Selectivity of probes for PET imaging of dopamine D3 receptors.

Robert K Doot, Jacob G Dubroff, Kyle J Labban, Robert H Mach

Journal: Neuroscience letters 2019;691():18-25

PMID: 29518538

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Abstract

Dopamine D3 receptors have key roles in behavioral reward, addiction, Parkinson's disease, and schizophrenia, and there is interest in studying their role in these disorders using PET. However, current PET radiotracers for studying D3 receptors in humans all bind to both D2 and D3 due to similarities between the two receptors. Selective D2 and D3 radioligands would aid investigation of the differences between D2 and D3 circuitry in the central nervous system. While there are currently in vitro measures of ligand D3/D2 selectivity, there is a need for an in vivo PET measure of D3/D2 selectivity. This review discusses current PET imaging of dopamine D2/D3 receptors and proposes methodology for quantitating in vivo selectivity of probes for PET imaging of dopamine D3 receptors.

Address: Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA. Electronic address: [email protected].; Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.

DOI: 10.1016/j.neulet.2018.03.006

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MeSH Terms: Autoradiography, Carbon Radioisotopes, Fluorine Radioisotopes, Humans, Ligands, Positron-Emission Tomography, Receptors, Dopamine D2, Receptors, Dopamine D3