Propofol is a widely used general anaesthetic with muscle relaxant properties. Similarly as\npropofol, the new general anaesthetic AZD3043 targets the GABAA receptor for its anaesthetic effects,\nbut the interaction with nicotinic acetylcholine receptors (nAChRs) has not been investigated. Notably,\nthere is a gap of knowledge about the interaction between propofol and the nAChRs found in the adult\nneuromuscular junction. The objective was to evaluate whether propofol or AZD3043 interact with\nthe �±1�²1�´�µ, �±3�²2, or �±7 nAChR subtypes that can be found in the neuromuscular junction and if there\nare any differences in affinity for those subtypes between propofol and AZD3043. Human nAChR\nsubtypes �±1�²1�´�µ, �±3�²2, and �±7 were expressed into Xenopus oocytes and studied with an automated\nvoltage-clamp. Propofol and AZD3043 inhibited ACh-induced currents in all of the nAChRs studied\nwith inhibitory concentrations higher than those needed for general anaesthesia. AZD3043 was\na more potent inhibitor at the adult muscle nAChR subtype compared to propofol. Propofol and\nAZD3043 inhibit nAChR subtypes that can be found in the adult NMJ in concentrations higher\nthan needed for general anaesthesia. This finding needs to be evaluated in an in vitro nerve-muscle\npreparation and suggests one possible explanation for the muscle relaxant effect of propofol seen\nduring higher doses.
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