, Sharma M, et al.  Clinical pharmacology of edrophonium in infants and children[J]. Anesthesiology, 1984, 61(4): 428-433.
[5] Morris R B, Cronnelly R, Miller R D, et al.  Pharmacokinetics of edrophonium in anephric and renal transplant patients[J]. British journal of anaesthesia, 1981, 53(12): 1311-1314.