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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
yellow
溶解性
DMSO: >10 mg/mL
创始人
Bayer
储存温度
room temp
SMILES字符串
COC(=O)C1=C(C)NC(C)=C(C1c2ccccc2[N+]([O-])=O)C(=O)OCC(C)C
InChI
1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3
InChI key
VKQFCGNPDRICFG-UHFFFAOYSA-N
基因信息
human ... CACNA1C(775) , CACNA1D(776) , CACNA1F(778) , CACNA1S(779)
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应用
Nisoldipine has been used:
- as a hit-antagonist to study its effects on oxytocin (OT)-induced myometrial Ca2+-mobilization and its potency to dampen uterine myometrial contractions
- as a calcium channel blocker to study its effects on cell viability in a human hepatic cancer HepG2 and rat renal epithelial NRK52E cell line
- as a component of the external IK1 recording solution to study the action potential in human pluripotent stem cell−derived cardiomyocytes (hiPS-CMs)
生化/生理作用
L-type (CaV1.2) calcium channel blocker; dihydropyridine-type calcium channel blocker with selectivity for smooth muscle (CaV1.2b) over cardiac muscle (CaV1.2a). Arterial vasodilator and antihypertensive agent.
特点和优势
This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
警示用语:
Warning
危险声明
危险分类
Acute Tox. 4 Oral
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
PloS one, 10(11), e0143243-e0143243 (2015-11-26)
The uterine myometrium (UT-myo) is a therapeutic target for preterm labor, labor induction, and postpartum hemorrhage. Stimulation of intracellular Ca2+-release in UT-myo cells by oxytocin is a final pathway controlling myometrial contractions. The goal of this study was to develop
European journal of pharmacology, 598(1-3), 94-97 (2008-09-18)
The non-selective muscarinic receptor antagonist propiverine impairs L-type Ca(2+) currents (I(Ca,L)) in human detrusor smooth muscle cells and atrial cardiomyocytes. Here, we have investigated the effects of three metabolites of propiverine on human cardiac I(Ca,L). Propiverine reduced I(Ca)(,L) with a
Yao xue xue bao = Acta pharmaceutica Sinica, 45(1), 49-54 (2011-03-01)
This study is to explore the activation of the Ca2+/CaM/CaN signal pathway in 5-HT-induced proliferation of rat pulmonary artery smooth muscle cells (PASMCs) and the inhibitory effect of m-nisoldipine (m-Nis) on this pathway. PASMCs were cultured with the explant technique.
International journal of pharmaceutics, 446(1-2), 136-144 (2013-02-21)
The aim of this study was to develop and characterize phospholipid bearing pellets for a poorly water-soluble drug, nisoldipine. Pellets were prepared using extrusion-spheronization technique containing microcrystalline cellulose, soy phosphatidylcholine (SPC), granulating fluid and lactose. Operational parameters such as extrusion
Nisoldipine exposures.
The American journal of emergency medicine, 26(3), 367-368 (2008-03-25)
商品
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