| Identification | Back Directory | [Name]
Traxoprodil mesylate | [CAS]
188591-67-5 | [Synonyms]
CP 101606 mesylate
Traxoprodil mesylate
CP-101606 mesylate >=98% (HPLC)
1-((1S,2S)-1-HYDROXY-1-(4-HYDROXYPHENYL)PROPAN-2-YL)-4-PHENYLPIPERIDIN-4-OL METHANESULFONATE | [Molecular Formula]
C21H29NO6S | [MDL Number]
MFCD12546332 | [MOL File]
188591-67-5.mol | [Molecular Weight]
423.52 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [color ]
white to beige | [InChIKey]
OZBWUANKVIMZIA-WRRDZZDISA-N | [SMILES]
OC1=CC=C([C@H](O)[C@H](C)N2CCC(O)(C3=CC=CC=C3)CC2)C=C1.CS(=O)(O)=O |
| Safety Data | Back Directory | [RIDADR ]
UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all | [WGK Germany ]
WGK 3 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral
Aquatic Acute 1
Eye Irrit. 2 |
| Hazard Information | Back Directory | [Uses]
Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM. | [Brand name]
Traxoprodil is INN. | [Biochem/physiol Actions]
CP-101606 mesylate (Traxoprodil mesylate) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. CP-101606 mesylate has been shown to be neuroprotective in animal models of brain injury and stroke. | [in vivo]
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]. | [References]
[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. DOI:10.1021/jm00016a017
[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. DOI:10.1007/s11011-016-9810-5
[3] Naspolini AP, et al. Traxoprodil decreases pentylenetetrazol-induced seizures. Epilepsy Res. 2012 Jun;100(1-2):12-9. DOI:10.1016/j.eplepsyres.2012.01.002 |
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Sigma-Aldrich
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021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Energy Chemical
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400-0056266 |
| Website: |
www.energy-chemical.com |
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