产品说明书
Orphenadrine citrate
 |
同义名 : | 奥芬那君柠檬酸盐 |
| CAS号 : | 4682-36-4 | |
| 货号 : | A292028 | |
| 分子式 : | C24H31NO8 | |
| 纯度 : | 98% | |
| 分子量 : | 461.505 | |
| MDL号 : | MFCD00079197 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(227.52 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 10 mg/mL(21.67 mM)，配合低频超声助溶 |
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| 动物实验配方： |
PO 0.5% CMC-Na 70 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 +/- 1.6 microM (n = 6). Orphenadrine exhibited relatively fast, concentration-dependent open channel blocking kinetics (Kon 0.013 +/- 0.002 10(6) M-1S-1) whereas the offset rate was concentration-independent (Koff 0.230 +/- 0.004 S-1)[3]. In the low micromolar range, orphenadrine enhanced electrically-evoked and exogenous noradrenaline contractile responses in the epididymal portion of rat vas deferens. It also induced spontaneous activity that was inhibited by prazosin (1 microM) but not by atropine (20 nM). It inhibited accumulation of [3H]noradrenaline in rat vas deferens (IC50 = 14.2+/-2.3 microM). Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05+/-0.20 microM)[4]. Orphenadrine with a more sensory-selective action over motor block exhibited more potent and longer spinal anesthesia when compared to lidocaine[5]. Orphenadrine given at a dose of 5.65 mg/kg elevated the electrical seizure threshold from 5.7 (5.4-6.1) to 6.8 (6.3-7.3) mA, while a dose of 2.8 mg/kg was ineffective[6]. The combination of orphenadrine and paracetamol enhances the antinociceptive effect of either drug in mice[7]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01509781 | in Situ Breast Cancer ... 展开 >> Invasive Breast Cancer 收起 << | Phase 3 | Unknown | - | Hungary ... 展开 >> National Institute of Oncology Recruiting Budapest, Hungary, 1122 Contact: Zoltan Matrai, M.D. +3612248600 ext 3302 matraidoc@gmail.com 收起 << |
| NCT02456116 | Pain, Postoperative | Not Applicable | Unknown | September 2015 | Austria ... 展开 >> Vienna General Hospital Recruiting Vienna, Austria, 1090 Contact: Gerhard M Hobusch, Dr. +4314040040830 gerhard.hobusch@meduniwien.ac.at Contact: Bernd Kubista, Prof. Dr. +4314040040830 bernd.kubista@meduniwien.ac.at 收起 << |
| NCT02445599 | Pain Inadequa... 展开 >>te or Impaired Respiratory Function 收起 << | Phase 4 | Completed | - | Hungary ... 展开 >> UNIVERSITY OF DEBRECEN FACULTY OF MEDICINE Department of Anesthesiology and Intensive Care Debrecen, Hajdú-Bihar, Hungary, 4032 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.67mL 4.33mL 2.17mL |
| 参考文献 |
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