Orphenadrine hydrochloride
Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
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- CAS No.: 341-69-5
- Formule: C18H24ClNO
- Masse moléculaire:305.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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NMDA Receptor 6 μM (Ki) |
In Vitro
Orphenadrine hydrochloride (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CGC cells (7-day-old Sprague Dawley rat)
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Concentration:6, 12, 24, 48 µM
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Incubation Time:24.5 h
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Result:Prevented cells from 3-NPA induced cellular aggregation,volume diminution and neurite fragmentation.
In Vivo
Orphenadrine hydrochloride (30 mg/kg; i.p.; once aday for 3 days) shows activity to against 3-NPA-induced neuronal damage in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague Dawley rats (275-300 g; 3-NPA toxicity model)[1].
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Dosage:10, 20, 30 mg/kg
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Administration:Intraperitoneal injection; once aday for 3 days (30 min before 3-NPA)
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Result:Reduced mortality of 3-NPA toxicity rats to 10-40% (3-NPA-treated animals showed general incoordination, drowsiness and general weakness).
Recovered 3-NPA-induced body weight loss, and when at 30 mg/kg reduced the level of PBR and expression of HSP27. (PBR and HSP27 are markers of neuronal damage).
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 341-69-5
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Masse moléculaire 305.84
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Formule C18H24ClNO
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SMILES
CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. 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]
[2]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Orphenadrine hydrochloride Related Classifications
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