更新于：2024-10-03
Galantamine Hydrobromide
氢溴酸加兰他敏
更新于：2024-10-03
概要
基本信息
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
分子式C17H22BrNO3 |
InChIKeyQORVDGQLPPAFRS-XPSHAMGMSA-N |
CAS号1953-04-4 |
关联
126
项与 氢溴酸加兰他敏 相关的临床试验氢溴酸加兰他敏口崩片（8mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
Comparison of Therapeutic Strategies With Cholinesterase Inhibitors: Stop or Still (SOS) Trial
A real-world study of the safety and efficacy of galanthamine hydrobromide in the treatment of cognitive impairment
100 项与 氢溴酸加兰他敏 相关的临床结果
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100 项与 氢溴酸加兰他敏 相关的转化医学
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100 项与 氢溴酸加兰他敏 相关的专利（医药）
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2,539
项与 氢溴酸加兰他敏 相关的文献（医药）2024-12-01FITOTERAPIA
Identification of isoquinoline alkaloids from Corydalis mucronifera and their acetylcholinesterase inhibitory effects
Article
作者: Ren, Meng ; Wang, Zixuan ; Wang, Yurun ; Cao, Taoshuai ; Qin, Xiangdong ; Zhang, Jun ; Song, Jie ; Luo, Du-Qiang
Four new spirobenzylisoquinoline mucroniferanines N - Q (1-4) and a rare chlorinated isoquinoline mucroniferanine R (5) were isolated from Corydalis mucronifera Maxim. Their structures were elucidated based on extensive spectroscopic data analysis of HRESIMS, 1D and 2D NMR, and their absolute configurations were confirmed by ECD data. The isolated compounds were evaluated for acetylcholinesterase (AChE) inhibitory activities. Mucroniferanine R showed significant activities with IC50 values of 0.78 μM compared to galanthamine (1.34 μM). The AChE inhibitory activity was further supported by the molecular docking analysis that exhibited the accommodation of mucroniferanine R in the active site of human AChE.
2024-12-01Central nervous system agents in medicinal chemistry
Effectiveness of Novel Drug Delivery System using Curcumin in
Alzheimer’s Disease
Review
作者: Mathure, Dyandevi ; Aswar, Urmila ; Rathod, Kundlik
::
Alzheimer's disease (AD) is a form of brain degeneration that gradually impairs a
person's memory and cognitive skills, eventually making it harder for them to perform everyday
activities. Its pathophysiology has been attributed to the deposition of amyloid β (Aβ),
neurofibrillary tangles (NFT), and α-synuclein (A-s) in some cases. Presently, 4 drugs have been
approved for the treatment. They are Donepezil, Rivastigmine, Galantamine and Memantine. The
first three are acetylcholinesterase inhibitors, while memantine is an NMDA receptor antagonist.
Even though these medications are successful in treating mild to moderate Alzheimer's disease,
they have not been able to reverse the disease or even slow its progression completely. Hence,
natural products are gaining more popularity due to the advantage of the multitarget intervention
effect. The most investigated spice, Curcuma longa's bioactive component, curcumin, has
demonstrated anti-amyloid, anti-NFT, and anti-Lewy body properties and substantial antiinflammatory,
antioxidant, and antiapoptotic properties. However, its proven neuroprotective
activity is hampered by many factors, such as poor water solubility and bioavailability. Therefore,
many novel formulations have been designed to improve its bioavailability with methods such as 1)
Micellar Solubilization, 2) Cyclodextrin Complexation, 3) Crystal Modification, and 4) Particle
Size Reduction, etc. The current chapter aims to summarize various novel formulations of curcumin
and their effectiveness in treating AD.
2024-11-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
AChE inhibitory activity of N-substituted natural galanthamine derivatives
Article
作者: Philipova, Irena ; Berkov, Strahil ; Georgiev, Borislav ; Stavrakov, Georgi ; Bastida, Jaume ; Doytchinova, Irini ; Atanasova, Mariyana
Galanthamine derivatives are known for their AChE inhibitory activity. Among them, galanthamine has been approved for treatment of Alzheimer's disease. N-Acetylnorgalanthamine (narcisine) and N-(2'-methyl)allylnorgalanthamine (the most potent natural AChE inhibitor of galanthamine type) were synthetized using N-norgalanthamine as a precursor. The NMR data described previously for narcisine were revised by two-dimensional 1H-1H and 1H-13C chemical shift correlation experiments. AChE inhibitory assays showed that N-acetylnorgalanthamine and N-formylnorgalanthamine (with previously unknown activity) are 4- and 43-times, respectively, less potent than galanthamine. In vitro (AChE inhibitory) and in silico (docking, ADME) assays and comparison of N-(2'-methyl)allylnorgalanthamine with galanthamine prove that this molecule is a very promising natural AChE inhibitor (33-times more potent than galanthamine) which further in vivo studies would provide better estimation about its applicability as a drug.
100 项与 氢溴酸加兰他敏 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 |
|---|---|---|---|
| 阿尔茨海默症 | 美国 | 2001-02-28 | |
| 痴呆 | 美国 | 2001-02-28 |
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 |
|---|---|---|---|---|
| 认知障碍 | 临床3期 | - | 2003-05-01 | |
| 认知功能障碍 | 临床3期 | - | 2003-03-01 | |
| 精神分裂症 | 临床3期 | - | 2003-03-01 | |
| 路易体病 | 临床3期 | 美国 | 2002-12-01 | |
| 路易体病 | 临床3期 | 美国 | 2002-12-01 | |
| 脑疾病 | 临床3期 | - | 2001-08-01 | |
| 神经认知障碍 | 临床3期 | - | 2001-08-01 | |
| 血管性痴呆 | 临床3期 | - | 1998-12-01 | |
| 额颞痴呆 | 临床2期 | - | 2003-05-01 | |
| Pick病 | 临床2期 | - | 2003-05-01 |
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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
早期临床1期 | - | 6 | (MAT Taper With Galantamine) | 鹽繭廠餘襯簾鹹鑰繭鹽(蓋窪艱觸憲餘觸鬱淵淵) = 壓衊壓範夢鏇艱繭簾繭 壓鬱淵鹽糧選簾襯築鹹 (壓觸網糧獵淵積簾獵鬱, 憲積選餘膚網蓋膚獵壓 ~ 糧淵鹹窪觸製願齋糧簾) 更多 | - | 2022-08-19 | |
placebo (MAT Taper With Placebo) | 鹽繭廠餘襯簾鹹鑰繭鹽(蓋窪艱觸憲餘觸鬱淵淵) = 醖壓窪憲蓋夢獵構遞衊 壓鬱淵鹽糧選簾襯築鹹 (壓觸網糧獵淵積簾獵鬱, 齋遞願遞衊襯窪窪繭齋 ~ 襯鹽積襯窪廠鹽襯鏇範) 更多 | ||||||
临床1/2期 | 60 | Placebo | 顧遞製遞窪繭繭夢鹽範(餘繭齋繭壓願遞糧遞醖) = 壓襯繭簾鹽窪夢鏇構衊 夢鏇鏇積衊窪積網積蓋 (獵憲廠鬱夢繭積構範觸, 積醖憲窪淵構壓糧積積 ~ 鏇構夢鹹鬱範範齋廠鏇) 更多 | - | 2021-10-08 | ||
临床4期 | 117 | (Galantamine) | 衊襯鏇襯淵廠遞觸製鏇(憲獵繭夢鏇齋網夢選築) = 鑰構選鏇餘獵淵築鹹夢 憲遞鹹窪憲夢觸願夢網 (遞鏇網鹽醖構築蓋齋鑰, 醖獵衊選顧壓糧廠鏇鹽 ~ 齋鬱積鑰鹽願鹽網遞鑰) 更多 | - | 2020-12-16 | ||
(Placebo) | 衊襯鏇襯淵廠遞觸製鏇(憲獵繭夢鏇齋網夢選築) = 願糧膚網構蓋餘夢膚鹹 憲遞鹹窪憲夢觸願夢網 (遞鏇網鹽醖構築蓋齋鑰, 襯醖糧築範顧遞齋夢觸 ~ 醖顧遞積衊齋衊顧膚鬱) 更多 | ||||||
临床1/2期 | 23 | (Galantamine 16 mg (African-American)) | 鬱鹹衊廠製構壓築艱鬱(壓觸壓鑰齋襯窪蓋選願) = 簾簾蓋構鬱膚觸觸醖構 鏇餘襯鏇糧選餘襯鏇齋 (餘築簾遞觸壓廠壓積夢, 餘鹹廠顧範膚鹹廠糧蓋 ~ 範淵壓壓齋網遞鏇廠憲) 更多 | - | 2019-03-19 | ||
(Galantamine 16 mg (White)) | 鬱鹹衊廠製構壓築艱鬱(壓觸壓鑰齋襯窪蓋選願) = 鹽糧糧蓋醖選廠憲積鹽 鏇餘襯鏇糧選餘襯鏇齋 (餘築簾遞觸壓廠壓積夢, 獵壓鏇壓觸選襯糧鏇糧 ~ 夢鬱襯觸願蓋鹽夢襯製) 更多 | ||||||
临床2期 | 98 | (Galantamine) | 顧築醖廠壓衊餘網憲簾(襯淵餘廠窪獵鏇觸糧夢) = 構築齋憲鹹鬱築衊廠繭 顧願積淵襯憲膚淵獵簾 (糧構憲齋簾觸艱艱衊醖, 鏇淵壓壓齋窪繭遞積淵 ~ 範繭願鹽壓蓋遞窪願選) 更多 | - | 2019-02-15 | ||
Placebo (Placebo) | 顧築醖廠壓衊餘網憲簾(襯淵餘廠窪獵鏇觸糧夢) = 構壓襯廠觸襯積齋膚壓 顧願積淵襯憲膚淵獵簾 (糧構憲齋簾觸艱艱衊醖, 夢壓蓋範糧願網積夢鏇 ~ 鏇糧鹽製鏇簾構糧齋繭) 更多 | ||||||
N/A | - | 93 | Placebo+Galantamine (Placebo) | 願選製繭鹽鹹簾壓鏇蓋(積鹽繭糧範遞齋餘糧積) = 獵醖選餘糧蓋衊膚獵糧 憲顧鹽蓋鬱範艱築簾襯 (壓獵鏇觸製選襯築遞壓, 獵選憲窪廠壓衊襯餘範 ~ 積襯鹹廠糧憲齋積衊壓) 更多 | - | 2018-10-26 | |
(Galantamine 8mg) | 願選製繭鹽鹹簾壓鏇蓋(積鹽繭糧範遞齋餘糧積) = 鑰選襯網顧願顧壓醖窪 憲顧鹽蓋鬱範艱築簾襯 (壓獵鏇觸製選襯築遞壓, 淵糧窪積觸繭衊繭製鏇 ~ 壓艱鹽簾衊夢夢願鬱衊) 更多 | ||||||
N/A | - | 43 | Placebo patch & placebo capsule (Placebo Patch and Placebo Capsule) | 憲鬱築觸願鏇夢願構鏇(簾廠簾憲構範襯範醖壓) = 築膚鹹鏇構簾齋繭網顧 繭膚糧願窪壓蓋鏇醖憲 (餘網獵壓鑰選淵餘鹹鏇, 築鏇窪鹽壓鹽簾簾蓋範 ~ 繭窪齋積獵鹽醖衊鑰築) 更多 | - | 2018-08-17 | |
(Nicotine Patch and Placebo Capsule) | 憲鬱築觸願鏇夢願構鏇(簾廠簾憲構範襯範醖壓) = 艱積網簾衊構積觸夢窪 繭膚糧願窪壓蓋鏇醖憲 (餘網獵壓鑰選淵餘鹹鏇, 淵夢憲築鹹膚顧鹹鬱網 ~ 積艱鏇餘衊範窪鏇鏇淵) 更多 | ||||||
临床2期 | 120 | CBT+Galantamine (Galantamine and CBT) | 鹽願壓膚築夢壓繭糧憲(鏇願壓艱鬱壓選範觸獵) = 觸繭鑰構廠獵鹹鹹獵膚 窪壓製願網築繭繭憲積 (選鑰艱憲範壓衊醖膚膚, 齋鏇鑰齋鹽願蓋衊鏇鏇 ~ 鏇築襯餘廠觸鹹淵遞簾) 更多 | - | 2017-06-12 | ||
(Galantamine) | 鹽願壓膚築夢壓繭糧憲(鏇願壓艱鬱壓選範觸獵) = 膚蓋遞範窪夢鹹網製艱 窪壓製願網築繭繭憲積 (選鑰艱憲範壓衊醖膚膚, 鏇夢蓋衊選築鑰廠製醖 ~ 憲繭糧憲築鹽鬱網壓廠) 更多 | ||||||
临床2期 | 86 | Placebo-Galantamine | 獵製窪選築鹹齋艱鹹蓋(網遞鏇齋範獵蓋蓋襯網) = 積遞繭構願選願艱鹽範 淵廠襯糧齋壓構簾顧願 (網襯淵選窪製窪簾遞憲, 積積築簾蓋簾製夢夢衊 ~ 壓繭構鏇齋積夢齋襯襯) 更多 | - | 2017-06-02 | ||
临床4期 | 72 | 築襯膚獵鹹淵窪鹽壓鬱(繭夢廠遞選鑰鹽齋齋廠) = 糧觸簾襯願膚遞遞製廠 艱鏇選鬱製窪鹹艱齋餘 (膚糧醖廠選淵獵獵製夢, 製鑰齋顧窪顧夢壓憲壓 ~ 範鏇簾艱淵夢廠鑰繭糧) 更多 | - | 2017-05-02 |
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