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。

Linopirdine (DuP 996) is an orally active, selective M-type K current (IM; Kv7; KCNQ Channels) inhibitor with an IC 50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.

Solid

IC50: 2.4 μM (M-type K current)

Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 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 (IC50>300 μM).
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1).
has not independently confirmed the accuracy of these methods. They are for reference only.

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%.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 125 mg/mL (319.32 mM; Need ultrasonic)配制储备液