{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,5,14]],"date-time":"2025-05-14T04:19:28Z","timestamp":1747196368298,"version":"3.40.5"},"reference-count":32,"publisher":"Public Library of Science (PLoS)","issue":"10","license":[{"start":{"date-parts":[[2023,10,12]],"date-time":"2023-10-12T00:00:00Z","timestamp":1697068800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Osaka Medical and Pharmaceutical University"},{"name":"Osaka Medical and Pharmaceutical University"}],"content-domain":{"domain":["www.plosone.org"],"crossmark-restriction":false},"short-container-title":["PLoS ONE"],"abstract":"<jats:p>Muscle relaxants are indispensable for surgical anesthesia. Early studies suggested that a classical non-depolarizing muscle relaxant pancuronium competitively binds to the ligand binding site to block nicotinic acetylcholine receptors (nAChR). Our group recently showed that nAChR which has two distinct subunit combinations are expressed in zebrafish muscles, \u03b1\u03b2\u03b4\u03b5 and \u03b1\u03b2\u03b4, for which potencies of pancuronium are different. Taking advantage of the distinct potencies, we generated chimeras between two types of nAChRs and found that the extracellular ACh binding site is not associated with the pancuronium sensitivity. Furthermore, application of either 2 \u03bcM or 100 \u03bcM ACh in native \u03b1\u03b2\u03b4\u03b5 or \u03b1\u03b2\u03b4 subunits yielded similar IC<jats:sub>50<\/jats:sub> of pancuronium. These data suggest that pancuronium allosterically inhibits the activity of zebrafish nAChRs.<\/jats:p>","DOI":"10.1371\/journal.pone.0292262","type":"journal-article","created":{"date-parts":[[2023,10,12]],"date-time":"2023-10-12T17:37:53Z","timestamp":1697132273000},"page":"e0292262","update-policy":"https:\/\/doi.org\/10.1371\/journal.pone.corrections_policy","source":"Crossref","is-referenced-by-count":1,"title":["Allosteric inhibition of muscle-type nicotinic acetylcholine receptors by a neuromuscular blocking agent pancuronium"],"prefix":"10.1371","volume":"18","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9655-4299","authenticated-orcid":true,"given":"Souhei","family":"Sakata","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fumihito","family":"Ono","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"340","published-online":{"date-parts":[[2023,10,12]]},"reference":[{"issue":"6","key":"pone.0292262.ref001","doi-asserted-by":"crossref","first-page":"551","DOI":"10.1046\/j.1365-2044.2000.01423.x","article-title":"Prelude to pancuronium and vecuronium","volume":"55","author":"AG McKenzie","year":"2000","journal-title":"Anaesthesia"},{"issue":"12","key":"pone.0292262.ref002","doi-asserted-by":"crossref","first-page":"565","DOI":"10.1007\/BF02958903","article-title":"The pharmacology of pancuronium bromide: a new non-depolarising neuromuscular blocking agent","volume":"7","author":"WR Buckett","year":"1968","journal-title":"Ir J Med Sci"},{"issue":"3","key":"pone.0292262.ref003","doi-asserted-by":"crossref","first-page":"671","DOI":"10.1111\/j.1476-5381.1968.tb00466.x","article-title":"The pharmacology of pancuronium bromide (Org.NA97), a new potent steroidal neuromuscular blocking agent","volume":"32","author":"WR Buckett","year":"1968","journal-title":"Br J Pharmacol Chemother"},{"issue":"7","key":"pone.0292262.ref004","doi-asserted-by":"crossref","first-page":"363","DOI":"10.1177\/014107680209500713","article-title":"Neuromuscular blocking drugs: discovery and development","volume":"95","author":"T. 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