What is Fasoracetam?
Fasoracetam, also known as NFC-1, NS-105, and LAM-105, is a nootropic that belongs to the racetam family. Common uses for this nootropic include memory enhancement, alleviation of depression, anxiety, and ADHD symptoms, and to protect against age-related memory loss.
While much of the evidence for this racetam comes from anecdotal reports, there have been numerous animal studies and a few human studies that help us to understand how this compound works and what benefits it may hold.
A newer member of the racetam family, it was developed over two decades ago in Japan as a therapeutic agent for those suffering from dementia. Unfortunately human clinical trials did not yield sufficient results in this department.
In 2016 Fasoracetam research was started again, this time for the treatment of anxiety, ADHD, and autism (1,2,3). These three conditions are often accompanied by a mutation in the glutamate receptor, which this drug may be able to help with. Presently it is in phase 2/3 clinical trials.
How Fasoracetam Works
- The main mechanisms of action for Fasoracetam include:
- Boosts acetylcholine release
- Stimulates metabotropic glutamate receptors
- Up-regulates GABA(B) receptors
Choline and Acetylcholine
Many of the nootropic benefits of Fasoracetam are thanks to its effects on the synthesis and release of the neurotransmitter acetylcholine (ACh) in the brain.
If you have ever taken a racetam nootropic you are likely familiar with this powerful neurotransmitter. ACh is largely responsible for memory and learning. In order for the body to produce ACh, it needs its precursor, choline.
Once choline crosses the blood-brain barrier, it is taken up by cholinergic nerve terminals by high affinity choline uptake, or HACU. This uptake into the neuron is believed the be the rate limiting step in ACh synthesis.
Fasoracetam has been found to increase HACU in the hippocampus and cerebral cortex brain regions, which is then used in the synthesis of ACh. (5) It was also found that ACh release from the cerebral cortex was enhanced when taking this drug.
Thus, supplementation with Fasoracetam enhances HACU and ACh synthesis in the brain, leading to benefits on memory and learning.
Glutamate is an excitatory neurotransmitter, meaning that it plays a role in motivation and excitement.
Taking Fasoracetam has been linked to the activation of metabotropic glutamate receptors, particularly in restoring the function of mGluR II and III.
Excess glutamate actually converts to GABA, meaning that it is a precursor to GABA. This conversion helps the body to maintain balance, helping to keep you calm and relaxed. Without this conversion you would experience an overly excitatory, anxious states.
GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter that is used to help you calm down. The GABA(B) receptor has been linked to the pathophysiology of depression and anxiety (7). When GABA levels decrease, depression, anxiety, and even insomnia levels can worsen. GABA has been shown to play a role not only in mood and sleep, but also cognition.
Studies have found that this nootropic upregulates GABA receptors through receptor antagonism, increasing the number of GABA receptors in the cerebral cortex. (5,6,7) This upregulation of GABA(B) receptors has been found to lead to depression relief. (7)
Benefits and Uses
When you comb through Reddit and LongeCity user reviews, you will find the majority of the benefits focus around improved mood and ability to focus.
Both animal studies and user reviews tout a potent antidepressant activity of this nootropic.
In studies on rats this drug was found to reduce depression symptoms through up-regulation of GABA(B) receptors. (7) This improvement was similar to that of rats taking desipramine, a common antidepressant medication. The benefits appeared to counteract learned helplessness, which is often associated with depression.
Thanks to the up-regulation of GABA(B) that was found in the above animal study to be helpful with depression, it would follow that this drug may also exhibit anxiolytic properties. (7) While more studies need to be conducted to confirm this property, dysfunction of the GABA-ergic system is also thought to play a role in anxiety. (9)
Presently this drug is being researched for its anxiolytic properties in a human clinical trial. (2)
The glutamatergic neurotransmitter system is thought to play a role in ADHD.
Recently the Food and Drug Administration approved an Investigational New Drug (IND) status for Fasoracetam for the treatment of those with ADHD who have a glutamate gene mutation (3,8). While this mutation is rare, this is promising for those who suffer from this cause of ADHD.
In a phase I clinical trial of 30 adolescents between 12 and 17 with ADHD and mutations in the mGluR network genes published in January of 2018, it was found that fasoracetam led to improvement in ADHD symptoms and was well tolerated. (11) These promising results pave the way for phase II and III clinical trials.
Animal studies suggest that this nootropic acts as a neuroprotectant, which can help prevent against age-related cognitive decline while also improving memory for those with memory impairment, such as the elderly. (5)
In a study on rats it was found that this drug reversed memory disruption caused by baclofen, a GABA(B) receptor agonist. The researchers concluded that Fasoracetam helped to reverse chemically-induced amnesia symptoms partly through the suppression of GABA(B) receptor-mediated responses and also through an increase in ACh release in the cortex.
Boosts Energy and Concentration
According to user reports, this supplement can yield moderate benefits for overall energy and ability to focus. One LongeCity user reported a short-lived boost in focus of about 3-4 hours following supplementation. As for energy, some users find it calming while others report increased mental energy.
Dosage and Half Life
This supplement is highly bioavailable, with roughly 79%-97% absorbed following oral administration. (8) It’s half-life is estimated to be between 4 and 6.5 hours.
Thanks to the lack of extensive human studies, the recommended dosages for this nootropic have not been established. Because of this it is highly advisable to start low and work your way up until your ideal dosage has been established.
Fasoracetam is typically sold as a powder or capsule. The typical dosage is 20 mg/day, split into two doses. You may want to start at 5 mg per dose and build up from there. Typically the highest dose for nootropic purposes is 60 mg/day, divided into two.
While this supplement can be used sublingually to increase absorption, the powder is bitter. As the powder is bitter and the capsules tend to come in 20 mg doses, you can purchase the powder and put it into your own capsules.
In the clinical trial for ADHD patients, 100, 200, and 400 mg doses twice daily are being tested. (3).
It’s been noted that the quantity of Fasoracetam needed tends to decline with age thanks to the removal of this drug from your system via your kidneys. As we get older our kidneys take more time to clear this drug from the system.
Because of the effect of Fasoracetam on the cholinergic system, it’s recommended to pair this nootropic with a highly bioavailable source of choline that is capable of crossing over the blood-brain barrier. Your best options are Alpha GPC and Citicoline.
This drug is considered to have a well-established safety profile when taken at 50-800 mg/day divided into two doses. (8)
The most common side effects of this nootropic, headache and fatigue, are believed to be due to its taxing effect on choline levels in the body. High affinity choline uptake guarantees that ACh synthesis is a higher priority than the use of choline in other processes in the body. (4) Thanks to this, if you do not have sufficient levels of choline for this supplement to draw from, your choline supply can be monopolized for the creation of ACh, leading to symptoms of low choline levels, such as headache and fatigue.
As discussed earlier, thanks to the effect on choline and ACh, it is best to take Fasoracetam with a quality choline source to avoid the above side effects.
It is dangerous to take exceptionally large doses of this drug. Doses of greater than 1,000 mg/day may lead to bradycardia, particularly when paired with the drug phenibut. (8) This is a condition where the heart rate slows to less than 60 bpm. Phenibut is used for anxiety and cognitive function benefits, and acts through activating GABA receptors.
The elderly or those with kidney problems should also use caution with this drug as its excretion from the body relies on the kidneys. If your kidneys are not functioning well this could lead to a dangerous accumulation of this drug in your system.
Stacking Fasoracetam with Phenibut
Phenibut is a drug that is very powerful when it comes to helping anxiety, stress, depression, and more. Unfortunately, users tend to build up tolerance very quickly thanks to its property as a GABA(B) agonist. Withdrawal symptoms can be severe, including suicidal thoughts, anxiety, and severe depression. a drug that is very powerful when it comes to helping anxiety, stress, depression, and more. Unfortunately, users tend to build up tolerance very quickly thanks to its property as a GABA(B) agonist. Withdrawal symptoms can be severe, including suicidal thoughts, anxiety, and severe depression.
Fasoracetam, through its antagonistic properties on GABA(B) receptors, may help to lesson the tolerance to GABA(B) agonists. These include not only Phenibut but also alcohol and Baclofen. There is a chance that this supplement may even act to counteract Phenibut overdose.
That said, users should proceed with caution in how much Fasoracetam they take with Phenibut. In one documented case a male taking 1,000 mg/day Fasoracetam with Phenibut experienced bradycardia. It is best to start with small amounts and only use what is needed to experience the results you are looking for.
Where to Buy
Foreracetam is one of the many nootropics that you will not find at your local store. The best way to purchase it is through reputable online vendors.
You can find Fasoracetam in both 20 mg capsules and powder form through Nootropics Depot and as 20 mg capsules through Pure Nootropics. These two online vendors offer the best quality nootropics on the market.
- Phase I single dose, open-label pharmacokinetic study and single-blind, placebo-controlled dose escalation study of NFC-1 in adolescents with ADHD (NFC1-GREAT) https://clinicaltrials.gov/ct2/show/NCT02286817
- Safety and efficacy study of NFC-1 in subjects aged 12-17 years with 22q11.2DS & associated neuropsychiatric conditions https://clinicaltrials.gov/ct2/show/NCT02895906
- Efficacy and safety of NFC-1 in adolescents with genetic disorders impacting mGluR and ADHD https://clinicaltrials.gov/ct2/show/NCT02777931
- IA2. Uptake of Choline, a Precursor of Acetylcholine https://web.williams.edu/imput/synapse/pages/IA2.html
- Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer https://www.ncbi.nlm.nih.gov/pubmed/10494996
- A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors primary in neuronal culture https://www.ncbi.nlm.nih.gov/pubmed/9272724
- Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of the GABA(B) receptor upregulation after repeated treatment https://www.ncbi.nlm.nih.gov/pubmed/9424016
- Phenibut overdose in combination with Fasoracetam: emerging drugs of abuse https://www.heighpubs.org/jcicm/pdf/jcicm-aid1001.pdf
- GABAB receptors and depression. Current status. https://www.ncbi.nlm.nih.gov/pubmed/20655491
- Involvement of metabotropic glutamate receptor in Gi- and Gs- dependent modulation of adenylate cyclase activity induced by a novel cognition enhancer NS-105 in rat brain. https://www.ncbi.nlm.nih.gov/pubmed/9134967
- Fasoracetam in adolescents with ADHD and glutamatergic gene network variants disrupting mGluR neurotransmitter signalling. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5770454/