Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592385 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
Two novel small molecule gonadotropin-releasing hormone (GnRH) receptor antagonists (12 and 13) of the furamide-class were synthesized and evaluated in vitro for their receptor binding affinities for the rat GnRH receptor. Radiolabeling with no carrier added fluorine-18 of the appropriate precursors was investigated in a one-step reaction. Log P (Octanol/PBS pH 7.4) and serum stability of the compounds were investigated. The antagonists showed low nM affinity for the rat GnRH receptor. 18F-radiolabled compounds were obtained in high radiochemical purity (>95%) and specific activity (>75 GBq/μmol). These findings suggest this class of compounds holds promise as potential probes for PET targeting of GnRH-receptor expression.
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Organic Chemistry
Authors
Dag Erlend Olberg, Kjetil Wessel Andressen, Finn Olav Levy, Jo Klaveness, Ira Haraldsen, Julie L. Sutcliffe,