Locomotor activation by theacrine, a purine alkaloid structurally similar to caffeine: Involvement of adenosine and dopamine receptors

  title={Locomotor activation by theacrine, a purine alkaloid structurally similar to caffeine: Involvement of adenosine and dopamine receptors},
  author={Allison A. Feduccia and Yuanyuan Wang and Jeffrey A. Simms and Henry Yi and Rui Li and Leonard F. Bjeldanes and Chuang-xing Ye and Selena E Bartlett},
  journal={Pharmacology Biochemistry and Behavior},

Assessment of the Drug-Drug Interaction Potential Between Theacrine and Caffeine in Humans.

Hemodynamic parameters were unaltered despite the pharmacokinetic interaction, suggesting that coadministration of caffeine and theacrine is safe at the doses administered, and Enhanced oral bioavailability is the most likely mechanism by which caffeine alters the ACrine exposure.

Theacrine, a purine alkaloid from kucha, protects against Parkinson's disease through SIRT3 activation.

A Two-Part Approach to Examine the Effects of Theacrine (TeaCrine®) Supplementation on Oxygen Consumption, Hemodynamic Responses, and Subjective Measures of Cognitive and Psychometric Parameters

The impact of theacrine (TeaCrine®, TC) was used to examine subjective dose–response, daily changes in cognitive and psychometric parameters, and changes in gas exchange and vital signs in humans to better ascertain the previously reported animal and human outcomes involvingTheacrine administration.

A Toxicological Evaluation of Methylliberine (Dynamine®)

The toxicological investigation of a pure, synthetic form of methylliberine, a methoxiuric acid present at low levels in various Coffea plants, found no toxicological data in the public domain, and no mortality or morbidity was observed and no toxicologically relevant clinical effects or effects on clinical pathology parameters were observed.

Safety of TeaCrine®, a non-habituating, naturally-occurring purine alkaloid over eight weeks of continuous use

These findings support the clinical safety and non-habituating neuro-energetic effects of TeaCrine® supplementation over 8 weeks of daily use (up to 300 mg/day) and there was no evidence of a tachyphylactic response that is typical of neuroactive agents such as caffeine and other stimulants.

Caffeine and Methylliberine: A Human Pharmacokinetic Interaction Study

It is found that methylliberine altered caffeine pharmacokinetics without a reciprocal interaction, which suggests caffeine may interact uniquely with different methylurates.

Assessment of Pharmacokinetic Interaction Potential Between Caffeine and Methylliberine

It is found that methylliberine altered caffeine pharmacokinetics without a reciprocal interaction, which suggests caffeine may interact uniquely with different methylurates.

Theacrine, a purine alkaloid obtained from Camellia assamica var. kucha, attenuates restraint stress-provoked liver damage in mice.

Oral administration of theacrine was found to decrease plasma ALT and AST levels, reduce hepatic mRNA levels of inflammatory mediators, and reverse the histologic damages in stressed mice, suggesting that the ACrine is possibly a good candidate for protecting against or treating lifestyle diseases and might contribute to the study of natural products.

Cognitive Performance and Mood Following Ingestion of a Theacrine-Containing Dietary Supplement, Caffeine, or Placebo by Young Men and Women

TheaTrim treatment does not result in a statistically significant improvement in cognitive performance but may favorably impact multiple subjective feelings related to energy and mood, as well as objective measures of cognitive performance, heart rate, and blood pressure.



Theacrine, a special purine alkaloid with sedative and hypnotic properties from Cammelia assamica var. kucha in mice

Results indicated that theacrine possessed potent sedative and hypnotic properties and its central nervous system effects were different from those of caffeine and theobromine.

Caffeine as a psychomotor stimulant: mechanism of action

The present review focuses on the effects of caffeine on striatal signal transduction and on their involvement in caffeine-mediated motor stimulation.

Involvement of adenosine A1 receptors in the discriminative-stimulus effects of caffeine in rats

Adenosine A1 receptor blockade is involved in the discriminative-stimulus effects of behaviorally relevant doses of caffeine; A2A receptor blockade does not play a central role in caffeine’s discrim inative effects and counteracts the A1 receptors-mediated discriminatives-stimuli effects of caffeine.

Adenosine receptors and behavioral actions of methylxanthines.

The data strongly suggest that the behavioral stimulant effects of methylxanthines involve a blockade of central adenosine receptors.

Subchronic caffeine administration sensitizes rats to the motor-activating effects of dopamine D1 and D2 receptor agonists

Subchronic caffeine, by sensitizing the motor stimulant effects of dopamine D1 and D2 receptor agonists, produces adaptive changes which might result in a potentiation of the dopaminergic component of drugs of abuse.

The stimulant effects of caffeine on locomotor behaviour in mice are mediated through its blockade of adenosine A2A receptors

The results suggest that the stimulant effect of low doses of caffeine is mediated by A2A receptor blockade while the depressant effect seen at higher doses under some conditions is explained by A1 receptor blockade.

The Stimulatory Action and the Development of Tolerance to Caffeine Is Associated with Alterations in Gene Expression in Specific Brain Regions

Neuron pathways that are regulated by adenosine A1 and/or A2A receptors and are targets for the stimulatory action of caffeine are identified and adaptive changes in gene expression in these brain areas were associated with the development of locomotor tolerance to caffeine.

Involvement of Adenosine A1 and A2A Receptors in the Motor Effects of Caffeine after its Acute and Chronic Administration

The results suggest that the motor-activating effects of acutely administered caffeine in rats involve the central blockade of both A1 and A2A receptors and that the residual motor-activation effects of caffeine in tolerant individuals might be mostly because of A2 a receptor blockade.