Orphenadrine
Based on 1 Customer Validation
Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation.
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- Reinheit: 99.71%
- CAS. Nr.: 83-98-7
- Formel: C18H23NO
- Molecular Weight:269.38
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Biologische Aktivität
NMDA receptor[1]; CYP450 2B[2]; Cholinesterase (ChE)[3]
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
12.6 μM
Compound: orphenadrine
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
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[PMID: 18788725] |
Orphenadrine (30-300 μM) exhibits relatively fast concentration-dependent open channel blocking kinetics with a Koff of 0.013[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NMDA open-channel
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Concentration:30, 100 and 300 μM
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Incubation Time:5 seconds; with 200 μM NMDA
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Result:Nearly completely inhibited [3H]MK-801 binding at 100 μM.
Exhibited relatively fast, concentration-dependent open channel blocking kinetics.
Orphenadrine (30 mg/kg; po; 3 d) Yes Protect rats from exposure to 3-nitropropionic acid (3-NPA) (30 mg/kg; 3 d), which causes neuronal damage in astrocytes. Markers: [(3)H]-PK 11195 and Increased expression levels of HSP27[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Liver tumor model in male rats pre-treated by N-diethylnitrosamine[2]
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Dosage:0, 750, 1500 ppm
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Administration:PO; for 6 weeks
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Result:Increased mRNA expression levels of Cyp2b1/2, Mrp2 and Cyclin D1.
Increased microsomal reactive oxygen species (ROS) production and oxidative stress markers such as thiobarbituric acid-reactive substances and 8-hydroxydeoxyguanosine.
Chemical Information
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CAS. Nr. 83-98-7
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Appearance Liquid
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Molecular Weight 269.38
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Formel C18H23NO
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Color Colorless to light yellow
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SMILES
CN(C)CCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2
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Synonyms
(±)-Orphenadrine
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (371.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Kornhuber J, 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. [Content Brief]
[2]. Morita R, et al. Liver tumor promoting effect of orphenadrine in rats and its possible mechanism of action including CAR activation and oxidative stress. J Toxicol Sci. 2013;38(3):403-13. [Content Brief]
[3]. Pubill D, et al. Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. Br J Pharmacol. 2001 Feb;132(3):693-702. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7122 mL | 18.5611 mL | 37.1223 mL | 92.8057 mL |
| 5 mM | 0.7424 mL | 3.7122 mL | 7.4245 mL | 18.5611 mL | |
| 10 mM | 0.3712 mL | 1.8561 mL | 3.7122 mL | 9.2806 mL | |
| 15 mM | 0.2475 mL | 1.2374 mL | 2.4748 mL | 6.1870 mL | |
| 20 mM | 0.1856 mL | 0.9281 mL | 1.8561 mL | 4.6403 mL | |
| 25 mM | 0.1485 mL | 0.7424 mL | 1.4849 mL | 3.7122 mL | |
| 30 mM | 0.1237 mL | 0.6187 mL | 1.2374 mL | 3.0935 mL | |
| 40 mM | 0.0928 mL | 0.4640 mL | 0.9281 mL | 2.3201 mL | |
| 50 mM | 0.0742 mL | 0.3712 mL | 0.7424 mL | 1.8561 mL | |
| 60 mM | 0.0619 mL | 0.3094 mL | 0.6187 mL | 1.5468 mL | |
| 80 mM | 0.0464 mL | 0.2320 mL | 0.4640 mL | 1.1601 mL | |
| 100 mM | 0.0371 mL | 0.1856 mL | 0.3712 mL | 0.9281 mL |
Orphenadrine Related Classifications
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