预约演示
更新于：2025-09-04
Nitrendipine
尼群地平
更新于：2025-09-04
概要
基本信息
原研机构- |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (1987-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C18H20N2O6 |
InChIKeyPVHUJELLJLJGLN-UHFFFAOYSA-N |
CAS号39562-70-4 |
关联
7
项与 尼群地平 相关的临床试验NCT04931108
The Effect of Nitrendipine/Atenolol Combination on Blood Pressure Variability of Patients With Grade 1 Hypertension Compared With Nitrendipine or Atenolol Monotherapy.
CTR20210720
尼群地平片（10 mg）人体生物等效性研究
NCT02217852
A Randomized, Open-label, Positive Drug Controlled Clinical Trials to Compare the Efficacy of Nitrendipine and Hydrochlorothiazide , Captopril Plus Hydrochlorothiazide and Beijing Hypotensive No.0 in Tibetan Hypertension
100 项与 尼群地平 相关的临床结果
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100 项与 尼群地平 相关的转化医学
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100 项与 尼群地平 相关的专利（医药）
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3,470
项与 尼群地平 相关的文献（医药）2025-07-01ANALYTICA CHIMICA ACTA
Multi-interaction (substituted-phenylcarbamate)-hydroxypropyl-β-cyclodextrin chiral stationary phases for liquid chromatography
Article
作者: Zhu, Junchao ; Xu, Wentao ; Xu, Linna ; Cheng, Dongping ; Tong, Shengqiang ; Chen, Songlin ; Ni, Huizhen ; Chu, Chu
BACKGROUND:
(Substituted-phenylcarbamate)-β-cyclodextrin (β-CD) chiral stationary phases (CSPs) showed high enantioselectivity and complementary capabilities compared to polysaccharide-based CSPs in liquid chromatography. Most of the previous works were about preparation and application of (substituted-phenylcarbamate)-β-CD, while very limited works was available reporting modified hydroxypropyl-β-CD (HP-β-CD) used for CSP. As matter of fact, HP-β-CD was more frequently used than native β-CD as chiral selector in many chiral separation techniques. Therefore, it was great of significance to investigate preparation of multi-interaction (substituted-phenylcarbamate)-HP-β-CD CSPs and its application in chiral separation.
RESULTS:
Three new multi-interaction (substituted-phenylcarbamate)-HP-β-CD CSPs were prepared and investigated, including (3-chloro-4-methylphenylcarbamate)-HP-β-CD CSP, (4-chloro-3-methylphenylcarbamate)-HP-β-CD CSP and (5-chloro-2-methylphenylcarbamate)-HP-β-CD CSP. The structure and morphology of the three chiral selectors as well as their stationary phase were characterized by 1H NMR spectra, elemental analysis, infrared spectroscopy, scanning electron microscopy and thermogravimetric analysis. Degree of substitution, stability, repeatability and reproducibility of the (substituted-phenylcarbamate)-HP-β-CD CSPs were investigated. A total of 56 racemic compounds were examined on the three (substituted-phenylcarbamate)-HP-β-CD CSPs using reversed-phase elution mode. It was found that enantioselective recognition capability of the three (substituted-phenylcarbamate)-HP-β-CD CSPs was greatly improved compared with that of traditional HP-β-CD CSPs, which was demonstrated by the number of successful enantioseparated racemates and increased enantioseparation efficiency. Applications of the three CSPs in high performance liquid chromatographic enantioseparations indicated that each of them showed different enantiorecognition ability toward different type of racemic structures, which showed high complementary enantiorecognition ability with traditional β-CD-based CSPs.
SIGNIFICANCE:
An efficient one-pot reaction strategy for synthesis of (substituted-phenylcarbamate)-HP-β-CD CSPs was developed. It was found that enantiorecognition and peak resolutions (Rs) were greatly improved compared with traditional HP-β-CD CSP and β-CD CSP. The improved chiral separation performance of multi-interaction HP-β-CD CSPs was demonstrated, providing valuable insights for the development of efficient chiral separation methods while expanding the potential applications of HP-β-CD in chiral liquid chromatography.
2025-06-01Journal of molecular and cellular cardiology plus
Matured hiPSC-derived cardiomyocytes possess dematuration plasticity
Article
作者: Meng, Fang ; Zebrowski, David C ; Andersson, Henrik ; Hidalgo-Gonzalez, Alejandro ; Später, Daniela ; Bjerre, Frederik Adam ; Wei, Ruofan ; Walentinsson, Anna ; Andersen, Ditte C ; Wang, Qing-Dong ; Poon, Ellen Ngar-Yun ; Kwok, Maxwell ; Hui, Yen Chin
Human induced Pluripotent Stem Cell-derived cardiomyocytes (hiPSC-CMs) are increasingly used to identify potential factors capable of inducing endogenous cardiomyocyte proliferation to regenerate the injured heart. L-type calcium channel blockers have previously been identified as a class of factors capable of inducing matured hiPSC-CMs to proliferate. However, the mechanism by which L-type calcium channel blockers promote hiPSC-CM proliferation remains unclear. Here we provide evidence that matured hiPSC-CMs possess plasticity to undergo dematuration in response to certain pharmacological compounds. Consistent with primary cardiomyocyte maturation during perinatal development, we found that centrosome disassembly occurs in hiPSC-CMs during plate-based, temporal, maturation. A small molecule screen identified nitrendipine, an L-type calcium channel blocker, and 1-NA-PP1, a Src kinase inhibitor, as factors capable of inducing centrosome reassembly in a subpopulation of hiPSC-CMs. Furthermore, centrosome-positive hiPSC-CMs were more likely to exhibit cell cycle activity than centrosome-negative hiPSC-CMs. In contrast, neither nitrendipine or 1-NA-PP1 induced centrosome reassembly, or cell cycle activity, in neonatal rat ventricular myocytes (NRVMs). Differential bulk transcriptome analysis indicated that matured hiPSC-CMs, but not NRVMs, treated with nitrendipine or 1-NA-PP1 undergo dematuration. ScRNA transcriptome analysis supported that matured hiPSC-CMs treated with either nitrendipine or 1-NA-PP1 undergo dematuration. Collectively, our results indicate that matured hiPSC-CMs, but not primary NRVMs, possess plasticity to undergo dematuration in response to certain pharmacological compounds such as L-type calcium channel blockers and Src-kinase inhibitors. This study shows that once mature, hiPSC-CMs may not maintain their maturity under experimental conditions which may have implications for experimental systems where the state of hiPSC-CM maturation is relevant.
2025-06-01BIOCHEMICAL PHARMACOLOGY
Inhibitory effects of nimodipine, nitrendipine and felodipine on tamoxifen metabolism and molecular docking
Article
作者: Xia, Hailun ; Shen, Yuxin ; Jiang, Zheli ; Chen, Xiaohai ; Shi, Lu ; Xu, Ren-Ai ; Hong, Fengsheng
Tamoxifen, a selective estrogen receptor modulator (SERM) used in breast cancer therapy, requires metabolic activation by CYP3A4 to exert its biological effects. This study evaluated the effects of calcium channel blockers nimodipine, nitrendipine and felodipine on tamoxifen metabolism by studying their interactions with tamoxifen in vitro and in vivo. Rat liver microsomes (RLM) and human liver microsomes (HLM) were used in this study to evaluate the inhibitory potential of nimodipine, nitrendipine and felodipine on tamoxifen metabolism in vitro. A total of 28 cardiovascular drugs, including calcium channel blockers, were screened in an RLM incubation system in vitro. In RLM, nimodipine, nitrendipine and felodipine had half-maximum inhibitory concentration (IC50) values of 5.55 µM, 11.86 µM and 7.71 µM, respectively. In HLM, the IC50 values were increased to 20.38 µM, 30.06 µM, and 44.45 µM for nimodipine, nitrendipine and felodipine, respectively. The kinetic assays indicated that nimodipine and felodipine inhibited the metabolism of tamoxifen in a competitive way, whereas nitrendipine showed non-competitive inhibition in RLM. However, felodipine exhibited non-competitive inhibition, and nimodipine and nitrendipine showed competitive inhibition in HLM. Pharmacokinetic studies in rats revealed that pretreatment with nimodipine and nitrendipine significantly increased the systemic exposure of tamoxifen, as demonstrated by increasing the area under the curve (AUC), the maximum concentration (Cmax) and decreasing the clearance (CLz/F). Finally, molecular docking studies supported these findings, showing potential interactions at the active site of CYP3A4. These results suggested the necessity for careful monitoring and possible dose adjustments of tamoxifen when co-administered with calcium channel blockers in clinic.
100 项与 尼群地平 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肾性高血压 | 日本 | 1998-03-12 | |
| 心绞痛 | 日本 | 1990-01-23 | |
| 高血压 | 中国 | 1987-01-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 1,405 | 範築範鑰範願蓋鑰憲遞(餘網鏇膚選鏇襯製廠遞) = 網網夢廠鹽製醖壓鏇淵 積網觸憲憲顧鹽鑰遞蓋 (製艱願願願積獵鬱淵網 ) | - | 2005-06-01 | |||
範築範鑰範願蓋鑰憲遞(餘網鏇膚選鏇襯製廠遞) = 蓋鏇鹹淵積鑰齋蓋網艱 積網觸憲憲顧鹽鑰遞蓋 (製艱願願願積獵鬱淵網 ) |
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