{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,16]],"date-time":"2026-03-16T10:43:27Z","timestamp":1773657807412,"version":"3.50.1"},"reference-count":26,"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":2950,"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":[[2001,1]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The mechanism of Na<jats:sup>+<\/jats:sup> channel block by three macrocyclic polyamine derivatives and two spider toxins was studied with voltage clamp and internal perfusion method in squid axons.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>All these chemicals specifically block Na<jats:sup>+<\/jats:sup> channels in the open state only from the internal surface, and do not affect K<jats:sup>+<\/jats:sup> channels.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The blocking effect is enhanced as the depolarizing pulse becomes larger. Blocked channels are unable to shift to the inactivated state.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In the case of cyclam and guanidyl\u2010side armed cyclam (G\u2010cyclam), quick release of these chemicals from the binding sites is proven by the increase in the tail current and prolongation of the time course of the off gating current. On the other hand, in the presence of N\u20104 and the spider toxins, their detachment was delayed significantly.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Molecular requirements for the block of Na<jats:sup>+<\/jats:sup> channels by these molecules are the presence of positive charge and hydrophobicity.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2001) <jats:bold>132<\/jats:bold>, 63\u201372; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0703765\">10.1038\/sj.bjp.0703765<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0703765","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T21:06:00Z","timestamp":1106946360000},"page":"63-72","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Novel mechanism of blocking axonal Na<sup>+<\/sup> channels by three macrocyclic polyamine analogues and two spider toxins"],"prefix":"10.1111","volume":"132","author":[{"given":"Masuhide","family":"Yakehiro","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yasuo","family":"Furukawa","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tohru","family":"Koike","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eiichi","family":"Kimura","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Terumi","family":"Nakajima","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kaoru","family":"Yamaoka","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Issei","family":"Seyama","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.2183\/pjab.62.359"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1085\/jgp.54.5.553"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1152\/physrev.1981.61.3.644"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1085\/jgp.63.5.533"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1085\/jgp.70.5.567"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1085\/jgp.80.5.641"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-3495(79)85202-9"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0896-6273(00)80680-7"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1113\/jphysiol.1970.sp009297"},{"key":"e_1_2_7_11_1","first-page":"225","article-title":"Mechanism of frequency\u2010dependent inhibition of sodium currents in frog myelinated nerve by the lidocaine derivative GEA 968","volume":"195","author":"COURTNEY K.R.","year":"1975","journal-title":"J. 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