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

Arneric, Stephen P.; Holladay, Mark; Williams, Michael

doi:10.1016/j.bcp.2007.06.033

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

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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Neuronal nicotinic acetylcholine receptors are a key target in medication development for nicotine dependence and other neuropsychiatric conditions.
“Neuronal nicotinic acetylcholine receptors (nAChRs) are a key target of drug discovery efforts for nicotine dependence, as well as for neuropsychiatric conditions (3).”
From Varenicline improves mood and cognition during smoking abstinence (2009) · cites this paper as [3]

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

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