Dataset Open Access
Teodoro, Rodrigo; Gündel, Daniel; Deuther-Conrad, Winnie; Toussaint, Magali; Wenzel, Barbara; Bormans, Guy; Kopka, Klaus; Brust, Peter; Moldovan, Rares-Petru
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rdf:about="https://doi.org/10.14278/rodare.2252"> <rdf:type rdf:resource="http://www.w3.org/ns/dcat#Dataset"/> <dct:type rdf:resource="http://purl.org/dc/dcmitype/Dataset"/> <dct:identifier rdf:datatype="http://www.w3.org/2001/XMLSchema#anyURI">https://doi.org/10.14278/rodare.2252</dct:identifier> <foaf:page rdf:resource="https://doi.org/10.14278/rodare.2252"/> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0002-1425-0567"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Teodoro, Rodrigo</foaf:name> <foaf:givenName>Rodrigo</foaf:givenName> <foaf:familyName>Teodoro</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0001-9743-2325"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Gündel, Daniel</foaf:name> <foaf:givenName>Daniel</foaf:givenName> <foaf:familyName>Gündel</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0003-3168-3062"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Deuther-Conrad, Winnie</foaf:name> <foaf:givenName>Winnie</foaf:givenName> <foaf:familyName>Deuther-Conrad</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0002-1136-3857"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Toussaint, Magali</foaf:name> <foaf:givenName>Magali</foaf:givenName> <foaf:familyName>Toussaint</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0001-7390-3575"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Wenzel, Barbara</foaf:name> <foaf:givenName>Barbara</foaf:givenName> <foaf:familyName>Wenzel</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Bormans, Guy</foaf:name> <foaf:givenName>Guy</foaf:givenName> <foaf:familyName>Bormans</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0003-4846-1271"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Kopka, Klaus</foaf:name> <foaf:givenName>Klaus</foaf:givenName> <foaf:familyName>Kopka</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0001-5555-7058"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Brust, Peter</foaf:name> <foaf:givenName>Peter</foaf:givenName> <foaf:familyName>Brust</foaf:familyName> </rdf:Description> </dct:creator> <dct:creator> <rdf:Description rdf:about="http://orcid.org/0000-0003-3119-7945"> <rdf:type rdf:resource="http://xmlns.com/foaf/0.1/Agent"/> <foaf:name>Moldovan, Rares-Petru</foaf:name> <foaf:givenName>Rares-Petru</foaf:givenName> <foaf:familyName>Moldovan</foaf:familyName> </rdf:Description> </dct:creator> <dct:title>Data publication: Enantioselective Synthesis, Structure Activity Relationship, Radiofluorination and Biological Evaluation of [18F]RM365, a Novel Radioligand for Imaging the Human Cannabinoid Receptor Type 2 (CB2R) in the Brain with PET</dct:title> <dct:publisher> <foaf:Agent> <foaf:name>Rodare</foaf:name> </foaf:Agent> </dct:publisher> <dct:issued rdf:datatype="http://www.w3.org/2001/XMLSchema#gYear">2023</dct:issued> <dcat:keyword>cannabinoid receptor type 2</dcat:keyword> <dcat:keyword>indole-2-carboxamide</dcat:keyword> <dcat:keyword>binding affinity</dcat:keyword> <dcat:keyword>radiochemistry</dcat:keyword> <dcat:keyword>fluorine-18 labeling</dcat:keyword> <dcat:keyword>positron-emission tomography</dcat:keyword> <dct:issued rdf:datatype="http://www.w3.org/2001/XMLSchema#date">2023-04-05</dct:issued> <owl:sameAs rdf:resource="https://rodare.hzdr.de/record/2252"/> <adms:identifier> <adms:Identifier> <skos:notation rdf:datatype="http://www.w3.org/2001/XMLSchema#anyURI">https://rodare.hzdr.de/record/2252</skos:notation> </adms:Identifier> </adms:identifier> <owl:sameAs rdf:resource="https://www.hzdr.de/publications/Publ-36778"/> <dct:isReferencedBy rdf:resource="https://www.hzdr.de/publications/Publ-35005"/> <dct:isVersionOf rdf:resource="https://doi.org/10.14278/rodare.2251"/> <dct:isPartOf rdf:resource="https://rodare.hzdr.de/communities/rodare"/> <dct:description><p>The development of cannabinoid receptor type 2 (CB2R) PET radioligands has been intensively explored due to the pronounced CB2R upregulation in various pathological conditions, such as neuroinflammation and cancer. Herein we report on the enantioselective synthesis of a series of highly affine fluorinated indole-2-carboxamide ligands targeting the CB2R in the brain. Compound RM365 was selected for PET radiotracer development due to its high CB2R affinity (Ki = 2.1 nM) and pronounced selectivity over CB1R (factor &gt; 300). A fully automated copper-mediated radiofluorination of [18F]RM365 was established starting from the corresponding aryl boronic acid pinacol ester precursor. Preliminary in vitro evaluation of [18F]RM365 indicated species differences in the binding to CB2R (KD of 2.32 nM for the human CB2R vs. KD &gt; 10000 nM for the rat CB2R). Metabolism studies in mice revealed high stability of [18F]RM365 with fractions of parent compound of &gt; 90% in the brain and &gt; 54% in the plasma at 30 min p.i. PET imaging in a rat model of local hCB2R(D80N) overexpression in the brain demonstrate the ability of [18F]RM365 to reach and selectively label the intracranial expressed hCB2R(D80N) with high signal-to-background ratio. Thus, [18F]RM365 is a very promising PET radioligand for the imaging of upregulated hCB2R expression under pathological conditions with high potential towards clinical application in humans.</p></dct:description> <dct:accessRights rdf:resource="http://publications.europa.eu/resource/authority/access-right/PUBLIC"/> <dct:accessRights> <dct:RightsStatement rdf:about="info:eu-repo/semantics/openAccess"> <rdfs:label>Open Access</rdfs:label> </dct:RightsStatement> </dct:accessRights> <dcat:distribution> <dcat:Distribution> <dct:rights> <dct:RightsStatement rdf:about="https://creativecommons.org/licenses/by/4.0/legalcode"> <rdfs:label>Creative Commons Attribution 4.0 International</rdfs:label> </dct:RightsStatement> </dct:rights> <dcat:accessURL rdf:resource="https://doi.org/10.14278/rodare.2252"/> </dcat:Distribution> </dcat:distribution> </rdf:Description> </rdf:RDF>
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