Ambenonium chloride  (Synonyms: WIN 8077 chloride)

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].

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

Ambenonium chloride 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 chloride shows inhibitory effect towards BChE with an IC₅₀ value of 7 μM (hBChE)^[2].

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

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].

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

608.47

C₂₈H₄₂Cl₄N₄O₂

115-79-7

Room temperature in continental US; may vary elsewhere.

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

• [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]