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Barnidipine(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Barnidipine(hydrochloride)图片
CAS NO:104757-53-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议
100mg电议

产品介绍
Barnidipine (hydrochloride) (Mepirodipine hydrochloride) 是一种 L 型钙拮抗剂 (CaA),对 [3H] initrendipine 结合位点 (Ki\u003d0.21 nmol/l) 具有高亲和力,对 CaA 受体具有选择性作用。
Cas No.104757-53-1
别名盐酸巴尼地平,YM 09730-5
化学名(4S)-3,5-pyridinedicarboxylic acid, 3-methyl 5-[(3S)-1-(phenylmethyl)-3-pyrrolidinyl] ester, monohydrochloride
Canonical SMILESCC1=C(C(O[C@@H]2CN(CC3=CC=CC=C3)CC2)=O)[C@H](C(C(OC)=O)=C(C)N1)C4=CC([N+]([O-])=O)=CC=C4.Cl
分子式C27H29N3O6o HCl
分子量528.0
溶解度≥ 16.3mg/mL in DMSO with gentle warming
储存条件4°C, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Barnidipine is a calcium-channel blocker.

A calcium channel, an ion channel which displays selective permeability to calcium ions, is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels.

In vitro: The effects of barnidipine on L-type Ca(2+) current (I(Ca(L))) were investigated in rat ventricular cardiomyocytes. It was found that barnidipine reduced I(Ca(L)) in a concentration and voltage dependent manne. Barnidipine induced a leftward shift of the steady-state inactivation curve of I(Ca(L)) [1].

In vivo: A previous study was conducted to investigate the influence of barnidipine treatment on early stage hypertension by determining the mesenteric and renal arteries as well as the kidney in L-NAME-induced hypertensive rats. Barnidipine was applied to rats after 2 weeks of L-NAME administration, and continued for the next 3 weeks concomitantly with L-NAME. Histopathological studies verified structural alterations in the arteries and the kidney. Moreover, a decrease in endothelial nitric oxide synthase expression was observed both in the arteries and kidney of hypertensive rats with barnidipine treatment [2].

Clinical trial: In patients with hypertension and type 2 diabetes mellitus, it was found that barnidipine treatment led to a significant reduction in blood pressure. Data recorded with ABPM also showed a similar trend. Barnidipine + losartan could reduce the levels of Hs-CRP, TNF-α, sVCAM-1, sICAM-1, and isoprostanes [3].

References:
[1] Wegener JW, Meyrer H, Rupp J, Nawrath H. Barnidipine block of L-type Ca(2+) channel currents in rat ventricular cardiomyocytes. Br J Pharmacol. 2000 Aug;130(8):2015-23.
[2] Alp Yildirim FI, Eker Kizilay D, Ergin B, Balci Ekmeki, Topal G, Kucur M, Demirci Tansel C, Uyde Doan BS.  Barnidipine ameliorates the vascular and renal injury in L-NAME-induced hypertensive rats. Eur J Pharmacol. 2015 Oct 5;764:433-42.
[3] Derosa G, Mugellini A, Pesce RM, D'Angelo A, Maffioli P.  Barnidipine compared to lercanidipine in addition to losartan on endothelial damage and oxidative stress parameters in patients with hypertension and type 2 diabetes mellitus. BMC Cardiovasc Disord. 2016 Apr 12;16:66.