Nilvadipine Calcium Channel 억제제

Nilvadipine strongly inhibits the chemotaxis of interleukin-1 (IL-1), leukotriene B4 (LTB4), platelet-derived growth factor (PDGF) with IC50 of 0.1 nM in rat aortic smooth muscle cells (SMC). [1] This compound is reported to increase renal blood flow and reduce filtration fraction in the isolated perfused hydronephrotic kidney, suggesting indirectly afferent and efferent arteriolar vasodilation. [2]

Nilvadipine preserves retinal morphology and electroretinogram responses in RCS rats during the initial stage of retinal degeneration. This compound significantly enhances rhodopsin kinase and alphaA-crystallin expression and suppression of caspase 1 and 2 expression in the retina of RCS rats. [3] It completely inhibits the vasoactivity elicited by Abeta in rat aortae and in human middle cerebral arteries. This chemical restores cortical perfusion levels in Tg APPsw to values similar to those observed in control littermates without notably affecting the CBF of control mice. [4] It suppresses ischemia (20 min)-reflow (20 min)-induced paw edema of mice (ED30:0.4 mg/kg i.v. and 2 mg/kg p.o.). This compound suppresses carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen. Nifedipine, nicardipine and nimodipine results in a suppression of 30% only with 100 mg/kg oral dosing in rats. It inhibits superoxide radical (O-2production from xanthine oxidase (XOD) both with lactate dehydrogenase + NADH method and cytochrome c method (IC50:90 and 100 mg/mL, respectively). [5]