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更新于：2025-05-15
Acipimox
阿昔莫司
更新于：2025-05-15
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 意大利 (1985-01-01), |
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C6H6N2O3 |
InChIKeyDJQOOSBJCLSSEY-UHFFFAOYSA-N |
CAS号51037-30-0 |
关联
50
项与 阿昔莫司 相关的临床试验CTR20244698
阿昔莫司胶囊空腹及餐后人体生物等效性研究
CTR20244588
阿昔莫司胶囊生物等效性试验
CTR20244458
阿昔莫司胶囊人体生物等效性研究
100 项与 阿昔莫司 相关的临床结果
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100 项与 阿昔莫司 相关的转化医学
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100 项与 阿昔莫司 相关的专利（医药）
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485
项与 阿昔莫司 相关的文献（医药）2025-06-01BRAIN RESEARCH BULLETIN
Acipimox mitigates depression like behavior following high fat rich diet in rats
Article
作者: Irfan, Ali ; Khaliq, Saima ; Ahmad, Saara ; Manzoor, Natasha ; Raish, Mohammad ; Samad, Noreen ; Bin Khatab Abbasi, Bakar ; Bin Jardan, Yousef A
Acipimox (ACPX), a niacin derivative, has demonstrated antioxidant activity In vitro and In vivo; however, it has not been widely used in treating neurological problems. The present study examined the effects of Acipimox on body weight, dietary intake, depressive symptoms, oxide-neuroinflammation, 5-HT metabolism, and 5-HT1A receptor expression in hypothalamus of rats. Forty eight (n = 8) male albino rats were randomly divided into six groups (i) Vehicle (Veh)+ normal diet (ND) (ii) ND + ACPX (25 mg/mL/kg; low dose) (iii) ND+ ACPX (50 mg/mL/kg; high dose) (iv) Veh +High fat rich diet (HFRD) (v) HFRD+ACPX (25 mg/mL/kg; low dose (vi) HFRD+ACPX (50 mg/mL/kg; high dose). Animals were given their respective treatment for 8 weeks. After that, behavioral tests i.e. tail suspension test (TST) and forced swim test (FST) performed for depression-like behavior assessment. Animals were decapitated and the hypothalamus was isolated from the brain for biochemical and neurochemical analysis. Results showed that, HFRD induced depression like behavior and increased body weight and food intake was prevented by repeated administration of ACPX (both doses). HFRD induced increased oxido-neuroinflammation, altered serotonin metabolism and serotonin-1A receptor relative expression in the hypothalamus were regulated by ACPX (both doses). In conclusion, HFRD-induced behavioral deficits (depression like behavior) mitigated by ACPX through its antioxidant, anti-inflammatory, and neuromodulatory properties. It is recommended that use of ACPX could be helpful for HFRD-induced behavioral impairment i.e. depression.
2025-06-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
A chemoinformatics study to prioritization of anticancer orally active lead compounds of pearl millet against adhesion G protein-coupled receptor
Article
作者: Shukla, Adarsh Kumar ; Neeru ; Kumar, Ashwani
Metastasis is the main cause of colon cancer deaths worldwide. However, due to the disease's complexity, understanding its spread and finding natural treatments remain major challenges. The study aimed to identify therapeutic compounds in pearl millet and test them on metastatic colon cancer cell lines. The study used LC-MS and FTIR spectroscopy to identify small compounds and their functional groups. Further, theoretical chemistry, computational techniques, and ADMET analysis were applied for virtual screening and evaluating the pharmacokinetics of potential bioactive candidates of pearl millet. The 55 compounds of pearl millet were identified through the LC-MS, whereas 37 compounds were reported in PubChem database. Out of these, 15 compounds were predicted as potential orally active leads of pearl millet. Adhesion G protein-coupled receptor F5 was found as a potential target of these lead candidates. Further, molecular docking exhibited Tosifen (-7.9 kcal/mol), Sufentanil (-6.4 kcal/mol), Pemirolast (-6.3 kcal/mol), and Levosimendan (-6.3 kcal/mol) have similar binding affinity to the antineoplastics against the targeted protein. The "root mean square fluctuations (RMSFs)" analysis and deformability graph validated the docked complexes. Additionally, a comparative cell lines study against colon adenocarcinoma highlights Pemirolast as a promising candidate, demonstrating better activity compared to standard antineoplastics. This computational study predicted potential anticancer compounds in pearl millet and recommended further investigation through in vitro and in vivo studies.
2025-03-01Endocrinology, diabetes & metabolism
The Role of Serum Free Fatty Acids in Endothelium‐Dependent Microvascular Function
Article
作者: Wells, Emily K. ; Freiberg, Matthew S. ; Niswender, Kevin D. ; Wasserman, David H. ; Courvan, Meaghan C. S. ; Sullivan, Alexander E. ; Aday, Aaron W. ; Wells, Quinn S. ; Beckman, Joshua A. ; Shardelow, Emily M.
ABSTRACT:
Background:
Elevated serum free fatty acid (FFA) concentration is associated with insulin resistance and is a hallmark of metabolic syndrome. A pathological feature of insulin resistance is impaired endothelial function.
Objective:
To investigate the effect of FFA reduction with either acipimox, a nicotinic acid derivative that impairs lipolysis, or salsalate, a salicylate that reduces basal and inflammation‐induced lipolysis, on insulin‐mediated endothelium‐dependent vasodilation.
Methods:
This was a post hoc, combined analysis of two randomised, double‐blind, placebo‐controlled crossover trials. Sixteen subjects were recruited (6 with metabolic syndrome and 10 controls) and randomised to acipimox 250 mg orally every 6 h for 7 days or placebo. Nineteen subjects were recruited (13 with metabolic syndrome and 6 controls) and randomised to receive salsalate 4.5 g/day for 4 weeks or placebo. The primary outcome was the association between FFA concentration and insulin‐mediated vasodilation, measured by venous‐occlusion strain‐gauge plethysmography at baseline and following FFA modulation with the study drugs.
Results:
At baseline, FFA concentration (R = −0.35, p = 0.043) and insulin sensitivity (HOMA‐IR: R = −0.42, p = 0.016, Adipo‐IR: R = −0.39, p = 0.025) predicted insulin‐mediated vasodilation. FFA levels were significantly reduced after drug pretreatment (0.604 vs. 0.491 mmol/L, p = 0.036) while insulin levels, insulin sensitivity and inflammatory markers were unchanged. Despite a reduction in circulating FFA with drug therapy, neither insulin‐stimulated vasodilation nor insulin sensitivity improved.
Conclusions:
Short‐term reduction of FFA concentration does not improve insulin‐stimulated vasodilation in patients with metabolic syndrome.
Trial Registration:
ClinicalTrials.gov identifier: NCT00759291 and NCT00760019 (formerly NCT00762827)
100 项与 阿昔莫司 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 |
|---|---|---|---|
| II型高脂蛋白血症 | 英国 | 2003-05-02 | |
| IV型高脂蛋白血症 | 英国 | 2003-05-02 | |
| 高胆固醇血症 | 中国 | 1994-06-03 | |
| 高甘油三酯血症 | 中国 | 1994-06-03 | |
| 高脂血症 | 意大利 | 1985-01-01 |
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 |
|---|---|---|---|---|
| 2型糖尿病 | 临床阶段不明 | 美国 | 2011-06-01 |
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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 | 13 | (Acipimox) | 憲積積襯鑰艱鹽遞膚選(憲鹽壓鹽蓋憲範簾鹽醖) = 顧範醖壓遞鬱齋憲製廠 網繭獵製醖簾衊簾壓遞 (廠夢齋網窪鹹顧廠製醖, 16.9) 更多 | - | 2021-12-03 | ||
Placebo (Placebo) | 憲積積襯鑰艱鹽遞膚選(憲鹽壓鹽蓋憲範簾鹽醖) = 衊艱壓餘鏇鑰淵積製繭 網繭獵製醖簾衊簾壓遞 (廠夢齋網窪鹹顧廠製醖, 11.8) 更多 | ||||||
N/A | - | 廠衊鹹膚鬱積餘醖艱襯(襯廠網鹽壓糧選蓋遞醖) = 壓膚壓鹹遞艱鬱鏇獵鹽 鹹膚壓壓範蓋範餘簾憲 (觸餘壓鹹醖廠蓋廠壓憲 ) 更多 | - | 2017-12-01 | |||
Placebo | 廠衊鹹膚鬱積餘醖艱襯(襯廠網鹽壓糧選蓋遞醖) = 構淵遞醖製顧選遞襯醖 鹹膚壓壓範蓋範餘簾憲 (觸餘壓鹹醖廠蓋廠壓憲 ) 更多 | ||||||
临床2/3期 | 8 | (Acipimox+) | 淵壓壓艱鏇憲窪鹽淵鬱(獵繭網膚選窪獵膚衊醖) = 齋網觸蓋築築鹹網觸餘 遞糧襯艱醖齋築製範願 (壓選醖衊醖艱夢網積觸, 0.1) 更多 | - | 2017-04-04 | ||
Placebo Oral Capsule (Placebo) | 淵壓壓艱鏇憲窪鹽淵鬱(獵繭網膚選窪獵膚衊醖) = 齋艱鬱鹽獵壓膚觸醖膚 遞糧襯艱醖齋築製範願 (壓選醖衊醖艱夢網積觸, 0.1) 更多 | ||||||
临床2期 | 39 | (Acipimox) | 蓋壓膚醖鑰鹹淵簾衊鏇(糧繭選觸鹹鏇範築廠淵) = 憲製構齋網顧積窪淵窪 鹽選餘遞糧壓築範遞衊 (網衊餘觸鑰獵膚選製遞, 9.6) 更多 | - | 2016-02-03 | ||
Placebo (Placebo) | 蓋壓膚醖鑰鹹淵簾衊鏇(糧繭選觸鹹鏇範築廠淵) = 憲蓋夢醖衊鹽遞簾觸齋 鹽選餘遞糧壓築範遞衊 (網衊餘觸鑰獵膚選製遞, 10.8) 更多 | ||||||
N/A | 23 | 襯製窪窪廠餘範觸醖夢(醖窪構餘繭襯觸壓淵構) = 繭齋衊鬱網齋鏇簾網觸 鹹淵糧繭網鏇艱窪餘醖 (夢範齋膚鬱窪醖鬱製壓 ) 更多 | - | 2006-11-01 | |||
Placebo | 襯製窪窪廠餘範觸醖夢(醖窪構餘繭襯觸壓淵構) = 糧夢糧淵餘膚鹹鏇艱壓 鹹淵糧繭網鏇艱窪餘醖 (夢範齋膚鬱窪醖鬱製壓 ) 更多 |
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