Orphenadrine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

奥芬那君是一种乙醇胺抗组胺类抗胆碱能化合物，具有显着的中枢神经系统 (CNS) 和外周作用，用于治疗疼痛性肌肉痉挛和其他类似病症，以及帕金森病的某些方面的治疗。

Orphenadrine is an anticholinergic drug of the ethanolamine antihistamine class with prominent central nervous system (CNS) and peripheral actions used to treat painful muscle spasms and other similar conditions, as well as the treatment of some aspects of Parkinson's disease. It is closely related to diphenhydramine. Therefore, it is related to other drugs used for Parkinson's, such as benztropine and trihexyphenidyl, and it is also structurally related to nefopam, which is a centrally acting yet nonopioid analgesic. The combination of anticholinergic effects and CNS penetration make orphenadrine useful for pain of all etiologies, including from: radiculopathy, muscles, and headaches.(In Vitro):Orphenadrine citrate (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells.(In Vivo):Orphenadrine citrate (10, 20, 30 mg/kg; i.p.; once aday for 3 days) reduces 3-NPA-induced mortality in a dose-dependent manner.Orphenadrine citrate (30 mg/kg; i.p.; once aday for 3 days) shows activity to against 3-NPA-induced neuronal damage in vivo.

Orphenadrine hydrochloride (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells.Cell Viability Assay Cell Line:CGC cells (7-day-old Sprague Dawley rat)Concentration:6, 12, 24, 48 μM Incubation Time:24.5 h Result:Prevented cells from 3-NPA induced cellular aggregation,volume diminution and neurite fragmentation.

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).

——

GPCR/G Protein

Histamine Receptor

H1 receptor| NMDA receptor| Noradrenaline transporter (Sodium-dependent)| Sodium Channel

Neurological Disease

——

341-69-5

305.85

C18H23NO·HCl

>98% (HPLC)

DMSO: 10 mM

Cl.CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C

——

(-20℃)

With Ice Pack

≥ 2 years