Journal of Applied Pharmacy
Open Access

Nisoldipine

Nisoldipine may be a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM. IC50 value: 10 nM Target: L-type Cav1.2 Nisoldipine may be a potent blocker of L-type calcium channels. Nisoldipine binds on to inactive calcium channels stabilizing their inactive conformation almost like other DHP CCBs. Nisoldipine displays selectivity for arterial smooth muscle cells thanks to great number of inactive channels and therefore the α1 subunit of the channel. Nisoldipine is about thirty times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels, which inhibits IKr (rapidly activating delayed-rectifier potassium current) with IC50 of 23 μM, &  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.

Nisoldipine is a pharmaceutical drug used for the treatment of chronic angina pectoris and hypertension. It is a calcium channel blocker of the dihydropyridine class. It is sold in the United States under the proprietary name Sular. Nisoldipine has tropism for cardiac blood vessels