Cited by 224Nicotinic Acetylcholine Receptors StudySmoking Behavior and CessationNeuroscience and Neuropharmacology Research

The DOI matches its Crossref record; 90 of the 93 references it cites were found in a registry or an index.

Neuronal nicotinic receptors: A perspective on two decades of drug discovery research

Arneric, Stephen P., Holladay, Mark, Williams, Michael·2007·Biochemical Pharmacology

DOI 10.1016/j.bcp.2007.06.033

Open this paper in CoChat — free account

Abstract

Neuronal nicotinic acetylcholine receptors (nAChRs) have been a target for drug discovery efforts, primarily for CNS indications, for the past two decades. While nicotine and related natural products have been used for smoking cessation in various formulations (e.g., gum, spray, patches), it was only in 2006 with the launch of varenicline (Chantix) by Pfizer for smoking cessation that a new chemical entity (NCE) originating from a rational medicinal chemistry effort targeting neuronal AChRs was approved. The current overview outlines the chronology of drug discovery efforts in nAChRs from the cloning of the receptor family in the 1980s, to initial research efforts at SIBIA, R.J. Reynolds and Abbott, to the current industry-wide interest in nAChR agonists as novel therapeutics for pain, schizophrenia and Alzheimer's Disease. Key events in the evolution of the nAChR field were the development of high throughput electrophysiological screening tools that provided the means to enable lead optimization efforts in medicinal chemistry and the discovery by John Daly at the NIH of the frog alkaloid, epibatidine, that provided the framework for the discovery of ABT-594, an alpha4beta2 agonist that is 200 times more potent than morphine as an analgesic. Over the next decade, it is anticipated that additional NCEs including antagonists and allosteric modulators (both positive and negative), interacting with various nAChR subtypes, will be advanced to the clinic in areas of high unmet medical need, e.g., pain, neurodegeneration, to provide novel medications with improved efficacy.

Integrity signals

Registry

Crossref · 10.1016/j.bcp.2007.06.033

Cites

90 of 90 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

This paper’s full text isn’t openly available, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

The cholinergic hypothesis of geriatric memory dysfunction
Bartus, R. T., Dean, R. L., Beer, B., & Lippa, A. S. (1982) · Science · doi:10.1126/science.7046051 · Cited by 5,545
Alzheimer's Disease: A Disorder of Cortical Cholinergic Innervation
Coyle, J. T., Price, D. L., & DeLong, M. R. (1983) · Science · doi:10.1126/science.6338589 · Cited by 3,052
The cholinergic hypothesis of Alzheimer’s disease: A review of progress
Francis, P. T., Palmer, A. M., Snape, M., & Wilcock, G. K. (1999) · Journal of Neurology, Neurosurgery & Psychiatry · doi:10.1136/jnnp.66.2.137 · Cited by 2,198 · cited 2×
“[6] Babic T, Francis PT, Palmer AM, Snape M, Wilcock GK.”
Background
A Century of Alzheimer's Disease
Goedert, M., & Spillantini, M. G. (2006) · Science · doi:10.1126/science.1132814 · Cited by 2,153
Efficacy of Varenicline, an α4β2 Nicotinic Acetylcholine Receptor Partial Agonist, vs Placebo or Sustained-Release Bupropion for Smoking Cessation<SUBTITLE>A Randomized Controlled Trial</SUBTITLE>
Jorenby, D. E. (2006) · JAMA · doi:10.1001/jama.296.1.56 · Cited by 1,635
Medicinal chemical properties of successful central nervous system drugs
Pajouhesh, H., & Lenz, G. R. (2005) · NeuroRx · doi:10.1602/neurorx.2.4.541 · Cited by 1,608
A study of the ‘desensitization’ produced by acetylcholine at the motor end‐plate
Katz, B., & Thesleff, S. (1957) · The Journal of Physiology · doi:10.1113/jphysiol.1957.sp005838 · Cited by 1,459
Identification of a Family of Muscarinic Acetylcholine Receptor Genes
Bonner, T. I., Buckley, N. J., Young, A. C., & Brann, M. R. (1987) · Science · doi:10.1126/science.3037705 · Cited by 1,423
Nicotinic Acetylcholine Receptors and Nicotinic Cholinergic Mechanisms of the Central Nervous System
Dani, J. A., & Bertrand, D. (2007) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.47.120505.105214 · Cited by 1,197
Comprehensive medicinal chemistry
Timmerman, H., Bast, A., der Goot, H. V., Vermeulen, N. P. E., & Zeelen, F. J. (1991) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(91)90535-z · Cited by 1,168

Show all 93 references

Research works printed but not linked: 7

Patrick, 1992, Drug abuse res. II. Structure, function and expression, NIDA Res Monograph, 126, 9
Arneric, 1994, ABT 418: A novel cholinergic ligand with cognition enhancing and anxiolytic activity. I. In vitro activity, J Pharmacol Exp Ther, 270, 310
Decker, 1994, ABT 418: A novel cholinergic ligand with cognition enhancing and anxiolytic activity. II. In vivo activity, J Pharmacol Exp Ther, 270, 319
Huang, 2006, The nicotinic alpha-7 receptor partial agonist MEM 3454 increases dopamine and acetylcholine release in rat media prefrontal cortex and hippocampus alone and in combination with risperidone, Neuropsychopharmacology, 31
Davis, 1932, Visceral pain, Surg Gynecol Obstet, 55, 418
Simon, 2000, Senorita with a necklace of tears, You’re The One Warner Bros. Records, CD 9, 47844
Marino, 2007, Schizophrenia, vol. 6, 17

Sorted by citations

Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system
Taly, A., Corringer, P., Guédin, D., Lestage, P. J., & Changeux, J. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2927 · Cited by 743
Pharmacological treatment of schizophrenia: a critical review of the pharmacology and clinical effects of current and future therapeutic agents
Miyamoto, S., Miyake, N., Jarskog, L. F., Fleischhacker, W. W., & Lieberman, J. A. (2012) · Molecular Psychiatry · doi:10.1038/mp.2012.47 · Cited by 584
Nicotinic acetylcholine receptors: From basic science to therapeutics
Hurst, R. S., Rollema, H., & Bertrand, D. (2012) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2012.08.012 · Cited by 543
Nicotinic ACh receptors as therapeutic targets in CNS disorders
Dineley, K. T., Pandya, A. A., & Yakel, J. L. (2015) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2014.12.002 · Cited by 460
A critical review on the potential impacts of neonicotinoid insecticide use: current knowledge of environmental fate, toxicity, and implications for human health
Thompson, D. A., Lehmler, H., Kolpin, D. W., Hladik, M. L., Vargo, J. D., Schilling, K. E., LeFevre, G. H., Peeples, T. L., Poch, M. C., LaDuca, L. E., et al. (2020) · Environmental Science Processes & Impacts · doi:10.1039/c9em00586b · Cited by 472
Natural products as a source of Alzheimer's drug leads
Williams, P., Sorribas, A., & Howes, M.-J. R. (2011) · Nat. Prod. Rep. · doi:10.1039/c0np00027b · Cited by 404
Removing Obstacles in Neuroscience Drug Discovery: The Future Path for Animal Models
Markou, A., Chiamulera, C., Geyer, M. A., Tricklebank, M., & Steckler, T. (2009) · Neuropsychopharmacology · doi:10.1038/npp.2008.173 · Cited by 328
Nicotinic Acetylcholine Receptor Signalling: Roles in Alzheimer’s Disease and Amyloid Neuroprotection
Buckingham, S. D., Jones, A. K., Brown, L. A., & Sattelle, D. B. (2009) · Pharmacological Reviews · doi:10.1124/pr.108.000562 · Cited by 312
Natural Products as a Foundation for Drug Discovery
Beutler, J. A. (2009) · Current Protocols in Pharmacology · doi:10.1002/0471141755.ph0911s46 · Cited by 306
Smoking and Pain
Shi, Y., Weingarten, T. N., Mantilla, C. B., Hooten, W. M., & Warner, D. O. (2010) · Anesthesiology · doi:10.1097/aln.0b013e3181ebdaf9 · Cited by 315
Potentiation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site
Young, G. T., Zwart, R., Walker, A., Sher, E., & Millar, N. S. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0804372105 · Cited by 262
Varenicline improves mood and cognition during smoking abstinence
Patterson, F., Jepson, C., Strasser, A. A., Loughead, J., Perkins, K. A., Gur, R. C., Frey, J. M., Siegel, S., & Lerman, C. (2009) · Biological Psychiatry · doi:10.1016/j.biopsych.2008.08.028 · Cited by 222
Toxins and drug discovery
Harvey, A. L. (2014) · Toxicon · doi:10.1016/j.toxicon.2014.10.020 · Cited by 227
Crystal structures of Lymnaea stagnalis AChBP in complex with neonicotinoid insecticides imidacloprid and clothianidin
Ihara, M., Okajima, T., Yamashita, A., Oda, T., Hirata, K., Nishiwaki, H., Morimoto, T., Akamatsu, M., Ashikawa, Y., Kuroda, S., et al. (2008) · Invertebrate Neuroscience · doi:10.1007/s10158-008-0069-3 · Cited by 161
(-)-Cytisine and derivatives: synthesis, reactivity, and applications.
Rouden, J., Lasne, M., Blanchet, J., & Baudoux, J. (2014) · Chemical Reviews · doi:10.1021/cr400307e · Cited by 113
Assembly and trafficking of nicotinic acetylcholine receptors (Review)
Millar, N. S., & Harkness, P. C. (2008) · Molecular Membrane Biology · doi:10.1080/09687680802035675 · Cited by 143
Diverse Actions and Target-Site Selectivity of Neonicotinoids: Structural Insights
Matsuda, K., Kanaoka, S., Akamatsu, M., & Sattelle, D. B. (2009) · Molecular Pharmacology · doi:10.1124/mol.109.055186 · Cited by 138
Solving the alpha-conotoxin folding problem: efficient selenium-directed on-resin generation of more potent and stable nicotinic acetylcholine receptor antagonists.
Muttenthaler, M., Nevin, S., Grishin, A., Ngo, S., Choy, P., Daly, N., Hu, S.-H., Armishaw, C., Wang, C., Lewis, R., et al. (2010) · Journal of the American Chemical Society · doi:10.1021/ja910602h · Cited by 119
Natural Products as a Foundation for Drug Discovery
Beutler, J. A. (2019) · Current Protocols in Pharmacology · doi:10.1002/cpph.67 · Cited by 138
α7 and non‐α7 nicotinic acetylcholine receptors modulate dopamine release in vitro and in vivo in the rat prefrontal cortex
Livingstone, P. D., Srinivasan, J., Kew, J. N. C., Dawson, L. A., Gotti, C., Moretti, M., Shoaib, M., & Wonnacott, S. (2009) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2009.06613.x · Cited by 133
Preclinical Models of Alzheimer's Disease: Relevance and Translational Validity
Mullane, K., & Williams, M. J. (2019) · Current Protocols in Pharmacology · doi:10.1002/cpph.57 · Cited by 129
Self-citation
Insight in nAChR subtype selectivity from AChBP crystal structures
Rucktooa, P., Smit, A. B., & Sixma, T. K. (2009) · Biochemical Pharmacology · doi:10.1016/j.bcp.2009.06.098 · Cited by 125
Nicotinic Acetylcholine Receptor-Based Blockade: Applications of Molecular Targets for Cancer Therapy
Wu, C., Lee, C., & Ho, Y. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-2434 · Cited by 126
Agonist activation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site
Gill, J. K., Savolainen, M. H., Young, G. T., Zwart, R., Sher, E., & Millar, N. S. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1017975108 · Cited by 121
The Concise Guide to PHARMACOLOGY 2013/14: Ligand‐Gated Ion Channels
Alexander, S. P. H., Benson, H. E., Faccenda, E., Pawson, A. J., Sharman, J. L., Spedding, M., Peters, J. A., Harmar, A. J., & Collaborators, C. (2013) · British Journal of Pharmacology · doi:10.1111/bph.12446 · Cited by 120
The nicotinic α6 subunit gene determines variability in chronic pain sensitivity via cross-inhibition of P2X2/3 receptors
Wieskopf, J. S., Mathur, J., Limapichat, W., Post, M. R., Alqazzaz, M., Sorge, R. E., Martin, L. J., Zaykin, D. V., Smith, S. B., Freitas, K., et al. (2015) · Science Translational Medicine · doi:10.1126/scitranslmed.3009986 · Cited by 114
Nicotinic Receptors in Neurodegeneration
Posadas, I., López‐Hernández, B., & Ceña, V. (2013) · Current Neuropharmacology · doi:10.2174/1570159x11311030005 · Cited by 116
Nicotinic receptors, allosteric proteins and medicine
Changeux, J., & Taly, A. (2008) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2008.01.001 · Cited by 115
The nicotinic acetylcholine receptor CHRNA5/A3/B4 gene cluster: Dual role in nicotine addiction and lung cancer
Improgo, M. R., Scofield, M. D., Tapper, A. R., & Gardner, P. D. (2010) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2010.05.003 · Cited by 108
Determination of the α-Conotoxin Vc1.1 Binding Site on the α9α10 Nicotinic Acetylcholine Receptor
Yu, R., Kompella, S. N., Adams, D. J., Craik, D. J., & Kaas, Q. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400041h · Cited by 95
A randomized, double-blind, placebo-controlled trial evaluating the efficacy and safety of ABT-594 in patients with diabetic peripheral neuropathic pain
Rowbotham, M. C., Duan, R. W., Thomas, J. W., Nothaft, W., & Bačkonja, M.-M. (2009) · Pain · doi:10.1016/j.pain.2009.06.013 · Cited by 91
Trends in Cell-Based Electrochemical Biosensors
Ding, L., Du, D., Zhang, X., & Ju, H. (2008) · Current Medicinal Chemistry · doi:10.2174/092986708786848514 · Cited by 90
Effects of sazetidine-A, a selective α4β2 nicotinic acetylcholine receptor desensitizing agent on alcohol and nicotine self-administration in selectively bred alcohol-preferring (P) rats
Rezvani, A. H., Slade, S., Wells, C., Petro, A., Lumeng, L., Li, T.-K., Xiao, Y., Brown, M. L., Paige, M. A., McDowell, B. E., et al. (2010) · Psychopharmacology · doi:10.1007/s00213-010-1878-8 · Cited by 88
Blockade of Neuronal α7-nAChR by α-Conotoxin ImI Explained by Computational Scanning and Energy Calculations
Yu, R., Craik, D. J., & Kaas, Q. (2011) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1002011 · Cited by 80
Differential contribution of genetic variation in multiple brain nicotinic cholinergic receptors to nicotine dependence: recent progress and emerging open questions
Greenbaum, L., & Lerer, B. (2009) · Molecular Psychiatry · doi:10.1038/mp.2009.59 · Cited by 73
Assembly of a π–π stack of ligands in the binding site of an acetylcholine-binding protein
Stornaiuolo, M., de Kloe, G. E., Rucktooa, P., Fish, A., van Elk, R., Edink, E. S., Bertrand, D., Smit, A. B., de Esch, I. J. P., & Sixma, T. K. (2013) · Nature Communications · doi:10.1038/ncomms2900 · Cited by 68
Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain
Gao, B.-X., Hierl, M., Clarkin, K., Juan, T., Nguyen, H. Q., van der Valk, M., Deng, H. X., Guo, W., Lehto, S. G., Matson, D. J., et al. (2010) · Pain · doi:10.1016/j.pain.2010.01.007 · Cited by 67
From smoking to lung cancer: the CHRNA5/A3/B4 connection
Improgo, M. R., Scofield, M. D., Tapper, A. R., & Gardner, P. D. (2010) · Oncogene · doi:10.1038/onc.2010.256 · Cited by 67
A Series of α7 Nicotinic Acetylcholine Receptor Allosteric Modulators with Close Chemical Similarity but Diverse Pharmacological Properties
Gill, J. K., Dhankher, P., Sheppard, T. D., Sher, E., & Millar, N. S. (2012) · Molecular Pharmacology · doi:10.1124/mol.111.076026 · Cited by 65
The screening toolbox of bioactive substances from natural products: A review
Wang, B., Deng, J., Gao, Y., Zhu, L., He, R., & Xu, Y. (2011) · Fitoterapia · doi:10.1016/j.fitote.2011.08.007 · Cited by 62
Recent advances in understanding the structure of nicotinic acetylcholine receptors
Zouridakis, M., Zisimopoulou, P., Poulas, K., & Tzartos, S. (2009) · IUBMB Life - A Journal of the International Union of Biochemistry and Molecular Biology · doi:10.1002/iub.170 · Cited by 65
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits
Cho, J. K., Ryu, Y. B., Long, M. J. C., Ryu, H. W., Yuk, H. J., Kim, D. W., Kim, H. J., Lee, W. S., & Park, K. H. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.02.044 · Cited by 59
Recent Developments in Novel Antidepressants Targeting α4β2-Nicotinic Acetylcholine Receptors
Yu, L.-F., Zhang, H.-K., Caldarone, B. J., Eaton, J. B., Lukas, R. J., & Kozikowski, A. P. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm401937a · Cited by 56
Therapeutic Approaches to Ion Channel Diseases
Camerino, D. C., Desaphy, J., Tricarico, D., Pierno, S., & Liantonio, A. (2008) · Advances in genetics · doi:10.1016/s0065-2660(08)00804-3 · Cited by 58
Inhibitory Evaluation of Sulfonamide Chalcones on β-Secretase and Acylcholinesterase
Kang, J., Cho, J., Curtis-Long, M. J., Ryu, H., Kim, J. H., Kim, H. J., Yuk, H., Kim, D. W., & Park, K. (2012) · Molecules · doi:10.3390/molecules18010140 · Cited by 47
Recent advances in screening of enzymes inhibitors based on capillary electrophoresis
Cheng, M., & Chen, Z. (2018) · Journal of Pharmaceutical Analysis · doi:10.1016/j.jpha.2018.05.002 · Cited by 53
Potential therapeutic uses of mecamylamine and its stereoisomers
Nickell, J. R., Grinevich, V. P., Siripurapu, K. B., Smith, A. M., & Dwoskin, L. P. (2013) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2013.04.005 · Cited by 55
Emerging Opportunities for Antipsychotic Drug Discovery in the Postgenomic Era
Marino, M. J., Knutsen, L. J. S., & Williams, M. R. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701094q · Cited by 52
Self-citation
Potentiation of analgesic efficacy but not side effects: Co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats
Zhu, C., Chin, C., Rustay, N. R., Zhong, C., Mikusa, J. P., Chandran, P., Salyers, A. K., Gomez, E. J., Simler, G. H., Lewis, L. G. R., et al. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.05.007 · Cited by 51
Neuronal receptors as targets for the action of amyloid-beta protein (Aβ) in the brain
Patel, A. N., & Jhamandas, J. H. (2012) · Expert Reviews in Molecular Medicine · doi:10.1017/s1462399411002134 · Cited by 51
Molecular Determinants for Competitive Inhibition of α4β2 Nicotinic Acetylcholine Receptors
Iturriaga‐Vásquez, P., Carbone, A. L., García‐Beltrán, O., Livingstone, P. D., Biggin, P. C., Cassels, B. K., Wonnacott, S., Zapata‐Torres, G., & Bermúdez, I. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.065490 · Cited by 50
Identification of Novel α4β2-Nicotinic Acetylcholine Receptor (nAChR) Agonists Based on an Isoxazole Ether Scaffold that Demonstrate Antidepressant-like Activity
Yu, L.-F., Tückmantel, W., Eaton, J. B., Caldarone, B. J., Fedolak, A., Hanania, T., Brunner, D., Lukas, R. J., & Kozikowski, A. P. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm201301h · Cited by 48
The Cholinergic Antagonist Gymnodimine Improves Aβ and Tau Neuropathology in an in Vitro Model of Alzheimer Disease
Alonso, E., Vale, C., Vieytes, M. R., LaFerla, F. M., Giménez‐Llort, L., & Botana, L. M. (2011) · Cellular Physiology and Biochemistry · doi:10.1159/000330086 · Cited by 48
Conotoxin Interactions with α9α10-nAChRs: Is the α9α10-Nicotinic Acetylcholine Receptor an Important Therapeutic Target for Pain Management?
Mohammadi, S. A., & Christie, M. (2015) · Toxins · doi:10.3390/toxins7103916 · Cited by 44
Varenicline for smoking cessation in people with schizophrenia: systematic review and meta-analysis
Kishi, T., & Iwata, N. (2014) · European Archives of Psychiatry and Clinical Neuroscience · doi:10.1007/s00406-014-0551-3 · Cited by 46
Novel Small Molecule α9α10 Nicotinic Receptor Antagonist Prevents and Reverses Chemotherapy-Evoked Neuropathic Pain in Rats
Wala, E. P., Crooks, P. A., McIntosh, J. M., & Holtman, J. R. (2012) · Anesthesia & Analgesia · doi:10.1213/ane.0b013e31825a3c72 · Cited by 43
Varenicline for smoking cessation: a narrative review of efficacy, adverse effects, use in at-risk populations, and adherence
Ebbert, J. O., Burke, M. V., & Hays, J. T. (2016) · Patient Preference and Adherence · doi:10.2147/ppa.s83469 · Cited by 44
Epiquinamide: A Poison That Wasn’t from a Frog That Was
Fitch, R. W., Sturgeon, G. D., Patel, S. R., Spande, T. F., Garraffo, H. M., Daly, J. W., & Blaauw, R. H. (2009) · Journal of Natural Products · doi:10.1021/np8005452 · Cited by 42
Contrasting Properties of α7-Selective Orthosteric and Allosteric Agonists Examined on Native Nicotinic Acetylcholine Receptors
Gill, J. K., Chatzidaki, A., Ursu, D., Sher, E., & Millar, N. S. (2013) · PLoS ONE · doi:10.1371/journal.pone.0055047 · Cited by 40
Effect of Nicotine on Immune System Function
Mahmoudzadeh, L., Froushani, S. M. A., Ajami, M., & Mahmoudzadeh, M. (2022) · Advanced Pharmaceutical Bulletin · doi:10.34172/apb.2023.008 · Cited by 45
α4β2* neuronal nicotinic receptor ligands (agonist, partial agonist and positive allosteric modulators) as therapeutic prospects for pain
Nirogi, R. V. S., Goura, V., Abraham, R., & Jayarajan, P. (2013) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2013.04.021 · Cited by 40
The contribution of agonist and antagonist activities of α4β2* nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data
Rollema, H., & Hurst, R. S. (2018) · Psychopharmacology · doi:10.1007/s00213-018-4921-9 · Cited by 42
Towards Combinatorial Approaches for Preserving Cognitive Fitness in Aging
Brem, A., & Sensi, S. L. (2018) · Trends in Neurosciences · doi:10.1016/j.tins.2018.09.009 · Cited by 38
Synthetic α-Conotoxin Mutants as Probes for Studying Nicotinic Acetylcholine Receptors and in the Development of Novel Drug Leads
Armishaw, C. J. (2010) · Toxins · doi:10.3390/toxins2061471 · Cited by 37
Characterizing Ligand-Gated Ion Channel Receptors with Genetically Encoded Ca++ Sensors
Yamauchi, J. G., Nemecz, Á., Nguyen, Q. T., Muller, A., Schroeder, L. F., Talley, T. T., Lindstrom, J. M., Kleinfeld, D., & Taylor, P. (2011) · PLoS ONE · doi:10.1371/journal.pone.0016519 · Cited by 37
A review of experimental techniques used for the heterologous expression of nicotinic acetylcholine receptors
Millar, N. S. (2009) · Biochemical Pharmacology · doi:10.1016/j.bcp.2009.06.015 · Cited by 36
Phase II Crossover Trial of Varenicline in Mild-to-Moderate Alzheimer's Disease
Kim, S. Y., Choi, S. H., Rollema, H., Schwam, E. M., McRae, T., Dubrava, S., & Jacobsen, J. (2013) · Dementia and Geriatric Cognitive Disorders · doi:10.1159/000355373 · Cited by 39
Aconitum and Delphinium alkaloids of curare-like activity. QSAR analysis and molecular docking of alkaloids into AChBP.
Turabekova, M., Rasulev, B., Dzhakhangirov, F., Leszczyńska, D., & Leszczynski, J. (2010) · European journal of medicinal chemistry · doi:10.1016/j.ejmech.2010.05.042 · Cited by 31
The novel small molecule α9α10 nicotinic acetylcholine receptor antagonist ZZ-204G is analgesic
Holtman, J. R., Dwoskin, L. P., Dowell, C. D., Wala, E. P., Zhang, Z., Crooks, P. A., & McIntosh, J. M. (2011) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2011.08.053 · Cited by 35
The potential role of nicotine in breast cancer initiation, development, angiogenesis, invasion, metastasis, and resistance to therapy
Khodabandeh, Z., Valilo, M., Velaei, K., & Tazehkand, A. P. (2022) · Breast Cancer · doi:10.1007/s12282-022-01369-7 · Cited by 37
Integrating multi-unit electrophysiology and plastic culture dishes for network neuroscience
Morales, R., Riss, M., Wang, L., Gavı́n, R., del Rı́o, J. A., Alcubilla, R., & Claverol-Tinturé, E. (2008) · Lab on a Chip · doi:10.1039/b802165a · Cited by 34
Design, Synthesis, and Pharmacological Characterization of Novel Spirocyclic Quinuclidinyl‐Δ2‐Isoxazoline Derivatives as Potent and Selective Agonists of α7 Nicotinic Acetylcholine Receptors
Dallanoce, C., Magrone, P., Matera, C., Frigerio, F., Grazioso, G., Amici, M. D., Fucile, S., Piccari, V., Frydenvang, K., Pucci, L., et al. (2011) · ChemMedChem · doi:10.1002/cmdc.201000514 · Cited by 35
Molecules to Selectively Target Receptors for Treatment of Pain and Neurogenic Inflammation
Andreev, Y. A., Vassilevski, A. A., & Kozlov, S. A. (2012) · Recent Patents on Inflammation & Allergy Drug Discovery · doi:10.2174/187221312798889266 · Cited by 32
Invertebrate nicotinic acetylcholine receptors -Targets for chemicals and drugs important in agriculture, veterinary medicine and human health
Sattelle, D. B. (2009) · Journal of Pesticide Science · doi:10.1584/jpestics.r09-02 · Cited by 34
Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes.
Zwart, R., Strotton, M., Ching, J., Astles, P., & Sher, E. (2014) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2014.01.031 · Cited by 30
Differential effects of subtype-specific nicotinic acetylcholine receptor agonists on early and late hippocampal LTP
Kroker, K. S., Rast, G. F., & Rosenbrock, H. (2011) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2011.09.167 · Cited by 31
Proton Transfer from the Inactive Gas-Phase Nicotine Structure to the Bioactive Aqueous-Phase Structure
Gaigeot, M., Cimas, Á., Seydou, M., Kim, J., Lee, S., & Schermann, J. (2010) · Journal of the American Chemical Society · doi:10.1021/ja103759v · Cited by 31
Consideration of allosterism and interacting proteins in the physiological functions of the serotonin transporter
Zhong, H., Sánchez, C., & Caron, M. G. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.09.020 · Cited by 30
Pathophysiology and Clinical Implications
Shi, Y., Weingarten, T. N., Mantilla, C. B., Hooten, W. M., & Warner, D. O. (2010) · Cited by 30
Treatment of imbalance with varenicline (Chantix®): report of a patient with fragile X tremor/ataxia syndrome
Zesiewicz, T. A., Sullivan, K. L., Freeman, A. A. H., & Juncos, J. L. (2008) · Acta Neurologica Scandinavica · doi:10.1111/j.1600-0404.2008.01070.x · Cited by 29
The alpha-7 nicotinic receptor partial agonist/5-HT3 antagonist RG3487 enhances cortical and hippocampal dopamine and acetylcholine release
Huang, M., Felix, A. R., Kwon, S., Lowe, D., Wallace, T. L., Santarelli, L., & Meltzer, H. Y. (2013) · Psychopharmacology · doi:10.1007/s00213-013-3373-5 · Cited by 27
Orthosteric and Allosteric Ligands of Nicotinic Acetylcholine Receptors for Smoking Cessation
Mohamed, T. S., Jayakar, S. S., & Hamouda, A. K. (2015) · Frontiers in Molecular Neuroscience · doi:10.3389/fnmol.2015.00071 · Cited by 27
Nicotinic acetylcholine receptors: Ex-vivo expression of functional, non-hybrid, heteropentameric receptors from a marine arthropod, Lepeophtheirus salmonis
Rufener, L., Kaur, K., Sarr, A., Aaen, S. M., & Horsberg, T. E. (2020) · PLoS Pathogens · doi:10.1371/journal.ppat.1008715 · Cited by 26
Acute effects of mecamylamine and varenicline on cognitive performance in non-smokers with and without schizophrenia
Roh, S., Hoeppner, S. S., Schoenfeld, D., Fullerton, C. A., Stoeckel, L. E., & Evins, A. E. (2013) · Psychopharmacology · doi:10.1007/s00213-013-3286-3 · Cited by 28
Demonstration of functional α4-containing nicotinic receptors in the medial habenula
Fonck, C., Nashmi, R., Salas, R., Zhou, C., Huang, Q., Biasi, M. D., Lester, R. A. J., & Lester, H. A. (2008) · Neuropharmacology · doi:10.1016/j.neuropharm.2008.08.021 · Cited by 26
Discovery of novel α7 nicotinic receptor antagonists
Peng, Y., Zhang, Q., Snyder, G. L., Zhu, H., Yao, W., Tomesch, J., Papke, R. L., O'Callaghan, J. P., Welsh, W. J., & Wennogle, L. P. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.06.103 · Cited by 25
Activation of α7 Nicotinic Receptors by Orthosteric and Allosteric Agonists: Influence on Single-Channel Kinetics and Conductance
Pałczyńska, M. M., Jindřichová, M., Gibb, A. J., & Millar, N. S. (2012) · Molecular Pharmacology · doi:10.1124/mol.112.080259 · Cited by 24
Principles of drug action
Evers, A. S., Maze, M., & Kharasch, E. D. (2011) · Cambridge University Press eBooks · doi:10.1017/cbo9780511781933.002 · Cited by 24
Alternative pharmacologic targets for the treatment of schizophrenia
Miyamoto, S., Jarskog, L. F., & Fleischhacker, W. W. (2013) · Current Opinion in Psychiatry · doi:10.1097/yco.0b013e32835d8296 · Cited by 23
Rat neuronal nicotinic acetylcholine receptors containing α7 subunit: pharmacological properties of ligand binding and function
Xiao, Y., Abdrakhmanova, G. R., Baydyuk, M., Hernandez, S. C., & Kellar, K. J. (2009) · Acta Pharmacologica Sinica · doi:10.1038/aps.2009.69 · Cited by 23
?7 Nicotinic Acetylcholine Receptors: A Therapeutic Target in the Structure Era
Taly, A., & Charon, S. (2012) · Current Drug Targets · doi:10.2174/138945012800398919 · Cited by 23
Neuroprotection by Nicotine Against Colchicine-Induced Apoptosis is Mediated by PI3-Kinase–Akt Pathways
Huang, X., Cheng, Z., Su, Q., Zhu, X., Wang, Q., Chen, R., & Wang, X. (2012) · International Journal of Neuroscience · doi:10.3109/00207454.2012.657377 · Cited by 23
Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts
Crestey, F., Jensen, A. A., Soerensen, C., Magnus, C. B., Andreasen, J. T., Peters, G. H. J., & Kristensen, J. L. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01895 · Cited by 22
Nicotinic Acetylcholine Receptor Subunit Alpha-5 Promotes Radioresistance via Recruiting E2F Activity in Oral Squamous Cell Carcinoma
Lin, C.-H., Lee, H., Kuei, C., Lin, H.-Y., Lu, L., Lee, F., Chang, J., Wang, J., Hsu, K., & Lin, Y. (2019) · Journal of Clinical Medicine · doi:10.3390/jcm8091454 · Cited by 22
A Role for Leu118 of Loop E in Agonist Binding to the α7 Nicotinic Acetylcholine Receptor
Amiri, S., Shimomura, M., Vijayan, R., Nishiwaki, H., Akamatsu, M., Matsuda, K., Jones, A. K., Sansom, M. S. P., Biggin, P. C., & Sattelle, D. B. (2008) · Molecular Pharmacology · doi:10.1124/mol.107.041590 · Cited by 21
CHRNA5 Contributes to Hepatocellular Carcinoma Progression by Regulating YAP Activity
Fu, Y., Ci, H., Du, W., Dong, Q., & Jia, H. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14020275 · Cited by 20
Effective Use of Animal Models for Therapeutic Development in Psychiatric and Substance Use Disorders
Phillips, A. G., Geyer, M. A., & Robbins, T. W. (2018) · Biological Psychiatry · doi:10.1016/j.biopsych.2018.01.014 · Cited by 21
Effects of nicotine on K+ currents and nicotinic receptors in astrocytes of the hippocampal CA1 region
Hernández‐Morales, M., & García‐Colunga, J. (2009) · Neuropharmacology · doi:10.1016/j.neuropharm.2009.01.024 · Cited by 19
Recent Understanding of the Molecular Mechanisms of Alzheimer?s Disease
Grimm, M. O. W., & Hartmann, T. (2011) · Journal of Addiction Research & Therapy · doi:10.4172/2155-6105.s5-004 · Cited by 20
Homology modeling and dynamics of the extracellular domain of rat and human neuronal nicotinic acetylcholine receptor subtypes α4β2 and α7
Bisson, W. H., Westera, G., Schubiger, P. A., & Scapozza, L. (2008) · Journal of Molecular Modeling · doi:10.1007/s00894-008-0340-x · Cited by 19

Authors: Arneric, S. P., Holladay, M., & Williams, M.
Affiliations: Northwestern University (US)
ORCID: Williams, Michael
Venue: Biochemical Pharmacology
Publisher: Elsevier BV
Published: 2007-10
Volume: 74
Issue: 8
Pages: 1092-1101
ISSN: 0006-2952 (ISSN-L)
DOI: 10.1016/j.bcp.2007.06.033
OpenAlex: W2080186118
Cited by: 208
References: 93
Citations by year: 2026: 1 · 2025: 3 · 2024: 1 · 2023: 3 · 2022: 7 · 2021: 1 · 2020: 5 · 2019: 5 · 2018: 10 · 2017: 5 · 2016: 12 · 2015: 14 · 2014: 9 · 2013: 19 · 2012: 16
FWCI: 1.82
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biochemical Pharmacology (publishedVersion)
PubMed (publishedVersion)
Funders: Abbott Laboratories
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Smoking Behavior and Cessation
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: neuronal nicotinic acetylcholine receptors, nicotinic agonists, history of drug discovery, varenicline, smoking cessation, epibatidine, alpha4beta2 receptor, analgesics, schizophrenia, Alzheimer's disease, pain, allosteric modulators, receptor antagonists, receptor cloning
MeSH terms: Animals, Cognition, Drug Industry, Humans, Neurons, Pain, Receptors, Nicotinic, Schizophrenia, Drug Design, Smoking Cessation

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Neuronal nicotinic receptors: A perspective on two decades of drug discovery research

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Citations

Cites

Cited by

Related

Metadata

Record

About these checks