利诺吡啶 (DUP996)

利诺吡啶 (DUP996)用途

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。

利诺吡啶 (DUP996)名称

[ CAS 号 ]:
105431-72-9

[ 中文名 ]:
利诺吡啶

[ 英文名 ]:
Linopirdine(DuP-996)

[中文别名 ]:

[英文别名 ]:

linopiridine
Dup 996
Linopirdine

利诺吡啶 (DUP996)生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> TRP频道

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

IC50: 2.4 μM (M-type K+ current)[1]

[体外研究]

Linopirdine(DuP 996)抑制IC50为16.3μM的IC(以中等过极化尾流测量,ImAHP)。Linopirdine(100μM)弱抑制K+漏电流、IL、瞬时外向电流、IA、延迟整流、IK和IAHP的慢成分,分别抑制28%、37%、36%和52%。混合Na+/K+内向整流电流IQ基本上不受Linopirdine的影响(IC50>300μM)[1]。利诺匹定作为TRPV1(瞬时受体电位香草醛1型)的激动剂[3]。

[体内研究]

利诺匹定(DuP 996；i.v.；0.1-6 mg/kg；增加剂量)瞬时(10-15分钟)和剂量依赖性地增加MAP高达15%[2]。动物模型：雄性Sprague-Dawley大鼠(300-350g)[2]剂量：0.1,0.5,1,3,6mg/kg给药：5次静脉推注递增剂量结果：MAP瞬时和剂量依赖性增加15%。

[参考文献]

[1]. Schnee ME, et al. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998 Aug;286(2):709-17.

[2]. Nassoiy SP, et al. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements afterhemorrhagic shock in rats. J Biomed Sci. 2017 Jan 17;24(1):8.

[3]. Neacsu C, et al. The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1. J Pharmacol Sci. 2010;114(3):332-40.

利诺吡啶 (DUP996)物理化学性质

[ 密度 ]:
1.255 g/cm3

[ 沸点 ]:
655.9ºC at 760 mmHg

[ 分子式 ]:
C₂₆H₂₁N₃O

[ 分子量 ]:
391.46400

[ 闪点 ]:
350.5ºC

[ 精确质量 ]:
391.16800

[ PSA ]:
46.09000

[ LogP ]:
4.94310

[ 蒸汽压 ]:
4.45E-17mmHg at 25°C

[ 折射率 ]:
1.669

[ 储存条件 ]:
2-8°C，密封，干燥

利诺吡啶 (DUP996)MSDS

详细MSDS(安全技术说明书)

利诺吡啶 (DUP996)安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933790090

利诺吡啶 (DUP996)合成路线

详细合成路线

利诺吡啶 (DUP996)上下游产品

利诺吡啶 (DUP996)上游产品

利诺吡啶 (DUP996)下游产品

利诺吡啶 (DUP996)海关

[ 海关编码 ]: 2933790090

[ 中文概述 ]:
2933790090 其他内酰胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:9.0% 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

利诺吡啶 (DUP996)文献

Ion channel expression in the developing enteric nervous system.

PLoS ONE 10(3) , e0123436, (2015)

The enteric nervous system arises from neural crest-derived cells (ENCCs) that migrate caudally along the embryonic gut. The expression of ion channels by ENCCs in embryonic mice was investigated usin...

Low expression of Kv7/M channels facilitates intrinsic and network bursting in the developing rat hippocampus.

J. Physiol. 586(Pt 22) , 5437-53, (2008)

Early in development, network activity in the hippocampus is characterized by recurrent synchronous bursts, whose cellular correlates are giant depolarizing potentials (GDPs). The propensity for gener...

Role of Kv7 channels in responses of the pulmonary circulation to hypoxia.

Am. J. Physiol. Lung Cell. Mol. Physiol. 308(1) , L48-57, (2015)

Hypoxic pulmonary vasoconstriction (HPV) is a beneficial mechanism that diverts blood from hypoxic alveoli to better ventilated areas of the lung, but breathing hypoxic air causes the pulmonary circul...

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