{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,13]],"date-time":"2026-10-13T16:59:16Z","timestamp":1791910756475,"version":"4.3.4"},"reference-count":27,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2009,1,30]],"date-time":"2009-01-30T00:00:00Z","timestamp":1233273600000},"content-version":"vor","delay-in-days":2040,"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":[[2003,7]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>We investigated the action of TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> on cloned Kv1.3 channels of the <jats:italic>Shaker<\/jats:italic> subfamily of voltage\u2010gated potassium channels, using the voltage\u2013clamp technique. Highly purified TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> was obtained from the venom of the Brazilian scorpion <jats:italic>Tityus serrulatus<\/jats:italic> using a new purification protocol. Our results show that TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> blocks Kv1.3 with high affinity in two expression systems.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> blockade of Kv1.3 channels expressed in <jats:italic>Xenopus<\/jats:italic> oocytes was found to be completely reversible and to exhibit a pH dependence. The <jats:italic>K<\/jats:italic><jats:sub>D<\/jats:sub> was 3.9 n<jats:sc>M<\/jats:sc> at pH 7.5, 9.5 n<jats:sc>M<\/jats:sc> at pH 7.0 and 94.5 n<jats:sc>M<\/jats:sc> at pH 6.5.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The blocking properties of TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> in a mammalian cell line (L929), stably transfected to express Kv1.3, were studied using the patch\u2013clamp technique. In this preparation, the toxin had a <jats:italic>K<\/jats:italic><jats:sub>D<\/jats:sub> of 19.8 n<jats:sc>M<\/jats:sc> at pH 7.4.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> was found to affect neither the voltage\u2010dependence of activation, nor the activation and deactivation time constants. The block appeared to be independent of the transmembrane voltage and the toxin did not interfere with the C\u2010type inactivation process.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Taken as a whole, our findings indicate that TsTX\u2010K<jats:italic>\u03b1<\/jats:italic> acts as a simple blocker of Kv1.3 channels. It is concluded that this toxin is a useful tool for probing not only the physiological roles of Kv1.2, but also those mediated by Kv1.3 channels.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2003) <jats:bold>139<\/jats:bold>, 1180\u20131186. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0705343\">10.1038\/sj.bjp.0705343<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0705343","type":"journal-article","created":{"date-parts":[[2003,7,18]],"date-time":"2003-07-18T16:12:02Z","timestamp":1058544722000},"page":"1180-1186","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":32,"title":["Tityustoxin\u2010K(alpha) blockade of the voltage\u2010gated potassium channel Kv1.3"],"prefix":"10.1111","volume":"139","author":[{"given":"Aldo Rogelis A","family":"Rodrigues","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eliane C","family":"Arantes","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Francisco","family":"Monje","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Walter","family":"Stuhmer","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wamberto Antonio","family":"Varanda","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,30]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/0896-6273(95)90104-3"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/0041-0101(89)90102-5"},{"key":"e_1_2_7_4_1","first-page":"932","article-title":"Polypeptide toxins from the venoms of old world and new world scorpion preferentially block different potassium channels","volume":"40","author":"BLAUSTEIN M.P.","year":"1991","journal-title":"Mol. 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