Thujone Exhibits Low Affinity for Cannabinoid Receptors But Fails to Evoke Cannabimimetic Responses

@article{Meschler1999ThujoneEL,
  title={Thujone Exhibits Low Affinity for Cannabinoid Receptors But Fails to Evoke Cannabimimetic Responses},
  author={Justin P Meschler and Allyn C. Howlett},
  journal={Pharmacology Biochemistry and Behavior},
  year={1999},
  volume={62},
  pages={473-480}
}
Absinthe, an abused drug in the early 1900s, has been speculated to activate the receptors responsible for marijuana intoxication (the CB1 cannabinoid receptor) (Nature 253:365-356; 1975). To test this hypothesis, we investigated oil of wormwood (Artemisia absinthium) the active plant product found in absinthe, and thujone, the active compound found in oil of wormwood. Radioligand receptor binding assays employing membrane preparations from rat brains containing CB1 cannabinoid receptors, and… Expand
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α-Thujone reduces 5-HT3 receptor activity by an effect on the agonist-induced desensitization
Abstract The convulsant effects of α-thujone, the psychotropic component of absinthe, were attributed to inhibitory actions at the GABAA receptor. Here, we investigated for the first time the 5-HT3… Expand
The Effects of Thujone on the Function of Nicotinic Acetylcholine Receptors
Thujone is a natural compound found in plants such as “wormwood” and “sage” and it’s also found in the alcoholic drink “Absinthe”. Thujone has been suggested as a neurotoxic compound and reported to… Expand
Monoterpene α-thujone exerts a differential inhibitory action on GABA(A) receptors implicated in phasic and tonic GABAergic inhibition.
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Evidence is provided that different GABAA receptor subtypes show distinct sensitivities to α-thujone and suggest that this compound may differentially affect tonic and phasic components of GABAergic inhibition. Expand
Modulation of GABAergic synaptic currents and current responses by α-thujone and dihydroumbellulone.
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Analysis of current responses to exogenous GABA revealed that 1a reduced their amplitude, affecting their onset, desensitization, and deactivation, suggesting an effect on receptor gating, supporting the effects of 1a on GABAergic inhibition as being due to specific interactions with GABA(A)Rs. Expand
Alpha-thujone (the active component of absinthe): gamma-aminobutyric acid type A receptor modulation and metabolic detoxification.
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Alpha-thujone in absinthe and herbal medicines is a rapid-acting and readily detoxified modulator of the GABA-gated chloride channel. Expand
Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and Development
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An overview of therapeutic potential of ligands and plants modulating cannabinoid receptors that may be of interest to pharmaceutical industry in search of new and safer drug discovery and development for future therapeutics is provided. Expand
Thujone and thujone-containing herbal medicinal and botanical products: toxicological assessment.
TLDR
There are still important gaps in the knowledge required to assess thujone toxicity, the most important ones being human dose-concentration-effect relationships including the elucidation of bioavailability, and the actual toxicological consequences of potential pharmacogenetic variations and environmental factors. Expand
Absinthe and gamma-aminobutyric acid receptors.
  • R. Olsen
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 2000
TLDR
Evidence that thujone acts as a γ-aminobutyric acid type A (GABAA) receptor chloride channel blocker, much like the plant convulsant picrotoxin, and related synthetic analogs is provided. Expand
Thujone, a widely debated volatile compound: What do we know about it?
Thujone is a volatile monoterpene ketone of plant origin which is produced by several plants that are frequently used for flavoring foods and beverages. The use of thujone and thujone-containing… Expand
Thujone, a widely debated volatile compound: What do we know about it?
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Experimental results show that the phenotypic manifestation and quantity of thujones in the essential oils depend on the plant organ and its developmental phase, as well as the weather conditions and growth habitat, which might influence the ratios and the possibly unique responses of the individual species. Expand
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