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Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $33 | In Stock | |
5 mg | $103 | In Stock | |
10 mg | $173 | In Stock | |
25 mg | $322 | In Stock | |
50 mg | $442 | In Stock | |
100 mg | $592 | In Stock | |
200 mg | $783 | In Stock | |
1 mL x 10 mM (in DMSO) | $118 | In Stock |
Description | Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site. |
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. |
Animal Research | 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. |
Alias | Thr-Pro-Pro-Thr-NH2 Trifluoroacetate, GLYX-13 Trifluoroacetate |
Molecular Weight | 527.49 |
Formula | C20H32F3N5O8 |
Cas No. | 1435786-04-1 |
Smiles | OC(=O)C(F)(F)F.C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(N)=O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (236.97 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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