Synthesis and in vitro evaluation of small-molecule [18 F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for …

…, FO Levy, J Klaveness, I Haraldsen, JL Sutcliffe

Index: Olberg, Dag Erlend; Andressen, Kjetil Wessel; Levy, Finn Olav; Klaveness, Jo; Haraldsen, Ira; Sutcliffe, Julie L. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 7 p. 1846 - 1850

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Abstract

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 ...