Comparison of Effects Anylocaine and Lidocaine on Ionic Channels of Isolated Neurones of Mollusc



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Abstract

: It was shown that local anesthetics anylocaine and lidocaine in concentration 0.1, 1, 10,100 and 1000 µM in dose-dependent manner suppressed sodium and potassium currents. The amplitude slow potassium currents after action of anesthetics in low concentration (from 0.1 up to 10 µM) grew by 5-10 % in comparison with the control, and after over higher doses was reduced. In concentration 1000 µM the amplitude of all ionic currents was reduced approximately on 50 %, i.e. it was not revealed selectivity of action of the investigated substances on ionic channels. Membranotropic action of anylocaine and lidocaine on neurons can be realized also through influence on nonspecific conductivity of membrane, potential of a superficial charge of membrane near to ionic channels, kinetics of activation or inactivation of ionic currents. Anylocaine by 10-15 % more suppressed sodium and potassium ionic currents than lidocaine, and rendered longer post actions, i.e. more strongly contacted with ionic channels.

About the authors

Nadezhda Pavlovna Lisitsyna

Tat'yana Aleksandrovna Petropavlovskaya

Irina Leonidovna Cherednik

Yuriy Dmitrievich Ignatov

Vladimir Ivanovich Pantsurkin

Anatoliy Ivanovich Vislobokov

Konstantin Nikolaevich Mel'nikov

Vera Anatol'evna Borisova

N P Lisitsyna

Kuban State Medical University

Kuban State Medical University

T A Petropavlovskaja

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

I L Cherednik

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

Yu D Ignatov

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

V I Pantsurkin

Perm State Pharmaceutical Academy

Perm State Pharmaceutical Academy

A I Vislobokov

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

К N Melnikov

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

V А Borisova

I.P. Pavlov State Medical University

I.P. Pavlov State Medical University

References

  1. Вислобоков А.И., Зайцев А.А., Игнатов Ю.Д., Савоськин А.Л. Мембранные механизмы действия на нервные клетки анестетиков, аналгетиков и противоаритмических средств. // Мед. акад. вестник. 2001. Т. 1, № 1. С. 25-33.
  2. Вислобоков А.И., Игнатов Ю.Д., Мельников К.Н. Фармакологическая модуляция ионных каналов мембраны нейронов. СПб.: Издательство СПбГМУ, 2006. 288 с.
  3. Галенко-Ярошевский А.П., Хоронько В.В., Пономарев В.В., и др. Многосторонность аспектов действия местных анестетиков. // Бюл. эксперим. биол. и мед. 2005. Т. 140, № 9. С. 28-
  4. Костюк П.Г., Крышталь О.А. Механизмы электрической возбудимости нервной клетки. М., 1981. 204 с.
  5. Панцуркин В.И., Алексеева И.В. Анилокаин, поиск, свойства. Начальный опыт применения лекарственных форм в медицинской практике: Монография. Пермь: ГОУ ВПО «ПГФА Росздрава», 2006. 173 с.
  6. Decher N., Pirard B., Bundis F., et al. Molecular basis for Kv1. 5 channel block: conservation of drugs binding sites among voltage-gated K+ channels. // J. Biol. Chem. 2004. Vol. 279, N 1. P. 394-400.
  7. Miller K.W. The nature of sites of general anaesthetic action. // Br.J. Anaesth. 2002. Vol. 89, N 1. P. 17-31.
  8. Nerbonne J.M. Molecular basis of functional voltage-gated K+ channel diversity in the ammalian myocardium. // J. Physiol. 2000. Vol. 525, N 2. P. 285-298.
  9. Nilsson J., Madeja M., Arhem P. Local anesthetic block of Kv channels: role of the S6 helix and the S5-S6 linker for bupivacaine action. // Mol. Pharmacol. 2003. Vol. 63. P. 1417-1429.
  10. Shimooka T., Shibata A., Terada H. The local anesthetic tetracaine destabilizes membrane structure by interaction with polar headgroups of phospholipids. // Bioch. et Bioph. Acta. 1992. Vol. 1104, N 2. P. 261-268.
  11. Sugiyama K., Muteki T. Local anesthetics depress the calcium current of rat sensory neurons in culture. // Anesthesiology. 1994. Vol. 80, N 6. P. 369-378.
  12. Yarov-Yarovoy V., Brown J., Sharp E.M., et al. Molecular determinants of voltage-dependent gating and binding of pore-blocking drugs in transmembrane segment IIIS6 of the Na(+) channel alpha subunit. // J. Biol. Chem. 2001. Vol. 5, N 276(1). P. 20-27.

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