In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases

. 2007 Feb ; 11 (2) : 101-6.

Jazyk angličtina Země Spojené státy americké Médium print

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/pmid17449453

In this work, two oximes for the treatment of tabun-inhibited acetylcholinesterase (AChE; EC 3.1.1.7), K074 (1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide) and K075 ((E)-1,4-bis(4-hydroxyiminomethylpyridinium)but-2-en dibromide), were tested in vitro as reactivators of AChE. Comparison was made with currently used AChE reactivators (pralidoxime, HI-6, methoxime and obidoxime). Human brain homogenate was taken as an appropriate source of the cholinesterases. As resulted, oxime K074 appears to be the most potent reactivator of tabun-inhibited AChE, with reactivation potency comparable to that of obidoxime. A second AChE reactivator, K075, does not attain as great a reactivation potency as K074, although its maximal reactivation (17%) was achieved at relevant concentrations for humans.

Zobrazit více v PubMed

Adv Clin Chem. 2004;38:151-216 PubMed

Arch Toxicol. 1996;70(8):497-503 PubMed

Neurotox Res. 2006 Jan;9(1):59-62 PubMed

J Toxicol Clin Toxicol. 2002;40(6):803-16 PubMed

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2914-7 PubMed

Bioorg Med Chem Lett. 2006 Feb;16(3):622-7 PubMed

J Enzyme Inhib Med Chem. 2003 Dec;18(6):529-35 PubMed

Pharmacol Toxicol. 1999 Jan;84(1):41-5 PubMed

Hum Exp Toxicol. 1999 Sep;18(9):560-5 PubMed

Mini Rev Med Chem. 2006 Mar;6(3):269-77 PubMed

J Appl Toxicol. 2005 Nov-Dec;25(6):491-5 PubMed

Neurotox Res. 2006 Jan;9(1):39-45 PubMed

J Enzyme Inhib Med Chem. 2005 Jun;20(3):233-7 PubMed

Biochem Pharmacol. 1989 Feb 15;38(4):633-40 PubMed

FEBS Lett. 1970 Oct 5;10(3):182-184 PubMed

Basic Clin Pharmacol Toxicol. 2004 Aug;95(2):81-6 PubMed

Drug Chem Toxicol. 1995 May-Aug;18(2-3):119-36 PubMed

Neurotox Res. 2004;6(7-8):565-70 PubMed

Arch Toxicol. 1999 Feb;73(1):7-14 PubMed

Chem Biol. 2003 Jun;10(6):491-502 PubMed

J Enzyme Inhib Med Chem. 2005 Oct;20(5):409-15 PubMed

Toxicology. 1999 Feb 15;132(2-3):111-8 PubMed

Neurotox Res. 2006 Jun;9(4):291-6 PubMed

Biochem Pharmacol. 2004 Dec 1;68(11):2237-48 PubMed

Najít záznam

Citační ukazatele

Nahrávání dat ...

Možnosti archivace

Nahrávání dat ...