Nisoldipine

Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity^{[1][2][7][11]}. In Vitro:Nisoldipine noncompetitively reduces the activity of human Paraoxonase 1, with an IC₅₀ of 13.987 μM^[3].
Nisoldipine (10-100 μM, 8-10 min) is about 30 times less selective for delayed-rectifier K⁺ channels than for L-type Ca2⁺ channels in fully polarised guinea-pig ventricular myocytes^[4].
Nisoldipine also displays antioxidant potency with IC₅₀ of 28.2 μM both before and after the addition of active oxygen^[5].
Nisoldipine (1 μM, 90 s) largely prevents the elevation in [Ca2⁺]i caused by Lipopolysaccharide in Kupffer cells^[6].
Nisoldipine (20 μM, 3 h pretreatment) exerts antiviral effect by interfering with the internalization of influenza A virus into A549 cells^[7].
Nisoldipine (a cumulative manner from 1 to 10 and 100 nM at 5-min intervals) decreases elevated coronary perfusion pressure in NG-nitro-L-arginine (HY-12115)-perfused rat hearts^[8].
In Vivo:Nisoldipine (10 ppm, intragastric feeding, 4 weeks) prevents alcoholic hepatitis caused by chronic intragastric ethanol exposure in the rat, possibly by inhibition of endotoxin-mediated Kupffer cell activation^[1].
Nisoldipine (1000 ppm, diet, 12-14 weeks) prevents the development of hypertension and attenuates concomitant cardiac and aortic hypertrophy in spontaneously hypertensive rats^[9].
Nisoldipine (1000 ppm, diet, 22 weeks) attenuates hypertension and protects the heart, reducing the incidence of microscopic scarring, reactive interstitial and perivascular fibrosis in spontaneously hypertensive rats^[10].
Nisoldipine (20-40 mg/kg, intragastric gavage, daily, from day 2 to day 21) attenuates foot-shock-induced post-traumatic stress disorder and restores normal corticosterone levels in mice^[11].