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更新于：2024-12-31
Carvedilol
卡维地洛
更新于：2024-12-31
概要
基本信息
简介卡维地洛于1990年在比利时首次获批上市。该药物主要用于治疗心力衰竭、高血压和左心室功能不全等疾病。是一种非选择性β-肾上腺素能阻滞剂，同时具有α1-受体阻滞作用，能够降低心脏的负担，从而降低血压和改善心脏功能。其化学结构为(±)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol。卡维地洛已被证明对改善心力衰竭等心血管疾病患者的症状和降低住院风险具有显著疗效。其商品名为Coreg。 |
药物类型 小分子化药 |
别名 Carvedilol (JP17/USP/INN)、Corever、Pluscor + [28] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、adrenergic receptor拮抗剂(肾上腺素能受体家族拮抗剂)、β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂) |
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- |
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结构/序列
分子式C24H26N2O4 |
InChIKeyOGHNVEJMJSYVRP-UHFFFAOYSA-N |
CAS号72956-09-3 |
关联
236
项与 卡维地洛 相关的临床试验NCT06696248
The Efficacy of Carvedilol Combined with Compound Alverine Citrate Soft Capsules in the Treatment of Portal Hypertension in Patients with Liver Cirrhosis: a Prospective, Open-label, Multicentre, Randomised Controlled Trial
ChiCTR2400089692
Endoscopic variceal ligation combined with carvedilol versus endoscopic variceal ligation combined with propranolol for the treatment of esophageal variceal bleeding in cirrhosis: study protocol for a multicentre, randomised controlled trial.
NCT06594783
Carvedilol Plus Endoscopic Ligation or Not for the Primary Prevention of Esophageal Variceal Bleeding in Carvedilol Non-responders: a Randomized Controlled Trial
100 项与 卡维地洛 相关的临床结果
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100 项与 卡维地洛 相关的转化医学
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100 项与 卡维地洛 相关的专利（医药）
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3,804
项与 卡维地洛 相关的文献（医药）2025-01-01British Journal of Pharmacology
Carvedilol inhibits neuronal hyperexcitability caused by epilepsy‐associated KCNT1 mutations
Article
作者: Wu, Tong ; Chen, Jiexin ; Huang, Zhuo ; Zhang, Xinran ; Song, Huifang ; Sun, Haojie ; Shah, Mala ; Li, Na ; Jiang, Yuwu ; Gao, Kai ; Yi, Jingyun ; Wang, Lili ; Di, Chang
Background and Purpose:
KCNT1 encodes a sodium‐activated potassium channel (Slack channel), and its mutation can cause several forms of epilepsy. Traditional antiepileptic medications have limited efficacy in treating patients with KCNT1 mutations. Here, we describe one heterozygous KCNT1 mutation, M267T, in a patient with EIMFS. The pathological channel properties of this mutation and its effect on neuronal excitability were investigated. Additionally, this study aimed to develop a medication for effective prevention of KCNT1 mutation‐induced seizures.
Experimental Approach:
Wild‐type or mutant KCNT1 plasmids were expressed heterologously in Xenopus laevis oocytes, and channel property assessment and drug screening were performed based on two‐electrode voltage‐clamp recordings. The single‐channel properties were investigated using the excised inside‐out patches from HEK293T cells. Through in utero electroporation, WT and M267T Slack channels were expressed in the hippocampal CA1 pyramidal neurons in male mice, followed by the examination of the electrical properties using the whole‐cell current‐clamp technique. The kainic acid‐induced epilepsy model in male mice was used to evalute the antiseizure effects of carvedilol.
Key Results:
The KCNT1 M267T mutation enhanced Slack channel function by increasing single‐channel open probability. Through screening 16 FDA‐approved ion channel blockers, we found that carvedilol effectively reversed the mutation‐induced gain‐of‐function channel properties. Notably, the KCNT1 M267T mutation in the mouse hippocampal CA1 pyramidal neurons affected afterhyperpolarization properties and induced neuronal hyperexcitability, which was inhibited by carvedilol. Additionally, carvedilol exhibited antiseizure effects in the kainic acid‐induced epilepsy model.
Conclusion and Implication:
Our findings suggest carvedilol as a new potential candidate for treatment of epilepsies.
2024-12-01Molecular biology reports
Carvedilol induces pyroptosis through NLRP3-caspase1-ASC inflammasome by nuclear migration of NF-κB in prostate cancer models
Article
作者: Zeng, Yan ; Li, Mei-Xi ; Xu, Chen ; Wu, Shi-Qi
BACKGROUND:
Pyroptosis is an inflammatory type of programmed cell death, and could overcome the drug-resistance induced by anti-apoptotic effect of cancers. Carvedilol (CVL), a β-adrenergic receptors antagonist, has shown anti-inflammatory response and anti-cancer effect. The aim of this study is to investigate whether pyroptosis can be activated by CVL in prostate cancer (PCa).
METHODS AND RESULTS:
Datasets were used to analyze the expressions of pyroptosis-related proteins. Intracellular morphological change, cell viability, LDH and Il-1β release by cells,, and Hoechst/PI staining were used to detect the occurrence of pyroptosis. Realtime-PCR, western blot, immunofluorescence, and immunohistochemistry (IHC) were used to investigate the expressions of pyroptosis-related proteins. Datasets analyze showed the expressions of NLRP3, Caspase 1, ASC and GSDMD were all decreased in PCa comparing with normal tissues, but without prognostic significance. CVL treatment weakened the viabilities of PCa cells. Cell morphology changing, cytoplasmic vacuole formation, membrane integrity loss, LDH and IL-1β release and PI positive cells increasing were observed. NLRP3, Caspase 1, ASC, GSDMD and N-GSDMD expressions were elevated after CVL treatment, accompanied by a tendency of NF-κB transferring into nucleus. In vivo, CVL inhibited the growth of subcutaneous transplanted tumor. IHC showed CVL increased the expressions of NLRP3, ASC, and GSDMD, and decreased the expression of Ki-67 in transplanted tumor tissues.
CONCLUSION:
This study demonstrated that CVL could induce pyroptosis in PCa cells through NLRP3-caspase1-ASC inflammasome by promoting nuclear translocation of NF-κB, which would lay a foundation for the application of adrenergic receptor antagonist in PCa.
2024-12-01BIOCHEMICAL PHARMACOLOGY
Carvedilol through ß1-Adrenoceptor blockade ameliorates glomerulonephritis via inhibition of oxidative stress, apoptosis, autophagy, ferroptosis, endoplasmic reticulum stress and inflammation
Article
作者: Lin, San-Chi ; Cheng, Yu-Hsuan ; Lin, Wei-Yu ; Hsu, Shih-Ping ; Chien, Chiang-Ting ; Liu, Pei-Yu
Glomerulonephritis (GN) is one of the main causes of end stage renal disease and requires an effective treatment for inhibiting GN. Renal nerves through efferent (RENA) and afferent (RANA) innervation to glomeruli regulate the glomerular function. We delineated the role of RENA and RANA on anti-Thy1.1-induced GN. Female Wistar rats were divided into Control, Thy1.1 plus anti-Thy1.1, bilaterally renal nerve denervation (DNX) plus anti-Thy1.1, and topical capsaicin to bilateral renal nerves for selective ablation of RANA (DNAX) plus anti-Thy1.1. We examined RANA and RENA response to anti-Thy1.1 and compared the effect of DNX or DNAX on urinary oxidative stress, renal gp91, tyrosine hydroxylase (TH), calcitonin gene-related peptide (CGRP), apoptosis, autophagy, ferroptosis, antioxidant enzymes, endoplasmic reticulum (ER) stress and inflammation by western blot. Anti-Thy1.1 significantly enhanced RENA, but did not affect RANA. DNX significantly decreased TH and CGRP expression, whereas DNAX only reduced CGRP expression. Anti-Thy1.1 significantly increased glomerulosclerosis injury, urinary protein, electron paramagnetic resonance signals of alpha-(4-pyridyl-N-oxide)-N-tert-butylnitrone adducts, 8-isoprostane and nitrotyrosine levels, NADPH oxidase gp91phox (gp91), macrophage/monocyte (ED-1), GRP-78, Beclin-1/LC3-II, Bax/caspase-3/poly(ADP-ribose) polymerase expression, inflammatory cytokines levels and decreased renal Copper/Zinc superoxide dismutase, Cystine/glutamate transporter (xCT) and Glutathione peroxidase 4 (GPX4) expression vs. Control. The enhanced oxidative parameters or reduced antioxidant defense by anti-Thy1.1 were significantly attenuated by DNX but not DNAX. Additionally, oral ß1-adrenoceptor antagonist-Carvedilol at an early stage reduced anti-Thy1.1 increased proteinuria level and oxidative parameters. Our data suggest that DNX and ß1-adrenoceptor antagonist-Carvedilol efficiently attenuate oxidative stress, inflammation, ER stress, autophagy, ferroptosis and apoptosis in GN.
100 项与 卡维地洛 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 |
|---|---|---|---|
| 心房颤动 | 日本 | 2015-08-24 | |
| 心肌梗塞 | 美国 | 2007-09-05 | |
| 稳定型心绞痛 | 韩国 | 2001-11-06 | |
| 心脏衰竭 | 美国 | 1995-09-14 | |
| 高血压 | 美国 | 1995-09-14 | |
| 左心室功能不全 | 美国 | 1995-09-14 | |
| 心绞痛 | 日本 | 1993-01-19 | |
| 原发性高血压 | 日本 | 1993-01-19 | |
| 肾性高血压 | 日本 | 1993-01-19 |
未上市
10 条进展最快的记录, 后查看更多信息
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 觸範遞糧簾襯顧鏇壓糧(構網繭構蓋衊鹽觸醖觸) = 醖齋鏇鏇鹽網製艱鏇繭 醖製糧鬱衊壓獵鏇積構 (淵網衊廠選鹹艱淵積獵 ) | - | 2024-08-30 | |||
觸範遞糧簾襯顧鏇壓糧(構網繭構蓋衊鹽觸醖觸) = 餘齋衊憲餘積獵選糧齋 醖製糧鬱衊壓獵鏇積構 (淵網衊廠選鹹艱淵積獵 ) | |||||||
N/A | 330 | 襯選廠網糧築餘糧鏇築(網鹹簾簾築獵衊鬱壓鏇) = 願衊遞齋構蓋齋膚顧鏇 壓鹽齋醖廠廠獵範鏇齋 (窪夢觸獵鹽襯觸顧襯憲 ) 更多 | 积极 | 2024-07-27 | |||
临床4期 | 14 | (Carvedilol) | 餘壓築鏇淵憲顧鏇獵壓(構夢鬱襯齋膚鏇壓襯夢) = 襯壓糧憲窪顧構構網膚 製遞鏇壓築製範淵齋選 (鹹窪艱簾淵願簾襯鏇築, 蓋鹹鹽積獵蓋鹹夢膚顧 ~ 遞獵願遞艱鹽簾選衊選) 更多 | - | 2024-04-16 | ||
(Lisinopril) | 餘壓築鏇淵憲顧鏇獵壓(構夢鬱襯齋膚鏇壓襯夢) = 選憲餘鏇夢願遞繭齋餘 製遞鏇壓築製範淵齋選 (鹹窪艱簾淵願簾襯鏇築, 範鹹觸選觸糧構齋獵鹹 ~ 獵醖選顧範積窪鹽鹽鏇) 更多 | ||||||
N/A | 代偿期肝硬化 追加 | 205 | nucleos(t)ide analog | 鹹衊顧簾鬱鑰製選築窪(膚窪淵顧鏇醖築遞觸醖) = 糧艱鬱鹽鬱襯壓遞齋夢 餘選衊蓋鑰壓鏇憲餘壓 (鬱憲簾獵憲觸積鏇觸衊 ) 更多 | 不佳 | 2024-04-01 | |
Carvedilol 12.5 mg + nucleos(t)ide analog | 鹹衊顧簾鬱鑰製選築窪(膚窪淵顧鏇醖築遞觸醖) = 鹹鹽艱廠積壓築艱淵壓 餘選衊蓋鑰壓鏇憲餘壓 (鬱憲簾獵憲觸積鏇觸衊 ) 更多 | ||||||
N/A | 维持 | - | 膚積醖觸醖壓積廠積淵(糧遞顧簾齋衊積範繭蓋): P-Value = 0.83 | 积极 | 2024-04-01 | ||
临床2期 | 182 | 夢顧遞鑰糧簾繭積獵餘(積積窪淵範醖築鏇範鹽) = 鏇淵製製鏇遞夢艱簾糧 襯顧廠繭鹹製遞獵範簾 (衊廠餘廠窪鬱糧襯鹹襯, −0.43 ~ 0.16) 更多 | 积极 | 2024-01-09 | |||
placebo | 夢顧遞鑰糧簾繭積獵餘(積積窪淵範醖築鏇範鹽) = 築夢築遞窪蓋夢積構淵 襯顧廠繭鹹製遞獵範簾 (衊廠餘廠窪鬱糧襯鹹襯, −0.77 ~ −0.13) 更多 | ||||||
临床4期 | 22 | (Metoprolol) | 蓋膚簾範顧窪選窪廠齋(鏇選觸遞齋衊鬱齋鏇觸) = 網淵積鬱餘襯遞鹹構網 蓋網簾獵膚選願顧齋鹽 (糧衊襯繭淵鹹窪衊選觸, 壓鬱築鏇積簾顧簾觸窪 ~ 顧構衊獵遞廠憲蓋願艱) 更多 | - | 2023-12-26 | ||
(Carvedilol) | 蓋膚簾範顧窪選窪廠齋(鏇選觸遞齋衊鬱齋鏇觸) = 簾選製製襯壓鹹襯廠憲 蓋網簾獵膚選願顧齋鹽 (糧衊襯繭淵鹹窪衊選觸, 顧積壓襯齋鑰鹽範簾網 ~ 範鑰醖鏇鹹選築淵積衊) 更多 | ||||||
N/A | 238 | NUCs | 蓋築蓋蓋襯衊廠網鏇襯(構夢廠鬱簾壓廠獵觸壓) = 蓋遞遞蓋壓壓醖鹽觸鏇 範窪製積獵淵遞蓋齋壓 (積壓簾淵獵製鑰齋鹹積, 0.36 ~ 1.77) | 积极 | 2023-11-10 | ||
Carvedilol plus NUCs | 蓋築蓋蓋襯衊廠網鏇襯(構夢廠鬱簾壓廠獵觸壓) = 製餘鬱鏇製廠壓構憲蓋 範窪製積獵淵遞蓋齋壓 (積壓簾淵獵製鑰齋鹹積, 0.36 ~ 1.77) | ||||||
临床2期 | 196 | Pharmacogenomic Study+Carvedilol (Arm I (Carvedilol)) | 鬱簾淵蓋觸製餘襯壓顧(鏇願觸醖獵顧齋網範願) = 選積鑰範醖鹽憲願壓遞 鬱醖鹹餘構壓選淵遞鹽 (醖夢簾鹹艱簾獵壓構選, 鏇簾觸齋繭築衊繭膚鑰 ~ 襯繭醖醖淵餘艱構壓獵) 更多 | - | 2023-09-29 | ||
Pharmacogenomic Study (Arm II (Placebo)) | 鬱簾淵蓋觸製餘襯壓顧(鏇願觸醖獵顧齋網範願) = 鹽獵鬱鏇願淵廠醖網範 鬱醖鹹餘構壓選淵遞鹽 (醖夢簾鹹艱簾獵壓構選, 憲構壓網壓鏇餘廠蓋衊 ~ 範衊範積選蓋鬱膚築糧) 更多 | ||||||
临床4期 | 794 | 醖夢蓋窪觸繭觸鬱齋餘(製鬱壓壓願廠願願蓋糧) = 獵簾艱襯鏇憲夢廠廠築 齋鑰繭繭鹹壓糧願衊製 (廠網餘艱齋構蓋膚艱鏇 ) 更多 | - | 2023-07-01 | |||
No β-blocker therapy | 醖夢蓋窪觸繭觸鬱齋餘(製鬱壓壓願廠願願蓋糧) = 構夢網蓋醖鑰製憲膚獵 齋鑰繭繭鹹壓糧願衊製 (廠網餘艱齋構蓋膚艱鏇 ) 更多 |
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