Orphenadrine citrate 是一种口服有效的非竞争性NMDA受体拮抗剂 (可透过血脑屏障)，其Ki值为6.0 μM。Orphenadrine citrate 能缓解因肌肉拉伤、扭伤或其他损伤引起的僵硬、疼痛和不适，也用于缓解帕金森病引起的颤抖。Orphenadrine citrate 具有较好的神经保护作用，可用于神经退行性疾病的研究。
| 生物活性 | Orphenadrine citrate is an orally active non-competitiveNMDA receptorantagonist (crosses the blood-brain barrier) with aKiof 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate 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[1][2]. |
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体外研究
(In Vitro) | Orphenadrine citrate (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells[1].
Cell Viability Assay[1] | 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. |
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体内研究
(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[1].
Orphenadrine citrate (30 mg/kg; i.p.; once aday for 3 days) shows activity to against 3-NPA-induced neuronal damage in vivo[1].
| Animal Model: | Adult male Sprague Dawley rats (275-300 g; 3-NPA toxicity model)[1]. | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(216.68 mM;Need ultrasonic) H2O : 10 mg/mL(21.67 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 36.67 mg/mL (79.46 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.42 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.42 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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