{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,30]],"date-time":"2026-07-30T05:05:30Z","timestamp":1785387930865,"version":"3.55.0"},"reference-count":55,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2009,1,29]],"date-time":"2009-01-29T00:00:00Z","timestamp":1233187200000},"content-version":"vor","delay-in-days":1489,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[2005,1]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>This work was aimed to determine if 1,5\u2010bis(4\u2010allyldimethylammoniumphenyl)pentan\u20103\u2010one dibromide (BW284c51), the most selective acetylcholinesterase inhibitor (AchEI), affects the nicotinic acetylcholine (Ach) receptor (AchR) function.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Purified <jats:italic>Torpedo<\/jats:italic> nicotinic AchRs were injected into <jats:italic>Xenopus laevis<\/jats:italic> oocytes and BW284c51 effects on Ach\u2010 and carbamylcholine (Cch)\u2010elicited currents were assessed using the voltage\u2010clamp technique.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>BW284c51 (up to 1\u2003m<jats:sc>M<\/jats:sc>) did not evoke any change in the oocyte membrane conductance. When BW284c51 (10\u2003p<jats:sc>M<\/jats:sc>\u2013100\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc>) and Ach were coapplied, Ach\u2010evoked currents (<jats:italic>I<\/jats:italic><jats:sub>Ach<\/jats:sub>) were reversibly inhibited in a concentration\u2010dependent manner (Hill coefficient, 1; IC<jats:sub>50<\/jats:sub>, 0.2\u20130.5\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> for 0.1\u20131000\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> Ach). Cch\u2010elicited currents showed a similar inhibition by BW284c51.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p><jats:italic>I<\/jats:italic><jats:sub>Ach<\/jats:sub> blockade by BW284c51 showed a strong voltage dependence, being only apparent at hyperpolarising potentials. BW284c51 also enhanced <jats:italic>I<\/jats:italic><jats:sub>Ach<\/jats:sub> desensitisation.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>BW284c51 changed the Ach concentration\u2010dependence curve of <jats:italic>Torpedo<\/jats:italic> AchR response from two\u2010site to single\u2010site kinetics, without noticeably affecting the EC<jats:sub>50<\/jats:sub> value.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The BW284c51 blocking effect was highly selective for nicotinic over muscarinic receptors. BW284c51 inhibition potency was stronger than that of tacrine, and similar to that of <jats:italic>d<\/jats:italic>\u2010tubocurarine (<jats:italic>d<\/jats:italic>\u2010TC). Coapplication of BW284c51 with either tacrine or <jats:italic>d<\/jats:italic>\u2010TC revealed synergistic inhibitory effects.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Our results indicate that BW284c51 antagonises nicotinic AchRs in a noncompetitive way by blocking the receptor channel, and possibly by other, yet unknown, mechanisms.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Therefore, besides acting as a selective AchEI, BW284c51 constitutes a powerful and reversible blocker of nicotinic AchRs that might be used as a valuable tool for understanding their function.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2005) <jats:bold>144<\/jats:bold>, 88\u201397. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0705965\">10.1038\/sj.bjp.0705965<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0705965","type":"journal-article","created":{"date-parts":[[2004,11,23]],"date-time":"2004-11-23T01:12:36Z","timestamp":1101172356000},"page":"88-97","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":27,"title":["The acetylcholinesterase inhibitor BW284c51 is a potent blocker of <i>Torpedo<\/i> nicotinic AchRs incorporated into the <i>Xenopus<\/i> oocyte membrane"],"prefix":"10.1111","volume":"144","author":[{"given":"Silvia","family":"Olivera\u2010Bravo","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Isabel","family":"Ivorra","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andr\u00e9s","family":"Morales","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.75.6.2994"},{"key":"e_1_2_7_3_1","doi-asserted-by":"crossref","first-page":"947","DOI":"10.1093\/oxfordjournals.jbchem.a123319","article-title":"Acetylcholine receptor\u2010mediated membrane current in oocytes injected with Electrophorus electricus mRNA: analyses of nicotine, succinylcholine, and decamethonium responses on the basis of the minimal model","volume":"108","author":"AOSHIMA H.","year":"1990","journal-title":"J. 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