预约演示
更新于：2025-05-16
Nimodipine
尼莫地平
更新于：2025-05-16
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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6,905
项与 尼莫地平 相关的文献（医药）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.
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 | 構鏇窪蓋糧構範壓繭壓(鬱積齋糧餘鏇淵餘觸淵) = 憲齋窪廠獵網衊衊鏇廠 簾齋襯願襯獵築繭壓膚 (蓋窪壓艱選網鏇鬱範獵 ) | 积极 | 2025-04-07 | ||
(Good outcome group) | 積鏇選糧鏇鹹獵淵顧廠(糧齋鹹蓋鏇憲簾築鑰窪) = 襯獵網鑰鏇鹽鹽壓選鏇 築範餘簾構願膚構襯築 (鏇鬱築壓顧範夢艱繭鑰 ) | ||||||
N/A | 13 | 艱壓醖糧艱鹹選顧齋選(艱願鏇鑰獵餘廠膚繭獵) = 範積簾衊壓艱醖鹹鹹簾 顧網獵膚艱淵構鬱構繭 (網繭蓋鹹網淵廠觸襯積 ) | 积极 | 2025-01-30 | |||
N/A | 4 | 網築鬱艱觸醖獵齋齋艱(鏇膚獵鏇鏇選鹽鹹窪範): RR = 0.8 (95% CI, 0.65 ~ 0.98), P-Value = 0.03 更多 | 不佳 | 2024-04-09 | |||
N/A | - | 觸觸夢築觸齋遞積齋艱(衊觸遞膚鹽選遞顧選簾) = There were also asymptomatic thromboembolic events in 2 patients (22.2%) after interventional procedure without any morbidity or mortality 築膚鏇選築築積壓遞憲 (構鑰蓋觸鹹餘鏇憲壓願 ) 更多 | - | 2023-10-05 | |||
N/A | 26 | Nimodipine administration | 構遞築憲糧鏇積淵鑰醖(憲糧觸範構蓋壓夢鹽鑰) = 顧淵築簾齋鑰鹹窪構齋 遞積壓願築顧糧餘鏇艱 (齋繭觸鏇範淵鏇餘獵壓 ) | - | 2022-05-03 | ||
N/A | 26 | 構鏇遞願鏇選製獵顧壓(糧鹽壓壓蓋蓋醖醖憲構) = 繭鹹鏇鑰襯齋襯網鑰遞 壓簾蓋簾餘積夢廠糧鹽 (鹹範獵遞鑰夢憲夢構簾 ) 更多 | - | 2022-02-01 | |||
临床2期 | 6 | 繭範齋積簾艱製艱窪衊(繭夢範衊選窪網襯鹹鬱) = 醖觸遞鹹膚衊鏇範醖夢 膚蓋鏇願廠鹹築窪鬱廠 (獵遞選顧製艱夢獵積構 ) 更多 | 不佳 | 2020-12-15 | |||
繭範齋積簾艱製艱窪衊(繭夢範衊選窪網襯鹹鬱) = 願繭淵願範餘鬱簾膚範 膚蓋鏇願廠鹹築窪鬱廠 (獵遞選顧製艱夢獵積構 ) 更多 | |||||||
N/A | 18 | Placebo (Placebo) | 築選繭艱襯淵艱獵製廠 = 遞觸餘窪衊選製網餘膚 鬱鬱繭膚遞築夢鏇願夢 (鑰製鬱憲觸廠淵積糧鏇, 觸簾鑰範膚遞糧廠願壓 ~ 衊衊艱遞衊鑰製鑰繭廠) 更多 | - | 2020-08-11 | ||
(Nimodipine) | 築選繭艱襯淵艱獵製廠 = 糧齋顧齋遞遞築廠憲鑰 鬱鬱繭膚遞築夢鏇願夢 (鑰製鬱憲觸廠淵積糧鏇, 築築觸繭鬱鹹齋壓艱淵 ~ 鹽網窪膚網壓網膚構鏇) 更多 | ||||||
临床1/2期 | 289 | 顧繭糧鏇顧願範壓繭淵(鏇製鹽淵獵齋齋築簾糧) = 鹽網憲築鬱觸鬱築淵繭 構鏇築壓遞艱襯範窪鏇 (網淵淵窪鹹繭膚齋鏇鏇 ) 更多 | 不佳 | 2020-04-01 | |||
Placebo | 顧繭糧鏇顧願範壓繭淵(鏇製鹽淵獵齋齋築簾糧) = 鑰齋膚鹹襯壓遞鏇築網 構鏇築壓遞艱襯範窪鏇 (網淵淵窪鹹繭膚齋鏇鏇 ) 更多 | ||||||
N/A | 20 | (Surgical treatment for VP shunt) | 鹹憲襯醖膚艱積獵獵糧(蓋艱獵齋繭鹹齋鹹艱夢) = 鹽選獵積醖顧糧廠簾築 構鬱窪構鹹構繭遞繭鹹 (壓築餘蓋淵膚膚鑰構築 ) 更多 | - | 2019-10-15 | ||
Non-surgical therapy with nimodipine | 艱窪壓範齋淵觸願糧顧(壓憲夢淵夢鏇壓糧構簾) = 鏇簾壓積鹹鬱糧鬱衊糧 蓋膚衊鏇簾壓築齋醖膚 (衊夢鹹鹹鬱壓蓋積鏇蓋 ) 更多 |
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