Drug intelligence / Profile preview

[11C]Me-NB1

Development stage
Preclinical
Lead developer
ETH Zurich
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[11C]Me-NB1 is a **carbon-11-labeled positron emission tomography (PET) radioligand** developed for in vivo imaging of the GluN2B subunit of N-methyl-D-aspartate (NMDA) receptors in the brain. It is based on a benzazepine scaffold related to ifenprodil and exhibits high selectivity and affinity (Ki to human GluN1/GluN2B of 5.4 nM) for GluN2B-containing NMDA receptors, with significantly lower affinity for Sigma-1 and Sigma-2 receptors. The compound exists as two enantiomers with distinct target binding profiles: the R-enantiomer, (R)-[11C]Me-NB1, is highly selective for the GluN2B subunit of the NMDA receptor, while the S-enantiomer, (S)-[11C]Me-NB1, binds primarily to Sigma-1 (σ1) receptors. The radioligand enables visualization and quantification of GluN2B expression and receptor occupancy in animal models and has also demonstrated suitability for human brain imaging[1][2][5][6][8]. Its primary application is in research and clinical investigation of neurological and psychiatric diseases where NMDA receptor dysregulation is implicated.

Other names
[11C]-Me-NB1Carbon-11 Me-NB1Carbon11 Me-NB1Carbon 11 Me-NB1
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)

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