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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
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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.

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Crossref · 10.1016/j.bcp.2007.06.033

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3 of the 93 references couldn’t be matched to a known paper.

Research works printed but not linked: 7

  1. Patrick, 1992, Drug abuse res. II. Structure, function and expression, NIDA Res Monograph, 126, 9
  2. Arneric, 1994, ABT 418: A novel cholinergic ligand with cognition enhancing and anxiolytic activity. I. In vitro activity, J Pharmacol Exp Ther, 270, 310
  3. Decker, 1994, ABT 418: A novel cholinergic ligand with cognition enhancing and anxiolytic activity. II. In vivo activity, J Pharmacol Exp Ther, 270, 319
  4. 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
  5. Davis, 1932, Visceral pain, Surg Gynecol Obstet, 55, 418
  6. Simon, 2000, Senorita with a necklace of tears, You’re The One Warner Bros. Records, CD 9, 47844
  7. Marino, 2007, Schizophrenia, vol. 6, 17

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Metadata

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

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