Ambenonium dichloride tetrahydrate (Synonyms: WIN 8077 dichloride tetrahydrate)

Cat. No.: HY-118533A: FAQs
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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).

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Ambenonium dichloride tetrahydrate Chemical Structure

CAS No. : 52022-31-8

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Description

IC₅₀ & Target

IC50: 0.7 nM (hAChE), 7 μM (hBChE)^[1]

In Vitro

Ambenonium dichloride tetrahydrate inhibits Acetyicholinesterase (AChE) in a rapidly reversible method, and shows strong inhibition with inhibition constant K_i of 0.12 nM against hAChE^[1].
Ambenonium dichloride tetrahydrate shows inhibitory effect towards BChE with an IC₅₀ value of 7 μM (hBChE)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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^[3].
Ambenonium dichloride tetrahydrate (6 mg/kg; p.o.; daily; 14 d) decreases the number of AChR in motorend-plates^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 day 360.

Molecular Weight

680.53

Formula

C₂₈H₅₀Cl₄N₄O₆

CAS No.

52022-31-8

SMILES

O=C(NCC[N+](CC)(CC)CC1=CC=CC=C1Cl)C(NCC[N+](CC)(CC)CC2=CC=CC=C2Cl)=O.[Cl-].[Cl-].O.O.O.O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hodge AS, et al. Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities. Mol Pharmacol. 1992 May. 41(5):937-42. [Content Brief]

[2]. Komloova M, et al. Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment. Bioorg Med Chem Lett. 2011 Apr 15. 21(8):2505-9. [Content Brief]

[3]. Hazama R, et al. Effects of long-term administration of ambenonium chloride on motor end-plate fine structure and acetylcholine receptor in rat. J Neurol Sci. 1981 Jul. 51(1):69-79. [Content Brief]

Ambenonium dichloride tetrahydrate Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ambenonium dichloride tetrahydrate52022-31-8WIN 8077 dichloride tetrahydrateCholinesterase (ChE)Myasthenia Gravismotor endplateAcetyicholinesteraseneuromuscular transmissionInhibitorinhibitorinhibit

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