Acetylcholinesterase reactivators (oximes) are compounds used for antidotal treatment in case of organophosphorus poisoning. The dissociation constants (pK(a1)) of ten standard or promising acetylcholinesterase reactivators were determined by ultraviolet absorption spectrometry. Two methods of spectra measurement (UV-vis spectrometry, FIA/UV-vis) were applied and compared. The soft and hard models for calculation of pK(a1) values were performed. The pK(a1) values were recommended in the range 7.00-8.35, where at least 10% of oximate anion is available for organophosphate reactivation. All tested oximes were found to have pK(a1) in this range. The FIA/UV-vis method provided rapid sample throughput, low sample consumption, high sensitivity and precision compared to standard UV-vis method. The hard calculation model was proposed as more accurate for pK(a1) calculation.
- MeSH
- acetylcholinesterasa analýza chemie MeSH
- chemie farmaceutická metody normy MeSH
- oximy analýza chemie MeSH
- reaktivátory cholinesterázy analýza chemie MeSH
- spektrofotometrie ultrafialová metody normy MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- validační studie MeSH
Various voltammetric methods (cyclic, DC, and differential pulse voltammetry) were tested for the title purpose. The last mentioned method with optimized parameters was finally chosen for the determination. A low LOD of 3.62.10−8 mol L−1 and a linear dynamic range from 2.5.10−7 to 2.10−5 mol L−1 were reached. An influence of possible interfering agents was studied as well. The proposed method was used in the analysis of pesticide preparation and of spiked samples of river water.
The cholinesterase biosensors are analytical devices suitable for assay of cholinesterase inhibitors in the course of suppression of the biorecognition element activity. Both acetylcholinesterase and butyrylcholinesterase are used for their assay. The biosensors can be used for assay of organophosphorus and carbamate pesticides, nerve agents, drugs in Alzheimer´s disease and myasthenia treatment. The review summarizes the knowledge of cholinesterases, their immobilization and inhibitors as well as shows examples of their activities.
- MeSH
- acetylcholinesterasa MeSH
- Alzheimerova nemoc MeSH
- biosenzitivní techniky * metody využití MeSH
- butyrylcholinesterasa MeSH
- cholinesterasové inhibitory * MeSH
- dichlorvos * analýza normy MeSH
- karbamáty * farmakologie MeSH
- lidé MeSH
- organofluorofosfonáty * farmakologie MeSH
- reaktivátory cholinesterázy analýza MeSH
- sarin farmakologie MeSH
- Check Tag
- lidé MeSH
New acetylcholinesterase reactivators with either a (E) or (Z)-but-2-ene connecting linker were recently prepared. The purity of the compounds was checked by HPLC and was found to be sufficient for in-vitro screening. All the discussed bispyridinium reactivators were analyzed by reversed-phase high performance liquid chromatography (RP-HPLC) to measure lipophilicity. The procedure was performed under isocratic conditions with methanol as organic modifier in the mobile phase using an end-capped non-polar C(18) stationary phase RP column. Relationships between the lipophilicity (logarithm of the RP-HPLC capacity factor, log k) and chemical structures of the studied compounds are discussed. Lipophilicity was different for the (E) and (Z) compounds and varied among the compounds in each of these groups. The lipophilicity differences also indicated an apparent influence of intramolecular interactions. Lipophilicity calculations (log P/Clog P) by means of commonly used software were not successful due to the presence of quaternary nitrogen atoms in the molecules of the reactivators.
- MeSH
- financování organizované MeSH
- kontaminace léku MeSH
- lipidy chemie MeSH
- molekulární struktura MeSH
- pyridinové sloučeniny chemie MeSH
- reagencia zkříženě vázaná chemie MeSH
- reaktivátory cholinesterázy analýza MeSH
- stereoizomerie MeSH
- vinylové sloučeniny MeSH
- vysokoúčinná kapalinová chromatografie metody MeSH
- MeSH
- antidota * analýza farmakologie MeSH
- chemie analytická MeSH
- farmacie MeSH
- lidé MeSH
- organofosforové sloučeniny * škodlivé účinky MeSH
- oximy analýza farmakologie MeSH
- reaktivátory cholinesterázy * analýza farmakologie MeSH
- spektrofotometrie metody využití MeSH
- statistika jako téma MeSH
- vojenská zařízení MeSH
- vojenské lékařství MeSH
- vysokoúčinná kapalinová chromatografie metody využití MeSH
- Check Tag
- lidé MeSH
