Dose-dependent tissue distribution of K117, a bis-pyridinium aldoxime, in rats

H. Kalász, Gellért Karvaly, Kamil Musilek, Kamil Kuca, Jung Young-Sik, Barbara Malawska, Ernest A. Adeghate, Syed M. Nurulain, Judit Szepesy, T. Zelles, K. Tekes

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Abstract

Background: Bis-pyridinium aldoximes are reactivators of the paraoxon-inhibited butyrylcholinesterase enzyme. Paraoxon is the active product of parathion, a widely used insecticide. Objective: The objective of this study is to examine the dose-dependent distribution of K117, a bis-pyridinium aldoxime in rat tissues. Materials and Methods: White male Wistar rats were intramuscularly injected with various doses of K117; the animals were sacrificed 30 minutes after injections. The dose-dependent body distribution of K117 was determined using reversed-phase HPLC. Results: Dose-dependent distribution of K117 in body tissues was linear in the serum and other body tissues throughout the whole range of the concentrations studied. However, the of distribution was not observed in the brain and cerebrospinal fluid, especially with high doses. Conclusion: The body distribution of K117 significantly depends on doses used, the p-value is: 500 nmol, i.m., when applied in the range of 100 to 10,000 nmol.

Original languageEnglish
Pages (from-to)1-6
Number of pages6
JournalOpen Medicinal Chemistry Journal
Volume13
Issue number1
DOIs
Publication statusPublished - Jan 1 2019

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Keywords

  • Dose-dependence
  • Intramuscular injections
  • K117
  • Linear pattern
  • Pharmacokinetics
  • Wistar rats

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Kalász, H., Karvaly, G., Musilek, K., Kuca, K., Young-Sik, J., Malawska, B., Adeghate, E. A., Nurulain, S. M., Szepesy, J., Zelles, T., & Tekes, K. (2019). Dose-dependent tissue distribution of K117, a bis-pyridinium aldoxime, in rats. Open Medicinal Chemistry Journal, 13(1), 1-6. https://doi.org/10.2174/1874104501913010001