117928-94-6|Rapastinel|CsnPharm

CAS No.: 117928-94-6

Rapastinel/雷帕替奈 Catalog No. CSN17520

Synonyms: GLYX-13;BV-102;TPPT-amide

Rapastinel is a putative NMDAR functional glycine-site partial agonist.

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技术信息

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].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02267629	Obsessive-Compulsive Disorder ... more >>(OCD) Collapse <<	Phase 2	Completed	-	United States, New York ... more >> New York State Psychiatric Insitute New York, New York, United States, 10032 Collapse <<
NCT02267629	-	-	Completed	-	-
NCT03560518	Depressive Disorder, Major	Phase 3	Recruiting	February 29, 2020	-

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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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4186 mL
- 12.0928 mL
- 24.1856 mL
- 5 mM
- 0.4837 mL
- 2.4186 mL
- 4.8371 mL
- 10 mM
- 0.2419 mL
- 1.2093 mL
- 2.4186 mL

技术信息

CAS号

117928-94-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H31N5O6

运输

蓝冰

分子量

413.47

别名

GLYX-13;BV-102;TPPT-amide;雷帕替奈

溶解度

DMSO	83.0 mg/mL (200.7 mM)
Water	82.0 mg/mL (198.3 mM)
Ethanol	82.0 mg/mL (198.3 mM)

动物实验配方

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