Pyridostigmine-d3 is intended for use as an internal standard for the quantification of pyridostigmine by GC- or LC-MS. Pyridostigmine is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE; IC50s = 0.35 and 1 μM, respectively, for the human enzymes).1 Pyridostigmine (10 µM) reduces decreases in AChE activity induced by the organophosphate pesticides diisopropyl fluorophosphate, chlorpyrifos-oxon, diazinon-oxon, paraoxon, and malaoxon in isolated bovine red blood cells.2 It also reduces soman-induced membrane depolarization and decreases in AChE activity in isolated human muscle bundles in a concentration-dependent manner.3 Pyridostigmine (3 mg/kg per day for four weeks) prevents tachycardia and increases in sympathetic tone in mice following myocardial infarction induced by left coronary artery ligation.4 Formulations containing pyridostigmine have been used in the treatment of myasthenia gravis and as neuromuscular protective agents against organophosphate poisoning.
1.Strelnik, A.D., Petukhov, A.S., Zueva, I.V., et al.Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profileBioorg. Med. Chem. Lett.26(16)4092-4094(2016) 2.Henderson, J.D., Glucksman, G., Leong, B., et al.Pyridostigmine bromide protection against acetylcholinesterase inhibition by pesticidesJ. Biochem. Mol. Toxicol.26(1)31-34(2012) 3.Maselli, R.A., Henderson, J.D., Ng, J., et al.Protection of human muscle acetylcholinesterase from soman by pyridostigmine bromideMuscle Nerve43(4)591-595(2011) 4.Durand, M.T., Becari, C., de Oliveira, M., et al.Pyridostigmine restores cardiac autonomic balance after small myocardial infarction in micePLoS One9(8)e104476(2014)