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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.

Author information

1
Norwegian Medical Cyclotron Centre, PO Box 4950, Nydalen, N-0424 Oslo, Norway.
2
Department of Pharmacology, Faculty of Medicine, University of Oslo, Norway.
3
School of Pharmacy, University of Oslo, Norway.
4
Department of Neuropsychiatry and Psychosomatic Medicine, Oslo University Hospital, Oslo, Norway.
5
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: jlsutcliffe@ucdavis.edu.

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. 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.

KEYWORDS:

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

PMID:
24613701
DOI:
10.1016/j.bmcl.2014.02.002
[Indexed for MEDLINE]

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