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Human disorders characterized by aberrant social interactions, such as autism and schizophrenia, may also involve abnormal oxytocin levels. GSK712043, GSK711320, and GSK664004, three antagonists exhibiting subnanomolar affinity for the human oxytocin receptor (hOTR) and high selectivity over vasopressin receptors were successfully labelled with carbon\u201011 with suitable yields (0.5\u20101GBq @EOS), high molar activity (275\u2010700\u00a0GBq\/\u03bcmol), and radiochemical purities. The in vivo regional uptake of these radiotracers was determined in porcine brain. [<jats:sup>11<\/jats:sup>C]GSK711320 baseline scan showed no significant brain uptake, and limited initial uptake was observed following administration of [<jats:sup>11<\/jats:sup>C]GSK712043 or [<jats:sup>11<\/jats:sup>C]GSK664004. The [<jats:sup>11<\/jats:sup>C]GSK712043 and [<jats:sup>11<\/jats:sup>C]GSK664004 kinetics were slow and peaked at around 2%ID\/L at 90\u00a0minutes post\u2010injection. For both tracers, the distribution of activity was homogeneous throughout the brain. All the tracers showed high uptake in the pituitary gland, especially [<jats:sup>11<\/jats:sup>C]GSK711320; however, its uptake could not be blocked by pretreatment with the known OTR antagonist, L368,899. In vivo evaluation of these candidates demonstrated that they are not suitable as central OTR PET imaging agents.<\/jats:p>","DOI":"10.1002\/jlcr.3535","type":"journal-article","created":{"date-parts":[[2017,7,3]],"date-time":"2017-07-03T03:42:47Z","timestamp":1499053367000},"page":"556-565","source":"Crossref","is-referenced-by-count":4,"title":["Radiosynthesis and evaluation of 1\u2010substituted 3\u2010(2,3\u2010dihydro\u20101H\u2010inden\u20102\u2010yl)\u20106\u2010(1\u2010ethylpropyl)\u2010(3<i>R<\/i>,6<i>R<\/i>)\u20102,5\u2010piperazinedione derivatives as PET tracers for imaging the central oxytocinergic system"],"prefix":"10.1002","volume":"60","author":[{"given":"Carmine","family":"Marzano","sequence":"first","affiliation":[{"name":"Imanova Limited, Burlington Danes Building Hammersmith Hospital  London UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Steen","family":"Jakobsen","sequence":"additional","affiliation":[{"name":"Aarhus University Hospital  Aarhus Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cristian","family":"Salinas","sequence":"additional","affiliation":[{"name":"Imanova Limited, Burlington Danes Building Hammersmith Hospital  London UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sac Pham","family":"Tang","sequence":"additional","affiliation":[{"name":"Imanova Limited, Burlington Danes Building Hammersmith Hospital  London UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dirk","family":"Bender","sequence":"additional","affiliation":[{"name":"Aarhus University Hospital  Aarhus Denmark"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jan","family":"Passchier","sequence":"additional","affiliation":[{"name":"Imanova Limited, Burlington Danes Building Hammersmith Hospital  London UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0688-1358","authenticated-orcid":false,"given":"Christophe","family":"Plisson","sequence":"additional","affiliation":[{"name":"Imanova Limited, Burlington Danes Building Hammersmith Hospital  London UK"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,9,21]]},"reference":[{"key":"e_1_2_6_2_1","first-page":"127","article-title":"Oxytocin: the great facilitator of life","volume":"88","author":"Lee H\u2010J","year":"2009","journal-title":"Prog Neurobiol"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0149-7634(05)80002-8"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.peptides.2004.05.019"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.1158668"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.pbb.2004.04.006"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00213-005-0293-z"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0306-4530(98)00064-X"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.psychres.2016.12.007"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.2174\/092986708783885291"},{"key":"e_1_2_6_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/0306-4530(94)90021-3"},{"key":"e_1_2_6_12_1","doi-asserted-by":"publisher","DOI":"10.1097\/PSY.0b013e318188ade4"},{"key":"e_1_2_6_13_1","doi-asserted-by":"publisher","DOI":"10.1038\/npp.2011.184"},{"key":"e_1_2_6_14_1","doi-asserted-by":"publisher","DOI":"10.1212\/WNL.37.6.1001"},{"key":"e_1_2_6_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/0196-9781(95)00039-M"},{"key":"e_1_2_6_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(92)91156-9"},{"key":"e_1_2_6_17_1","first-page":"105","article-title":"Preparation and biodistribution of [67Ga]\u2010labeled oxytocin for SPECT purposes","volume":"7","author":"Jalilian AR","year":"2009","journal-title":"Iran J Radiat Res"},{"key":"e_1_2_6_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2012.02.019"},{"key":"e_1_2_6_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2012.10.116"},{"key":"e_1_2_6_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2013.07.045"},{"key":"e_1_2_6_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2016.04.097"},{"key":"e_1_2_6_22_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.5b01080"},{"key":"e_1_2_6_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2016.10.035"},{"key":"e_1_2_6_24_1","unstructured":"LeachC LiddleJ PeaceS PhilipJ SmithIED TerrellLR.1 6\u2010Substituted (3R 6R) \u20103\u2010 (2 3\u2010dihydro\u20101H\u2010inden\u20102\u2010yl)\u20102 5\u2010piperazinedione derivatives as oxytocin receptor antagonists for the treatment of pre\u2010term labour dysmenorrhea and endometriosis.2006; 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