{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,14]],"date-time":"2026-05-14T13:32:41Z","timestamp":1778765561506,"version":"3.51.4"},"reference-count":45,"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":516,"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":[[2007,9]]},"abstract":"<jats:sec><jats:title>Background and purpose:<\/jats:title><jats:p>Blockade of AMPA (\u03b1\u2010amino\u20103\u2010hydroxy\u20105\u2010methyl\u20104\u2010isoxazolepropionic acid) receptors is a good treatment option for a variety of central nervous system disorders. The present study evaluated the neuroprotective and anticonvulsant effects of EGIS\u20108332, a non\u2010competitive AMPA receptor antagonist, as a potential drug candidate.<\/jats:p><\/jats:sec><jats:sec><jats:title>Experimental approach:<\/jats:title><jats:p>AMPA antagonist effects of EGIS\u20108332 were measured using patch\u2010clamp techniques. Neuroprotective and anticonvulsant effects of EGIS\u20108332 were evaluated in various experimental models, relative to those of GYKI 53405.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key results:<\/jats:title><jats:p>EGIS\u20108332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA\u2010 and quisqualate\u2010induced excitotoxicity in primary cultures of telencephalon neurons (IC<jats:sub>50<\/jats:sub>=5.1\u20109.0\u2003<jats:italic>\u03bc<\/jats:italic>M),<jats:italic>in vitro<\/jats:italic>. Good anticonvulsant actions were obtained in maximal electroshock\u2010, sound\u2010 and chemically\u2010induced seizures (range of ED<jats:sub>50<\/jats:sub>=1.4\u201014.0 mg kg<jats:sup>\u22121<\/jats:sup>i.p.) in mice. Four days after transient global cerebral ischaemia, EGIS\u20108332 decreased neuronal loss in the hippocampal CA1 area in gerbils and rats. EGIS\u20108332 dose\u2010dependently reduced cerebral infarct size after permanent middle cerebral artery occlusion in mice and rats (minimum effective dose=3 mg kg<jats:sup>\u22121<\/jats:sup>i.p.). Side effects of EGIS\u20108332 emerged much above its pharmacologically active doses. A tendency for better efficacy of GYKI 53405 than that of EGIS\u20108332 was observed in anticonvulsant tests that reached statistical significance in few cases, while the contrary was perceived in cerebral ischaemia tests.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusions and implications:<\/jats:title><jats:p>EGIS\u20108332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic>(2007)<jats:bold>152<\/jats:bold>, 151\u2013160; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0707362\">10.1038\/sj.bjp.0707362<\/jats:ext-link><\/jats:p><\/jats:sec>","DOI":"10.1038\/sj.bjp.0707362","type":"journal-article","created":{"date-parts":[[2007,7,2]],"date-time":"2007-07-02T12:34:52Z","timestamp":1183379692000},"page":"151-160","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Neuroprotective and anticonvulsant effects of EGIS\u20108332, a non\u2010competitive AMPA receptor antagonist, in a range of animal models"],"prefix":"10.1111","volume":"152","author":[{"given":"G","family":"Gigler","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"K","family":"M\u00f3ricz","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M","family":"\u00e1goston","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"A","family":"Sim\u00f3","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M","family":"Albert","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"A","family":"Benedek","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G","family":"Kapus","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"S","family":"Kert\u00e9sz","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M","family":"Vegh","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"J","family":"Bark\u00f3czy","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"B","family":"Mark\u00f3","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G","family":"Szab\u00f3","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"\u00c9","family":"Matucz","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"I","family":"Gacs\u00e1lyi","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G","family":"L\u00e9vay","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"suffix":"Jr","given":"L G","family":"H\u00e1rsing","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G","family":"Sz\u00e9n\u00e1si","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0968-0896(00)00133-4"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0028-3908(96)00156-6"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(99)00541-5"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1038\/jcbfm.1988.88"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0361-9230(97)00025-7"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/0920-1211(91)90018-B"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1212\/WNL.58.11.1680"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.2628027100"},{"key":"e_1_2_8_10_1","doi-asserted-by":"crossref","first-page":"7","DOI":"10.1016\/S0031-6997(24)01394-2","article-title":"The glutamate receptor ion channels","volume":"51","author":"Dingledine R","year":"1999","journal-title":"Pharmacol Rev"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm0580003"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainresbull.2005.03.012"},{"key":"e_1_2_8_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainresbull.2005.08.018"},{"key":"e_1_2_8_14_1","doi-asserted-by":"publisher","DOI":"10.1023\/A:1025666207754"},{"key":"e_1_2_8_15_1","doi-asserted-by":"publisher","DOI":"10.3109\/10520298009067258"},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm991086d"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejphar.2005.06.031"},{"key":"e_1_2_8_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0361-9230(99)00186-0"},{"key":"e_1_2_8_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ncl.2005.10.004"},{"key":"e_1_2_8_20_1","first-page":"333","article-title":"A pharmacological investigation of 2,5\u2010bis\u2010(3\u2010diethylaminopropylamino) benzoquinone\u2010bis\u2010benzylchloride (WIN 2747): a new curarimimetic drug","volume":"100","author":"Hoppe JO","year":"1950","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_8_21_1","doi-asserted-by":"publisher","DOI":"10.1007\/BF00401402"},{"key":"e_1_2_8_22_1","doi-asserted-by":"publisher","DOI":"10.1615\/CritRevNeurobiol.v16.i12.140"},{"key":"e_1_2_8_23_1","doi-asserted-by":"publisher","DOI":"10.1023\/B:PHAM.0000016245.74809.41"},{"key":"e_1_2_8_24_1","doi-asserted-by":"publisher","DOI":"10.1254\/jjp.74.253"},{"key":"e_1_2_8_25_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(97)01046-7"},{"key":"e_1_2_8_26_1","doi-asserted-by":"publisher","DOI":"10.1056\/NEJMoa052980"},{"key":"e_1_2_8_27_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-8993(02)03700-9"},{"key":"e_1_2_8_28_1","first-page":"18","article-title":"The reliability of graphic estimates of relative potency from dose\u2013per cent effect curves","volume":"108","author":"Litchfield JT","year":"1953","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_8_29_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0028-3908(96)00155-4"},{"key":"e_1_2_8_30_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainres.2004.05.098"},{"key":"e_1_2_8_31_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainres.2006.09.043"},{"key":"e_1_2_8_32_1","doi-asserted-by":"crossref","first-page":"1492","DOI":"10.1016\/S0022-3565(24)38297-7","article-title":"SPD 502: a water\u2010soluble and in vivo long\u2010lasting AMPA antagonist with neuroprotective activity","volume":"289","author":"Nielsen EO","year":"1999","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_8_33_1","doi-asserted-by":"publisher","DOI":"10.2174\/0929867013373877"},{"key":"e_1_2_8_34_1","doi-asserted-by":"publisher","DOI":"10.1124\/pr.57.2.7"},{"key":"e_1_2_8_35_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainres.2005.12.106"},{"key":"e_1_2_8_36_1","first-page":"319","article-title":"Comparative assays of antiepileptic drugs in mice and rats","volume":"106","author":"Swinyard EA","year":"1952","journal-title":"J Pharmacol Exp Ther"},{"key":"e_1_2_8_37_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0361-9230(01)00516-0"},{"key":"e_1_2_8_38_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ddstr.2004.08.018"},{"key":"e_1_2_8_39_1","first-page":"41","article-title":"2,3\u2010Benzodiazepine AMPA antagonists","volume":"13","author":"Tarnawa I","year":"1998","journal-title":"Restor Neurol Neurosci"},{"key":"e_1_2_8_40_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.95.18.10960"},{"key":"e_1_2_8_41_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.neuint.2006.11.003"},{"key":"e_1_2_8_42_1","doi-asserted-by":"publisher","DOI":"10.2174\/1381612024607135"},{"key":"e_1_2_8_43_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568007053544129"},{"key":"e_1_2_8_44_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1471-4159.1987.tb00971.x"},{"key":"e_1_2_8_45_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.brainres.2005.06.064"},{"key":"e_1_2_8_46_1","doi-asserted-by":"publisher","DOI":"10.1016\/0920-1211(93)90054-B"}],"container-title":["British Journal of Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0707362","content-type":"unspecified","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0707362","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/pdf\/10.1038\/sj.bjp.0707362","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,1,18]],"date-time":"2025-01-18T02:37:59Z","timestamp":1737167879000},"score":1,"resource":{"primary":{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/10.1038\/sj.bjp.0707362"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2007,9]]},"references-count":45,"journal-issue":{"issue":"1","published-print":{"date-parts":[[2007,9]]}},"alternative-id":["10.1038\/sj.bjp.0707362"],"URL":"https:\/\/doi.org\/10.1038\/sj.bjp.0707362","archive":["Portico"],"relation":{},"ISSN":["0007-1188","1476-5381"],"issn-type":[{"value":"0007-1188","type":"print"},{"value":"1476-5381","type":"electronic"}],"subject":[],"published":{"date-parts":[[2007,9]]},"assertion":[{"value":"2009-01-29","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}