产品
编 号：F377439
分子式：C28H50Cl4N4O6
分子量：680.53
分子式：C28H50Cl4N4O6
分子量：680.53
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CAS No: 52022-31-8
产品详情
生物活性：
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
体内研究：
Ambenonium dichloride tetrahydrate (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.Ambenonium dichloride tetrahydrate (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates.Animal Model:Female Sprague Dawley rats (weight 250 g) with myasthenia gravis
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 day 360.
体外研究：
Ambenonium dichloride tetrahydrate inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant Ki of 0.12 nM against hAChE.Ambenonium dichloride tetrahydrate shows inhibitory effect towards BChE with an IC50 value of 7 μM (hBChE).
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
体内研究：
Ambenonium dichloride tetrahydrate (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.Ambenonium dichloride tetrahydrate (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates.Animal Model:Female Sprague Dawley rats (weight 250 g) with myasthenia gravis
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 day 360.
体外研究：
Ambenonium dichloride tetrahydrate inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant Ki of 0.12 nM against hAChE.Ambenonium dichloride tetrahydrate shows inhibitory effect towards BChE with an IC50 value of 7 μM (hBChE).
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