2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Neuronal Signaling
  3. iGluR Cytochrome P450 Cholinesterase (ChE)
  4. Orphenadrine

Orphenadrine  (Synonyms: (±)-Orphenadrine)

Cat. No.: HY-157959 Purity: 99.11%
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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 cytochrome P450 (CYP) 2B 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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Orphenadrine Chemical Structure

Orphenadrine Chemical Structure

CAS No. : 83-98-7

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Other Forms of Orphenadrine:

Orphenadrine Related Antibodies

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Description

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 cytochrome P450 (CYP) 2B 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[1][2][3].

IC50 & Target

NMDA receptor[1]; CYP450 2B[2]; Cholinesterase (ChE)[3]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
12.6 μM
Compound: orphenadrine
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
[PMID: 18788725]
In Vitro

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.

Orphenadrine Related Antibodies

Cell Viability Assay[1]

Cell Line: NMDA open-channel
Concentration: 30, 100 and 300 μM
Incubation Time: 5 seconds; with 200 μM NMDA
Result: Nearly completely inhibited [3H]MK-801 binding at 100 μM.
Exhibited relatively fast, concentration-dependent open channel blocking kinetics.
In Vivo

In a study of the tumor-promoting effects of Orphenadrine, male rats were pretreated with a single intraperitoneal injection of N-diethylnitrosamine (DEN) for 2 weeks. Orphenadrine (0, 750, 1500 ppm; po; 6 wk) accelerates hepatocyte proliferation and induces liver tumor-promoting activity[2].
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.

Animal Model: Liver tumor model in male rats pre-treated by N-diethylnitrosamine[2]
Dosage: 0, 750, 1500 ppm
Administration: PO; for 6 weeks
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.
Molecular Weight

269.38

Formula

C18H23NO
CAS No.
Appearance

<25°C Solid,>25°C Liquid

Color

Light yellow to brown

SMILES

CN(C)CCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7122 mL 18.5611 mL 37.1223 mL
5 mM 0.7424 mL 3.7122 mL 7.4245 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Orphenadrine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Orphenadrine83-98-7(±)-OrphenadrineiGluRCytochrome P450Cholinesterase (ChE)Ionotropic glutamate receptorsCYPsInhibitorinhibitorinhibit

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