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Decamethonium is a depolarizing neuromuscular blocking agent.1 It is a partial agonist of muscle-type nicotinic acetylcholine receptors (nAChRs).2 Decamethonium activates α1β1-containing adult mouse muscle-type nAChRs expressed in X. laevis oocytes with an EC50 value of 40 µM using voltage clamp electrophysiology. It is also a nondepolarizing antagonist of neuronal-type nAChRs, inhibiting mouse α7-, α3β2-, α3β4-, and α4β2-containing receptors with IC50 values of 7.4, 405, 28, and 59 µM, respectively. Decamethonoium is a competitive antagonist of α4β2-containing nAChRs expressed in SH-EP1 cells (IC50 = 52 µM for the human receptor).3 It also inhibits electric eel acetylcholinesterase (AChE) and blocks electrically-evoked tibialis muscle twitches in anesthetized cats with ED95 values of 35 and 70 µg/kg for cats under chloralose and ether anesthesia, respectively.1,4 Formulations containing decamethonium have been used to induce paralysis during anesthesia.
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1. The action of D-
2. Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes. J. Pharmacol. Exp. Ther. 333(2), 501-518 (2010).
3. Characterization of human α4β2-
4. Effects of edrophonium, serine, decamethonium, d-