利诺吡啶
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- CAS号:
- 105431-72-9
- 英文名:
- 1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
- 英文别名:
- linopiridine;Linopirdine2HCl;LINOPIRDINE (DUP996);LINOPIRDINE DIHYDROCHLORIDE;1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one;1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one;1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one;2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-;1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride;1,3-Dihydro-1-Phenyl-3,3-Bis(4-Pyridinylmethyl)-2H-Indol-2-One(WXC03502)
- 中文名:
- 利诺吡啶
- 中文别名:
- 利诺吡啶;利诺哌啶;1,3-二氢-1-苯基-3,3-双(4-吡啶基甲基)-2H-吲哚-2-酮
- CBNumber:
- CB6283722
- 分子式:
- C26H21N3O
- 分子量:
- 391.46
- MOL File:
- 105431-72-9.mol
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利诺吡啶化学性质
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熔点:
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186-186.5 °C
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沸点:
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655.9±50.0 °C(Predicted)
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密度:
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1?+-.0.06 g/cm3(Predicted)
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储存条件:
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Desiccate at RT
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溶解度:
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DMSO: >10mg/mL
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酸度系数(pKa):
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6.01±0.10(Predicted)
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形态:
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A crystalline solid
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颜色:
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white to off-white
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利诺吡啶性质、用途与生产工艺
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。
IC50: 2.4 μM (M-type K
+
current)
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).
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%.
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Animal Model:
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Male Sprague-Dawley rats (300-350 g)
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Dosage:
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0.1, 0.5, 1, 3, 6 mg/kg
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Administration:
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5 intravenous bolus injections of increasing doses
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Result:
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Transiently and dose-dependently increases MAP by up to 15%.
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利诺吡啶
上下游产品信息
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利诺吡啶
生产厂家
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利诺吡啶国内生产厂家
105431-72-9, 利诺吡啶 相关搜索:
- Potassium channel
- Pharmaceuticals
- DuP 996
- 高端化学
- C26H21N3O2HCl
- 利诺哌啶
- 1,3-二氢-1-苯基-3,3-双(4-吡啶基甲基)-2H-吲哚-2-酮
- 利诺吡啶
- 105431-72-9
- Kv7,enhancing,inhibit,DuP-996,TRP Channel,Inhibitor,Transient receptor potential channels,KcsA,current,acetylcholine,Channels,Linopirdine,DuP996,orally,Potassium Channel,TRPV1,KCNQ,M-type,cognition
- 1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one
- 2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-
- 1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride
- 1,3-Dihydro-1-Phenyl-3,3-Bis(4-Pyridinylmethyl)-2H-Indol-2-One(WXC03502)
- linopiridine
- 1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one
- 1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one
- DuP 996, 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one
- Linopirdine2HCl
- LINOPIRDINE (DUP996)
- 1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
- LINOPIRDINE DIHYDROCHLORIDE