Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR ( EC 50 =0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF , and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma.
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