Basic information Safety Supplier Related

GLYX13

Basic information Safety Supplier Related

GLYX13 Basic information

Product Name:
GLYX13
Synonyms:
  • Rapastinel Trifluoroacetate
  • GLYX 13,inhibit,Rapastinel Trifluoroacetate,GLYX13,GLYX-13,Inhibitor,Rapastinel,Ionotropic glutamate receptors,iGluR
  • Rapastinel Trifluoroacetate, 10 mM in DMSO
CAS:
1435786-04-1
MF:
C20H32F3N5O8
MW:
527.5
Mol File:
1435786-04-1.mol
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GLYX13 Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMSO : 125 mg/mL (236.97 mM)
form 
Solid
color 
White to off-white
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GLYX13 Usage And Synthesis

Uses

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.

in vivo

Rapastinel Trifluoroacetate is an NMDA receptor modulator with glycine-site partial agonist properties and currently in a phase II clinical development program as an adjunctive therapy for major depressive disorder. Mice given Rapastinel Trifluoroacetate (1.0 mg/kg) prior to acute ketamine (30 mg/kg) show clear preference for novel compare to familiar objects (P<0.01)[1]. Rapastinel Trifluoroacetate produces an antidepressant like effect in the USVs test, as indexed by an increase in hedonic 50-kHz USVs [F(1,20)=12.4, P<0.05] and a decrease in aversive 20-kHz USVs [F(1,20)=6.8, P<0.05]. Rapastinel Trifluoroacetate also produces an anxiolytic effect in the open field, as indexed by increased center time [F(1,20)=19.2, P<0.05] without altering locomotor activity as measured by line crosses [F(1,20)=0.0, P>0.05][2].

IC 50

NMDA Receptor

References

[1] Rajagopal L, et al. GLYX-13 (rapastinel) ameliorates subchronic phencyclidine- and ketamine-induced declarative memory deficits in mice. Behav Brain Res. 2016 Feb 15;299:105-10. DOI:10.1016/j.bbr.2015.10.060
[2] 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 Nov 12;308:202-11. DOI:10.1016/j.neuroscience.2015.09.004

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