Novel Acetylcholinesterase Reactivator – Oxime K048 – Reactivation Activity In Vitro

Title: Novel Acetylcholinesterase Reactivator – Oxime K048 – Reactivation Activity In Vitro

Volume: 6 Issue: 1

Author(s): Kamil Kuca, Jan Marek, Jana Zdarova-Karasova, Miroslav Pohanka, Jan Korabecny and Huba Kalasz

Affiliation:

Keywords: Oxime, reactivator, K048, nerve agent, pesticide, acetylcholinesterase, antidote

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.

Cite this article as:

Kuca Kamil, Marek Jan, Zdarova-Karasova Jana, Pohanka Miroslav, Korabecny Jan and Kalasz Huba, Novel Acetylcholinesterase Reactivator – Oxime K048 – Reactivation Activity In Vitro, Medicinal Chemistry 2010; 6 (1) . https://dx.doi.org/10.2174/157340610791208709