Nisoldipine

L-type Cav1.2

388.41

Ethanol ：56 mg/mL (144.2 mM)
DMSO ：71 mg/mL (182.8 mM)

黄色结晶性粉末

Nisoldipine is a potent blocker of L-type calcium channels. Nisoldipine binds directly to inactive calcium channels stabilizing their inactive conformation Similar to other DHP CCBs. Nisoldipine displays selectivity for arterial smooth muscle cells due to great number of inactive channels and the α1 subunit of the channel. Nisoldipine is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels, which inhibits IKr (rapidly activating delayed-rectifier K+ current) with IC50 of 23 μM, and IKs (slowly activating delayed-rectifier K+ current)with IC50 of 40 μM in guinea-pig ventricular myocytes. Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen. This is tested by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC13-ADP).

Nisoldipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. This results in vasodilation and an overall decrease in blood pressure, based on which Nisoldipine is used to treat mild to moderate essential hypertension, chronic stable angina and Prinzmetal's variant angina. Nisoldipine shows some ability in patients with Timothy syndrome having Cav1.2 missense mutation G406R with IC50 of 267 nM, which is helpful to treat TS.

尼索地平

C₂₀H₂₄N₂O₆

63675-72-9