Automated preparation of the dopamine D2/3 receptor agonist ligand [11C]-(+)-PHNO for human PET imaging studies

Carbon-11 labelled (+)-4-Propyl-3,4,4a,5,6,10b-hexahydro-2H-naphtho[1,2-b][1,4]oxazin-9-ol ([11C]-(+)-PHNO) is used as a high-affinity state, dopamine D2/3 receptor ligand in clinical PET studies. To facilitate its use, robust, rapid, efficient and GMP compliant methods are required for the manufacturing and QC testing processes. Additionally, to allow for full quantification of the resulting signal in the CNS, a reliable method is required to establish the parent plasma concentration over the course of the scan. This paper provides high-quality methods to support clinical application of [11C]-(+)-PHNO.

► Fully automated synthesis of [11C]-(+)-PHNO. ► Rapid multi-step synthesis and QC analysis. ► Reproducible synthesis process typically yielding more than 3 GBq of [11C]-(+)-PHNO. ► Very low failure rate.