نتایج جستجو برای: cholinesterase inhibitors
تعداد نتایج: 191405 فیلتر نتایج به سال:
The cholinesterase inhibitors donepezil, rivastigmine and galantamine have a modest and transient benefit in Alzheimer's disease. Their known adverse effects include bradycardia. A Canadian case-control study conducted between 2003 and 2008 showed a statistically significant increase in the risk of hospitalisation for bradycardia among patients who had been taking a cholinesterase inhibitor for...
biomarkers are assigned as early warning systems regarding aquatic organisms exposed to pollutants. among which, however, measurement of esterase enzymes activity specially cholinesterase of fish tissues, is a marker for exposure to organophosphate pesticide and carbamates, and this biomarker has been used widely in broad range of investigations. a number of capoeta capoeta gracilis (:cyprinida...
The cholinergic system is known to show deterioration during aging and Alzheimer's disease. In response, a therapeutic approach to Alzheimer's disease has been to attempt to compensate for the decrease in central cholinergic function by potentiating the activity of the remaining intact cholinergic cells with cholinesterase inhibitors. In this study treatment with the long-lasting cholinesterase...
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 Alzheim...
The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with expected activity against disease-modifying and symptomatic targets. A series of 15 drug-like various substituted derivatives of 2-(benzylamino-2-hy...
OBJECTIVE Lethal sepsis occurs when an excessive inflammatory response evolves that cannot be controlled by physiologic anti-inflammatory mechanisms, such as the recently described cholinergic anti-inflammatory pathway. Here we studied whether the cholinergic anti-inflammatory pathway can be activated by pharmacologic cholinesterase inhibition in vivo. DESIGN Prospective, randomized laborator...
Cholinesterases are important biological targets responsible for regulation of cholinergic transmission, and their inhibitors are used for the treatment of Alzheimer's disease. To design new cholinesterase inhibitors, of different structure-based design strategies was followed, including the modification of compounds from a previously developed library and a fragment-based design approach. This...
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