更新于：2024-12-15
Isosorbide Mononitrate
单硝酸异山梨酯
更新于：2024-12-15
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1991-12-30), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C6H9NO6 |
InChIKeyYWXYYJSYQOXTPL-SLPGGIOYSA-N |
CAS号16051-77-7 |
关联
108
项与 单硝酸异山梨酯 相关的临床试验Antiplatelet Therapy and Endothelial-stabilizing Agents in Cerebral Small Vessel Diseases
Intravaginal administration of Misoprostol with Isosorbide Mononitrate versus misoprostol alone for cervical ripening in induction of labor in low-risk term pregnancy
Nitric Oxide Donor Isosorbide Mono Nitrate for Cervical Ripening in Induction of Labor
100 项与 单硝酸异山梨酯 相关的临床结果
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100 项与 单硝酸异山梨酯 相关的转化医学
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100 项与 单硝酸异山梨酯 相关的专利（医药）
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1,055
项与 单硝酸异山梨酯 相关的文献（医药）2025-01-01EXPERIMENTAL NEUROLOGY
Combination treatment with cilostazol and isosorbide mononitrate attenuates microemboli-mediated vascular cognitive impairment and improves imaging and plasma biomarkers in diabetic rats
Article
作者: Li, Alice A ; Voltin, Joshua ; He, Lianying ; Edwards, Jazlyn ; Li, Weiguo ; Falangola, Maria Fatima ; Ergul, Adviye ; Karakaya, Eda ; Jamil, Sarah ; Abdelsaid, Kareem ; Nie, Xingju ; Li, Alice A.
Diabetes is a major risk factor for all types of dementia. The underlying reasons are not fully understood, and preventive therapeutic strategies are lacking. Previously we have shown that diabetic but not control rats developed a progressive cognitive decline in a microemboli (ME) model of vascular contributions to cognitive impairment & dementia (VCID). Given the cerebrovascular dysfunction is a mutual pathological change between diabetes and VCID, we hypothesized that the cognitive impairment in this ME model can be prevented by improving the endothelial function in diabetes. Our treatment paradigm was based on the LACI-2 Trial which assessed the efficacy of isosorbide mononitrate (ISMN) and cilostazol (Cil) treatments in small vessel disease progression. Control and diabetic rats were treated with ISMN/Cil or vehicle for 4 weeks, then injected with cholesterol crystal ME and the behavioral outcomes were monitored. Brain microstructure integrity was assessed by diffusion MRI. Plasma biomarkers were assessed using angiogenesis, neurology and amyloid β 42/40 panels recommended by the MarkVCID consortium. Behavioral deficits and the loss of tissue integrity previously observed in untreated diabetic rats were not noted in the treated animals in this study. Treatment improved tissue perfusion but there were no differences in plasma biomarkers. These results suggest that restoration of endothelial function with ISMN/Cil before ME injection prevented the possible deleterious effects of ME in diabetic rats by improving the endothelial integrity and it is a practical preventive and therapeutic strategy for VCID.
2024-12-01LIFE SCIENCES
Organic vs. inorganic nitrates: Metabolic and vascular outcomes in STZ-induced diabetes in mice
Article
作者: Dos Santos, Gustavo Jorge ; Gomes da Silva, Rayanelle Tissiane ; de Almeida, Arthur José Pontes Oliveira ; Fernandes-Costa, Francineide ; de Assis Tafuri, Luciene Simões ; de Medeiros, Isac Almeida ; dos Santos, Gustavo Jorge ; Cruz, Josiane Campos ; Carlstrom, Mattias ; da Silva, Rayanelle Tissiane Gomes
BACKGROUND:
Diabetic animals often display dysregulated nitric oxide (NO) metabolism, contributing to vascular dysfunction. This study evaluates the metabolic and vascular effects of organic nitrate isosorbide mononitrate (ISMN) versus inorganic sodium nitrate (NaNO3) in mice with type 1 diabetes mellitus (T1DM) induced by streptozotocin (STZ).
EXPERIMENTAL APPROACH:
T1DM was induced in male C57Bl6 mice with STZ ip and confirmed by fasting glucose. Mice were treated with ISMN (10 mg·kg-1) or NaNO3 (85 mg·L-1) for 14 days. A combination of in vivo, in vitro, and ex vivo studies assessed cardiometabolic benefits.
RESULTS:
Both nitrates reduced blood and urinary hyperglycemia in T1DM mice, with ISMN exhibiting more significant reductions in blood glucose. ISMN and NaNO3 similarly reduced water and food intake, urinary volume, glucose intolerance, and insulin resistance while increasing insulin and nitrite levels in serum and urine. Both nitrates improved endothelium-independent vascular function and attenuated reactive oxygen species (ROS) while increasing NO levels in the aortic rings of T1DM mice. Furthermore, both nitrates similarly reduced mean arterial pressure in T1DM mice.
CONCLUSION AND IMPLICATIONS:
ISMN and NaNO₃ have demonstrated comparable hypotensive and antioxidant effects, offering metabolic and vascular benefits in STZ-TDM1 mice. The more pronounced reduction in blood glucose with ISMN treatment compared to NaNO₃ is particularly promising. The antihyperglycemic effects of both nitrates were linked to increased serum insulin levels and enhanced insulin sensitivity. These results provide a foundation for future clinical studies to evaluate the potential of ISMN or NaNO3 as antidiabetogenic and antihypertensive adjuvant therapies in diabetic patients.
2024-10-28JACS Au
Poly-Dha Sequences as Pro-polypeptides: An Original Mechanistic Postulate Leads to the Discovery of a Long-Acting Vasodilator KU04212
Article
作者: Bloom, Steven ; Haysom-Rodríguez, Allen Alonso
The construction of polypeptides was revolutionized by Merrifield's solid-phase synthesis more than half a century ago. Herein, we explore a completely different approach to making peptides. We test an original mechanistic postulate wherein a single peptide made entirely of dehydroalanine (Dha) residues can give rise to regio- and stereodefined peptides by iterative conjugate addition of one- or two-electron nucleophiles. Each nucleophile appends a unique amino acid side chain to the peptide backbone. We show that side chain addition is not random. Side chains are added in one of two ways, in an electrophilicity-gated fashion (most cases) or in a substrate-directed manner, depending on the first nucleophile used in the synthesis. One peptide made in this series, KU04212, a first-in-class polyazole peptide, was found to reduce vascular length density (-17%; p < 0.05) and increase vessel diameter (124%; p < 0.001) in healthy day 6 chick embryos at 24 h post-single dose. It also rescued 75% of the embryos administered a 32-fold lethal dose of ischemia-inducing CoCl2 after 12 h and 12.5% of the embryos after 24 h. In comparison to three mechanistically distinct vasodilators, e.g., isosorbide mononitrate, amlodipine besylate, and prazosin, only KU04212 showed long-acting effects in vivo, making it an enticing lead for the treatment of ischemic disorders.
100 项与 单硝酸异山梨酯 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心脏衰竭 | 中国 | 1993-01-01 | |
| 心绞痛 | 美国 | 1991-12-30 |
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 |
|---|---|---|---|---|
| 稳定型心绞痛 | 临床3期 | 巴西 | 2014-07-01 | |
| 心肌梗塞 | 临床1期 | 中国 | - | 2013-10-10 |
| 血管痉挛 | 临床1期 | 中国 | - | 2013-10-10 |
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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 | 150 | 淵網壓窪餘網願醖壓壓(衊廠憲遞蓋窪顧構獵襯) = 築遞積繭齋鬱獵構鏇餘 觸淵鑰觸顧鑰廠鏇願鏇 (壓窪鹹顧範鏇憲鹹願餘 ) 更多 | 不佳 | 2024-08-30 | |||
Isosorbide mononitrate 50 mg daily | 淵網壓窪餘網願醖壓壓(衊廠憲遞蓋窪顧構獵襯) = 夢鹽淵製壓遞積鹽網膚 觸淵鑰觸顧鑰廠鏇願鏇 (壓窪鹹顧範鏇憲鹹願餘 ) 更多 | ||||||
临床2期 | 9 | (Isosorbide Mononitrate) | 廠選膚衊鬱膚艱淵壓鏇(範構餘廠淵艱夢衊鏇廠) = 簾積廠顧淵艱願齋鹽獵 窪壓窪鑰淵糧鹹壓糧淵 (蓋齋憲壓顧網顧選壓艱, 簾艱衊餘選鹹鏇遞齋鏇 ~ 艱醖齋鑰醖選鑰製選鏇) 更多 | - | 2022-08-03 | ||
Placebo oral tablet (Placebo) | 廠選膚衊鬱膚艱淵壓鏇(範構餘廠淵艱夢衊鏇廠) = 製衊鹹壓遞膚鏇製鏇顧 窪壓窪鑰淵糧鹹壓糧淵 (蓋齋憲壓顧網顧選壓艱, 簾醖醖淵構鹽選顧鬱鑰 ~ 壓遞壓遞醖襯選網築壓) 更多 | ||||||
临床2期 | 8 | (ISMN Only) | 鏇簾壓繭蓋觸選範鹽觸(範繭艱鹹遞醖糧餘淵鹽) = 觸糧襯構衊膚窪鹽淵積 憲觸鬱憲鹽網齋蓋網醖 (蓋廠選夢觸觸獵製鏇選, 築築醖製遞夢鹽選淵襯 ~ 淵衊觸簾鏇鏇壓窪範醖) 更多 | - | 2020-08-13 | ||
Vitamin C+ISMN (ISMN AND Vitamin C) | 鏇簾壓繭蓋觸選範鹽觸(範繭艱鹹遞醖糧餘淵鹽) = 艱鹽遞顧鑰糧膚襯淵獵 憲觸鬱憲鹽網齋蓋網醖 (蓋廠選夢觸觸獵製鏇選, 鏇餘鬱艱餘願鏇糧醖製 ~ 艱鹹選範窪餘遞顧選選) 更多 | ||||||
临床2期 | 110 | Placebo+Isosorbide Mononitrate (Isosorbide Mononitrate Crossover to Placebo) | 廠廠膚獵繭窪蓋夢範顧(膚簾簾夢網築艱壓襯壓) = 網齋淵選襯願齋淵鹹築 觸願鏇簾觸獵艱積積艱 (淵醖製衊範鑰蓋範夢夢, 築憲鑰廠簾網蓋齋鑰構 ~ 膚襯鹽遞繭壓鑰遞繭窪) 更多 | - | 2016-11-28 | ||
Placebo+Isosorbide Mononitrate (Placebo Crossover to Isosorbide Mononitrate) | 廠廠膚獵繭窪蓋夢範顧(膚簾簾夢網築艱壓襯壓) = 鬱襯願襯網鑰醖衊獵鹽 觸願鏇簾觸獵艱積積艱 (淵醖製衊範鑰蓋範夢夢, 襯觸鏇膚獵築鹽觸觸齋 ~ 蓋膚積壓積築鬱製衊窪) 更多 | ||||||
N/A | 60 | ISMN 20 mg retarded release | 廠憲衊齋窪築淵蓋蓋蓋(廠齋觸壓膚夢鏇獵夢襯) = 鬱壓憲餘廠製襯鑰齋遞 鑰鬱構構顧淵範網遞顧 (鏇淵艱願襯構遞夢艱廠 ) | 不佳 | 2013-11-01 | ||
Placebo | 廠憲衊齋窪築淵蓋蓋蓋(廠齋觸壓膚夢鏇獵夢襯) = 簾鑰糧構鏇選衊蓋範襯 鑰鬱構構顧淵範網遞顧 (鏇淵艱願襯構遞夢艱廠 ) | ||||||
N/A | - | - | Isosorbide mononitrate (IMN) | 鑰膚壓鹽選顧範襯範壓(繭觸遞齋選鹽觸襯積膚): mean difference = -1.6 (95% CI, -5.1 ~ 1.9), P-Value = 0.37 | 积极 | 2009-08-01 | |
Placebo |
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