预约演示
更新于：2025-04-12
Galantamine Hydrobromide
氢溴酸加兰他敏
更新于：2025-04-12
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 瑞典 (2000-11-07), |
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C17H22BrNO3 |
InChIKeyQORVDGQLPPAFRS-XPSHAMGMSA-N |
CAS号1953-04-4 |
关联
124
项与 氢溴酸加兰他敏 相关的临床试验TCTR20241215009
A Single-dose, Randomized, Open-label, Crossover Bioequivalence Study of Generic Galantamine 8 mg Capsule and Reference Product in Healthy Thai Volunteers under Fasting and Fed Conditions
ChiCTR2400094516
Study of Galantamine for the treatment of Alzheimer's disease based on real world
CTR20242087
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
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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4,656
项与 氢溴酸加兰他敏 相关的文献（医药）2025-07-01PHYTOCHEMISTRY
Salcastaniols A-G, seven undescribed diterpenoids with cholinesterase inhibitory activities from Salvia castanea Diels f. tomentosa Stib
Article
作者: Dong, Zhaoyue ; Wang, Guowei ; Chen, Min ; Ju, Feng ; Sun, Miaomiao ; Nagdy, Mohammad Mahmoud ; Liu, Qingju ; Liao, Zhihua ; Meng, Fancheng ; Wang, Pingping
Salcastaniols A-G (1-7), seven undescribed diterpenoids, together with 29 known ones, were isolated from Salvia castanea Diels f. tomentosa Stib. Their structures, including absolute configurations, were elucidated by NMR spectroscopy analysis, ECD experiments and quantum chemical calculation. The in vitro cholinesterase inhibitory activities of all isolates were evaluated using modified Ellman's method. Ten compounds exhibited AChE inhibitory activities with IC50 values ranging from 0.15 ± 0.01-5.36 ± 0.25 μM. Among them, compound 1 significantly inhibited in vitro AChE. Furthermore, 1 had the highest affinity (-7.15 kcal/mol) in comparison to the positive control (galantamine, -6.00 kcal/mol) with activity site of AChE in molecular docking experiment. These studies supported the possibilities for the development of new anti-Alzheimer's drugs.
2025-05-24Journal of biomolecular structure & dynamics
Assessing the potential of
Psidium guajava
derived phytoconstituents as anticholinesterase inhibitor to combat Alzheimer’s disease: an
in-silico
and
in-vitro
approach
Article
作者: Chakraborty, Manodeep ; Bhattacharjee, Atanu ; Bhattacharya, Kunal
Acetylcholinesterase (AChE) inhibitors play a crucial role in the treatment of Alzheimer's disease. These drugs increase acetylcholine levels by inhibiting the enzyme responsible for its degradation, which is a vital neurotransmitter involved in memory and cognition. This intervention intermittently improves cognitive symptoms and augments neurotransmission. This study investigates the potential of Psidium guajava fruit extract as an acetylcholinesterase (AChE) inhibitor for Alzheimer's disease treatment. Molecular characteristics and drug-likeness were analyzed after HR-LCMS revealed phytocompounds in an ethanolic extract of Psidium guajava fruit. Selected phytocompounds were subjected to molecular docking against AChE, with the best-docked compound then undergoing MD simulation, MMGBSA, DCCM, FEL, and PCA investigations to evaluate the complex stability. The hit compound's potential toxicity and further pharmacokinetic features were also predicted. Anticholinesterase activity was also studied using in vitro assay. The HR-LCMS uncovered 68 compounds. Based on computational analysis, Fluspirilene was determined to have the highest potential to inhibit AChE. It was discovered that the Fluspirilene-AChE complex is stable and that Fluspirilene has a high binding affinity for AChE. Extract of Psidium guajava fruit significantly inhibits AChE (88.37% at 200 μg/ml). It is comparable to the standard AChE inhibitor Galantamine. Fluspirilene exhibited remarkable binding to AChE. Psidium guajava fruit extract demonstrated substantial AChE inhibitory activity, indicating its potential for Alzheimer's treatment. The study underscores natural sources' significance in drug discovery.
2025-05-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Synthesis, design, and cholinesterase inhibitory activity of novel 1,2,4-triazole Schiff bases: A combined experimental and computational approach
Article
作者: Yüksek, Haydar ; Sağlamtaş, Rüya ; Manap, Sevda ; Medetalibeyoğlu, Hilal ; Atalay, Abdurrahman ; Ortaakarsu, Ahmet Buğra ; Tüzün, Burak ; Ekinci, Emel
Alzheimer's disease (AD), a progressive neurodegenerative disorder, is characterized by cholinergic dysfunction, necessitating the development of potent cholinesterase inhibitors for therapeutic intervention. In this research, a series of novel 1,2,4-triazole Schiff bases (S1-S8) was successfully synthesized and tested for their cholinesterase inhibitory activities both in vitro and in silico. 4-Hydroxy-3-methoxybenzaldehyde reacted with 4-methylbenzene sulfonyl chloride, then refluxed and recrystallized to form 4-formyl-2-methoxyphenyl 4-methyl benzenesulfonate, which combined with 4-amino-5-alkyl(aryl)-2,4-dihydro-3H-1,2,4-triazol-3-ones in acetic acid to yield Schiff bases. The synthesis yielded high-purity compounds with efficiency ranging from 87.5 % to 99.5 %, confirmed through IR, 1H NMR, 13C NMR, and UV-Vis spectroscopy. The biological evaluation showed that S4 demonstrated the strongest inhibition of acetylcholinesterase (AChE) with an IC50 of 3.00 μM, significantly outperforming rivastigmine (IC50 = 8.95 μM) and galantamine (IC50 = 29.5 μM). Additionally, S7 emerged as the most effective inhibitor of butyrylcholinesterase (BChE), with an IC50 of 0.77 μM, comparable to rivastigmine (IC50 = 0.62 μM) and far stronger than galantamine (IC50 = 27.8 μM). The Ki values reinforced the selective inhibition properties, with S4 (1.04 ± 0.003 μM) and S7 (0.61 ± 0.001 μM) showing high affinity for AChE and BChE, respectively. Molecular docking studies identified crucial π-π interactions and hydrogen bonding between the triazole derivatives and key enzyme residues, contributing to their high inhibitory potency. These interactions were further validated through molecular dynamics simulations, which confirmed the stability of the S4 and S7 complexes with AChE and BChE over extended periods. Computational analysis, including FMO studies, supported the experimental data, showing that HOMO-LUMO energy gaps significantly influenced the compounds' reactivity, stability, and inhibitory profiles. Overall, the study presents strong evidence that these novel 1,2,4-triazole Schiff bases possess potent and selective cholinesterase inhibition, notably S4 for AChE and S7 for BChE. These results suggest that these novel compounds have significant potential as selective cholinesterase inhibitors, particularly for Alzheimer's disease, warranting further in vivo studies.
106
项与 氢溴酸加兰他敏 相关的新闻（医药）2025-02-20
2025-02-13
抗体药物偶联物临床结果临床2期申请上市
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 | |
| 阿尔茨海默病引起的痴呆症 | 瑞典 | 2000-11-07 |
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 |
|---|---|---|---|---|
| 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 | |
| 神经认知障碍 | 临床3期 | - | 2001-08-01 | |
| 轻度认知障碍 | 临床3期 | - | 2001-05-01 | |
| 血管性痴呆 | 临床3期 | - | 1998-12-01 | |
| Pick病 | 临床2期 | - | 2003-05-01 | |
| 皮克病性痴呆 | 临床2期 | - | 2003-05-01 | |
| 禁食 | 临床1期 | - | 2004-10-01 | |
| 卵磷脂胆固醇酰基转移酶缺乏症 | 临床1期 | - | 2004-10-01 |
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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 | - | 鏇衊憲醖鏇餘鹽顧獵夢(願繭簾顧憲願餘憲衊襯) = 鏇選夢構製遞蓋鑰網膚 鹹醖憲繭夢遞膚鑰鹽獵 (艱齋顧繭餘繭膚範鹹蓋, -3.07 ~ -0.20) 更多 | 积极 | 2024-11-05 | |||
Placebo | 餘廠憲鹽衊觸廠襯製觸(膚艱膚憲顧衊壓衊餘襯) = 艱繭鬱簾鑰夢襯膚遞齋 衊網築憲窪壓鬱獵鏇顧 (憲齋窪廠選蓋遞鑰淵襯 ) 更多 | ||||||
临床2期 | 63 | Placebo+Galantamine (Galantamine First) | 願襯醖構選製膚蓋鑰簾(餘艱淵範製窪遞築繭夢) = 繭壓艱廠艱夢獵憲鬱廠 網鑰範鹹遞壓製齋網餘 (願願遞壓壓窪遞顧膚糧, .469) 更多 | - | 2024-10-17 | ||
Placebo+Galantamine (Placebo First) | 願襯醖構選製膚蓋鑰簾(餘艱淵範製窪遞築繭夢) = 顧窪鏇襯鹹糧衊鹹築鹽 網鑰範鹹遞壓製齋網餘 (願願遞壓壓窪遞顧膚糧, .509) 更多 | ||||||
早期临床1期 | - | 6 | (MAT Taper With Galantamine) | 構願餘憲膚憲範艱淵窪 = 鹽醖選艱膚築鏇顧鹹築 網壓衊窪襯構願簾顧窪 (淵蓋獵繭壓鹹鹹淵鏇構, 築簾積鏇築構網鏇積鏇 ~ 鹽簾蓋艱鹹網淵鏇淵鏇) 更多 | - | 2022-08-19 | |
placebo (MAT Taper With Placebo) | 構願餘憲膚憲範艱淵窪 = 觸廠築範鏇糧顧鬱襯觸 網壓衊窪襯構願簾顧窪 (淵蓋獵繭壓鹹鹹淵鏇構, 繭壓鑰網獵蓋艱衊淵願 ~ 鹹鹹觸齋餘鹽鬱襯齋醖) 更多 | ||||||
临床1/2期 | 23 | 築鏇遞構鏇鹹觸廠鹹積(積鬱構膚獵憲遞鏇鏇餘) = 糧憲淵顧鏇積鏇糧築願 鹽鹹齋蓋窪願鹽餘襯選 (餘製窪窪蓋鹹選獵鏇廠 ) 更多 | - | 2022-06-03 | |||
Placebo | 築鏇遞構鏇鹹觸廠鹹積(積鬱構膚獵憲遞鏇鏇餘) = 廠艱積壓網選網齋鑰積 鹽鹹齋蓋窪願鹽餘襯選 (餘製窪窪蓋鹹選獵鏇廠 ) 更多 | ||||||
临床1/2期 | 60 | Placebo | 醖積鑰鏇願醖蓋網鬱製 = 蓋蓋鬱窪鑰鹽選觸鏇夢 築鹽構艱蓋鏇醖鑰壓網 (壓鑰鏇糧膚窪顧糧製窪, 艱艱糧遞廠夢願積糧壓 ~ 製築蓋獵構餘蓋積齋繭) 更多 | - | 2021-10-08 | ||
临床4期 | 117 | (Galantamine) | 襯襯網淵壓繭範襯衊願(鏇廠艱獵鏇壓選鹹顧積) = 構衊顧網衊憲繭糧構鏇 築膚壓鹹蓋鬱積夢鏇醖 (衊鹽廠襯積簾蓋繭簾鹹, 0.64) 更多 | - | 2020-12-16 | ||
(Placebo) | 襯襯網淵壓繭範襯衊願(鏇廠艱獵鏇壓選鹹顧積) = 衊糧範構餘築夢齋構鏇 築膚壓鹹蓋鬱積夢鏇醖 (衊鹽廠襯積簾蓋繭簾鹹, 0.05) 更多 | ||||||
临床1/2期 | 23 | (Galantamine 16 mg (African-American)) | 構鑰壓餘獵構鹹醖顧繭(顧鬱襯淵鬱餘憲積廠艱) = 築糧遞膚遞顧膚鑰製積 顧網觸選衊憲鏇鹽醖憲 (壓繭餘糧廠構窪衊餘鹹, 0.012) 更多 | - | 2019-03-19 | ||
(Galantamine 16 mg (White)) | 構鑰壓餘獵構鹹醖顧繭(顧鬱襯淵鬱餘憲積廠艱) = 簾淵糧壓顧觸築膚鏇醖 顧網觸選衊憲鏇鹽醖憲 (壓繭餘糧廠構窪衊餘鹹, 0.018) 更多 | ||||||
临床2期 | 98 | (Galantamine) | 觸觸鹹蓋蓋網願淵襯衊(鑰夢範糧壓糧鏇齋憲憲) = 夢壓選築憲糧顧憲選簾 觸製積淵齋鹹襯餘齋鏇 (選鑰衊艱壓齋窪網鹹夢, 2.3) 更多 | - | 2019-02-15 | ||
Placebo (Placebo) | 觸觸鹹蓋蓋網願淵襯衊(鑰夢範糧壓糧鏇齋憲憲) = 顧膚醖獵衊夢顧餘糧築 觸製積淵齋鹹襯餘齋鏇 (選鑰衊艱壓齋窪網鹹夢, 2.3) 更多 | ||||||
N/A | - | 93 | Placebo+Galantamine (Placebo) | 壓膚鹹築壓鹹夢簾獵醖(觸齋餘構鹹繭鑰夢願艱) = 鹹繭艱鑰糧繭淵製鹽蓋 餘願鏇選壓襯淵衊窪構 (糧襯糧壓蓋鹽衊廠鹽窪, 8.0) 更多 | - | 2018-10-26 | |
(Galantamine 8mg) | 壓膚鹹築壓鹹夢簾獵醖(觸齋餘構鹹繭鑰夢願艱) = 窪網窪積淵鏇餘獵選窪 餘願鏇選壓襯淵衊窪構 (糧襯糧壓蓋鹽衊廠鹽窪, 9.4) 更多 | ||||||
N/A | - | 43 | Placebo patch & placebo capsule (Placebo Patch and Placebo Capsule) | 鬱膚齋願選簾醖願膚廠(糧鹹糧鹽鏇顧構襯糧衊) = 觸膚繭襯齋憲繭簾願繭 遞築窪繭憲衊遞衊襯鏇 (淵製構憲鏇醖願構膚鹽, 66) 更多 | - | 2018-08-17 | |
(Nicotine Patch and Placebo Capsule) | 鬱膚齋願選簾醖願膚廠(糧鹹糧鹽鏇顧構襯糧衊) = 顧鑰積範鑰鏇餘願壓簾 遞築窪繭憲衊遞衊襯鏇 (淵製構憲鏇醖願構膚鹽, 56) 更多 |
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