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Bioorg Med Chem Lett. 2014 Apr 1;24(7):1846-50. doi: 10.1016/j.bmcl.2014.02.002. Epub 2014 Feb 10.

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

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Norwegian Medical Cyclotron Centre, PO Box 4950, Nydalen, N-0424 Oslo, Norway.
Department of Pharmacology, Faculty of Medicine, University of Oslo, Norway.
School of Pharmacy, University of Oslo, Norway.
Department of Neuropsychiatry and Psychosomatic Medicine, Oslo University Hospital, Oslo, Norway.
Department of Biomedical Engineering, University of California Davis, Davis, CA, USA; Department of Internal Medicine, Division of Hematology & Oncology, University of California Davis, 2921 Stockton Boulevard Sacramento, CA 95817, USA; Center for Molecular and Genomic Imaging, University of California Davis, Davis, CA, USA. Electronic address:


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. LogP (Octanol/PBS pH 7.4) and serum stability of the compounds were investigated. The antagonists showed low nM affinity for the rat GnRH receptor. (18)F-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.


Fluorine-18; Gonadotropin-releasing hormone (GnRH) receptor antagonists; Luteinizing hormone releasing hormone (LHRH); Positron emission tomography (PET); Small molecule

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