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First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor.

Richard FjellakselAna OteizaMontserrat Martin-ArmasPatrick J RissOle Kristian HjelstuenSamuel KuttnerJørn H HansenRune Sundset
Published in: BMC research notes (2018)
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.
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