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

ABSTRACT:

Introduction

We recently reported ¹¹C-NR2B-SMe ([S-methyl-¹¹C](R,S)-7-thiomethoxy-3-(4-(4-methyl-phenyl)butyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1-ol) and its enantiomers as candidate radioligands for imaging the GluN2B subunit within rat N-methyl-D-aspartate receptors. However, these radioligands gave unexpectedly high and displaceable binding in rat cerebellum, possibly due to cross-reactivity with sigma-1 (σ1) receptors. This study investigated ¹¹C-labeled enantiomers of a close analogue (7-methoxy-3-(4-(p-tolyl)butyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1-ol; NR2B-Me) of ¹¹C-NR2B-SMe as new candidate GluN2B radioligands. PET was used to evaluate these radioligands in rats and to assess potential cross-reactivity to σ1 receptors.

SUBMITTER: Cai L 

PROVIDER: S-EPMC10076467 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature