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编 号:F328069
分子式:C18H24ClNO
分子量:305.84
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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.

体内研究:
Orphenadrine hydrochloride (10, 20, 30 mg/kg; i.p.; once aday for 3 days) reduces 3-NPA-induced mortality in a dose-dependent manner.Orphenadrine hydrochloride (30 mg/kg; i.p.; once aday for 3 days) shows activity to against 3-NPA-induced neuronal damage in vivo.Animal Model:Adult male Sprague Dawley rats (275-300 g; 3-NPA toxicity model).
Dosage:10, 20, 30 mg/kg
Administration:Intraperitoneal injection; once aday for 3 days (30 min before 3-NPA)
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).

体外研究:
Orphenadrine hydrochloride (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells.
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