{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,16]],"date-time":"2026-10-16T14:11:33Z","timestamp":1792159893785,"version":"4.4.0"},"reference-count":54,"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":2585,"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":[[2002,1]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>This study examined the action of gabapentin (gabapentin,1\u2010(aminomethyl) cyclohexane acetic acid (Neurontin\u00ae)) on voltage\u2010gated calcium (Ca<jats:sup>2+<\/jats:sup>) channel influx recorded in cultured rat dorsal root ganglion (DRG) neurones.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Voltage\u2010gated Ca<jats:sup>2+<\/jats:sup> influx was monitored using both fura\u20102 based fluorescence Ca<jats:sup>2+<\/jats:sup> imaging and the whole\u2010cell patch clamp technique.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Imaging of intracellular Ca<jats:sup>2+<\/jats:sup> transients revealed that gabapentin inhibited KCl (30\u2003m<jats:sc>M<\/jats:sc>)\u2010evoked voltage\u2010dependent Ca<jats:sup>2+<\/jats:sup> influx. Both the duration for 50% of the maximum response (W50) and total Ca<jats:sup>2+<\/jats:sup> influx were significantly reduced by \u223c25\u201030% in the presence of gabapentin (25\u2003\u03bc<jats:sc>M<\/jats:sc>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Gabapentin potently inhibited the peak whole\u2010cell Ca<jats:sup>2+<\/jats:sup> channel current (I<jats:sub>Ba<\/jats:sub>) in a dose\u2010dependent manner with an estimated IC<jats:sub>50<\/jats:sub> value of 167\u2003n<jats:sc>M<\/jats:sc>. Block was incomplete and saturated at a maximal concentration of 25\u2003\u03bc<jats:sc>M<\/jats:sc>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Inhibition was significantly decreased in the presence of the neutral amino acid <jats:sc>L<\/jats:sc>\u2010isoleucine (25\u2003\u03bc<jats:sc>M<\/jats:sc>) but unaffected by application of the GABA<jats:sub>B<\/jats:sub> antagonist, saclofen (200\u2003\u03bc<jats:sc>M<\/jats:sc>), suggesting a direct action on the \u03b1<jats:sub>2<\/jats:sub>\u03b4 subunit of the Ca<jats:sup>2+<\/jats:sup> channel.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Gabapentin inhibition was voltage\u2010dependent, producing an \u223c7\u2003mV hyperpolarizing shift in current voltage properties and reducing a non\u2010inactivating component of whole\u2010cell current activated at relatively depolarized potentials.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The use of specific Ca<jats:sup>2+<\/jats:sup> channel antagonists revealed a mixed pharmacology of the gabapentin\u2010sensitive current (N\u2010, L\u2010 and P\/Q\u2010type), which is dominated by N\u2010type current.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The present study is the first to demonstrate that gabapentin directly mediates inhibition of voltage\u2010gated Ca<jats:sup>2+<\/jats:sup> influx in DRG neurones, providing a potential means for gabapentin to effectively mediate spinal anti\u2010nociception.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2002) <jats:bold>135<\/jats:bold>, 257\u2013265; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0704439\">10.1038\/sj.bjp.0704439<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0704439","type":"journal-article","created":{"date-parts":[[2006,6,7]],"date-time":"2006-06-07T19:20:37Z","timestamp":1149708037000},"page":"257-265","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":194,"title":["Gabapentin inhibits high\u2010threshold calcium channel currents in cultured rat dorsal root ganglion neurones"],"prefix":"10.1111","volume":"135","author":[{"given":"K G","family":"Sutton","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"D J","family":"Martin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R D","family":"Pinnock","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"K","family":"Lee","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R H","family":"Scott","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":"10.1001\/jama.280.21.1831"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.273.39.25458"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0885-3924(99)00033-0"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0304-3940(99)00057-9"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1097\/00000542-200004000-00031"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1007\/s002100000275"},{"key":"e_1_2_7_8_1","first-page":"145","article-title":"Gabapentin in the prophylaxis of migraine: a double\u2010blind randomized placebo\u2010controlled study","volume":"151","author":"DI TRAPANI G.","year":"2000","journal-title":"Clin. 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