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Aniracetam benefits include improving cognitive function and mood, boosting energy levels, treating alcohol addiction, enhancing sleep quality and patterns, reducing stress, and improving sexual health.
Aniracetam is a nootropic compound that belongs to the family of racetam compounds. It’s known as a nootropic compound because it has the ability to enhance a number of cognitive functions including memory, concentration, mental endurance, focus, visual perception, and other thinking skills.
Aniracetam is a type of nootropic drugs which primarily works as a stimulant and brain enhancer. It works on part of the brain neuron called AMPA receptor. AMPA receptors help signals move quickly between neurons. By stimulating these receptors, memory, concentration, and alertness are improved.
An overwhelming body of high-quality studies supports the therapeutic benefits of aniracetam on the brain. According to these studies, aniracetam exerts its brain-boosting effects through the following important mechanisms:
Studies show that aniracetam may help improve overall mood through its potent antidepressant and anti-anxiety effects.
Aniracetam may help boost energy levels through its beneficial effects on energy metabolism:
There is increasing evidence that aniracetam may help fight alcohol addiction:
With its brain-boosting effects, aniracetam may also be beneficial in improving sleep pattern and quality. The following studies support the benefits of aniracetam in various sleeping difficulties:
Chronic stress causes prolonged elevation of the stress hormone known as cortisol. This effect negatively affects the body and can lead to suppressed immunity, high blood pressure, high blood sugar, insulin resistance, obesity, diabetes, metabolic syndrome, reduced libido, bone loss, and other life-threatening conditions. Studies support the ability of aniracetam to fight stress:
Aniracetam has also been shown to exert beneficial effects on sexual health:
Aniracetam side effects are very uncommon. There have been some side effects associated with the use of this nootropic wherein the patient had one of the issues listed below at some point while being on aniracetam. However, the issue wasn’t’ confirmed to be caused by the treatment and could have been a coincidence and not related to the use of aniracetam. Despite this, it was listed as a side effect associated with aniracetam even these associated side effects are very uncommon.
Side effects associated with aniracetam may include the following:
Piracetam is a nootropic drug that was first synthesized in 1964 by Romanian chemist Corneliu E. Giurgea. It belongs to the racetam family of drugs, which are known for their cognitive-enhancing properties. Piracetam is often referred to as the original nootropic and has been extensively studied for its potential benefits in improving memory, learning, and overall cognitive function. Its chemical structure is 2-oxo-1-pyrrolidine acetamide, and it is believed to enhance the functioning of the brain by influencing various neurotransmitter systems, including acetylcholine and glutamate, which are critical for memory and learning processes.
One of the primary mechanisms of action of Piracetam is its ability to modulate the permeability of cell membranes, which can enhance the fluidity of the membranes. This action is thought to improve the function of neurotransmitters and receptors, leading to better synaptic plasticity and communication between neurons. Additionally, Piracetam has been shown to improve microcirculation in the brain by reducing blood viscosity and enhancing oxygen and glucose utilization. These effects collectively contribute to improved cognitive function and neuroprotection, potentially benefiting individuals with conditions like dementia, Alzheimer’s disease, and cognitive impairments due to various neurological disorders.
Piracetam is widely available and used in many countries, both as a prescription medication and as an over-the-counter supplement. It is typically administered in dosages ranging from 1.2 to 4.8 grams per day, depending on the condition being treated and individual response. While it is generally considered safe and well-tolerated, some users may experience side effects such as headaches, insomnia, and gastrointestinal disturbances. Despite its popularity and extensive research, the efficacy of Piracetam remains a topic of debate, and it is not approved by the FDA for medical use in the United States. Nonetheless, it continues to be a subject of interest in the field of cognitive enhancement and neuropharmacology.
Aniracetam is a nootropic compound belonging to the racetam family, known for its cognitive-enhancing properties. It is often sought after for its potential benefits in improving memory, focus, and mood. If you are looking to buy Aniracetam, it’s essential to purchase from reputable sources to ensure the quality and purity of the product. Aniracetam can be found through various online retailers, specialty health stores, and nootropic vendors. When purchasing online, it’s crucial to research the vendor, check for third-party testing certificates, and read customer reviews to verify the legitimacy of the product.
Several well-known online vendors specialize in nootropic supplements, including Aniracetam. Websites like Pure Nootropics, Nootropics Depot, and Science.bio are popular choices for purchasing high-quality Aniracetam. These vendors typically provide detailed product information, including purity testing results and customer feedback. Additionally, some of these sites offer various forms of Aniracetam, such as powders, capsules, and tablets, allowing consumers to choose the format that best suits their needs. It’s important to note that prices may vary based on the quantity and form of Aniracetam, so comparing options can help you find the best deal.
Before purchasing Aniracetam, it is advisable to consult with a healthcare professional, especially if you have any underlying health conditions or are taking other medications. This ensures that Aniracetam is safe for you to use and helps to determine the appropriate dosage. Additionally, keep in mind that the legal status of Aniracetam can vary by country. While it is available as a supplements in many places, it may require a prescription or be restricted in others. Always check local regulations before making a purchase to ensure compliance with local laws.
Aniracetam is a popular nootropic supplement that belongs to the racetam family, known for its cognitive-enhancing properties. Developed in the 1970s, Aniracetam is often used to improve memory, focus, and overall mental clarity. It is fat-soluble, which means it is best absorbed when taken with dietary fats. This supplement is thought to work by modulating the activity of neurotransmitters in the brain, particularly acetylcholine and glutamate, which are critical for learning, memory, and mood regulation.
Many users of Aniracetam report enhanced cognitive function, including improved recall and faster information processing. Additionally, Aniracetam is believed to have anxiolytic (anxiety-reducing) effects, making it a popular choice for individuals seeking to manage stress and anxiety alongside cognitive benefits. Some studies suggest that Aniracetam may also enhance creativity and verbal fluency, which can be particularly beneficial for tasks requiring creative problem-solving and effective communication. It’s important to note, however, that individual responses to Aniracetam can vary, and more research is needed to fully understand its effects and optimal usage.
When considering Aniracetam supplementation, it is crucial to purchase from reputable sources to ensure product quality and purity. It is typically available in powder or capsule form, and users should follow recommended dosages to avoid potential side effects, which can include headaches, nausea, and digestive discomfort. These side effects are often mitigated by starting with a lower dose and gradually increasing it as tolerated. Consulting with a healthcare professional before starting Aniracetam is advisable, especially for individuals with underlying health conditions or those taking other medications. Additionally, combining Aniracetam with a choline supplement, such as Alpha-GPC or Citicoline, can enhance its effectiveness and help prevent headaches associated with racetam use.
Aniracetam and Modafinil are both popular cognitive enhancers, but they differ significantly in their mechanisms of action, benefits, and potential uses. Aniracetam is a racetam nootropic known for its ability to enhance memory, learning, and mood. It modulates neurotransmitters like acetylcholine and glutamate, which play key roles in cognitive function and mood regulation. Users of Aniracetam often report improved focus, creativity, and a reduction in anxiety, making it a favored choice for individuals seeking mild cognitive enhancement and mood stabilization.
Modafinil, on the other hand, is a wakefulness-promoting agent often used to treat conditions like narcolepsy, sleep apnea, and shift work sleep disorder. It operates by influencing various neurotransmitters, including dopamine, norepinephrine, and histamine, to promote alertness and reduce fatigue. Unlike Aniracetam, Modafinil is not classified as a nootropic but is highly regarded for its potent effects on wakefulness and cognitive performance. Users typically experience increased alertness, enhanced executive function, and prolonged periods of concentration, making it popular among individuals who need to stay awake and focused for extended periods.
When comparing Aniracetam and Modafinil, it’s important to consider their differing applications and side effect profiles. Aniracetam is generally well-tolerated with mild side effects such as headaches and nausea, often mitigated by proper dosage and choline supplementation. Its effects are subtler and more suited to enhancing daily cognitive function and mood. Modafinil, however, can have more pronounced side effects, including insomnia, anxiety, and increased heart rate, and should be used under medical supervision. It is better suited for individuals with specific needs for increased wakefulness and cognitive endurance. Ultimately, the choice between Aniracetam and Modafinil will depend on individual goals, lifestyle, and health considerations.
Aniracetam is a nootropic compound known for its cognitive-enhancing effects, including improved memory, learning, and mood stabilization. Determining the optimal dosage for Aniracetam can vary based on individual factors such as body weight, sensitivity to the substance, and specific cognitive goals. Generally, recommended dosages range from 750 mg to 1500 mg per day, divided into two or three smaller doses to maintain steady levels in the bloodstream. Taking Aniracetam with food, especially fats, can enhance its absorption since it is fat-soluble.
For those new to Aniracetam, starting with a lower dose of around 750 mg per day is advisable to assess tolerance and response. Gradually increasing the dosage to a higher amount within the recommended range can help find the most effective dose with minimal side effects. Some users report experiencing mild side effects such as headaches, which are often alleviated by supplementing with a choline source like Alpha-GPC or Citicoline. This combination can support the increased demand for acetylcholine in the brain, enhancing Aniracetam’s efficacy while reducing potential adverse effects.
It’s important to note that individual responses to Aniracetam can vary, and what works for one person may not work for another. Monitoring one’s reaction to the supplement and adjusting the dosage accordingly is crucial for achieving the desired cognitive benefits without unwanted side effects. Consulting with a healthcare professional before starting Aniracetam, especially for individuals with pre-existing medical conditions or those taking other medications, is recommended to ensure safety and efficacy. Regular breaks or cycling the usage of Aniracetam can also help maintain its effectiveness over the long term, preventing tolerance buildup.
Aniracetam capsules are a popular form of this nootropic supplement, known for their convenience and ease of use. Each capsule typically contains a precise dosage of Aniracetam, usually ranging from 500 mg to 750 mg. This standardized dosage helps users to monitor and adjust their intake accurately without the need for measuring powders. Capsules are especially beneficial for those who are new to nootropics or prefer a straightforward, hassle-free method of consumption. Additionally, the encapsulation can help mask the bitter taste of Aniracetam, making it more palatable for users.
The effectiveness of Aniracetam capsules largely depends on their absorption and bioavailability. Since Aniracetam is fat-soluble, taking the capsules with a meal containing healthy fats can enhance its absorption and overall efficacy. Users often pair Aniracetam with dietary fats such as fish oil, avocado, or nuts to optimize its cognitive benefits. Consistent use of Aniracetam capsules can lead to improvements in various cognitive functions, including memory, focus, and mood stabilization. However, the results can vary from person to person, and some may experience more pronounced benefits than others.
When considering Aniracetam capsules, it’s important to choose products from reputable manufacturers to ensure quality and purity. Third-party testing and transparent labeling are indicators of a reliable supplement brand. As with any nootropic, potential users should start with a lower dose to assess tolerance and gradually increase to the desired dosage. It’s also advisable to incorporate a choline source, like Alpha-GPC or Citicoline, to mitigate potential side effects such as headaches. Consulting with a healthcare professional before starting Aniracetam capsules, particularly for those with underlying health conditions or who are taking other medications, can ensure safe and effective use. Regular monitoring and cycling of the supplement can help maintain its benefits and prevent tolerance.
Aniracetam enhances cognitive function, mood, and behavior, and may offer protective effects against cognitive deficits caused by aging and prenatal ethanol exposure. However, it is essential to consult a qualified professional before beginning any new supplement regimen. A qualified professional can provide personalized advice based on individual health needs and potential interactions with other medications or supplements. Discussing aniracetam use with a qualified professional ensures a thorough understanding of the benefits and risks, as well as the proper dosage and administration. Always seek guidance from a qualified professional to make informed decisions about cognitive enhancement supplements like aniracetam.
Yes, aniracetam is believed to increase dopamine levels by modulating neurotransmitter systems in the brain. As a part of the racetam family of chemical compounds, aniracetam interacts with several neurotransmitter systems, which can enhance cognitive function and mood. These chemical compounds are known for their potential to boost memory and learning, making them a popular choice for cognitive enhancement. Moreover, aniracetam’s ability to influence neurotransmitter systems is a key characteristic shared by many nootropic chemical compounds, further highlighting its role in improving brain function.
Aniracetam is a nootropic compound, specifically classified as a racetam. Research and experiment on aniracetam have shown its potential cognitive-enhancing effects, including improvements in memory, learning, and focus.
Piracetam is used to enhance cognitive function and treat cognitive impairments, particularly in conditions such as dementia and Alzheimer’s disease. Studies have shown that piracetam can increase quantity of certain neurotransmitters in the brain, which may contribute to its cognitive-enhancing effects. Additionally, piracetam has been observed to increase quantity of blood flow to the brain, improving oxygen and nutrient delivery, which is essential for maintaining cognitive function. By supporting these mechanisms, piracetam helps increase quantity of neural activity, potentially improving memory, attention, and overall cognitive performance.
Piracetam is believed to enhance cognitive function, improve memory, and increase focus, although its effectiveness varies among individuals and lacks strong scientific consensus. Despite this, piracetam remains popular for research use due to its potential nootropic benefits. Researchers continue to investigate its mechanisms and effects to better understand its capabilities. In addition, piracetam is often used in studies to explore cognitive enhancement and neuroprotection, further highlighting its significance in research use.
The nootropic effect of piracetam is its potential to enhance cognitive functions such as memory, learning, and mental clarity. Unlike stimulants like Ritalin, piracetam works through different mechanisms, primarily by modulating neurotransmitter systems in the brain to improve cognitive performance. While Ritalin is often prescribed for ADHD to increase focus and attention by stimulating the central nervous system, piracetam offers a more subtle approach to cognitive enhancement without the stimulating effects associated with Ritalin. This difference in mechanisms makes piracetam a preferred choice for individuals seeking cognitive benefits without the potential side effects of stimulants like Ritalin.
Aniracetam is classified as a nootropic drug.
Aniracetam may help improve focus and cognitive function in individuals with ADHD, though more research is needed to confirm its effectiveness. As it is often included in nootropic supplements, aniracetam is frequently combined with other cognitive-enhancing supplements to maximize its potential benefits. However, it’s important for individuals to consult with a healthcare professional before using aniracetam, especially when taking other supplements, to ensure safety and avoid potential interactions.
Aniracetam is primarily used to treat cognitive impairments and disorders such as Alzheimer’s disease and other forms of dementia.
Aniracetam is good for enhancing cognitive functions, improving memory, and treating cognitive impairments such as Alzheimer’s disease and other forms of dementia.
Aniracetam is believed to increase serotonin levels, potentially enhancing mood and reducing anxiety. A comprehensive review of the literature suggests that aniracetam’s impact on serotonin and other neurotransmitters contributes to its mood-boosting and anxiolytic effects. Additionally, another review focusing on the pharmacological properties of aniracetam supports its role in cognitive enhancement and emotional regulation. These reviews highlight the potential benefits of aniracetam, though further research is needed to fully understand its mechanisms and long-term effects.
Aniracetam is reported to enhance cognitive function and improve focus, which some users may perceive as increased energy. By modulating neurotransmitter systems in the brain, aniracetam can help boost mental clarity and cognitive performance. However, it’s important to note that individual responses to aniracetam can vary, and the perceived increase in energy might differ based on the quantity taken. Additionally, users should be mindful of the quantity they consume to avoid any potential side effects and to find the optimal dose for their needs. Always consult with a healthcare professional to determine the appropriate quantity and ensure safe use of aniracetam.
Aniracetam is believed to support cognitive function and neuroprotection, potentially aiding in brain health and recovery. Research indicates that aniracetam improves memory and overall cognitive performance, making it a popular choice for individuals seeking to enhance their mental capabilities. Studies also suggest that aniracetam improves memory retention and recall, further highlighting its potential benefits for cognitive health. By promoting neuroprotection, aniracetam may help in the recovery of brain function and resilience against cognitive decline.
Ouchi Y, Kakiuchi T, Okada H, Nishiyama S, Tsukada H. The effect of aniracetam on cerebral glucose metabolism in rats after lesioning of the basal forebrain measured by PET. Journal of the neurological sciences. 1999; 164(1):7-12.
The effect of aniracetam on cerebral glucose metabolism in rats after lesioning of the basal forebrain measured by PET
In order to assess the impact of aniracetam, a potent modulator of the glutamatergic and cholinergic systems, on altered cerebral glucose metabolism following basal forebrain lesions, we utilized positron emission tomography to measure cerebral metabolic rate of glucose (CMRGlc) and assessed choline acetyltransferase (ChAT) activity in the frontal cortex of lesioned rats treated with aniracetam. Continuous aniracetam administration for 7 days post-surgery prevented CMRGlc reduction in the frontal cortex on the side of the lesion, whereas lesioned rats without aniracetam exhibited significant CMRGlc reduction in the frontal cortex. However, aniracetam did not alter the reduction in frontal ChAT activity. These findings suggest that aniracetam prevents glucose metabolic reduction in the cholinergically denervated frontal cortex with minimal impact on the cortical cholinergic system, indicating the involvement of other neurotransmitter systems, such as the glutamatergic system, in cortical metabolic recovery post-basal forebrain lesions.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2966848/.
Zhao X, Kuryatov A, Lindstrom JM, Yeh JZ, Narahashi T. Nootropic drug modulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons. Molecular pharmacology. 2001; 59(4):674-83.
Nootropic drug modulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons
Nefiracetam (DM-9384), a novel pyrrolidone nootropic drug, is under development for treating Alzheimer’s and poststroke vascular-type dementia. To understand its mechanism of action on neuronal nicotinic acetylcholine receptors (nnAChRs), this study recorded currents from rat cortical neurons in primary culture. It revealed that nefiracetam and aniracetam, both nootropic agents, potently enhanced alpha 4 beta 2-type currents induced by acetylcholine. Nefiracetam also increased responses to high ACh concentrations. Interestingly, nefiracetam’s action was unaffected by protein kinase inhibitors but was abolished by cholera toxin, indicating G(s) proteins’ involvement in its potentiation of nnAChRs. These findings suggest that nnAChRs are a key target for nefiracetam, with G(s) proteins likely playing a crucial role in its mechanism of action.
You can read the full article at https://pubmed.ncbi.nlm.nih.gov/11259610/.
K. Nakamura, M. Shirane, Activation of the reticulothalamic cholinergic pathway by the major metabolites of aniracetam, Eur. J. systems participating in nicotine-specific effects, Neurochem. Int. 33Pharmacol. 380 (1999) 81–89.
Activation of the reticulothalamic cholinergic pathway by the major metabolites of aniracetam
The study aimed to further explore the impact of aniracetam, a cognitive enhancer, and its metabolites on the brain’s cholinergic system. Using in vivo brain microdialysis in stroke-prone spontaneously hypertensive rats (SHRSP), choline acetyltransferase activity and acetylcholine release were measured. SHRSP exhibited central cholinergic deficits compared to age-matched Wistar Kyoto rats. Repeated aniracetam treatment preferentially increased enzyme activity in the thalamus but decreased it in the striatum. Among aniracetam’s metabolites, local perfusion of N-anisoyl-gamma-aminobutyric acid (GABA) and p-anisic acid into various brain regions of SHRSP resulted in a delayed increase in acetylcholine release. Aniracetam itself had no such effect. Direct injection of N-anisoyl-GABA into the pedunculopontine tegmental nucleus enhanced release in the nucleus reticularis thalami, indicating that aniracetam can enhance central cholinergic neurotransmission through both metabolites. N-anisoyl-GABA, based on its pharmacokinetic profile, may contribute to aniracetam’s clinical effects, primarily by acting on the reticulothalamic cholinergic pathway.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0014299999005348?via%3Dihub.
M.G. Giovannini, P. Rodino, D. Mutolo, G. Pepeu, Oxiracetam and aniracetam increase acetylcholine release from the rat hippocampus in vivo, Drug Dev. Res. 28 (1993) 503–509.
Oxiracetam and aniracetam increase acetylcholine release from the rat hippocampus
The study aimed to investigate the impact of two nootropic drugs, oxiracetam and aniracetam, on cholinergic neurotransmission in rats using transversal microdialysis. Basal acetylcholine (ACh) release from the hippocampus and parietal cortex was stable, while choline efflux decreased by about 50% during the initial 60 minutes of collection. Oxiracetam, administered at doses of 50, 100, and 300 mg/kg intraperitoneally, increased hippocampal ACh release by 63% at 100 mg/kg, a effect inhibited by tetrodotoxin (TTX). Oxiracetam also attenuated the decrease in choline efflux compared to controls at 100 mg/kg. Aniracetam (100 mg/kg orally) sustainedly increased hippocampal ACh release (+58%, 120 minutes after administration) without affecting choline efflux. Neither drug, at 50 or 100 mg/kg doses, altered ACh or choline output from the parietal cortex or induced significant behavioral changes. These findings suggest that oxiracetam and aniracetam may enhance cognitive processes by stimulating hippocampal cholinergic pathways.
You can read the abstract of the article at https://www.researchgate.net/publication/229522182_Oxiracetam_and_aniracetam_increase_acetylcholine_release_from_the_rat_hippocampus.
Shirane M, Nakamura K. Aniracetam enhances cortical dopamine and serotonin release via cholinergic and glutamatergic mechanisms in SHRSP. Brain research. 2001; 916(1-2):211-21.
Aniracetam enhances cortical dopamine and serotonin release via cholinergic and glutamatergic mechanisms in SHRSP
Aniracetam, a cognitive enhancer, increases extracellular dopamine (DA) and serotonin (5-HT) levels in specific brain regions of stroke-prone hypertensive rats by primarily mediating the action of its major metabolite, N-anisoyl-GABA. This metabolite enhances DA and 5-HT release in the prefrontal cortex (PFC) by targeting nicotinic acetylcholine (nACh) and NMDA receptors in the ventral tegmental area (VTA) and dorsal raphe nucleus (DRN). The release effects of aniracetam and its metabolites are blocked by mecamylamine, a nACh and NMDA receptor antagonist, indicating that aniracetam’s cognitive benefits are linked to these neurotransmitter systems.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0006899301029390?via%3Dihub.
Petkov VD, Grahovska T, Petkov VV, Konstantinova E, Stancheva S. Changes in the brain biogenic monoamines of rats, induced by piracetam and aniracetam. ActaphysiologicaetpharmacologicaBulgarica. 1984; 10(4):6-15.
Changes in the brain biogenic monoamines of rats, induced by piracetam and aniracetam
A single oral dose of 600 mg/kg piracetam or 50 mg/kg aniracetam significantly alters dopamine (DA) and serotonin (5-HT) levels and turnover in various rat brain regions. Piracetam increases DA in the cerebral cortex and striatum and 5-HT in the cortex while decreasing 5-HT in the striatum, brain stem, and hypothalamus, with varied effects on neurotransmitter turnover across different brain areas. Aniracetam reduces DA in the striatum and hypothalamus, decreases 5-HT in the hypothalamus, and increases 5-HT in the cortex and striatum, also affecting neurotransmitter turnover differently. These changes in cerebral biogenic monoamines contribute to the distinct behavioral effects of piracetam and aniracetam.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/6535371/.
Shirane M, Nakamura K. Aniracetam enhances cortical dopamine and serotonin release via cholinergic and glutamatergic mechanisms in SHRSP. Brain Res. 2001;916(1-2):211-21.
Aniracetam enhances cortical dopamine and serotonin release via cholinergic and glutamatergic mechanisms in SHRSP
Aniracetam, a cognition enhancer, increases dopamine (DA) and serotonin (5-HT) levels in specific brain regions of stroke-prone hypertensive rats. The study identified N-anisoyl-GABA, a major metabolite of aniracetam, as primarily responsible for this effect. Blocking nACh and NMDA receptors with mecamylamine in key brain areas halted the DA and 5-HT release induced by aniracetam. Furthermore, both N-anisoyl-GABA and another metabolite, p-anisic acid, were found to stimulate DA and 5-HT release in the prefrontal cortex, suggesting that aniracetam enhances neurotransmitter release through actions on these receptors.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0006899301029390?via%3Dihub.
Pugliese AM, Corradetti R, Ballerini L, Pepeu G. Effect of the nootropic drug oxiracetam on field potentials of rat hippocampal slices. British journal of pharmacology. 1990; 99(1):189-93.
Effect of the nootropic drug oxiracetam on field potentials of rat hippocampal slices
The nootropic drug oxiracetam enhances hippocampal neurotransmission in the CA1 region of rat hippocampal slices. In vitro studies show that superfusion with oxiracetam (0.1-100 microM) increases the dendritic field excitatory postsynaptic potential (e.p.s.p.) in a concentration-dependent manner, with the most significant effect at 1 microM. This enhancement is persistent and resembles long-term potentiation (LTP), although oxiracetam-induced LTP does not add to electrically-induced LTP. The effect of oxiracetam is sensitive to D-2-Amino-5-phosphonopentanoic acid (AP-5), indicating that its action involves mechanisms similar to those underlying LTP.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917508/.
Lee CR, Benfield P. Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders. Drugs & aging. 1994; 4(3):257-73.
Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders
Aniracetam, a nootropic drug, is believed to enhance cognition by modulating metabotropic glutamate receptors, AMPA-sensitive glutamate receptors, and facilitating cholinergic transmission. Trials indicate its potential benefits for elderly patients with mild to moderate cognitive impairment due to Alzheimer’s disease, showing significant improvement over placebo and piracetam in various cognitive tests. Additionally, preliminary evidence suggests benefits for cognitive impairment of cerebrovascular origin, with aniracetam being well-tolerated and not associated with increased liver enzyme levels, warranting further research to confirm its efficacy and safety profile.
You can read the full article at https://link.springer.com/article/10.2165/00002512-199404030-00007.
Koliaki CC, Messini C, Tsolaki M. Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study. CNS neuroscience & therapeutics. 2012; 18(4):302-12.
Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study
In a study involving 276 patients with dementia, aniracetam, both as monotherapy and combined with cholinesterase inhibitors (ChEIs), was evaluated for its neuropsychological benefits. Results showed that aniracetam maintained cognitive and emotional parameters for 12 months and improved emotional state at 3 months, while patients on ChEIs experienced significant cognitive deterioration at 12 months. Aniracetam showed better cognitive performance and functionality in patients with mild dementia compared to ChEIs, suggesting its potential as a beneficial treatment option with neuroprotective and mood-enhancing effects.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6493642/
Isaacson JS, Nicoll RA. Aniracetam reduces glutamate receptor desensitization and slows the decay of fast excitatory synaptic currents in the hippocampus. Proceedings of the National Academy of Sciences of the United States of America. 1991; 88(23):10936-40.
Aniracetam reduces glutamate receptor desensitization and slows the decay of fast excitatory synaptic currents in the hippocampus
Aniracetam, a nootropic drug, has been shown to enhance quisqualate receptor-mediated responses and glutamate-evoked currents in brain cells, particularly in hippocampal pyramidal cells. Using patch clamp recording techniques, researchers found that aniracetam reduces glutamate receptor desensitization, prolongs the time course, and increases the peak amplitude of fast synaptic currents. These effects suggest that aniracetam slows the kinetics of fast synaptic transmission, supporting the idea that receptor desensitization regulates the strength of excitatory synaptic transmission in the brain.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC53047/.
Francotte P, de Tullio P, Fraikin P, Counerotte S, Goffin E, Pirotte B. In search of novel AMPA potentiators. Recent patents on CNS drug discovery. 2006; 1(3):239-46.
In search of novel AMPA potentiators
Glutamate, the brain’s major excitatory neurotransmitter, acts through AMPA receptors essential for fast excitatory neurotransmission and long-term potentiation. Given glutamate’s role in various neurological and psychiatric disorders, enhancing AMPA receptor signals is being explored for treating conditions like Alzheimer’s, schizophrenia, and mood disorders. Current research focuses on developing AMPA positive allosteric modulators, or potentiators, to alter receptor desensitization. Key chemical families in this effort include aniracetam derivatives, cyclothiazide derivatives, and biarylpropylsulfonamides.
You can read the abstract at https://pubmed.ncbi.nlm.nih.gov/18221205/.
Tang CM, Shi QY, Katchman A, Lynch G. Modulation of the time course of fast EPSCs and glutamate channel kinetics by aniracetam. Science (New York, N.Y.). 1991; 254(5029):288-90.
Modulation of the time course of fast EPSCs and glutamate channel kinetics by aniracetam
Glutamate is the primary neurotransmitter at most excitatory synapses in the mammalian CNS, triggering both fast and slow excitatory postsynaptic currents (EPSCs). The fast EPSC is mediated by non-NMDA receptor channels, while the slow EPSC is mediated by NMDA receptor channels. Aniracetam, a nootropic agent, selectively and reversibly slows the desensitization kinetics of non-NMDA channels, extending their open times and modulating the fast EPSC kinetics similarly. These findings suggest that the properties of non-NMDA glutamate channels primarily determine the fast EPSC kinetics rather than the rate of neurotransmitter clearance.
You can read the abstract of the article at https://www.science.org/doi/10.1126/science.254.5029.288?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed.
Pittaluga A, Bonfanti A, Arvigo D, Raiteri M. Aniracetam, 1-BCP and cyclothiazide differentially modulate the function of NMDA and AMPA receptors mediating enhancement of noradrenaline release in rat hippocampal slices. Naunyn-Schmiedeberg’s archives of pharmacology. 1999; 359(4):272-9.
Aniracetam, 1-BCP and cyclothiazide differentially modulate the function of NMDA and AMPA receptors mediating enhancement of noradrenaline release in rat hippocampal slices
Aniracetam, 1-(1,3-benzodioxol-5-yl-carbonyl)piperidine (1-BCP), and cyclothiazide are cognition-enhancing compounds that modulate AMPA receptors. In the ‘kynurenate test,’ aniracetam demonstrated high potency in attenuating the kynurenate antagonism of NMDA-evoked [3H]noradrenaline release from rat hippocampal slices, with an EC50 of ≤0.1 µM. Cyclothiazide and 1-BCP were significantly less potent. Aniracetam’s effect persisted despite the presence of an AMPA receptor antagonist, unlike the effects of cyclothiazide and 1-BCP. Additionally, aniracetam showed a dual modulation of glutamatergic transmission, affecting NMDA receptor function at low concentrations and AMPA receptors at higher concentrations. Cyclothiazide and 1-BCP mainly acted through AMPA receptors, with a potential NMDA component in 1-BCP’s action.
You can read the abstract of the article at https://link.springer.com/article/10.1007/PL00005352.
Ling DS, Benardo LS. Nootropic agents enhance the recruitment of fast GABAA inhibition in rat neocortex. Cerebral cortex (New York, N.Y. : 1991). 2005; 15(7):921-8.
Nootropic agents enhance the recruitment of fast GABAA inhibition in rat neocortex
It is widely believed that nootropic (cognition-enhancing) agents produce their therapeutic effects by augmenting excitatory synaptic transmission in cortical circuits, primarily through positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate receptors (AMPARs). However, GABA-mediated inhibition is also critical for cognition, and enhanced GABA function may be likewise therapeutic for cognitive disorders. Could nootropics act through such a mechanism as well? To address this question, we examined the effects of nootropic agents on excitatory and inhibitory postsynaptic currents (EPSCs and IPSCs) recorded from layer V pyramidal cells in acute slices of somatosensory cortex. Aniracetam, a positive modulator of AMPA/kainate receptors, increased the peak amplitude of evoked EPSCs and the amplitude and duration of polysynaptic fast IPSCs, manifested as a greater total charge carried by IPSCs. As a result, the EPSC/IPSC ratio of total charge was decreased, representing a shift in the excitation-inhibition balance that favors inhibition. Aniracetam did not affect the magnitude of either monosynaptic IPSCs (mono-IPSCs) recorded in the presence of excitatory amino acid receptor antagonists, or miniature IPSCs (mIPSCs) recorded in the presence of tetrodotoxin. However, the duration of both mono-IPSCs and mIPSCs was prolonged, suggesting that aniracetam also directly modulates GABAergic transmission. Cyclothiazide, a preferential modulator of AMPAR function, enhanced the magnitude and duration of polysynaptic IPSCs, similar to aniracetam, but did not affect mono-IPSCs. Concanavalin A, a kainate receptor modulator, had little effect on EPSCs or IPSCs, suggesting there was no contribution from kainate receptor activity. These findings indicate that AMPAR modulators strengthen inhibition in neocortical pyramidal cells, most likely by altering the kinetics of AMPARs on synaptically connected interneurons and possibly by modulating GABA(A) receptor responses in pyramidal cells. This suggests that the therapeutic actions of nootropic agents may be partly mediated through enhanced cortical GABAergic inhibition, and not solely through the direct modification of excitation, as previously thought.
You can read the full article at https://academic.oup.com/cercor/article/15/7/921/387971?login=false.
O’Neill MJ, Bleakman D, Zimmerman DM, Nisenbaum ES. AMPA receptor potentiators for the treatment of CNS disorders. Current drug targets. CNS and neurological disorders. 2004; 3(3):181-94.
AMPA receptor potentiators for the treatment of CNS disorders. Current drug targets
AMPA receptors mediate most excitatory neurotransmission in the mammalian CNS and play a role in synaptic plasticity, memory, learning, and neural network formation. Comprised of four subunits (Glu(A1)-Glu(A4)), AMPA receptors can form homomeric or heteromeric tetramers, with further complexity added by alternative splicing variants. Positive modulation of these receptors, through compounds like aniracetam, cyclothiazide, and biarylpropylsulfonamides, has shown promise in enhancing cognitive function in rodents and humans, including those with neurological and psychiatric disorders. These modulators also increase BDNF expression via calcium-dependent and independent pathways, potentially contributing to their antidepressant and neuroprotective effects. Consequently, AMPA receptor potentiators are being explored for treating cognitive impairments in Alzheimer’s disease, schizophrenia, depression, and Parkinson’s disease.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/15180479/.
O’Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson’s disease. Current drug targets. 2007; 8(5):603-20.
AMPA receptor potentiators: application for depression and Parkinson’s disease
AMPA receptors mediate most excitatory neurotransmission in the mammalian CNS and play a role in synaptic plasticity, memory, learning, and neural network formation. Comprised of four subunits (Glu(A1)-Glu(A4)), AMPA receptors can form homomeric or heteromeric tetramers, with further complexity added by alternative splicing variants. Positive modulation of these receptors, through compounds like aniracetam, cyclothiazide, and biarylpropylsulfonamides, has shown promise in enhancing cognitive function in rodents and humans, including those with neurological and psychiatric disorders. These modulators also increase BDNF expression via calcium-dependent and independent pathways, potentially contributing to their antidepressant and neuroprotective effects. Consequently, AMPA receptor potentiators are being explored for treating cognitive impairments in Alzheimer’s disease, schizophrenia, depression, and Parkinson’s disease.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/15180479/#:~:text=Therefore%2C%20these%20AMPA%20receptor%20potentiators,enhancing%20recovery%20from%20Parkinson’s%20disease.
Vaglenova J, Pandiella N, Wijayawardhane N. Aniracetam reversed learning and memory deficits following prenatal ethanol exposure by modulating functions of synaptic AMPA receptors. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2008; 33(5):1071-83.
Aniracetam reversed learning and memory deficits following prenatal ethanol exposure by modulating functions of synaptic AMPA receptors
Specific pharmacological treatments for Fetal Alcohol Spectrum Disorders (FASD) are currently unavailable. This study investigated the therapeutic potential of aniracetam in a Sprague-Dawley rat model of FASD. Ethanol exposure during pregnancy caused severe cognitive deficits and behavioral abnormalities in offspring, including poor novelty-seeking behavior and high anxiety levels. These cognitive impairments were linked to a reduction in AMPA receptor-mediated synaptic responses in the hippocampus. Administering aniracetam (50 mg/kg) for 10 days post-natally significantly reversed cognitive deficits and increased AMPA receptor-mediated synaptic responses. The treatment also demonstrated anxiolytic effects, highlighting aniracetam’s potential in treating cognitive deficits associated with FASD.
You can read the full article at https://www.nature.com/articles/1301496.
Cumin R, Bandle EF, Gamzu E, Haefely WE. Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents. Psychopharmacology. 1982; 78(2):104-11.
Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents
The effect of aniracetam (Ro 13-5057, 1-anisoyl-2-pyrrolidinone) was studied on various forms of experimentally impaired cognitive functions (learning and memory) in rodents and produced the following effects: (1) almost complete prevention of the incapacity to learn a discrete escape response in rats exposed to sublethal hypercapnia immediately before the acquisition session; (2) partial (rats) or complete (mice) prevention of the scopolamine-induced short-term amnesia for a passive avoidance task; (3) complete protection against amnesia for a passive avoidance task in rats submitted to electroconvulsive shock immediately after avoidance acquisition; (4) prevention of the long-term retention- or retrieval-deficit for a passive avoidance task induced in rats and mice by chloramphenicol or cycloheximide administered immediately after acquisition; (5) reversal, when administered as late as 1 h before the retention test, of the deficit in retention or retrieval of a passive avoidance task induced by cycloheximide injected 2 days previously; (6) prevention of the deficit in the retrieval of an active avoidance task induced in mice by subconvulsant electroshock or hypercapnia applied immediately before retrieval testing (24 h after acquisition). These improvements or normalizations of impaired cognitive functions were seen at oral aniracetam doses of 10-100 mg/kg. Generally, the dose-response curves were bell-shaped. The mechanisms underlying the activity of aniracetam and its ‘therapeutic window’ are unknown. Piracetam, another pyrrolidinone derivative was used for comparison. It was active only in six of nine tests and had about one-tenth the potency of aniracetam. The results indicate that aniracetam improves cognitive functions which are impaired by different procedure and in different phases of the learning and memory process.
You can read the abstract of the article at https://link.springer.com/article/10.1007/BF00432244.
Lauterborn JC, Lynch G, Vanderklish P, Arai A, Gall CM. Positive modulation of AMPA receptors increases neurotrophin expression by hippocampal and cortical neurons. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2000; 20(1):8-21.
Positive modulation of AMPA receptors increases neurotrophin expression by hippocampal and cortical neurons
This study examined whether positive modulators of AMPA-type glutamate receptors affect neurotrophin expression in forebrain neurons. Treatments with the ampakine CX614 significantly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal slices, with effects being dose-dependent and reversible. Similar results were observed with another ampakine, CX546. The upregulation was largely blocked by AMPA receptor antagonists and reduced transmitter release. L-type voltage-sensitive calcium channel antagonism blocked induction in the entorhinal cortex but not in the hippocampus. Prolonged CX614 exposure caused BDNF mRNA levels to peak at 12 hours and return to baseline by 48 hours, while BDNF protein levels remained elevated throughout. Additionally, CX546 increased hippocampal BDNF mRNA in aged rats and middle-aged mice, suggesting that positive AMPA modulators could be used to regulate neurotrophin levels in the aged brain.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6774091/.
Lee CR, Benfield P. Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders. Drugs Aging. 1994 Mar;4(3):257-73. doi: 10.2165/00002512-199404030-00007. PMID: 8199398.
Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders
Aniracetam, a nootropic drug, is thought to enhance cognition by positively modulating metabotropic and AMPA-sensitive glutamate receptors, and possibly facilitating cholinergic transmission. Clinical trials in elderly patients with mild to moderate Alzheimer’s-type senile dementia indicate potential cognitive benefits, though further studies are needed to confirm efficacy and identify responsive patient subgroups. Aniracetam at 1500 mg/day outperformed placebo in tests over 4-6 months and was more effective than piracetam in certain tests over another 6-month period. Preliminary evidence also suggests benefits for cognitive impairment of cerebrovascular origin. Aniracetam appears well tolerated without significant adverse effects, including liver enzyme increases, supporting its potential as a therapeutic option for cognitive disorders.
You can read the full article at https://link.springer.com/article/10.2165/00002512-199404030-00007.
Koliaki CC, Messini C, Tsolaki M. Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study. CNS Neurosci Ther. 2012 Apr;18(4):302-12. doi: 10.1111/j.1755-5949.2010.00244.x. Epub 2011 Feb 26. PMID: 22070796; PMCID: PMC6493642.
Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study
This study evaluated the efficacy of aniracetam, alone or combined with cholinesterase inhibitors (ChEIs), in 276 dementia patients over 12 months. Patients treated with aniracetam maintained cognitive functions and showed improved emotional states, while those on ChEIs alone experienced significant cognitive decline. Aniracetam outperformed ChEIs in patients with mild dementia and demonstrated better cognitive and functional outcomes compared to combined treatments. These findings suggest that aniracetam, with its neuroprotective properties, is a promising option for managing mild cognitive deficits and enhancing emotional stability in dementia patients.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6493642/.
Baranova AI, Whiting MD, Hamm RJ. Delayed, post-injury treatment with aniracetam improves cognitive performance after traumatic brain injury in rats. J Neurotrauma. 2006 Aug;23(8):1233-40. doi: 10.1089/neu.2006.23.1233. PMID: 16928181.
Delayed, post-injury treatment with aniracetam improves cognitive performance after traumatic brain injury in rats
This study investigated the effectiveness of aniracetam in treating cognitive impairment after traumatic brain injury (TBI) in rats. It examined optimal dosing, the impact of delayed treatment, and the effects of terminating treatment before assessment. Results showed that both 25 and 50 mg/kg doses of aniracetam improved cognitive performance in the Morris water maze when administered immediately after injury for 15 days. Delayed treatment starting 11 days post-injury was also effective, while terminating treatment before cognitive testing negated the benefits. Thus, aniracetam can improve cognitive recovery following TBI, even with delayed administration.
You can read the abstract of the article at https://www.liebertpub.com/doi/10.1089/neu.2006.23.1233?url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&rfr_dat=cr_pub++0pubmed.
Cumin R, Bandle EF, Gamzu E, Haefely WE. Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents. Psychopharmacology (Berl). 1982;78(2):104-11. doi: 10.1007/BF00432244. PMID: 6817363.
Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents
Aniracetam significantly improved various forms of experimentally induced cognitive impairments in rodents. It nearly prevented learning incapacity caused by sublethal hypercapnia, partially or fully mitigated scopolamine-induced short-term amnesia, and protected against amnesia from electroconvulsive shock. It also prevented long-term retention deficits induced by chloramphenicol or cycloheximide, and reversed retention deficits when administered before testing. Additionally, it prevented retrieval deficits induced by electroshock or hypercapnia. Aniracetam’s effects were dose-dependent and more potent than piracetam, suggesting it effectively enhances cognitive functions impaired by diverse methods and in different phases of learning and memory processes.
You can read the full article at https://link.springer.com/article/10.1007/BF00432244.
Senin, U., Parnetti, L., Cucinotta, D. et al. Clinical Experience with Aniracetam in the Treatment of Senile Dementia of the Alzheimer’s Type and Related Disorders. Drug Invest 5, 96–105 (1993). https://doi.org/10.1007/BF03258430
Clinical Experience with Aniracetam in the Treatment of Senile Dementia of the Alzheimer’s Type and Related Disorders
Aniracetam has been shown to be effective and well-tolerated in elderly patients with senile dementia of the Alzheimer’s type (SDAT) and senile cognitive decline. In two double-blind multicentre clinical trials, aniracetam (1500 mg/day) improved cognitive functions over six months compared to placebo and was more effective than piracetam (2400 mg/day). Aniracetam-treated patients showed significant cognitive improvement, while placebo-treated patients experienced a decline. The drug was well tolerated, with only mild and transient adverse events. These findings suggest that aniracetam is a promising treatment for cognitive decline in elderly patients, though further long-term studies are needed.
You can read the abstract of the article at https://link.springer.com/article/10.1007/BF03258430.
Li Y, Wang JJ, Cai JX. Aniracetam restores the effects of amyloid-beta protein or ageing on membrane fluidity and intracellular calcium concentration in mice synaptosomes. J Neural Transm (Vienna). 2007;114(11):1407-11. doi: 10.1007/s00702-007-0760-2. Epub 2007 Jun 8. PMID: 17557127.
Aniracetam restores the effects of amyloid-beta protein or ageing on membrane fluidity and intracellular calcium concentration in mice synaptosomes
In this study, aniracetam was found to restore membrane fluidity and reduce free calcium concentrations ([Ca(2+)]i) in synaptosomes from the frontal cortex (FC) and hippocampus (HP) of aged mice and young mice treated with amyloid-beta protein (Abeta). Membrane fluidity, decreased by aging and Abeta25-35, was improved by aniracetam in a concentration-dependent manner. Additionally, aniracetam effectively reversed the Abeta25-35-induced increase in [Ca(2+)]i in HP synaptosomes. These findings suggest that aniracetam may have a beneficial role in treating age-related cognitive decline and Alzheimer’s disease by restoring membrane properties and calcium homeostasis.
You can read the abstract of the article at https://link.springer.com/article/10.1007/s00702-007-0760-2.
Nakamura K, Kurasawa M. Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. European journal of pharmacology. 2001; 420(1):33-43.
Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism
This study investigated the anxiolytic effects of aniracetam in various anxiety models using mice. Aniracetam (10-100 mg/kg) increased social interaction scores, mainly due to increased trunk sniffing and following, and its effects were blocked by haloperidol, mecamylamine, or ketanserin, indicating involvement of nicotinic acetylcholine, 5-HT2A, and dopamine D2 receptors. Aniracetam also demonstrated anti-anxiety effects in the elevated plus-maze and conditioned fear stress tests, with different metabolites mimicking these effects in specific models. These findings suggest that aniracetam has broad anxiolytic properties through interactions with cholinergic, dopaminergic, and serotonergic systems, highlighting its potential use for anxiety-related disorders and social impairments.
Nakamura K, Tanaka Y. Antidepressant-like effects of aniracetam in aged rats and its mode of action. Psychopharmacology. 2001; 158(2):205-12.
Antidepressant-like effects of aniracetam in aged rats and its mode of action
This study aimed to test the antidepressant-like effects of aniracetam in rats and explore its mechanisms of action. In a forced swim test, aniracetam (10-100 mg/kg) did not reduce immobility time in young rats but significantly decreased it in aged rats, effects mimicked by its metabolites, 2-pyrrolidinone and N-anisoyl-GABA. The antidepressant-like effects were reversed by mecamylamine and haloperidol, slightly by ketanserin, and potentiated by scopolamine, suggesting that aniracetam’s efficacy is more pronounced when brain dysfunction accompanies stress and is likely mediated by enhancing dopaminergic transmission through nicotinic acetylcholine receptor stimulation.
You can read the abstract of the article at https://link.springer.com/article/10.1007/s002130100849.
O’Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson’s disease. Current drug targets. 2007; 8(5):603-20.
AMPA receptor potentiators: application for depression and Parkinson’s disease
AMPA receptors, which mediate most excitatory neurotransmission and contribute to synaptic plasticity, are composed of four subunits (Glu(A1)-Glu(A4)) and exhibit further diversity through RNA splicing. Positive modulation of AMPA receptors, through compounds like aniracetam and other potentiators, has shown therapeutic potential for cognitive deficits. These modulators enhance cognitive function in rodents and humans by increasing hippocampal activity and BDNF expression via calcium-dependent and independent pathways, including MAPK signaling. This modulation suggests benefits for treating cognitive impairment in Alzheimer’s, schizophrenia, depression, and neuroprotection in Parkinson’s disease.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/15180479/#:~:text=Therefore%2C%20these%20AMPA%20receptor%20potentiators,enhancing%20recovery%20from%20Parkinson’s%20disease.
Deutschenbaur L, Beck J, Kiyhankhadiv A. Role of calcium, glutamate and NMDA in major depression and therapeutic application. Progress in neuro-psychopharmacology & biological psychiatry. 2016; 64:325-33.
Role of calcium, glutamate and NMDA in major depression and therapeutic application
Major depression, a prevalent and recurrent mental illness, has recently seen promising treatment developments through the glutamatergic system, particularly with ketamine. Evidence indicates that targeting excitatory amino acid neurotransmitter glutamate, specifically through NMDA receptor antagonists and AMPA agonists, has significant antidepressant properties. These treatments can foster new synaptic connections and reverse stress-induced neuronal changes. Numerous compounds, including ketamine, memantine, amantadine, and others targeting glutamatergic signaling, show potential as future therapeutic options for major depression, opening new avenues for effective treatments.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0278584615000494?via%3Dihub.
Knapp RJ, Goldenberg R, Shuck C. Antidepressant activity of memory-enhancing drugs in the reduction of submissive behavior model. European journal of pharmacology. 2002; 440(1):27-35.
Antidepressant activity of memory-enhancing drugs in the reduction of submissive behavior model
This study evaluated the effects of nootropic drugs on depressive behavior using a competition test where two food-restricted rats competed for access to a feeder. Nootropic drugs, including piracetam, aniracetam, and Ampalex, were compared to antidepressants fluoxetine and desimpramine, with diazepam as a control. Administered intraperitoneally for three weeks, both antidepressants and nootropic drugs reduced submissive behavior, with Ampakines showing a dose-dependent effect and quicker onset of activity compared to fluoxetine. The effects of Ampakines diminished after treatment cessation. These findings suggest that Ampakines and other memory-enhancing drugs may have potential antidepressant effects, highlighting a possible link between cognition and depression.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0014299902013389?via%3Dihub.
Nakamura K. Aniracetam: its novel therapeutic potential in cerebral dysfunctional disorders based on recent pharmacological discoveries. CNS drug reviews. 2002; 8(1):70-89.
Aniracetam: its novel therapeutic potential in cerebral dysfunctional disorders based on recent pharmacological discoveries
Aniracetam, a pyrrolidinone-type cognition enhancer, is clinically used for behavioral and psychological symptoms of dementia, particularly after stroke and in Alzheimer’s disease. Recent studies in behavioral pharmacology, biochemistry, and pharmacokinetics suggest new potential uses for aniracetam in treating various CNS disorders. This review highlights aniracetam’s effects in rodent models of mental function impairment and cerebral dysfunction, noting that its major metabolites may contribute to its pharmacological impact. The animal models include conditions such as hypoattention, impulsiveness, anxiety, depression, and sleep disorders, which are related to various clinical disorders. Although animal model results are promising, clinical efficacy remains to be confirmed through trials. The review also discusses new insights into aniracetam’s mechanisms of action, target sites, and effects on signal transduction.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6741661/.
Senin U, Abate G, Fieschi C, Gori G, Guala A, Marini G, Villardita C, Parnetti L. Aniracetam (Ro 13-5057) in the treatment of senile dementia of Alzheimer type (SDAT): results of a placebo controlled multicentre clinical study. Eur Neuropsychopharmacol. 1991 Dec;1(4):511-7. doi: 10.1016/0924-977x(91)90004-e. PMID: 1822317.
Aniracetam (Ro 13-5057) in the treatment of senile dementia of Alzheimer type (SDAT): results of a placebo controlled multicentre clinical study
In a double-blind, randomized study involving 109 elderly patients with mild to moderate cognitive impairment meeting NINCDS-ADRDA criteria for probable Alzheimer’s disease, aniracetam was administered for 6 months. The aniracetam group showed significant improvement in psychobehavioral parameters compared to the placebo group, which exhibited steady deterioration. The study confirmed aniracetam’s efficacy and excellent tolerability in enhancing cognitive functions in these patients.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/0924977X9190004E?via%3Dihub.
Sakurai T, Hatanaka S, Tanaka S, Yamasaki T, Kojima H, Akashi A. Protective effect of DM-9384, a novel pyrrolidone derivative, against experimental cerebral anoxia. Japanese journal of pharmacology. 1990; 54(1):33-43.
Protective effect of DM-9384, a novel pyrrolidone derivative, against experimental cerebral anoxia
DM-9384 demonstrated significant protective effects against various types of cerebral anoxia in animal models. Oral administration of DM-9384 notably prolonged survival time in mice and rats under normobaric hypoxia and provided significant protection against hypobaric hypoxia, histotoxic anoxia, and cerebral ischemia at specific doses. Unlike other drugs such as bifemelane, piracetam, aniracetam, and pramiracetam, which showed variable effectiveness, DM-9384 consistently attenuated hypoxia-induced hypolocomotion and cerebral energy metabolism disturbances without affecting normal brain function. These findings characterize DM-9384 as a broad-spectrum anti-anoxic drug with minimal central nervous system depression, likely due to its ability to improve cerebral energy metabolism.
You can read the abstract of the article at https://www.jstage.jst.go.jp/article/jphs1951/54/1/54_1_33/_article.
Retrieved from https://erowid.org/references/refs_view.php?ID=8850.
Cannady R, Fisher KR, Graham C, Crayle J, Besheer J, Hodge CW. Potentiation of amygdala AMPA receptor activity selectively promotes escalated alcohol self-administration in a CaMKII-dependent manner. Addiction biology. 2017; 22(3):652-664.
Potentiation of amygdala AMPA receptor activity selectively promotes escalated alcohol self-administration in a CaMKII-dependent manner
Growing evidence suggests that drugs of abuse hijack glutamate-linked neuroplasticity mechanisms in reward-related brain regions. This study shows that glutamate AMPA receptor (AMPAR) activity in the amygdala is crucial for the reinforcing effects of alcohol, a key step in addiction development. Self-administration of low-dose alcohol in alcohol-preferring rats increases AMPAR phosphorylation in the amygdala and nucleus accumbens. Site-specific infusion of the AMPAR positive modulator aniracetam in the amygdala enhances alcohol, but not sucrose, self-administration, suggesting a role for AMPARs in alcohol reinforcement. Additionally, inhibition of CaMKII, a kinase involved in AMPAR signaling, reduces alcohol self-administration and blocks aniracetam-induced escalation, indicating that AMPAR-CaMKII signaling in the amygdala promotes increased alcohol consumption.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4935658/.
Cannady R, Fisher KR, Durant B, Besheer J, Hodge CW. Enhanced AMPA receptor activity increases operant alcohol self-administration and cue-induced reinstatement. Addiction biology. 2013; 18(1):54-65.
Enhanced AMPA receptor activity increases operant alcohol self-administration and cue-induced reinstatement
Long-term alcohol exposure leads to neuroadaptations that enhance excitatory neurotransmission and AMPA receptor signaling. This study explored the role of increased AMPA receptor activity using aniracetam, a positive allosteric modulator, in alcohol self-administration and cue-induced relapse in alcohol-preferring rats. Aniracetam pre-treatment significantly increased alcohol-reinforced responses without affecting locomotor activity, an effect blocked by an AMPA receptor antagonist. Aniracetam did not impact sucrose-reinforced responses, indicating a selective effect on alcohol reinforcement. Additionally, aniracetam potentiated cue-induced reinstatement of alcohol-seeking behavior. These findings suggest that enhanced AMPA receptor activity facilitates alcohol consumption and seeking, contributing to alcohol abuse disorders.
You can read the full article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3535558/.
Rial D, Takahashi RN, Morato GS. Aniracetam and DNQX affect the acquisition of rapid tolerance to ethanol in mice. Pharmacology, biochemistry, and behavior. 2009; 92(1):32-8.
Aniracetam and DNQX affect the acquisition of rapid tolerance to ethanol in mice
Several studies have highlighted the role of learning in rapid tolerance development and the importance of glutamate-mediated neurotransmission. This study examined the influence of the AMPA/kainate receptor system on rapid ethanol tolerance using the rotarod test. Mice pretreated with aniracetam, an AMPA/kainate receptor agonist, before ethanol administration showed facilitated rapid tolerance to ethanol, while those pretreated with DNQX, an AMPA receptor antagonist, showed blocked rapid tolerance. Furthermore, DNQX blocked aniracetam-induced facilitation of ethanol tolerance. These findings suggest that non-NMDA receptors are involved in the development of rapid ethanol tolerance.
You can read the full article at https://www.sciencedirect.com/science/article/abs/pii/S0091305708003493?via%3Dihub.
MA H, ZHU G. The dopamine system and alcohol dependence. Shanghai Archives of Psychiatry. 2014;26(2):61-68. doi:10.3969/j.issn.1002-0829.2014.02.002.
The dopamine system and alcohol dependence
The article titled “The dopamine system and alcohol dependence” by Ma and Zhu, published in the Shanghai Archives of Psychiatry in 2014, discusses the role of the dopamine system in alcohol dependence. The study explores the neurobiological mechanisms related to the dopamine neurotransmitter system and its involvement in alcohol dependence and addiction. Understanding the interplay between dopamine and alcohol dependence is crucial for developing insights into the neurobiology of addiction and potential treatment approaches for alcohol use disorders.
You can read the abstract of this article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4120286/.
Banerjee N. Neurotransmitters in alcoholism: A review of neurobiological and genetic studies. Indian Journal of Human Genetics. 2014;20(1):20-31. doi:10.4103/0971-6866.132750.
Neurotransmitters in alcoholism: A review of neurobiological and genetic studies
The review article titled “Neurotransmitters in alcoholism: A review of neurobiological and genetic studies” by Banerjee, published in the Indian Journal of Human Genetics in 2014, provides an overview of the role of neurotransmitters in alcoholism. The review summarizes findings from neurobiological and genetic studies related to neurotransmitter systems and their involvement in alcohol use disorders. Understanding the complex interactions between neurotransmitters and alcoholism is essential for unraveling the underlying mechanisms of alcohol addiction and may inform the development of targeted interventions and treatments for individuals with alcohol-related issues.
You can read the abstract of this article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4065474/.
Noble EP. Alcoholism and the dopaminergic system: a review. Addiction biology. 1996; 1(4):333-48.
Alcoholism and the dopaminergic system: a review
The review article titled “Alcoholism and the dopaminergic system: a review” by Noble, published in Addiction Biology in 1996, provides an in-depth review of the relationship between alcoholism and the dopaminergic system. The study delves into the neurobiological aspects of alcohol addiction, focusing on how dopamine, a key neurotransmitter, plays a role in the development and maintenance of alcohol use disorders. This review synthesizes existing research on the dopaminergic system and its implications for understanding and addressing alcoholism, contributing to our knowledge of the neurobiology of addiction.
You can read the abstract of this article at https://onlinelibrary.wiley.com/doi/abs/10.1080/1355621961000124956.
Di Chiara G. Alcohol and dopamine. Alcohol health and research world. 1997; 21(2):108-14.
Alcohol and dopamine
The article titled “Alcohol and dopamine” by Di Chiara, published in Alcohol Health and Research World in 1997, discusses the relationship between alcohol consumption and the dopamine neurotransmitter system. The article provides insights into how alcohol affects dopamine release and signaling in the brain, which is important for understanding the rewarding and reinforcing properties of alcohol and its role in addiction. Understanding the interaction between alcohol and the dopamine system is crucial for comprehending the neurobiology of alcohol use and addiction.
You can read the abstract of this article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6826820/
Cui JF, Yang W, Xie YM, Sun Y, Zhuang Y, Wang YY. [Real-world analysis of concurrent diseases and medicine use among patients with insomnia]. ZhongguoZhongyaozazhi = Zhongguozhongyaozazhi = China journal of Chinese materiamedica. 2014; 39(18):3519-26.
Real-world analysis of concurrent diseases and medicine use among patients with insomnia
The article titled “[Real-world analysis of concurrent diseases and medicine use among patients with insomnia]” by Cui et al., published in the Zhongguo Zhongyao Zazhi (China Journal of Chinese Materia Medica) in 2014, presents a real-world analysis of the co-occurring medical conditions and medication usage patterns among patients with insomnia. The study likely examines the prevalence of other health conditions that coincide with insomnia and the medications commonly used by these patients as part of their treatment regimens. Understanding these patterns in real-world clinical settings can provide insights into the management and comorbidities associated with insomnia.
You can read the abstract of this article at https://europepmc.org/article/med/25532388.
Katsunuma H, Shimizu T, Ogawa K, Kubo H, Ishida H, Yoshihama A. Treatment of insomnia by concomitant therapy with Zopiclone and Aniracetam in patients with cerebral infarction, cerebroatrophy, Alzheimer’s disease and Parkinson’s disease. Psychiatry and clinical neurosciences. 1998; 52(2):198-200.
Treatment of insomnia by concomitant therapy with Zopiclone and Aniracetam in patients with cerebral infarction, cerebroatrophy, Alzheimer’s disease and Parkinson’s disease
The study titled “Treatment of insomnia by concomitant therapy with Zopiclone and Aniracetam in patients with cerebral infarction, cerebroatrophy, Alzheimer’s disease and Parkinson’s disease” by Katsunuma et al., published in Psychiatry and Clinical Neurosciences in 1998, explores the use of a combination therapy involving Zopiclone and Aniracetam for the treatment of insomnia in patients with various neurological conditions, including cerebral infarction, cerebroatrophy, Alzheimer’s disease, and Parkinson’s disease. The study likely examines the efficacy and safety of this combination treatment approach for managing insomnia in patients with these neurological disorders. Understanding how such treatments impact sleep quality in these patient populations is essential for improving their overall well-being and quality of life.
You can read the abstract of this article at https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1440-1819.1998.tb01028.x.
Kimura M, Okano S, Inoué S. Effects of aniracetam on impaired sleep patterns in stroke-prone spontaneously hypertensive rats. Psychiatry and clinical neurosciences. 2000; 54(3):314-6.
Effects of aniracetam on impaired sleep patterns in stroke‐prone spontaneously hypertensive rats
The study titled “Effects of aniracetam on impaired sleep patterns in stroke-prone spontaneously hypertensive rats” by Kimura et al., published in Psychiatry and Clinical Neurosciences in 2000, investigates the impact of aniracetam on sleep patterns in stroke-prone spontaneously hypertensive rats. The research likely examines how aniracetam, a nootropic compound, affects sleep quality and patterns in these rats, which are a model for hypertension and stroke susceptibility. Understanding the effects of aniracetam on sleep in this specific rat model provides insights into its potential therapeutic applications for sleep-related issues and neurological conditions.
You can read the abstract of this article at https://onlinelibrary.wiley.com/doi/abs/10.1046/j.1440-1819.2000.00693.x.
Kimura M, Okano S, Inoué S. Effects of aniracetam on impaired sleep patterns in stroke-prone spontaneously hypertensive rats. Psychiatry Clin Neurosci. 2000 Jun;54(3):314-6. doi: 10.1046/j.1440-1819.2000.00693.x. PMID: 11186092.
Effects of aniracetam on impaired sleep patterns in stroke‐prone spontaneously hypertensive rats
The study titled “Effects of aniracetam on impaired sleep patterns in stroke-prone spontaneously hypertensive rats” by Kimura et al., published in Psychiatry and Clinical Neurosciences in June 2000, explores the impact of aniracetam on sleep patterns in stroke-prone spontaneously hypertensive rats. The research investigates whether aniracetam, a nootropic compound, can modify sleep patterns in this specific rat model, which is prone to hypertension and stroke. Understanding the potential effects of aniracetam on sleep in this context contributes to our knowledge of its therapeutic applications, particularly in the context of neurological conditions and sleep disturbances.
You can read the abstract of this article at https://onlinelibrary.wiley.com/doi/abs/10.1046/j.1440-1819.2000.00693.x.
Ling DS, Benardo LS. Nootropic agents enhance the recruitment of fast GABAA inhibition in rat neocortex. Cerebral cortex (New York, N.Y. : 1991). 2005; 15(7):921-8.
Nootropic Agents Enhance the Recruitment of Fast GABAA Inhibition in Rat Neocortex
The study titled “Nootropic agents enhance the recruitment of fast GABAA inhibition in rat neocortex” by Ling and Benardo, published in the journal Cerebral Cortex in 2005, investigates the effects of nootropic agents on the recruitment of fast GABAA inhibition in the neocortex of rats. Nootropic agents are known for their cognitive-enhancing properties, and this research likely explores how these substances impact the inhibitory GABAA receptor system in the brain’s neocortex. Understanding the mechanisms by which nootropics influence neural inhibition can provide insights into their potential for enhancing cognitive function.
You can read the abstract of this article at https://academic.oup.com/cercor/article-abstract/15/7/921/387971.
Nakamura K, Kurasawa M. Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43. doi: 10.1016/s0014-2999(01)01005-6. PMID: 11412837.
Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism
The study titled “Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism” by Nakamura and Kurasawa, published in the European Journal of Pharmacology in May 2001, investigates the anxiolytic (anxiety-reducing) effects of aniracetam in three distinct mouse models of anxiety. The research likely explores the behavioral and neurobiological mechanisms through which aniracetam exerts its anxiolytic effects. Understanding the potential anti-anxiety properties of aniracetam and its underlying mechanisms can provide valuable insights for the development of treatments for anxiety-related disorders.
You can read the abstract of this article at https://www.sciencedirect.com/science/article/pii/S0014299901010056.
Both S, Everaerd W, Laan E, Gooren L. Effect of a single dose of levodopa on sexual response in men and women. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2005; 30(1):173-83.
Effect of a single dose of levodopa on sexual response in men and women
The study titled “Effect of a single dose of levodopa on sexual response in men and women” by Both et al., published in Neuropsychopharmacology in 2005, investigates the impact of a single dose of levodopa on sexual response in both men and women. Levodopa is a medication commonly used to treat Parkinson’s disease, and this research likely examines its effects on sexual function and response. Understanding the influence of levodopa on sexual behavior and arousal in both genders can provide valuable insights into its potential impact on sexual health and functioning.
You can read the abstract of this article at https://www.nature.com/articles/1300580.
Simonsen U, Comerma-Steffensen S, Andersson KE. Modulation of Dopaminergic Pathways to Treat Erectile Dysfunction. Basic & clinical pharmacology & toxicology. 2016; 119 Suppl 3:63-74.
Modulation of dopaminergic pathways to treat erectile dysfunction
The article titled “Modulation of Dopaminergic Pathways to Treat Erectile Dysfunction” by Simonsen et al., published in Basic & Clinical Pharmacology & Toxicology in 2016, discusses the potential use of dopaminergic pathways modulation as a therapeutic approach for treating erectile dysfunction (ED). The article likely explores how targeting dopaminergic mechanisms can influence the physiology and regulation of penile erection and addresses the potential pharmacological interventions that can enhance erectile function. Understanding the role of dopamine and its modulation in the context of ED treatment can provide insights into novel therapeutic strategies for individuals with this condition.
You can read the abstract of this article at https://onlinelibrary.wiley.com/doi/abs/10.1111/bcpt.12653.
Steers WD. Pharmacologic Treatment of Erectile Dysfunction. Reviews in Urology. 2002;4(Suppl 3):S17-S25.
Pharmacologic treatment of erectile dysfunction
The article titled “Pharmacologic Treatment of Erectile Dysfunction” by Steers WD, published in Reviews in Urology in 2002, discusses the pharmacological approaches for the treatment of erectile dysfunction (ED). It likely provides an overview of various medications, including phosphodiesterase type 5 (PDE5) inhibitors like sildenafil (Viagra), as well as other treatment options available for ED. Understanding the pharmacological treatments for ED is essential for healthcare professionals and individuals seeking effective therapies for this condition.
You can read the abstract of this article at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1476024/.
Hull EM, Muschamp JW, Sato S. Dopamine and serotonin: influences on male sexual behavior. Physiology & behavior. 2004; 83(2):291-307.
Dopamine and serotonin: influences on male sexual behavior
The article titled “Dopamine and serotonin: influences on male sexual behavior” by Hull EM, Muschamp JW, and Sato S, published in Physiology & Behavior in 2004, discusses the roles of dopamine and serotonin in influencing male sexual behavior. It likely explores the neurochemical mechanisms and pathways through which these neurotransmitters affect sexual function and behavior in males. Understanding the interplay between dopamine and serotonin in the context of sexual behavior can provide insights into the underlying neural processes and potential implications for sexual health and dysfunction.
You can read the abstract of this article at https://www.sciencedirect.com/science/article/pii/S0031938404003579.
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