利诺吡啶
- CAS号:105431-72-9
- 英文名:1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
- 中文名:利诺吡啶
- CBNumber:CB6283722
- 分子式:C26H21N3O
- 分子量:391.46
- MOL File:105431-72-9.mol
- 熔点 :186-186.5 °C
- 沸点 :655.9±50.0 °C(Predicted)
- 密度 :1?+-.0.06 g/cm3(Predicted)
- 储存条件 :Desiccate at RT
- 溶解度 :DMSO: >10mg/mL
- 酸度系数(pKa) :6.01±0.10(Predicted)
- 形态 :A crystalline solid
- 颜色 :white to off-white
- WGK Germany :3
利诺吡啶性质、用途与生产工艺
- 生物活性 Linopirdine (DuP 996) 是一种具有口服活性的，选择性 M 型 K+ 电流 (IM；Kv7；KCNQ Channels) 抑制剂，IC50 为 2.4 μM。Linopirdine 是 TRPV1 激活剂。Linopirdine 是一种公认的认知增强药物，可增加大鼠脑组织中乙酰胆碱的释放。
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靶点
IC50: 2.4 μM (M-type K + current)
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体外研究
Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC 50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K + leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na + /K + inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC 50 >300 μM).
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1).
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体内研究
Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%.
Animal Model: Male Sprague-Dawley rats (300-350 g) Dosage: 0.1, 0.5, 1, 3, 6 mg/kg Administration: 5 intravenous bolus injections of increasing doses Result: Transiently and dose-dependently increases MAP by up to 15%.
- 公司名称：SIGMA
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- 国家：瑞士
- 产品数：6896
- 优势度：91
