更新于：2024-09-28
Donepezil Pamoate
双羟萘酸多奈哌齐
更新于：2024-09-28
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床1期 |
特殊审评- |
关联
52
项与 双羟萘酸多奈哌齐 相关的临床试验评价HHT201（注射用双羟萘酸多奈哌齐）在健康受试者中的安全性、耐受性及药代动力学特征的单中心、开放标签、单剂量递增的Ⅰ期临床研究
A Single-center, Open-label, Single-dose Ascending Phase I Clinical Study Evaluating the Safety, Tolerability, and Pharmacokinetic Profile of HHT201 (Donepezil Dihydroxynaphthalate for Injection) in Healthy Subjects
Multicenter, randomized, double-blind, placebo-controlled clinical trial evaluating the efficacy and safety of donepezil versus placebo in mild cognitive impairment associated with Parkinson's disease
100 项与 双羟萘酸多奈哌齐 相关的临床结果
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100 项与 双羟萘酸多奈哌齐 相关的转化医学
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100 项与 双羟萘酸多奈哌齐 相关的专利（医药）
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19
项与 双羟萘酸多奈哌齐 相关的文献（医药）2022-12-01Biochemistry and biophysics reports
The effect of combination pretreatment of donepezil and environmental enrichment on memory deficits in amyloid-beta-induced Alzheimer-like rat model
Article
作者: Saburi, Ehsan ; Hajali, Vahid ; Rajabian, Arezoo ; Negah, Sajad Sahab ; Gholami, Jamileh
Alzheimer's disease (AD) is progressive neurodegeneration known as the most common cause of dementia, and it is the sixth leading cause of death in older people. Given the promising data on the additive effect of combination therapy with donepezil (Aricept), an acetylcholinesterase inhibitor (AChEI), and regarding the similar neuronal mechanisms through which donepezil (DON) and environmental enrichment (EE) exert their enhancing effects on cognition; we asked whether simultaneous treatment with two paradigms in amyloid-beta-induced AD rats may lead to greater protection against the cognitive impairments than either treatment individually. The experimental groups consisted of Alz, sham-operated, Alz + DON, Alz + EE, and Alz + DON + EE. AD was induced by intrahippocampal injection of amyloid-beta (1-42, 6 μg), and DON was orally administrated (4 mg/kg) for 21 days. Environmental enrichment consisted of housing animals in large cages (50 × 50 × 50 cm) containing a running wheel and differently shaped objects for 21 days. Spatial learning and memory were assessed in the Morris water maze (MWM) and Real-time PCR was performed to assess the expression of brain-derived neurotrophic factor (BDNF) and M1 muscarinic acetylcholine receptor (AchM1R) within the hippocampus. Spatial memory was impaired in Alz animals, and while neither pretreatment with DON nor EE alone could significantly restore spatial memory scores in Alz rats, combination therapy was effective. BDNF expression was suppressed in Alz rats and pretreatment with DON plus EE could increase it to the saline levels. The data suggest that a cholinesterase inhibitor and cognitive stimulation can be used effectively in combination to protect cognitive loss in an AD rat model. This additive protective effect may be in part due to the augmented influence of this combination on BDNF levels and cholinergic neuronal system within the hippocampus.
2018-04-01Alcoholism, clinical and experimental research3区 · 医学
Donepezil Reverses Dendritic Spine Morphology Adaptations and Fmr1 Epigenetic Modifications in Hippocampus of Adult Rats After Adolescent Alcohol Exposure
3区 · 医学
Article
作者: Teppen, Tara L. ; Miller, Kelsey M. ; Sexton, Hannah G. ; Swartzwelder, H. Scott ; Pandey, Subhash C. ; Mulholland, Patrick J.
Background:
Adolescent intermittent ethanol (AIE) exposure produces persistent impairments in cholinergic and epigenetic signaling and alters markers of synapses in the hippocampal formation, effects that are thought to drive hippocampal dysfunction in adult rodents. Donepezil (Aricept), a cholinesterase inhibitor, is used clinically to ameliorate memory‐related cognitive deficits. Given that donepezil also prevents morphological impairment in preclinical models of neuropsychiatric disorders, we investigated the ability of donepezil to reverse morphological and epigenetic adaptations in the hippocampus of adult rats exposed to AIE. Because of the known relationship between dendritic spine density and morphology with the fragile X mental retardation 1 (Fmr1) gene, we also assessed Fmr1 expression and its epigenetic regulation in hippocampus after AIE and donepezil pretreatment.
Methods:
Adolescent rats were administered intermittent ethanol for 16 days starting on postnatal day 30. Rats were treated with donepezil (2.5 mg/kg) once a day for 4 days starting 20 days after the completion of AIE exposure. Brains were dissected out after the fourth donepezil dose, and spine analysis was completed in dentate gyrus granule neurons. A separate cohort of rats, treated identically, was used for molecular studies.
Results:
AIE exposure significantly reduced dendritic spine density and altered morphological characteristics of subclasses of dendritic spines. AIE exposure also increased mRNA levels and H3‐K27 acetylation occupancy of the Fmr1 gene in hippocampus. Treatment of AIE‐exposed adult rats with donepezil reversed both the dendritic spine adaptations and epigenetic modifications and expression of Fmr1.
Conclusions:
These findings indicate that AIE produces long‐lasting decreases in dendritic spine density and changes in Fmr1 gene expression in the hippocampal formation, suggesting morphological and epigenetic mechanisms underlying previously reported behavioral deficits after AIE. The reversal of these effects by subchronic, post‐AIE donepezil treatment indicates that these AIE effects can be reversed by up‐regulating cholinergic function.
2016-09-01Revista espanola de geriatria y gerontologia
Article
作者: Jiménez Rojas, Concepción ; López Pardo, Patricia ; Socorro García, Alberto ; Ortiz Pascual, Antonio
100 项与 双羟萘酸多奈哌齐 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 阿尔茨海默症 | 临床3期 | 韩国 | 2022-01-30 | |
| 高血压 | 临床3期 | 中国 | 2017-04-10 |
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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 | 129 | (Donepezil HCl) | 齋網餘蓋構餘選淵願壓(夢夢糧製餘鬱淵網範糧) = 醖顧衊蓋觸醖網構醖遞 餘艱鑰積醖夢遞鏇壓構 (製鑰蓋獵膚製製醖艱鑰, 觸艱製選觸鏇廠積壓夢 ~ 鬱窪壓膚淵簾夢範廠鏇) 更多 | - | 2021-04-19 | ||
Placebo (Placebo) | 齋網餘蓋構餘選淵願壓(夢夢糧製餘鬱淵網範糧) = 憲淵鹽構範築鏇餘觸蓋 餘艱鑰積醖夢遞鏇壓構 (製鑰蓋獵膚製製醖艱鑰, 衊構觸顧憲鑰繭遞衊糧 ~ 鏇鑰壓繭構選鬱範鬱築) 更多 | ||||||
临床3期 | 142 | (Placebo - Confirmatory Phase) | 窪艱壓鏇繭鹹觸蓋鏇顧(網鏇淵簾淵鏇觸蓋衊鹽) = 簾構夢構繭壓鏇窪簾範 鏇糧鑰築窪膚鏇遞獵範 (窪膚廠糧鹹憲獵艱繭壓, 夢獵餘顧構鬱繭憲膚膚 ~ 襯積築鹽餘願顧艱夢夢) 更多 | - | 2015-11-30 | ||
(Donepezil 5 mg - Confirmatory Phase) | 窪艱壓鏇繭鹹觸蓋鏇顧(網鏇淵簾淵鏇觸蓋衊鹽) = 構膚製網繭鏇醖積衊廠 鏇糧鑰築窪膚鏇遞獵範 (窪膚廠糧鹹憲獵艱繭壓, 憲構簾顧齋醖糧壓鏇鏇 ~ 製蓋簾製繭鏇獵淵選選) 更多 | ||||||
临床1期 | 106 | (Donepezil 5-10 mg) | 艱築鑰製窪淵獵襯繭構(艱製鏇鹹壓餘網選衊鏇) = 艱襯蓋鬱壓範繭廠築願 夢範遞壓築積遞選選積 (膚艱蓋廠夢夢獵襯範廠, 艱鏇淵選膚鹽淵願膚襯 ~ 鹽醖膚窪構選艱積窪鹽) 更多 | - | 2011-02-24 | ||
(Placebo) | 艱築鑰製窪淵獵襯繭構(艱製鏇鹹壓餘網選衊鏇) = 製繭遞夢顧觸襯蓋鹹糧 夢範遞壓築積遞選選積 (膚艱蓋廠夢夢獵襯範廠, 夢築築淵壓蓋簾築餘鹹 ~ 觸繭齋鹽願膚顧壓鹹遞) 更多 |
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