Development of PET and SPECT Probes for Glutamate Receptors
ABSTRACT
L-Glutamate and its receptors (GluRs) play a key role in excitatory neurotransmission
within the mammalian central nervous system (CNS). Impaired regulation
of GluRs has also been implicated in various neurological disorders. GluRs
are classified into two major groups: ionotropic GluRs (iGluRs), which
are ligand-gated ion channels, and metabotropic GluRs (mGluRs), which are
coupled to heterotrimeric guanosine nucleotide binding proteins (G-proteins).
Positron emission tomography (PET) and single photon emission computed
tomography (SPECT) imaging of GluRs could provide a novel view of CNS function
and of a range of brain disorders, potentially leading to the development
of new drug therapies. Although no satisfactory imaging agents have yet
been developed for iGluRs, several PET ligands for mGluRs have been successfully
employed in clinical studies. This paper reviews current progress towards
the development of PET and SPECT probes for GluRs.