1435786-04-1

1435786-04-1 structure
1435786-04-1 structure
  • Name: Rapastinel Trifluoroacetate
  • Chemical Name: Rapastinel Trifluoroacetate
  • CAS Number: 1435786-04-1
  • Molecular Formula: C20H32F3N5O8
  • Molecular Weight: 527.49
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
  • Create Date: 2018-04-19 17:28:18
  • Modify Date: 2024-01-07 18:36:31
  • 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.

Name Rapastinel Trifluoroacetate
Description 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.
Related Catalog
Target

NMDA receptor[1]

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].
Animal Admin Male C57BL/6J mice are used in this study. Mice are group housed (five/cage) in a controlled environment held at 21±2°C with a 14:10 h light-dark period (lights on:±05:00 am). All experiments are conducted during the light phase. Food and water are available ad libitum. For acute drug treatments, Rapastinel Trifluoroacetate (1.0 mg/kg, iv) is administered 30 min prior to the acquisition trial of the novel object recognition (NOR) task to the subchronic ketamine or subchronic phencyclidine (PCP)-treated animals[1].
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.

[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.

Molecular Formula C20H32F3N5O8
Molecular Weight 527.49
Storage condition 2-8℃