Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization

A potent sigma-2 receptor ligand, known as PB28, was tritium radiolabelled and biologically evaluated. The results showed that [3H]PB28 and the corresponding unlabelled PB28 had superimposed pharmacodynamic properties. This radioligand appears as a potential candidate for receptor binding and in living cells assays.

Graphical abstractThe radiosynthesis and pharmacodymamic properties of the powerful sigma-2 agonist PB28 (Kd = 0.12 nM) are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide