Cholinesterase Inhibitors in Alzheimer’s Disease: Evaluation of Clinical Studies

Author(s):  
Bengt Winblad ◽  
Abdu Adem ◽  
Lars Backman ◽  
Agneta Nordberg ◽  
Fredrik Elinder ◽  
...  
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.


2012 ◽  
Vol 134 (1) ◽  
pp. 8-25 ◽  
Author(s):  
Haythum O. Tayeb ◽  
Hyun Duk Yang ◽  
Bruce H. Price ◽  
Frank I. Tarazi

2009 ◽  
Vol 22 (1) ◽  
pp. 114-119 ◽  
Author(s):  
Luca Rozzini ◽  
Barbara Vicini Chilovi ◽  
Marta Conti ◽  
Erik Bertoletti ◽  
Marina Zanetti ◽  
...  

ABSTRACTBackground: This study examines the joint effect on cognition of selective serotonin re-uptake inhibitors (SSRIs) and cholinesterase inhibitors (AChEIs) in depressed patients affected by Alzheimer's disease (AD) living at home.Methods: The study was conducted in two different outpatient neurological clinics. 338 patients with probable AD were treated with ChEis (donepezil, rivastigmine and galantamine) as per the clinician's judgment and were observed for nine months. At study entry, participants underwent a multidimensional assessment evaluating cognitive, functional and psychobehavioral domains. All patients were evaluated at baseline, after one (T1), three (T2) and nine months (T3). Patients were grouped in three different categories (patients not depressed and not treated with SSRIs, patients depressed and treated with SSRIs, and patients depressed but not treated with SSRIs).Results: At baseline 182 were diagnosed as not depressed and not treated with SSRIs, 66 as depressed and treated with SSRIs, and 90 as depressed but not treated with SSRIs. The mean change in MMSE score from baseline to nine months showed that depressed patients not treated worsened in comparison with those not depressed and not treated with SSRIs (mean change −0.8 ± 2.3 vs 0.04 ± 2.9; p = 0.02) and patients depressed and treated with SSRI (mean change −0.8 ± 2.3 vs 0.1 ± 2.5; p = 0.03).Conclusions: In AD patients treated with AChEIs, SSRIs may exert some degree of protection against the negative effects of depression on cognition.


Author(s):  
C. A. Johns ◽  
R. C. Mohs ◽  
E. Hollander ◽  
B. M. Davis ◽  
B. S. Greenwald ◽  
...  

2006 ◽  
Vol 14 (7S_Part_19) ◽  
pp. P1067-P1068
Author(s):  
Pradeep Anand Ravindranath ◽  
Rema Raman ◽  
Tiffany W. Chow ◽  
Michael S. Rafii ◽  
Paul S. Aisen ◽  
...  

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