Rapastinel

• CAT Number: I000635
• CAS Number: 117928-94-6
• Molecular Formula: C18H31N5O6
• Molecular Weight: 413.5
• Purity: ≥95%
• Target: NMDA Receptor
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: Store at -20℃
• IUPAC Name: (2S)-1-[(2S)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]pyrrolidine-2-carboxamide
• InChI: InChI=1S/C18H31N5O6/c1-9(24)13(19)18(29)23-8-4-6-12(23)17(28)22-7-3-5-11(22)16(27)21-14(10(2)25)15(20)26/h9-14,24-25H,3-8,19H2,1-2H3,(H2,20,26)(H,21,27)/t9-,10-,11+,12+,13+,14+/m1/s1
• InChIKey: GIBQQARAXHVEGD-BSOLPCOYSA-N
• SMILES: O=C([C@@H](N)[C@H](O)C)N1[C@H](C(N2[C@H](C(N[C@H](C(N)=O)[C@H](O)C)=O)CCC2)=O)CCC1

Rapastinel (Cat.No:I000635) is a novel antidepressant drug and an NMDA receptor modulator. It belongs to the class of amino acid derivatives and has been studied for its rapid-acting antidepressant effects. Rapastinel works by enhancing synaptic plasticity and improving mood. Clinical trials are ongoing to evaluate its efficacy and safety for depression treatment.

Reference

1:Modulation of the activity of N-methyl-d-aspartate receptors as a novel treatment option for depression: current clinical evidence and therapeutic potential of rapastinel (GLYX-13). Vasilescu AN, Schweinfurth N, Borgwardt S, Gass P, Lang UE, Inta D, Eckart S.Neuropsychiatr Dis Treat. 2017 Mar 31;13:973-980. doi: 10.2147/NDT.S119004. eCollection 2017. Review. PMID: 28408831 Free PMC Article2:Effect of a Novel NMDA Receptor Modulator, Rapastinel (Formerly GLYX-13), in OCD: Proof of Concept. Rodriguez CI, Zwerling J, Kalanthroff E, Shen H, Filippou M, Jo B, Simpson HB, Burch RM, Moskal JR.Am J Psychiatry. 2016 Dec 1;173(12):1239-1241. No abstract available. PMID: 27903098 3:Comparison of R-ketamine and rapastinel antidepressant effects in the social defeat stress model of depression. Yang B, Zhang JC, Han M, Yao W, Yang C, Ren Q, Ma M, Chen QX, Hashimoto K.Psychopharmacology (Berl). 2016 Oct;233(19-20):3647-57. doi: 10.1007/s00213-016-4399-2. Epub 2016 Aug 4. PMID: 27488193 Free PMC Article4:The Development of Rapastinel (Formerly GLYX-13); A Rapid Acting and Long Lasting Antidepressant. Moskal JR, Burgdorf JS, Stanton PK, Kroes RA, Disterhoft JF, Burch RM, Khan MA.Curr Neuropharmacol. 2017;15(1):47-56. Review. PMID: 26997507 5:GLYX-13 (rapastinel) ameliorates subchronic phencyclidine- and ketamine-induced declarative memory deficits in mice. Rajagopal L, Burgdorf JS, Moskal JR, Meltzer HY.Behav Brain Res. 2016 Feb 15;299:105-10. doi: 10.1016/j.bbr.2015.10.060. Epub 2015 Nov 26. PMID: 26632337 Free PMC Article6:The long-lasting antidepressant effects of rapastinel (GLYX-13) are associated with a metaplasticity process in the medial prefrontal cortex and hippocampus. Burgdorf J, Zhang XL, Weiss C, Gross A, Boikess SR, Kroes RA, Khan MA, Burch RM, Rex CS, Disterhoft JF, Stanton PK, Moskal JR.Neuroscience. 2015 Nov 12;308:202-11. doi: 10.1016/j.neuroscience.2015.09.004. Epub 2015 Sep 4. PMID: 26343295 Free PMC Article7:Rapastinel (GLYX-13) has therapeutic potential for the treatment of post-traumatic stress disorder: Characterization of a NMDA receptor-mediated metaplasticity process in the medial prefrontal cortex of rats. Burgdorf J, Kroes RA, Zhang XL, Gross AL, Schmidt M, Weiss C, Disterhoft JF, Burch RM, Stanton PK, Moskal JR.Behav Brain Res. 2015 Nov 1;294:177-85. doi: 10.1016/j.bbr.2015.07.039. Epub 2015 Jul 22. PMID: 26210936 Free PMC Article