{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T00:40:49Z","timestamp":1787013649930,"version":"build-2736575974"},"reference-count":66,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2009,1,30]],"date-time":"2009-01-30T00:00:00Z","timestamp":1233273600000},"content-version":"vor","delay-in-days":2009,"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":[[2003,8]]},"abstract":"\n \n \n \n The existence of multiple classes of neuropeptide Y (NPY) receptors (Y\n 1<\/jats:sub>\n , Y\n 2<\/jats:sub>\n , Y\n 4<\/jats:sub>\n , Y\n 5<\/jats:sub>\n and y\n 6<\/jats:sub>\n ) is now well established. However, one of the major difficulties in the study of these various receptor subtypes is the current lack of highly selective probes to investigate a single receptor class. Up to most recently, this was particularly true for the Y\n 4<\/jats:sub>\n and Y\n 5<\/jats:sub>\n subtypes.\n <\/jats:p>\n <\/jats:list-item>\n \n \n [hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY, the first highly selective Y\n 5<\/jats:sub>\n agonist, was iodinated using the chloramine T method and purified by high\u2010pressure liquid chromatography.\n <\/jats:p>\n <\/jats:list-item>\n \n \n Binding performed in rat brain homogenates revealed that equilibrium was reached after 120 min (\n t<\/jats:italic>\n 1\/2<\/jats:sub>\n =21 min) and 60 min (\n t<\/jats:italic>\n 1\/2<\/jats:sub>\n =12 min) at 25 and 100 p\n M<\/jats:sc>\n [\n 125<\/jats:sup>\n I][hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY, respectively.\n <\/jats:p>\n <\/jats:list-item>\n \n \n Isotherm saturation binding experiments demonstrated that [\n 125<\/jats:sup>\n I][hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY binds to an apparent single population with high\u2010affinity (\n K<\/jats:italic>\n D<\/jats:sub>\n of 1.2 and 1.7 n\n M<\/jats:sc>\n ) and low\u2010capacity (\n B<\/jats:italic>\n max<\/jats:sub>\n of 14\u00b13 fmol\/100,000 cells and 20\u00b15 fmol\/mg protein) sites in Y\n 5<\/jats:sub>\n receptor HEK293\u2010transfected cells and rat brain membrane homogenates, respectively. No specific [\n 125<\/jats:sup>\n I][hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY binding sites could be detected in Y\n 1<\/jats:sub>\n , Y\n 2<\/jats:sub>\n or Y\n 4<\/jats:sub>\n receptors transfected HEK293 cells, demonstrating the high selectivity of this ligand for the Y\n 5<\/jats:sub>\n subtype.\n <\/jats:p>\n <\/jats:list-item>\n \n \n Competition binding experiments performed in rat brain membrane homogenates and Y\n 5<\/jats:sub>\n \u2010receptor transfected HEK293 cells demonstrated that specific [\n 125<\/jats:sup>\n I][hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY binding was competed with high affinity by Y\n 5<\/jats:sub>\n agonists and antagonists such as [Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY, [hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY, hPP, CGP71683A and JCF109, but not by Y\n 1<\/jats:sub>\n (BIBP3226), Y\n 2<\/jats:sub>\n (BIIE0246) and Y\n 1<\/jats:sub>\n \/Y\n 4<\/jats:sub>\n (GR231118) preferential ligands.\n <\/jats:p>\n <\/jats:list-item>\n \n \n Taken together, these data demonstrate that [\n 125<\/jats:sup>\n I][hPP\n 1\u201317<\/jats:sub>\n , Ala\n 31<\/jats:sup>\n , Aib\n 32<\/jats:sup>\n ]NPY is the first highly selective Y\n 5<\/jats:sub>\n radioligand to be developed. This new probe should prove most useful for further detailed studies of the molecular and pharmacological properties of this receptor subtype in brain and peripheral tissues.\n <\/jats:p>\n <\/jats:list-item>\n <\/jats:list>\n <\/jats:p>\n \n British Journal of Pharmacology<\/jats:italic>\n (2003)\n 139<\/jats:bold>\n , 1360\u20131368. doi:\n 10.1038\/sj.bjp.0705376<\/jats:ext-link>\n <\/jats:p>","DOI":"10.1038\/sj.bjp.0705376","type":"journal-article","created":{"date-parts":[[2003,7,30]],"date-time":"2003-07-30T11:17:24Z","timestamp":1059563844000},"page":"1360-1368","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Development and characterization of a highly selective neuropeptide Y Y5 receptor agonist radioligand: [\n 125<\/sup>\n I][hPP\n 1\u201317<\/sub>\n , Ala\n 31<\/sup>\n , Aib\n 32<\/sup>\n ]NPY"],"prefix":"10.1111","volume":"139","author":[{"given":"Yvan","family":"Dumont","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mira","family":"Thakur","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Annette","family":"Beck\u2010Sickinger","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alain","family":"Fournier","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R\u00e9mi","family":"Quirion","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,30]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(96)00832-1"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/0003-2697(76)90527-3"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/(SICI)1099-1387(200003)6:3<97::AID-PSC236>3.0.CO;2-E"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M000626200"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1021\/bi0201421"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0196-9781(01)00339-4"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(73)90196-2"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI4188"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.92.20.9067"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(99)00650-0"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/0167-0115(96)00074-2"},{"key":"e_1_2_7_13_1","first-page":"136","article-title":"Pharmacological characterization of the selective nonpeptide neuropeptide Y Y1 receptor antagonist BIBP 3226","volume":"275","author":"DOODS H.N.","year":"1995","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_7_14_1","doi-asserted-by":"publisher","DOI":"10.1139\/y99-119"},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0703162"},{"key":"e_1_2_7_16_1","doi-asserted-by":"crossref","first-page":"5565","DOI":"10.1523\/JNEUROSCI.18-15-05565.1998","article-title":"Expression and characterization of the neuropeptide Y Y5 receptor subtype in the rat brain","volume":"18","author":"DUMONT Y.","year":"1998","journal-title":"J. Neurosci."},{"key":"e_1_2_7_17_1","first-page":"673","article-title":"Characterization of neuropeptide Y binding sites in rat brain membrane preparations using [125I][Leu31, Pro34]peptide YY and [125I]peptide YY3\u201336 as selective Y1 and Y2 radioligands","volume":"272","author":"DUMONT Y.","year":"1995","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_7_18_1","doi-asserted-by":"publisher","DOI":"10.1002\/(SICI)1098-2396(199602)22:2<139::AID-SYN7>3.0.CO;2-E"},{"key":"e_1_2_7_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(90)94189-5"},{"key":"e_1_2_7_20_1","doi-asserted-by":"publisher","DOI":"10.1002\/(SICI)1096-9861(19981221)402:3<372::AID-CNE6>3.0.CO;2-2"},{"key":"e_1_2_7_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/B978-012304990-2\/50005-6"},{"key":"e_1_2_7_22_1","first-page":"375","volume-title":"Handbook of Chemical Neuroanatomy, Vol 16. Peptide Receptor, Part 1","author":"DUMONT Y.","year":"2000"},{"key":"e_1_2_7_23_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0702983"},{"key":"e_1_2_7_24_1","doi-asserted-by":"crossref","first-page":"372","DOI":"10.1093\/oso\/9780198509165.003.0019","volume-title":"Understanding G Protein\u2010coupled Receptors and their Role in the CNS","author":"DUMONT Y.","year":"2002"},{"key":"e_1_2_7_25_1","doi-asserted-by":"publisher","DOI":"10.1097\/00001756-199603220-00013"},{"key":"e_1_2_7_26_1","volume-title":"2002 Abstract Viewer\/Itinerary Planner","author":"DUMONT Y.","year":"2002"},{"key":"e_1_2_7_27_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-5793(92)81490-D"},{"key":"e_1_2_7_28_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0702594"},{"key":"e_1_2_7_29_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm00168a014"},{"key":"e_1_2_7_30_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.87.1.182"},{"key":"e_1_2_7_31_1","doi-asserted-by":"publisher","DOI":"10.3181\/00379727-218-44263"},{"key":"e_1_2_7_32_1","doi-asserted-by":"publisher","DOI":"10.1054\/npep.1999.0057"},{"key":"e_1_2_7_33_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0306-4522(96)00340-5"},{"key":"e_1_2_7_34_1","doi-asserted-by":"publisher","DOI":"10.1016\/0197-0186(92)90067-2"},{"key":"e_1_2_7_35_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(96)00797-2"},{"key":"e_1_2_7_36_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0196-9781(96)00346-4"},{"key":"e_1_2_7_37_1","doi-asserted-by":"publisher","DOI":"10.1038\/382168a0"},{"key":"e_1_2_7_38_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.270.45.26758"},{"key":"e_1_2_7_39_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.271.42.26315"},{"key":"e_1_2_7_40_1","doi-asserted-by":"publisher","DOI":"10.1038\/194495a0"},{"key":"e_1_2_7_41_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0165-6147(99)01303-6"},{"key":"e_1_2_7_42_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(95)00179-O"},{"key":"e_1_2_7_43_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0306-4522(96)00639-2"},{"key":"e_1_2_7_44_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0149-7634(01)00066-5"},{"key":"e_1_2_7_45_1","first-page":"817","article-title":"Neuropeptide Y1 subtype pharmacology of a recombinantly expressed neuropeptide receptor","volume":"41","author":"KRAUSE J.","year":"1992","journal-title":"Mol. Pharmacol."},{"key":"e_1_2_7_46_1","doi-asserted-by":"crossref","first-page":"10935","DOI":"10.1016\/S0021-9258(19)49854-2","article-title":"Cloning and functional expression of a human neuropeptide Y\/peptide YY receptor of the Y1 type","volume":"267","author":"LARHAMMAR D.","year":"1992","journal-title":"J. Biol. Chem."},{"key":"e_1_2_7_47_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1460-9568.1993.tb00231.x"},{"key":"e_1_2_7_48_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.270.49.29123"},{"key":"e_1_2_7_49_1","doi-asserted-by":"publisher","DOI":"10.1016\/0306-4522(90)90367-D"},{"key":"e_1_2_7_50_1","first-page":"73","article-title":"Developing transgenic neuropeptide Y rats","volume":"153","author":"MICHALKIEWICZ M.","year":"2000","journal-title":"Methods Mol. Biol."},{"key":"e_1_2_7_51_1","first-page":"143","article-title":"XVI. International Union of Pharmacology recommendations for the nomenclature of neuropeptide Y, peptide YY, and pancreatic polypeptide receptors","volume":"50","author":"MICHEL M.C.","year":"1998","journal-title":"Pharmacol. Rev."},{"key":"e_1_2_7_52_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(98)00171-X"},{"key":"e_1_2_7_53_1","first-page":"91","article-title":"Neuropeptide Y Y1 receptor\u2010deficient mice. Generation and characterization","volume":"153","author":"PEDRAZZINI T.","year":"2000","journal-title":"Methods Mol. Biol."},{"key":"e_1_2_7_54_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0024-3205(02)02159-8"},{"key":"e_1_2_7_55_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-8993(99)02119-8"},{"key":"e_1_2_7_56_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.132043299"},{"key":"e_1_2_7_57_1","doi-asserted-by":"publisher","DOI":"10.1101\/gad.979102"},{"key":"e_1_2_7_58_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(96)00818-7"},{"key":"e_1_2_7_59_1","first-page":"275","article-title":"Pharmacological characterization of (125)I\u20101229U91 binding to Y1 and Y4 neuropeptide Y\/peptide YY receptors","volume":"293","author":"SCHOBER D.A.","year":"2000","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_7_60_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0196-9781(97)00455-5"},{"key":"e_1_2_7_61_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(97)01031-5"},{"key":"e_1_2_7_62_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.79.18.5485"},{"key":"e_1_2_7_63_1","doi-asserted-by":"publisher","DOI":"10.1038\/296659a0"},{"key":"e_1_2_7_64_1","doi-asserted-by":"publisher","DOI":"10.1016\/0169-328X(95)00176-S"},{"key":"e_1_2_7_65_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(96)00863-1"},{"key":"e_1_2_7_66_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0166-2236(98)01284-3"},{"key":"e_1_2_7_67_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0702084"}],"container-title":["British Journal of Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0705376","content-type":"unspecified","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0705376","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/pdf\/10.1038\/sj.bjp.0705376","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2024,1,10]],"date-time":"2024-01-10T05:23:21Z","timestamp":1704864201000},"score":1,"resource":{"primary":{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/10.1038\/sj.bjp.0705376"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2003,8]]},"references-count":66,"journal-issue":{"issue":"7","published-print":{"date-parts":[[2003,8]]}},"alternative-id":["10.1038\/sj.bjp.0705376"],"URL":"https:\/\/doi.org\/10.1038\/sj.bjp.0705376","archive":["Portico"],"relation":{},"ISSN":["0007-1188","1476-5381"],"issn-type":[{"value":"0007-1188","type":"print"},{"value":"1476-5381","type":"electronic"}],"subject":[],"published":{"date-parts":[[2003,8]]},"assertion":[{"value":"2009-01-30","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}