"目录号: HY-14284
Membrane Transporter/Ion Channel-
Nilvadipine 是一种有效的钙离子通道 (calcium channel) 拮抗剂，IC50为 0.1 nM。
Calcium Channel
相关产品
Verapamil hydrochloride-Chlorpromazine hydrochloride-Neomycin sulfate-Nifedipine-Acetylcholine chloride-Diltiazem hydrochloride-Mibefradil dihydrochloride-Bay-K-8644 ((R)-(+)-)-Nimodipine-Cilnidipine-Dantrolene sodium hemiheptahydrate-Nicardipine Hydrochloride-Amlodipine besylate-Cromolyn sodium-Levetiracetam-
生物活性
Description
Nilvadipine is a potentcalcium channelantagonist, and theIC50value is around 0.1 nM.
IC50& Target
IC50: 0.1 nM (Calcium channel)[1]
In Vitro
In an in vitro experiment on inhibition of migration of rat aortic smooth muscle cells, using Zymosan-activated air pouch exudate as a chemoattractant in modified Boyden chambers.The IC50value is 0.033 nM for Nilvadipine (FR34235). Effects of Nilvadipine on proliferation of rat aortic smooth muscle cells and rabbit platelet aggregation is also examined. Nilvadipine should be useful for preventing and treating atherosclerosis. Inhibition of smooth muscle cell migration is thought to be its mechanism of antiatherogenic activity[2]. The antioxidant effect of calcium antagonist Nilvadipine is studied by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC13-ADP) with IC50of 25.1 μM. Nilvadipine shows antioxidant effects both before and after the addition of active oxygen, and reduces the dihydroxyfumarate (DHF) auto-oxidation rate, is chain-breaking and preventive antioxidants. Nicardipine, which shows an antioxidant effect only before exposure to active oxygen and reduced the DHF auto-oxidation rate, is mainly a preventive antioxidant[3].
In Vivo
The antiatherogenic activity of Nilvadipine (FR34235), a calcium antagonist, is examined in rabbits with carotid arteries sheathed with polyethylene cuffs, and compared with that of Nifedipine, Verapamil and Diltiazem. Nilvadipine is given intramuscularly in daily doses of 0.01-10 mg/kg for 3 weeks, starting on the day of cuff-placement. FR34235 dose-dependently inhibits the cuff-induced intimal thickening[2]. Nilvadipine affords significant protection against thinning of retinal layers in the RCS rat during retinal degeneration. Electron microscopy shows that marked irregularity in the photoreceptor OS in the untreated retina[4].
Clinical Trial
NCT02017340
Prof Brian Lawlor-University of Dublin, Trinity College-Molecular Medicine Ireland LBG-Alzheimer Europe-Archer Pharmaceuticals, Inc.-E-Search Limited-University College Dublin-King's College London-Istituto Di Ricerche Farmacologiche Mario Negri-University Hospital, Lille-University of Ulm-Szeged University-Goeteborgs Universitet-University College Cork-Aristotle University Of Thessaloniki-Stichting Katholieke Universiteit-St. James's Hospital, Ireland
Alzheimer's Disease
April 24, 2013
Phase 3
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References
[1].Nomoto A, et al. Smooth muscle cell migration induced by inflammatory cell products and its inhibition by a potent calcium antagonist, Nilvadipine. Atherosclerosis. 1988 Aug;72(2-3):213-9.
[2].Nomoto A, et al. Antiatherogenic activity of FR34235 (Nilvadipine), a new potent calcium antagonist. Effect on cuff-induced intimal thickening of rabbit carotid artery. Atherosclerosis. 1987 Apr;64(2-3):255-61.
[3].Sugawara H, et al. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8.
[4].Yamazaki H, et al. Preservation of retinal morphology and functions in royal college surgeons rat by Nilvadipine, a Ca(2+) antagonist. Invest Ophthalmol Vis Sci. 2002 Apr;43(4):919-26.