| Edrophonium (chloride)acetylcholinesterase (AChE) inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.82%
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| Cas No. | 116-38-1 | SDF | Download SDF |
| Synonyms | Enlon®,Tensilon® | ||
| Chemical Name | N-ethyl-3-hydroxy-N,N-dimethyl-benzenaminium, monochloride | ||
| Canonical SMILES | OC1=CC([N+](C)(C)CC)=CC=C1.[Cl-] | ||
| Formula | C10H16NO • Cl | M.Wt | 201.7 |
| Solubility | ≥7.6mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
