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Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase
by
Szimrók, Zoltán
, Adeghate, Jennifer
, Karvaly, Gellért
, Kalász, Huba
, Tekes, Kornélia
in
Animals
/ Antidotes - metabolism
/ butyrylcholinesterase
/ Butyrylcholinesterase - metabolism
/ Chlorine
/ distribution
/ Drug dosages
/ Homogenization
/ k-203
/ k-867
/ k-870
/ Male
/ Mass spectrometry
/ Organophosphate Poisoning - drug therapy
/ Oximes - pharmacokinetics
/ pyridinium aldoxime
/ Pyridinium Compounds - pharmacokinetics
/ Rats
/ Rats, Wistar
/ rp-hplc
/ Scientific imaging
2020
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Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase
by
Szimrók, Zoltán
, Adeghate, Jennifer
, Karvaly, Gellért
, Kalász, Huba
, Tekes, Kornélia
in
Animals
/ Antidotes - metabolism
/ butyrylcholinesterase
/ Butyrylcholinesterase - metabolism
/ Chlorine
/ distribution
/ Drug dosages
/ Homogenization
/ k-203
/ k-867
/ k-870
/ Male
/ Mass spectrometry
/ Organophosphate Poisoning - drug therapy
/ Oximes - pharmacokinetics
/ pyridinium aldoxime
/ Pyridinium Compounds - pharmacokinetics
/ Rats
/ Rats, Wistar
/ rp-hplc
/ Scientific imaging
2020
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Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase
by
Szimrók, Zoltán
, Adeghate, Jennifer
, Karvaly, Gellért
, Kalász, Huba
, Tekes, Kornélia
in
Animals
/ Antidotes - metabolism
/ butyrylcholinesterase
/ Butyrylcholinesterase - metabolism
/ Chlorine
/ distribution
/ Drug dosages
/ Homogenization
/ k-203
/ k-867
/ k-870
/ Male
/ Mass spectrometry
/ Organophosphate Poisoning - drug therapy
/ Oximes - pharmacokinetics
/ pyridinium aldoxime
/ Pyridinium Compounds - pharmacokinetics
/ Rats
/ Rats, Wistar
/ rp-hplc
/ Scientific imaging
2020
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Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase
Journal Article
Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase
2020
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Overview
Our aim was to find chlorine-substituted antidotes against organophosphate poisoning and compare their pharmacokinetics to their parent compound, K-203. White male Wistar rats were intramuscularly injected with K-203, K-867 or K-870. Serum, brain, kidneys, liver, lung, eyes, and testes tissues were taken after 5, 15, 30, 60, and 120 min and analyzed using reversed-phase high-performance liquid chromatography. K-203, K-867, or K-870 was present in every tissue that was analyzed, including the serum, the eyes, testes, liver, kidneys, lungs, and the brain. The serum levels of K-867 and K-870 (chlorine-substituted derivatives of K-203) were nearly constant between 15 and 30 min, while their parent compound (K-203) showed peak level at 15 min after the administration of 30 µmol/rat. Neither K-203, nor K-867 or K-870 were toxic at a dose of 100 µmol/200 g in rats. Chlorine-substitution of K-867 and K-870 produced limited absorbance and distribution compared to their parent compound, K203.
Publisher
MDPI AG,MDPI
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