Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors

Autor:	Lisheng Cai, Jeih-San Liow, Cheryl L. Morse, Sanjay Telu, Riley Davies, Lester S. Manly, Sami S. Zoghbi, Frederick T. Chin, Robert B. Innis, Victor W. Pike
Jazyk:	angličtina
Rok vydání:	2023
Předmět:	GluN2B NMDA receptor σ1 receptor NR2B-Me PET Medical physics. Medical radiology. Nuclear medicine R895-920
Zdroj:	EJNMMI Research, Vol 13, Iss 1, Pp 1-11 (2023)
Druh dokumentu:	article
ISSN:	2191-219X
DOI:	10.1186/s13550-023-00975-6
Popis:	Key points Question: Do GluN2B radioligands 11C-NR2B-Me enantiomers show cross-binding with σ1 receptors in brain in vivo? Pertinent findings: 11C-(+)-NR2B-Me, 11C-(−)-NR2B-Me, 11C-(S)-NR2B-SMe, and 11C-(R)-NR2B-SMe give specific signals in whole rat brain that could be pre-blocked and displaced using ligands that specifically target GluN2B receptors, but not by σ1 ligand FTC-146. Implications for patient care: 11C-(−)-NR2B-Me does not show cross-binding with σ1 receptor in rat brain using PET imaging. This radioligand may be promising for human PET imaging.
Databáze:	Directory of Open Access Journals
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