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

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 alph...

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Detalles Bibliográficos
Autores principales: Fjellaksel, Richard, Oteiza, Ana, Martin-Armas, Montserrat, Riss, Patrick J., Hjelstuen, Ole Kristian, Kuttner, Samuel, Hansen, Jørn H., Sundset, Rune
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6238273/
https://www.ncbi.nlm.nih.gov/pubmed/30442192
http://dx.doi.org/10.1186/s13104-018-3924-2
Descripción
Sumario: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. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1186/s13104-018-3924-2) contains supplementary material, which is available to authorized users.