4.1 Article

Neuroimaging with Radiopharmaceuticals Targeting the Glutamatergic System

Journal

CHIMIA
Volume 74, Issue 12, Pages 960-967

Publisher

SWISS CHEMICAL SOC
DOI: 10.2533/chimia.2020.960

Keywords

Glutamate receptors; GluN2B subunit of the ionotropic NMDA receptor; Metabotropic glutamate receptor subtype 5 (mGluR5); PET tracer evaluation

Funding

  1. Technology Transfer Project of the Personalized Health and Related Technology (PHRT) initiative of the ETH Domain [PHRT-512]
  2. Swiss National Science Foundation [310030E160403/1, 310030E_182872/1]
  3. Swiss National Science Foundation (SNF) [310030E_182872] Funding Source: Swiss National Science Foundation (SNF)

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Radiopharmacy at ETH has worked on the development of novel PET tracers for neuro-, cardiac- and tumor imaging for many years. In this paper, our efforts on targeting the glutamatergic system of the metabotropic glutamate receptor subtype 5 (mGluR5) and the ionotropic N-methyl-D-aspartate (NMDA) receptor are summarized. We briefly described the principles of positron emission tomography (PET) tracer development for the central nervous system (CNS) and the radiolabeling methods used in our laboratory. To assess the radioligands, results of in vitro autoradiography, biodistribution, and metabolite studies as well as PET imaging data are discussed. Furthermore, key PET parameters for kinetic modeling and quantification methods are provided. Two mGluR5 PET tracers, [C-11]ABP688 and [F-18]PSS232, were translated in our GMP labs and evaluated in human subjects. The newly developed GluN2B PET tracer [11C]Me-NB1 is currently being investigated in a first-in-human PET study and several F-18 labeled tracers are being evaluated in non-human primates in which the first-in-class will be translated for human studies.

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