Evaluation of a First PET Tracer Suitable for Imaging the Sigma-2 Receptor in the Brain of Nonhuman Primates

Mol Pharm. 2024 Jan 1;21(1):194-200. doi: 10.1021/acs.molpharmaceut.3c00750. Epub 2023 Nov 28.

Abstract

The sigma-2 receptor (σ2R), recently identified as transmembrane protein 97, is expressed in many cell types and mediates important functions in both the peripheral and central nervous systems. Over the years, σ2R has emerged as a potential therapeutic target for cancer and neurological disorders such as Alzheimer's disease (AD). The currently available σ2R radiotracers have been developed primarily for cancer imaging with limited brain uptake. Here, we report the evaluation of the first brain penetrant 18F-labeled radiotracer suitable for positron emission tomography (PET) imaging of σ2R in nonhuman primate brain.

Keywords: SYB4; brain imaging; nonhuman primate; radiotracer; sigma-2.

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Macaca mulatta
  • Neoplasms*
  • Positron-Emission Tomography / methods
  • Primates
  • Radiopharmaceuticals*

Substances

  • sigma-2 receptor
  • Radiopharmaceuticals