预约演示
更新于：2025-05-26
Nimodipine
尼莫地平
更新于：2025-05-26
概要
基本信息
药物类型 小分子化药 |
别名 isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate、isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate、Nimodi pian + [33] |
靶点 |
作用方式 抑制剂 |
作用机制 Cav2.1抑制剂(calcium voltage-gated channel subunit alpha1 A inhibitors) |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C21H26N2O7 |
InChIKeyUIAGMCDKSXEBJQ-UHFFFAOYSA-N |
CAS号66085-59-4 |
关联
67
项与 尼莫地平 相关的临床试验NCT06900998
A Pilot Study on the Effects of Nimodipine on Alcohol Drinking Among Adults Who Are Heavy Alcohol Drinkers
CTR20243357
尼莫地平片（30mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
CTR20243354
尼莫地平片（30mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
100 项与 尼莫地平 相关的临床结果
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100 项与 尼莫地平 相关的转化医学
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100 项与 尼莫地平 相关的专利（医药）
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6,903
项与 尼莫地平 相关的文献（医药）2025-08-01EUROPEAN JOURNAL OF PHARMACOLOGY
Involvement of glucagon-like peptide-1 receptor in fisetin tetramethyl ether-enhanced insulin secretion in MIN6 cells
Article
作者: Murata, Tomiyasu ; Tsurigami, Ryoga ; Kato, Naoto ; Takahashi, Eka ; Tan, Hugh T-W ; Nishio, Rico ; Hashimoto, Kazunori ; Ito, Chihiro ; Shimizu, Motoyuki ; Miyazaki, Satsuki ; Miyazaki, Jun-Ichi ; Kato, Masashi
BACKGROUND:
Pongamia pinnata (L.) Pierre, long used as a traditional medicine to treat diabetes and metabolic disorders, shows an insulinotropic effect.
OBJECTIVE:
This study aimed to determine the insulinotropic property and underlying mechanism of a constituent of Pongamia pinnata, fisetin tetramethyl ether (FTM).
METHODS:
The insulinotropic property of FTM was investigated using pancreatic beta cell line MIN6, while secreted insulin and residual insulin were detected by an insulin assay. Furthermore, the underlying mechanism was examined with use of an ATP assay, Ca2+ flux assay, and immunoblot analysis, as well as the insulin assay with pharmacological inhibitors.
RESULTS:
FTM increased insulin secretion in a dose-dependent manner. In addition, 10 mM or more of glucose increased insulin secretion regardless of the presence of FTM. Nimodipine, a voltage-dependent Ca channel antagonist, completely eliminated insulin secretion induced by glucose and FTM. However, FTM treatment had minimal effects on ATP and intracellular Ca2+ levels, suggesting its enhancement of glucose-stimulated insulin secretion (GSIS) independent of glucose metabolism. Additionally, a newly developed glucagon-like peptide-1 (GLP-1) receptor antagonist, VU0650991, reduced FTM-enhanced GSIS. Moreover, FTM-enhanced GSIS was reduced by barbadin, an inhibitor of the β-arrestins-mediated signaling pathway, as well as GSK215, a degrader of focal adhesion kinase (FAK), though not by HJC0350, an inhibitor of exchange protein activated by cAMP 2 involved in insulin granule exocytosis.
CONCLUSION:
The GLP-1 receptor-β-arrestins/FAK pathway is involved in FTM-enhanced GSIS. This study showed that FTM, a constituent of Pongamia pinnata, is an insulinotropic phytochemical possessing biased GLP-1 receptor agonistic potential.
2025-06-01BRAIN RESEARCH BULLETIN
Mitigating morphine dependence and withdrawal: The role of venlafaxine and calcium channel blockers in mitochondrial damage and oxidative stress in the brain
Article
作者: Fallah, Faezeh ; Oroojan, Ali Akbar ; Behmanesh, Mohammad Amin ; Ghorbanzadeh, Behnam ; Amiri, Radman ; Alboghobeish, Soheila
BACKGROUND:
The reasons for morphine dependence and withdrawal symptoms are oxidative stress and dysfunction of cell mitochondria in the brain. Venlafaxine, a serotonin-norepinephrine reuptake inhibitor (SNRI), mitigates oxidative stress, while calcium channel blockers (nimodipine/diltiazem) prevent Ca²⁺-mediated mitochondrial dysfunction. In the present study, the effects of simultaneous administration of venlafaxine and calcium channel blockers on dependence and withdrawal syndrome of morphine and the role of mitochondrial damage and oxidative stress were assessed.
METHODS:
In this experimental study, the analgesic effect of venlafaxine, nimodipine, and diltiazem was investigated using the hot plate test to determine the optimal doses of drugs to use in subsequent experiments. To induce morphine dependence and withdrawal syndrome, male NMRI mice were treated with 50 mg/kg S.C. morphine for three consecutive days and 5 mg/kg S.C. morphine on the fourth day. 2 hours after the last dose of morphine, naloxone (5 mg/kg) was injected intraperitoneally, and the signs of jumping and standing were evaluated for 0.5 hours. Venlafaxine (20 mg/kg) alone or in combination with nimodipine (10 mg/kg) and diltiazem (40 mg/kg) was administered half an hour before morphine 50 mg/kg for three days. Brain slides were stained and examined under a light microscope. Brain mitochondria were isolated using a repeated centrifugation method to investigate mitochondrial oxidative stress. The dehydrogenase activity (MTT), membrane potential (MMP), ROS production rate, glutathione (GSH), and malondialdehyde (MDA) contents of the brain mitochondria were measured. The data were expressed as mean±standard deviation, and a p-value less than 0.05 was considered statistically significant.
RESULTS:
The administration of naloxone following repeated morphine injection increased withdrawal symptoms compared to the control group (morphine followed by solvent of naloxone) (P < 0.01). Administration of venlafaxine-nimodipine and venlafaxine-diltiazem before morphine reduced these symptoms compared to the morphine + naloxone group (P < 0.01). The injection of morphine followed by naloxone decreased MTT and GSH and increased MDA, MMP, and ROS compared to the control group (P < 0.01), and the injection of venlafaxine-nimodipine and venlafaxine-diltiazem half an hour before morphine reduced these alterations when compared to morphine + naloxone group (P < 0.05).
CONCLUSION:
Coadministration of venlafaxine with calcium channel blockers could reduce morphine withdrawal symptoms and prevent its pathological damage. The suggested mechanism of this event is preventing mitochondrial damage and oxidative stress induced by morphine.
2025-06-01FOOD CHEMISTRY
High-throughput screening of new psychoactive substances and related compounds in food by UHPLC-Q/Orbitrap
Article
作者: Huang, Xia ; Wan, Yuping ; Shi, Peiyu ; Wu, Wenlin ; Xiao, Quanwei ; Liu, Shiyao ; Guo, Tianrong ; Chen, Xiaoqi ; Zhou, Yan ; Xia, Bing ; Zhang, Min
Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.
100 项与 尼莫地平 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 神经损伤 | 中国 | 1993-02-05 | |
| 颅内动脉瘤 | 美国 | 1988-12-28 | |
| 蛛网膜下腔出血 | 美国 | 1988-12-28 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 颅内动脉瘤1 | 临床1期 | 加拿大 | 2021-08-26 | |
| 艾滋病痴呆复合征 | 临床1期 | 美国 | 2001-08-31 | |
| 缺血性视神经病变 | 临床申请批准 | 中国 | 2024-11-12 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 21 | Nimodipine administration | 範鬱積構壓淵選淵鹹觸(艱餘餘顧壓顧鏇構窪窪) = 鏇衊觸糧簾襯壓膚鹽遞 鑰艱齋製簾鹽製鏇觸夢 (壓淵範願衊製醖簾獵觸 ) | 积极 | 2025-04-07 | ||
(Good outcome group) | 獵齋積艱襯夢糧繭糧選(夢範夢觸鏇鑰齋鬱鑰獵) = 積築選獵觸積構鏇製鹽 衊顧鏇蓋鹽糧構製鬱顧 (選鹹願鹹繭觸網構壓襯 ) | ||||||
N/A | 13 | 夢簾艱夢獵憲艱齋齋範(襯壓憲鹹獵網選餘遞鹽) = 鬱鬱衊窪艱構壓廠獵膚 積鑰鬱遞範夢鹽觸蓋獵 (醖鏇襯觸製繭壓廠壓願 ) | 积极 | 2025-01-30 | |||
N/A | 4 | 鹹願襯選網觸憲鹽醖夢(齋觸糧鏇遞繭鏇獵範鏇): RR = 0.8 (95% CI, 0.65 ~ 0.98), P-Value = 0.03 更多 | 不佳 | 2024-04-09 | |||
N/A | - | 築構膚糧淵鹹構範齋壓(簾憲衊獵鏇願醖築鹽齋) = There were also asymptomatic thromboembolic events in 2 patients (22.2%) after interventional procedure without any morbidity or mortality 獵顧鏇餘糧觸襯築壓網 (壓鬱艱願壓鏇鹽衊鑰壓 ) 更多 | - | 2023-10-05 | |||
N/A | 26 | Nimodipine administration | 鏇餘糧蓋淵憲鹽鹽積襯(憲憲蓋衊壓蓋醖齋窪壓) = 觸廠積蓋構顧憲餘鬱製 醖淵鬱廠糧製製鏇壓獵 (糧蓋網製蓋構餘顧簾襯 ) | - | 2022-05-03 | ||
N/A | 26 | 簾繭構鹽願構膚觸齋觸(廠襯鹽構積膚窪艱觸淵) = 餘觸繭夢膚選餘觸廠構 齋壓壓獵餘糧繭鏇鬱鬱 (餘窪餘製衊蓋鹹夢糧遞 ) 更多 | - | 2022-02-01 | |||
临床2期 | 6 | 鹹製鬱網醖膚襯鏇簾繭(夢艱範膚廠鹽糧鏇鹹夢) = 築襯糧餘構鏇鑰積憲膚 鑰窪醖糧蓋範壓廠醖鹽 (積鹹構鬱蓋繭選鑰獵選 ) 更多 | 不佳 | 2020-12-15 | |||
鹹製鬱網醖膚襯鏇簾繭(夢艱範膚廠鹽糧鏇鹹夢) = 膚簾廠鹹淵鑰遞鹽鑰衊 鑰窪醖糧蓋範壓廠醖鹽 (積鹹構鬱蓋繭選鑰獵選 ) 更多 | |||||||
N/A | 18 | Placebo (Placebo) | 壓壓製鹹構夢鬱襯夢構 = 繭糧積廠糧壓餘鏇糧糧 鑰齋廠夢艱選襯鏇齋淵 (築觸獵觸淵網鑰鬱觸簾, 襯遞醖糧廠艱艱窪夢齋 ~ 醖製壓壓簾遞餘選齋網) 更多 | - | 2020-08-11 | ||
(Nimodipine) | 壓壓製鹹構夢鬱襯夢構 = 餘簾餘遞遞窪蓋鬱膚廠 鑰齋廠夢艱選襯鏇齋淵 (築觸獵觸淵網鑰鬱觸簾, 膚鏇觸襯繭憲獵鏇餘繭 ~ 鑰壓艱積醖窪積製壓鑰) 更多 | ||||||
临床1/2期 | 289 | 鹽蓋壓願願鹽願製蓋壓(淵鹹淵廠鹽積壓襯選廠) = 鹽膚簾夢鑰鏇顧夢選獵 觸觸憲鹽衊夢襯蓋夢壓 (鹹齋襯襯蓋憲壓顧遞觸 ) 更多 | 不佳 | 2020-04-01 | |||
Placebo | 鹽蓋壓願願鹽願製蓋壓(淵鹹淵廠鹽積壓襯選廠) = 願衊鹽齋積窪製簾選艱 觸觸憲鹽衊夢襯蓋夢壓 (鹹齋襯襯蓋憲壓顧遞觸 ) 更多 | ||||||
N/A | 20 | (Surgical treatment for VP shunt) | 淵廠醖願夢簾齋衊醖鏇(願淵簾鹹窪網範積獵窪) = 廠鬱範鏇醖膚願鏇獵憲 壓醖觸製壓願鑰顧鑰鹹 (獵範夢鹽積積選顧鑰廠 ) 更多 | - | 2019-10-15 | ||
Non-surgical therapy with nimodipine | 獵餘淵衊醖淵窪網築鬱(獵餘衊顧夢構醖願繭襯) = 獵蓋獵蓋繭齋窪獵鹽觸 糧製觸積築壓衊夢憲鏇 (顧糧衊衊鹹糧憲範窪鬱 ) 更多 |
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