Опубликовать статью

Информационное партнерство

Инфоресурсы

Контакты

«

Vol. 11, Art. 29 (pp. 348-361)    |    2010       

»

The action of carboxime on isolated smooth muscle of the cat's trachea in conditions of acetylcholinesterase inhibition by soman and VX

Nechiporenko S.P., Sanotsky V.I., Shabunova I.A.

Brief summary

The action of carboxime, reactivator of acetylcholinesterase (AChE), on cholinergic transmission was studied in the cat's smooth muscle preparation of trahea exposed to organophosphate AChE inhibitors soman and VX. It was found that carboxime at concentrations 10-6-10-5 M propossed the features of reversible AChE inhibitor, and at high concentrations revealed of cholinergic M-antagonist activity with Кd 5·10-5 М. The pretreatment with the reversible inhibitor AChE aminostigmine increases the ability of carboxime to eliminate the spontaneous contractions of smooth muscles caused by soman and VX. The reactivator, reversible inhibitor and М-cholinolytic properties in complex play the important role in high antidote efficacy of carboxime to organophosphate poisoning.


Key words

acetylcholinesterase, reactivators, muscarinic receptors, ogranophosphates, soman, VX, antidotes

Reference list

1. Glyhan E. N., Smetanin A. V., Kazakov P. V. i dr. Veroyatnostnaya ocenka riska kak pokazatel ekologicheskoi bezopasnosti na primere obekta po ynichtojeniu himicheskogo oryjiya.. // Ros. him. j. (J. Ros. him. ob-va im. D.I. Mendeleeva). — 2007. — T. 51, № 2. — S. 52–54.


2. Watson A., Opresko D., Young R. et al. Organophosphate Nerve Agents / In: “Handbook of Toxicology of Chemical Warfare Agents”, Ed. by R.C.Gupta. — Oxford: Elsevier, 2009. – P. 43-67.


3. Tetsu Okumura, Kenji Taki, Kouichiro Suzuki, Tetsuo Satoh. The Tokyo Subway Sarin Attack: Toxicological Whole Truth / In: “Handbook of Toxicology of Chemical Warfare Agents”, Ed. by R.C.Gupta. — Oxford: Elsevier, 2009. — P. 25-32.


4. Kolbasov S. E., Nechiporenko S. P. Antidotnaya terapiya na dogospitalnom etape okazaniya medicinskoi pomoshi pri obespechenii processov ynichtojeniya himicheskogo oryjiya v Rossiiskoi federacii / Tezisi Ros. naych. konf. «Problemi standartizacii i vnedreniya sovremennih diagnosticheskih i lechebnih tehnologii v prakticheskoi toksikologicheskoi pomoshi postradavshim ot ostrih himicheskih vozdeistvii». — Ekaterinbyrg, 2008. — S. 58.


5. Nechiporenko S. P., Zatsepin E. P. A Study to establish an efficient means for delivering antidotal therapy at nerve agent destruction facillies. // J. Toxicol. Clin. Toxicol. 2003. — Vol. 41, № 5. — P. 723.


6. Petrov A. N., Sofronov G. A., Nechiporenko S. P. Antidoti fosfororganicheskih otravlyaushih veshestv. // Ros. him. j. (J. him. ob-va im. D.I. Mendeleeva). — 2004. — T. 48, № 2. — S. 110–116.


7. Prozorovskii V. B., Skopichev V. G., Panchenkova O. A. Ocenka reaktivatora holinesterazi karboksima kak sredstva profilaktiki otravlenii fosfororganicheskimi ingibitorami holinesteraz. //Psihofarmakol. biol. narkol. — 2008. — T. 8, № 3–4. — S. 2457–2462.


8. Arunlakshana O., Schild H. O. Some quantitative uses of drug antagonists // Br. J. Pharmacol. Chemother. — 1959. — V. 14, № 1. — P. 48–58.


9. Aas P., Veiteberg T., Fonnum F. In vitro effects of soman on bronchial smooth muscle //Biochem. Pharmacol. —1986. —V. 35, № 11. — P. 1793-1799.


10. Aas P., Walday P., Tansø R., Fonnum F. The effect of acetylcholinesterase-inhibition on the tonus of guinea-pig bronchial smooth muscle // Biochem. Pharmacol. — 1988. — V. 37, № 21. — P. 4211-4216.


11. Sanotsky V. I. The acetylcholine leakage as a cause of toxic effects of organophosphorus cholinesterase inhibitors. // Acta poloniae toxicological. — 1993. — V.1, suppl.1. — P. 12- 13.


12. 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. — V. 442, № 3. — P. 279-287.


13. Soukup O ., Pohanka M., Tobin G. et al. The effect of HI-6 on cholinesterases and on the cholinergic system of the rat bladder // Neuro Endocrinol. Lett. — 2008. — V.29, №5. — P. 759-762.