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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.
| Targets |
N-methyl-D-aspartate (NMDA) receptors, Ki = 1.8 μM (uncompetitive antagonism) [2]
- Muscarinic acetylcholine receptors (minor affinity, unspecified subtypes) [1] |
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| 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].
In primary cortical neurons, Orphenadrine Citrate (10 μM, 30 μM) prevented 3-nitropropionic acid (3-NP)-induced neurotoxicity: cell viability increased by 35% (10 μM) and 58% (30 μM) compared to 3-NP-treated controls, and lactate dehydrogenase (LDH) release (toxicity marker) was reduced by 28% (10 μM) and 42% (30 μM) [1] - In NMDA receptor binding assays, Orphenadrine Citrate (0.1 μM-10 μM) exhibited uncompetitive antagonism, inhibiting [3H]MK-801 binding to NMDA receptors with a Ki value of 1.8 μM [2] - Patch-clamp studies on cultured neurons showed that Orphenadrine Citrate (5 μM, 10 μM) concentration-dependently inhibited NMDA-induced inward currents, reducing peak current amplitude by 40% (5 μM) and 65% (10 μM) without affecting AMPA or GABA receptor currents [2] |
| 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].
In mice treated with 3-NP (20 mg/kg, intraperitoneal injection, once daily for 7 days) to induce neurotoxicity, oral administration of Orphenadrine Citrate (25 mg/kg, 50 mg/kg, once daily for 7 days) alleviated neurological deficits: locomotor activity increased by 32% (25 mg/kg) and 55% (50 mg/kg), and striatal lesions (assessed by histology) were reduced by 45% (50 mg/kg) compared to 3-NP-only group [1] - Orphenadrine Citrate (50 mg/kg) reversed 3-NP-induced reduction in striatal ATP levels (increased by 60%) and glutathione (GSH) content (increased by 52%), and decreased malondialdehyde (MDA) levels (reduced by 38%) in mouse brain tissue [1] |
| Enzyme Assay |
NMDA receptor binding assay: Membrane fractions prepared from rat brain (enriched in NMDA receptors) were incubated with serial concentrations of Orphenadrine Citrate (0.01 μM-100 μM) in the presence of [3H]MK-801 (a selective NMDA receptor ligand). Incubation was carried out at 25°C for 90 minutes, and unbound ligands were removed by filtration through glass fiber filters. Bound radioactivity was measured using a liquid scintillation counter, and Ki value was calculated via nonlinear regression analysis of displacement curves [2]
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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. Primary cortical neuron neurotoxicity assay: Cortical neurons were isolated from embryonic rats and cultured for 7-10 days. Cells were pretreated with Orphenadrine Citrate (10 μM, 30 μM) for 1 hour, then exposed to 3-NP (10 mM) for 24 hours. Cell viability was assessed by MTT assay, and LDH release was measured via spectrophotometry to evaluate cytotoxicity. Parallel cultures were used for morphological observation of neuronal integrity [1] - NMDA receptor current recording assay: Cultured neurons were placed in a recording chamber, and whole-cell patch-clamp recordings were performed. Orphenadrine Citrate (5 μM, 10 μM) was added to the extracellular solution, and NMDA-induced currents (activated by 100 μM NMDA + 10 μM glycine) were recorded before and after drug application. Current amplitude and kinetics were analyzed to determine the inhibitory effect [2] |
| 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). 3-NP-induced neurotoxicity mouse model: Male mice were randomly divided into control, 3-NP-treated, and Orphenadrine Citrate-treated groups. 3-NP was administered via intraperitoneal injection at 20 mg/kg once daily for 7 days to induce neurotoxicity. Orphenadrine Citrate was dissolved in normal saline and administered via oral gavage at 25 mg/kg and 50 mg/kg once daily, 1 hour before 3-NP injection, for 7 days. Control mice received normal saline via both routes. Locomotor activity was measured using an open-field test, and mice were sacrificed on day 8 to collect brain tissues for ATP, GSH, MDA detection and histological analysis [1] |
| Toxicity/Toxicokinetics |
At concentrations ≤30 μM, no significant in vitro cytotoxicity to primary cortical neurons was observed [1]
-The plasma protein binding rate of ocphenadrine citrate was approximately 90% [2] |
| References | |
| Additional Infomation |
Orphenadrine citrate is a citrate salt composed of equimolar amounts of oysterone and citric acid. It possesses a variety of pharmacological effects, including NMDA receptor antagonist, H1 receptor antagonist, parasympathetic nerve blocker, muscle relaxant, and muscarinic receptor antagonist. It contains oysterone. Ophenadrine citrate is the citrate form of oysterone and has muscle relaxant effects. Although its mechanism of action is not fully elucidated, oysterone 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 neuromuscular blockade or affect the crossed extensor reflex. It is a muscarinic receptor antagonist used to treat drug-induced Parkinson's disease and relieve pain caused by muscle spasms. See also: Ophenadrine (containing active ingredient). Aspirin; Caffeine; Ophenadrine citrate (ingredient).
Olfenadrine citrate is a centrally acting drug with dual characteristics: a non-competitive NMDA receptor antagonist and a weakly muscarinic acetylcholine receptor antagonist[1][2] - Its neuroprotective effect is achieved by inhibiting excessive activation of NMDA receptors, reducing oxidative stress, and maintaining mitochondrial function (maintaining ATP and GSH levels)[1] - Clinically, it is used to treat muscle spasms, Parkinson's disease-related stiffness, and neuropathic pain[1][2] - It does not cross-react with AMPA or GABA receptors and is selective for NMDA receptors at therapeutic concentrations[2] |
| 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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