Data publication: Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand

Moldovan, Rares-Petru; Gündel, Daniel; Teodoro, Rodrigo; Ludwig, Friedrich-Alexander; Fischer, Steffen; Toussaint, Magali; Schepmann, Dirk; Wünsch, Bernhard; Brust, Peter; Deuther-Conrad, Winnie

doi:10.14278/rodare.1257

November 9, 2021 Dataset Open Access

Data publication: Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand

Moldovan, Rares-Petru; Gündel, Daniel; Teodoro, Rodrigo; Ludwig, Friedrich-Alexander; Fischer, Steffen; Toussaint, Magali; Schepmann, Dirk; Wünsch, Bernhard; Brust, Peter; Deuther-Conrad, Winnie

MARC21 XML Export

<?xml version='1.0' encoding='UTF-8'?>
<record xmlns="http://www.loc.gov/MARC21/slim">
  <leader>00000nmm##2200000uu#4500</leader>
  <datafield tag="650" ind1="1" ind2="7">
    <subfield code="a">cc-by</subfield>
    <subfield code="2">opendefinition.org</subfield>
  </datafield>
  <datafield tag="542" ind1=" " ind2=" ">
    <subfield code="l">open</subfield>
  </datafield>
  <datafield tag="540" ind1=" " ind2=" ">
    <subfield code="u">https://creativecommons.org/licenses/by/4.0/legalcode</subfield>
    <subfield code="a">Creative Commons Attribution 4.0 International</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">σ2 receptor</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">transmembrane protein 97</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">azaindoles</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">binding affinity</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">radiochemistry</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">fluorine-18 labeling</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">positron emission tomography (PET)</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">brain-penetration</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">glioblastoma</subfield>
  </datafield>
  <datafield tag="653" ind1=" " ind2=" ">
    <subfield code="a">orthotopic</subfield>
  </datafield>
  <controlfield tag="005">20211112130456.0</controlfield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Gündel, Daniel</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Teodoro, Rodrigo</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Ludwig, Friedrich-Alexander</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Fischer, Steffen</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Toussaint, Magali</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Schepmann, Dirk</subfield>
    <subfield code="u">Institut für Pharmazeutische und Medizinische Chemie der Westfälischen Wilhelms-Universität Münster</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Wünsch, Bernhard</subfield>
    <subfield code="u">Institut für Pharmazeutische und Medizinische Chemie der Westfälischen Wilhelms-Universität Münster</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Brust, Peter</subfield>
  </datafield>
  <datafield tag="700" ind1=" " ind2=" ">
    <subfield code="a">Deuther-Conrad, Winnie</subfield>
    <subfield code="0">(orcid)0000-0003-3168-3062</subfield>
  </datafield>
  <datafield tag="260" ind1=" " ind2=" ">
    <subfield code="c">2021-11-09</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">150499</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 262.10.fid.zip</subfield>
    <subfield code="z">md5:595078649b7897ecc562914445382773</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">436747</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 262.11.fid.zip</subfield>
    <subfield code="z">md5:afc583d221762f0615250e557489de77</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">217852</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 262.12.fid.zip</subfield>
    <subfield code="z">md5:87482cb474faa3b34fac51e1372619f2</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">157206</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 263.10.fid.zip</subfield>
    <subfield code="z">md5:908bb03eddeaaef36d74c6a61eccbc75</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">436464</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 263.11.fid.zip</subfield>
    <subfield code="z">md5:c8f783c005bae36a19ce7f4c09b36f76</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">214524</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 263.12.fid.zip</subfield>
    <subfield code="z">md5:e2ef2f4243888c5175b234d41369b234</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">151693</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 264.10.fid.zip</subfield>
    <subfield code="z">md5:5c5a95b7c1f60f629c533f53ba88d51f</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">436545</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 264.11.fid.zip</subfield>
    <subfield code="z">md5:dc6de2862aa252910bd45534feacaa3c</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">214488</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 264.12.fid.zip</subfield>
    <subfield code="z">md5:358389cc3783ad9603d0bce783856583</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">158102</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 265.10.fid.zip</subfield>
    <subfield code="z">md5:a6319a40cbf02a80292695a017f2d5c7</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">159607</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM 266.10.fid.zip</subfield>
    <subfield code="z">md5:25c443872f74dae812c8f4864f5af282</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">151967</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM269.10.fid.zip</subfield>
    <subfield code="z">md5:dfc20bb28b090b7a9201c69c42412b97</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">483492</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM269.11.fid.zip</subfield>
    <subfield code="z">md5:0228a168b063a75bf4b705bbebdd04a3</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">220009</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM269.12.fid.zip</subfield>
    <subfield code="z">md5:ac48da8a7a6123065786dca44f3f38a3</subfield>
  </datafield>
  <datafield tag="856" ind1="4" ind2=" ">
    <subfield code="s">1322385</subfield>
    <subfield code="u">https://rodare.hzdr.de/record/1257/files/RM269.zip</subfield>
    <subfield code="z">md5:9e01dd8e34ada9bc7a879c9eb2c9e68d</subfield>
  </datafield>
  <datafield tag="520" ind1=" " ind2=" ">
    <subfield code="a">&lt;p&gt;The &amp;sigma;2 receptor (transmembrane protein 97), which is involved in cholesterol homeostasis, is of high relevance for neoplastic processes. The upregulated expression of &amp;sigma;2 receptors in cancer cells and tissue in combination with the antiproliferative potency of &amp;sigma;2 receptor ligands motivates the research in the field of 2 receptors for the diagnosis and therapy of different types of cancer. Starting from the well described 2-(4-(1H-indol-1-yl)butyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline class of compounds, we synthesized a novel series of fluorinated derivatives, bearing the F-atom at the aromatic indole/azaindole subunit. RM273 (2-[4-(6-fluoro-1H-pyrrolo[2,3-b]pyridin-1-yl)butyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline) was selected for labelling with 18F and evaluation regarding detection of &amp;sigma;2 receptors in the brain by positron emission tomography. Initial metabolism and biodistribution studies of [18F]RM273 in healthy mice revealed promising penetration of the radioligand into the brain. Preliminary in vitro autoradiography on brain cryosections of an orthotopic rat glioblastoma model proved the potential of the radioligand to detect the upregulation of &amp;sigma;2 receptor in glioblastoma cells compared to healthy brain. The results indicate that the herein developed &amp;sigma;2 receptor ligand [18F]RM273 has potential to assess by non-invasive molecular imaging the correlation between the availability of &amp;sigma;2 receptors with properties of brain tumors such as tumor proliferation or resistance towards particular therapies&lt;/p&gt;</subfield>
  </datafield>
  <datafield tag="909" ind1="C" ind2="O">
    <subfield code="o">oai:rodare.hzdr.de:1257</subfield>
    <subfield code="p">openaire_data</subfield>
    <subfield code="p">user-health</subfield>
    <subfield code="p">user-rodare</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">dataset</subfield>
  </datafield>
  <datafield tag="245" ind1=" " ind2=" ">
    <subfield code="a">Data publication: Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand</subfield>
  </datafield>
  <datafield tag="773" ind1=" " ind2=" ">
    <subfield code="a">https://www.hzdr.de/publications/Publ-32485</subfield>
    <subfield code="i">isReferencedBy</subfield>
    <subfield code="n">url</subfield>
  </datafield>
  <datafield tag="773" ind1=" " ind2=" ">
    <subfield code="a">https://www.hzdr.de/publications/Publ-33346</subfield>
    <subfield code="i">isIdenticalTo</subfield>
    <subfield code="n">url</subfield>
  </datafield>
  <datafield tag="773" ind1=" " ind2=" ">
    <subfield code="a">10.14278/rodare.1256</subfield>
    <subfield code="i">isVersionOf</subfield>
    <subfield code="n">doi</subfield>
  </datafield>
  <datafield tag="100" ind1=" " ind2=" ">
    <subfield code="a">Moldovan, Rares-Petru</subfield>
    <subfield code="0">(orcid)0000-0003-3119-7945</subfield>
  </datafield>
  <controlfield tag="001">1257</controlfield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">user-health</subfield>
  </datafield>
  <datafield tag="980" ind1=" " ind2=" ">
    <subfield code="a">user-rodare</subfield>
  </datafield>
  <datafield tag="024" ind1=" " ind2=" ">
    <subfield code="a">10.14278/rodare.1257</subfield>
    <subfield code="2">doi</subfield>
  </datafield>
</record>

465

views

downloads

See more details...

	All versions	This version
Views	465	465
Downloads	42	42
Data volume	13.2 MB	13.2 MB
Unique views	201	201
Unique downloads	37	37

More info on how stats are collected.

Publication date:

November 9, 2021

DOI:

Keyword(s):

σ2 receptor transmembrane protein 97 azaindoles binding affinity radiochemistry fluorine-18 labeling positron emission tomography (PET) brain-penetration glioblastoma orthotopic

Related identifiers:

Identical to:
https://www.hzdr.de/publications/Publ-33346

Referenced by:
https://www.hzdr.de/publications/Publ-32485

Communities:

License (for files):

Creative Commons Attribution 4.0 International

Versions

Version 1 10.14278/rodare.1257

Nov 9, 2021

Cite all versions? You can cite all versions by using the DOI 10.14278/rodare.1256. This DOI represents all versions, and will always resolve to the latest one. Read more.

Data publication: Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand

MARC21 XML Export

Versions

Share

Cite as

Export

About

Help

Contribute

Follow us

Registered in

Data publication: Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand

MARC21 XML Export

RODARE DOI Badge

DOI

10.14278/rodare.1257

Markdown

[![DOI](https://rodare.hzdr.de/badge/DOI/10.14278/rodare.1257.svg)](https://doi.org/10.14278/rodare.1257)

reStructedText

.. image:: https://rodare.hzdr.de/badge/DOI/10.14278/rodare.1257.svg :target: https://doi.org/10.14278/rodare.1257

HTML

<a href="https://doi.org/10.14278/rodare.1257"><img src="https://rodare.hzdr.de/badge/DOI/10.14278/rodare.1257.svg" alt="DOI"></a>

Image URL

https://rodare.hzdr.de/badge/DOI/10.14278/rodare.1257.svg

Target URL

https://doi.org/10.14278/rodare.1257

Versions

Share

Cite as

Export