Effects of novel tacrine-related cholinesterase inhibitors in the reversal of 3-quinuclidinyl benzilate-induced cognitive deficit in rats —Is there a potential for Alzheimer’s disease treatment?

2016 ◽  
Vol 612 ◽  
pp. 261-268 ◽  
Author(s):  
Jan Misik ◽  
Jan Korabecny ◽  
Eugenie Nepovimova ◽  
Alzbeta Kracmarova ◽  
Jiri Kassa
2004 ◽  
Vol 59 (3-4) ◽  
pp. 293-296 ◽  
Author(s):  
Pavla Zdražilová ◽  
Šárka Štĕpánková ◽  
Karel Komers ◽  
Karel Ventura ◽  
Alexander Čegan

The power of chosen carbamates and hydrazinium derivatives (carbazates) to inhibit the hydrolysis of acetylthiocholine by butyrylcholinesterase or acetylcholinesterase was tested. The determined pI50 values (= negative logarithm of the molar concentration inhibiting the enzyme activity by 50%) of the tested substances were compared with pI50 values of the commercially used drugs for the Alzheimer’s disease treatment - rivastigmine and galanthamine.


2021 ◽  
Vol 112 ◽  
pp. 104974
Author(s):  
Galina F. Makhaeva ◽  
Sofya V. Lushchekina ◽  
Nadezhda V. Kovaleva ◽  
Tatiana Yu. Astakhova ◽  
Natalia P. Boltneva ◽  
...  

2018 ◽  
Vol 76 (7) ◽  
pp. 444-451 ◽  
Author(s):  
Flávia Silva de Moraes ◽  
Mariana Lima Cerqueira de Souza ◽  
Giancarlo Lucchetti ◽  
Alessandra Lamas Granero Lucchetti

ABSTRACT In light of the high cost of dementia treatment, there is legislation authorizing free distribution of cholinesterase inhibitors to those suffering from Alzheimer’s disease in Brazil. However, the existence of this free distribution does not guarantee adequate distribution. Objectives The present study aimed to investigate the trends of prescriptions and the coverage of Alzheimer’s disease treatment using cholinesterase inhibitors from public pharmacies dispensing high-cost drugs in Brazil. Methods This was a retrospective study that collected data from the Brazilian public Unified Health System. All cholinesterase inhibitors distributed at no cost to Brazilians during the year 2014, as well as the estimated number and percentages of patients who used these medications, were evaluated and compared to data from the year 2008. Results Our estimates indicated that 9.7% of the population having dementia syndromes used cholinesterase inhibitors, as well as 16.1% of those with Alzheimer’s disease in Brazil. A clear disparity was noted between the use and distribution of cholinesterase inhibitors, depending on the region in which they were found. Over time, an increase in the distribution of cholinesterase inhibitors has been noted. In 2008, that use was 12.0% whereas, in 2014, it was 16.1%, an increase of 34% in six years. Conclusion It was estimated that 16.1% of patients with Alzheimer’s disease in Brazil use cholinesterase inhibitors. These values have increased and, in spite of not being satisfactory, they indicate a potential for improvement. However, there is still a significant disparity among the regions.


2019 ◽  
Vol 19 (8) ◽  
pp. 688-705
Author(s):  
Taibi Ben Hadda ◽  
Abdur Rauf ◽  
Hsaine Zgou ◽  
Fatma Sezer Senol ◽  
Ilkay Erdogan Orhan ◽  
...  

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.


Author(s):  
Eva Mezeiova ◽  
Martina Hrabinova ◽  
Vendula Hepnarova ◽  
Daniel Jun ◽  
Jana Janockova ◽  
...  

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