{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,2]],"date-time":"2025-11-02T19:48:48Z","timestamp":1762112928093},"reference-count":28,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2009,2,12]],"date-time":"2009-02-12T00:00:00Z","timestamp":1234396800000},"content-version":"vor","delay-in-days":4091,"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":[[1997,12]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>In the present study, we investigated the ability of a recently introduced non\u2010xanthine A<jats:sub>2A<\/jats:sub> receptor antagonist, ZM241385 (4\u2010(2\u2010[7\u2010amino\u20102\u2010(2\u2010furyl{1,2,4}\u2010triazolo{2,3\u2010a{1,3,5}triazin\u20105\u2010yl\u2010aminoethyl)phenol) to displace binding of the prototypical A<jats:sub>2A<\/jats:sub> adenosine receptor agonist [<jats:sup>3<\/jats:sup>H]CGS21680 (2\u2010[4\u2010(2\u2010<jats:italic>p<\/jats:italic>\u2010carboxyethyl)phenylamino]\u20105\u2032\u2010<jats:italic>N<\/jats:italic>\u2010ethylcarboxamidoadenosine) and to modify the facilitatory responses caused by the A<jats:sub>2A<\/jats:sub> selective agonists, CGS21680 and HENECA (2\u2010hexynl\u20105\u2032\u2010<jats:italic>N<\/jats:italic>\u2010ethylcarboxamidoadenosine) in rat hippocampal preparations.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>ZM241385 was nearly equipotent to displace [<jats:sup>3<\/jats:sup>H]CGS21680 (30\u2003n<jats:sc>M<\/jats:sc>) binding to hippocampal (K<jats:sub>i<\/jats:sub> of 0.52\u2003n<jats:sc>M<\/jats:sc>) and to striatal membranes (K<jats:sub>i<\/jats:sub> of 0.35\u2003n<jats:sc>M<\/jats:sc>), whereas HENECA was a more potent displacer of [<jats:sup>3<\/jats:sup>H]CGS21680 binding to striatal (K<jats:sub>i<\/jats:sub> of 4.5\u2003n<jats:sc>M<\/jats:sc>) than to hippocampal membranes (K<jats:sub>i<\/jats:sub> of 19\u2003n<jats:sc>M<\/jats:sc>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>HENECA (3\u201330\u2003n<jats:sc>M<\/jats:sc>) was equipotent with CGS21680 to facilitate veratridine\u2010evoked [<jats:sup>3<\/jats:sup>H]acetylcholine release from superfused hippocampal synaptosomes and ZM241385 (20\u2003n<jats:sc>M<\/jats:sc>) inhibited the facilitatory effects of both HENECA (30\u2003n<jats:sc>M<\/jats:sc>) and CGS21680 (30\u2003n<jats:sc>M<\/jats:sc>); this antagonism was mimicked by CSC (250\u2003n<jats:sc>M<\/jats:sc>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In contrast, CGS21680 (10\u201330\u2003n<jats:sc>M<\/jats:sc>) was more potent than HENECA (10\u201330\u2003n<jats:sc>M<\/jats:sc>) to facilitate synaptic transmission in Schaffer fibres\/CA1 pyramid synapses of hippocampal slices and the facilitatory effect of CGS21680 (10\u2003n<jats:sc>M<\/jats:sc>) was blocked by ZM241385 (20\u2003n<jats:sc>M<\/jats:sc>) whereas CSC (250\u2003n<jats:sc>M<\/jats:sc>) caused a 40% attenuation of this CGS21680\u2010induced facilitation.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>These results indicate that ZM241385 is the first A<jats:sub>2A<\/jats:sub> antagonist with equal potency to displace [<jats:sup>3<\/jats:sup>H]CGS21680 binding to striatal and limbic regions, and with general efficiency to antagonize HENECA\u2010 or CGS21680\u2010mediated facilitatory responses in the hippocampus.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p>","DOI":"10.1038\/sj.bjp.0701507","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:18:18Z","timestamp":1106939898000},"page":"1279-1284","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":68,"title":["ZM241385 is an antagonist of the facilitatory responses produced by the A<sub>2A<\/sub> adenosine receptor agonists CGS21680 and HENECA in the rat hippocampus"],"prefix":"10.1111","volume":"122","author":[{"given":"Rodrigo A.","family":"Cunha","sequence":"first","affiliation":[]},{"given":"M.","family":"Dolores Constantino","sequence":"additional","affiliation":[]},{"given":"J.","family":"Alexandre Ribeiro","sequence":"additional","affiliation":[]}],"member":"311","published-online":{"date-parts":[[2009,2,12]]},"reference":[{"key":"e_1_2_5_2_1","doi-asserted-by":"publisher","DOI":"10.1089\/dna.1996.15.329"},{"key":"e_1_2_5_3_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1471-4159.1994.63010207.x"},{"key":"e_1_2_5_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(94)91066-9"},{"key":"e_1_2_5_5_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1460-9568.1994.tb00245.x"},{"key":"e_1_2_5_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/0304-3940(95)11833-I"},{"key":"e_1_2_5_7_1","doi-asserted-by":"publisher","DOI":"10.1007\/BF00168627"},{"key":"e_1_2_5_8_1","volume-title":"Excerpta Medica International Congress Series","author":"Cunha R.A.","year":"1997"},{"key":"e_1_2_5_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/0306-4522(94)90373-5"},{"key":"e_1_2_5_10_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1471-4159.1996.67010374.x"},{"key":"e_1_2_5_11_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm00062a005"},{"key":"e_1_2_5_12_1","first-page":"888","article-title":"[3H]CGS21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain","volume":"251","author":"Jarvis M.F.","year":"1989","journal-title":"J. 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