Jane Eyre Adapted

Lodge, Sara; Tredell, Nicolas

doi:10.1007/978-1-137-08603-7_8

Cited by 1 publication

(1 citation statement)

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“…These modulatory functions have positioned KARs as potential therapeutic targets, and thus KAR antagonists have emerged for the amelioration of several neurological disorders such as epilepsy, migraine and chronic pain. [127][128][129] Compared with the development of other iGluR PET tracers, the progress of imaging KARs has lagged behind, possibly due to unavailability of suitable high-affinity and high-selectivity ligands. The only candidate KAR PET tracer [ 11 C]51 (Figure 4) to date was reported by Suzuki in 2011, which undesirably showed higher affinity to AMPARs rather than to KARs.…”

Section: Pet Tracer Development Towards Imaging Karsmentioning

confidence: 99%

Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting N-Methyl-d-aspartate (NMDA), α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors

Chen

Josephson

et al. 2018

J. Med. Chem.

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Ionotropic glutamate receptors (iGluRs) mediate excitatory neurotransmission within the mammalian central nervous system. iGluRs exist as three main groups: N-methyl-d-aspartate receptors (NMDARs), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs), and kainate receptors. The past decades have witnessed a remarkable development of PET tracers targeting different iGluRs including NMDARs and AMPARs, and several of the tracers have advanced to clinical imaging studies. Here, we assess the recent development of iGluR PET probes, focusing on tracer design, brain kinetics, and performance in PET imaging studies. Furthermore, this review will not only present challenges in the tracer development but also provide novel approaches in conjunction with most recent drug discovery efforts on these iGluRs, including subtype-selective NMDAR and transmembrane AMPAR regulatory protein modulators and positive allosteric modulators (PAMs) of AMPARs. These approaches, if successful as PET tracers, may provide fundamental knowledge to understand the roles of iGluR receptors under physiological and pathological conditions.

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Section: Pet Tracer Development Towards Imaging Karsmentioning

confidence: 99%