Biodistribution and dosimetry of the GluN2B-specific NMDA receptor PET radioligand (R)-[¹¹C]Me-NB1.

ABSTRACT:

Background

The NMDA receptor (NMDAR) plays a key role in the central nervous system, e.g., for synaptic transmission. While synaptic NMDARs are thought to have protective characteristics, activation of extrasynaptic NMDARs might trigger excitotoxic processes linked to neuropsychiatric disorders. Since extrasynaptic NMDARs are typically GluN2B-enriched, the subunit is an interesting target for drug development and treatment monitoring. Recently, the novel GluN2B-specific PET radioligand (R)-[¹¹C]Me-NB1 was investigated in rodents and for the first time successfully translated to humans. To assess whether (R)-[¹¹C]Me-NB1 is a valuable radioligand for (repeated) clinical applications, we evaluated its safety, biodistribution and dosimetry.

Methods

Four hea

SUBMITTER: Rischka L 

PROVIDER: S-EPMC9418393 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature