dc.date.accessioned | 2024-02-20T18:09:26Z | |
dc.date.available | 2024-02-20T18:09:26Z | |
dc.date.created | 2023-10-31T13:54:38Z | |
dc.date.issued | 2023 | |
dc.identifier.citation | Németh, Enikő Gyuricza, Barbara Forgács, Viktória Cumming, Paul Henriksen, Gjermund Marton, János Bauer, Beate Mikecz, Pál Fekete, Anikó . Optimization of a Nucleophilic Two-Step Radiosynthesis of 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) for PET Imaging of Brain Opioid Receptors. International Journal of Molecular Sciences. 2023, 24(17) | |
dc.identifier.uri | http://hdl.handle.net/10852/108358 | |
dc.description.abstract | We have established a method for nucleophilic one-pot, two-step radiosynthesis of the popular opioid receptor radioligand 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) from the novel precursor 6-O-(2-tosyloxyethyl)-6-O-desmethyl- 3-O-trityl-diprenorphine (TE-TDDPN), which we designate as the Henriksen precursor. We undertook an optimization of the synthesis conditions, aiming to enhance the accessibility of [18F]FE-DPN for positron emission tomography (PET) studies of μ-opioid receptors. Herein, we report an optimized direct nucleophilic 18F-fluorination and the deprotection conditions for a fully automated radiosynthesis of [18F]FE-DPN on a modified GE Tracerlab FX FE synthesis panel. Starting from 1–1.5 GBq of [18F]fluoride and applying an Oasis Max 1cc cartridge for fluorine-18 trapping with a reduced amount of K2CO3 (5.06 μmol K+ ion), [18F]FE-DPN ([18F]11) was produced with 44.5 ± 10.6 RCY (decay-corrected), high radiochemical purity (>99%), and a molar activity of 32.2 ± 11.8 GBq/μmol in 60–65 min. | |
dc.language | EN | |
dc.rights | Attribution 4.0 International | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.title | Optimization of a Nucleophilic Two-Step Radiosynthesis of 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) for PET Imaging of Brain Opioid Receptors | |
dc.title.alternative | ENEngelskEnglishOptimization of a Nucleophilic Two-Step Radiosynthesis of 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) for PET Imaging of Brain Opioid Receptors | |
dc.type | Journal article | |
dc.creator.author | Németh, Enikő | |
dc.creator.author | Gyuricza, Barbara | |
dc.creator.author | Forgács, Viktória | |
dc.creator.author | Cumming, Paul | |
dc.creator.author | Henriksen, Gjermund | |
dc.creator.author | Marton, János | |
dc.creator.author | Bauer, Beate | |
dc.creator.author | Mikecz, Pál | |
dc.creator.author | Fekete, Anikó | |
cristin.unitcode | 185,51,0,0 | |
cristin.unitname | Institutt for medisinske basalfag | |
cristin.ispublished | true | |
cristin.fulltext | original | |
cristin.qualitycode | 1 | |
dc.identifier.cristin | 2190551 | |
dc.identifier.bibliographiccitation | info:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=International Journal of Molecular Sciences&rft.volume=24&rft.spage=&rft.date=2023 | |
dc.identifier.jtitle | International Journal of Molecular Sciences | |
dc.identifier.volume | 24 | |
dc.identifier.issue | 17 | |
dc.identifier.pagecount | 0 | |
dc.identifier.doi | https://doi.org/10.3390/ijms241713152 | |
dc.type.document | Tidsskriftartikkel | |
dc.type.peerreviewed | Peer reviewed | |
dc.source.issn | 1661-6596 | |
dc.type.version | PublishedVersion | |
cristin.articleid | 13152 | |