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donepezil</title> <meta name="description" content="Search results for: donepezil"> <meta name="keywords" content="donepezil"> <meta name="viewport" content="width=device-width, initial-scale=1, minimum-scale=1, maximum-scale=1, user-scalable=no"> <meta charset="utf-8"> <link href="https://cdn.waset.org/favicon.ico" type="image/x-icon" rel="shortcut icon"> <link href="https://cdn.waset.org/static/plugins/bootstrap-4.2.1/css/bootstrap.min.css" rel="stylesheet"> <link href="https://cdn.waset.org/static/plugins/fontawesome/css/all.min.css" rel="stylesheet"> <link href="https://cdn.waset.org/static/css/site.css?v=150220211555" rel="stylesheet"> </head> <body> <header> <div class="container"> <nav class="navbar navbar-expand-lg navbar-light"> <a class="navbar-brand" href="https://waset.org"> <img src="https://cdn.waset.org/static/images/wasetc.png" alt="Open Science Research Excellence" title="Open Science Research Excellence" /> </a> <button class="d-block d-lg-none navbar-toggler ml-auto" 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id="custom-search-input"> <div class="input-group"> <i class="fas fa-search"></i> <input type="text" class="search-query" name="q" placeholder="Author, Title, Abstract, Keywords" value="donepezil"> <input type="submit" class="btn_search" value="Search"> </div> </div> </form> </div> </div> <div class="row mt-3"> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Commenced</strong> in January 2007</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Frequency:</strong> Monthly</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Edition:</strong> International</div> </div> </div> <div class="col-sm-3"> <div class="card"> <div class="card-body"><strong>Paper Count:</strong> 7</div> </div> </div> </div> <h1 class="mt-3 mb-3 text-center" style="font-size:1.6rem;">Search results for: donepezil</h1> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">7</span> Combined Treatment of Aged Rats with Donepezil and the Gingko Extract EGb 761® Enhances Learning and Memory Superiorly to Monotherapy</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Linda%20Bl%C3%BCmel">Linda Blümel</a>, <a href="https://publications.waset.org/abstracts/search?q=Bettina%20Bert"> Bettina Bert</a>, <a href="https://publications.waset.org/abstracts/search?q=Jan%20Brosda"> Jan Brosda</a>, <a href="https://publications.waset.org/abstracts/search?q=Heidrun%20Fink"> Heidrun Fink</a>, <a href="https://publications.waset.org/abstracts/search?q=Melanie%20Hamann"> Melanie Hamann</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Age-related cognitive decline can eventually lead to dementia, the most common mental illness in elderly people and an immense challenge for patients, their families and caregivers. Cholinesterase inhibitors constitute the most commonly used antidementia prescription medication. The standardized Ginkgo biloba leaf extract EGb 761® is approved for treating age-associated cognitive impairment and has been shown to improve the quality of life in patients suffering from mild dementia. A clinical trial with 96 Alzheimer´s disease patients indicated that the combined treatment with donepezil and EGb 761® had fewer side effects than donepezil alone. In an animal model of cognitive aging, we compared the effect of combined treatment with EGb 761® or donepezil monotherapy and vehicle. We compared the effect of chronic treatment (15 days of pretreatment) with donepezil (1.5 mg/kg p. o.), EGb 761® (100 mg/kg p. o.), or the combination of the two drugs, or vehicle in 18 – 20 month old male OFA rats. Learning and memory performance were assessed by Morris water maze testing, motor behavior in an open field paradigm. In addition to chronic treatment, the substances were administered orally 30 minutes before testing. Compared to the first day and to the control group, only the combination group showed a significant reduction in latency to reach the hidden platform on the second day of testing. Moreover, from the second day of testing onwards, the donepezil, the EGb 761® and the combination group required less time to reach the hidden platform compared to the first day. The control group did not reach the same latency reduction until day three. There were no effects on motor behavior. These results suggest a superiority of the combined treatment of donepezil with EGb 761® compared to monotherapy. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=age-related%20cognitive%20decline" title="age-related cognitive decline">age-related cognitive decline</a>, <a href="https://publications.waset.org/abstracts/search?q=dementia" title=" dementia"> dementia</a>, <a href="https://publications.waset.org/abstracts/search?q=ginkgo%20biloba%20leaf%20extract%20EGb%20761%C2%AE" title=" ginkgo biloba leaf extract EGb 761®"> ginkgo biloba leaf extract EGb 761®</a>, <a href="https://publications.waset.org/abstracts/search?q=learning%20and%20memory" title=" learning and memory"> learning and memory</a>, <a href="https://publications.waset.org/abstracts/search?q=old%20rats" title=" old rats"> old rats</a> </p> <a href="https://publications.waset.org/abstracts/35854/combined-treatment-of-aged-rats-with-donepezil-and-the-gingko-extract-egb-761-enhances-learning-and-memory-superiorly-to-monotherapy" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/35854.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">368</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">6</span> Application of Discrete-Event Simulation in Health Technology Assessment: A Cost-Effectiveness Analysis of Alzheimer’s Disease Treatment Using Real-World Evidence in Thailand</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Khachen%20Kongpakwattana">Khachen Kongpakwattana</a>, <a href="https://publications.waset.org/abstracts/search?q=Nathorn%20Chaiyakunapruk"> Nathorn Chaiyakunapruk</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Background: Decision-analytic models for Alzheimer’s disease (AD) have been advanced to discrete-event simulation (DES), in which individual-level modelling of disease progression across continuous severity spectra and incorporation of key parameters such as treatment persistence into the model become feasible. This study aimed to apply the DES to perform a cost-effectiveness analysis of treatment for AD in Thailand. Methods: A dataset of Thai patients with AD, representing unique demographic and clinical characteristics, was bootstrapped to generate a baseline cohort of patients. Each patient was cloned and assigned to donepezil, galantamine, rivastigmine, memantine or no treatment. Throughout the simulation period, the model randomly assigned each patient to discrete events including hospital visits, treatment discontinuation and death. Correlated changes in cognitive and behavioral status over time were developed using patient-level data. Treatment effects were obtained from the most recent network meta-analysis. Treatment persistence, mortality and predictive equations for functional status, costs (Thai baht (THB) in 2017) and quality-adjusted life year (QALY) were derived from country-specific real-world data. The time horizon was 10 years, with a discount rate of 3% per annum. Cost-effectiveness was evaluated based on the willingness-to-pay (WTP) threshold of 160,000 THB/QALY gained (4,994 US$/QALY gained) in Thailand. Results: Under a societal perspective, only was the prescription of donepezil to AD patients with all disease-severity levels found to be cost-effective. Compared to untreated patients, although the patients receiving donepezil incurred a discounted additional costs of 2,161 THB, they experienced a discounted gain in QALY of 0.021, resulting in an incremental cost-effectiveness ratio (ICER) of 138,524 THB/QALY (4,062 US$/QALY). Besides, providing early treatment with donepezil to mild AD patients further reduced the ICER to 61,652 THB/QALY (1,808 US$/QALY). However, the dominance of donepezil appeared to wane when delayed treatment was given to a subgroup of moderate and severe AD patients [ICER: 284,388 THB/QALY (8,340 US$/QALY)]. Introduction of a treatment stopping rule when the Mini-Mental State Exam (MMSE) score goes below 10 to a mild AD cohort did not deteriorate the cost-effectiveness of donepezil at the current treatment persistence level. On the other hand, none of the AD medications was cost-effective when being considered under a healthcare perspective. Conclusions: The DES greatly enhances real-world representativeness of decision-analytic models for AD. Under a societal perspective, treatment with donepezil improves patient’s quality of life and is considered cost-effective when used to treat AD patients with all disease-severity levels in Thailand. The optimal treatment benefits are observed when donepezil is prescribed since the early course of AD. With healthcare budget constraints in Thailand, the implementation of donepezil coverage may be most likely possible when being considered starting with mild AD patients, along with the stopping rule introduced. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=Alzheimer%27s%20disease" title="Alzheimer's disease">Alzheimer's disease</a>, <a href="https://publications.waset.org/abstracts/search?q=cost-effectiveness%20analysis" title=" cost-effectiveness analysis"> cost-effectiveness analysis</a>, <a href="https://publications.waset.org/abstracts/search?q=discrete%20event%20simulation" title=" discrete event simulation"> discrete event simulation</a>, <a href="https://publications.waset.org/abstracts/search?q=health%20technology%20assessment" title=" health technology assessment"> health technology assessment</a> </p> <a href="https://publications.waset.org/abstracts/107180/application-of-discrete-event-simulation-in-health-technology-assessment-a-cost-effectiveness-analysis-of-alzheimers-disease-treatment-using-real-world-evidence-in-thailand" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/107180.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">129</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">5</span> Silymarin Reverses Scopolamine-Induced Memory Deficit in Object Recognition Test in Rats: A Behavioral, Biochemical, Histopathological and Immunohistochemical Study</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Salma%20A.%20El-Marasy">Salma A. El-Marasy</a>, <a href="https://publications.waset.org/abstracts/search?q=Reham%20M.%20Abd-Elsalam"> Reham M. Abd-Elsalam</a>, <a href="https://publications.waset.org/abstracts/search?q=Omar%20A.%20Ahmed-Farid"> Omar A. Ahmed-Farid</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Dementia is characterized by impairments in memory and other cognitive abilities. This study aims to elucidate the possible ameliorative effect of silymarin on scopolamine-induced dementia using the object recognition test (ORT). The study was extended to demonstrate the role of cholinergic activity, oxidative stress, neuroinflammation, brain neurotransmitters and histopathological changes in the anti-amnestic effect of silymarin in demented rats. Wistar rats were pretreated with silymarin (200, 400, 800 mg/kg) or donepezil (10 mg/kg) orally for 14 consecutive days. Dementia was induced after the last drug administration by a single intraperitoneal dose of scopolamine (16 mg/kg). Then behavioral, biochemical, histopathological, and immunohistochemical analyses were then performed. Rats pretreated with silymarin counteracted scopolamine-induced non-spatial working memory impairment in the ORT and decreased acetylcholinesterase (AChE) activity, reduced malondialdehyde (MDA), elevated reduced glutathione (GSH), restored gamma-aminobutyric acid (GABA) and dopamine (DA) contents in the cortical and hippocampal brain homogenates. Silymarin dose-dependently reversed scopolamine-induced histopathological changes. Immunohistochemical analysis showed that silymarin dose-dependently mitigated protein expression of a glial fibrillary acidic protein (GFAP) and nuclear factor kappa-B (NF-κB) in the brain cortex and hippocampus. All these effects of silymarin were similar to that of the standard anti-amnestic drug, donepezil. This study reveals that the ameliorative effect of silymarin on scopolamine-induced dementia in rats using the ORT maybe in part mediated by, enhancement of cholinergic activity, anti-oxidant and anti-inflammatory activities as well as mitigation in brain neurotransmitters and histopathological changes. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=dementia" title="dementia">dementia</a>, <a href="https://publications.waset.org/abstracts/search?q=donepezil" title=" donepezil"> donepezil</a>, <a href="https://publications.waset.org/abstracts/search?q=object%20recognition%20test" title=" object recognition test"> object recognition test</a>, <a href="https://publications.waset.org/abstracts/search?q=rats" title=" rats"> rats</a>, <a href="https://publications.waset.org/abstracts/search?q=silymarin" title=" silymarin"> silymarin</a>, <a href="https://publications.waset.org/abstracts/search?q=scopolamine" title=" scopolamine"> scopolamine</a> </p> <a href="https://publications.waset.org/abstracts/90170/silymarin-reverses-scopolamine-induced-memory-deficit-in-object-recognition-test-in-rats-a-behavioral-biochemical-histopathological-and-immunohistochemical-study" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/90170.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">138</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">4</span> Design, Synthesis and Evaluation of 4-(Phenylsulfonamido)Benzamide Derivatives as Selective Butyrylcholinesterase Inhibitors</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Sushil%20Kumar%20Singh">Sushil Kumar Singh</a>, <a href="https://publications.waset.org/abstracts/search?q=Ashok%20Kumar"> Ashok Kumar</a>, <a href="https://publications.waset.org/abstracts/search?q=Ankit%20%20Ganeshpurkar"> Ankit Ganeshpurkar</a>, <a href="https://publications.waset.org/abstracts/search?q=Ravi%20Singh"> Ravi Singh</a>, <a href="https://publications.waset.org/abstracts/search?q=Devendra%20Kumar"> Devendra Kumar</a> </p> <p class="card-text"><strong>Abstract:</strong></p> In spectrum of neurodegenerative diseases, Alzheimer’s disease (AD) is characterized by the presence of amyloid β plaques and neurofibrillary tangles in the brain. It results in cognitive and memory impairment due to loss of cholinergic neurons, which is considered to be one of the contributing factors. Donepezil, an acetylcholinesterase (AChE) inhibitor which also inhibits butyrylcholinesterase (BuChE) and improves the memory and brain’s cognitive functions, is the most successful and prescribed drug to treat the symptoms of AD. The present work is based on designing of the selective BuChE inhibitors using computational techniques. In this work, machine learning models were trained using classification algorithms followed by screening of diverse chemical library of compounds. The various molecular modelling and simulation techniques were used to obtain the virtual hits. The amide derivatives of 4-(phenylsulfonamido) benzoic acid were synthesized and characterized using 1H & 13C NMR, FTIR and mass spectrometry. The enzyme inhibition assays were performed on equine plasma BuChE and electric eel’s AChE by method developed by Ellman et al. Compounds 31, 34, 37, 42, 49, 52 and 54 were found to be active against equine BuChE. N-(2-chlorophenyl)-4-(phenylsulfonamido)benzamide and N-(2-bromophenyl)-4-(phenylsulfonamido)benzamide (compounds 34 and 37) displayed IC50 of 61.32 ± 7.21 and 42.64 ± 2.17 nM against equine plasma BuChE. Ortho-substituted derivatives were more active against BuChE. Further, the ortho-halogen and ortho-alkyl substituted derivatives were found to be most active among all with minimal AChE inhibition. The compounds were selective toward BuChE. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=Alzheimer%20disease" title="Alzheimer disease">Alzheimer disease</a>, <a href="https://publications.waset.org/abstracts/search?q=butyrylcholinesterase" title=" butyrylcholinesterase"> butyrylcholinesterase</a>, <a href="https://publications.waset.org/abstracts/search?q=machine%20learning" title=" machine learning"> machine learning</a>, <a href="https://publications.waset.org/abstracts/search?q=sulfonamides" title=" sulfonamides "> sulfonamides </a> </p> <a href="https://publications.waset.org/abstracts/122292/design-synthesis-and-evaluation-of-4-phenylsulfonamidobenzamide-derivatives-as-selective-butyrylcholinesterase-inhibitors" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/122292.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">139</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">3</span> Protective Effect of the Histamine H3 Receptor Antagonist DL77 in Behavioral Cognitive Deficits Associated with Schizophrenia</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=B.%20Sadek">B. Sadek</a>, <a href="https://publications.waset.org/abstracts/search?q=N.%20Khan"> N. Khan</a>, <a href="https://publications.waset.org/abstracts/search?q=D.%20%C5%81a%C5%BCewska"> D. Łażewska</a>, <a href="https://publications.waset.org/abstracts/search?q=K.%20Kie%C4%87-Kononowicz"> K. Kieć-Kononowicz</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The eﬀects of the non-imidazole histamine H3 receptor (H3R) antagonist DL77 in passive avoidance paradigm (PAP) and novel object recognition (NOR) task in MK801-induced cognitive deficits associated with schizophrenia (CDS) in adult male rats, and applying donepezil (DOZ) as a reference drug were investigated. The results show that acute systemic administration of DL77 (2.5, 5, and 10 mg/kg, i.p.) significantly improved MK801-induced (0.1 mg/kg, i.p.) memory deficits in PAP. The ameliorating activity of DL77 (5 mg/kg, i.p.) in MK801-induced deficits was partly reversed when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL, 10 mg/kg, i.p.) or with the antimuscarinic antagonist scopolamine (SCO, 0.1 mg/kg, i.p.), but not with the CNS penetrant H1R antagonist pyrilamine (PYR, 10 mg/kg, i.p.). Moreover, the memory enhancing effect of DL77 (5 mg/kg, i.p.) in MK801-induced memory deficits in PAP was strongly reversed when rats were pretreated with a combination of ZOL (10 mg/kg, i.p.) and SCO (1.0 mg/kg, i.p.). Furthermore, the significant ameliorative effect of DL77 (5 mg/kg, i.p.) on MK801-induced long-term memory (LTM) impairment in NOR test was comparable to the DOZ-provided memory-enhancing effect, and was abrogated when animals were pretreated with the histamine H3R agonist R-(α)-methylhistamine (RAMH, 10 mg/kg, i.p.). However, DL77(5 mg/kg, i.p.) failed to provide procognitive effect on MK801-induced short-term memory (STM) impairment in NOR test. In addition, DL77 (5 mg/kg) did not alter anxiety levels and locomotor activity of animals naive to elevated-plus maze (EPM), demonstrating that improved performances with DL77 (5 mg/kg) in PAP or NOR are unrelated to changes in emotional responding or spontaneous locomotor activity. These results provide evidence for the potential of H3Rs for the treatment of neurodegenerative disorders related to impaired memory function, e.g. CDS. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=histamine%20H3%20receptor" title="histamine H3 receptor">histamine H3 receptor</a>, <a href="https://publications.waset.org/abstracts/search?q=antagonist" title=" antagonist"> antagonist</a>, <a href="https://publications.waset.org/abstracts/search?q=learning" title=" learning"> learning</a>, <a href="https://publications.waset.org/abstracts/search?q=memory%20impairment" title=" memory impairment"> memory impairment</a>, <a href="https://publications.waset.org/abstracts/search?q=passive%20avoidance%20paradigm" title=" passive avoidance paradigm"> passive avoidance paradigm</a>, <a href="https://publications.waset.org/abstracts/search?q=novel%20object%20recognition" title=" novel object recognition"> novel object recognition</a> </p> <a href="https://publications.waset.org/abstracts/74343/protective-effect-of-the-histamine-h3-receptor-antagonist-dl77-in-behavioral-cognitive-deficits-associated-with-schizophrenia" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/74343.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">203</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">2</span> The Ameliorative Effects of the Histamine H3 Receptor Antagonist/Inverse Agonist DL77 on MK801-Induced Memory Deficits in Rats</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=B.%20Sadek">B. Sadek</a>, <a href="https://publications.waset.org/abstracts/search?q=N.%20Khan"> N. Khan</a>, <a href="https://publications.waset.org/abstracts/search?q=Shreesh%20K.%20Ojha"> Shreesh K. Ojha</a>, <a href="https://publications.waset.org/abstracts/search?q=Adel%20Sadeq"> Adel Sadeq</a>, <a href="https://publications.waset.org/abstracts/search?q=D.%20Lazewska"> D. Lazewska</a>, <a href="https://publications.waset.org/abstracts/search?q=K.%20Kiec-Kononowicz"> K. Kiec-Kononowicz</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The involvement of Histamine H3 receptors (H3Rs) in memory and the potential role of H3R antagonists in pharmacological control of neurodegenerative disorders, e.g., Alzheimer disease (AD) is well established. Therefore, the memory-enhancing effects of the H3R antagonist DL77 on MK801-induced cognitive deficits were evaluated in passive avoidance paradigm (PAP) and novel object recognition (NOR) tasks in adult male rats, applying donepezil (DOZ) as a reference drug. Animals pretreated with acute systemic administration of DL77 (2.5, 5, and 10 mg/kg, i.p.) were significantly ameliorated in regard to MK801-induced memory deficits in PAP. The ameliorative effect of most effective dose of DL77 (5 mg/kg, i.p.) was abrogated when animals were pretreated with a co-injection with the H3R agonist R-(α)-methylhistamine (RAMH, 10 mg/kg, i.p.). Moreover, and in the NOR paradigm, DL77 (5 mg/kg, i.p.) reversed MK801-induced deficits long-term memory (LTM), and the DL77-provided procognitive effect was comparable to that of reference drug DOZ, and was reversed when animals were co-injected with RAMH (10 mg/kg, i.p.). However, DL77(5 mg/kg, i.p.) failed to alter short-term memory (STM) impairment in NOR test. Furthermore, DL77 (5 mg/kg) failed to induce any alterations of anxiety and locomotor behaviors of animals naive to elevated-plus maze (EPM), indicating that the ameliorative effects observed in PAP or NOR tests were not associated to alterations in emotions or in natural locomotion of tested animals. These results reveal the potential contribution of H3Rs in modulating CNS neurotransmission systems associated with neurodegenerative disorders, e.g., AD. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=histamine%20H3%20receptor" title="histamine H3 receptor">histamine H3 receptor</a>, <a href="https://publications.waset.org/abstracts/search?q=antagonist" title=" antagonist"> antagonist</a>, <a href="https://publications.waset.org/abstracts/search?q=learning%20and%20memory" title=" learning and memory"> learning and memory</a>, <a href="https://publications.waset.org/abstracts/search?q=Alzheimer%27s%20disease" title=" Alzheimer's disease"> Alzheimer's disease</a>, <a href="https://publications.waset.org/abstracts/search?q=neurodegeneration" title=" neurodegeneration"> neurodegeneration</a>, <a href="https://publications.waset.org/abstracts/search?q=passive%20avoidance%20paradigm" title=" passive avoidance paradigm"> passive avoidance paradigm</a>, <a href="https://publications.waset.org/abstracts/search?q=novel%20object%20recognition" title=" novel object recognition"> novel object recognition</a>, <a href="https://publications.waset.org/abstracts/search?q=behavioral%20research" title=" behavioral research"> behavioral research</a> </p> <a href="https://publications.waset.org/abstracts/89786/the-ameliorative-effects-of-the-histamine-h3-receptor-antagonistinverse-agonist-dl77-on-mk801-induced-memory-deficits-in-rats" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/89786.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">155</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">1</span> Circadian-Clock Controlled Drug Transport Across Blood-Cerebrospinal Fluid Barrier</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Andr%C3%A9%20Furtado">André Furtado</a>, <a href="https://publications.waset.org/abstracts/search?q=Rafael%20Mineiro"> Rafael Mineiro</a>, <a href="https://publications.waset.org/abstracts/search?q=Isabel%20Gon%C3%A7alves"> Isabel Gonçalves</a>, <a href="https://publications.waset.org/abstracts/search?q=Cec%C3%ADlia%20Santos"> Cecília Santos</a>, <a href="https://publications.waset.org/abstracts/search?q=Telma%20Quintela"> Telma Quintela</a> </p> <p class="card-text"><strong>Abstract:</strong></p> The development of therapies for central nervous system (CNS) disorders is one of the biggest challenges of current pharmacology, given the unique features of brain barriers, which limit drug delivery. Efflux transporters (ABC transporters) expressed at the blood-cerebrospinal fluid barrier (BCSFB), are the main obstacles for the delivery of therapeutic compounds into the CNS, compromising the effective treatment of brain cancer, brain metastasis from peripheral cancers, or even neurodegenerative disorders. It is thus extremely important to understand the regulation of these transporters for reducing their expression while treating a brain disorder or choosing the most appropriate conditions for drug administration. Based on the fact that the BCSFB have fine-tuned biological rhythms, studying the circadian variation of drug transport processes is critical for choosing the most appropriate time of the day for drug administration. In our study, using an in vitro model of the BCSFB, we characterized the circadian transport profile of methotrexate (MTX) and donepezil (DNPZ), two drugs involved in the treatment of cancer and Alzheimer’s Disease symptoms, respectively. We found that MTX is transported across the basal and apical membranes of the BCSFB in a circadian way. The circadian pattern of an ABC transporter, Abcc4, might be partially responsible for MTX circadian transport. Furthermore, regarding the DNPZ transport study, we observed that the regulation of Abcg2 expression by the circadian rhythm will impact the circadian-dependent transport of DNPZ across the BCSFB. Overall, our results will contribute to the current knowledge on brain pharmacoresistance at the BCSFB by disclosing how circadian rhythms control drug delivery to the brain, setting the grounds for a potential application of chronotherapy to brain diseases to enhance the efficacy of medications and minimize their side effects. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=blood-cerebrospinal%20fluid%20barrier" title="blood-cerebrospinal fluid barrier">blood-cerebrospinal fluid barrier</a>, <a href="https://publications.waset.org/abstracts/search?q=ABC%20transporters" title=" ABC transporters"> ABC transporters</a>, <a href="https://publications.waset.org/abstracts/search?q=drug%20transport" title=" drug transport"> drug transport</a>, <a href="https://publications.waset.org/abstracts/search?q=chronotherapy" title=" chronotherapy"> chronotherapy</a> </p> <a href="https://publications.waset.org/abstracts/193438/circadian-clock-controlled-drug-transport-across-blood-cerebrospinal-fluid-barrier" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/193438.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">13</span> </span> </div> </div> </div> </main> <footer> <div id="infolinks" class="pt-3 pb-2"> <div class="container"> <div style="background-color:#f5f5f5;" class="p-3"> <div class="row"> <div class="col-md-2"> <ul class="list-unstyled"> About <li><a href="https://waset.org/page/support">About Us</a></li> <li><a href="https://waset.org/page/support#legal-information">Legal</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/WASET-16th-foundational-anniversary.pdf">WASET celebrates its 16th foundational anniversary</a></li> </ul> </div> <div 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