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更新于：2025-04-16
Eprosartan Mesylate
依普沙坦
更新于：2025-04-16
概要
基本信息
药物类型 小分子化药 |
别名 (E)-2-butyl-1-(p-carboxybenzyl)-α-2-thenylimidazole-5-acrylic acid、(E)-3-[2-n-butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid、(E)-α{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid + [18] |
靶点 |
作用方式 拮抗剂 |
作用机制 AT1R拮抗剂(血管紧张素II-1型受体拮抗剂) |
治疗领域 |
非在研适应症- |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1997-12-22), |
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C24H28N2O7S2 |
InChIKeyDJSLTDBPKHORNY-XMMWENQYSA-N |
CAS号144143-96-4 |
关联
9
项与 依普沙坦 相关的临床试验NCT04606563
Host Response Mediators in Coronavirus (COVID-19) Infection - Is There a Protective Effect of Losartan and Other ARBs on Outcomes of Coronavirus Infection?
EUCTR2010-019155-22-DE
A Prospective, Randomized, Double-Blind, Parallel-Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects with Essential Hypertension
NCT01631227
A Prospective, Randomized Double-blind Parallel Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects With Mild to Moderate Essential Hypertension
100 项与 依普沙坦 相关的临床结果
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100 项与 依普沙坦 相关的转化医学
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100 项与 依普沙坦 相关的专利（医药）
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766
项与 依普沙坦 相关的文献（医药）2025-02-12CURRENT PHARMACEUTICAL DESIGN
Eprosartan Reduces Inflammation and Oxidative Stress in Ethanol-induced Hepatotoxicity
Article
作者: Mansourian, Mahboubeh ; Jahantab, Mohammad Bagher ; Karimi, Farzaneh ; Larki, Rozina Abbasi ; Mirghaed, Ali Taheri ; Azizi, Mahdokht ; Behrouj, Hamid ; Mehrabi, Sadrollah ; Daryabor, Gholamreza ; Abdzadeh, Soroor ; Doustimotlagh, Amir Hossein
Introduction::
Eprosartan is an effective blood pressure medication that blocks the Angiotensin
Type 1 (AT1) receptor. The studies conducted on Eprosartan showed anti-oxidative stress effects and modulating
inflammatory mechanisms. The current research is designed to clarify and examine the possible advantageous
impacts of Eprosartan against chronic ethanol-induced hepatic damage.
Method::
Twenty-four male Sprague-Dawley rats were haphazardly separated into four groups. The control
group received normal saline 1 g/kg for 35 days (group 1). The EtOH group received 7 g/kg of 40% ethanol
orally for 35 days (group 2). The EtOH+ EP group was pretreated with 60 mg/kg of Eprosartan dissolved in
normal saline orally and, after 60 minutes, received 7 g/kg of 40% ethanol orally for 35 days (group 3). The
EP group received only Eprosartan 60 mg/kg dissolved in normal saline for 35 days (group 4). The levels of
biochemical parameters, oxidative stress markers, pro-inflammatory cytokines, and histopathological staining
were evaluated in serum and liver tissue. The interactive behavior of Eprosartan with Tumor Necrosis Factor-α
(TNF-α) protein was also explained by molecular docking.
Results::
Pre-treatment with Eprosartan (60 mg/kg) notably diminished the elevation in serum alanine aminotransferase
(ALT), aspartate aminotransferase (AST) and Gamma-Glutamyl Transferase (GGT) enzymes, total
triglyceride, cholesterol, total bilirubin, and inflammatory cytokines including TNF-α, Interleukin-1β (IL-1β)
and Interleukin-6 (IL-6) levels, which were induced by alcohol administration (P-value ≤ 0.05). In the Eprosartan
pre-treated group, malondialdehyde and protein carbonyl content of liver tissue were remarkably diminished,
as compared to the ethanol-induced rats. In addition, histopathological results approved the indicated
finding. Molecular docking research gives insights into potential interactions of Eprosartan with TNF-α protein.
Conclusion::
Our results revealed that the pre-treatment with Eprosartan (60 mg/kg) preserves against chronic
alcohol-induced hepatic damage.
2024-12-01SCIENCE OF THE TOTAL ENVIRONMENT
Chemical profiling of organic contaminants in rural surface waters combining target and non-target LC-HRMS/MS analysis
Article
作者: Martínez-Piernas, Ana B. ; Moreno-González, David ; Fernández-García, Alfonso ; Martínez-Piernas, Ana B ; García-Reyes, Juan F. ; Gilbert-López, Bienvenida ; García-Reyes, Juan F
The pollution of natural waters by contaminants of emerging concern (CECs) is one of the pressing problems due to their global distribution and potential negative effects on the environment and human health. In rural areas with lower population density and limited industrial development, less contamination is expected. However, the lack of wastewater treatment plants (WWTPs) or their poor removal efficiency can lead to significant input of pollutants. In this context, 11 streams of rural areas in the Guadalquivir River basin, southeast of Spain, were studied over two years to obtain an overview of the origin and distribution of contaminants. A target method using solid-phase extraction and liquid chromatography coupled to high resolution mass spectrometry (LC-HRMS) was developed for the analysis of 316 compounds in surface waters. A total of 78 target analytes were detected, comprising pesticides, pharmaceuticals, personal care products (PCPs), transformation products (TPs), and industrial chemicals. The flame retardant tributyl phosphate (16-3572 ng L-1) was detected in all samples, followed by caffeine (30-8090 ng L-1) and the analgesic tramadol (3-1493 ng L-1). The target approach was combined with a non-target analysis (NTA) strategy to obtain an overall perspective of the chemical profile of unexpected or unknown compounds in the samples. Up to 79 contaminants were tentatively identified, and 12 of them were finally confirmed with standards. Most of the contaminants determined by NTA were pharmaceuticals and their TPs. The results indicated that most of CECs have an urban origin despite traditional agriculture is the main economic activity in this region. Moreover, the absence of WWTPs in small towns is significant, as contamination levels at these sites were comparable to or higher than those in larger populations with sewage treatments.
2024-11-01WATER RESEARCH
Adaptation towards catabolic biodegradation of trace organic contaminants in activated sludge
Article
作者: Brison, Antoine ; Fenner, Kathrin ; Seller-Brison, Carolin ; Yu, Yaochun ; Robinson, Serina L
Trace organic contaminants (TrOCs) are omnipresent in wastewater treatment plants (WWTPs), yet, their removal during wastewater treatment is oftentimes incomplete and underlying biotransformation mechanisms are not fully understood. In this study, we elucidate how different factors, including pre-exposure levels and duration, influence microbial adaptation towards catabolic TrOC biodegradation and its potential role in biological wastewater treatment. Four sequencing batch reactors (SBRs) were operated in parallel in three succeeding phases, adding and removing a selection of 26 TrOCs at different concentration levels. After each phase of SBR operation, a series of batch experiments was conducted to monitor biotransformation kinetics of those same TrOCs across various spike concentrations. For half of our test TrOCs, we detected increased biotransformation in sludge pre-exposed to TrOC concentrations ≥5 µg L-1 over a 30-day period, with most significant differences observed for the insect repellent DEET and the artificial sweetener saccharin. Accordingly, 16S rRNA amplicon sequencing revealed enrichment of taxa that have previously been linked to catabolic biodegradation of several test TrOCs, e.g., Bosea sp. and Shinella sp. for acesulfame degradation, and Pseudomonas sp. for caffeine, cyclamate, DEET, metformin, paracetamol, and isoproturon degradation. We further conducted shotgun metagenomics to query for gene products previously reported to be involved in the TrOCs' biodegradation pathways. In the future, directed microbial adaptation may be a solution to improve bioremediation of TrOCs in contaminated environments or in WWTPs.
100 项与 依普沙坦 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 |
|---|---|---|---|
| 原发性高血压 | 澳大利亚 | 1998-06-15 | |
| 高血压 | 美国 | 1997-12-22 |
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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 | 原发性高血压 N-terminal pro-brain natriuretic peptide (NT-proBNP) | 165 | 蓋齋獵範製鹽築鹹襯積(襯構壓憲選鏇鬱積醖選) = 遞衊顧衊憲遞鏇窪襯鹽 鏇顧夢襯鹽蓋遞膚積夢 (淵鏇積築窪願齋簾膚構 ) | - | 2018-08-27 | ||
临床3期 | 665 | Placebo Eprosartan mesylate+Eprosartan (Eprosartan) | 遞襯選齋壓夢構齋襯觸(鬱獵鏇鹹積範艱簾築餘) = 餘膚鑰鹹衊顧鏇構襯範 積鬱醖淵觸構觸積遞鑰 (顧築窪範蓋鹹淵構齋鑰, 7.7) 更多 | - | 2014-05-26 | ||
Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate) | 遞襯選齋壓夢構齋襯觸(鬱獵鏇鹹積範艱簾築餘) = 築鹹鹹壓網艱艱膚餘鹽 積鬱醖淵觸構觸積遞鑰 (顧築窪範蓋鹹淵構齋鑰, 7.5) 更多 | ||||||
临床4期 | 1,405 | 鹽鏇醖窪鑰鬱糧淵衊淵(製襯廠鏇壓網網簾窪醖) = 鑰製範醖構糧鹽窪膚鑰 築構遞廠積獵鏇餘選選 (夢壓鬱齋憲壓餘鹽網淵 ) | - | 2005-06-01 | |||
鹽鏇醖窪鑰鬱糧淵衊淵(製襯廠鏇壓網網簾窪醖) = 顧鹽顧夢觸窪選願獵繭 築構遞廠積獵鏇餘選選 (夢壓鬱齋憲壓餘鹽網淵 ) |
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