Sites of excitatory and inhibitory actions of alcohols on neuronal α2β4 nicotinic acetylcholine receptors

Journal of Pharmacology and Experimental Therapeutics

Volumn 307, Issue 1, 2003, Pages 42-52

  Borghese, Cecilia M ^a   Henderson, L Ashley ^a   Bleck, Virginia ^a   Trudell, James R ^b   Harris, R Adron ^a  

^a UNIVERSITY OF TEXAS AT AUSTIN   (United States)

^b STANFORD UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALCOHOL; BUTANOL; CYSTEINE; ISOFLURANE; NICOTINIC RECEPTOR; OCTANOL; PENTANOL; THIOL DERIVATIVE; THIOL GROUP; URETHAN;

ANIMAL CELL; ARTICLE; BINDING SITE; CONTROLLED STUDY; COVALENT BOND; FEMALE; MUTAGENESIS; NERVE CELL; NONHUMAN; OOCYTE; PRIORITY JOURNAL; VOLTAGE CLAMP; XENOPUS LAEVIS;

ALCOHOLS; ANIMALS; ELECTROPHYSIOLOGY; FEMALE; MUTAGENESIS, SITE-DIRECTED; NEURONS; OOCYTES; RECEPTORS, NICOTINIC; XENOPUS LAEVIS;

EID: 0141630638     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.053710     Document Type: Article

References (40)

1. Akabas MH, Kaufmann C, Archdeacon P, and Karlin A (1994) Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the α subunit. Neuron 13:919-927.
2. Alifimoff JK, Firestone LL, and Miller KW (1989) Anaesthetic potencies of primary alkanols: implications for the molecular dimensions of the anaesthetic site. Br J Pharmacol 96:9-16.
3. Arias HR (1998) Binding sites for exogenous and endogenous non-competitive inhibitors of the nicotinic acetylcholine receptor. Biochim Biophys Acta 1376:173-220.
4. Bertaccini E and Trudell JR (2002) Predicting the transmembrane secondary structure of ligand-gated ion channels. Protein Eng 15:443-453.
5. Borghese CM, Ali DN, Bleck V, and Harris RA (2002) Acetylcholine and alcohol sensitivity of neuronal nicotinic acetylcholine receptors: mutations in transmembrane domains. Alcoholism Clin Exp Res 26:1764-1772.
6. Bradley RJ, Sterz R, and Peper K (1984) The effects of alcohols and diols at the nicotinic acetylcholine receptor of the neuromuscular junction. Brain Res 295:101-112.
7. Cardoso RA, Brozowski SJ, Chavez-Noriega LE, Harpold M, Valenzuela CF, and Harris RA (1999) Effects of ethanol on recombinant human neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes. J Pharmacol Exp Ther 289:774-780.
8. Chang G, Spencer RH, Lee AT, Barclay MT, and Rees DC (1998) Structure of the MscL homolog from mycobacterium tuberculosis: a gated mechanosensitive ion channel. Science (Wash DC) 282:2220-2226.
9. Colquhoun D (1998) Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br J Pharmacol 125:924-947.
10. Dilger JP and Vidal AM (1994) Cooperative interactions between general anesthetics and QX-222 within the pore of the acetylcholine receptor ion channel. Mol Pharmacol 45:169-175.
11. Forman SA, Miller KW, and Yellen G (1995) A discrete site for general anesthetics on a postsynaptic receptor. Mol Pharmacol 48:574-581.
12. Forman SA and Zhou Q (2000) Nicotinic receptor pore mutations create a sensitive inhibitory site for ethanol. Alcoholism Clin Exp Res 24:1363-1368.
13. Franks NP and Lieb WR (1994) Molecular and cellular mechanisms of general anesthesia. Nature (Lond) 367:607-614.
14. Godden EL, Harris RA, and Dunwiddie TV (2001) Correlation between molecular volume and the effects of n-alcohols on human neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes. J Pharmacol Exp Ther 296:716-722.
15. Hara K and Harris RA (2002) The anesthetic mechanism of urethane: the effects on neurotransmitter-gated ion channels. Anesth Analg 94:313-318.
16. A receptor α1 subunit: implications for modulation by inhaled anesthetics and ion channel structure. Neuropharmacology 43:669-678.
17. A receptor. J Neurosci 21: RC136.
18. Karlin A (2002) Emerging structure of the nicotinic acetylcholine receptors. Nat Rev Neurosci 3:102-114.
19. Kruse SW, Zhao R, Smith DP, and Jones DNM (2003) Defining an alcohol-binding motif in proteins: insights from structural and computational studies of the Drosophila protein LUSH. Nat Struct Biol 10:694-700.
20. Mascia MP, Machu TK, and Harris RA (1996) Enhancement of homomeric glycine receptor function by long-chain alcohols and anaesthetics. Br J Pharmacol 119:1331-1336.
21. Mascia MP, Trudell JR, and Harris RA (2000) Specific binding sites for alcohols and anesthetics on ligand-gated ion channels. Proc Natl Acad Sci USA 97:9305-9310.
22. A and glycine receptors. Nature (Lond) 389:385-389.
23. Miyazawa A, Fujiyoshi Y, and Unwin N (2003) Structure and gating mechanism of the acetylcholine receptor pore. Nature (Lond) 423:949-955.
24. Opella SJ, Marassi FM, Gesell JJ, Valente AP, Kim Y, Oblatt-Montal M, and Montal M (1999) Structures of the M2 channel-lining segments from nicotinic acetylcholine and NMDA receptors by NMR spectroscopy. Nat Struct Biol 6:374-379.
25. Picciotto MR, Caldarone BJ, King SL, and Zachariou V (2000) Nicotinic receptors in the brain: links between molecular biology and behavior. Neuropsychopharmacology 22:451-465.
26. Pratt MB, Husain SS, Miller KW, and Cohen JB (2000) Identification of sites of incorporation in the nicotinic acetylcholine receptor of a photoactivable general anesthetic. J Biol Chem 275:29441-29451.
27. Roberts DD, Lewis SD, Ballou DP, Olson ST, and Shafer JA (1986) Reactivity of small thiolate anions and cysteine-25 in papain toward methyl methanethiosulfonate. Biochemistry 25:5595-5601.
28. Söderpalm B, Ericson M, Olausson P, Blomqvist O, and Engel JA (2000) Nicotinic mechanisms involved in the dopamine activating and reinforcing properties of ethanol. Behav Brain Res 113:85-96.
29. Trudell JR and Bertaccini E (2002) Molecular modelling of specific and non-specific anaesthetic interactions. Br J Anaesth 89:32-40.
30. Wenningmann I, Barann M, Vidal AM, and Dilger JP (2001) The effects of isoflurane on acetylcholine receptor channels. 3. Effects of conservative polar-to-nonpolar mutations within the channel pore. Mol Pharmacol 60:584-594.
31. Wick MJ, Mihic SJ, Ueno S, Mascia MP, Trudell JR, Brozowski SJ, Ye Q, Harrison NL, and Harris RA (1998) Mutations of γ-aminobutyric acid and glycine receptors change alcohol cutoff: evidence for an alcohol receptor? Proc Natl Acad Sci USA 95:6504-6509.
32. Wood SC, Forman SA, and Miller KW (1991) Short chain and long chain alkanols have different sites of action on nicotinic acetylcholine receptor channels from Torpedo. Mol Pharmacol 39:332-338.
33. Yamakura T, Bertaccini E, Trudell JR, and Harris RA (2001) Anesthetics and ion channels: molecular models and sites of anesthetic action. Annu Rev Pharmacol Toxicol 41:23-51.
34. Ye Q, Koltchine VV, Mihic SJ, Mascia MP, Wick MJ, Finn SE, Harrison NL, and Harris RA (1998) Enhancement of glycine receptor function by ethanol is inversely correlated with molecular volume at position α267. J Biol Chem 273:3314-3319.
35. Yoshikawa S, Shinzawa-Itoh K, Nakashima R, Yaono R, Yamashita E, Inoue N, Yao M, Fei MJ, Libeu CP, Mizushima T, et al. (1998) Redox-coupled crystal structural changes in bovine heart cytochrome c oxidase. Science (Wash DC) 280:1723-1729.
36. Zhang H and Karlin A (1998) Contribution of the β subunit M2 segment to the ion-conducting pathway of the acetylcholine receptor. Biochemistry 37:7952-7964.
37. Zhang Y, Trudell JR, Mascia MP, Laster MJ, Gong DH, Harris RA, and Eger EI II (2000) The anesthetic potencies of alkanethiols for rats: relevance to theories of narcosis. Anesth Analg 91:1294-1299.
38. Zhou QL, Zhou Q, and Forman SA (2000) The n-alcohol site in the nicotinic receptor pore is a hydrophobic patch. Biochemistry 39:14920-14926.
39. Zuo Y, Aistrup GL, Marszalec W, Gillespie A, Chavez-Noriega LE, Yeh JZ, and Narahashi T (2001) Dual action of n-alcohols on neuronal nicotinic acetylcholine receptors. Mol Pharmacol 60:700-711.
40. Zuo Y, Kuryatov A, Lindstrom JM, Yeh JZ, and Narahashi T (2002) Alcohol modulation of neuronal nicotinic acetylcholine receptors is α subunit dependent. Alcoholism Clin Exp Res 26:779-784.