{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,24]],"date-time":"2025-10-24T07:48:48Z","timestamp":1761292128191},"reference-count":22,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2003,12,8]],"date-time":"2003-12-08T00:00:00Z","timestamp":1070841600000},"content-version":"vor","delay-in-days":7,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2003,12]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>As part of a programme to develop fluorescence\u2010based methods for the study of the interactions between G\u2010protein coupled receptors (GPCRs) and their ligands the preparation of low molecular weight fluorescence\u2010labelled neuropeptide Y (NPY) Y<jats:sub>5<\/jats:sub> antagonists is reported. The naphthylsulfonyl group in the potent quinazoline\u2010type NPY Y<jats:sub>5<\/jats:sub> receptor antagonist CGP 71683A was replaced with a dansyl, nitrobenzoxadiazole (NBD) or acridine\u20109\u2010carbonyl group. In radioligand binding studies on human Y<jats:sub>5<\/jats:sub> receptor expressing HEC\u20101B cells the substances labelled with acridine (K<jats:sub>i<\/jats:sub> 311 nM) and NBD (K<jats:sub>i<\/jats:sub> &gt; 1000 nM) proved to be moderately active or inactive, respectively. By contrast, a K<jats:sub>i<\/jats:sub> value of 49 nM was found for the dansyl analogue compared to 2 nM for CGP 71683A. No binding to Y<jats:sub>1<\/jats:sub> receptors (SK\u2010N\u2010MC cells, displacement of [<jats:sup>3<\/jats:sup>H]propionyl\u2010NPY) was detected for the new compounds at concentrations \u2264 1 \u03bcM.<\/jats:p>","DOI":"10.1002\/ardp.200300813","type":"journal-article","created":{"date-parts":[[2003,12,11]],"date-time":"2003-12-11T09:01:18Z","timestamp":1071133278000},"page":"585-590","source":"Crossref","is-referenced-by-count":7,"title":["Preparation of Fluorescent Nonpeptidic Neuropeptide Y Receptor Ligands: Analogues of the Quinazoline\u2010type Anti\u2010obesity Y<sub>5<\/sub> Antagonist CGP 71683A"],"prefix":"10.1002","volume":"336","author":[{"given":"Liantao","family":"Li","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Matthias","family":"Mayer","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Erich","family":"Schneider","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Elvira","family":"Schreiber","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G\u00fcnther","family":"Bernhardt","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shiqi","family":"Peng","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Armin","family":"Buschauer","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2003,12,8]]},"reference":[{"key":"e_1_2_1_2_2","first-page":"51","author":"Mayer M.","year":"2000","journal-title":"Arch. 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