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 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^[1]. Traxoprodil at a dose of 20 and 40 mg/kg exhibits antidepressant activity in the Forced swim test and it is not related to changes in animals’ locomotor activity^[2]. Traxoprodil (20 nM i.c.v.) increases the latency to generalized tonic-clonic seizures induced by PTZ (70 mg/kg; i.p.). Traxoprodil (60 mg/kg, p.o.) increases the latency to clonic and generalized seizures, and decreases the total time spent in seizures^[3].

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

423.52

C₂₁H₂₉NO₆S

188591-67-5

CS(=O)(O)=O.OC1(C2=CC=CC=C2)CCN(CC1)[C@@H](C)[C@H](C3=CC=C(C=C3)O)O

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]