Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-11C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ1-Receptor–Targeted PET Imaging

• Published in: The Journal of nuclear medicine (1978) Vol. 60; no. 8; pp. 1167 - 1173
• Main Authors: Haider, Ahmed, Herde, Adrienne Müller, Krämer, Stefanie D, Varisco, Jasmine, Keller, Claudia, Frauenknecht, Katrin, Auberson, Yves P, Temme, Louisa, Robaa, Dina, Sippl, Wolfgang, Schibli, Roger, Wünsch, Bernhard, Mu, Linjing, Ametamey, Simon M
• Format: Journal Article
• Language: English
• Published: New York Society of Nuclear Medicine 01.08.2019
• Subjects: Autoradiography; Binding; Brain; Brain slice preparation; Cerebellum; Cortex; Enantiomers; Forebrain; Glutamic acid receptors (ionotropic); High performance liquid chromatography; Imaging; Liquid chromatography; N-Methyl-D-aspartic acid receptors; Neostriatum; Neuroimaging; Occupancy; Phenolic compounds; Phenols; Positron emission; Positron emission tomography; Precursors; Radiochemistry; Radioisotopes; Receptors; Rodents; Selectivity; Target recognition; Thalamus; Tomography

The study aims to investigate the performance characteristics of the enantiomers of 11C-Me-NB1, a recently reported PET imaging probe that targets the GluN2B subunit of N-methyl-d-aspartate (NMDA) receptors. Methods: Reference compound Me-NB1 (inhibition constant for hGluN1/GluN2B, 5.4 nM) and the p...