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

  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},

The Effects of Thujone on the Function of Nicotinic Acetylcholine Receptors

Thujone inhibits human nAChRs with different potencies using the two electrode voltage clamp method and was found to be independent of membrane potential and did not compete with ACh.

Modulation of GABAergic synaptic currents and current responses by α-thujone and dihydroumbellulone.

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.

Alpha-thujone (the active component of absinthe): gamma-aminobutyric acid type A receptor modulation and metabolic detoxification.

Alpha-thujone in absinthe and herbal medicines is a rapid-acting and readily detoxified modulator of the GABA-gated chloride channel.

Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and Development

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.

Absinthe and gamma-aminobutyric acid receptors.

  • R. Olsen
  • Biology
    Proceedings of the National Academy of Sciences of the United States of America
  • 2000
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.

Thujone, a widely debated volatile compound: What do we know about it?

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.

Care and Feeding of the Endocannabinoid System: A Systematic Review of Potential Clinical Interventions that Upregulate the Endocannabinoid System

Evidence indicates that several classes of pharmaceuticals upregulate the eCB system, including analgesics, non-steroidal anti-inflammatory drugs, opioids, glucocorticoids, antidepressants, antipsychotics, anxiolytics, and anticonvulsants.



Nonclassical cannabinoid analgetics inhibit adenylate cyclase: development of a cannabinoid receptor model.

It is postulated that the receptor that is associated with the regulation of adenylate cyclase in vitro may be the same receptor as that mediating analgesia in vivo, and a conceptualization of the cannabinoid analgetic receptor is presented.

Cannabinoid receptor agonists and antagonists

The major advances of the last five years are the emergence of selective CB2 agonists (Merck, Sanofi) with potential applications as immunomodulants and the development of the first selective CB1 antagonist SR141716, followed recently by the first CB2 antagonist SR 144528.

In vivo characterization of a specific cannabinoid receptor antagonist (SR141716A): inhibition of delta 9-tetrahydrocannabinol-induced responses and apparent agonist activity.

It is not clear whether this pharmacological activity represents an uncharacterized action of SR141716A, or an index of tonic activity of an endogenous cannabinergic system, but it will be useful in establishing the biochemical events responsible for the in vivo effects of exogenous cannabinoids, as well as inestablishing the existence of a putative endogenous cannabinoidergic system.

Determination and characterization of a cannabinoid receptor in rat brain.

The criteria for a high affinity, stereoselective, pharmacologically distinct cannabinoid receptor in brain tissue have been fulfilled.

Cannabinoid inhibition of adenylate cyclase. Biochemistry of the response in neuroblastoma cell membranes.

  • A. Howlett
  • Biology, Chemistry
    Molecular pharmacology
  • 1985
It is inferred that the cannabimimetic compounds must act via regulatory mechanisms similar to those operating for receptor-mediated inhibition of adenylate cyclase, as well as by muscarinic cholinergic compounds.

Modulation by mu-opioid agonists of guanosine-5'-O-(3-[35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells.

The opioid agonist-mediated stimulation of [35S]GTP gamma S binding in SH-SY5Y cell membranes provides a "functional" measure of agonist occupation of mu-opioid receptors and offers a simple method for the determination of efficacy and intrinsic activity of mu

Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations.

The results suggest that CB1 and CB2 can be considered as tissue-selective antigens of the central nervous system and immune system, respectively, and cannabinoids may exert specific receptor-mediated actions on the immune system through the CB2 receptor.