Ambenonium (chloride)

Ambenonium is an inhibitor of acetylcholinesterase (AChE; IC₅₀ = 0.7 nM).¹ It is selective for AChE over butyrylcholinesterase (BChE; IC₅₀ = 6.82 µM). Ambenonium (10 µM) increases the secretion of amyloid precursor protein (APP) in primary rat basal forebrain cells.² It induces repetitive firing of electrically stimulated gastrocnemius muscle in anesthetized cats when administered intra-arterially at a dose of 5 µg/animal.³ Ambenonium (3 µg/animal) inhibits paralysis induced by the neuromuscular blocking agents tubocurarine or decamethonium (Item No. 24907) in anesthetized cats.⁴ Formulations containing ambenonium have previously been used in the treatment of myasthenia gravis.

WARNING This product is not for human or veterinary use.

1. Musilek, K., Komloova, M., Holas, O., et al. Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage - implications for early Myasthenia gravis treatment. Eur. J. Med. Chem. 46(2), 811-818 (2011).

2. Pakaski, M., Rakonczay, Z., and Kasa, P. Reversible and irreversible acetylcholinesterase inhibitors cause changes in neuronal amyloid precursor protein processing and protein kinase C level in vitro. Neurochem. Int. 38(3), 219-226 (2001).

3. Blaber, L.C., and Bowman, W.C. The effects of some drugs on the repetitive discharges produced in nerve and muscle by anticholinesterases. Int. J. Neuropharmacol. 2(1-2), 1-16 (1963).

4. Blaber, L.C. The antagonism of muscle relaxants by ambenonium and methoxyambenonium in the cat. Br. J. Pharmacol. Chemother. 15(3), 476-484 (1960).