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Rapastinel

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Chemical Structure| 117928-94-6 同义名 : GLYX-13;BV-102;TPPT-amide
CAS号 : 117928-94-6
货号 : A119976
分子式 : C18H31N5O6
纯度 : 99%+
分子量 : 413.469
MDL号 : MFCD12912477
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(72.56 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 N-methyl-D-aspartate receptor (NMDAR) is an ionotropic glutamate receptor that is expressed throughout the central nervous system where it has been found to have a key role in regulating glutamatergic signaling that controls signaling and plasticity at excitatory synapses[3]. Rapastinel is an NMDAR modulator that has characteristics of a glycine site partial agonist. It is a robust cognitive enhancer and facilitates hippocampal long-term potentiation (LTP) of synaptic transmission in slices. Rapastinel produced an antidepressant like effect in the USVs (ultrasonic vocalization) 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 also produced 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]. Further, A single dose of rapastinel (3 mg/kg IV) facilitated learning and memory in multiple models 1 day to 1 week post-dosing. A single in vivo dose of rapastinel (3 mg/kg IV) in 2–3 month old male SD rats significantly enhanced the magnitude of long-term potentiation (LTP) of synaptic transmission compared to vehicle treated controls. In male 2–3 month old rats, rapastinel (3 mg/kg IV) significantly induced increases in mature spines in distal dendrites of the dentate gyrus and Layer 5 of the MPFC 24 hrs post-dosing[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.09mL

2.42mL

1.21mL

24.19mL

4.84mL

2.42mL
参考文献

[1]Zhang XL, Sullivan JA, et al. A NMDA receptor glycine site partial agonist, GLYX-13, simultaneously enhances LTP and reduces LTD at Schaffer collateral-CA1 synapses in hippocampus. Neuropharmacology. 2008 Dec;55(7):1238-50.

[2]Moskal JR, Kuo AG, et al. GLYX-13: a monoclonal antibody-derived peptide that acts as an N-methyl-D-aspartate receptor modulator. Neuropharmacology. 2005 Dec;49(7):1077-87.

[3]Rapid Antidepressant Effects: Moving Right Along

[4]The Long-Lasting Antidepressant Effects of Rapastinel (GLYX-13) Are Associated With a Metaplasticity Process in the Medial Prefrontal Cortex and Hippocampus