{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,23]],"date-time":"2026-08-23T18:46:08Z","timestamp":1787510768570,"version":"build-2736575974"},"reference-count":33,"publisher":"SAGE Publications","issue":"2","license":[{"start":{"date-parts":[[2024,8,21]],"date-time":"2024-08-21T00:00:00Z","timestamp":1724198400000},"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 Cereb Blood Flow Metab"],"published-print":{"date-parts":[[2025,2]]},"abstract":"<jats:p>\n                    Two complimentary techniques were used to estimate occupancy of pimavanserin (a selective 5-HT\n                    <jats:sub>2A\/2C<\/jats:sub>\n                    inverse agonist) to 5-HT\n                    <jats:sub>2A<\/jats:sub>\n                    and 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    receptors in non-human primate brains. One employed the 5-HT\n                    <jats:sub>2A\/2C<\/jats:sub>\n                    selective radioligand [\n                    <jats:sup>11<\/jats:sup>\n                    C]CIMBI-36 combined with quantification of binding potentials in brain regions known to be enriched in 5-HT\n                    <jats:sub>2A<\/jats:sub>\n                    (cortex) or 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    (choroid plexus) receptors to estimate occupancy. Pimavanserin was 6\u201310 fold more potent displacing [\n                    <jats:sup>11<\/jats:sup>\n                    C]CIMBI-36 from cortex (ED\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20090.007\u2009mg\/kg; EC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20090.6\u2009ng\/ml) than from choroid plexus (ED\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=0.046\u2009mg\/kg; EC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20096.0\u2009ng\/ml). The assignment of [\n                    <jats:sup>11<\/jats:sup>\n                    C]CIMBI-36 binding to 5-HT\n                    <jats:sub>2A<\/jats:sub>\n                    and 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    receptors by anatomical brain structure was confirmed using the 5-HT\n                    <jats:sub>2A<\/jats:sub>\n                    selective inverse agonist MDL 100,907 and the 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    selective antagonist SB 242584 to displace [\n                    <jats:sup>11<\/jats:sup>\n                    C]CIMBI-36. The second technique employed a novel, 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    selective tracer called [\n                    <jats:sup>11<\/jats:sup>\n                    C]AC1332. [\n                    <jats:sup>11<\/jats:sup>\n                    C]AC1332 bound robustly to choroid plexus, moderately to hippocampus, and minimally to cortex. Pimavanserin displaced [\n                    <jats:sup>11<\/jats:sup>\n                    C]AC1332 with similar potency (ED\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20090.062\u2009mg\/kg; EC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20092.5\u2009ng\/ml) as its potency displacing [\n                    <jats:sup>11<\/jats:sup>\n                    C]CIMBI-36 binding from choroid plexus. These results demonstrate the feasibility of simultaneously estimating drug occupancy of 5-HT\n                    <jats:sub>2A<\/jats:sub>\n                    and 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    receptors in vivo, and the utility of a novel 5-HT\n                    <jats:sub>2C<\/jats:sub>\n                    receptor selective tracer ligand.\n                  <\/jats:p>","DOI":"10.1177\/0271678x241276312","type":"journal-article","created":{"date-parts":[[2024,8,22]],"date-time":"2024-08-22T02:54:35Z","timestamp":1724295275000},"page":"352-364","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":3,"title":["Imaging the 5-HT\n                    <sub>2C<\/sub>\n                    receptor with PET: Evaluation of 5-HT\n                    <sub>2C<\/sub>\n                    and 5-HT\n                    <sub>2A<\/sub>\n                    affinity of pimavanserin in the primate brain"],"prefix":"10.1177","volume":"45","author":[{"ORCID":"https:\/\/orcid.org\/0009-0005-1809-058X","authenticated-orcid":false,"given":"Khanum","family":"Ridler","sequence":"first","affiliation":[{"name":"Invicro, London, UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gaia","family":"Rizzo","sequence":"additional","affiliation":[{"name":"Invicro, London, UK"},{"name":"Division of Brain Sciences, Imperial College London, London, UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ethan S","family":"Burstein","sequence":"additional","affiliation":[{"name":"ACADIA Pharmaceuticals Inc., San Diego, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anton","family":"Forsberg Mor\u00e9n","sequence":"additional","affiliation":[{"name":"Center for Psychiatry Research, Karolinska Institutet"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vladimir","family":"Stepanov","sequence":"additional","affiliation":[{"name":"Center for Psychiatry Research, Karolinska Institutet"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Christer","family":"Halldin","sequence":"additional","affiliation":[{"name":"Center for Psychiatry Research, Karolinska Institutet"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3612-6687","authenticated-orcid":false,"given":"Eugenii A","family":"Rabiner","sequence":"additional","affiliation":[{"name":"Invicro, London, UK"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"179","published-online":{"date-parts":[[2024,8,21]]},"reference":[{"key":"e_1_3_5_2_2","doi-asserted-by":"publisher","DOI":"10.2174\/1568026619666190709101449"},{"key":"e_1_3_5_3_2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1460-9568.2007.05567.x"},{"key":"e_1_3_5_4_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-3223(98)00132-2"},{"key":"e_1_3_5_5_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.biopsych.2009.09.011"},{"key":"e_1_3_5_6_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.tips.2013.08.001"},{"key":"e_1_3_5_7_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.pharmthera.2015.11.009"},{"key":"e_1_3_5_8_2","doi-asserted-by":"publisher","DOI":"10.4103\/0976-500X.130158"},{"key":"e_1_3_5_9_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2006.10.029"},{"key":"e_1_3_5_10_2","doi-asserted-by":"publisher","DOI":"10.1038\/sj.jcbfm.9600493"},{"key":"e_1_3_5_11_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.neuroimage.2013.08.035"},{"key":"e_1_3_5_12_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm970424c"},{"issue":"44","key":"e_1_3_5_13_2","first-page":"385","article-title":"Evaluation of [C-11]7-Chloro-2-[4-Methoxy-3-(2-(4-Methylpiperidin-1-Yl)ethoxy)phenyl]isoindolin-1-One as a PET imaging agent for 5-HT2C receptors in the nonhuman primate brain","author":"Goodman M","year":"2019","unstructured":"Goodman M, Zeng F, Nye J, et\u00a0al. Evaluation of [C-11]7-Chloro-2-[4-Methoxy-3-(2-(4-Methylpiperidin-1-Yl)ethoxy)phenyl]isoindolin-1-One as a PET imaging agent for 5-HT2C receptors in the nonhuman primate brain ACNP 58th annual meeting: poster session III, poster W66. 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