Traxoprodil
(Synonyms: 曲索罗地) 目录号 : GC30839
An antagonist of NR2B subunit-containing NMDA receptors
Cas No.:134234-12-1
Sample solution is provided at 25 µL, 10mM.
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CP 101,606 is a noncompetitive antagonist of NMDA receptors containing the NR2B subunit (Kd = 4.2 nM).1 CP 101,606 is highly selective for NR1/NR2B-containing NMDA receptors over NR1, NR2A, and NR2B subunits alone and NR1/NR2A receptors in HEK293 cell homogenates. In vivo, CP 101,606 (30 mg/kg, s.c.) inhibits mechanical hyperalgesia following carrageenan challenge in rats.2 It also inhibits licking behavior in rats induced by capsaicin and phorbol-12-myristate-13-acetate . CP 101,606 reverses catalepsy in rats induced by haloperidol with an ED50 value of 0.4 mg/kg.3 CP 101,606 (1 mg/kg, s.c.) alone or in combination with L-DOPA methyl ester temporarily improves parkinsonian symptoms in an MPTP model of Parkinson's disease in rhesus monkeys.
1.Chazot, P.L., Lawrence, S., and Thompson, C.L.Studies on the subtype selectivity of CP-101,606: Evidence for two classes of NR2B-selective NMDA receptor antagonistsNeuropharmacology42(3)319-324(2002) 2.Taniguchi, K., Shinjo, K., Mizutani, M., et al.Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonistBr. J. Pharmacol.122(5)809-812(1997) 3.Steece-Collier, K., Chambers, L.K., Jaw-Tsai, S.S., et al.Antiparkinsonian actions of CP-101,606, an antagonist of NR2B subunit-containing N-methyl-d-aspartate receptorsExp. Neurol.163(1)239-243(2000)
Animal experiment: | Rats[3]The effect of traxoprodil and SPD on PTZ-induced seizures is investigated by injecting the Adult (90-100 days-old) male Wistar rats (250-300 g) with traxoprodil (0.2, 2 or 20 nM/site), SPD (0.02, 0.2 or 2 nM/site), or with vehicle (0.9% NaCl, 1 μL) 15 min before the administration of PTZ (35 or 70 mg/kg, i.p.)[3].Mice[2]The Forced swim test is done on male Albino Swiss mice (25-30 g). Traxoprodil (5, 10, 20, 40 mg/kg), imipramine and saline are administered i.p. 60 min before the test. The antidepressant activity is measured[2]. |
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. | |
| Cas No. | 134234-12-1 | SDF | |
| 别名 | 曲索罗地 | ||
| Canonical SMILES | OC1(C2=CC=CC=C2)CCN([C@@H](C)[C@@H](O)C3=CC=C(O)C=C3)CC1 | ||
| 分子式 | C20H25NO3 | 分子量 | 327.42 |
| 溶解度 | DMSO : ≥ 150 mg/mL (458.13 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0542 mL | 15.2709 mL | 30.5418 mL |
| 5 mM | 0.6108 mL | 3.0542 mL | 6.1084 mL |
| 10 mM | 0.3054 mL | 1.5271 mL | 3.0542 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet