Local Anesthetics: Interaction With Biological Membranes And With The Voltage-gated Sodium Channel [anestésicos Locais: Interação Com Membranas Biológicas E Com O Canal De Sódio Voltagem-dependente]

Many theories about the mechanism of action of local anesthetics (LA) are described in the literature. Two types of theories can be distinguished: those that focus on the direct effects of LA on their target protein in the axon membranes, i.e. the voltage-gated sodium channel and the ones that take into account the interaction of anesthetic molecules with the lipid membrane phase for the reversible nerve blockage. Since there is a direct correlation between LA hydrophobicity and potency, it is crucial to take this physico-chemical property into account to understand the mechanism of action of LA, be it on the sodium channel protein, lipid(s), or on the whole membrane phase.31717751783Gupta, S.P., (1991) Chem. Rev, 91, p. 1109Lochynski, S., Frackwiak, B., Librowski, T., Czarnecki, R., Grochowski, J., Serda, P., Pasenkiewicz-Gierula, M., (2002) Tetrahedron, 13, p. 873de Araújo, D.R., Pinto, L.M.A., Braga, A.F.A., de Paula, E., (2003) Rev. Bras. Anestesiol, 53, p. 663Covino, B.G., Vassalo, H.G., (1985) Anestésicos Locais: Mecanismos de ação e uso clínico, , Grune and Stratton: New YorkGuyton, A. C.Hall, J. E.Tratado de Fisiologia Médica, Guanabara Koogan S.A.: Rio de Janeiro, 1996de Jong, R.H., (1994) Local Anesthetics, , C.C. Thomas: SpringfieldMartin, D.G., Watson, C.E., Gold, M.B., Woodard, C.L., Baskin, S.I., (1995) J. Appl. Toxicol, 15, p. 153Tucker, G.T., Mather, L.E., (1975) Br. J. Anaesth, 213, p. 224Fraceto, L.F., Oyama-Jr, S., Nakaie, C.R., Spisni, A., de Paula, E., Pertinhez, T.A., (2006) Biophys. Chem, 123, p. 29Malheiros, S.V.P., Gottardo, L., Pinto, L.M.A., Yokaichiya, D.K., Fraceto, L.F., Meirelles, N.C., de Paula, E., (2004) Biophys. Chem, 100, p. 213Malamed, S.F., (2001) Manual de anestesia local, , 4a ed, Guanabara Koogan: Rio de JaneiroStrichartz, G.R., Ritchie, J.M., (1987) Local Anesthetics, Handbook of Experimental Pharmacology, , Springer-Verlag: Berlinde Paula, E., Schreier, S., (1996) Braz. J. Med. Biol. Res, 29, p. 877Arias, H.R., (1998) Biochim. Biophys. Acta, 1376, p. 173Slater, J.S., Kelly, M.B., Larkin, J.D., Ho, C., Mazurek, A., Taddeo, F.J., Yeager, M.D., Stubbs, C.D., (1997) J. Biol. Chem, 272, p. 6167Kalipatnapu, S., Chattopadhyay, A., (2004) Cell. Mol. Neurobiol, 24, p. 403Hirata, M., Sakaguchi, M., Mochida, C., Sotozono, C., Kageyama, K., Kuroda, Y., Hirose, M., (2004) Anesthesiology, 100, p. 1206Cohen, S.P., Mao, J., (2003) Acta. Anaesthesiol. Scand, 47, p. 910Hodgkin, A.L., Huxley, A.F., (1952) J. Physiol, 117, p. 500Narahashi, T., Yamada, M., (1969) Nature, 223, p. 748Frazier, D.T., Narahashi, T., Yamada, M., (1970) J. Pharmacol. Exp. Ther, 171, p. 45Pinto, L.M.A., Yokaichiya, D.K., Fraceto, L.F., de Paula, E., (2000) Biophys. Chem, 87, p. 213Noda, M., Ideda, M., Kayana, T., Suzuki, H., Takeshima, H., Kurasaki, M., Takahashi, H., Numa, S., (1986) Nature, 320, p. 188Ragsdale, D.S., McPhee, J.C., Scheuer, R., Catterall, W.A., (1994) Science, 265, p. 1724Ragsdale, D.S., McPhee, J.C., Scheuer, R., Catterall, W.A., (1996) Proc. Natl. Acad. Sci. U.S.A, 93, p. 9270Hille, B., (1977) J. Gen. Physiol, 69, p. 497Hondeghem, L.M., Katzung, B.G., (1977) Biochim. Biophys. Acta, 472, p. 373Starmer, C.F., (1987) Biophys. J, 52, p. 405O'Reilly, J.P., (1999) J. Physiol, 515, p. 61Lee, A.G., (1976) Biochim. Biophys. Acta, 448, p. 34Skou, J.C., (1954) Acta Pharmacol. Toxicol, 10, p. 317Seeman, P., (1996) Biochem. Pharmacol, 15, p. 1753Seelig, A., (1987) Biochim. Biophys. Acta, 899, p. 196Trudell, J.R., (1977) Anesthesiology, 46, p. 5Gallová, J., Balgavý, P., (1997) Biochim. Biophys. Acta, 1325, p. 189Hill, M.W., (1974) Biochim. Biophys. Acta, 356, p. 117Lee, A.G., (1976) Nature, 262, p. 545Lee, A.G., (1978) Biochim. Biophys. Acta, 514, p. 95Ueda, I., Tashiro, C., Arakawa, K., (1977) Anesthesiology, 46, p. 327Schopflin, M., Fingeli, U.P., Perlia, X., (1987) J. Am. Chem. Soc, 109, p. 2375Auger, M., Jarrel, H.C., Smith, I.C.P., Wong, P.T.T., Siminovitch, D.J., Mantsch, H.H., (1987) Biochemistry, 26, p. 8513Auger, M., Smith, I.C.P., Mantsch, H.H., Wong, P.T.T., (1990) Biochemistry, 29, p. 2008Lever, M.J., Miller, K.W., Paton, W.D.M., Smith, E.B., (1971) Nature, 231, p. 368Bradley, D.J., Richards, C.D., (1984) Br. J. Pharmacol, 81, p. 161Fraceto, L.F., de Paula, E., (2006) Rev. Ciênc. Farm. Basica Apl, 27, p. 27Sikaris, K.A., Sawyer, W.H., (1982) Biochem. Pharmacol, 31, p. 2625Hutterer, R., Kramir, K., Schneider, F.W., Hof, M., (1997) Chem. Phys. Lipids, 90, p. 11Gargiulo, R.J., Giotta, G.J., Wang, H.H., (1973) J. Med. Chem, 16, p. 707Giotta, G.J., Chan, D.S., Wang, H.H., (1974) Arch. Biochem. Biophys, 163, p. 453Schreier, S., Frezzatti Jr., W.A., Araujo, P.S., Chaimovich, H., Cuccovia, I.M., (1984) Biochim. Biophys. Acta, 769, p. 231Schreier, S., Amaral, A.T., Stachissini, A.S., Bianconi, M.L., (1986) Bull. Magn. Res, 8, p. 166Frezatti Jr., W.A., Toselli, W.R., Schreier, S., (1986) Biochim. Biophys. Acta, 1235, p. 189de Paula, E., Schreier, S., (1985) Biochim. Biophys. Acta, 1240, p. 25Fraceto, L.F., Pinto, L.M.A., Franzoni, L., Braga, A.A.C., Spisni, A., Schreier, S., de Paula, E., (2002) Biophys. Chem, 99, p. 229Hauser, H., Dawson, R.M.C., (1968) Biochem. J, 109, p. 909Cerbon, J., (1972) Biochim. Biophys. Acta, 290, p. 51Darke, A., Finer, E.G., Flook, A.G., Phillips, M.C., (1972) J. Mol. Biol, 63, p. 265Finer, E.G., Flook, A.G., Hauser, H., (1972) Biochim. Biophys. Acta, 260, p. 49Lee, A.G., Birdsall, J.M., Levine, Y.K., Metcalfe, J.C., (1972) Biochim. Biophys. Acta, 255, p. 43Boulanger, Y., Schreier, S., Leitch, L.C., Smith, I.C.P., (1980) Can. J. Biochem, 58, p. 986Boulanger, Y., Schreier, S., Smith, I.C.P., (1981) Biochemistry, 20, p. 6824Westman, J., Boulanger, Y., Ehrenberg, A., Smith, I.C.P., (1982) Biochim. Biophys. Acta, 685, p. 315Browning, J.L., Akutsu, H., (1982) Biochim. Biophys. Acta, 684, p. 172Kelusky, E.C., (1983) Tese de Doutorado, , University of Ottawa, CanadaKelusky, E.C., Smith, I.C.P., (1984) Can. J. Biochem. Cell. Biol, 62, p. 178Kuroda, Y., Ogawa, M., Nasu, H., Terashima, M., Kasahara, M., Kiyama, Y., Wakita, M., Nakagawa, T., (1996) Biophys. J, 71, p. 1911Yokono, S., Ogli, K., Miura, S., Ueda, I., (1989) Biochim. Biophys. Acta, 982, p. 300Kuroda, Y., Fujiwara, Y., (1987) Biochim. Biophys. Acta, 903, p. 395Wakita, M., Kuroda, Y., Fujiwara, Y., Nakagawa, T., (1992) Chem. Phys. Lipids, 62, p. 45Lissi, E., Bianconi, M.L., Amaral, A.T., de Paula, E., Blanch, L.E.B., Schreier, S., (1990) Biochim. Biophys. Acta, 1021, p. 46Godwin, S.A., Cox, J.R., Wright, S.N., (2005) Biophys. Chem, 113, p. 1Catterall, W.A., (1992) Physiol. Rev, 72, p. 515Fozzard, H.A., Hanck, D.A., (1996) Physiol. Rev, 76, p. 887Marban, E., Yamagish, T., Tomaselli, F., (1998) J. Physiol, 508, p. 647Lai, J., Porreca, F., Hunter, J.C., Gold, M.S., (2004) Annu. Rev. Pharmacol. Toxicol, 44, p. 371Hamill, O.P., Marty, A., Neher, E., Sakmann, B., Sigworth, F.J., (1981) Pfluegers Arch, 391, p. 85Scheuer, T., (1999) J. Gen. Physiol, 113, p. 3Doyle, A.D., Cabral, J.M., Pfuetzner, R.A., Kuo, A., Gubbis, J.M., Cohen, S.L., Chait, B.T., (1998) Science, 280, p. 69Rohl, C.A., Boeckman, F.A., Baker, C., Scheuer, T., Catterall, W.A., Klevit, R.E., (1999) Biochemistry, 38, p. 855Yarov-Yarovoy, V., McPhee, J.C., Idsvoog, D., Pate, C., Scheuer, T., Catterall, W.A., (2002) J. Biol. Chem, 277, p. 35393Cestéle, S., Catterall, W.A., (2000) Biochimie, 82, p. 883Grant, A.O., (2001) Am. J. Medicine, 110, p. 296Balser, J.R., (1999) Cardiovasc. Res, 42, p. 327Scholz, A., (2002) Br. J. Anesth, 89, p. 52Ogata, N., Ohishi, Y., (2002) Jpn. J. Pharmacol, 88, p. 365Ragsdale, D.S., Avoli, M., (1998) Brain Res. Revs, 26, p. 16Katz, A.M., (1998) Am. J. Med, 104, p. 179Nau, C., Wang, G.K., (2004) J. Membrane Biol, 201, p. 1Patton, D.E., West, J.W., Catterall, W.A., Goldin, A.L., (1992) Proc. Natl Acad. Sci. U.S.A, 89, p. 10905Zamponi, G.W., French, R.J., (1994) Biophys. J, 67, p. 1040Wang, G.K., Quan, C., Wang, S., (1998) Eur. J. Phys, 435, p. 293Li, H.L., Galue, A., Meadows, L., Ragsdale, D.S., (1999) Mol. Pharmacol, 55, p. 134Kondratiev, A., Tomaselli, G.F., (2003) Mol. Pharmacol, 64, p. 741Bennett, G., Deer, T., Stuart, D.P., Rauck, R., Yaksh, T., Hassenbusch, S.J., (2000) J. Pain Symp. Manag, 20, p. 44McPhee, J.C., Ragsdale, D.S., Scheuer, T., Catterall, W.A., (1998) J. Biol. Chem, 270, p. 12025McPhee, J.C., Ragsdale, D.S., Scheuer, T., Catterall, W.A., (1996) Proc. Natl. Acad. Sci. U.S.A, 93, p. 9270Mitrovic, N., Lerche, H., Heine, R., Fleischhauer, R., Pika-Hartlaub, U., Hartlaub, U., George, A.L., Lehmann-Horn, F., (1996) Neurosci. Lett, 214, p. 9Tang, L., Kallen, R.G., Horn, R., (1996) J.Gen. Physiol, 108, p. 89Lerche, H., Peter, W., Fleischhauser, R., Pika-Hartlaub, U., Malina, T., Mitrovic, N., Lehmann-Horn, F., (1997) J. Physiol, 505, p. 345Filatov, G.N., Nguyen, T.P., Kraner, S.D., Barchi, R.L., (1998) J. Gen. Physiol, 111, p. 703Yang, R.H., (1995) Neuron, 15, p. 213Yang, N., George, A.L., Horn, R., (1996) Neuron, 16, p. 113Miyamoto, K., Nakagawa, T., Kuroda, Y., (2001) J. Peptide Res, 58, p. 193Skidmore, R.A., Patterson, J.D., Tomsick, R.S., (1996) Dermatol. Surg, 22, p. 511Butterworth, J.F., Strichartz, G.R., (1990) Anesthesiology, 72, p. 711Sunami, A., Dudley, S.C., Fozzard, H.A., (1997) Proc. Natl Acad. Sci. U.S.A, 94, p. 1412