Radiosynthesis of (N-[11C]methyl)benperidol for PET investigation of D2 receptor binding

Abstract

Abstract A procedure for the reliable production of the novel PET D2 receptor ligand (N-[11C]methyl)benperidol ([11C]NMB) is described. The method is based on N-methylation of benperidol using [11C]methyl iodide from the PETtrace MeI MicroLab, with product purification via normal-phase HPLC. Batch yields of 2.5±0.9 GBq (68±25 mCi) of [11C]NMB are routinely (n=16) obtained, with a radiochemical purity >98% and an average specific activity of over 40.7 TBq (1100 Ci)/mmol. The overall radiosynthesis, purification, and pre-release quality control testing is accomplished within 50 minutes. The procedure described herein produces a radiopharmaceutical product that is suitable for D2 receptor studies using PET or microPET imaging.