Rapastinel Trifluoroacetate 是一种NMDA受体调节剂，具有甘氨酸位点部分激动剂性质，有研究抑郁症的潜力。

Rapastinel Trifluoroacetate is an NMDA receptor modulator with glycine-site partial agonist properties.

Rapastinel Trifluoroacetate, a tetrapeptide (Thr-Pro-Pro-Thr-amide), has been reported to have fast acting antidepressant properties in man based upon its N-methyl-D-aspartate receptor (NMDAR) glycine site functional partial agonism.

C57BL/6J mice given a single dose or subchronic ketamine (30 mg/kg.i.p.) showed acute or persistent deficits in NOR, respectively.?Acute i.v. rapastinel (1.0 mg/kg), did not induce NOR deficit.?Pre-treatment with Rapastinel Trifluoroacetate?significantly prevented acute ketamine-induced NOR deficit.?Rapastinel Trifluoroacetate?(1.0 mg/kg, but not 0.3 mg/kg, iv) significantly reversed both subchronic ketamine- and subchronic PCP-induced NOR deficits.?Rapastinel Trifluoroacetate?also potentiated the atypical antipsychotic drug with antidepressant properties, lurasidone, to restore NOR in subchronic ketamine-treated mice.?Unlike ketamine,Rapastinel Trifluoroacetate?does not induce a declarative memory deficit in mice, and can prevent or reverse the ketamine-induced NOR deficit.?Further study is required to determine if these differences translate during clinical use of ketamine and rapastinel as fast acting antidepressant drugs and if rapastinel could have non-ionotropic effects as an add-on therapy with antipsychotic/antidepressant medications.

1435786-04-1

C20H32F3N5O8

527.498

Thr-Pro-Pro-Thr-NH2 Trifluoroacetate;GLYX-13 Trifluoroacetate

DMSO:125 mg/mL (236.97 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years