Synthesis of [11C]NR2B-SMe for evaluation as a PET radioligand for NR2B subunits in NMDA receptors

Conclusions: [11C]NR2B-SMe was readily synthesized, and showed high brain uptake in rat, which could be pre-blocked by NR2B-SMe itself, elipodil, ifenprodil, and by a selective sigma-1 receptor ligand. Because sigma-1 receptors serve as multitasking ion channel protein chaperones [4] with involvement in modulation of NMDA activity [5], and are now known to interact directly with the N-terminal domains of NR1 and NR2B subunits [6], further study is required to characterize the nature of the specific binding of [11C]NR2B-SMe in rat brain and its utility in brain research. These studies are ongoing. Research Support: Intramural Research Program of the National Insitutes of Health (NIMH). References: [1] Zhuo M, Neuropharmacology, 2017, 112, 228. [2] Kassenbrock A, Vasdev N, Liang SH. Curr. Top. Med. Chem. 2016; 16, 1830. [3] Krämer SD et al.,J. Nucl. Med. doi:10.2967/jnumed.117.200451. [4] Chu UB, Ruoho AE, Mol Phamrmacol. 2016, 89, 143. [5] Zhang XJ et al., Neurosignals 2011, 19, 110. [6] Balasuriya D et al., J. Neurosci 2013, 33, 18219.
Source: Journal of Nuclear Medicine - Category: Nuclear Medicine Authors: Tags: Probes for Neuroimaging I Source Type: research