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.

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 p

SUBMITTER: Nemeth E 

PROVIDER: S-EPMC10487412 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature