491872-39-0
Chemical Structure
Rapastinel acetate
Synonym(s): GLYX-13 acetate
- CAS No.: 491872-39-0
- Formula:C20H35N5O8
- Molecular Weight:473.52
IUPAC Name: (S)-1-(L-threonyl-L-prolyl)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)pyrrolidine-2-carboxamide acetate
InChIKey: MNEQLJKNUQMKNP-GDLIIDCZSA-N
SMILES: CC(O)=O.O=C(N(CCC1)[C@@H]1C(N[C@H](C(N)=O)[C@H](O)C)=O)[C@H](CCC2)N2C([C@@H](N)[C@H](O)C)=O
Biological Activity: Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate 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 acetate 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 acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma[1][2][3][4][5].
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Rapastinel acetate | Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate 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 acetate 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 acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma. | |||||||||||||||||||||
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- [1]. Shen M, et al. ERK/mTOR signaling may underlying the antidepressant actions of rapastinel in mice. Transl Psychiatry. 2022;12(1):522. Published 2022 Dec 22. [Content Brief]
- [2]. Qi J, et al. Propofol attenuates the adhesion of tumor and endothelial cells through inhibiting glycolysis in human umbilical vein endothelial cells. Acta Biochim Biophys Sin (Shanghai). 2019;51(11):1114-1122. [Content Brief]
- [3]. Burgdorf J, et al. The long-lasting antidepressant effects of rapastinel (GLYX-13) are associated with a metaplasticity process in the medial prefrontal cortex and hippocampus. Neuroscience. 2015;308:202-211. [Content Brief]
- [4]. Rajagopal L, et al. Repeated administration of rapastinel produces exceptionally prolonged rescue of memory deficits in phencyclidine-treated mice. Behav Brain Res. 2022;432:113964. [Content Brief]
- [5]. Donello JE, et al. Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects. Int J Neuropsychopharmacol. 2019;22(3):247-259. [Content Brief]
Keywords
