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Aniracetam (Draganon, Sarpul, Ampamet, Memodrin, Referan) is also known as 1-[(4-methoxyphenyl)carbonyl]pyrrolidin-2-one.
It is classified both as a Racetam and an Ampakine nootropic substance with interactions with the cholinergic, dopaminergic, serotonergic and glutamatergic systems.
Aniracetam is a lipophilic derivative of Piracetam, exhibiting many of the same same effects with an estimated 3-6x increased potency. It increases cholinergic neurotransmission as is typical of the Racetam class of nootropics.
It also positively modulates glutamatergic activity via AMPA receptors and is considered the model for Ampakine agents. Additional mechanisms of action involve Dopaminergic, Serotonergic and GABAergic pathways.
Observed effects in research trials include the following:
- Enhances cognitive function in impaired individuals.
- Increases levels of Brain-Derived Neurotrophic Factor.
- Exhibits anxiolytic properties and an increase in social interaction.
- Reduces signs of depression and impulsive behaviors.
- Exerts a neuroprotective effect.
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Product Name: Aniracetam (Draganon, Sarpul, Ampamet, Memodrin, Referan)
Chemical Name: 1-[(4-methoxybenzoyl)]- 2-pyrrolidinone
Formula: C12H13NO3
Molecular Weight: 219.237 g/mol
CAS Number: 72432-10-1
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Aniracetam Research
Related Topics
- What is Aniracetam?
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- Best Way to Take
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- Aniracetam for Sale
- Buyer's Guide
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- Stacking with Piracetam
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- Comparison to Piracetam
- Comparison to Oxiracetam
- Comparison to Pramiracetam
- Comparison to Noopept
Aniracetam was derived from Piracetam in the 1970’s by the Hoffmann-La Roche pharmaceutical company.
Initial research found it to be a more potent analogue of Piracetam, earning it the prefix “Ani” which in Japanese means “big brother.”
Aniracetam has been studied for its behavior altering, cognitive enhancement properties and as a neuroprotective agent for the treatment of Alzheimer’s disease and senile cognitive disorders.
Aniracetam’s pharmacological profile is similar to Piracetam, though it exhibits a greater anxiolytic and anti-depressive effect than its parent molecule.
Like Piracetam, it is hypothesized to facilitate cholinergic transmission. Unlike Piracetam, Aniracetam is fat-soluble which may contribute to its increased potency. [1]
Aniracetam is also a positive modulator of metabotropic gultamate receptors and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic AMPA excitatory receptors.
It is considered to be the first AMPAkine compound invented and is the prototype for other Ampakines that have followed.
Aniracetam Chemical Structure
Like Piracetam, Aniracetam has a 2-pyrrolidinone nucleus which is the distinctive feature of the Racetam family of compounds.
However, where Piracetam has an amine group, Aniracetam has a methylated phenyl group. This modification gives Aniracetam greater fat solubility which results in a potency between 3 – 6 times greater than Piracetam.
Pharmacokinetics
Oral Bio-availability was between 8.6 – 11.4% in rats when consumed on an empty stomach. [3]
Given its lipophilic nature, bio-availability should be improved when consumed with fatty acids, however no studies are available that examine this.
Serum levels of Aniracetam peak at 2.3mcg/L with a 300mg dosage and 14.1mcg/L following a 1200mg dose. It has a Cmax of 8.75+/-7.82 and 8.65+/-8.7ng/mL and a Tmax of 0.4+/-0.1 following a 400 mg dosage. [4]
The elimination half-life of Aniracetam is a rapid 35 minutes following oral ingestion. Within 48 hours of administration, 84% of the dosage was eliminated in urine, 0.8% in feces and 11% was expelled as carbon dioxide. [1]
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Metabolites
There is a high degree of first pass hepatic metabolism into the metabolites 2-pyrrolidinone, N-anisoyl-GABA, and anisic acid.
N-anisoyl-GABA is the primary metabolite, making up 70% by weight of the initial dosage following transformation by the liver. [4]
A study on the attentional and vigilance task performance of rats given Aniracetam found that 2-pyrrolidinone and N-anisoyl-GABA are the main active metabolites.
Both of these compounds partially mimicked the effects of Aniracetam in improving 8-OHDPAT-induced attentional and vigilance impairments. [8]
Aniracetam Mechanisms of Action
The mechanism of action for Aniracetam is not fully understood, however trials have shown it to exhibit cholinergic, dopaminergic, serotonergic, glutamatergic and indirect adrenergic effects.
Like Piracetam and other Racetam nootropics, Aniracetam is a positive modulator of Nicotinic receptors for the neurotransmitter acetylcholine.
In animal studies, it alleviates memory and learning impairments caused by cholinergic antagonists.
It is also observed to increase acetylcholine release from the hippocampus in rat trials and facilitates an increase in cholinergic neurotransmission. [36]
AMPA Glutamatergic Receptors
Aniracetam is a positive allosteric modulator of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA, quisqualate) receptors for the neurotransmitter Glutamate.
It also positively modulates metabotropic glutamate receptors. [1]
These neuro-receptors mediate fast synaptic transmission in the central nervous system and are integral to synaptic plasticity and Long-Term Potentiation by which memories are stored.
Aniracetam binds to non-active AMPA receptors and modifies them so they exhibit a reduced rate of desensitization. This results in a greater level of activation when Glutamate or other agonists are present.
Aniracetam is also a positive modulator of kainate Glutamatergic receptors but does not directly influence NMDA receptors. [15]
GABAergic Receptors
Aniracetam has been observed to enhance cortical GABAergic inhibition. It was found to increase the total charge of Inhibitory Post-Synaptic Currents (IPSC’s).
Research indicates that Aniracetam may strengthen inhibitory neurotransmission at neocortical pyramidal cells by modulating GABA-A responses. [21]
Serotonergic Receptors
Turnover is a measure of the amount and rate at which a neurotransmitter is transmitted across the synaptic cleft and re-synthesized within the pre-synaptic neuron.
An increased rate of turnover means that more of a neurotransmitter is being used while a decreased rate means that less is being used.
Aniracetam administered at 50 mg/kg was found to delay Serotonin (5-HT) turnover in the hypothalamus and increase 5-HT turnover in the cortex, striatum and stem. [6]
Dopaminergic Receptors
Aniracetam at 50 mg/kg reduced Dopamine turnover rates in the striatum. It further reduced dopamine levels in the striatum and hypothalamus.
In another study, Aniracetam was found to facilitate dopaminergic signalling via dopamine release and dopamine D2 receptor activation through stimulation of excitatory nicotinic acetylcholine receptors. [6]
Adrenergic Receptors
Indirectly, Aniracetam is observed to increase [3H]noradrenaline (norepinephrine) release in the rat hippocampus.
This is mediated by Aniracetam’s effects on AMPA receptors which leads to enhanced noradrenaline (norepinephrine) secretions from neurons. The result is a slight stimulatory effect on the Central Nervous System.
This effect is only observed in larger dosages of Aniracetam yielding high micromolar concentrations of at least 100µM. [20]
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Aniracetam for Cognitive Enhancement
Aniracetam was found to improve cognitive function in elderly patients diagnosed with mild to moderate impairments caused by senile dementia of the Alzheimer type (SDAT). [1]
It decreased the rate of ionotropic AMPA receptor desensitization in the hippocampus, leading to enhanced glutamatergic signalling.
It also increased EPSPs in the fibre-CA3 synapses suggesting a mechanism for improved memory formation. [17]
Ampakine nootropics in general have been found to increase levels of Brain-derived Neurotrophic factor (BDNF) in entorhinal/hippocampal slices.
This protein is integral to the maintenance, growth and development of new neurons leading to improved neuroplasticity and memory function.
Ampakine-induced upregulation is attributed to AMPA receptor agonists and was not reversed when an NMDA receptor antagonist was administered. [29]
Neuroprotection
Aniracetam reverses some forms of cognitive damage caused by prenatal alcohol exposure. [35] It can also protect the brain against damage caused by electroconvulsive shock and cerebral ischaemia. [1]
It is shown to reduce impairments caused by cerebrovascular disorders and defects.
In patients with cognitive deficits caused by cerebrovascular disease, a 1000mg/day Aniracetam dosage for 1 month and a 1500mg/day dosage for 4 months were both found to be more effective than a placebo at reducing impairments. [1]
A 1500mg dosage of Aniracetam also reduced scopolamine-induced cognitive impairments in healthy young individuals. It was found to be more effective than a 2400mg dosage of Piracetam on the same model. [23, 1]
Anxiolytic and Anti-Depressant Properties
Aniracetam is observed to improve anxiety in rats leading to an increase in social interactions.
This anxiolytic effect was observed between dosages of 10mg/kg to 100mg/kg of bodyweight. It has also been found to reduce impulsiveness in rat behavior. [24]
Aniracetam also exhibits an anti-depressant effect in aged (25-30 months old) rats as measured by reduced immobility times in a forced swim test. This result was not repeated in trials with younger (9 week old) rats.
This effect is attributed to its metabolites 2-pyrrolidinone and N-anisoyl-GABA which lead to increased dopaminergic transmission via stimulation of nicotinic acetylcholine receptors. [25]
Aniracetam Safety and Side Effects
Aniracetam shows a high degree of tolerability with no detected liver toxicity. No increases in liver enzymes have been observed following hepatic Aniracetam metabolism.
Human trials are limited and there have not been any established rates of incidents for serious adverse effects.
Mild side effects have been reported consisting of restlessness, anxiety, and sleeplessness. Less common side effects include “headache, somnolence, vertigo, mild epigastric pain, nausea, diarrhoea and rash.” [1]
Dosage and Administration
Oral Aniracetam administration has been studied at dosages between 600mg per day to 1500mg per day.
Patients with Senile Dementia of the Alzheimer’s Type (SDAT) are treated at 1000mg to 1500mg per day taken as a single dose or as two 750mg oral tablets per day.
In Japan, dosages of 200mg taken three times a day is recommended for patients with anxiety or depression symptoms following a cerebral infarction. [1]
Study Summaries
Vaglenova J, et al. Aniracetam reversed learning and memory deficits following prenatal ethanol exposure by modulating functions of synaptic AMPA receptors. Neuropsychopharmacology. 2008 Apr;33(5):1071-83. Epub 2007 Jul 4.
Aniracetam was found to reverse certain cognitive deficits caused by Fetal Alcohol Syndrome (FAS) and Fetal Alcohol Spectrum Disorders (FASD).
In rats administered ethanol (alcohol) at 4 g/kg/24 h; 38% v/v throughout the pregnancy, severe cognitive disabilities developed in the offspring.
Administering 50 mg/kg Aniracetam dosages for 10 days after birth starting on the 18th day lead to a reversal of cognitive deficits. The improvements were mediated through post-natal modulation of AMPA receptors in the hippocampal CA-1 pyramidal cells. [35]
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.
Aniracetam was found to benefit elderly patients with mild to moderate cognitive impairment caused by senile dementia of the Alzheimer type.
Dosages of 1500mg/day for 4 and 6 months were significantly more effective than a placebo at improving cognitive function as measured by a battery of 18 tests.
Aniracetam 1500 mg performed better than the placebo in 18 of 18 tests and performed better than 2400mg/day of Piracetam in 8 of 18 tests in a 6 month trial.
The study found that Aniracetam is well tolerated and does not result in an increase in liver enzyme levels. [1]
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- 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.
- Yoshii M, Watabe S. Enhancement of neuronal calcium channel currents by the nootropic agent, nefiracetam (DM-9384), in NG108-15 cells. Brain Res. 1994 Apr 11;642(1-2):123-31.
- Ogiso T, et al. Pharmacokinetics of aniracetam and its metabolites in rats. J Pharm Sci. 1998 May;87(5):594-8.
- Tian Y, et al. Pharmacokinetics and bioequivalence study of aniracetam after single-dose administration in healthy Chinese male volunteers. 2008;58(10):497-500. doi: 10.1055/s-0031-1296547.
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- Zhang J, et al. Sensitive and selective liquid chromatography-tandem mass spectrometry method for the quantification of aniracetam in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Oct 15;858(1-2):129-34. Epub 2007 Aug 21.
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- Ouchi Y, et al. The effect of aniracetam on cerebral glucose metabolism in rats after lesioning of the basal forebrain measured by PET. J Neurol Sci. 1999 Mar 15;164(1):7-12.
- Ito I, et al. Allosteric potentiation of quisqualate receptors by a nootropic drug aniracetam. J Physiol. 1990 May;424:533-43.
- Zhao X, et al. Nootropic drug modulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons. Mol Pharmacol. 2001 Apr;59(4):674-83.
- Shirane M, Nakamura K. Aniracetam enhances cortical dopamine and serotonin release via cholinergic and glutamatergic mechanisms in SHRSP. Brain Res. 2001 Oct 19;916(1-2):211-21.
- Eleore L, et al. Modulation of the glutamatergic receptors (AMPA and NMDA) and of glutamate vesicular transporter 2 in the rat facial nucleus after axotomy. Neuroscience. 2005;136(1):147-60. Epub 2005 Sep 21.
- Ozawa S, Kamiya H, Tsuzuki K. Glutamate receptors in the mammalian central nervous system. Prog Neurobiol. 1998 Apr;54(5):581-618.
- Isaacson JS, Nicoll RA. Aniracetam reduces glutamate receptor desensitization and slows the decay of fast excitatory synaptic currents in the hippocampus. Proc Natl Acad Sci U S A. 1991 Dec 1;88(23):10936-40.
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- Tang CM, et al. Modulation of the time course of fast EPSCs and glutamate channel kinetics by aniracetam. Science. 1991 Oct 11;254(5029):288-90.
- Isaacson JS, Nicoll RA. Aniracetam reduces glutamate receptor desensitization and slows the decay of fast excitatory synaptic currents in the hippocampus. Proc Natl Acad Sci U S A. 1991 Dec 1;88(23):10936-40.
- Kaneko S, et al. Effects of several cerebroprotective drugs on NMDA channel function: evaluation using Xenopus oocytes and {3H}MK-801 binding. Eur J Pharmacol. 1991 Jun 19;207(2):119-28.
- Pittaluga A, et al. Aniracetam, 1-BCP and cyclothiazide differentially modulate the function of NMDA and AMPA receptors mediating enhancement of noradrenaline release in rat hippocampal slices. Naunyn Schmiedebergs Arch Pharmacol. 1999 Apr;359(4):272-9.
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- Vaglenova J, et al. Aniracetam reversed learning and memory deficits following prenatal ethanol exposure by modulating functions of synaptic AMPA receptors. Neuropsychopharmacology. 2008 Apr;33(5):1071-83. Epub 2007 Jul 4.
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Article last updated on: July 24th, 2018 by Nootriment