2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Neuronal Signaling
  3. iGluR Cytochrome P450 Cholinesterase (ChE)
  4. Orphenadrine

Orphenadrine  (Synonyms: (±)-Orphenadrine)

目录号: HY-157959
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摩尔计算器

Orphenadrine ((±)-Orphenadrine) 是一种骨骼肌松弛剂和 NMDA 拮抗剂，还具有抗帕金森病、抗组胺、抗震颤、抗痉挛和镇痛的作用。Orphenadrine 能够抑制剂 [3H]MK-801 与 NMDA 受体的苯环己哌啶 (PCP) 结合位点的结合。Orphenadrine 还是抗胆碱能剂和细胞色素 P450 (CYP) 2B 诱导剂。Orphenadrine 可能发挥促肿瘤作用，导致 CAR 核易位，导致微粒体活性氧 (ROS) 的产生和氧化应激。Orphenadrine 还发挥神经细胞保护作用，可保护大鼠小脑颗粒细胞 (CGC) 免受 3-NPA 诱导的死亡，对 NMDA 受体过度激活介导的神经退行性疾病有抑制潜力。

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Orphenadrine Chemical Structure

Orphenadrine Chemical Structure

CAS No. : 83-98-7

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规格 价格 是否有货
1 mg ￥225
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Orphenadrine 相关抗体

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查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation[1][2][3].

IC50 & Target

NMDA receptor[1]; CYP450 2B[2]; Cholinesterase (ChE)[3]
体外研究
(In Vitro)

Orphenadrine (30-300 μM) 表现出相对快速的浓度依赖性开放通道阻断动力学，Koff 为 0.013[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Orphenadrine 相关抗体:

Cell Viability Assay[1]

Cell Line: NMDA open-channel
Concentration: 30, 100 and 300 μM
Incubation Time: 5 seconds; with 200 μM NMDA
Result: Nearly completely inhibited [3H]MK-801 binding at 100 μM.
Exhibited relatively fast, concentration-dependent open channel blocking kinetics.
体内研究
(In Vivo)

在 Orphenadrine 的促肿瘤作用研究中，对雄性大鼠做单次腹腔注射 N-二乙基亚硝胺 (DEN) 的预处理 2 周。Orphenadrine (0, 750, 1500 ppm; po; 6 wk) 加速肝细胞增殖，诱导肝脏肿瘤促进活性[2].
Orphenadrine (30 mg/kg; po; 3 d) 可避免大鼠受 3-硝基丙酸 (3-NPA) (30 mg/kg; 3 d) 影响，而导致星形胶质细胞中神经元损伤标记物： [(3)H]-PK 11195 和 HSP27 的表达水平增加[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Liver tumor model in male rats pre-treated by N-diethylnitrosamine[2]
Dosage: 0, 750, 1500 ppm
Administration: PO; for 6 weeks
Result: Increased mRNA expression levels of Cyp2b1/2, Mrp2 and Cyclin D1.
Increased microsomal reactive oxygen species (ROS) production and oxidative stress markers such as thiobarbituric acid-reactive substances and 8-hydroxydeoxyguanosine.
分子量

269.38

Formula

C18H23NO
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

Orphenadrine 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Orphenadrine83-98-7(±)-OrphenadrineiGluRCytochrome P450Cholinesterase (ChE)Ionotropic glutamate receptorsCYPsInhibitorinhibitorinhibit

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