{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,30]],"date-time":"2026-04-30T08:00:06Z","timestamp":1777536006969,"version":"3.51.4"},"reference-count":157,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2015,11,1]],"date-time":"2015-11-01T00:00:00Z","timestamp":1446336000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Pharmacological Research"],"published-print":{"date-parts":[[2015,11]]},"DOI":"10.1016\/j.phrs.2015.08.018","type":"journal-article","created":{"date-parts":[[2015,8,28]],"date-time":"2015-08-28T22:05:46Z","timestamp":1440799546000},"page":"9-17","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":21,"special_numbering":"C","title":["Multiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy"],"prefix":"10.1016","volume":"101","author":[{"given":"Patricio","family":"Iturriaga-V\u00e1squez","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jans","family":"Alzate-Morales","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Isabel","family":"Bermudez","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rodrigo","family":"Varas","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Miguel","family":"Reyes-Parada","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.phrs.2015.08.018_bib0005","doi-asserted-by":"crossref","first-page":"127","DOI":"10.1016\/j.sbi.2006.01.013","article-title":"Can we rationally design promiscuous drugs?","volume":"16","author":"Hopkins","year":"2006","journal-title":"Curr. Opin. Struct. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0010","doi-asserted-by":"crossref","first-page":"269","DOI":"10.2174\/157016306780368117","article-title":"Pathway analysis for design of promiscuous drugs and selective drug mixtures","volume":"3","author":"Sivachenko","year":"2006","journal-title":"Curr. Drug Discov. Technol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0015","doi-asserted-by":"crossref","first-page":"682","DOI":"10.1038\/nchembio.118","article-title":"Network pharmacology: the next paradigm in drug discovery","volume":"4","author":"Hopkins","year":"2008","journal-title":"Nat. Chem. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0020","doi-asserted-by":"crossref","first-page":"1520","DOI":"10.2174\/092986708784638843","article-title":"What does systems biology mean for drug development?","volume":"15","author":"Schrattenholz","year":"2008","journal-title":"Curr. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0025","doi-asserted-by":"crossref","first-page":"505","DOI":"10.1146\/annurev-pharmtox-010611-134520","article-title":"Systems pharmacology: network analysis to identify multiscale mechanisms of drug action","volume":"52","author":"Zhao","year":"2012","journal-title":"Annu. Rev. Pharmacol. Toxicol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0030","doi-asserted-by":"crossref","first-page":"361","DOI":"10.1146\/annurev-pharmtox-010611-134630","article-title":"Novel computational approaches to polypharmacology as a means to define responses to individual drugs","volume":"52","author":"Xie","year":"2012","journal-title":"Annu. Rev. Pharmacol. Toxicol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0035","doi-asserted-by":"crossref","first-page":"1201","DOI":"10.2174\/13816128113199990066","article-title":"Network-based strategies can help mono- and poly-pharmacology drug discovery: a systems biology view","volume":"20","author":"Engin","year":"2014","journal-title":"Curr. Pharm. Des."},{"key":"10.1016\/j.phrs.2015.08.018_bib0040","doi-asserted-by":"crossref","first-page":"7874","DOI":"10.1021\/jm5006463","article-title":"Polypharmacology challenges and opportunities in drug discovery","volume":"57","author":"Anighoro","year":"2014","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0045","doi-asserted-by":"crossref","first-page":"353","DOI":"10.1038\/nrd1346","article-title":"Magic shotguns versus magic bullets: selectively non\u2010selective drugs for mood disorders and schizophrenia","volume":"3","author":"Roth","year":"2004","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2015.08.018_bib0050","doi-asserted-by":"crossref","first-page":"115","DOI":"10.1016\/j.tips.2009.11.006","article-title":"Unveiling the role of network and systems biology in drug discovery","volume":"31","author":"Pujol","year":"2010","journal-title":"Trends Pharmacol. Sci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0055","doi-asserted-by":"crossref","first-page":"579","DOI":"10.1038\/nrd3478","article-title":"Trends in the exploitation of novel drug targets","volume":"10","author":"Rask-Andersen","year":"2011","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2015.08.018_bib0060","doi-asserted-by":"crossref","first-page":"41","DOI":"10.1586\/ecp.12.74","article-title":"Polypharmacology drug discovery for the future","volume":"6","author":"Reddy","year":"2013","journal-title":"Expert Rev. Clin. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0065","doi-asserted-by":"crossref","first-page":"485","DOI":"10.4155\/fmc.14.25","article-title":"Polypharmacology the rise of multitarget drugs over combination therapies","volume":"6","author":"Rosini","year":"2014","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0070","doi-asserted-by":"crossref","first-page":"e201401003","DOI":"10.5936\/csbj.201401003","article-title":"Exploring compound promiscuity patterns and multi-target activity spaces","volume":"9","author":"Hu","year":"2014","journal-title":"Comput. Struct. Biotechnol. J."},{"key":"10.1016\/j.phrs.2015.08.018_bib0075","doi-asserted-by":"crossref","first-page":"87","DOI":"10.1007\/s10822-011-9493-2","article-title":"Is there a future for computational chemistry in drug research?","volume":"26","author":"Maggiora","year":"2012","journal-title":"J. Comput. Aided Mol. Des."},{"key":"10.1016\/j.phrs.2015.08.018_bib0080","doi-asserted-by":"crossref","first-page":"268","DOI":"10.1016\/j.tips.2012.03.007","article-title":"Structure-based drug screening for G-protein-coupled receptors","volume":"33","author":"Shoichet","year":"2012","journal-title":"Trends Pharmacol. Sci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0085","doi-asserted-by":"crossref","first-page":"187","DOI":"10.1038\/nchem.217","article-title":"The rise of fragment\u2010based drug discovery","volume":"1","author":"Murray","year":"2009","journal-title":"Nat. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0090","doi-asserted-by":"crossref","first-page":"23","DOI":"10.1016\/j.drudis.2011.08.002","article-title":"The role of fragment-based and computational methods in polypharmacology","volume":"17","author":"Bottegoni","year":"2012","journal-title":"Drug Discov. Today."},{"key":"10.1016\/j.phrs.2015.08.018_bib0095","doi-asserted-by":"crossref","first-page":"492","DOI":"10.1021\/ci2003544","article-title":"Exploring polypharmacology using a ROCS-based target fishing approach","volume":"52","author":"Abdul Hameed","year":"2012","journal-title":"J. Chem. Inf. Model"},{"key":"10.1016\/j.phrs.2015.08.018_bib0100","doi-asserted-by":"crossref","first-page":"134","DOI":"10.1021\/ci2002022","article-title":"Drug effect prediction by polypharmacology-based interaction profiling","volume":"52","author":"Simon","year":"2012","journal-title":"J. Chem. Inf. Model."},{"key":"10.1016\/j.phrs.2015.08.018_bib0105","doi-asserted-by":"crossref","first-page":"413","DOI":"10.1016\/j.ddtec.2006.12.008","article-title":"In silico target fishing: predicting biological targets from chemical structure","volume":"3","author":"Jenkins","year":"2006","journal-title":"Drug Discov. Today Technol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0110","doi-asserted-by":"crossref","first-page":"176","DOI":"10.1002\/minf.200900081","article-title":"Structure-based approaches to target fishing and ligand profiling","volume":"29","author":"Rognan","year":"2010","journal-title":"Mol. Inf."},{"key":"10.1016\/j.phrs.2015.08.018_bib0115","doi-asserted-by":"crossref","first-page":"1069","DOI":"10.2174\/15680266113139990028","article-title":"Recent trends and future prospects in computational GPCR drug discovery: from virtual screening to polypharmacology","volume":"13","author":"Carrieri","year":"2013","journal-title":"Curr. Top. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0120","doi-asserted-by":"crossref","first-page":"691","DOI":"10.1038\/nchembio.117","article-title":"Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases","volume":"4","author":"Apsel","year":"2008","journal-title":"Nat. Chem. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0125","doi-asserted-by":"crossref","first-page":"129","DOI":"10.1007\/BF02780338","article-title":"Ligand-gated ion channels. Homology and diversity","volume":"4","author":"Cockcroft","year":"1990","journal-title":"Mol. Neurobiol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0130","doi-asserted-by":"crossref","first-page":"554","DOI":"10.1016\/S0959-440X(94)90218-6","article-title":"Neurotransmitter-gated ion channels as unconventional allosteric proteins","volume":"4","author":"Galzi","year":"1994","journal-title":"Curr. Opin. Struct. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0135","doi-asserted-by":"crossref","first-page":"569","DOI":"10.1146\/annurev.ne.17.030194.003033","article-title":"GABAA receptor channels","volume":"17","author":"Macdonald","year":"1994","journal-title":"Annu. Rev. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0140","doi-asserted-by":"crossref","first-page":"159","DOI":"10.1016\/0166-2236(95)98370-E","article-title":"GABAC receptor","volume":"18","author":"Bormann","year":"1995","journal-title":"Trends Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0145","doi-asserted-by":"crossref","first-page":"735","DOI":"10.1002\/bies.950161008","article-title":"The inhibitory neuronal glycine receptor","volume":"16","author":"B\u00e9chade","year":"1994","journal-title":"Bioessays"},{"key":"10.1016\/j.phrs.2015.08.018_bib0150","doi-asserted-by":"crossref","first-page":"707","DOI":"10.1038\/371707a0","article-title":"Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans","volume":"371","author":"Cully","year":"1994","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0155","doi-asserted-by":"crossref","first-page":"11","DOI":"10.1038\/nn787","article-title":"Two cDNAs coding for histamine-gated ion channels in D. melanogaster","volume":"5","author":"Gisselmann","year":"2002","journal-title":"Nat. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0160","doi-asserted-by":"crossref","first-page":"2000","DOI":"10.1074\/jbc.M107635200","article-title":"Identification of two novel Drosophila melanogaster histamine-gated chloride channel subunits expressed in the eye","volume":"277","author":"Zheng","year":"2002","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0165","doi-asserted-by":"crossref","first-page":"155","DOI":"10.1007\/BF00167110","article-title":"Molecular evolution of the nicotinic acetylcholine receptor: an example of multigene family in excitable cells","volume":"40","author":"Le Novere","year":"1995","journal-title":"J. Mol. Evol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0170","doi-asserted-by":"crossref","first-page":"121","DOI":"10.1016\/0166-2236(95)93887-4","article-title":"Evolutionary history of the ligand-gated ion-channel superfamily of receptors","volume":"18","author":"Ortells","year":"1995","journal-title":"Trends Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0175","doi-asserted-by":"crossref","first-page":"340","DOI":"10.1093\/nar\/27.1.340","article-title":"The ligand gated ion channel database","volume":"27","author":"Le Novere","year":"1999","journal-title":"Nucleic Acids Res."},{"key":"10.1016\/j.phrs.2015.08.018_bib0180","doi-asserted-by":"crossref","first-page":"417","DOI":"10.1007\/BF02247415","article-title":"Nicotinic systems and cognitive function","volume":"108","author":"Levin","year":"1992","journal-title":"Psychopharmacol"},{"key":"10.1016\/j.phrs.2015.08.018_bib0185","doi-asserted-by":"crossref","first-page":"805","DOI":"10.1038\/19756","article-title":"Reduced antinociception in mice lacking neuronal nicotinic receptor subunits","volume":"38","author":"Marubio","year":"1999","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0190","doi-asserted-by":"crossref","first-page":"55","DOI":"10.1038\/nrn1298","article-title":"The neurobiology of nicotine addiction: bridging the gap from molecules to behaviour","volume":"5","author":"Laviolette","year":"2004","journal-title":"Nat. Rev. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0195","doi-asserted-by":"crossref","first-page":"1003","DOI":"10.1517\/13543776.13.7.1003","article-title":"Neuronal nicotinic acetylcholine receptor ligands as potential analgesics","volume":"13","author":"Bunnelle","year":"2003","journal-title":"Exp. Opin. Ther. Patents"},{"key":"10.1016\/j.phrs.2015.08.018_bib0200","doi-asserted-by":"crossref","first-page":"4169","DOI":"10.1021\/jm970377o","article-title":"Neuronal nicotinic acetylcholine receptors as targets for drug discovery","volume":"40","author":"Holladay","year":"1997","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0205","doi-asserted-by":"crossref","first-page":"461","DOI":"10.1016\/S0022-3565(24)35314-5","article-title":"Neuronal nicotinic acetylcholine receptors as novel drug targets","volume":"292","author":"Lloyd","year":"2000","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0210","doi-asserted-by":"crossref","first-page":"7820","DOI":"10.1523\/JNEUROSCI.23-21-07820.2003","article-title":"Subunit composition of functional nicotinic receptors in dopaminergic neurons investigated with knock-out mice","volume":"23","author":"Champtiaux","year":"2003","journal-title":"J. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0215","first-page":"101","volume":"144","author":"Lindstrom","year":"2000"},{"key":"10.1016\/j.phrs.2015.08.018_bib0220","doi-asserted-by":"crossref","first-page":"482","DOI":"10.1016\/j.tips.2006.07.004","article-title":"Brain nicotinic acetylcholine receptors: native subtypes and their relevance","volume":"27","author":"Gotti","year":"2005","journal-title":"Trends Pharmacol. Sci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0225","doi-asserted-by":"crossref","first-page":"9","DOI":"10.1016\/S0026-895X(25)10925-5","article-title":"[3H]Cytisine binding to nicotinic cholinergic receptors in brain","volume":"39","author":"Pabreza","year":"1991","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0230","doi-asserted-by":"crossref","first-page":"21795","DOI":"10.1074\/jbc.M114.555136","article-title":"Non-equivalent ligand selectivity of agonist sites in (\u03b14\u03b22) 2\u03b14 nicotinic acetylcholine receptors: a key determinant of agonist efficacy","volume":"289","author":"Mazzaferro","year":"2014","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0235","doi-asserted-by":"crossref","first-page":"847","DOI":"10.1016\/0896-6273(90)90344-F","article-title":"A neuronal nicotinic acetylcholine receptor subunit (\u03b17) is developmentally regulated and forms a homo-oligomeric channel blocked by \u03b1-BTX","volume":"5","author":"Couturier","year":"1990","journal-title":"Neuron"},{"key":"10.1016\/j.phrs.2015.08.018_bib0240","doi-asserted-by":"crossref","first-page":"1","DOI":"10.3389\/fnins.2014.00426","article-title":"Nicotinic receptor modulation to treat alcohol and drug dependence","volume":"8","author":"Rahman","year":"2015","journal-title":"Front. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0245","doi-asserted-by":"crossref","first-page":"4705","DOI":"10.1021\/jm040219e","article-title":"Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations","volume":"48","author":"Jensen","year":"2005","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0250","doi-asserted-by":"crossref","first-page":"283","DOI":"10.2174\/1568026043451393","article-title":"Physiological roles of neuronal nicotinic receptor subtypes: new insights on the nicotinic modulation of neurotransmitter release, synaptic transmission and plasticity","volume":"4","author":"Sher","year":"2004","journal-title":"Curr. Top. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0255","doi-asserted-by":"crossref","first-page":"361","DOI":"10.1016\/j.brainresbull.2005.09.018","article-title":"Dopamine release in human neocortical slices: characterization of inhibitory autoreceptors and of nicotinic acetylcholine receptor-evoked release","volume":"68","author":"L\u00f6ffler","year":"2006","journal-title":"Brain Res. Bull."},{"key":"10.1016\/j.phrs.2015.08.018_bib0260","doi-asserted-by":"crossref","first-page":"72","DOI":"10.1016\/j.neuropharm.2004.09.005","article-title":"Different nicotinic acetylcholine receptor subtypes mediating striatal and prefrontal cortical [3H]dopamine release","volume":"48","author":"Cao","year":"2005","journal-title":"Neuropharmacol"},{"key":"10.1016\/j.phrs.2015.08.018_bib0265","doi-asserted-by":"crossref","first-page":"1526","DOI":"10.1124\/mol.65.6.1526","article-title":"Subunit composition and pharmacology of two classes of striatal presynaptic nicotinic acetylcholine receptors mediating dopamine release in mice","volume":"65","author":"Salminen","year":"2004","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0270","doi-asserted-by":"crossref","first-page":"651","DOI":"10.1124\/jpet.301.2.651","article-title":"Characterization of nicotinic agonist-induced [3H]dopamine release from synaptosomes prepared from four mouse brain regions","volume":"301","author":"Grady","year":"2002","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0275","doi-asserted-by":"crossref","first-page":"513","DOI":"10.1007\/s10571-005-3968-4","article-title":"Nicotinic agonists, antagonists, and modulators from natural sources","volume":"25","author":"Daly","year":"2005","journal-title":"Cel. Mol. Neurobiol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0280","doi-asserted-by":"crossref","first-page":"45","DOI":"10.1016\/0014-5793(90)81231-C","article-title":"Methyllycaconitine A selective probe for neuronal \u03b1lph\u03b1-bungarotoxin binding sites","volume":"270","author":"Ward","year":"1990","journal-title":"FEBS Lett."},{"key":"10.1016\/j.phrs.2015.08.018_bib0285","doi-asserted-by":"crossref","first-page":"79","DOI":"10.1016\/0014-2999(95)00191-M","article-title":"Erysodine, a competitive antagonist at neuronal nicotinic acetylcholine receptors","volume":"280","author":"Decker","year":"1995","journal-title":"Eur. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0290","doi-asserted-by":"crossref","first-page":"366","DOI":"10.1124\/mol.110.065490","article-title":"Molecular determinants for competitive inhibition of alpha4beta2 nicotinic acetylcholine receptors","volume":"78","author":"Iturriaga-V\u00e1squez","year":"2010","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0295","doi-asserted-by":"crossref","first-page":"393","DOI":"10.1002\/med.10037","article-title":"Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applications","volume":"23","author":"Romanelli","year":"2003","journal-title":"Med. Res. Rev."},{"key":"10.1016\/j.phrs.2015.08.018_bib0300","doi-asserted-by":"crossref","first-page":"865","DOI":"10.1124\/mol.64.4.865","article-title":"Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors","volume":"64","author":"Jensen","year":"2003","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0305","doi-asserted-by":"crossref","first-page":"93","DOI":"10.1016\/0014-2999(89)90012-5","article-title":"Pharmacological activity of N-methyl-carbamylcholine, a novel acetylcholine receptor agonist with selectivity for nicotinic receptors","volume":"173","author":"Boksa","year":"1989","journal-title":"Eur. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0310","doi-asserted-by":"crossref","first-page":"1413","DOI":"10.1016\/S0022-3565(25)21302-7","article-title":"RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization","volume":"279","author":"Bencherif","year":"1996","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0315","doi-asserted-by":"crossref","first-page":"204","DOI":"10.1046\/j.1471-4159.2000.0750204.x","article-title":"The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype","volume":"75","author":"Papke","year":"2000","journal-title":"J. Neurochem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0320","doi-asserted-by":"crossref","first-page":"2308","DOI":"10.1111\/j.1471-4159.1993.tb03519.x","article-title":"(+)-Anatoxin-A is a potent agonist at neuronal nicotinic acetylcholine receptors","volume":"60","author":"Thomas","year":"1993","journal-title":"J. Neurochem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0325","doi-asserted-by":"crossref","first-page":"1657","DOI":"10.1016\/S1359-6446(05)03665-2","article-title":"From ligand design to therapeutic efficacy: the challenge for nicotinic receptor research","volume":"10","author":"Cassels","year":"2005","journal-title":"Drug Discov. Today."},{"key":"10.1016\/j.phrs.2015.08.018_bib0330","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.ejphar.2006.02.012","article-title":"C3-halogenation of cytisine generates potent and efficacious nicotinic receptor agonists","volume":"536","author":"Abin-Carriquiry","year":"2006","journal-title":"Eur. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0335","doi-asserted-by":"crossref","first-page":"3474","DOI":"10.1021\/jm050069n","article-title":"Varenicline An \u03b14\u03b22 nicotinic receptor partial agonist for smoking cessation","volume":"48","author":"Coe","year":"2005","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0340","doi-asserted-by":"crossref","first-page":"985","DOI":"10.1016\/j.neuropharm.2006.10.016","article-title":"Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid","volume":"52","author":"Rollema","year":"2007","journal-title":"Neuropharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0345","doi-asserted-by":"crossref","first-page":"509","DOI":"10.1016\/S0022-3565(25)12301-X","article-title":"Epibatidine A nicotinic acetyicholine receptor agonist releases monoaminergic neurotransmitters: In vitro and in vivo evidence in rats","volume":"276","author":"Sacaan","year":"1996","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0350","doi-asserted-by":"crossref","first-page":"100","DOI":"10.1111\/j.1527-3458.2006.00100.x","article-title":"A-85380: a pharmacological probe for the preclinical and clinical investigation of the alphabeta neuronal nicotinic acetylcholine receptor","volume":"12","author":"Rueter","year":"2006","journal-title":"CNS Drug Rev."},{"key":"10.1016\/j.phrs.2015.08.018_bib0355","doi-asserted-by":"crossref","first-page":"725","DOI":"10.1016\/0028-3908(96)84644-2","article-title":"A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: In vitro pharmacological properties of a novel, high affinity \u03b14\u03b22 nicotinic acetylcholine receptor ligand","volume":"35","author":"Sullivan","year":"1996","journal-title":"Neuropharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0360","doi-asserted-by":"crossref","first-page":"2783","DOI":"10.1523\/JNEUROSCI.20-08-02783.2000","article-title":"UB-165: A novel nicotinic agonist with subtype selectivity implicates the a4b2* subtype in the modulation of dopamine release from rat striatal synaptosomes","volume":"20","author":"Sharples","year":"2000","journal-title":"J. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0365","doi-asserted-by":"crossref","first-page":"1383","DOI":"10.1016\/S0022-3565(25)13086-3","article-title":"Nicotinic agonists differ in activation and desensitization of 86Rb+ efflux from mouse thalamic synaptosomes","volume":"277","author":"Marks","year":"1996","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0370","doi-asserted-by":"crossref","first-page":"410","DOI":"10.1016\/S0022-3565(24)36807-7","article-title":"Pharmacology of Lobeline, a nicotinic receptor ligand","volume":"282","author":"Damaj","year":"1997","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0375","doi-asserted-by":"crossref","first-page":"1432","DOI":"10.1016\/S0022-3565(24)36537-1","article-title":"Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake","volume":"280","author":"Teng","year":"1997","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0380","doi-asserted-by":"crossref","first-page":"847","DOI":"10.1038\/nature04708","article-title":"Recent advances in Cys-loop receptor structure and function","volume":"440","author":"Sine","year":"2006","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0385","doi-asserted-by":"crossref","first-page":"3635","DOI":"10.1038\/sj.emboj.7600828","article-title":"Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations","volume":"24","author":"Hansen","year":"2005","journal-title":"EMBO J."},{"key":"10.1016\/j.phrs.2015.08.018_bib0390","doi-asserted-by":"crossref","first-page":"777","DOI":"10.1016\/j.bcp.2009.06.098","article-title":"Insight in nAChR subtype selectivity from AChBP crystal structures","volume":"78","author":"Rucktooa","year":"2009","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0395","doi-asserted-by":"crossref","first-page":"269","DOI":"10.1038\/35077011","article-title":"Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors","volume":"411","author":"Brejc","year":"2001","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0400","doi-asserted-by":"crossref","first-page":"E3028","DOI":"10.1073\/pnas.1208208109","article-title":"Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines","volume":"109","author":"Spurny","year":"2012","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0405","doi-asserted-by":"crossref","first-page":"270","DOI":"10.1038\/nature13293","article-title":"Crystal structure of a human GABAA receptor","volume":"512","author":"Miller","year":"2014","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0410","doi-asserted-by":"crossref","first-page":"1042","DOI":"10.1016\/j.bcp.2013.07.001","article-title":"Structural insights into Cys-loop receptor function and ligand recognition","volume":"86","author":"Nys","year":"2013","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0415","doi-asserted-by":"crossref","first-page":"511","DOI":"10.1016\/j.bbagen.2014.05.007","article-title":"Crystallographic studies of pharmacological sites in pentameric ligand-gated ion channels","volume":"1850","author":"Sauguet","year":"2015","journal-title":"Biochim. Biophys. Acta."},{"key":"10.1016\/j.phrs.2015.08.018_bib0420","doi-asserted-by":"crossref","first-page":"41299","DOI":"10.1074\/jbc.C200462200","article-title":"Tryptophan fluorescence reveals conformational changes in the acetylcholine binding protein","volume":"277","author":"Hansen","year":"2002","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0425","doi-asserted-by":"crossref","first-page":"733","DOI":"10.1038\/nrd2927","article-title":"Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system","volume":"8","author":"Taly","year":"2009","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.phrs.2015.08.018_bib0430","doi-asserted-by":"crossref","first-page":"96","DOI":"10.1016\/j.tips.2014.12.002","article-title":"Nicotinic ACh receptors as therapeutic targets in CNS disorders","volume":"36","author":"Dineley","year":"2015","journal-title":"Trends Pharmacol. Sci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0435","doi-asserted-by":"crossref","first-page":"50","DOI":"10.1016\/j.pharmthera.2014.05.004","article-title":"Role for the nicotinic cholinergic system in movement disorders; therapeutic implications","volume":"144","author":"Quik","year":"2014","journal-title":"Pharmacol. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0440","doi-asserted-by":"crossref","first-page":"16","DOI":"10.1038\/npp.2011.199","article-title":"Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia","volume":"37","author":"Jones","year":"2012","journal-title":"Neuropsychopharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0445","doi-asserted-by":"crossref","first-page":"2217","DOI":"10.4155\/fmc.12.172","article-title":"Allosteric modulators of \u03b14\u03b22 nicotinic acetylcholine receptors: a new direction for antidepressant drug discovery","volume":"4","author":"Mantione","year":"2012","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0450","doi-asserted-by":"crossref","first-page":"513","DOI":"10.1016\/B978-0-12-420118-7.00013-5","article-title":"Nicotinic receptor antagonists as treatments for nicotine abuse","volume":"69","author":"Crooks","year":"2014","journal-title":"Adv. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0455","doi-asserted-by":"crossref","first-page":"165","DOI":"10.1146\/annurev-pharmtox-010611-134525","article-title":"Drugs for allosteric sites on receptors","volume":"54","author":"Wenthur","year":"2014","journal-title":"Annu. Rev. Pharmacol. Toxicol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0460","doi-asserted-by":"crossref","first-page":"153","DOI":"10.1016\/B978-0-12-381264-3.00005-9","article-title":"Positive and negative modulation of nicotinic receptors","volume":"80","author":"Arias","year":"2010","journal-title":"Adv. Protein Chem. Struct. Biol"},{"key":"10.1016\/j.phrs.2015.08.018_bib0465","doi-asserted-by":"crossref","first-page":"915","DOI":"10.1016\/j.bcp.2011.05.001","article-title":"Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations","volume":"82","author":"Williams","year":"2011","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0470","doi-asserted-by":"crossref","first-page":"e1002612","DOI":"10.1371\/journal.pcbi.1002612","article-title":"Rational engineering of enzyme allosteric regulation through sequence evolution analysis","volume":"8","author":"Yang","year":"2012","journal-title":"PLoS Comput. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0475","doi-asserted-by":"crossref","first-page":"293","DOI":"10.1016\/j.cell.2013.03.034","article-title":"Allostery in disease and in drug discovery","volume":"153","author":"Nussinov","year":"2013","journal-title":"Cell"},{"key":"10.1016\/j.phrs.2015.08.018_bib0480","series-title":"Pharmacology of Nicotinic Acetylcholine Receptors from the Basic and Therapeutic Perspectives","first-page":"151","article-title":"Allosteric modulation of nicotinic acetylcholine receptors","author":"Arias","year":"2011"},{"key":"10.1016\/j.phrs.2015.08.018_bib0485","doi-asserted-by":"crossref","first-page":"952","DOI":"10.1016\/j.bcp.2011.04.020","article-title":"Allosteric modulators of the \u03b14\u03b22 subtype of neuronal nicotinic acethtylcholine receptors","volume":"82","author":"Pandya","year":"2011","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0490","doi-asserted-by":"crossref","first-page":"710","DOI":"10.1124\/mol.111.076026","article-title":"A series of \u03b17 nicotinic acetylcholine receptor allosteric modulators with close chemical similarity but diverse pharmacological properties","volume":"81","author":"Gill","year":"2012","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0495","doi-asserted-by":"crossref","first-page":"3552","DOI":"10.1074\/jbc.M114.619221","article-title":"Structurally similar allosteric modulators of \u03b17 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects","volume":"290","author":"Gill-Thind","year":"2015","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0500","doi-asserted-by":"crossref","first-page":"14686","DOI":"10.1073\/pnas.0804372105","article-title":"Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site","volume":"105","author":"Young","year":"2008","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0505","doi-asserted-by":"crossref","first-page":"5867","DOI":"10.1073\/pnas.1017975108","article-title":"Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site","volume":"108","author":"Gill","year":"2011","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0510","doi-asserted-by":"crossref","first-page":"1306","DOI":"10.1016\/j.neuropharm.2011.07.035","article-title":"Competitive binding at a nicotinic receptor transmembrane site of two \u03b17-selective positive allosteric modulators with differing effects on agonist-evoked desensitization","volume":"61","author":"Collins","year":"2011","journal-title":"Neuropharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0515","doi-asserted-by":"crossref","first-page":"181","DOI":"10.1016\/j.ejphar.2014.01.072","article-title":"The therapeutic promise of positive allosteric modulation of nicotinic receptors","volume":"727","author":"Uteshev","year":"2014","journal-title":"Eur. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0520","doi-asserted-by":"crossref","first-page":"2098","DOI":"10.1016\/j.biocel.2009.05.015","article-title":"Is the inhibition of nicotinic acetylcholine receptors by bupropion involved in its clinical actions?","volume":"41","author":"Arias","year":"2009","journal-title":"Int. J. Biochem. Cell Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0525","doi-asserted-by":"crossref","first-page":"211","DOI":"10.1007\/978-3-642-25758-2_8","article-title":"Nicotinic mechanisms in the treatment of psychotic disorders: A focus on the \u03b17 nicotinic receptor","volume":"213","author":"Olincy","year":"2012","journal-title":"Handb. Exp. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0530","series-title":"Carbamazepine: Medical Uses, Pharmacokinetics and Adverse Effects","first-page":"33","article-title":"Effect of carbamazepine and related compounds on ligand-gated ion channels: possible implications for synaptic transmission and side effects","author":"Di Resta","year":"2013"},{"key":"10.1016\/j.phrs.2015.08.018_bib0535","first-page":"456","article-title":"Cholinergic modulation by opioid receptor ligands: potential application to Alzheimer\u2019s disease","volume":"13","author":"Motel","year":"2013","journal-title":"Mini Rev. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0540","doi-asserted-by":"crossref","first-page":"6285","DOI":"10.1021\/cr3000829","article-title":"Ligand-gated ion channels: new insights into neurological disorders and ligand recognition","volume":"112","author":"Lemoine","year":"2012","journal-title":"Chem. Rev."},{"key":"10.1016\/j.phrs.2015.08.018_bib0545","doi-asserted-by":"crossref","first-page":"891","DOI":"10.1016\/j.bcp.2011.06.034","article-title":"Targeting the nicotinic alpha7 acetylcholine receptor to enhance cognition in disease","volume":"82","author":"Wallace","year":"2011","journal-title":"Biochem. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0550","doi-asserted-by":"crossref","first-page":"366","DOI":"10.1007\/s00894-005-0057-z","article-title":"Acetylcholine nicotinic receptors: finding the putative binding site of allosteric modulators using the blind docking approach","volume":"12","author":"Iorga","year":"2006","journal-title":"J. Mol. Model."},{"key":"10.1016\/j.phrs.2015.08.018_bib0555","doi-asserted-by":"crossref","first-page":"1874","DOI":"10.1002\/cmdc.200900320","article-title":"Structural model for the binding sites of allosterically potentiating ligands on nicotinic acetylcholine receptors","volume":"4","author":"Luttmann","year":"2009","journal-title":"Chem. Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0560","doi-asserted-by":"crossref","first-page":"695","DOI":"10.1080\/07391102.2011.10508600","article-title":"In search of allosteric modulators of \u03b17-nAChR by solvent density guided virtual screening","volume":"28","author":"Dey","year":"2011","journal-title":"J. Biomol. Struct. Dyn."},{"key":"10.1016\/j.phrs.2015.08.018_bib0565","doi-asserted-by":"crossref","first-page":"485","DOI":"10.1523\/JNEUROSCI.3483-12.2013","article-title":"Physostigmine and galanthamine bind in the presence of agonist at the canonical and noncanonical subunit interfaces of a nicotinic acetylcholine receptor","volume":"33","author":"Hamouda","year":"2013","journal-title":"J. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0570","doi-asserted-by":"crossref","first-page":"10066","DOI":"10.1021\/bi901271w","article-title":"[3H]Chlorpromazine photolabeling of the Torpedo nicotinic acetylcholine receptor identifies two state dependent binding sites in the ion channel","volume":"48","author":"Chiara","year":"2009","journal-title":"Biochemistry"},{"key":"10.1016\/j.phrs.2015.08.018_bib0575","doi-asserted-by":"crossref","first-page":"22051","DOI":"10.1074\/jbc.M801332200","article-title":"Identification of binding sites in the nicotinic acetylcholine receptor for TDBzl-etomidate, a photoreactive positive allosteric effector","volume":"283","author":"Nirthanan","year":"2008","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0580","doi-asserted-by":"crossref","first-page":"480","DOI":"10.1007\/s12031-013-0150-1","article-title":"Photoaffinity labeling of nicotinic receptors: diversity of drug binding sites","volume":"53","author":"Hamouda","year":"2014","journal-title":"J. Mol. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0585","doi-asserted-by":"crossref","first-page":"8734","DOI":"10.1523\/JNEUROSCI.1859-09.2009","article-title":"The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptors","volume":"29","author":"Seo","year":"2009","journal-title":"J. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0590","doi-asserted-by":"crossref","first-page":"3907","DOI":"10.1073\/pnas.0730718100","article-title":"Structural effects of quinacrine binding in the open channel of the acetylcholine receptor","volume":"100","author":"Yu","year":"2003","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0595","doi-asserted-by":"crossref","first-page":"13870","DOI":"10.1523\/JNEUROSCI.2652-11.2011","article-title":"Single-channel and structural foundations of neuronal \u03b17 acetylcholine receptor potentiation","volume":"31","author":"daCosta","year":"2011","journal-title":"J. Neurosci."},{"key":"10.1016\/j.phrs.2015.08.018_bib0600","first-page":"1389","article-title":"NMR structures of the human \u03b17 nAChR transmembrane domain and associated anesthetic binding sites","volume":"2014","author":"Bondarenko","year":"1838","journal-title":"Biochim. Biophys. Acta"},{"key":"10.1016\/j.phrs.2015.08.018_bib0605","first-page":"398","article-title":"NMR resolved multiple anesthetic binding sites in the TM domains of the \u03b14\u03b22 nAChR","volume":"2013","author":"Bondarenko","year":"1828","journal-title":"Biochim. Biophys. Acta"},{"key":"10.1016\/j.phrs.2015.08.018_bib0610","doi-asserted-by":"crossref","first-page":"307","DOI":"10.1016\/j.bbamem.2014.03.014","article-title":"Atomistic insights into human Cys-loop receptors by solution NMR","volume":"1848","author":"Mowrey","year":"2015","journal-title":"Biochim. Biophys. Acta."},{"key":"10.1016\/j.phrs.2015.08.018_bib0615","doi-asserted-by":"crossref","first-page":"895","DOI":"10.1016\/j.jmb.2007.03.067","article-title":"Galanthamine and non-competitive inhibitor binding to ACh-binding protein: evidence for a binding site on non-alpha-subunit interfaces of heteromeric neuronal nicotinic receptors","volume":"369","author":"Hansen","year":"2007","journal-title":"J. Mol. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0620","doi-asserted-by":"crossref","first-page":"54","DOI":"10.1038\/nature10139","article-title":"Principles of activation and permeation in an anion-selective Cys-loop receptor","volume":"474","author":"Hibbs","year":"2011","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0625","doi-asserted-by":"crossref","first-page":"1330","DOI":"10.1038\/nsmb.1933","article-title":"Structural basis of open channel block in a prokaryotic pentameric ligand-gated ion channel","volume":"17","author":"Hilf","year":"2010","journal-title":"Nat. Struct. Mol. Biol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0630","doi-asserted-by":"crossref","first-page":"E2543","DOI":"10.1073\/pnas.1418289112","article-title":"Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the \u03b17 nicotinic acetylcholine receptor","volume":"112","author":"Spurny","year":"2015","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0635","doi-asserted-by":"crossref","first-page":"137","DOI":"10.1016\/j.neuropharm.2014.12.006","article-title":"The nicotinic acetylcholine receptor and its prokaryotic homologues: Structure, conformational transitions & allosteric modulation","volume":"96","author":"Cecchini","year":"2015","journal-title":"Neuropharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0640","doi-asserted-by":"crossref","first-page":"350","DOI":"10.4161\/chan.29444","article-title":"Allosteric regulation of pentameric ligand-gated ion channels: an emerging mechanistic perspective","volume":"8","author":"Taly","year":"2014","journal-title":"Channels"},{"key":"10.1016\/j.phrs.2015.08.018_bib0645","doi-asserted-by":"crossref","first-page":"e223","DOI":"10.1016\/j.ddtec.2012.07.007","article-title":"The concept of allosteric modulation: an overview","volume":"10","author":"Changeux","year":"2013","journal-title":"Drug Discov. Today Technol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0650","doi-asserted-by":"crossref","first-page":"157","DOI":"10.1016\/j.neuropharm.2014.11.011","article-title":"The role of the M4 lipid-sensor in the folding, trafficking, and allosteric modulation of nicotinic acetylcholine receptors","volume":"96","author":"H\u00e9nault","year":"2015","journal-title":"Neuropharmacology"},{"key":"10.1016\/j.phrs.2015.08.018_bib0655","doi-asserted-by":"crossref","first-page":"35997","DOI":"10.1074\/jbc.M113.498618","article-title":"Two distinct allosteric binding sites at \u03b14\u03b22 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys-loop receptors","volume":"288","author":"Olsen","year":"2013","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0660","doi-asserted-by":"crossref","first-page":"6595","DOI":"10.1073\/pnas.1301909110","article-title":"Stoichiometry for drug potentiation of a pentameric ion channel","volume":"110","author":"daCosta","year":"2013","journal-title":"Proc. Natl. Acad. Sci. U. S. A."},{"key":"10.1016\/j.phrs.2015.08.018_bib0665","doi-asserted-by":"crossref","first-page":"5824","DOI":"10.1002\/j.1460-2075.1996.tb00969.x","article-title":"Identification of calcium binding sites that regulate potentiation of a neuronal nicotinic acetylcholine receptor","volume":"15","author":"Galzi","year":"1996","journal-title":"EMBO J."},{"key":"10.1016\/j.phrs.2015.08.018_bib0670","doi-asserted-by":"crossref","first-page":"893","DOI":"10.1016\/S0896-6273(02)00632-3","article-title":"Novel modulation of neuronal nicotinic acetylcholine receptors by association with the endogenous prototoxin lynx1","volume":"33","author":"Iba\u00f1ez-Tallon","year":"2002","journal-title":"Neuron"},{"key":"10.1016\/j.phrs.2015.08.018_bib0675","doi-asserted-by":"crossref","DOI":"10.1124\/mol.115.099663","article-title":"A Molecular Pharmacologist's Guide to GPCR Crystallography","author":"Piscitelli","year":"2015","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0680","doi-asserted-by":"crossref","first-page":"500","DOI":"10.1016\/j.bbagen.2014.04.011","article-title":"The use of LeuT as a model in elucidating binding sites for substrates and inhibitors in neurotransmitter transporters","volume":"1850","author":"Loland","year":"2015","journal-title":"Biochim. Biophys. Acta."},{"key":"10.1016\/j.phrs.2015.08.018_bib0685","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/B978-0-12-386467-3.00001-7","article-title":"Structural properties of human monoamine oxidases A and B","volume":"100","author":"Binda","year":"2011","journal-title":"Int. Rev. Neurobiol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0690","doi-asserted-by":"crossref","first-page":"10","DOI":"10.1016\/j.cbi.2010.01.042","article-title":"Acetylcholinesterase from 3D structure to function","volume":"187","author":"Dvir","year":"2010","journal-title":"Chem. Biol. Interact."},{"key":"10.1016\/j.phrs.2015.08.018_bib0695","doi-asserted-by":"crossref","first-page":"1971","DOI":"10.4155\/fmc.12.147","article-title":"Chemogenomics in drug discovery: computational methods based on the comparison of binding sites","volume":"4","author":"Vulpetti","year":"2012","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.phrs.2015.08.018_bib0700","doi-asserted-by":"crossref","first-page":"116","DOI":"10.1021\/cr040415t","article-title":"Synthesis and pharmacology of galantamine","volume":"106","author":"Marco-Contelles","year":"2006","journal-title":"Chem. Rev."},{"key":"10.1016\/j.phrs.2015.08.018_bib0705","doi-asserted-by":"crossref","first-page":"321","DOI":"10.1016\/S0014-5793(99)01637-3","article-title":"Structure of acetylcholinesterase complexed with (\u2212)-galanthamine at 2.3 A resolution","volume":"463","author":"Greenblatt","year":"1999","journal-title":"FEBS Lett."},{"key":"10.1016\/j.phrs.2015.08.018_bib0710","doi-asserted-by":"crossref","first-page":"182","DOI":"10.1002\/1097-0134(20010201)42:2<182::AID-PROT50>3.0.CO;2-1","article-title":"Three-dimensional structure of a complex of galanthamine (Nivalin) with acetylcholinesterase from Torpedo californica: implications for the design of new anti-Alzheimer drugs","volume":"42","author":"Bartolucci","year":"2001","journal-title":"Proteins"},{"key":"10.1016\/j.phrs.2015.08.018_bib0715","doi-asserted-by":"crossref","first-page":"2425","DOI":"10.1021\/bi300101r","article-title":"Bupropion binds to two sites in the Torpedo nicotinic acetylcholine receptor transmembrane domain: a photoaffinity labeling study with the bupropion analogue [(125)I]-SADU-3-72","volume":"51","author":"Pandhare","year":"2012","journal-title":"Biochemistry"},{"key":"10.1016\/j.phrs.2015.08.018_bib0720","doi-asserted-by":"crossref","first-page":"e25790","DOI":"10.1371\/journal.pone.0025790","article-title":"The atypical stimulant and nootropic modafinil interacts with the dopamine transporter in a different manner than classical cocaine-like inhibitors","volume":"6","author":"Schmitt","year":"2011","journal-title":"PLoS One"},{"key":"10.1016\/j.phrs.2015.08.018_bib0725","doi-asserted-by":"crossref","first-page":"85","DOI":"10.1038\/nature12533","article-title":"X-ray structure of dopamine transporter elucidates antidepressant mechanism","volume":"503","author":"Penmatsa","year":"2013","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0730","doi-asserted-by":"crossref","first-page":"1198","DOI":"10.1111\/j.1528-1157.1999.tb00848.x","article-title":"Mutated nicotinic receptors responsible for autosomal dominant nocturnal frontal lobe epilepsy are more sensitive to carbamazepine","volume":"40","author":"Picard","year":"1999","journal-title":"Epilepsia"},{"key":"10.1016\/j.phrs.2015.08.018_bib0735","doi-asserted-by":"crossref","first-page":"4896","DOI":"10.1038\/ncomms5896","article-title":"Structural analyses of Ca2\u207a\/CaM interaction with NaV channel C-termini reveal mechanisms of calcium-dependent regulation","volume":"5","author":"Wang","year":"2014","journal-title":"Nat. Commun."},{"key":"10.1016\/j.phrs.2015.08.018_bib0740","doi-asserted-by":"crossref","first-page":"131","DOI":"10.6026\/97320630011131","article-title":"Computer aided identification of sodium channel blockers in the clinical treatment of epilepsy using molecular docking tools","volume":"11","author":"Shaheen","year":"2015","journal-title":"Bioinformation"},{"key":"10.1016\/j.phrs.2015.08.018_bib0745","doi-asserted-by":"crossref","first-page":"308","DOI":"10.1016\/j.ejphar.2014.10.046","article-title":"Effects of antihistamines on the function of human \u03b17-nicotinic acetylcholine receptors","volume":"746","author":"Sadek","year":"2015","journal-title":"Eur. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0750","doi-asserted-by":"crossref","first-page":"65","DOI":"10.1038\/nature10236","article-title":"Structure of the human histamine H1 receptor complex with doxepin","volume":"475","author":"Shimamura","year":"2011","journal-title":"Nature"},{"key":"10.1016\/j.phrs.2015.08.018_bib0755","doi-asserted-by":"crossref","first-page":"427","DOI":"10.1111\/j.1476-5381.1996.tb15208.x","article-title":"In vitro and in vivo profile of SB 206,553, a potent 5-HT2C\/5-HT2B receptor antagonist with anxiolytic-like properties","volume":"117","author":"Kennett","year":"1996","journal-title":"Br. J. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0760","doi-asserted-by":"crossref","first-page":"863","DOI":"10.1016\/S0026-895X(24)23183-7","article-title":"Novel actions of inverse agonists on 5-HT2C receptor systems","volume":"55","author":"Berg","year":"1999","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0765","doi-asserted-by":"crossref","first-page":"766","DOI":"10.1124\/jpet.108.146514","article-title":"Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B\/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b\u2032]di pyrrole-1(2H)-carboxamide)","volume":"328","author":"Dunlop","year":"2009","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"10.1016\/j.phrs.2015.08.018_bib0770","doi-asserted-by":"crossref","first-page":"e0134444","DOI":"10.1371\/journal.pone.0134444","article-title":"Similarities between the binding sites of SB-206553 at serotonin type 2 and \u03b17 acetylcholine nicotinic receptors: rationale for its polypharmacological profile","volume":"10","author":"M\u00f6ller-Acu\u00f1a","year":"2015","journal-title":"PLoS One"},{"key":"10.1016\/j.phrs.2015.08.018_bib0775","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/S0026-895X(25)08675-4","article-title":"Agonist responses of neuronal nicotinic acetylcholine receptors are potentiated by a novel class of allosterically acting ligands","volume":"49","author":"Schrattenholz","year":"1996","journal-title":"Mol. Pharmacol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0780","doi-asserted-by":"crossref","first-page":"847","DOI":"10.1111\/j.1469-445X.1999.01837.x","article-title":"Blockage of mouse muscle nicotinic receptors by serotonergic compounds","volume":"84","author":"Garc\u00eda-Colunga","year":"1999","journal-title":"Exp. Physiol."},{"key":"10.1016\/j.phrs.2015.08.018_bib0785","doi-asserted-by":"crossref","first-page":"479","DOI":"10.1002\/neu.10146","article-title":"Unconventional ligands and modulators of nicotinic receptors","volume":"53","author":"Pereira","year":"2002","journal-title":"J. Neurobiol."}],"container-title":["Pharmacological Research"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1043661815001863?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S1043661815001863?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,5,30]],"date-time":"2025-05-30T08:08:48Z","timestamp":1748592528000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S1043661815001863"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2015,11]]},"references-count":157,"alternative-id":["S1043661815001863"],"URL":"https:\/\/doi.org\/10.1016\/j.phrs.2015.08.018","relation":{},"ISSN":["1043-6618"],"issn-type":[{"value":"1043-6618","type":"print"}],"subject":[],"published":{"date-parts":[[2015,11]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Multiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy","name":"articletitle","label":"Article Title"},{"value":"Pharmacological Research","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.phrs.2015.08.018","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"Copyright \u00a9 2015 Elsevier Ltd. All rights reserved.","name":"copyright","label":"Copyright"}]}}