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Traxoprodil

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Chemical Structure| 134234-12-1 同义名 : CP101,606;CP 98,113;(+)-CP 101,606
CAS号 : 134234-12-1
货号 : A294642
分子式 : C20H25NO3
纯度 : 99%+
分子量 : 327.417
MDL号 : MFCD00926469
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(183.25 mM)，配合低频超声助溶，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 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]. Traxoprodil at a dose of 20 and 40 mg/kg exhibited antidepressant activity in the FST (forced swim test) and it was not related to changes in animals' locomotor activity[4]. Traxoprodil (20nmol i.c.v.) increased the latency to generalized tonic-clonic seizures induced by PTZ (70mg/kg; i.p.). Traxoprodil (60mg/kg, p.o.) increased the latency to clonic and generalized seizures, and decreased the total time spent in seizures[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
NCT00163085 Parkinson's Disease Phase 2 Completed - United States, Oregon ... 展开 >> 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 <<
实验方案
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
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