Top performers, both professionals, and students are always seeking smart drugs that can maximize their cognitive ability to give them an edge in their highly competitive worlds. Aniracetam is one of those intelligence boosters that many individuals eagerly want. It enjoys a popular international following, scientific backing and many decades of trusted use in the market. That is because it greatly improves mental performance by enhancing learning, retaining knowledge, verbal smoothness and even has neuroprotective ability.   

 

What is Aniracetam?

Aniracetam, also known as N-anisoyl-2-pyrrolidinone, is a fat-soluble racetam that has an additional anosiyl ring with a methoxy group, which replaces the amine group of Piracetam. (1)  This modification is necessary to enhance fat solubility. The anosiyl-methoxy group also makes it different and five times more potent than its elder cousin, Piracetam.

 

How Does Aniracetam Work?

When taken orally, Aniracetam is quickly broken down and passes through the hepatic metabolism. It is then absorbed into the bloodstream and carried to various cells where it acts as an AMPA receptor modulator. (2) Aniracetam takes about 20 minutes to start being effective, and its half-life is between 1 and 2.5 hours. For this reason, Aniracetam is best for short bursts of intense work, and it has to be taken at regular intervals throughout the day.

The 4-isoxazolepropionic acid (AMPA) receptors are the most commonly found receptors in the nervous system. They mediate fast synaptic transmission of neural messages in the central nervous system. (3) AMPA is also one of the three subsets of glutamate receptors that are important for neural communication, memory formation, and learning.

Activation of AMPA receptors potentiates the release of noradrenaline, a catecholamine neurotransmitter that acts during sympathetic nervous stimulation. Noradrenaline causes vasoconstriction, which redirects blood supply to the essential organs like the brain, heart, lungs, and kidneys. The brain benefits explicitly in that messages are relayed faster, thinking is hastened, and one can make quick decisions. (4)

Additionally, Aniracetam also acts as a cholinergic. (5) It enhances dopamine and serotonin release in the prefrontal cortex mainly by facilitating the action of N-anisoyl-GABA on nicotinic acetylcholine receptors. Activation of the cholinergic system improves cognitive function and brain health. (6)

Aniracetam is also known to enhance cerebral blood flow and activity in the area of the brain that is responsible for collective and holistic thinking. (7)

 

What are the Top Benefits of Aniracetam?

  • 1. Anxiolytic
  • Aniracetam has been shown to reduce the measures of anxiety, both in laboratory animals and humans. It does so through activation of serotonergic, dopaminergic and cholinergic systems. (8) Serotonin plays a role in allaying anxiety and actually, dipping levels of serotonin are the leading cause of anxiety disorders. A study published in the Journal of Neuropsychopharmacology in 2013, demonstrated that mice without 5-HT1A receptor (a serotonin receptor) early in life, developed anxiety in adulthood. Moreover, some anxiolytic drugs like Selective Serotonin Reuptake Inhibitors (SSRIs) work by blocking reabsorption of serotonin in the brain, in order to make more serotonin available.

    The dopaminergic system, also affected by Aniracetam, modulates GABA and glutamate neurotransmitters. (9) Gamma-aminobutyric acid (GABA) is the primary neurotransmitter that is well-known to counterbalance the excessive excitations of the brain, in the same way, that an anxiolytic known as benzodiazepine works.

    Aniracetam also calms anxiety by lessening social inhibitions and improving verbal fluency, thus helping people with social anxiety feel relaxed and express themselves more fluidly. Therefore, if preparing for a presentation or you experience stage fright, then Aniracetam is the nootropic of choice.

  • 2. Helps Boost Mood

  • Another very positive effect of Aniracetam is that it has an anti-depressant effect and mood enhancing quality. It primarily enhances mood by increasing serotonin and dopamine, the two main neurotransmitters that are associated with positive feelings. (10) There have been various studies that have investigated this specific effect of Aniracetam, all proving that it boosts mood.

    For instance, the results of a study (11) that used 100mg/kg of Aniracetam on young rats showed that it was effective in improving mobility, as the rats were subjected to a involuntary swim stress-induced motionlessness test. The investigators credited this to the combined effects of 2-pyrrolidinone and N-anisoyl-GABA on the dopaminergic transmission pathway. The fact that this study used young rats suggests that Aniracetam can be quite useful on a young brain, that is not necessarily damaged or has experienced deterioration related to aging.

    Taking Aniracetam regularly is hence a way to ensure that one wakes up and faces the day full of energy and with motivation for completing daily tasks.

  • 3. Improves Focus

  • Aniracetam increases attentiveness by reducing impulsivity caused by distractions. The effect is that Aniracetam users have a better awareness of their surroundings and can thus broaden their attention span. With greater attention, one can significantly ease the task at hand that requires intense mental focus. These effects are due to increases in acetylcholine receptor activation.

    It also exhibits other effects such as increasing noradrenaline levels in the brain, for a stimulant upshot that intensifies alertness and attention.

    In a study (12) carried out to assess the effects of Aniracetam on attention deficit and low vigilance, the researchers were able to demonstrate that it; improves arousal when performing mental tasks, increases response speed and accuracy. The changes were mainly mediated by stimulation of serotonin, cholinergic and glutamatergic systems.

  • 4. Increases Memory

  • In the hippocampus, the region that is associated with new memory formations, aniracetam has been found to decrease the rate of desensitization of receptors and encourage acetylcholine release. Together, these two actions improve reasoning, language, and attention, thereby creating a conducive environment for both short and long-term memory.  Other than refining general memory formation, aniracetam is also powerful when it comes to speeding up the recall process. This is the critical cognitive function that helps us to remember the right things at the right time.

    In a study (13) published in the Journal of the European College of Neuropsychopharmacology, 190 elderly patients suffering mild to moderate cognitive impairment and fulfilled the criteria for dementia, were given Aniracetam for six months. The study participants then underwent clinical, behavioral and psychological evaluation after every month. At the end of the study period, the participants showed significant improvement in memory and other psychobehavioral parameters.

    In another study (14) on rats, the researchers noted that the study subjects had improved memory, learning, and muscle movement after administration of aniracetam for seven days. The investigators attributed these changes to increase in acetylcholine levels, which enhances the process of consolidation of memory traces.

  • 5. Could Help Improve Sleep

  • Through the serotonergic system, aniracetam helps regulate the body’s sleep-wake cycle. It appears to increase Rapid Eye Movement (REM) sleep activity and promote lucid dreams. (15) Some users also report that it has a sedating and tranquilizing effect, which is what helps one to fall asleep quickly. This effect is also in direct relation to anti-depressant and anxiolytic qualities Aniracetam, which calm the mind and alleviate stress.

    For Aniracetam to improve sleep quality, it should not be taken close to bedtime. If taken late at night, it causes delayed time for onset of sleep instead. This is because it has a stimulatory effect that increases mental energy, making it difficult to shut off the mind.

  • 6. Helps with Brain Damage Recovery

  • Aniracetam alleviates the damage done to memory and learning by cholinergic antagonists, cerebral ischemia, and electroconvulsive shock. (16) It also protects against scopolamine-induced impairment. (17) Scopolamine, also known as the devil’s breath, is a drug that criminals use to erase memory and render one incapable of exercising their free will. Aniracetam reverses its effect by improving cognitive functioning in the different phases of learning and memory process.

    Another interesting neuroprotective feature of aniracetam is that it reverses the effects of fetal alcohol syndrome, by increasing the amount of AMPA receptors in the hippocampus. (18) This indicates that intake of Aniracetam enhances the growth of neurons and even has the ability to promote recovery after a traumatic brain injury. This claim is further supported by a study (19) published in the Neuroscience Letters journal. The study assesses the neurotrophic effects of aniracetam, and the results showed that Aniracetam influences remodeling of neural network after injury.

    Aniracetam also promotes brain damage recovery by increasing blood circulation and at the same time improving energy and oxygen supply. This is particularly important for people who have suffered cerebral infarction such as in strokes. (20)

    Suggested Dosage, Synergies, and Administration of Aniracetam

    For dosage, laboratory settings use strengths between 10mg/kg and 100mg/kg. Most nootropic users use doses as low as 400mg with desirable effect. It is also common for some users to go as high as 1000 to 1500mg in two divided doses (500 to 750mg) twice daily. (7) Aniracetam is a bit potent, so taking higher doses may put extra strain on the body as it gets absorbed fast. When starting off, begin with the lower doses then gradually scale higher. It is also recommended that the doses should remain the same throughout the day and daily, to maintain a steady state in circulation.

    It is critical to note that the doses are adjusted according to individual needs. It is therefore crucial to always consult the doctor before taking any drug, not just Aniracetam. It is also very vital to mention whether you have any underlying medical conditions or you are on any other medications.

    Aniracetam is fat soluble (7), thus needs to be taken with a meal rich in good fats such as eggs and yogurt, for the best results possible. Moreover, it can be taken with an oil supplement such as fish oil, to enhance its absorption.  

    Aniracetam is available as a powder, capsules or tablets. The powder formulation is digested and absorbed quicker while the pills take more time for their effects to be seen. However, Aniracetam as a powder has a bitter taste that some people cannot stand. If that is a problem, then getting capsules is a better purchase.

    All nootropics have some level of unwanted side effects, and Aniracetam is no exception. The most common side effects of aniracetam are headaches, fatigue, nausea, insomnia and general distress. However, these side effects are fairly mild and not enough to discredit the use of Aniracetam in any way.

    Combining different racetams is a good idea since they all have different mechanisms of action. The most frequent combination is that of Aniracetam and Piracetam or Aniracetam and Oxiracetam. It is also a prudent idea to stack Aniracetam with a source of choline (alpha GPC or CDP choline), to mitigate the headaches that are a common occurrence when taking racetams. (21) Aniracetam increases the uptake and utilization of acetylcholine, and a deficiency of choline will undoubtedly lead to headaches. It therefore makes sense to supply the raw materials (choline) for acetylcholine formation.

     

    History and Origin of Aniracetam

    The first synthesized member of the racetam family was Piracetam, then the second one, (Aniracetam) followed shortly after. Aniracetam was first made in the 1970s by Hoffmann-La Roche, a Swiss multinational company that operates as a Pharmaceuticals and Diagnostics. (22)  

    Currently, Aniracetam is sold as a prescription drug in Europe as a remedy for memory decline caused by aging and neurodegenerative disorders, but in the United States it is unregulated and only sold for research purposes. However, it is still legal to buy and own Aniracetam for personal use in the US.  

    Final Thoughts on Aniracetam

    Aniracetam has remained to be one of the most potent and popular racetams throughout the years. It is widely renowned as a brain-boosting drug that sharpens cognitive functions such as mental endurance, attention and focus, memory, and visual perception. Another reason for its widespread use is that it has a comparatively smaller number of side effects and very low toxicity levels, making it tolerable for many users.

    Here is a summary of Aniracetam.

      • Aniracetam was developed in the 1970s as the second in the racetams family, after Piracetam.
  • It has an anosiyl ring with a methoxy group, which makes it distinct from other racetams, and also makes it fat soluble. This feature gives it the ability to be absorbed into most of the body cells including the brain
    • Aniracetam primarily works by activating the cholinergic, dopaminergic, and serotonergic systems. It also upregulates AMPA receptors, increases levels of noradrenaline and improves cerebral blood flow.
    • It is an anxiolytic that inhibits social anxiety and improves verbal fluency.
    • Has an antidepressant effect that boosts mood by increasing serotonin and dopamine levels
    • Improves memory and speeds up the recall process
    • Aniracetam is also said to improve sleep patterns by increasing REM sleep activity and alleviating stress.
    • Helps in brain damage recovery caused by ischemia, cholinergic antagonists, scopolamine, and aging.
    • Effective doses range from 400mg to 1500mg in two to three divided doses.
    • Most frequently reported side effects include headaches, insomnia, nausea and general gastrointestinal distress.
    • It can be stacked with other racetams, choline sources and fish oil supplements to improve absorption, for synergistic effects and to lessen side effects.

     

    Reference Links  

  • https://pubchem.ncbi.nlm.nih.gov/compound/aniracetam#section=Mass-Spectrometry
  • https://www.ncbi.nlm.nih.gov/pubmed/10344525
  • https://www.sciencedirect.com/topics/neuroscience/ampa-receptor
  • https://www.sciencedaily.com/terms/sympathetic_nervous_system.htm
  • https://www.ncbi.nlm.nih.gov/pubmed/11597608
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  • https://examine.com/supplements/aniracetam/
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  • https://www.ncbi.nlm.nih.gov/pubmed/17609677
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  • https://www.ncbi.nlm.nih.gov/pubmed/10869393
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1444064/
  • https://patents.google.com/patent/EP0044088A2/en