Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties.
説明 | Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. |
In vivo | 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. |
動物実験 | 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. |
別名 | Thr-Pro-Pro-Thr-NH2 Trifluoroacetate, GLYX-13 Trifluoroacetate |
分子量 | 527.49 |
分子式 | C20H32F3N5O8 |
CAS No. | 1435786-04-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (236.97 mM)
You can also refer to dose conversion for different animals. 詳細
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Rapastinel Trifluoroacetate 1435786-04-1 Membrane transporter/Ion channel Neuroscience NMDAR iGluR GLYX 13 inhibit GLYX13 GLYX-13 Inhibitor Rapastinel GLYX13 Trifluoroacetate Thr-Pro-Pro-Thr-NH2 Trifluoroacetate Ionotropic glutamate receptors GLYX-13 Trifluoroacetate GLYX 13 Trifluoroacetate inhibitor