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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BioMed Central
2018
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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. |
format | Online Article Text |
id | pubmed-6238273 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
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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