Nowadays PSMA ligands are widely used for radiotheragnostic purposes of prostate cancer. The goal of this study was to synthesize and estimate stability in vitro of copper complex with diacetate bispidine ligand (Bisp1), its bifunctional derivative (Bisp-alkyne) and its conjugate – bispidine-PSMA ligand (PSMA-Bisp) to evaluate the possibility of applying one as radiotheragnostic agent. The synthesis for PSMA-Bisp conjugate was developed and realized with good yields. All newly synthesized compounds were characterized by a set of physicochemical methods: 1H and 13C NMR, HRMS and LCMS (for final molecules). Subsequently, Bisp1 and Bisp-alkyne and its derivative PSMA-Bisp were labelled by 64Cu at mild conditions. In vitro studies of the labelled conjugate [64Cu]Cu-PSMA-Bisp have shown the great stability in model solutions. Finally, [64Cu]Cu-PSMA-Bisp was compared to well-known PSMA-617 conjugate labelled with 64Cu and they have showed similar stability in excess of bovine serum (BVS), and at the same time labelling PSMA-Bisp with 64Cu is characterized by extremely high kinetics at mild conditions, while labeling PSMA-617 with 64Cu requires heating (90 °C) [PMCID: PMC5435610]. Thus, the conjugate PSMA-Bisp could be promising candidate for further investigations expanded in vitro and in vivo investigations.