Caffeine as a psychomotor stimulant: mechanism of action

  title={Caffeine as a psychomotor stimulant: mechanism of action},
  author={Gilberto Fisone and Anders Borgkvist and Alessandro Usiello},
  journal={Cellular and Molecular Life Sciences CMLS},
The popularity of caffeine as a psychoactive drug is due to its stimulant properties, which depend on its ability to reduce adenosine transmission in the brain. Adenosine A1 and A2A receptors are expressed in the basal ganglia, a group of structures involved in various aspects of motor control. Caffeine acts as an antagonist to both types of receptors. Increasing evidence indicates that the psychomotor stimulant effect of caffeine is generated by affecting a particular group of projection… 
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The action of caffeine within the striatum is described to provide a possible molecular mechanism at the basis of the psychomotor and reinforcing properties of this pharmacological agent.
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    Medicine and science in sports and exercise
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Evidence of caffeine's effects on the motor evoked potential, Hoffman reflex, self-sustained firing of the alpha motor neuron, and pain and force sensation are presented as well as limitations and considerations of using the drug in human neuromuscular studies are presented.


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A role for adenosine in a diverse array of neural phenomena, which include regulation of sleep and the level of arousal, neuroprotection, regulation of seizure susceptibility, locomotor effects, analgesia, mediation of the effects of ethanol, and chronic drug use, is established.
Caffeine Induces Dopamine and Glutamate Release in the Shell of the Nucleus Accumbens
It is demonstrated that systemic administration of behaviorally relevant doses of caffeine can preferentially increase extracellular levels of dopamine and glutamate in the shell of the NAc, suggesting that caffeine, because of its ability to block adenosine A1 receptors, shares neurochemical properties with other psychostimulants, which could contribute to the widespread consumption of caffeine-containing beverages.
Involvement of DARPP-32 phosphorylation in the stimulant action of caffeine
It is shown that the stimulatory effect of caffeine on motor activity in mice was greatly reduced following genetic deletion of DARPP-32 (dopamine- and cyclic AMP-regulated phosphoprotein of relative molecular mass 32,000), and caffeine increased the state of phosphorylation of DAR PP-32 at Thr 75.
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The GABAergic striopallidal neuron, which is a key component of the indirect striatal efferent pathway, is a main locus for A2-D2 interactions in the brain and possibly a main target for the central actions of adenosine agonists and antagonists.