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Evaluation of the efficacy of new acetylcholinesterase inhibitors by Ellman's method
Mackurová, Michaela ; Čečková, Martina (advisor) ; Pourová, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Performed at: University of defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Department of Toxicology and Military Pharmacology Candidate: Michaela Mackurová Leader of diploma thesis: Doc. PharmDr. Martina Čečková, Ph.D. Supervisor: mjr. PharmDr. Vendula Hepnarová, Ph.D. Title of diploma thesis: Measurement of the efficacy of new acetylcholinesterase inhibitors using the Ellman method Cholinesterases (ChEs) belong to an important group of enzymes in our body. The best known acetylcholinesterase and butyrylcholinesterase play an important role in the treatment of many diseases, including Alzheimer's disease (AD). It is a neurodegenerative disease that occurs mainly in the elderly. It is one of the most common forms of dementia and its incidence is still increasing. To date, no effective therapy for AD has been developed, only symptomatic treatment is available. It is therefore necessary to look for therapeutics that would be able to stop or cure this serious disease. The aim of this work was to determine the inhibitory contraction of newly synthesized potential drugs AD against both ChEs. A total of 27 tacrine derivatives were tested, which were enriched with substituents...
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Název v anglickém jazyce: Evaluation of the efficacy of quarternary acetylcholinesterase reactivators in vivo.
Mackurová, Michaela ; Vopršalová, Marie (advisor) ; Pourová, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Performed at: University of defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Department of Toxicology and Military Pharmacology Student: Michaela Mackurová Leader of diploma thesis: PharmDr. Marie Vopršalová, CSc. Supervisor: kpt. PharmDr. Vendula Hepnarová, Ph.D. Title of diploma thesis: Evaluation of the efficacy of quarternary acetylcholinesterase reactivators in vivo NPL belongs to compounds of organic phosphorus and they are very common cause of poisoning as organophosphorus nerve agent. They can be absorbed by various routes - inhalated, ingest or by transdermal penetration. The problem is ineffective therapy and there is still no broad-spectrum reactivator able to efficiently restore AChE activity after intoxication by various organophosphates that will penetrates into CNS. The main aim of this experiment was to determine and compare the reactivating efficacy of two newly developed oximes K869 and K870 with commonly used oximes K160 and HI-6 against intoxication of sarin. The activity of reactivation was determined by standard spectrophotometric Ellman's method with using male Wistar laboraty rats. The results were evaluated as percentage of reactivation...
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