The automated radiosynthesis and purification of the opioid receptor antagonist, [6-O-methyl-11C]diprenorphine on the GE TRACERlab FXFE radiochemistry module.

[6-O-Methyl-(11)C]diprenorphine ([(11)C]diprenorphine) is a positron emission tomography ligand used to probe the endogenous opioid system in vivo. Diprenorphine acts as an antagonist at all of the opioid receptor subtypes, that is, μ (mu), κ (kappa) and δ (delta). The radiosynthesis of [(11)C]diprenorphine using [(11)C]methyl iodide produced via the 'wet' method on a home-built automated radiosynthesis set-up has been described previously. Here, we describe a modified synthetic method to [(11)C]diprenorphine performed using [(11)C]methyl iodide produced via the gas phase method on a GE TRACERlab FXFE radiochemistry module. Also described is the use of [(11)C]methyl triflate as the carbon-11 methylating agent for the [(11)C]diprenorphine syntheses. [(11)C]Diprenorphine was produced to good manufacturing practice standards for use in a clinical setting. In comparison to previously reported [(11)C]diprenorphine radiosyntheisis, the method described herein gives a higher specific activity product which is advantageous for receptor occupancy studies. The radiochemical purity of [(11)C]diprenorphine is similar to what has been reported previously, although the radiochemical yield produced in the method described herein is reduced, an issue that is inherent in the gas phase radiosynthesis of [(11)C]methyl iodide. The yields of [(11)C]diprenorphine are nonetheless sufficient for clinical research applications. Other advantages of the method described herein are an improvement to both reproducibility and reliability of the production as well as simplification of the purification and formulation steps. We suggest that our automated radiochemistry route to [(11)C]diprenorphine should be the method of choice for routine [(11)C]diprenorphine productions for positron emission tomography studies, and the production process could easily be transferred to other radiochemistry modules such as the TRACERlab FX C pro.

Fairclough M ，Prenant C ，Brown G ，McMahon A ，Lowe J ，Jones A ... -  《-》

Fully automated and reproducible radiosynthesis of high specific activity [¹¹C]raclopride and [¹¹C]Pittsburgh compound-B using the combination of two commercial synthesizers.

Gómez-Vallejo V ，Llop J 《-》

Automated radiosynthesis of [(18)F]ciprofloxacin.

We transferred the previously published manual synthesis of [(18)F]ciprofloxacin (decay-corrected RCY: 5.5±1.0%) to an automated synthesis module (TRACERlab(TM) FXFDG, GE Healthcare) and observed a strong decrease in RCY (0.4±0.4%). When replacing the standard 15-mL glassy carbon reactor of the synthesis module with a 3-mL V-shaped borosilicate glass reactor a considerable improvement in RCY was observed. [(18)F]Ciprofloxacin was obtained in a RCY of 2.7±1.4% (n=23) with a specific activity at EOS of 1.4±0.5GBq/µmol in a synthesis time of 160min.

Stanek J ，Mairinger S ，Wanek T ，Kuntner C ，Müller M ，Langer O ... -  《-》

Automated radiosynthesis of [18F]PBR111 and [18F]PBR102 using the Tracerlab FXFN and Tracerlab MXFDG module for imaging the peripheral benzodiazepine receptor with PET.

[(18)F]PBR111 and [(18)F]PBR102 are selective radioligands for imaging of the Peripheral Benzodiazepine Receptor (PBR). We have developed a fully automated method for the radiosynthesis of [(18)F]PBR111 and [(18)F]PBR102 in the Tracerlab FX(FN) (30±2% radiochemical yield non-decay-corrected for both tracers) and Tracerlab MX(FDG) (25±2% radiochemical yield non-decay-corrected for both tracers) from the corresponding p-toluenesulfonyl precursors. For all tracers, radiochemical purity was >99% and specific activity was >150GBq/μmol after less than 60min of preparation time.

Bourdier T ，Pham TQ ，Henderson D ，Jackson T ，Lam P ，Izard M ，Katsifis A ... -  《-》

Optimization of a Nucleophilic Two-Step Radiosynthesis of 6-O-(2-[(18)F]fluoroethyl)-6-O-desmethyl-diprenorphine ([(18)F]FE-DPN) for PET Imaging of Brain Opioid Receptors.

Németh E ，Gyuricza B ，Forgács V ，Cumming P ，Henriksen G ，Marton J ，Bauer B ，Mikecz P ，Fekete A ... -  《INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES》