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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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| Affiliation: | 1. Department of Pharmaceutical Technology, University of Regensburg, Regensburg 93053, Germany;2. Macromolecular Chemistry II, University of Bayreuth, Bayreuth 95440, Germany;3. Center for Electron Microscopy at the Institute for Anatomy, University of Regensburg, Regensburg 93053, Germany;4. IPhaTec, Frankfurt am Main 60388, Germany;5. Pharmaceutical Development, Aeterna Zentaris GmbH, Frankfurt am Main 60314, Germany |
| 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. |
| Keywords: | Gonadotropin-releasing hormone (GnRH) receptor antagonists Luteinizing hormone releasing hormone (LHRH) Positron emission tomography (PET) Fluorine-18 Small molecule |
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