Experts and Doctors on cholinesterase inhibitors in Czech Republic
Locale: Czech Republic
Topic: cholinesterase inhibitors
Pejchal V, Å tÄ›pÃ¡nkovÃ¡ Å, PejchalovÃ¡ M, KrÃ¡lovec K, Havelek R, RÅ¯Å¾iÄkovÃ¡ Z, et al
. Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors. Bioorg Med Chem. 2016;24:1560-72 pubmed publisher
..In conclusion, our results indicate, that these derivatives could be promising in an effective therapeutic intervention for Alzheimer's disease. ..
Bajgar J, Cabal J, Kassa J, PavlÃk M. Natural Detoxification Capacity to Inactivate Nerve Agents Sarin and VX in the Rat Blood. Acta Medica (Hradec Kralove). 2015;58:128-30 pubmed publisher
..The results demonstrated that sarin can be naturally detoxified on the contrary to VX. Described method can be used as model for other studies dealing with changes of cholinesterases in the blood following different factors. ..
Kassa J, HatlapatkovÃ¡ J, Å½ÄÃ¡rovÃ¡ KarasovÃ¡ J. The Evaluation of the Potency of Newly Developed Oximes (K727, K733) and Trimedoxime to Counteract Acute Neurotoxic Effects of Tabun in Rats. Acta Medica (Hradec Kralove). 2015;58:135-43 pubmed publisher
..Therefore, the newly developed oximes are not suitable for the replacement of commonly used oximes such as trimedoxime in the treatment of acute tabun poisonings. ..
KvÄ›tina J, TachecÃ I, PavlÃk M, KopÃ¡ÄovÃ¡ M, Rejchrt S, Douda T, et al
. Use of electrogastrography in preclinical studies of cholinergic and anticholinergic agents in experimental pigs. Physiol Res. 2015;64 Suppl 5:S647-52 pubmed
..After that period, the areas of amplitudes decreased significantly to the lowest values at the 60-90-min interval. In conclusion, cholinergic and anticholinergic agents affect differently EGG in experimental pigs. ..
KrÃ¡tkÃ½ M, Å tÄ›pÃ¡nkovÃ¡ Å, VorÄÃ¡kovÃ¡ K, Å varcovÃ¡ M, VinÅ¡ovÃ¡ J. Novel Cholinesterase Inhibitors Based on O-Aromatic N,N-Disubstituted Carbamates and Thiocarbamates. Molecules. 2016;21: pubmed publisher
..Mild cytotoxicity for HepG2 cells and consequent satisfactory calculated selectivity indexes qualify several derivatives for further optimization. ..
Mzik M, Korabecny J, Nepovimova E, Vorisek V, Palicka V, Kuca K, et al
. An HPLC-MS method for the quantification of new acetylcholinesterase inhibitor PC 48 (7-MEOTA-donepezil like compound) in rat plasma: Application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2016;1020:85-9 pubmed publisher
..86 mg/kg PC 48 to rats for the first time. Pharmacokinetic parameters for PC 48 include Cmax 39.09 ± 4.45 ng/mL,Tmax 5.00 ± 3.08 min, AUC0-t 23374 ± 4045 min ng/mL and t1/2 1065 ± 246 min. ..
Kuca K, Cabal J, Kassa J, Jun D, Hrabinova M. A comparison of the potency of the oxime HLö-7 and currently used oximes (HI-6, pralidoxime, obidoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods. Acta Medica (Hradec Kralove). 2005;48:81-6 pubmed
Pohanka M, Jun D, Kuca K. Photometric microplate assay for estimation of the efficacy of paraoxon-inhibited acetylcholinesterase reactivation. J Enzyme Inhib Med Chem. 2008;23:781-4 pubmed
..The best results were obtained using obidoxime where reactivation was near to 80%. Suitability of photometric microplates for following of reactivation procedures is discussed. ..
Hoskovcova M, Halamek E, Kobliha Z. Efficacy of structural homoloques and isomers of pralidoxime in reactivation of immobilised acetylcholinesterase inhibited with sarin, cyclosarin and soman. Neuro Endocrinol Lett. 2009;30 Suppl 1:152-5 pubmed
..Evaluation of effectivity of aldoxime reactivators is provided by simple means. The method allows rapid in vitro evaluation of the reactivators without being disturbed by excess of the organophosphate or reactivator. ..