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枸酸芬那君 /Orphenadrine citrate {[allProObj[0].p_purity_real_show]}

货号：A292028 同义名： 奥芬那君柠檬酸盐

Orphenadrine Citrate is both an uncompetitive NMDA receptor antagonist IC50 value of 16.2 µM and a mAChR antagonist with IC50 value of 0.37 µM.

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Orphenadrine citrate 化学结构 CAS号：4682-36-4
Orphenadrine citrate 化学结构
CAS号：4682-36-4
Orphenadrine citrate 3D分子结构
CAS号：4682-36-4
Orphenadrine citrate 化学结构 CAS号：4682-36-4
Orphenadrine citrate 3D分子结构 CAS号：4682-36-4
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Orphenadrine citrate 纯度/质量文件 产品仅供科研

货号：A292028 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 NMDA receptor ↓ 其他靶点 纯度
Empirical Formula ✔ 97%
Dizocilpine maleate +++

NMDA receptor, Kd: 37.2 nM

 		99%+
Felbamate +

NMDAR, IC50: 1.8 mM

 		98%
(-)-Dizocilpine maleate ++++

NMDA receptor, Ki: 30.5 nM

 		98%
Ifenprodil tartrate +++

NMDA Receptor, IC50: 0.3 μM

 		98%
Spermidine ✔ Autophagy 98% GC
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Orphenadrine citrate 生物活性

靶点

  • AChR
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].

Orphenadrine citrate 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 <<

Orphenadrine citrate 参考文献

[1]Pubill D, Canudas AM, et al. Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12.

[2]Kornhuber J, Parsons CG, et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46.

[3]Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46

[4]Pubill D, Canudas AM, Pallàs M, Sureda FX, Escubedo E, Camins A, Camarasa J. Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12

[5]Chen YW, Tzeng JI, Chen YC, Hung CH, Wang JJ. Intrathecal orphenadrine elicits spinal block in the rat. Eur J Pharmacol. 2014 Nov 5;742:125-30

[6]Czuczwar M, Cieszczyk J, Czuczwar K, Kiś J, Saran T, Turski WA. Influence of orphenadrine upon the protective activity of various antiepileptics in the maximal electroshock-induced convulsions in mice. Pharmacol Rep. 2009 Jul-Aug;61(4):732-6

[7]Hunskaar S, Berge OG, Hole K. Orphenadrine citrate increases and prolongs the antinociceptive effects of paracetamol in mice. Acta Pharmacol Toxicol (Copenh). 1986 Jul;59(1):53-9

Orphenadrine citrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.67mL

4.33mL

2.17mL

Orphenadrine citrate 技术信息

CAS号4682-36-4
分子式C24H31NO8
分子量 461.505
别名 奥芬那君柠檬酸盐
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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
动物实验配方

PO 0.5% CMC-Na 70 mg/mL suspension

Tags: Orphenadrine | 4682-36-4 | iGluR | Ionotropic glutamate receptors | NMDA Receptor Antagonist | Membrane Transporter/Ion Channel | Neuronal Signaling | iGluR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Orphenadrine citrate 纯度/质量文件 | Orphenadrine citrate 亚型比较 | Orphenadrine citrate 生物活性 | Orphenadrine citrate 临床数据 | Orphenadrine citrate 参考文献 | Orphenadrine citrate 实验方案 | Orphenadrine citrate 技术信息

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