Pharmacological Characterization of [
NMDA receptors
Neuroimaging
Positron-emission tomography
Journal
Molecular imaging and biology
ISSN: 1860-2002
Titre abrégé: Mol Imaging Biol
Pays: United States
ID NLM: 101125610
Informations de publication
Date de publication:
08 2023
08 2023
Historique:
received:
21
10
2022
accepted:
01
03
2023
revised:
27
02
2023
medline:
12
7
2023
pubmed:
23
3
2023
entrez:
22
3
2023
Statut:
ppublish
Résumé
NMDA receptors (NMDARs) dysfunction plays a central role in the physiopathology of psychiatric and neurodegenerative disorders whose mechanisms are still poorly understood. The development of a PET (positron emission tomography) tracer able to selectively bind to the NMDARs intra-channel PCP site may make it possible to visualize NMDARs in an open and active state. We describe the in vitro pharmacological characterization of [ The affinity of the non-radioactive analog for the intra-channel PCP site was determined in a radioligand competition assay using [ FNM displayed IC In spite of FNM's poor affinity for NMDAR PCP site, this study supports the ability of this tracer to track massive activation of NMDARs in neurological diseases.
Identifiants
pubmed: 36944798
doi: 10.1007/s11307-023-01811-y
pii: 10.1007/s11307-023-01811-y
pmc: PMC10333392
doi:
Substances chimiques
Receptors, N-Methyl-D-Aspartate
0
Phencyclidine
J1DOI7UV76
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
692-703Informations de copyright
© 2023. The Author(s).
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