Novel acetylcholinesterase reactivator - Oxime K048 - Reactivation activity in vitro

Kamil Kuca, Jan Marek, Jana Zdarova-Karasova, Miroslav Pohanka, Jan Korabecny, H. Kalász

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

A novel acetylcholinesterase (AChE) reactivator, a bispyridinium aldoxime named K048, was first synthesized in 2003. It is a promising antidote against tabun poisoning. Afterwards, other studies on several cholinesterases (ChE) of different species (humans, rats, etc.) and models (in vitro or in vivo) were conducted. We tested this oxime against nine different AChE inhibitors using in vitro tests on rat brain homogenate as source of enzyme. Our results showed that oxime K048 reached promising reactivation activity in case of all tested AChE inhibitors, except cyclosarin, at oxime concentration 10-3 M. At a concentration of 10-5 M, which is more common for human use, only methylchlorpyrifos-inhibited AChE was reactivated.

Original languageEnglish
Pages (from-to)1-5
Number of pages5
JournalMedicinal Chemistry
Volume6
Issue number1
DOIs
Publication statusPublished - Jan 2010

Fingerprint

Oximes
Acetylcholinesterase
Cholinesterase Inhibitors
Antidotes
Cholinesterases
Poisoning
Brain
Enzymes
In Vitro Techniques

Keywords

  • Acetylcholinesterase
  • Antidote
  • K048
  • Nerve agent
  • Oxime
  • Pesticide
  • Reactivator

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Novel acetylcholinesterase reactivator - Oxime K048 - Reactivation activity in vitro. / Kuca, Kamil; Marek, Jan; Zdarova-Karasova, Jana; Pohanka, Miroslav; Korabecny, Jan; Kalász, H.

In: Medicinal Chemistry, Vol. 6, No. 1, 01.2010, p. 1-5.

Research output: Contribution to journalArticle

Kuca, Kamil ; Marek, Jan ; Zdarova-Karasova, Jana ; Pohanka, Miroslav ; Korabecny, Jan ; Kalász, H. / Novel acetylcholinesterase reactivator - Oxime K048 - Reactivation activity in vitro. In: Medicinal Chemistry. 2010 ; Vol. 6, No. 1. pp. 1-5.
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