In Vivo [¹⁸F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates.

ABSTRACT: As one of the major excitatory ion channels in the brain, NMDA receptors have been a leading research target for neuroscientists, physicians, medicinal chemists, and pharmaceutical companies for decades. Molecular imaging of NMDA receptors by means of positron emission tomography (PET) with [¹⁸F]GE-179 quickly progressed to clinical PET studies, but a thorough understanding of its binding specificity has been missing and has thus limited signal interpretation. Here a preclinical study with [¹⁸F]GE-179 in rodents and nonhuman primates (NHPs) is presented in an attempt to characterize [¹⁸F]GE-179 signal specificity. Rodent PET/CT was used to study drug occupancy and functional manipulation in rats by pretreating animals with NMDA targeted blocking/modulating

SUBMITTER: Schoenberger M 

PROVIDER: S-EPMC5894869 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature