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Items: 1 to 50 of 176


An intersubunit electrostatic interaction in the GABAA receptor facilitates its responses to benzodiazepines.

Pflanz NC, Daszkowski AW, Cornelison GL, Trudell JR, Mihic SJ.

J Biol Chem. 2018 May 25;293(21):8264-8274. doi: 10.1074/jbc.RA118.002128. Epub 2018 Apr 5.


Inter- and Intra-Subunit Butanol/Isoflurane Sites of Action in the Human Glycine Receptor.

McCracken ML, Gorini G, McCracken LM, Mayfield RD, Harris RA, Trudell JR.

Front Mol Neurosci. 2016 Jun 14;9:45. doi: 10.3389/fnmol.2016.00045. eCollection 2016.


Identification of an Inhibitory Alcohol Binding Site in GABAA ρ1 Receptors.

Borghese CM, Ruiz CI, Lee US, Cullins MA, Bertaccini EJ, Trudell JR, Harris RA.

ACS Chem Neurosci. 2016 Jan 20;7(1):100-8. doi: 10.1021/acschemneuro.5b00246. Epub 2015 Nov 25.


Ethanol Modulation is Quantitatively Determined by the Transmembrane Domain of Human α1 Glycine Receptors.

Horani S, Stater EP, Corringer PJ, Trudell JR, Harris RA, Howard RJ.

Alcohol Clin Exp Res. 2015 Jun;39(6):962-8. doi: 10.1111/acer.12735. Epub 2015 May 14.


Manipulations of extracellular Loop 2 in α1 GlyR ultra-sensitive ethanol receptors (USERs) enhance receptor sensitivity to isoflurane, ethanol, and lidocaine, but not propofol.

Naito A, Muchhala KH, Trang J, Asatryan L, Trudell JR, Homanics GE, Alkana RL, Davies DL.

Neuroscience. 2015 Jun 25;297:68-77. doi: 10.1016/j.neuroscience.2015.03.034. Epub 2015 Mar 28.


Molecular modeling of a tandem two pore domain potassium channel reveals a putative binding site for general anesthetics.

Bertaccini EJ, Dickinson R, Trudell JR, Franks NP.

ACS Chem Neurosci. 2014 Dec 17;5(12):1246-52. doi: 10.1021/cn500172e. Epub 2014 Oct 31.


Glycine and GABA(A) ultra-sensitive ethanol receptors as novel tools for alcohol and brain research.

Naito A, Muchhala KH, Asatryan L, Trudell JR, Homanics GE, Perkins DI, Davies DL, Alkana RL.

Mol Pharmacol. 2014 Dec;86(6):635-46. doi: 10.1124/mol.114.093773. Epub 2014 Sep 22.


P2X4 receptors (P2X4Rs) represent a novel target for the development of drugs to prevent and/or treat alcohol use disorders.

Franklin KM, Asatryan L, Jakowec MW, Trudell JR, Bell RL, Davies DL.

Front Neurosci. 2014 Jun 24;8:176. doi: 10.3389/fnins.2014.00176. eCollection 2014. Review.


Alcohol dependence: molecular and behavioral evidence.

Trudell JR, Messing RO, Mayfield J, Harris RA.

Trends Pharmacol Sci. 2014 Jul;35(7):317-23. doi: 10.1016/ Epub 2014 May 25. Review.


Synthesis and functional survey of new Tacrine analogs modified with nitroxides or their precursors.

Kálai T, Altman R, Maezawa I, Balog M, Morisseau C, Petrlova J, Hammock BD, Jin LW, Trudell JR, Voss JC, Hideg K.

Eur J Med Chem. 2014 Apr 22;77:343-50. doi: 10.1016/j.ejmech.2014.03.026. Epub 2014 Mar 12.


Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics.

Howard RJ, Trudell JR, Harris RA.

Pharmacol Rev. 2014 Feb 10;66(2):396-412. doi: 10.1124/pr.113.007468. Print 2014. Review.


Avermectins differentially affect ethanol intake and receptor function: implications for developing new therapeutics for alcohol use disorders.

Asatryan L, Yardley MM, Khoja S, Trudell JR, Hyunh N, Louie SG, Petasis NA, Alkana RL, Davies DL.

Int J Neuropsychopharmacol. 2014 Jun;17(6):907-16. doi: 10.1017/S1461145713001703. Epub 2014 Jan 22.


Endothelial fate mapping in mice with pulmonary hypertension.

Qiao L, Nishimura T, Shi L, Sessions D, Thrasher A, Trudell JR, Berry GJ, Pearl RG, Kao PN.

Circulation. 2014 Feb 11;129(6):692-703. doi: 10.1161/CIRCULATIONAHA.113.003734. Epub 2013 Nov 7.


Structural models of ligand-gated ion channels: sites of action for anesthetics and ethanol.

Olsen RW, Li GD, Wallner M, Trudell JR, Bertaccini EJ, Lindahl E, Miller KW, Alkana RL, Davies DL.

Alcohol Clin Exp Res. 2014 Mar;38(3):595-603. doi: 10.1111/acer.12283. Epub 2013 Oct 24. Review.


GABA(A) receptor transmembrane amino acids are critical for alcohol action: disulfide cross-linking and alkyl methanethiosulfonate labeling reveal relative location of binding sites.

Borghese CM, Hicks JA, Lapid DJ, Trudell JR, Harris RA.

J Neurochem. 2014 Feb;128(3):363-75. doi: 10.1111/jnc.12476. Epub 2013 Oct 28.


Stabilization of the GluCl ligand-gated ion channel in the presence and absence of ivermectin.

Yoluk O, Brömstrup T, Bertaccini EJ, Trudell JR, Lindahl E.

Biophys J. 2013 Aug 6;105(3):640-7. doi: 10.1016/j.bpj.2013.06.037.


Zinc-dependent modulation of α2- and α3-glycine receptor subunits by ethanol.

McCracken LM, Trudell JR, McCracken ML, Harris RA.

Alcohol Clin Exp Res. 2013 Dec;37(12):2002-10. doi: 10.1111/acer.12192. Epub 2013 Jul 29.


Inhibition versus potentiation of ligand-gated ion channels can be altered by a single mutation that moves ligands between intra- and intersubunit sites.

Brömstrup T, Howard RJ, Trudell JR, Harris RA, Lindahl E.

Structure. 2013 Aug 6;21(8):1307-16. doi: 10.1016/j.str.2013.06.018. Epub 2013 Jul 25.


Assessment of homology templates and an anesthetic binding site within the γ-aminobutyric acid receptor.

Bertaccini EJ, Yoluk O, Lindahl ER, Trudell JR.

Anesthesiology. 2013 Nov;119(5):1087-95. doi: 10.1097/ALN.0b013e31829e47e3.


Mutation of a zinc-binding residue in the glycine receptor α1 subunit changes ethanol sensitivity in vitro and alcohol consumption in vivo.

McCracken LM, Blednov YA, Trudell JR, Benavidez JM, Betz H, Harris RA.

J Pharmacol Exp Ther. 2013 Feb;344(2):489-500. doi: 10.1124/jpet.112.197707. Epub 2012 Dec 10.


Molecular mechanism for the dual alcohol modulation of Cys-loop receptors.

Murail S, Howard RJ, Broemstrup T, Bertaccini EJ, Harris RA, Trudell JR, Lindahl E.

PLoS Comput Biol. 2012;8(10):e1002710. doi: 10.1371/journal.pcbi.1002710. Epub 2012 Oct 4.


Induced changes in protein receptors conferring resistance to anesthetics.

Bertaccini EJ, Trudell JR.

Curr Opin Anaesthesiol. 2012 Aug;25(4):405-10. doi: 10.1097/ACO.0b013e328354fda8. Review.


Charge and geometry of residues in the loop 2 β hairpin differentially affect agonist and ethanol sensitivity in glycine receptors.

Perkins DI, Trudell JR, Asatryan L, Davies DL, Alkana RL.

J Pharmacol Exp Ther. 2012 May;341(2):543-51. doi: 10.1124/jpet.111.190942. Epub 2012 Feb 22.


Teaching an old GABA receptor new tricks.

Trudell JR, Bertaccini E, Maciver MB.

Anesth Analg. 2012 Aug;115(2):270-3. doi: 10.1213/ANE.0b013e31824a0b3c. Epub 2012 Feb 17. Review.


The TM2 6' position of GABA(A) receptors mediates alcohol inhibition.

Johnson WD 2nd, Howard RJ, Trudell JR, Harris RA.

J Pharmacol Exp Ther. 2012 Feb;340(2):445-56. doi: 10.1124/jpet.111.188037. Epub 2011 Nov 9.


Characterization of two mutations, M287L and Q266I, in the α1 glycine receptor subunit that modify sensitivity to alcohols.

Borghese CM, Blednov YA, Quan Y, Iyer SV, Xiong W, Mihic SJ, Zhang L, Lovinger DM, Trudell JR, Homanics GE, Harris RA.

J Pharmacol Exp Ther. 2012 Feb;340(2):304-16. doi: 10.1124/jpet.111.185116. Epub 2011 Oct 28.


Structural basis for alcohol modulation of a pentameric ligand-gated ion channel.

Howard RJ, Murail S, Ondricek KE, Corringer PJ, Lindahl E, Trudell JR, Harris RA.

Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):12149-54. doi: 10.1073/pnas.1104480108. Epub 2011 Jul 5.


Alcohol-binding sites in distinct brain proteins: the quest for atomic level resolution.

Howard RJ, Slesinger PA, Davies DL, Das J, Trudell JR, Harris RA.

Alcohol Clin Exp Res. 2011 Sep;35(9):1561-73. doi: 10.1111/j.1530-0277.2011.01502.x. Epub 2011 Jun 15. Review.


Microsecond simulations indicate that ethanol binds between subunits and could stabilize an open-state model of a glycine receptor.

Murail S, Wallner B, Trudell JR, Bertaccini E, Lindahl E.

Biophys J. 2011 Apr 6;100(7):1642-50. doi: 10.1016/j.bpj.2011.02.032.


Linking of Glycine Receptor Transmembrane Segments Three and Four Allows Assignment of Intrasubunit-Facing Residues.

McCracken LM, McCracken ML, Gong DH, Trudell JR, Harris RA.

ACS Chem Neurosci. 2010 Jul;1(7):482.


Modeling anesthetic binding sites within the glycine alpha one receptor based on prokaryotic ion channel templates: the problem with TM4.

Bertaccini EJ, Wallner B, Trudell JR, Lindahl E.

J Chem Inf Model. 2010 Dec 27;50(12):2248-55. doi: 10.1021/ci100266c. Epub 2010 Nov 30.


A transmembrane amino acid in the GABAA receptor β2 subunit critical for the actions of alcohols and anesthetics.

McCracken ML, Borghese CM, Trudell JR, Harris RA.

J Pharmacol Exp Ther. 2010 Dec;335(3):600-6. doi: 10.1124/jpet.110.170472. Epub 2010 Sep 8.


Normal mode gating motions of a ligand-gated ion channel persist in a fully hydrated lipid bilayer model.

Bertaccini EJ, Trudell JR, Lindahl E.

ACS Chem Neurosci. 2010 Aug 18;1(8):552-8. doi: 10.1021/cn100026t. Epub 2010 Jun 11.


Ivermectin antagonizes ethanol inhibition in purinergic P2X4 receptors.

Asatryan L, Popova M, Perkins D, Trudell JR, Alkana RL, Davies DL.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):720-8. doi: 10.1124/jpet.110.167908. Epub 2010 Jun 11.


Molecular targets and mechanisms for ethanol action in glycine receptors.

Perkins DI, Trudell JR, Crawford DK, Alkana RL, Davies DL.

Pharmacol Ther. 2010 Jul;127(1):53-65. doi: 10.1016/j.pharmthera.2010.03.003. Epub 2010 Apr 23. Review.


Disruption of an intersubunit electrostatic bond is a critical step in glycine receptor activation.

Todorovic J, Welsh BT, Bertaccini EJ, Trudell JR, Mihic SJ.

Proc Natl Acad Sci U S A. 2010 Apr 27;107(17):7987-92. doi: 10.1073/pnas.1001845107. Epub 2010 Apr 12.


Zinc enhances ethanol modulation of the alpha1 glycine receptor.

McCracken LM, Trudell JR, Goldstein BE, Harris RA, Mihic SJ.

Neuropharmacology. 2010 Mar;58(3):676-81. doi: 10.1016/j.neuropharm.2009.11.001. Epub 2009 Nov 11.


Loop 2 structure in glycine and GABA(A) receptors plays a key role in determining ethanol sensitivity.

Perkins DI, Trudell JR, Crawford DK, Asatryan L, Alkana RL, Davies DL.

J Biol Chem. 2009 Oct 2;284(40):27304-14. doi: 10.1074/jbc.M109.023598. Epub 2009 Aug 5.


Identifying the binding site(s) for antidepressants on the Torpedo nicotinic acetylcholine receptor: [3H]2-azidoimipramine photolabeling and molecular dynamics studies.

Sanghvi M, Hamouda AK, Jozwiak K, Blanton MP, Trudell JR, Arias HR.

Biochim Biophys Acta. 2008 Dec;1778(12):2690-9. doi: 10.1016/j.bbamem.2008.08.019. Epub 2008 Sep 10.


Roles for loop 2 residues of alpha1 glycine receptors in agonist activation.

Crawford DK, Perkins DI, Trudell JR, Bertaccini EJ, Davies DL, Alkana RL.

J Biol Chem. 2008 Oct 10;283(41):27698-706. doi: 10.1074/jbc.M802384200. Epub 2008 Jul 25.


General anesthetics have additive actions on three ligand gated ion channels.

Jenkins A, Lobo IA, Gong D, Trudell JR, Solt K, Harris RA, Eger EI 2nd.

Anesth Analg. 2008 Aug;107(2):486-93. doi: 10.1213/ane.0b013e31817b70c1.


Ethanol's molecular targets.

Harris RA, Trudell JR, Mihic SJ.

Sci Signal. 2008 Jul 15;1(28):re7. doi: 10.1126/scisignal.128re7. Review.


Targets for ethanol action and antagonism in loop 2 of the extracellular domain of glycine receptors.

Perkins DI, Trudell JR, Crawford DK, Alkana RL, Davies DL.

J Neurochem. 2008 Aug;106(3):1337-49. doi: 10.1111/j.1471-4159.2008.05476.x. Epub 2008 May 12.


Effect of cobratoxin binding on the normal mode vibration within acetylcholine binding protein.

Bertaccini EJ, Lindahl E, Sixma T, Trudell JR.

J Chem Inf Model. 2008 Apr;48(4):855-60. doi: 10.1021/ci700456s. Epub 2008 Mar 19.


Molecular modeling and mutagenesis reveals a tetradentate binding site for Zn2+ in GABA(A) alphabeta receptors and provides a structural basis for the modulating effect of the gamma subunit.

Trudell JR, Yue ME, Bertaccini EJ, Jenkins A, Harrison NL.

J Chem Inf Model. 2008 Feb;48(2):344-9. doi: 10.1021/ci700324a. Epub 2008 Jan 16.


Normal-mode analysis of the glycine alpha1 receptor by three separate methods.

Bertaccini EJ, Trudell JR, Lindahl E.

J Chem Inf Model. 2007 Jul-Aug;47(4):1572-9. Epub 2007 Jun 30.


Evidence that ethanol acts on a target in Loop 2 of the extracellular domain of alpha1 glycine receptors.

Crawford DK, Trudell JR, Bertaccini EJ, Li K, Davies DL, Alkana RL.

J Neurochem. 2007 Sep;102(6):2097-2109. doi: 10.1111/j.1471-4159.2007.04680.x. Epub 2007 Jun 11.


The common chemical motifs within anesthetic binding sites.

Bertaccini EJ, Trudell JR, Franks NP.

Anesth Analg. 2007 Feb;104(2):318-24.


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