{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,1]],"date-time":"2026-05-01T15:03:46Z","timestamp":1777647826330,"version":"3.51.4"},"reference-count":23,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,1,30]],"date-time":"2009-01-30T00:00:00Z","timestamp":1233273600000},"content-version":"vor","delay-in-days":3348,"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":[[1999,12]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The functional and electrophysiological effects of IMID\u20104F (2\u2010[<jats:italic>N<\/jats:italic>\u2010(2,6\u2010dichlorophenyl)\u2010<jats:italic>N<\/jats:italic>\u2010(4\u2010flurorobenzyl)amino]imidazoline), a fluoro\u2010benzyl derivative of clonidine, on vascular K<jats:sub>ATP<\/jats:sub> channels were investigated. In pig coronary artery, IMID\u20104F inhibited the vasorelaxation response to the K<jats:sub>ATP<\/jats:sub> channel opener levcromakalim with a pK<jats:sub>B<\/jats:sub> value of approximately 7.1. IMID\u20104F (30\u2003\u03bc<jats:sc>M<\/jats:sc>) did not affect the vasorelaxation response to sodium nitroprusside (SNP).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In rat mesenteric artery smooth muscle cells IMID\u20104F (1\u201310\u2003\u03bc<jats:sc>M<\/jats:sc>) caused a concentration\u2010dependent depolarization of membrane potential. IMID\u20104F (10\u2003\u03bc<jats:sc>M<\/jats:sc>) abolished the hyperpolarizing effects of levcromakalim (10\u2003\u03bc<jats:sc>M<\/jats:sc>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In patch clamp experiments using rat mesenteric artery smooth muscle cells, K<jats:sub>ATP<\/jats:sub> channel currents induced by levcromakalim (10\u2003\u03bc<jats:sc>M<\/jats:sc>) were inhibited by IMID\u20104F (0.3\u20133\u2003\u03bc<jats:sc>M<\/jats:sc>) in a concentration\u2010dependent manner. The calculated IC<jats:sub>50<\/jats:sub> for IMID\u20104F inhibiting K<jats:sub>ATP<\/jats:sub> channel current was approximately 0.8\u2003\u03bc<jats:sc>M<\/jats:sc>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Radioligand binding studies using bovine aortic smooth muscle cell membranes showed that IMID\u20104F (30\u2003\u03bc<jats:sc>M<\/jats:sc>) did not displace binding to the K<jats:sub>ATP<\/jats:sub> channel opener [<jats:sup>3<\/jats:sup>H]\u2010P1075. However, both levcromakalim (10\u2003\u03bc<jats:sc>M<\/jats:sc>) and glibenclamide (10\u2003\u03bc<jats:sc>M<\/jats:sc>) caused significant displacement of [<jats:sup>3<\/jats:sup>H]\u2010P1075.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>These studies show that the imidazoline compound IMID\u20104F is one of the most potent antagonists of arterial K<jats:sub>ATP<\/jats:sub> channels identified. Vasorelaxation, hyperpolarization and K<jats:sup>+<\/jats:sup> currents through K<jats:sub>ATP<\/jats:sub> channels were all inhibited by IMID\u20104F at micromolar concentrations. Radioligand binding studies indicate that IMID\u20104F does not bind to the same site as levcromakalim or as glibenclamide. Considering other evidence, it is likely that IMID\u20104F acts by interacting directly with the pore of the K<jats:sub>IR<\/jats:sub> channel, rather than through the sulphonylurea subunit of the K<jats:sub>ATP<\/jats:sub> channel complex.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1999) <jats:bold>128<\/jats:bold>, 1636\u20131642; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702925\">10.1038\/sj.bjp.0702925<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702925","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T20:29:41Z","timestamp":1106944181000},"page":"1636-1642","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Functional and electrophysiological effects of a novel imidazoline\u2010based K<sub>ATP<\/sub> channel 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