Literature DB >> 24613701

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.

Dag Erlend Olberg1, Kjetil Wessel Andressen2, Finn Olav Levy2, Jo Klaveness3, Ira Haraldsen4, Julie L Sutcliffe5.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2014        PMID： 24613701     DOI： 10.1016/j.bmcl.2014.02.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Highlights of articles published in annals of nuclear medicine 2016.

Authors:  Hossein Jadvar
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-07-28       Impact factor: 9.236

2.  In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues.

Authors:  József Murányi; Attila Varga; Bianka Gurbi; Pál Gyulavári; Gábor Mező; Tibor Vántus
Journal:  J Vis Exp       Date:  2017-03-21       Impact factor: 1.355

3.  Efficient capture of circulating tumor cells with low molecular weight folate receptor-specific ligands.

Authors:  Yingwen Hu; Danyang Chen; John V Napoleon; Madduri Srinivasarao; Sunil Singhal; Cagri A Savran; Philip S Low
Journal:  Sci Rep       Date:  2022-05-20       Impact factor: 4.996

Review 4.  Recent Development of Non-Peptide GnRH Antagonists.

Authors:  Feng-Ling Tukun; Dag Erlend Olberg; Patrick J Riss; Ira Haraldsen; Anita Kaass; Jo Klaveness
Journal:  Molecules       Date:  2017-12-09       Impact factor: 4.411

5.  Discovery of a Lead Brain-Penetrating Gonadotropin-Releasing Hormone Receptor Antagonist with Saturable Binding in Brain.

Authors:  Roberto B W Bekker; Richard Fjellaksel; Trine Hjornevik; Syed Nuruddin; Waqas Rafique; Jørn H Hansen; Rune Sundset; Ira H Haraldsen; Patrick J Riss
Journal:  ChemMedChem       Date:  2020-08-10       Impact factor: 3.466
  5 in total

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