ArticlePloS one2016
Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism.
Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
20 citing papers in PubMed, 83 citations in OpenAlex.
- Kavalactones support motivation to move during intensive training in males preparing for military special operations forces.Journal of the International Society of Sports Nutrition · 2024Trial
- Neuroimaging Insights: Kava's (Nutrients · 2023Trial
- Kava (Nutrients · 2026Review
- Kava (Piper methysticum) consumption patterns and conceptualizations: results from an online survey.Substance abuse treatment, prevention, and policy · 2026Article
- Efficacy and Safety of Herbal Supplements with Anxiolytic, Antidepressant, and Sedative Action: A Review of Clinical Data and Toxicological Risks.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Clinically characterizing adults who use kava or kratom: Substance use disorder assessment challenges for increasingly popular botanical products.Drug and alcohol dependence reports · 2025Article
- Developing an approach for evaluating the cardiotoxic potential of botanicals.Frontiers in toxicology · 2025Review
- Efficacy and safety of pharmacotherapy in chronic insomnia: A review of clinical guidelines and case reports.The mental health clinician · 2023Review
- Isobolographic analysis of adjunct antiseizure activity of the FDA-approved cannabidiol with neurosteroids and benzodiazepines in adult refractory focal onset epilepsy.Experimental neurology · 2023Article
- Intrinsic Ability of the β-Oxidation Pathway To Produce Bioactive Styrylpyrones.Angewandte Chemie (International ed. in English) · 2022Article
- Article
- Engineered biosynthesis of plant polyketides by type III polyketide synthases in microorganisms.Frontiers in bioengineering and biotechnology · 2022Review
- Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC).Biochemical pharmacology · 2021Article
- Construction of an Artificial Biosynthetic Pathway for the Styrylpyrone Compound 11-Methoxy-Bisnoryangonin Produced in EngineeredFrontiers in microbiology · 2021Article
- Kava as a Clinical Nutrient: Promises and Challenges.Nutrients · 2020Review
- Evaluation of Anti-Convulsive Properties of Aqueous Kava Extract on Zebrafish Using the PTZ-Induced Seizure Model.Brain sciences · 2020Article
- A New Hypothesis on Anxiety, Sleep Insufficiency, and Viral Infections; Reciprocal Links to Consider in Today's "World vs. COVID-19" Endeavors.Frontiers in psychiatry · 2020Review
- A Behavioral Survey of the Effects of Kavalactones onJournal of experimental neuroscience · 2017Article
- Interactions of Desmethoxyyangonin, a Secondary Metabolite fromEvidence-based complementary and alternative medicine : eCAM · 2017Article
- Herbal Highs: Review on Psychoactive Effects and Neuropharmacology.Current neuropharmacology · 2017Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Extracts of the pepper plant kava (Piper methysticum) are effective in alleviating anxiety in clinical trials. Despite the long-standing therapeutic interest in kava, the molecular target(s) of the pharmacologically active constituents, kavalactones have not been established. γ-Aminobutyric acid type A receptors (GABAARs) are assumed to be the in vivo molecular target of kavalactones based on data from binding assays, but evidence in support of a direct interaction between kavalactones and GABAARs is scarce and equivocal. In this study, we characterised the functional properties of the major anxiolytic kavalactone, kavain at human recombinant α1β2, β2γ2L, αxβ2γ2L (x = 1, 2, 3 and 5), α1βxγ2L (x = 1, 2 and 3) and α4β2δ GABAARs expressed in Xenopus oocytes using the two-electrode voltage clamp technique. We found that kavain positively modulated all receptors regardless of the subunit composition, but the degree of enhancement was greater at α4β2δ than at α1β2γ2L GABAARs. The modulatory effect of kavain was unaffected by flumazenil, indicating that kavain did not enhance GABAARs via the classical benzodiazepine binding site. The β3N265M point mutation which has been previously shown to profoundly decrease anaesthetic sensitivity, also diminished kavain-mediated potentiation. To our knowledge, this study is the first report of the functional characteristics of a single kavalactone at distinct GABAAR subtypes, and presents the first experimental evidence in support of a direct interaction between a kavalactone and GABAARs.
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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.