Rapastinel Trifluoroacetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rapastinel Trifluacetate 是一种 NMDA 受体调节剂，具有甘氨酸位点部分激动剂特性。

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

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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].

GLYX-13 Trifluoroacetate | Thr-Pro-Pro-Thr-NH2 Trifluoroacetate

Membrane Transporter/Ion Channel

NMDAR

NMDA receptor

Neurological Disease

Bipolar depression; Major depressive disorder; Neuropathic pain

1435786-04-1

527.49

C20H32F3N5O8

>98% (HPLC)

DMSO:125 mg/mL (236.97 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years