Traxoprodil mesylate  (Synonyms: CP101,606 mesylate)

Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC₅₀ of 10 nM.

Traxoprodil 可有效阻断氟哌啶醇诱导的僵直症，ED₅₀ 小于 1 mg/kg。Traxoprodil 在 1 mg/kg 时可有效阻断 NMDA (ip) 刺激的小鼠 cfos 诱导^[1]。20 和 40 mg/kg 剂量的 Traxoprodil 在强迫游泳试验中表现出抗抑郁活性，并且与动物运动活动的变化无关^[2]。Traxoprodil (20 nM icv) 增加由 PTZ (70 mg/kg；ip) 诱导的全身强直阵挛发作的潜伏期。Traxoprodil (60 mg/kg，口服) 可延长阵挛性发作和全面性发作的潜伏期，并减少癫痫发作的总时间^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

423.52

C₂₁H₂₉NO₆S

188591-67-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chenard BL, 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.  [Content Brief]

  [2]. Poleszak E, et al. 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.  [Content Brief]

  [3]. Naspolini AP, et al. Traxoprodil decreases pentylenetetrazol-induced seizures. Epilepsy Res. 2012 Jun;100(1-2):12-9.  [Content Brief]