Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) 是一种具有甘氨酸位点部分激动剂性质的 NMDA 受体调节剂。Rapastinel Trifluoroacetate 有潜力用于抑郁症的研究

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.

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NMDA receptor

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). 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].M

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 125 mg/mL (236.97 mM; Need ultrasonic)配制储备液