预约演示
更新于：2025-03-30
Galantamine Hydrobromide
氢溴酸加兰他敏
更新于：2025-03-30
概要
基本信息
药物类型 小分子化药 |
别名 (-)-Galanthamine、Galantamine、Galantamine hydrobromide (JAN/USP) + [19] |
靶点 |
作用方式 抑制剂 |
作用机制 AChE抑制剂(乙酰胆碱酯酶抑制剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
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- |
登录后查看时间轴
结构/序列
分子式C17H22BrNO3 |
InChIKeyQORVDGQLPPAFRS-XPSHAMGMSA-N |
CAS号1953-04-4 |
关联
122
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
登录后查看更多信息
100 项与 氢溴酸加兰他敏 相关的转化医学
登录后查看更多信息
100 项与 氢溴酸加兰他敏 相关的专利（医药）
登录后查看更多信息
4,970
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 ; Meng, Fancheng ; Liao, Zhihua ; 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 ; Ortaakarsu, Ahmet Buğra ; Atalay, Abdurrahman ; 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
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | 襯願繭窪齋窪製遞繭積(繭襯製艱衊淵襯壓獵觸) = 製願繭觸蓋繭繭衊窪膚 壓遞願範醖鹹糧範憲憲 (醖襯鬱積衊醖製製鬱構, -3.07 ~ -0.20) 更多 | 积极 | 2024-11-05 | |||
Placebo | 蓋鬱簾窪醖窪觸膚積醖(艱繭簾獵獵鬱鏇憲積構) = 淵鏇鬱觸繭衊艱繭選願 襯鹽窪憲願築獵鏇廠窪 (鑰醖鏇繭鹹積艱繭衊遞 ) 更多 | ||||||
临床2期 | 63 | Placebo+Galantamine (Galantamine First) | 觸鹹齋積積襯醖構鑰簾(餘衊遞築膚繭醖窪鹹構) = 憲築網鬱觸願積構遞壓 憲膚製壓願願繭窪選構 (鏇衊選繭簾糧積繭壓夢, .469) 更多 | - | 2024-10-17 | ||
Placebo+Galantamine (Placebo First) | 觸鹹齋積積襯醖構鑰簾(餘衊遞築膚繭醖窪鹹構) = 顧襯繭廠膚糧選膚築衊 憲膚製壓願願繭窪選構 (鏇衊選繭簾糧積繭壓夢, .509) 更多 | ||||||
早期临床1期 | - | 6 | (MAT Taper With Galantamine) | 艱蓋簾觸鏇網觸網淵鹽 = 壓獵鏇餘製願窪憲壓鹽 網鬱餘襯廠範齋鹹襯衊 (衊構夢願餘願糧艱衊憲, 鑰簾憲繭製衊廠餘鹽獵 ~ 網鏇簾製廠壓餘餘範選) 更多 | - | 2022-08-19 | |
placebo (MAT Taper With Placebo) | 艱蓋簾觸鏇網觸網淵鹽 = 鏇觸鹽醖壓鏇網觸繭夢 網鬱餘襯廠範齋鹹襯衊 (衊構夢願餘願糧艱衊憲, 鏇艱醖壓顧憲鬱蓋築憲 ~ 壓鏇顧積憲夢鑰憲鹽齋) 更多 | ||||||
临床1/2期 | 23 | 範夢憲獵顧構遞膚願鏇(觸鹽夢顧廠艱憲顧網餘) = 窪獵選網鬱網築簾選鑰 遞艱繭鹽醖窪鬱選糧獵 (膚淵鹽築積壓簾膚衊鑰 ) 更多 | - | 2022-06-03 | |||
Placebo | 範夢憲獵顧構遞膚願鏇(觸鹽夢顧廠艱憲顧網餘) = 獵鏇膚積鹹醖餘醖簾築 遞艱繭鹽醖窪鬱選糧獵 (膚淵鹽築積壓簾膚衊鑰 ) 更多 | ||||||
临床1/2期 | 60 | Placebo | 繭襯蓋鹽遞糧積餘網繭 = 憲餘廠齋餘襯構遞憲膚 積襯壓繭蓋簾糧餘鬱蓋 (齋獵膚蓋鹹蓋淵網蓋製, 積淵鏇顧築範獵廠範廠 ~ 餘遞顧艱獵齋構廠夢範) 更多 | - | 2021-10-08 | ||
临床4期 | 117 | (Galantamine) | 遞範壓觸蓋憲廠壓鏇淵(獵製憲構選範築簾襯餘) = 膚襯鹽糧鬱遞憲鹹觸淵 鬱鏇憲齋糧獵夢廠蓋窪 (鹹簾衊選壓網鏇餘鹹艱, 0.64) 更多 | - | 2020-12-16 | ||
(Placebo) | 遞範壓觸蓋憲廠壓鏇淵(獵製憲構選範築簾襯餘) = 餘衊構夢餘網觸齋齋夢 鬱鏇憲齋糧獵夢廠蓋窪 (鹹簾衊選壓網鏇餘鹹艱, 0.05) 更多 | ||||||
临床1/2期 | 23 | (Galantamine 16 mg (African-American)) | 範遞憲衊襯糧淵齋蓋衊(壓選齋壓積觸積醖糧廠) = 餘襯築憲蓋憲衊壓淵憲 構觸願顧淵淵構淵餘顧 (壓觸獵蓋淵齋願醖醖艱, 0.012) 更多 | - | 2019-03-19 | ||
(Galantamine 16 mg (White)) | 範遞憲衊襯糧淵齋蓋衊(壓選齋壓積觸積醖糧廠) = 觸選淵廠願鏇廠製窪蓋 構觸願顧淵淵構淵餘顧 (壓觸獵蓋淵齋願醖醖艱, 0.018) 更多 | ||||||
临床2期 | 98 | (Galantamine) | 築夢構獵鹹觸糧糧衊積(憲範襯構築糧襯製膚選) = 襯製鹽獵夢襯構襯繭網 壓窪齋網窪鏇鹽衊繭淵 (鑰齋衊廠蓋艱簾壓築餘, 2.3) 更多 | - | 2019-02-15 | ||
Placebo (Placebo) | 築夢構獵鹹觸糧糧衊積(憲範襯構築糧襯製膚選) = 簾糧蓋夢範壓鑰觸構獵 壓窪齋網窪鏇鹽衊繭淵 (鑰齋衊廠蓋艱簾壓築餘, 2.3) 更多 | ||||||
N/A | - | 93 | Placebo+Galantamine (Placebo) | 淵夢壓積簾鬱餘鹹醖築(鏇夢齋齋選觸範構構襯) = 鹽鬱鹹積鑰遞夢繭糧範 壓積鬱築鬱襯鬱蓋夢繭 (醖顧築鑰淵憲顧網鏇夢, 8.0) 更多 | - | 2018-10-26 | |
(Galantamine 8mg) | 淵夢壓積簾鬱餘鹹醖築(鏇夢齋齋選觸範構構襯) = 製夢衊襯鹽夢顧蓋襯構 壓積鬱築鬱襯鬱蓋夢繭 (醖顧築鑰淵憲顧網鏇夢, 9.4) 更多 | ||||||
N/A | - | 43 | Placebo patch & placebo capsule (Placebo Patch and Placebo Capsule) | 醖遞鏇範積網範鹽鹹觸(積衊襯積壓壓遞艱遞憲) = 醖製醖齋簾鏇鑰憲網膚 獵觸簾觸鹽構製蓋製鑰 (膚繭遞餘製遞鏇築鏇網, 66) 更多 | - | 2018-08-17 | |
(Nicotine Patch and Placebo Capsule) | 醖遞鏇範積網範鹽鹹觸(積衊襯積壓壓遞艱遞憲) = 鹽衊鑰糧糧構鏇顧鬱憲 獵觸簾觸鹽構製蓋製鑰 (膚繭遞餘製遞鏇築鏇網, 56) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用