{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,4]],"date-time":"2026-05-04T01:28:22Z","timestamp":1777858102884,"version":"3.51.4"},"reference-count":66,"publisher":"SAGE Publications","issue":"2","license":[{"start":{"date-parts":[[2012,10,31]],"date-time":"2012-10-31T00:00:00Z","timestamp":1351641600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":["journals.sagepub.com"],"crossmark-restriction":true},"short-container-title":["J Psychopharmacol"],"published-print":{"date-parts":[[2013,2]]},"abstract":"<jats:p>\n                    Accumulating evidence supports a role for \u03ba\u2212opioid receptor antagonists in the treatment of mood disorders. Standard \u03ba-antagonists have an unusual pharmacodynamic action, with a single injection blocking receptor signaling for several weeks. Here, we have characterized the \u03ba-selective properties of two ligands, 5\u2019-(2-aminomethyl) naltrindole (5\u2019-AMN) and N-((Naltrindol-5-yl) methyl) pentanimidamide (5\u2019-MABN), to identify whether modifications of the naltrindole side chain produces short-acting \u03ba-antagonists. Opioid receptor binding affinity and activity were assessed using [\n                    <jats:sup>3<\/jats:sup>\n                    H]-diprenorphine binding, guanosine-5\u2019-O-(3-[35S]-thio) triphosphate ([\n                    <jats:sup>35<\/jats:sup>\n                    S]-GTP\u03b3S) binding and isolated guinea-pig ileum. Pharmacodynamic profiles of 5\u2019-AMN and 5\u2019-MABN (1\u201310 mg\/kg) were investigated using the tail-withdrawal assay and diuresis. Efficacy was also determined in depression- and anxiety-related behavioral paradigms in CD-1 mice. Both 5\u2019-AMN and 5\u2019-MABN had high affinity for \u03ba\u2212receptors ( K\n                    <jats:sub>i<\/jats:sub>\n                    1.36\u00b10.98 and 0.27\u00b10.08, respectively) and were revealed as potent \u03ba-antagonists ( pA\n                    <jats:sub>2<\/jats:sub>\n                    7.43 and 8.18, respectively) and \u03bc-receptor antagonists ( pA\n                    <jats:sub>2<\/jats:sub>\n                    7.62 and 7.85, respectively) in the ileum. Contrary to our hypothesis, in vivo, 5\u2019-AMN and 5\u2019-MABN displayed long-lasting antagonist effects in mice, reducing the antinociceptive actions of U50,488 (10 mg\/kg) at 28 and 21 days post-injection, respectively. Interestingly, while 5\u2019-AMN and 5\u2019-MABN were not \u03ba-selective, both compounds did show significant antidepressant- and anxiolytic-like effects at 7\u201314 days post-injection in mice.\n                  <\/jats:p>","DOI":"10.1177\/0269881112464828","type":"journal-article","created":{"date-parts":[[2012,11,1]],"date-time":"2012-11-01T20:41:52Z","timestamp":1351802512000},"page":"192-202","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":16,"title":["In vivo and in vitro characterization of naltrindole-derived ligands at the \u03ba-opioid receptor"],"prefix":"10.1177","volume":"27","author":[{"given":"Joseph J","family":"Casal-Dominguez","sequence":"first","affiliation":[{"name":"Department of Pharmacy and Pharmacology, University of Bath, Bath, UK"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mary","family":"Clark","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, University of Michigan, Ann Arbor, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"John R","family":"Traynor","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, University of Michigan, Ann Arbor, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Stephen M","family":"Husbands","sequence":"additional","affiliation":[{"name":"Department of Pharmacy and Pharmacology, University of Bath, Bath, UK"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sarah J","family":"Bailey","sequence":"additional","affiliation":[{"name":"Department of Pharmacy and Pharmacology, University of Bath, Bath, UK"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"179","published-online":{"date-parts":[[2012,10,31]]},"reference":[{"key":"bibr1-0269881112464828","doi-asserted-by":"publisher","DOI":"10.1046\/j.1471-4159.1998.70020635.x"},{"key":"bibr2-0269881112464828","doi-asserted-by":"publisher","DOI":"10.2174\/138161209788168100"},{"key":"bibr3-0269881112464828","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(87)90397-9"},{"key":"bibr4-0269881112464828","doi-asserted-by":"crossref","first-page":"415","DOI":"10.1016\/S0031-6997(25)06961-3","volume":"4","author":"Blaschko H","year":"1952","journal-title":"Pharmacol 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