{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,15]],"date-time":"2026-09-15T17:02:28Z","timestamp":1789491748232,"version":"build-2803163510"},"reference-count":52,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2026,8,17]],"date-time":"2026-08-17T00:00:00Z","timestamp":1786924800000},"content-version":"vor","delay-in-days":16,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"},{"start":{"date-parts":[[2026,8,1]],"date-time":"2026-08-01T00:00:00Z","timestamp":1785542400000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/doi.wiley.com\/10.1002\/tdm_license_1.1"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2026,8]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>\n                    Among the human neuropeptide Y (NPY) receptors, the Y\n                    <jats:sub>5<\/jats:sub>\n                    receptor (Y\n                    <jats:sub>5<\/jats:sub>\n                    R) represents a potential therapeutic target for the treatment of obesity and stress\u2010related diseases. As the Y\n                    <jats:sub>5<\/jats:sub>\n                    R is expressed in various malignant tumors, it is also considered a potential target for cancer diagnosis and therapy. Although numerous non\u2010peptidic Y\n                    <jats:sub>5<\/jats:sub>\n                    R antagonists with high binding affinity have been reported, only labeled peptidic agonists are used in routine Y\n                    <jats:sub>5<\/jats:sub>\n                    R competition binding assays, which are needed for the development and characterization of Y\n                    <jats:sub>5<\/jats:sub>\n                    R ligands. In the present study, three radiolabeled derivatives of the high\u2010affinity Y\n                    <jats:sub>5<\/jats:sub>\n                    R antagonist CGP71683A (\n                    <jats:bold>1<\/jats:bold>\n                    ) were synthesized ([\n                    <jats:sup>3<\/jats:sup>\n                    H]\n                    <jats:bold>26<\/jats:bold>\n                    , [\n                    <jats:sup>3<\/jats:sup>\n                    H]\n                    <jats:bold>32<\/jats:bold>\n                    , [\n                    <jats:sup>3<\/jats:sup>\n                    H]\n                    <jats:bold>42<\/jats:bold>\n                    ) and studied in saturation binding assays using adherent or suspended HEC\u20101B\u2010hY\n                    <jats:sub>5<\/jats:sub>\n                    R cells or membrane preparations thereof. Their\n                    <jats:italic>K<\/jats:italic>\n                    <jats:sub>d<\/jats:sub>\n                    values (1.5\u201313\u2009nM) were consistent with the\n                    <jats:italic>K<\/jats:italic>\n                    <jats:sub>i<\/jats:sub>\n                    values (1.3\u201311\u2009nM) of the non\u2010labeled analogs. However, all synthesized radioligands exhibited very high non\u2010specific binding, primarily caused by binding of the radioligands to cellular membranes, which limits their use as tool compounds in radiochemical Y\n                    <jats:sub>5<\/jats:sub>\n                    R binding assays. Nevertheless, a competition binding assay with [\n                    <jats:sup>3<\/jats:sup>\n                    H]\n                    <jats:bold>32<\/jats:bold>\n                    and the endogenous Y\n                    <jats:sub>5<\/jats:sub>\n                    R agonist hNPY afforded a\n                    <jats:italic>K<\/jats:italic>\n                    <jats:sub>i<\/jats:sub>\n                    that was in agreement with literature data.\n                  <\/jats:p>","DOI":"10.1002\/ardp.70314","type":"journal-article","created":{"date-parts":[[2026,8,17]],"date-time":"2026-08-17T12:42:21Z","timestamp":1786970541000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis and Characterization of Tritium\u2010Labeled Neuropeptide Y Y\n                    <sub>5<\/sub>\n                    Receptor Ligands Derived From CGP71683A"],"prefix":"10.1002","volume":"359","author":[{"given":"Franziska","family":"Schettler","sequence":"first","affiliation":[{"name":"Institute of Pharmacy, Faculty of Chemistry and Pharmacy University of Regensburg Regensburg Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4620-4650","authenticated-orcid":false,"given":"Pierre","family":"Koch","sequence":"additional","affiliation":[{"name":"Institute of Pharmacy, Faculty of Chemistry and Pharmacy University of Regensburg Regensburg Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8095-8627","authenticated-orcid":false,"given":"Max","family":"Keller","sequence":"additional","affiliation":[{"name":"Institute of Pharmacy, Faculty of Chemistry and Pharmacy University of Regensburg Regensburg Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2026,8,17]]},"reference":[{"key":"e_1_2_10_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0021\u20109258(17)42339\u20108"},{"key":"e_1_2_10_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0031\u20106997(24)01352\u20108"},{"key":"e_1_2_10_4_1","doi-asserted-by":"publisher","DOI":"10.1523\/JNEUROSCI.18\u201015\u201005565.1998"},{"key":"e_1_2_10_5_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1460\u20109568.1999.00553.x"},{"key":"e_1_2_10_6_1","doi-asserted-by":"publisher","DOI":"10.1006\/bbrc.1998.8647"},{"key":"e_1_2_10_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0701028"},{"key":"e_1_2_10_8_1","doi-asserted-by":"publisher","DOI":"10.1177\/1535370218774889"},{"key":"e_1_2_10_9_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M000626200"},{"key":"e_1_2_10_10_1","doi-asserted-by":"publisher","DOI":"10.1038\/382168a0"},{"key":"e_1_2_10_11_1","doi-asserted-by":"publisher","DOI":"10.1152\/ajpregu.1999.277.5.R1428"},{"key":"e_1_2_10_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.pnpbp.2021.110349"},{"key":"e_1_2_10_13_1","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.108.144634"},{"key":"e_1_2_10_14_1","doi-asserted-by":"publisher","DOI":"10.1038\/onc.2014.253"},{"key":"e_1_2_10_15_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI131919"},{"key":"e_1_2_10_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.peptides.2013.07.029"},{"key":"e_1_2_10_17_1","doi-asserted-by":"publisher","DOI":"10.1186\/s12885\u2010023\u201010993\u20101"},{"key":"e_1_2_10_18_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0705376"},{"key":"e_1_2_10_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.npep.2004.04.007"},{"key":"e_1_2_10_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejphar.2008.10.021"},{"key":"e_1_2_10_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/bs.mcb.2015.11.004"},{"key":"e_1_2_10_22_1","doi-asserted-by":"publisher","DOI":"10.1002\/jlcr.3617"},{"key":"e_1_2_10_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/s0960\u2010894x(00)00177\u20103"},{"key":"e_1_2_10_24_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI4188"},{"key":"e_1_2_10_25_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.bioconjchem.7b00103"},{"key":"e_1_2_10_26_1","doi-asserted-by":"publisher","DOI":"10.1016\/s0960\u2010894x(02)00287\u20101"},{"key":"e_1_2_10_27_1","doi-asserted-by":"publisher","DOI":"10.1358\/DOF.2002.027.03.658519"},{"key":"e_1_2_10_28_1","unstructured":"H.R\u00fceger T.Schmidlin P.Rigollier et al. 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