{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,16]],"date-time":"2026-10-16T01:08:52Z","timestamp":1792112932665,"version":"4.4.0"},"reference-count":35,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2009,1,29]],"date-time":"2009-01-29T00:00:00Z","timestamp":1233187200000},"content-version":"vor","delay-in-days":3622,"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":[[1999,3]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The previously described complex behaviour of the CCK<jats:sub>B<\/jats:sub>\/gastrin receptor antagonist, L\u2010365,260, in radioligand binding assays could be explained by a variable population of two binding sites. We have investigated whether other CCK<jats:sub>B<\/jats:sub>\/gastrin receptor ligands (PD134,308, PD140,376, YM022 and JB93182) can distinguish between these sites.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In the mouse cortex assay, Hill slopes were not different from unity and the ligand pK<jats:sub>I<\/jats:sub> values did not differ when either [<jats:sup>125<\/jats:sup>I]\u2010BH\u2010CCK\u20108S or [<jats:sup>3<\/jats:sup>H]\u2010PD140,376 was used as label as expected for a single site (G<jats:sub>2<\/jats:sub>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In the rat cortex, where previous analysis of replicate (<jats:italic>n<\/jats:italic>=48) L\u2010365,260 data indicated the presence of two CCK<jats:sub>B<\/jats:sub>\/gastrin sites (G<jats:sub>1<\/jats:sub> and G<jats:sub>2<\/jats:sub>), the competition data for PD134,308, PD140,376, YM022 and JB93182 could be explained by a homogeneous population of CCK<jats:sub>B<\/jats:sub>\/gastrin sites because the Hill slope estimates were not significantly different from unity. However, the estimated affinity values for JB93182 and YM022 were significantly higher and that for PD134,308 was significantly lower than those obtained in the mouse cortex when the same radioligand was used. In view of our previous data obtained with L\u2010365,260, the rat cortex data were also interpreted using a two\u2010site model. In this analysis, SR27897 expressed \u223c9 fold, PD134,308 \u223c13 fold and PD140,376 \u223c11 fold selectivity for the G<jats:sub>2<\/jats:sub> site. In contrast, JB93182 expressed \u223c23 fold and YM022 \u223c4 fold selectivity for the G<jats:sub>1<\/jats:sub> site. If the two\u2010site interpretation of the data is valid then, because of its reverse selectivity to L\u2010365,260, JB93182 has been identified as a compound which if radiolabelled could provide a test of this receptor subdivision.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1999) <jats:bold>126<\/jats:bold>, 1496\u20131503; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702448\">10.1038\/sj.bjp.0702448<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702448","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:42:34Z","timestamp":1106941354000},"page":"1496-1503","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Analysis of the behaviour of selected CCK<sub>B<\/sub>\/gastrin receptor antagonists in radioligand binding assays performed in mouse and rat cerebral cortex"],"prefix":"10.1111","volume":"126","author":[{"given":"E A","family":"Harper","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"E P","family":"Griffin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"N P","family":"Shankley","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J W","family":"Black","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":"10.1038\/362348a0"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(94)90737-4"},{"key":"e_1_2_7_4_1","first-page":"241P","article-title":"RPR101367, a new potent and selective non\u2010peptide CCKB receptor antagonist","volume":"116","author":"BERTRAND P.","year":"1995","journal-title":"Br. 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