预约演示
更新于：2025-04-28
Huperzine A
石杉碱甲
更新于：2025-04-28
概要
基本信息
药物类型 小分子化药 |
别名 HupA oral、Qian-ceng-ta、BIS-001 + [6] |
作用方式 抑制剂、拮抗剂 |
作用机制 AChE抑制剂(乙酰胆碱酯酶抑制剂)、NMDA receptor拮抗剂(谷氨酸[NMDA]受体复合体拮抗剂) |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (1994-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、罕见儿科疾病 (美国) |
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结构/序列
分子式C15H18N2O |
InChIKeyZRJBHWIHUMBLCN-YQEJDHNASA-N |
CAS号102518-79-6 |
关联
36
项与 石杉碱甲 相关的临床试验ChiCTR2400092753
A randomized, controlled, double-blind, single-center study of huperzine A injection in improving cognitive dysfunction after brain injury
NCT06798896
RENAISSANCE 2: a Double-Blind, Randomized, Placebo-Controlled, Multicenter, Parallel-Group Study to Evaluate the Efficacy, Safety, and Tolerability of SPN-817 in Adults with Focal Onset Seizures
NCT06570655
The Study of Pharmacokinetics and Pharmacodynamics of Huperzine a Injection in Healthy Chinese Subjects
100 项与 石杉碱甲 相关的临床结果
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100 项与 石杉碱甲 相关的转化医学
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100 项与 石杉碱甲 相关的专利（医药）
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1,473
项与 石杉碱甲 相关的文献（医药）2025-05-15RAPID COMMUNICATIONS IN MASS SPECTROMETRY
Improved Protective Effects and Pharmacokinetics of Huperzine A Derivative H14 in Soman Poisoning: A Comparative Study With Huperzine A in Rats
Article
作者: Zong, Xingxing ; Wei, Jingchen ; Zhang, Yi ; Liu, Dongxin ; Li, Liqin ; Yang, Guixiang ; Cui, Yalan ; Jin, Qian ; Chen, Xuejun ; Wang, Chen
ABSTRACT:
Rationale:
N‐[2‐Hydroxy‐3,5‐dimethylbenzilidene]‐Hup A (H14) is a derivative of huperzine A (Hup A) that demonstrates superior protective effects against soman (GD) compared to Hup A. This study aims to evaluate the protective efficacy of H14 pretreatment against GD in rats and to provide an analytical framework for the pharmacokinetic evaluation of H14 in experimental animals.
Methods:
The study employed protective ratios (PR) as an evaluation criterion to assess the efficacy of H14 and Hup A in preventing GD in vivo. Liquid–liquid extraction techniques were utilized to extract H14 and its metabolite, Hup A, from plasma. The extracted plasma samples were then analyzed using an ultra‐high‐performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) method for the simultaneous quantification of H14 and Hup A.
Results:
The PR values for the 6‐ and 12‐h Hup A groups were 1.26 and 1.08, respectively. In contrast, the 6, 12, and 24‐h H14 groups demonstrated PR values of 2.81, 1.98, and 1.18, respectively, indicating extended protective capabilities compared to Hup A. All validation parameters for the UHPLC–MS/MS method, including linearity, specificity, precision, accuracy, matrix effect, and stability, met the acceptance criteria established by FDA guidelines. The pharmacokinetic analysis indicates that H14, after conversion to Hup A in vivo, significantly extends the duration of Hup A concentrations in the body, leading to more effective prevention of GD poisoning compared to Hup A alone.
Conclusions:
H14 demonstrates superior efficacy in preventing GD poisoning compared to Hup A. Furthermore, this analytical approach offers a reliable and efficient method for the pharmacokinetic evaluation of H14 in experimental animals.
2025-05-01NEUROSCIENCE
Reevaluating Alzheimer’s disease treatment: Can phytochemicals bridge the therapeutic Gap?
Review
作者: Mehta, Dinesh Kumar ; Das, Rina ; Roy, Kishor Kumar
Alzheimer's disease (AD) is a growing neurological disorder giving impact cognition and memory, posing a global health challenge with over 55 million individuals affected. It is the 7th foremost cause of dying worldwide, and its pervasiveness is expected to twofold in each five years, reaching 115 million by 2050. AD is characterized by neurofibrillary tangles, senile plaques, and oxidative stress, leading to synaptic failure and cognitive decline. Currently, there is no cure, and available FDA-approved drugs provide only symptomatic relief. The disease progresses through five phases- mild cognitive impairment (MCI), very severe, severe, moderate and mild AD. Research on AD focuses on various neurodegenerative pathways, including inflammation, oxidative stress, genetic factors, environmental variables, and amyloid-beta accumulation. Existing FDA-accepted drugs, like rivastigmine, memantine, galantamine, and donepezil, primarily address early symptoms but have limitations, including side effects and high costs. In this context, phytochemicals from plants, such as resveratrol, huperzine, quercetin, galantamine, and rosmarinic acid, show promise as potential treatments for AD and overcome the challenges and limitation of conventional treatment. These natural substances are being investigated for their ability to lower the risk of AD safely. However, there is a lack of comprehensive knowledge about their application, necessitating further research and clinical trials to explore their potential benefits and limitations. This review serves as an essential reference for advancing future studies on Alzheimer's disease. By thoroughly analyzing neurodegenerative pathways, addressing drug limitations, and highlighting the potential of phytochemicals, we establish a strong foundation for developing innovative therapeutic strategies. Closing the knowledge gap related to the use of phytochemicals in Alzheimer's management is not just important; it is critical for creating novel and more effective treatments for this challenging neurological condition.
2025-05-01JOURNAL OF MOLECULAR STRUCTURE
Design, synthesis, molecular docking, DFT analysis, dynamics simulation and cytotoxicity evaluation of coumarin derivatives as acetylcholinesterase (AChE) inhibitors against alzheimer's disease
作者: Singh, Vishal K. ; Rai, Shivangi ; Ahmad, Iqrar ; Singh, Ramendra K. ; Agrawal, Mohit
A new series of coumarin carboxamide derivatives has been synthesized as probable acetylcholinesterase (AChE) inhibitors against alzheimer′s disease.The physicochem. parameters, drug-like properties of all compounds were assessed followed by mol. docking and mol. dynamics simulation (MDS) targeting the active site of AChE (PDB ID: 1EVE).The unique chem. structure of coumarin derivatives allows them to form strong hydrogen bonds, π-π interactions, or hydrophobic interactions, which disrupt AChE′s normal function and prevent the breakdown of acetylcholine.The compounds formed hydrogen bonds with amino acids residues Phe288(2.13 Å), Tyr70(2.02 Å), Tyr121(2.30 Å), Asp72(1.93 Å), Lys413(1.97 Å), Gln69(2.16 Å), Gln526(2.41 Å), and Arg289(1.83 Å).The higher binding affinities, especially compounds 3 and 10, with binding energies of -8.71 and -8.52 kcal/mol and predicted EC50 values of 1.09 x 10-7 and 9.12 x 10-8 resp., which were comparable to the reference drugs.Several parameters like RMSD, RMSF and RGyr of mol. dynamics simulation (MDS) were found satisfactory for the complexes formed by compounds 3 and 10 with the target protein and it showcased robust stability over 100 ns duration.The cytotoxicity screening also revealed that compounds 3 and 10 exhibited less toxicity against HEK293 cell lines.The higher stability of complexes formed by compounds 3 and 10 with AChE, lower predicted EC50 and cytotoxicity clearly endorsed that compounds 3 and 10 might act as potential inhibitors of AChE and can be taken forward to generate new potential candidates.
100 项与 石杉碱甲 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 | 中国 | 1994-01-01 |
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 |
|---|---|---|---|---|
| 耐药性癫痫 | 临床2期 | 澳大利亚 | 2023-02-07 | |
| 癫痫发作 | 临床2期 | 澳大利亚 | 2023-02-07 | |
| 癫痫部分性发作 | 临床2期 | 澳大利亚 | 2018-04-10 | |
| 创伤性脑损伤 | 临床2期 | 美国 | 2013-12-01 | |
| 认知功能障碍 | 临床2期 | 美国 | 2013-12-01 | |
| 癫痫 | 临床1期 | 美国 | 2022-01-30 | |
| 学习障碍 | 临床1期 | - | 2020-07-02 | |
| 学习障碍 | 临床1期 | - | 2020-07-02 | |
| 记忆障碍 | 临床1期 | - | 2020-07-02 | |
| 记忆障碍 | 临床1期 | - | 2020-07-02 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 14 | (Huperzine A) | 鬱淵憲艱衊鏇糧夢齋遞(膚淵窪網積憲選簾繭壓) = 襯夢獵獵窪衊鑰窪襯鏇 網壓壓遞鏇醖獵鬱鹽網 (膚膚夢鏇齋窪觸膚艱範, 12.35) 更多 | - | 2019-10-07 | ||
Placebo (Placebo) | 鬱淵憲艱衊鏇糧夢齋遞(膚淵窪網積憲選簾繭壓) = 積積蓋蓋鏇餘鏇製窪衊 網壓壓遞鏇醖獵鬱鹽網 (膚膚夢鏇齋窪觸膚艱範, 18.73) 更多 |
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