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Volumn 112, Issue 5, 1998, Pages 611-621

Delimiting the binding site for quaternary ammonium lidocaine derivatives in the acetylcholine receptor channel

Author keywords

Cysteine mutagenesis; Methanethiosulfonate; Open channel block; Reaction kinetics

Indexed keywords

2 AMINOETHYLMETHANE THIOSULFONIC ACID; ACETYLCHOLINE; CHOLINERGIC RECEPTOR; CYSTEINE; GLUTAMIC ACID; LEUCINE; LIDOCAINE DERIVATIVE; LIDOCAINE ETHOBROMIDE; N [(2,6 DIMETHYLPHENYL)CARBAMOYLMETHYL]TRIMETHYLAMMONIUM; QUATERNARY AMMONIUM DERIVATIVE; RECEPTOR SUBUNIT; SERINE; SULFONIC ACID DERIVATIVE; TRIMETHYLAMMONIUM SALT DERIVATIVE; UNCLASSIFIED DRUG; VALINE;

EID: 0031772578     PISSN: 00221295     EISSN: None     Source Type: Journal    
DOI: 10.1085/jgp.112.5.611     Document Type: Article
Times cited : (36)

References (51)
  • 1
    • 0017104508 scopus 로고
    • Drug blockade of open end-plate channels
    • Adams, P.R. 1976. Drug blockade of open end-plate channels. J. Physiol. (Camb.). 260:532-552.
    • (1976) J. Physiol. (Camb.) , vol.260 , pp. 532-552
    • Adams, P.R.1
  • 2
    • 0028809730 scopus 로고
    • Identification of acetylcholine receptor channel-lining residues in the MI segment of the alpha subunit
    • Akabas, M.H., and A. Karlin. 1995. Identification of acetylcholine receptor channel-lining residues in the MI segment of the alpha subunit. Biochemistry. 34:12496-12500.
    • (1995) Biochemistry , vol.34 , pp. 12496-12500
    • Akabas, M.H.1    Karlin, A.2
  • 3
    • 0027987062 scopus 로고
    • Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the alpha subunit
    • Akabas, M.H., C. Kaufmann, P. Archdeacon, and A. Karlin. 1994. Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the alpha subunit. Neuron. 13:919-927.
    • (1994) Neuron. , vol.13 , pp. 919-927
    • Akabas, M.H.1    Kaufmann, C.2    Archdeacon, P.3    Karlin, A.4
  • 4
    • 0026485739 scopus 로고
    • Acetylcholine receptor channel structure probed in cysteine-substitution mutants
    • Akabas, M.H., D.A. Stauffer, M. Xu, and A. Karlin. 1992. Acetylcholine receptor channel structure probed in cysteine-substitution mutants. Science. 258:307-310.
    • (1992) Science , vol.258 , pp. 307-310
    • Akabas, M.H.1    Stauffer, D.A.2    Xu, M.3    Karlin, A.4
  • 5
    • 0025856536 scopus 로고
    • Neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes have a pentameric quaternary structure
    • Anand, R., W.G. Conroy, R. Schoepfer, P. Whiting, and J. Lindstrom. 1991. Neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes have a pentameric quaternary structure. J. Biol. Chem. 266:11192-11198.
    • (1991) J. Biol. Chem. , vol.266 , pp. 11192-11198
    • Anand, R.1    Conroy, W.G.2    Schoepfer, R.3    Whiting, P.4    Lindstrom, J.5
  • 6
    • 0018199153 scopus 로고
    • The mode of action of antagonists of the excitatory response to acetylcholine in Aplysia neurones
    • Ascher, P.R., A. Marty, and T.O. Neild. 1978. The mode of action of antagonists of the excitatory response to acetylcholine in Aplysia neurones. J. Physiol. (Camb.). 278:207-235.
    • (1978) J. Physiol. (Camb.) , vol.278 , pp. 207-235
    • Ascher, P.R.1    Marty, A.2    Neild, T.O.3
  • 8
    • 0025355129 scopus 로고
    • An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor
    • Charnet, P., C. Labarca, R.J. Leonard, N.J. Vogelaar, L. Czyzyk, A. Gouin, N. Davidson, and H.A. Lester. 1990. An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor. Neuron. 4:87-95.
    • (1990) Neuron. , vol.4 , pp. 87-95
    • Charnet, P.1    Labarca, C.2    Leonard, R.J.3    Vogelaar, N.J.4    Czyzyk, L.5    Gouin, A.6    Davidson, N.7    Lester, H.A.8
  • 9
    • 0021284542 scopus 로고
    • Trifluoperazine reduces inward ionic currents and secretion by separate mechanisms in bovine chromaffin cells
    • Clapham, D.E., and E. Neher. 1984. Trifluoperazine reduces inward ionic currents and secretion by separate mechanisms in bovine chromaffin cells. J. Physiol. (Camb.). 353:541-564.
    • (1984) J. Physiol. (Camb.) , vol.353 , pp. 541-564
    • Clapham, D.E.1    Neher, E.2
  • 11
    • 0025828670 scopus 로고
    • Pentameric structure and subunit stoichiometry of a neuronal nicotinic acetylcholine receptor
    • Cooper, E., S. Couturier, and M. Ballivel. 1991. Pentameric structure and subunit stoichiometry of a neuronal nicotinic acetylcholine receptor. Nature. 350:235-238.
    • (1991) Nature , vol.350 , pp. 235-238
    • Cooper, E.1    Couturier, S.2    Ballivel, M.3
  • 12
    • 0025291849 scopus 로고
    • 3H]quinacrine azide in the active state of the nicotinic acetylcholine receptor
    • 3H]quinacrine azide in the active state of the nicotinic acetylcholine receptor. J. Biol. Chem. 265:11017-11029.
    • (1990) J. Biol. Chem. , vol.265 , pp. 11017-11029
    • DiPaola, M.1    Kao, P.N.2    Karlin, A.3
  • 14
    • 0021287043 scopus 로고
    • Some effects of procaine at the toad end-plate are not consistent with a simple channel-blocking model
    • Gage, P.W., and R.E. Wachtel. 1984. Some effects of procaine at the toad end-plate are not consistent with a simple channel-blocking model. J. Physiol. (Camb.). 346:331-339
    • (1984) J. Physiol. (Camb.) , vol.346 , pp. 331-339
    • Gage, P.W.1    Wachtel, R.E.2
  • 15
    • 0030051784 scopus 로고    scopus 로고
    • Agitoxin footprinting the Shaker potassium channel pore
    • Gross, A., and R. MacKinnon. 1996. Agitoxin footprinting the Shaker potassium channel pore. Neuron. 16:399-406.
    • (1996) Neuron. , vol.16 , pp. 399-406
    • Gross, A.1    MacKinnon, R.2
  • 16
    • 0020621092 scopus 로고
    • Multiple sites of action for noncompetitive blockers on acetylcholine receptor rich membrane fragments from torpedo marmorata
    • Heidmann, T., R.E. Oswald, and J.P. Changeux. 1983. Multiple sites of action for noncompetitive blockers on acetylcholine receptor rich membrane fragments from torpedo marmorata. Biochemistry. 22:3112-3127.
    • (1983) Biochemistry , vol.22 , pp. 3112-3127
    • Heidmann, T.1    Oswald, R.E.2    Changeux, J.P.3
  • 17
    • 0023268737 scopus 로고
    • Interaction of non-competitive inhibitors with the acetylcholine receptor. The site specificity and spectroscopic properties of ethidium binding
    • Herz, J.M., D.A. Johnson, and P. Taylor. 1987. Interaction of non-competitive inhibitors with the acetylcholine receptor. The site specificity and spectroscopic properties of ethidium binding. J. Biol. Chem. 262:7238-7247.
    • (1987) J. Biol. Chem. , vol.262 , pp. 7238-7247
    • Herz, J.M.1    Johnson, D.A.2    Taylor, P.3
  • 18
    • 0017332486 scopus 로고
    • Local anesthetics: Hydrophilic and hydrophobic pathways for the drug-receptor reaction
    • Hille, B. 1977. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J. Gen. Physiol. 69:497-515.
    • (1977) J. Gen. Physiol. , vol.69 , pp. 497-515
    • Hille, B.1
  • 19
    • 0019190219 scopus 로고
    • Acetylcholine-induced current in perfused rat myoballs
    • Horn, R., and M.S. Brodwick. 1980. Acetylcholine-induced current in perfused rat myoballs. J. Gen. Physiol. 75:297-321.
    • (1980) J. Gen. Physiol. , vol.75 , pp. 297-321
    • Horn, R.1    Brodwick, M.S.2
  • 20
    • 0019176153 scopus 로고
    • Asymmetry of the acetylcholine channel revealed by quaternary anesthetics
    • Horn, R., M.S. Brodwick, and W.D. Dickey. 1980. Asymmetry of the acetylcholine channel revealed by quaternary anesthetics. Science. 210:205-207.
    • (1980) Science , vol.210 , pp. 205-207
    • Horn, R.1    Brodwick, M.S.2    Dickey, W.D.3
  • 21
    • 0022458822 scopus 로고
    • The ion channel of the nicotinic acetylcholine receptor is formed by the homologous helices M II of the receptor subunits
    • Hucho, F., W. Oberthur, and F. Lottspeich. 1986. The ion channel of the nicotinic acetylcholine receptor is formed by the homologous helices M II of the receptor subunits. FEBS Lett. 205:137-142.
    • (1986) FEBS Lett. , vol.205 , pp. 137-142
    • Hucho, F.1    Oberthur, W.2    Lottspeich, F.3
  • 23
    • 0024918350 scopus 로고
    • Explorations of the nicotinic acetylcholine receptor
    • Karlin, A. 1989. Explorations of the nicotinic acetylcholine receptor. Harvey Lect. 85:71-107.
    • (1989) Harvey Lect. , vol.85 , pp. 71-107
    • Karlin, A.1
  • 24
    • 0029593370 scopus 로고
    • Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins
    • Karlin, A., and M.H. Akabas. 1995. Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins. Neuron. 15:1231-1244.
    • (1995) Neuron. , vol.15 , pp. 1231-1244
    • Karlin, A.1    Akabas, M.H.2
  • 25
    • 0019982185 scopus 로고
    • Cocaine and phencyclidine inhibition of the acetylcholine receptor: Analysis of the mechanisms of action based on measurements of ion flux in the millisecond-to-minute time region
    • Karpen, J.W., H. Aoshima, L.G. Abood, and G.P. Hess. 1982. Cocaine and phencyclidine inhibition of the acetylcholine receptor: analysis of the mechanisms of action based on measurements of ion flux in the millisecond-to-minute time region. Proc. Natl. Acad. Sci. USA. 79:2509-2513.
    • (1982) Proc. Natl. Acad. Sci. USA , vol.79 , pp. 2509-2513
    • Karpen, J.W.1    Aoshima, H.2    Abood, L.G.3    Hess, G.P.4
  • 26
    • 0028035084 scopus 로고
    • Differential effects of sulfhydryl reagents on saxitoxin and tetrodotoxin block of voltage-dependent Na channels
    • Kirsch, G.E., M. Alam, and H.A. Hartmann. 1994. Differential effects of sulfhydryl reagents on saxitoxin and tetrodotoxin block of voltage-dependent Na channels. Biophys. J. 67:2305-2315.
    • (1994) Biophys. J. , vol.67 , pp. 2305-2315
    • Kirsch, G.E.1    Alam, M.2    Hartmann, H.A.3
  • 27
    • 0018351106 scopus 로고
    • Identification of a local anesthetic binding site in nicotinic post-synaptic membranes isolated from Torpedo marmorata electric tissue
    • Krodel, E.K., R.A. Beckman, and J.B. Cohen. 1979. Identification of a local anesthetic binding site in nicotinic post-synaptic membranes isolated from Torpedo marmorata electric tissue. Mol. Pharmacol. 15:294-312.
    • (1979) Mol. Pharmacol. , vol.15 , pp. 294-312
    • Krodel, E.K.1    Beckman, R.A.2    Cohen, J.B.3
  • 28
    • 0024213680 scopus 로고
    • Evidence that the M2 membrane-spanning region lines the ion channel pore of the nicotinic receptor
    • Leonard, R.J., G.G. Labarca, P. Charnet, N. Davidson, and H.A. Lester. 1988. Evidence that the M2 membrane-spanning region lines the ion channel pore of the nicotinic receptor. Science. 242: 1578-1581.
    • (1988) Science , vol.242 , pp. 1578-1581
    • Leonard, R.J.1    Labarca, G.G.2    Charnet, P.3    Davidson, N.4    Lester, H.A.5
  • 29
    • 0031059313 scopus 로고    scopus 로고
    • Quinacrine and ethidium bromide bind the same locus on the nicotinic acetylcholine receptor from Torpedo californica
    • Lurtz, M.M., M.L. Hareland, and S.E. Pedersen. 1997. Quinacrine and ethidium bromide bind the same locus on the nicotinic acetylcholine receptor from Torpedo californica. Biochemistry. 36:2068-2075.
    • (1997) Biochemistry , vol.36 , pp. 2068-2075
    • Lurtz, M.M.1    Hareland, M.L.2    Pedersen, S.E.3
  • 30
    • 0019732133 scopus 로고
    • A study of desensitization of acetylcholine receptors using nerve-released transmitter in the frog
    • Magleby, K.L., and B.S. Pallotta. 1981. A study of desensitization of acetylcholine receptors using nerve-released transmitter in the frog. J. Physiol. (Camb.). 316:225-250.
    • (1981) J. Physiol. (Camb.) , vol.316 , pp. 225-250
    • Magleby, K.L.1    Pallotta, B.S.2
  • 31
    • 0020460321 scopus 로고
    • Meproadifen reaction with the ionic channel of the acetylcholine receptor: Potentiation of agonist-induced desensitization at the frog neuromuscular junction
    • Maleque, M.A., C. Souccar, J.B. Cohen, and E.X. Albuquerque. 1982. Meproadifen reaction with the ionic channel of the acetylcholine receptor: potentiation of agonist-induced desensitization at the frog neuromuscular junction. Mol. Pharmacol. 22:636-647.
    • (1982) Mol. Pharmacol. , vol.22 , pp. 636-647
    • Maleque, M.A.1    Souccar, C.2    Cohen, J.B.3    Albuquerque, E.X.4
  • 32
    • 0020646202 scopus 로고
    • The charge carried by single-channel currents of rat cultured muscle cells in the presence of local anaesthetics
    • Neher, E. 1983. The charge carried by single-channel currents of rat cultured muscle cells in the presence of local anaesthetics. J. Physiol. (Camb.). 339:663-678.
    • (1983) J. Physiol. (Camb.) , vol.339 , pp. 663-678
    • Neher, E.1
  • 33
    • 0017905087 scopus 로고
    • Local anaesthetics transiently block currents through single acetylcholine-receptor channels
    • Neher, E., and J.H. Steinbach. 1978. Local anaesthetics transiently block currents through single acetylcholine-receptor channels. J. Physiol. (Camb.). 277:153-176.
    • (1978) J. Physiol. (Camb.) , vol.277 , pp. 153-176
    • Neher, E.1    Steinbach, J.H.2
  • 34
    • 0020560273 scopus 로고
    • 3H] phencyclidine binding to acetylcholine receptor rich membrane fragments from Torpedo marmorata
    • 3H] phencyclidine binding to acetylcholine receptor rich membrane fragments from Torpedo marmorata. Biochemistry. 22:3128-3136.
    • (1983) Biochemistry , vol.22 , pp. 3128-3136
    • Oswald, R.E.1    Heidmann, T.2    Changeux, J.P.3
  • 35
    • 0031781630 scopus 로고    scopus 로고
    • State-dependent accessibility and electrostatic potential in the channel of the acetylcholine receptor: Inferences from rates of reaction of thiosulfonates with substituted cysteines in the M2 segment of the alpha subunit
    • Pascual, J.M., and A. Karlin. 1998. State-dependent accessibility and electrostatic potential in the channel of the acetylcholine receptor: inferences from rates of reaction of thiosulfonates with substituted cysteines in the M2 segment of the alpha subunit. J. Gen. Physiol. 111:717-739.
    • (1998) J. Gen. Physiol. , vol.111 , pp. 717-739
    • Pascual, J.M.1    Karlin, A.2
  • 36
    • 0029097866 scopus 로고
    • Multiple residues specify external tetraethylammonium blockade in voltage-gated potassium channels
    • Pascual, J.M., C.C. Shieh, G.E. Kirsch, and A.M. Brown. 1995. Multiple residues specify external tetraethylammonium blockade in voltage-gated potassium channels. Biophys. J. 69:428-434.
    • (1995) Biophys. J. , vol.69 , pp. 428-434
    • Pascual, J.M.1    Shieh, C.C.2    Kirsch, G.E.3    Brown, A.M.4
  • 40
    • 0025195179 scopus 로고
    • 3H]chlorpromazine labels three amino acids of the acetylcholine receptor gamma subunit: Implications for the alpha-helical organization of regions MII and for the structure of the ion channel
    • 3H]chlorpromazine labels three amino acids of the acetylcholine receptor gamma subunit: implications for the alpha-helical organization of regions MII and for the structure of the ion channel. Proc. Natl. Acad. Sci. USA. 87:4675-4679.
    • (1990) Proc. Natl. Acad. Sci. USA , vol.87 , pp. 4675-4679
    • Revah, F.1    Galzi, J.L.2    Giraudat, J.3    Haumont, P.Y.4    Lederer, F.5    Changeux, J.P.6
  • 41
    • 0017356264 scopus 로고
    • A quantitative analysis of local anaesthetic alteration of miniature end-plate currents and end-plate current fluctuations
    • Ruff, R.L. 1977. A quantitative analysis of local anaesthetic alteration of miniature end-plate currents and end-plate current fluctuations. J. Physiol. (Camb.). 264:89-124.
    • (1977) J. Physiol. (Camb.) , vol.264 , pp. 89-124
    • Ruff, R.L.1
  • 42
    • 0022920987 scopus 로고
    • Slow permeation of organic cations in acetylcholine receptor channels
    • Sanchez, J.A., J.A. Dani, D. Siemen, and B. Hille. 1986. Slow permeation of organic cations in acetylcholine receptor channels. J. Gen. Physiol. 87:983-1001.
    • (1986) J. Gen. Physiol. , vol.87 , pp. 983-1001
    • Sanchez, J.A.1    Dani, J.A.2    Siemen, D.3    Hille, B.4
  • 43
    • 0028222912 scopus 로고
    • Voltage clamping of Xenopus laevis oocytes utilizing agarose-cushion electrodes
    • Schreibmayer, W., H.A. Lester, and N. Dascal. 1994. Voltage clamping of Xenopus laevis oocytes utilizing agarose-cushion electrodes. Pflügers Arch. 426:453-458.
    • (1994) Pflügers Arch. , vol.426 , pp. 453-458
    • Schreibmayer, W.1    Lester, H.A.2    Dascal, N.3
  • 44
    • 0020380861 scopus 로고
    • Local anesthetics and histrionicotoxin are allosteric inhibitors of the acetylcholine receptor. Studies of clonal muscle cells
    • Sine, S.M., and P. Taylor. 1982. Local anesthetics and histrionicotoxin are allosteric inhibitors of the acetylcholine receptor. Studies of clonal muscle cells. J. Biol. Chem. 257:8106-8114.
    • (1982) J. Biol. Chem. , vol.257 , pp. 8106-8114
    • Sine, S.M.1    Taylor, P.2
  • 45
    • 0028355745 scopus 로고
    • Electrostatic potential of the acetylcholine binding sites in the nicotinic receptor probed by reactions of binding-site cysteines with charged methanethiosulfonates
    • Stauffer, D.A., and A. Karlin. 1994. Electrostatic potential of the acetylcholine binding sites in the nicotinic receptor probed by reactions of binding-site cysteines with charged methanethiosulfonates. Biochemistry. 33:6840-6849.
    • (1994) Biochemistry , vol.33 , pp. 6840-6849
    • Stauffer, D.A.1    Karlin, A.2
  • 46
    • 0028839461 scopus 로고
    • Mutations in the M1 region of the nicotinic acetylcholine receptor alter the sensitivity to inhibition by quinacrine
    • Tamamizu, S., A.P. Todd, and M.G. McNamee. 1995. Mutations in the M1 region of the nicotinic acetylcholine receptor alter the sensitivity to inhibition by quinacrine. Cell. Mol. Neurobiol. 15:427-438.
    • (1995) Cell. Mol. Neurobiol. , vol.15 , pp. 427-438
    • Tamamizu, S.1    Todd, A.P.2    McNamee, M.G.3
  • 47
    • 0032102496 scopus 로고    scopus 로고
    • The location of the gate in the acetylcholine receptor channel
    • Wilson, G.G., and A. Karlin. 1998. The location of the gate in the acetylcholine receptor channel. Neuron. 20:1269-1281.
    • (1998) Neuron. , vol.20 , pp. 1269-1281
    • Wilson, G.G.1    Karlin, A.2
  • 48
    • 0015879604 scopus 로고
    • Ionic blockage of sodium channels in nerve
    • Woodhull, A.M. 1973. Ionic blockage of sodium channels in nerve. J. Gen. Physiol. 61:687-708.
    • (1973) J. Gen. Physiol. , vol.61 , pp. 687-708
    • Woodhull, A.M.1
  • 49
    • 0028970548 scopus 로고
    • Interaction of picrotoxin with GABA(A) receptor channel-lining residues probed in cysteine mutants
    • Xu, M., D.F. Covey, and M.H. Akabas. 1995. Interaction of picrotoxin with GABA(A) receptor channel-lining residues probed in cysteine mutants. Biophys. J. 69:1858-1867.
    • (1995) Biophys. J. , vol.69 , pp. 1858-1867
    • Xu, M.1    Covey, D.F.2    Akabas, M.H.3
  • 50
    • 0031456382 scopus 로고    scopus 로고
    • Identification of acetylcholine receptor channel-lining residues in the M1 segment of the beta subunit
    • Zhang, H., and A. Karlin. 1997. Identification of acetylcholine receptor channel-lining residues in the M1 segment of the beta subunit. Biochemistry. 36:15856-15864.
    • (1997) Biochemistry , vol.36 , pp. 15856-15864
    • Zhang, H.1    Karlin, A.2
  • 51
    • 0032474432 scopus 로고    scopus 로고
    • Contribution of the beta subunit M2 segment to the ion-conducting pathway of the acetylcholine receptor
    • Zhang, H., and A. Karlin. 1998. Contribution of the beta subunit M2 segment to the ion-conducting pathway of the acetylcholine receptor. Biochemistry. 37:7952-7964.
    • (1998) Biochemistry , vol.37 , pp. 7952-7964
    • Zhang, H.1    Karlin, A.2


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