Benidipine HCl

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Chemical Structure| 91599-74-5 同义名 : 盐酸贝尼地平 ;KW-3049;Benidipine (hydrochloride);(±)-Benidipine;Benidipine hydrochloride
CAS号 : 91599-74-5
货号 : A214046
分子式 : C28H32ClN3O6
纯度 : 98%
分子量 : 542.02
MDL号 : MFCD06407650
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

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

DMSO: 35 mg/mL(64.57 mM)，配合低频超声助溶，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
描述 Benidipine hydrochloride, a calcium channel blocker (CCB), inhibited SFTSV (Severe fever with thrombocytopenia syndrome virus) replication in vitro. Benidipine hydrochloride was revealed to inhibit virus infection through impairing virus internalization and genome replication[3]. Histopathologically neuroprotective effects of benidipine hydrochloride was seen in the cerebral cortex tissues. Benidipine hydrochloride can play a certain protective role in the cerebral I/R injury. The protective effect of this agent may be related to the improvement on the antioxidant capacity of brain tissue and the inhibition of overproduction of inflammatory cytokines[4]. Moreover, patients with hypertension have high plasma TBARS (thiobarbituric acid reactive substance), and benidipine hydrochloride decreases not only blood pressure but also oxidative stress in the clinical practice[5]. Benidipine has a more potent antihypertensive effect than cilnidipine and also a renoprotective effect, indicating the high usefulness of benidipine in hypertensive patients with diabetes[6]. Combination therapy with benidipine hydrochloride and candesartan cilexetil may contribute to the suppression of arteriosclerosis and may be useful for elderly hypertensive patients with diabetes mellitus[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
NCT00135551 Cardiovascular Disease Phase 4 Completed - Japan ... 展开 >> Department of Medicine and Clinical Science, Yamaguchi University Graduate School of Medicine Ube, Yamaguchi, Japan, 755-8505 收起 <<
NCT02646397 Chronic Kidney Disease Phase 4 Unknown December 2017 China, Shanghai ... 展开 >> Department of Nephrology, Shanghai Changzheng Hospital Shanghai, Shanghai, China, 200003 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.22mL

1.84mL

0.92mL

18.45mL

3.69mL

1.84mL
参考文献

[1]Choi NY, Choi H, et al. Neuroprotective effects of amlodipine besylate and benidipine hydrochloride on oxidative stress-injured neural stem cells. Brain Res. 2014 Mar 10;1551:1-12.

[2]Higo K, Karasawa A, et al. Protective effects of benidipine hydrochloride(KW-3049), a calcium antagonist, against experimental arterial calcinosis and endothelial dysfunction in rats. J Pharmacobiodyn. 1992 Mar;15(3):113-20.

[3]Li H, Zhang LK, Li SF, et al. Calcium channel blockers reduce severe fever with thrombocytopenia syndrome virus (SFTSV) related fatality. Cell Res. 2019;29(9):739‐753

[4]Çakir T, Yücetaş ŞC, Yazici GN, Sunar M, Arslan YK, Süleyman H. Effects of Benidipine Hydrochloride on Ischemia/Reperfusion-Induced Inflammatory and Oxidative Brain İnjury in Rats [published online ahead of print, 2019 Sep 23]. Turk Neurosurg. 2019;10.5137/1019-5149.JTN.27372-19.3

[5]Suzuki O, Yoshida T, Tani S, et al. Antioxidative effects of benidipine hydrochloride in patients with hypertension independent of antihypertensive effects. Relationship between blood pressure and oxidative stress. Arzneimittelforschung. 2004;54(9):505‐512

[6]Seino H, Miyaguchi S, Yamazaki T, Ota S, Yabe R, Suzuki S. Effect of benidipine hydrochloride, a long-acting T-type calcium channel blocker, on blood pressure and renal function in hypertensive patients with diabetes mellitus. Analysis after switching from cilnidipine to benidipine. Arzneimittelforschung. 2007;57(8):526‐531

[7]Sasaki H, Kanai S, Oyama T, Miyashita Y, Yamamura S, Shirai K. Effect of combination therapy of benidipine hydrochloride and candesartan cilexetil on serum lipid metabolism and blood pressure in elderly hypertensive patients with type 2 diabetes mellitus. J Atheroscler Thromb. 2006;13(3):149‐157