444151-94-4Relevant articles and documents
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
Olberg, Dag Erlend,Andressen, Kjetil Wessel,Levy, Finn Olav,Klaveness, Jo,Haraldsen, Ira,Sutcliffe, Julie L.
, p. 1846 - 1850 (2014)
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.
RADIOLABELED GNRH ANTAGONISTS AS PET IMAGING AGENTS
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, (2014/12/12)
Provided herein is technology relating to imaging agents for positron emission tomography (PET) and particularly, but not exclusively, to a gonadotropin-releasing hormone (GnRH) antagonist radiolabeled with positron emitting nuclides and to methods of visualizing GnRH receptors in the central nervous system by PET from administration of such compounds to warm-blooded animals for diagnostic purposes.