First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
AuthorFjellaksel, Richard; Oteiza, Ana; Martin, armas maria montserrat; Riss, Patrick; Hjelstuen, Ole Kristian; Kuttner, Samuel; Hansen, Jørn H; Sundset, Rune
Objectives: In vivo evaluations of a gonadotropin releasing hormone-receptor single photon emission computed tomography radiotracer for non-invasive detection of gonadotropin releasing homone-receptors in brain.
Results: We have used a simple, robust and high-yielding procedure to radiolabel an alpha-halogenated bioactive compound with high radiochemical yield. Literature findings showed similar alpha-halogenated compounds suitable for in vivo evaluations. The compound was found to possess nano molar affinity for the gonadotropin releasing hormone-receptor in a competition dependent inhibition study. Furthermore, liquid chromatography-mass spectrometry analysis in saline, human and rat serum resulted in 46%, 52% and 44% stability after incubation for 1 h respectively. In addition, rat brain single photon emission computed tomography and biodistribution studies gave further insight into the nature of the compound as a radiotracer.