Kateřina Janská Evaluation of the kinetics of acetylcholinesterase inhibitors in vitro Diploma thesis Charles University in Prag, Faculty of Pharmacy in Hradec Králové Pharmacy Department of Biological and Medical Sciences Supervisor: Doc. MUDr. Josef Herink, DrSc. Consultant: PharmDr. Vendula Šepsová The aim of the thesis was to determine the type of an inhibition of newly synthesized AChEI and to find out if AChEI structure changes influence the type of an inhibition. Altogether 12 substances (7 tacrine hybrides and 5 7-methoxy- donepezil hybrids) were investigated. The inhibition potential of the tested substances was studied in vitro on the human recombinant AChE. Spectrophotometric Ellman method was utilized as the measurement tool. The noncompetitive type of an inhibition for substances EN 1-5, PC-25 and PC-33, mixed type of an inhibition for substances PC-48 and PC-49, uncompetitive type of an inhibition for substances EN-6, EN-7 and competitive type of an inhibition for the substance PC-37 was determined. The greatest inhibition potential according to Ki values were found for substances EN-7 and PC-37. Substances PC-37 and PC-48 were determined as substances with the biggest affinity to the AChE. The type of an inhibition has been influenced by a substituent position in PC substances and by...
| Identifer | oai:union.ndltd.org:nusl.cz/oai:invenio.nusl.cz:341476 |
| Date | January 2014 |
| Creators | Janská, Kateřina |
| Contributors | Herink, Josef, Hrdina, Radomír |
| Source Sets | Czech ETDs |
| Language | Czech |
| Detected Language | English |
| Type | info:eu-repo/semantics/masterThesis |
| Rights | info:eu-repo/semantics/restrictedAccess |
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