Novel acetylcholinesterase reactivator K112 and its cholinergic properties

Biomedicine and Pharmacotherapy

Volumn 64, Issue 8, 2010, Pages 541-545

  Soukup, O ^a   Kristofikova, Z ^d   Proska, J ^e   Tobin, G ^f   Patocka, J ^g   Marek, J ^a   Jun, D ^a,b   Fusek, J ^a   Ripova, D ^d   Kuca, K ^a,b,c  

^a UNIVERSITY OF DEFENCE   (Czech Republic)

^b UNIVERSITY OF DEFENCE   (Czech Republic)

^c J E PURKINJE UNIVERSITY   (Czech Republic)

^d NATIONAL INSTITUTE OF MENTAL HEALTH   (Czech Republic)

^e CZECH TECHNICAL UNIVERSITY IN PRAGUE   (Czech Republic)

^f UNIVERSITY OF GOTHENBURG   (Sweden)

^g UNIVERSITY OF SOUTH BOHEMIA   (Czech Republic)

Author keywords

Cholinergic system; Non reactivation; Organophosphate

Indexed keywords

4,40 BIS(HYDROXYIMINOMETHYL) 1,10 (1,2 PHENYLENEDIMETHYL)BISPYRIDINIUM DIBROMIDE; ACETYLCHOLINE; ACETYLCHOLINESTERASE; CHOLINESTERASE REACTIVATOR; K 112; MEMBRANE PROTEIN; MUSCARINIC M2 RECEPTOR; MUSCARINIC RECEPTOR; ORGANOPHOSPHATE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTICHOLINERGIC EFFECT; ARTICLE; BLADDER; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME REACTIVATION; HEART; IC 50; IN VITRO STUDY; MALE; MEMBRANE FLUIDITY; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BLOCKING;

ACETYLCHOLINESTERASE; ANIMALS; CHOLINESTERASE INHIBITORS; CHOLINESTERASE REACTIVATORS; DOSE-RESPONSE RELATIONSHIP, DRUG; HEART; HEART RATE; HIPPOCAMPUS; MEMBRANE FLUIDITY; MUSCLE CONTRACTION; MUSCLE, SMOOTH; ORGANOPHOSPHORUS COMPOUNDS; OXIMES; POISONING; PROTEIN BINDING; PYRIDINIUM COMPOUNDS; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTOR, MUSCARINIC M2; RECOMBINANT PROTEINS; SWINE; SYNAPTOSOMES; URINARY BLADDER;

EID: 77956875837     PISSN: 07533322     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.biopha.2010.01.002     Document Type: Article

References (22)

1. Marrs T.C. Organophosphate poisoning. Pharmacol Ther 1993, 58:51-66.
2. Patocka J., Kuca K., Jun D. Acetylcholinesterase and butyrylcholinesterase - important enzymes of human body. Acta Medica (Hradec Kralove) 2004, 47:215-228.
3. Bajgar J. Organophosphates/nerve agent poisoning: mechanism of action, diagnosis, prophylaxis, and treatment. Adv Clin Chem 2004, 38:151-216.
4. Kassa J. Review of oximes in the antidotal treatment of poisoning by organophosphorus nerve agents. J Toxicol Clin Toxicol 2002, 40:803-816.
5. Tattersall J.E. Ion channel blockade by oximes and recovery of diaphragm muscle from soman poisoning in vitro. Br J Pharmacol 1993, 108:1006-1015.
6. van Helden H.P., Busker R.W., Melchers B.P., Bruijnzeel P.L. Pharmacological effects of oximes: how relevant are they?. Arch Toxicol 1996, 70:779-786.
7. Alkondon M., Albuquerque E.X. The nonoxime bispyridinium compound SAD-128 alters the kinetic-properties of the nicotinic acetylcholine-receptor ion channel - a possible pechanism for antidotal effects. J Pharmacol Exp Ther 1989, 250:842-852.
8. Musilek K., Kuca K., Jun D., Dohnal V., Dolezal M. Synthesis of a novel series of bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase. J Enzyme Inhib Med Chem 2005, 20:409-415.
9. Musilek K., Holas O., Kuca K., Jun D., Dohnal V., Dolezal M. Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. J Enzyme Inhib Med Chem 2007, 22:425-432.
10. Hrabinova M., Musilek K., Jun D., Kuca K. New group of xylene linker-containing acetylcholinesterase reactivators as antidotes against the nerve agent cyclosarin. J Enzyme Inhib Med Chem 2006, 21:515-519.
11. Loke W.K., Sim M.K., Go M.L. O-substituted derivatives of pralidoxime: muscarinic properties and protection against soman effects in rats. Eur J Pharmacol 2002, 442:279-287.
12. Tucek S. Regulation of acetylcholine synthesis in the brain. J Neurochem 1985, 44:11-24.
13. --dependent neurotransmitter transporters: drugs, substrates, presynaptic receptors, and signaling systems. Pharmacol Ther 2001, 92:21-55.
14. Ellman G.L., Courtney K.D., Andres V., Featherstone R.M. A new and rapid colorimetric determination of acetylcholinesterase activity. Biochem Pharmacol 1961, 7. 88-&.
15. Giglio D., Aronsson P., Eriksson L., Tobin G. In vitro characterization of parasympathetic and sympathetic responses in cyclophosphamide-induced cystitis in the rat. Basic Clin Pharmacol Toxicol 2007, 100:96-108.
16. Ogura H., Kosasa T., Kuriya Y., Yamanishi Y. Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol 2000, 22:609-613.
17. Musilkova J., Tucek S. The binding of cholinesterase-inhibitors tacrine (terahydroaminoacridine) and 7-methoxytacrine to muscarinic acetylcholine-receptors in rat-brain in the presence of eserine. Neurosci Lett 1991, 125:113-116.
18. Trankle C., Dittmann A., Schulz U., Weyand O., Buller S., Johren K., et al. Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors. Mol Pharmacol 2005, 68:1597-1610.
19. Soukup O., Pohanka M., Tobin G., Jun D., Fusek J., Musilek K., et al. The effect of HI-6 on cholinesterases and on the cholinergic system of the rat bladder. Neuro Endocrinol Lett 2008, 29:759-762.
20. Oydvin O.K., Tanso R., Aas P. Pre-junctional effects of oximes on H-3-acetylcholine release in rat hippocampal slices during soman intoxication. Eur J Pharmacol 2005, 516:227-234.
21. Lundy P.M., Raveh L., Amitai G. Development of the bisquaternary oxime HI-6 toward clinical use in the treatment of organophosphate nerve agent poisoning. Toxicol Rev 2006, 25:231-243.
22. Hamilton M.G., Lundy P.M. HI-6 therapy of soman and tabun poisoning in primates and rodents. Arch Toxicol 1989, 63:144-149.