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

利诺吡啶化学性质

安全信息

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。
靶点

IC50: 2.4 μM (M-type K ⁺ current)
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).

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%.

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