Nr2b

Conclusions: The 1 receptor-selective radioligand [18F]FTC146 was used in PET imaging of rat brain. It showed high brain uptake, which could be pre-blocked by self, a 1 receptor ligand BD1047, and a NR2B-selective ligand NR2B-SMe, but at markedly different ED50 values. The ED50 for avidly brain-penetrant NR2B-SMe gave by far the highest value, implying only weak interaction with 1 receptors. Influence of 1 receptors on the PET imaging of NR2B receptors with [11C]NR2B-SMe is therefore likely negligible. Research Support: Intramural Research Program of the National Insitutes of Health (NIMH). References: [1] Zhuo M, Neuropharmacology, 2017, 112, 228. [2] Kassenbrock A, et al., Curr. Top. Med. Chem. 2016; 16, 1830. [3] Cai L et al., J. Nucl. Med. 2020, In press. [4] Pabba M and Sibille E. Mol. Neuropsychiatry, 2015, 1, 47. [5] James ML et al., J. Med. Chem. 2012, 55, 8272.

Source: Journal of Nuclear Medicine - May 14, 2020 Category: Nuclear Medicine Authors: Cai, L., Liow, J.-S., Morse, C., Davies, R., Manly, L., Zoghbi, S., Innis, R., Pike, V. Tags: Basic Science - Synaptic activity and other mechanisms Source Type: research