Traxoprodil
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货号：A294642
同义名：
CP101,606;CP 98,113
Traxoprodil a selective antagonist of the NR2B subunit of the NMDA receptor.
Traxoprodil 化学结构
Traxoprodil 3D分子结构
规格
价格
会员价
库存
数量
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Traxoprodil 质控信息
Empirical Formula
✔
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Dizocilpine maleate
+++
NMDA receptor, Kd: 37.2 nM
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Felbamate
+
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(-)-Dizocilpine maleate
++++
NMDA receptor, Ki: 30.5 nM
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Ifenprodil tartrate
+++
NMDA Receptor, IC50: 0.3 μM
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Spermidine
✔
Autophagy
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Evans Blue
✔
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IEM-1754
+
GluR3, IC50: 6 μM
GluR1, IC50: 6 μM
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Latrepirdine 2HCl
✔
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(-)-Huperzine A
+++
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CTEP
++++
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MPEP
++
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Riluzole
✔
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Traxoprodil 生物活性
描述
Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM. Traxoprodil is potent at blocking haloperidol-induced catalepsy and with an ED50 less than 1 mg/kg. Traxoprodil is effective at 1 mg/kg to block NMDA (ip) stimulated cfos induction in mice[3] [4] [5]
Traxoprodil 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
NCT00163085
Parkinson's Disease
Phase 2
Completed
-
United States, Oregon
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Pfizer Investigational Site
Portland, Oregon, United States, 97239 收起 <<
NCT00163059
Depressive Disorder, Major
Phase 2
Completed
-
United States, Kansas
... 展开 >>
Pfizer Investigational Site
Wichita, Kansas, United States, 67214-2878 收起 <<
Traxoprodil 参考文献
[1] Taylor TJ, Diringer K, et al. Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers. Clin Pharmacokinet. 2006;45(10):989-1001.
[2] Chenard BL, Bordner J, et al. (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. J Med Chem. 1995 Aug 4;38(16):3138-45.
[3] Chenard BL, Bordner J, Butler TW, Chambers LK, Collins MA, De Costa DL, Ducat MF, Dumont ML, Fox CB, Mena EE, et al. (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. J Med Chem. 1995 Aug 4;38(16):3138-45
[4] Poleszak E, Stasiuk W, Szopa A, Wyska E, Serefko A, Oniszczuk A, Wo ko S, wi der K, Wla P. Traxoprodil, a selective antagonist of the NR2B subunit of the NMDA receptor, potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice. Metab Brain Dis. 2016 Aug;31(4):803-14
[5] Naspolini AP, Cocco AR, Villa Martignoni F, Oliveira MS, Furian AF, Rambo LM, Rubin MA, Barron S, Mello CF. Traxoprodil decreases pentylenetetrazol-induced seizures. Epilepsy Res. 2012 Jun;100(1-2):12-9
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Traxoprodil 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.05mL
0.61mL
0.31mL
15.27mL
3.05mL
1.53mL
30.54mL
6.11mL
3.05mL
Traxoprodil 技术信息
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