Nilvadipine

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Chemical Structure| 75530-68-6 同义名 : FR34235; FK235; Nilvadipine, Escor, Nivadil, FR-34235, FK-235; SKF 102362; (±)-Nilvadipine; CL 287,389
CAS号 : 75530-68-6
货号 : A382623
分子式 : C19H19N3O6
纯度 : 98%
分子量 : 385.37
MDL号 : -
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(129.75 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel

    Calcium channel, IC50:0.03 nM
描述 Nilvadipine is a potent calcium channel antagonist, and the IC50 value is around 0.1 nM. Nilvadipine, acting as an inhibitor of spleen tyrosine kinase (SYK), is effective at reducing inflammation, tau hyperphosphorylation and amyloid production in AD mouse models[3]. Nilvadipine (FR34235) was also calcium antagonist with IC50 of 3.3 X 10(-11) M. FR34235 should be useful for preventing and treating atherosclerosis[4]. Nicardipine, which showed an antioxidant effect only before exposure to active oxygen and reduced the DHF (dihydroxyfumarate) auto-oxidation rate, was mainly a preventive antioxidant[5]. Nilvadipine (3.2 mg/kg, i.p.) significantly prevented the impairment of spatial memory and neuronal apoptosis in this model[6]. Treatment with Nilvadipine mitigated the TBI-induced inflammatory response in aged r-mTBI (Mild traumatic brain injury) animals and significantly improved spatial memory[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02017340 Alzheimer's Disease Phase 3 Completed - France ... 展开 >> Centre Hospitalier Universitaire d'Amiens (CHU Amiens) Amiens, France Centre Hospitalier Universitaire de Bethune (CH Bethune) Bethune, France Centre Hospitalier Universitaire de Caen (CHU Caen) Caen, France Centre Hospitalier Universitaire de Calais (CHU Calais) Calais, France Centre Hospitalier Universitaire de Lens (CHU Lens) Lens, France Centre Hospitalier Regional et Universitaire de Lille (CHRU Lille) Lille, France Centre Hospitalier Universitaire de Saint Philibert (GHICL) Lille, France Germany University of Ulm Ulm, Germany Greece "G. Papanicolaou" Hospital Athens, Greece "G.Papageorgiou" Hospital Athens, Greece AXEPA Hospital Athens, Greece Hungary Szeged University Szeged, Hungary Ireland University College Cork Cork, Ireland St James Hospital Dublin, Ireland Italy Hospital of Brescia Brescia, Italy Hospital Castellanza Castellanza, Italy Hospital of Genoa Genoa, Italy Hospital of Milan Milan, Italy Netherlands Hospital of Arnhem Arnhem, Netherlands Hospital of Maastricht Maastricht, Netherlands Hospital of Nijmegen Nijmegen, Netherlands Sweden Gothenburg Univeristy Gothenburg, Sweden United Kingdom Kings College London London, United Kingdom 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.97mL

2.59mL

1.30mL

25.95mL

5.19mL

2.59mL
参考文献

[1]Ozawa Y, Hayashi K, et al. Renal afferent and efferent arteriolar dilation by nilvadipine: studies in the isolated perfused hydronephrotic kidney. J Cardiovasc Pharmacol. 1999 Feb;33(2):243-7.

[2]Nomoto A, Mutoh S, 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.

[3]Morin A, Mouzon B, Ferguson S, Paris D, Browning M, Stewart W, Mullan M, Crawford F. Nilvadipine suppresses inflammation via inhibition of P-SYK and restores spatial memory deficits in a mouse model of repetitive mild TBI. Acta Neuropathol Commun. 2020 Oct 19;8(1):166

[4]Nomoto A, Hirosumi J, Sekiguchi C, Mutoh S, Yamaguchi I, Aoki H. 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

[5]Sugawara H, Tobise K, Kikuchi K. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8

[6]Iwasaki K, Egashira N, Takagaki Y, Yoshimitsu Y, Hatip-Al-Khatib I, Mishima K, Fujiwara M. Nilvadipine prevents the impairment of spatial memory induced by cerebral ischemia combined with beta-amyloid in rats. Biol Pharm Bull. 2007 Apr;30(4):698-701

[7]Morin A, Mouzon B, Ferguson S, Paris D, Saltiel N, Lungmus C, Mullan M, Crawford F. Treatment With Nilvadipine Mitigates Inflammatory Pathology and Improves Spatial Memory in Aged hTau Mice After Repetitive Mild TBI. Front Aging Neurosci. 2018 Oct 11;10:292