Traxoprodil Mesylate

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Chemical Structure| 189894-57-3 同义名 : -
CAS号 : 189894-57-3
货号 : A698608
分子式 : C21H35NO9S
纯度 : 95%
分子量 : 477.57
MDL号 : MFCD22377951
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 Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM. Traxoprodil is effective at 1 mg/kg to block NMDA (ip) stimulated cfos induction in mice[1]. Traxoprodil (20nmol i.c.v.) increased the latency to generalized tonic-clonic seizures induced by PTZ (pentylenetetrazol) (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[2]. 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[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL

参考文献

[1]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

[2]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

[3]Poleszak E, Stasiuk W, Szopa A, Wyska E, Serefko A, Oniszczuk A, Wośko S, Świąder K, Wlaź 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