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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Orphenadrine Citrate (BS-5930; BS5930; BS 5930; Disipal), the citrate salt of Orphenadrine, is an uncompetitive NMDA receptor antagonist and a potent skeletal muscle relaxant with antispastic and analgesic activities. Orphenadrine has been used to treat drug-induced parkinsonism and to relieve pain from muscle spasm, also used as an antispastic and analgesic drug.
| ln Vitro |
Cerebellar granule cells exposed to 3-NPA-induced neurotoxicity exhibit neuroprotective effects when exposed to orphenadrine citrate (12 µM; 24.5 h)[1].
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| ln Vivo |
Orphenadrine citrate (10, 20, 30 mg/kg; ip; once daily for 3 days) decreases mortality caused by 3-NPA in a way that is dose-dependent[1]. In vivo, orphenadrine citrate (30 mg/kg; ip; once daily for three days) exhibits efficacy against 3-NPA-induced neuronal damage[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: CGC cells (7-day-old Sprague Dawley rat) Tested Concentrations: 6, 12, 24, 48 µM Incubation Duration: 24.5 h Experimental Results: Prevented cells from 3-NPA induced cellular aggregation, volume diminution and neurite fragmentation. |
| Animal Protocol |
Animal/Disease Models: Adult male Sprague Dawley rats (275-300 g; 3-NPA toxicity model)[1].
Doses: 10, 20, 30 mg/kg Route of Administration: intraperitoneal (ip)injection; one time/day for 3 days (30 min before 3-NPA). Experimental Results: decreased mortality of 3-NPA toxicity rats to 10-40% (3-NPA-treated animals demonstrated general incoordination, drowsiness and general weakness). Recovered 3-NPA-induced body weight loss, and when at 30 mg/kg decreased the level of PBR and expression of HSP27. (PBR and HSP27 are markers of neuronal damage). |
| References | |
| Additional Infomation |
Orphenadrine citrate is a citrate salt which comprises equimolar amounts of orphenadrine and citric acid. It has a role as a NMDA receptor antagonist, a H1-receptor antagonist, a parasympatholytic, a muscle relaxant and a muscarinic antagonist. It contains an orphenadrine.
Orphenadrine Citrate is the citrate salt form of orphenadrine with a muscle relaxant property. Although the mechanism of action has not been fully elucidated, orphenadrine citrate appears to block cholinergic receptors, thereby interfering with the transmission of nerve impulses from the spinal cord to the muscles. It does not produce myoneural block, nor does it affect crossed extensor reflexes. A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. See also: Orphenadrine (has active moiety); Aspirin; caffeine; orphenadrine citrate (component of). |
| Molecular Formula |
C18H23NO.C6H8O7
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| Molecular Weight |
461.5
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| Exact Mass |
461.205
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| CAS # |
4682-36-4
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| Related CAS # |
Orphenadrine-d3 citrate;Orphenadrine hydrochloride;341-69-5
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| PubChem CID |
83823
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| Appearance |
White to off-white solid powder
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| Density |
1.014 g/cm3
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| Boiling Point |
363ºC at 760 mmHg
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| Melting Point |
132-134ºC
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| Flash Point |
107.1ºC
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| LogP |
2.759
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
33
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UQZKYYIKWZOKKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H23NO.ClH/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16;/h4-12,18H,13-14H2,1-3H3;1H
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| Chemical Name |
N,N-dimethyl-2-(phenyl(o-tolyl)methoxy)ethan-1-amine hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 36.67 mg/mL (79.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1668 mL | 10.8342 mL | 21.6685 mL | |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3337 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04509336 | Terminated | Drug: Orphenadrine Drug: Baclofen |
Cirrhosis | Mansoura University | August 20, 2020 | Not Applicable |
| NCT02423395 | Recruiting | Drug: orphenadrine Drug: Placebo |
Liver Cirrhosis Muscle Cramps |
Sherief Abd-Elsalam | January 2015 | Phase 3 |
| NCT02665286 | Completed Has Results | Drug: Orphenadrine Drug: Methocarbamol Drug: Placebo |
Low Back Pain | Montefiore Medical Center | March 2016 | Phase 4 |
| NCT05322603 | Completed | Drug: Analgesics Non Opioid (Neodolpasse manufactured by Fresenius Kabi) Drug: Analgesics |
Analgesia | Petrovsky National Research Centre of Surgery |
March 18, 2022 | Not Applicable |
| NCT02449369 | Completed | Drug: Preop acetaminophen IV Drug: Preop orphenadrine IV Drug: Postop oral oxycodone & acetaminophen |
Unilateral Knee Arthroplasty | AdventHealth | April 2015 | Phase 4 |
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