{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,13]],"date-time":"2026-02-13T13:01:50Z","timestamp":1770987710185,"version":"3.50.1"},"reference-count":51,"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":1796,"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":[[2004,3]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>2\u2010<jats:italic>p<\/jats:italic>\u2010(2\u2010carboxyethylphenethylamino\u20105\u2032\u2010ethylcarboxamidoadenosine) (CGS 21680) is considered the reference compound to study adenosine A<jats:sub>2A<\/jats:sub> receptors. However, CGS 21680 binding in the cerebral cortex, where adenosine A<jats:sub>1<\/jats:sub> receptors are predominant, displays a mixed A<jats:sub>2A<\/jats:sub>\/A<jats:sub>1<\/jats:sub> receptor pharmacology. We now use adenosine A<jats:sub>1<\/jats:sub> and A<jats:sub>2A<\/jats:sub> receptor knockout mice to investigate the characteristics of cortical [<jats:sup>3<\/jats:sup>H]CGS 21680 binding.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>[<jats:sup>3<\/jats:sup>H]CGS 21680 binding to the cerebral cortex was strongly reduced in adenosine A<jats:sub>1<\/jats:sub> receptor knockout mice, but only slightly reduced in A<jats:sub>2A<\/jats:sub> receptor knockout mice compared with the corresponding wild\u2010type littermates.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Another selective A<jats:sub>2A<\/jats:sub> receptor ligand, [<jats:sup>3<\/jats:sup>H]\u20105\u2010amino\u20107\u2010(2\u2010phenylethyl)\u20102\u2010(2\u2010furyl)\u2010pyrazolo[4,3\u2010<jats:italic>e<\/jats:italic>]\u20101,2,4\u2010triazolo[1,5\u2010<jats:italic>c<\/jats:italic>]pyrimidine ([<jats:sup>3<\/jats:sup>H]SCH 58261), displayed a saturable binding to mouse cortical membranes, albeit with a binding density 20 times lower than that of striatal membranes, and this [<jats:sup>3<\/jats:sup>H]SCH58261 binding was abolished in both striatal and cortical membranes of A<jats:sub>2A<\/jats:sub> receptor knockout mice and unchanged in A<jats:sub>1<\/jats:sub> receptor knockout mice.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The presence of A<jats:sub>2A<\/jats:sub> receptors in cortical neurons was further confirmed by Western blot in mouse cortical nerve terminal membranes.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>It is concluded that, although A<jats:sub>2A<\/jats:sub> receptors are present in the cerebral cortex, the purportedly selective A<jats:sub>2A<\/jats:sub> receptor agonist [<jats:sup>3<\/jats:sup>H]CGS 21680 binds in the cerebral cortex to an entity that requires the presence of adenosine A<jats:sub>1<\/jats:sub> receptors. Thus, CGS 21680 should be used with care in all preparations where adenosine A<jats:sub>1<\/jats:sub> receptors out\u2010number A<jats:sub>2A<\/jats:sub> receptors.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2004) <jats:bold>141<\/jats:bold>, 1006\u20131014. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0705692\">10.1038\/sj.bjp.0705692<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0705692","type":"journal-article","created":{"date-parts":[[2004,3,17]],"date-time":"2004-03-17T17:13:07Z","timestamp":1079543587000},"page":"1006-1014","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":85,"title":["Binding of the prototypical adenosine A<sub>2A<\/sub> receptor agonist CGS 21680 to the cerebral cortex of adenosine A<sub>1<\/sub> and A<sub>2A<\/sub> receptor knockout mice"],"prefix":"10.1111","volume":"141","author":[{"given":"Lu\u00edsa V","family":"Lopes","sequence":"first","affiliation":[]},{"given":"Linda","family":"Halldner","sequence":"additional","affiliation":[]},{"given":"Nelson","family":"Rebola","sequence":"additional","affiliation":[]},{"given":"Bj\u00f6rn","family":"Johansson","sequence":"additional","affiliation":[]},{"given":"Catherine","family":"Ledent","sequence":"additional","affiliation":[]},{"given":"Jian Fan","family":"Chen","sequence":"additional","affiliation":[]},{"given":"Bertil B","family":"Fredholm","sequence":"additional","affiliation":[]},{"given":"Rodrigo A","family":"Cunha","sequence":"additional","affiliation":[]}],"member":"311","published-online":{"date-parts":[[2009,1,30]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1161\/01.STR.0000060204.67672.8B"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1007\/s002100100456"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0704613"},{"key":"e_1_2_7_5_1","first-page":"331","article-title":"Characterization of the A2 adenosine receptor labelled with [3H]NECA in rat striatal membranes","volume":"29","author":"BRUNS R.F.","year":"1986","journal-title":"Mol. 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