Name | ambenonium chloride |
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Synonyms |
Ambestigmin
EINECS 204-107-5 Mytelase Ambenonium Dichloride MFCD00153762 |
Description | Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE)[1][2]. |
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Related Catalog | |
Target |
Acetylcholinesterase:0.7 nM (IC50) Acetylcholinesterase:0.12 nM (Ki) Butyrylcholinesterase:7 μM (IC50) |
In Vitro | Ambenonium chloride inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant Ki of 0.12 nM against hAChE[1]. Ambenonium chloride shows inhibitory effect towards BChE with an IC50 value of 7 μM (hBChE)[2]. |
In Vivo | Ambenonium chloride (6 mg/kg; p.o.; daily; 30-60 d) results an adverse effect on neuromuscular transmission in long-term administration, and induces hypersensitivity to stimulation in myasthenia gravis mice modle[3]. Ambenonium chloride (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates[3]. Animal Model: Female Sprague Dawley rats (weight 250 g) with myasthenia gravis[3] Dosage: 6 mg/kg Administration: Oral gavage; daily; 14, 30, 60, 90, 360 days (Stop administration 24 h in advance) Result: Resulted general activity decreasing and hypersensity to stimulation in rats during day 30-60, but these behaviors disappeared on day 90. Induced degeneration and simplification of the postsynaptic folds, widening of the synaptic clefts, increased number of the postsynaptic vesicles, and reduction in the number of the AChR in the postsynaptic membrane on days 360. |
References |
Melting Point | 196-199° |
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Molecular Formula | C28H42Cl4N4O2 |
Molecular Weight | 608.47100 |
Exact Mass | 606.20600 |
PSA | 58.20000 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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Hazard Codes | T+ |
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Risk Phrases | R28 |
Safety Phrases | S28;S45;S36/S37 |
RIDADR | UN 2811 6.1/PG 2 |