Neostigmine is a reversible inhibitor of acetylcholinesterase (AChE; Kd = 260 μM).1 In a rat model of knee joint inflammation, intrathecal administration of neostigmine (2-30 μg) increases endogenous acetylcholine levels and dose-dependently increases the latency of paw withdrawal in response to thermal and mechanical stimuli (ED50s = 6.6 and 3.5 μg, respectively).2 Neostigmine (5 μg, i.p.) restores muscle action potentials in mice with a thymopoietin-induced neuromuscular block.3 Formulations containing neostigmine have been used in the treatment of myasthenia gravis and Ogilvie syndrome.
1.Milkani, E., Lambert, C.R., and McGimpsey, W.G.Direct detection of acetylcholinesterase inhibitor binding with an enzyme-based surface plasmon resonance sensorAnal. Biochem.408(2)212-219(2011) 2.Buerkle, H., Boschin, M., Marcus, M.A.E., et al.Central and peripheral analgesia mediated by the acetylcholinesterase-inhibitor neostigmine in the rat inflamed knee joint modelAnesth. Analg.86(5)1027-1032(1998) 3.Goldstein, G., and Schlesinger, D.H.Thymopoietin and myasthenia gravis: neostigmine-responsive neuromuscular block produced in mice by a synthetic peptide fragment of thymopoietinLancet2(7928)256-259(1975)