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Pharmaceuticals 2016, 9(1), 8; doi:10.3390/ph9010008

Propofol and AZD3043 Inhibit Adult Muscle and Neuronal Nicotinic Acetylcholine Receptors Expressed in Xenopus Oocytes

1
Department of Anesthesiology, Surgical Services and Intensive Care Medicine, Karolinska University Hospital, SE-171 76 Stockholm, Sweden
2
Department of Physiology and Pharmacology, Section for Anesthesiology and Intensive Care Medicine, Karolinska Institutet, SE-171 76 Stockholm, Sweden
3
Department of Neuroscience, AstraZeneca Research and Development, CNS&Pain Innovative Medicines, AstraZeneca R&D, SE-151 85, Södertälje, Sweden
Present address: Ipsen Innovation, 91140 Les Ulis, France.
Present address: Pelago Biosciences AB, 171 65 Solna, Sweden.
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 17 December 2015 / Revised: 27 January 2016 / Accepted: 29 January 2016 / Published: 6 February 2016
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Abstract

Propofol is a widely used general anaesthetic with muscle relaxant properties. Similarly as propofol, the new general anaesthetic AZD3043 targets the GABAA receptor for its anaesthetic effects, but the interaction with nicotinic acetylcholine receptors (nAChRs) has not been investigated. Notably, there is a gap of knowledge about the interaction between propofol and the nAChRs found in the adult neuromuscular junction. The objective was to evaluate whether propofol or AZD3043 interact with the α1β1δε, α3β2, or α7 nAChR subtypes that can be found in the neuromuscular junction and if there are any differences in affinity for those subtypes between propofol and AZD3043. Human nAChR subtypes α1β1δε, α3β2, and α7 were expressed into Xenopus oocytes and studied with an automated voltage-clamp. Propofol and AZD3043 inhibited ACh-induced currents in all of the nAChRs studied with inhibitory concentrations higher than those needed for general anaesthesia. AZD3043 was a more potent inhibitor at the adult muscle nAChR subtype compared to propofol. Propofol and AZD3043 inhibit nAChR subtypes that can be found in the adult NMJ in concentrations higher than needed for general anaesthesia. This finding needs to be evaluated in an in vitro nerve-muscle preparation and suggests one possible explanation for the muscle relaxant effect of propofol seen during higher doses. View Full-Text
Keywords: anesthesia; intravenous anesthesia; propofol; AZD3043; nicotinic achetylcholine receptors anesthesia; intravenous anesthesia; propofol; AZD3043; nicotinic achetylcholine receptors
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MDPI and ACS Style

Jonsson Fagerlund, M.; Krupp, J.; Dabrowski, M.A. Propofol and AZD3043 Inhibit Adult Muscle and Neuronal Nicotinic Acetylcholine Receptors Expressed in Xenopus Oocytes. Pharmaceuticals 2016, 9, 8.

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