Németh, Enikő; Gyuricza, Barbara; Forgács, Viktória; Cumming, Paul; Henriksen, Gjermund; Marton, János; Bauer, Beate; Mikecz, Pál; Fekete, Anikó (2023). 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, 24(17) MDPI 10.3390/ijms241713152
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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.
Item Type: |
Journal Article (Original Article) |
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Division/Institute: |
04 Faculty of Medicine > Department of Radiology, Neuroradiology and Nuclear Medicine (DRNN) > Clinic of Nuclear Medicine |
UniBE Contributor: |
Cumming, Paul |
Subjects: |
600 Technology > 610 Medicine & health |
ISSN: |
1422-0067 |
Publisher: |
MDPI |
Language: |
English |
Submitter: |
Pubmed Import |
Date Deposited: |
11 Sep 2023 14:16 |
Last Modified: |
11 Sep 2023 14:24 |
Publisher DOI: |
10.3390/ijms241713152 |
PubMed ID: |
37685958 |
Uncontrolled Keywords: |
6,14-ethenomorphinans 6-O-(2-[18F]fluoroethyl)-6-O-desmethyl-diprenorphine nucleophilic radiosynthesis opioid receptors orvinols positron emission tomography |
BORIS DOI: |
10.48350/186192 |
URI: |
https://boris.unibe.ch/id/eprint/186192 |
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