CX516

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Chemical Structure| 154235-83-3 同义名 : 安帕莱克斯 ;BDP 12; Ampalex.; Benzoyl-Piperidine-12; SPD 420; Ampakine CX 516
CAS号 : 154235-83-3
货号 : A240364
分子式 : C14H15N3O
纯度 : 99%
分子量 : 241.29
MDL号 : MFCD00943201
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Ampalex (Ampakine, CX516) is an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) [3]. This AMPAkine can be administered directly into the prefrontal cortex to provide analgesia, and that prefrontal AMPAkine infusion, similar to systemic administration, can provide added pain relief to complement morphine analgesia[4]. BDNF(brain-derived neurotrophic factor) expression is influenced by lower doses of, and shorter treatments with, the ampakine than is AMPAR expression[5].
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
NCT00858689 Fragile X Syndrome Not Applicable Completed - Canada, Ontario ... 展开 >> Surrey Place Centre Toronto, Ontario, Canada, M5S 2C2 收起 <<
NCT00858689 - Completed - -
NCT00235352 Schizophrenia Phase 2 Phase 3 Completed - United States, Massachusetts ... 展开 >> Freedom Trail Clinic Boston, Massachusetts, United States, 02114 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.14mL

0.83mL

0.41mL

20.72mL

4.14mL

2.07mL

41.44mL

8.29mL

4.14mL

参考文献

[1]Goff DC, Lamberti JS, et al. A placebo-controlled add-on trial of the Ampakine, CX516, for cognitive deficits in schizophrenia. Neuropsychopharmacology. 2008 Feb;33(3):465-72.

[2]Johnson SA, Simmon VF. Randomized, double-blind, placebo-controlled international clinical trial of the Ampakine CX516 in elderly participants with mild cognitive impairment: a progress report. J Mol Neurosci. 2002 Aug-Oct;19(1-2):197-200.

[3]Goff DC, Lamberti JS, Leon AC, Green MF, Miller AL, Patel J, Manschreck T, Freudenreich O, Johnson SA. A placebo-controlled add-on trial of the Ampakine, CX516, for cognitive deficits in schizophrenia. Neuropsychopharmacology. 2008 Feb;33(3):465-72. doi: 10.1038/sj.npp.1301444. Epub 2007 May 9. PMID: 17487227; PMCID: PMC3098468.

[4]Sun Y, Liu K, Martinez E, Dale J, Huang D, Wang J. AMPAkines and morphine provide complementary analgesia. Behav Brain Res. 2017 Sep 15;334:1-5. doi: 10.1016/j.bbr.2017.07.020. Epub 2017 Jul 19. PMID: 28734765; PMCID: PMC5621600.

[5]Lauterborn JC, Pineda E, Chen LY, Ramirez EA, Lynch G, Gall CM. Ampakines cause sustained increases in brain-derived neurotrophic factor signaling at excitatory synapses without changes in AMPA receptor subunit expression. Neuroscience. 2009 Mar 3;159(1):283-95. doi: 10.1016/j.neuroscience.2008.12.018. Epub 2008 Dec 24. PMID: 19141314; PMCID: PMC2746455.