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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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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
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author Fjellaksel, Richard
Oteiza, Ana
Martin-Armas, Montserrat
Riss, Patrick J.
Hjelstuen, Ole Kristian
Kuttner, Samuel
Hansen, Jørn H.
Sundset, Rune
author_facet Fjellaksel, Richard
Oteiza, Ana
Martin-Armas, Montserrat
Riss, Patrick J.
Hjelstuen, Ole Kristian
Kuttner, Samuel
Hansen, Jørn H.
Sundset, Rune
author_sort Fjellaksel, Richard
collection PubMed
description 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.
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spelling pubmed-62382732018-11-23 First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor Fjellaksel, Richard Oteiza, Ana Martin-Armas, Montserrat Riss, Patrick J. Hjelstuen, Ole Kristian Kuttner, Samuel Hansen, Jørn H. Sundset, Rune BMC Res Notes Research Note 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. BioMed Central 2018-11-15 /pmc/articles/PMC6238273/ /pubmed/30442192 http://dx.doi.org/10.1186/s13104-018-3924-2 Text en © The Author(s) 2018 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research Note
Fjellaksel, Richard
Oteiza, Ana
Martin-Armas, Montserrat
Riss, Patrick J.
Hjelstuen, Ole Kristian
Kuttner, Samuel
Hansen, Jørn H.
Sundset, Rune
First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title_full First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title_fullStr First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title_full_unstemmed First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title_short First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
title_sort first in vivo evaluation of a potential spect brain radiotracer for the gonadotropin releasing hormone receptor
topic Research Note
url 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
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