ArticlePloS one2015
Nicotinic Activity of Arecoline, the Psychoactive Element of "Betel Nuts", Suggests a Basis for Habitual Use and Anti-Inflammatory Activity.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
53 citing papers in PubMed, 1 synthesis or guideline pooled it, 125 citations in OpenAlex.
- Betel nut chewing and the risk of chronic kidney disease: evidence from a meta-analysis.International urology and nephrology · 2018Pooled it
- Arecoline as a Novel Scaffold Targeting the ATAD2 Bromodomain for Cell Cycle Modulation.Pharmaceutics · 2026Article
- An evolutionary perspective on the use of betel nut and its effects on health outcomes.Evolution, medicine, and public health · 2026Article
- Targeting monoamine oxidases for the treatment of betel quid dependence: a potential pharmacological and neurobiological approach.Frontiers in pharmacology · 2026Review
- Therapeutic Potential of Methanolic Extract ofJournal of pharmacopuncture · 2025Article
- Neuromodulatory Effects of Arecoline on Anxiety-like Behavior in Mice Exposed to Chronic Unpredictable Mild Stress.International journal of molecular sciences · 2025Article
- Arecoline upregulates CD155 expression to facilitate immune evasion in oral squamous cell carcinoma.Journal for immunotherapy of cancer · 2025Article
- Neuroprotective Effects and Mechanisms of Arecoline Against HInternational journal of molecular sciences · 2025Article
- Article
- Development of Subcritical Water Extraction for Areca Alkaloids and Its Influence on the Structure of Areca Nut Husk.Molecules (Basel, Switzerland) · 2025Article
- In vitro hydrolysis of areca nut xenobiotics in human liver.Drug metabolism and pharmacokinetics · 2025Article
- Modulation of neural activity and gene expression by arecoline.Frontiers in integrative neuroscience · 2025Article
- Comprehensive Insights into Arecoline Hydrobromide: Pharmacology, Toxicity, and Pharmacokinetics.Medical science monitor : international medical journal of experimental and clinical research · 2024Review
- Research on the Anti-Fatigue Effects and Mechanisms of Arecoline in Sleep-Deprived Mice.Nutrients · 2024Article
- Overlap in oncogenic and pro-inflammatory pathways associated with areca nut and nicotine exposure.Cancer pathogenesis and therapy · 2024Article
- Functions and pharmacology of α2β2 nicotinic acetylcholine receptors; in and out of the shadow of α4β2 nicotinic acetylcholine receptors.Biochemical pharmacology · 2024Article
- Design, synthesis, and evaluation of novel arecoline-linked amino acid derivatives for insecticidal and antifungal activities.Scientific reports · 2024Article
- Bioactive Components of Areca Nut: An Overview of Their Positive Impacts Targeting Different Organs.Nutrients · 2024Review
- Comprehensive insights into areca nut: active components and omics technologies for bioactivity evaluation and quality control.Frontiers in pharmacology · 2024Review
- A Critical Interpretive Synthesis of the Role of Arecoline in Oral Carcinogenesis: Is the Local Cholinergic Axis a Missing Link in Disease Pathophysiology?Pharmaceuticals (Basel, Switzerland) · 2023Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Habitual chewing of "betel nut" preparations constitutes the fourth most common human self-administration of a psychoactive substance after alcohol, caffeine, and nicotine. The primary active ingredient in these preparations is arecoline, which comes from the areca nut, the key component of all such preparations. Arecoline is known to be a relatively non-selective muscarinic partial agonist, accounting for many of the overt peripheral and central nervous system effects, but not likely to account for the addictive properties of the drug. We report that arecoline has activity on select nicotinic acetylcholine receptor (nAChR) subtypes, including the two classes of nAChR most related to the addictive properties of nicotine: receptors containing α4 and β2 subunits and those which also contain α6 and β3 subunits. Arecoline is a partial agonist with about 6-10% efficacy for the α4* and α6* receptors expressed in Xenopus oocytes. Additionally, arecoline is a silent agonist of α7 nAChR; while it does not activate α7 receptors when applied alone, it produces substantial activation when co-applied with the positive allosteric modulator PNU-120696. Some α7 silent agonists are effective inhibitors of inflammation, which might account for anti-inflammatory effects of arecoline. Arecoline's activity on nAChR associated with addiction may account for the habitual use of areca nut preparations in spite of the well-documented risk to personal health associated with oral diseases and cancer. The common link between betel and tobacco suggests that partial agonist therapies with cytisine or the related compound varenicline may also be used to aid betel cessation attempts.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.