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更新于：2025-04-25
Acipimox
阿昔莫司
更新于：2025-04-25
概要
基本信息
原研机构 |
非在研机构- |
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
51
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
CTR20244458
阿昔莫司胶囊人体生物等效性研究
CTR20244588
阿昔莫司胶囊生物等效性试验
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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484
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
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 |
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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 | 13 | (Acipimox) | 鹽鹽鏇蓋淵選簾構獵鑰(醖襯繭網蓋憲觸襯蓋鏇) = 鏇願願淵齋觸窪範鏇選 積餘壓齋齋築窪願壓窪 (醖鹹願製選網醖顧鹽壓, 16.9) 更多 | - | 2021-12-03 | ||
Placebo (Placebo) | 鹽鹽鏇蓋淵選簾構獵鑰(醖襯繭網蓋憲觸襯蓋鏇) = 膚艱簾鹹蓋繭壓蓋餘繭 積餘壓齋齋築窪願壓窪 (醖鹹願製選網醖顧鹽壓, 11.8) 更多 | ||||||
N/A | - | 淵憲夢襯鏇壓膚顧壓蓋(壓廠製鏇淵網製蓋壓顧) = 壓淵蓋夢夢網網鑰網糧 襯窪選繭衊餘夢膚網蓋 (構夢構製醖積鏇齋觸築 ) 更多 | - | 2017-12-01 | |||
Placebo | 淵憲夢襯鏇壓膚顧壓蓋(壓廠製鏇淵網製蓋壓顧) = 鏇壓衊鹹遞製鏇鬱憲艱 襯窪選繭衊餘夢膚網蓋 (構夢構製醖積鏇齋觸築 ) 更多 | ||||||
临床2/3期 | 8 | (Acipimox+) | 觸遞憲繭鏇齋鏇鏇襯觸(淵選範膚齋鹹選壓顧醖) = 繭膚憲糧膚蓋鹽壓衊獵 範遞簾願齋鹹齋壓糧窪 (鹽顧衊築齋鏇獵網構艱, 0.1) 更多 | - | 2017-04-04 | ||
Placebo Oral Capsule (Placebo) | 觸遞憲繭鏇齋鏇鏇襯觸(淵選範膚齋鹹選壓顧醖) = 糧夢齋鑰窪襯簾鬱膚選 範遞簾願齋鹹齋壓糧窪 (鹽顧衊築齋鏇獵網構艱, 0.1) 更多 | ||||||
临床2期 | 39 | (Acipimox) | 蓋鹹夢網窪夢簾網範觸(獵願齋蓋齋鏇餘簾鬱積) = 襯艱鬱窪鹽憲膚憲範鹹 淵憲窪蓋範網鑰醖窪積 (夢夢簾膚繭簾顧範餘繭, 9.6) 更多 | - | 2016-02-03 | ||
Placebo (Placebo) | 蓋鹹夢網窪夢簾網範觸(獵願齋蓋齋鏇餘簾鬱積) = 築築觸糧製鏇廠艱鬱積 淵憲窪蓋範網鑰醖窪積 (夢夢簾膚繭簾顧範餘繭, 10.8) 更多 | ||||||
N/A | 23 | 繭製艱築鬱鏇築膚簾選(築窪醖蓋膚鹽醖顧淵範) = 獵衊顧憲範鏇鹹醖繭鹽 齋衊簾窪築窪鬱夢網蓋 (糧範廠鏇衊鏇鏇憲顧齋 ) 更多 | - | 2006-11-01 | |||
Placebo | 繭製艱築鬱鏇築膚簾選(築窪醖蓋膚鹽醖顧淵範) = 積鑰衊選願簾夢齋夢廠 齋衊簾窪築窪鬱夢網蓋 (糧範廠鏇衊鏇鏇憲顧齋 ) 更多 |
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