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Fasoracetam
What is Fasoracetam?
Fasoracetam is one of the most recently developed drugs in the racetam family. Fasoracetam is also sometimes known as NS-105, NFC 1, LAM 105, or MDGN-001.
The compound was first developed as a potential treatment for vascular dementia. However, after failing stage-three clinical trials due to a lack of efficacy, further development was ceased.
In recent years, neuroscientists have started to investigate the potential benefits of fasoracetam in treating disorders which include genetic mutations which affect glutamatergic receptors; this includes adolescents with ADHD, autism and anxiety. The drug is now at stage-2 clinical trials.
Fasoracetam appears to interact and modulate three major neurochemical systems in the brain; acetylcholine, GABA and glutamate.
Since fasoracetam is fairly new, the substance has not yet been widely studied. However, there have been some cellular and animal studies, along with human clinical trials, which suggest the compound may have multiple brain benefits.
Brain Benefits and Mode of Action
May Improve Cognition and Memory
Improvements to memory and cognition are some of the primary effects which are expressed by users. Unfortunately, there aren’t any publicly available human clinical studies to support these claims.
However, a small number of animal studies have investigated the cognitive and memory effects of fasoracetam in rodents. One study found that fasoracetam administration was able to attenuate or reverse experimentally induced memory loss.
Human clinical studies have begun to investigate fasoracetam as a potential treatment for ADHD. ADHD is a common psychiatric condition which is characterised by poor focus, lack of concentration, disorganised thoughts, impulsiveness, hyperactivity and trouble with various cognitive tasks.
One small-scale study demonstrated that fasoracetam effectively treated teenagers with a form of ADHD which was related to a genetic variation in a glutamate receptor gene. The compound effectively reduced symptoms of ADHD. There are also some indications that these effects were long-lasting, with many participants continuing to experience reduced symptoms after fasoracetam had stopped.
Mode of action: Since fasoracetam can act on a number of neurochemical systems, it’s likely that the drug has a number of biochemical mechanism which underlie its apparent effects of cognition and memory.
Firstly, fasoracetam can act on a subgroup of glutamatergic receptors known as metabotropic glutamate receptors (mGluRs). These receptors form a crucial part of the glutamatergic system, and play important roles in memory, learning and mood. There are eight mGluR subunits, two of which act to increase excitatory activity and size which inhibit excess excitation which could lead to excitotoxicity.
Animal studies have shown that fasoracetam can modulate and restore function of two types of inhibitory mGluRs, which helps to balance glutamatergic activity in the brain. Some neuroscientists have suggested that fasoracetam may regulate the whole mGluR system, which may restore balance across the entirety of the glutamatergic system. This mechanism would explain why fasoracetam can treat ADHD, a condition which is typically characterised by reduced glutamate activity. Overall, by balancing glutamate activity, fasoracetam may be able to produce a feeling of mental ‘sharpness’ and increased focus, without acting as a classical stimulant.
Other members of the racetam family of molecules which modulate acetylcholine levels have been shown to have robust effects on learning, memory and cognition.
Specifically, fasoracetam has been demonstrated to increase the uptake of the acetylcholine precursor, choline, in the cortex and hippocampus. These two ‘higher order’ brain regions are deeply implicated in all cognitive and memory-related tasks. It is probable that fasoracetam could exert similar cognition-enhancing effects to other members of the racetam class of drugs.
May Improve Anxiety and Stabilise Mood
Many fasoracetam users report mood stabalising effects. In particular, users report that fasoracetam produces improvement to mood, while also fostering a feeling of relaxation and calmness. Hence, many people find fasoracetam useful for the treatment of anxiety.
There aren’t yet any formal human clinical studies to support these claims. However, some preliminary animal research does offer positive indicates. One study found that rodents who were administered fasoracetam were less prone to learned helplessness, and showed a reduction in anxiety and depression-like behaviours.
Mode of action: Fasoracetam acts on two of the most influential and important brain neurotrasmitters; GABA and glutamate.
These neurotransmitters help to maintain the optimal balance of excitation and inhibition in neuronal circuits. Any disruption to this balance can have severe negative consequences. Aberrant GABA/glutamate activity has been associated with a variety of psychiatric disorders, including schizophrenia, bipolar disorder, anxiety and depression. By balancing the function of these neurotransmitters, fasoracetam may be assist with maintaining a stable mood.
Fasoracetam has been demonstrated to increase GABA-B receptor activity, meaning that more inhibitory GABA is available across the central nervous system. GABA is one of the primary inhibitory neurotransmitters which can exert calming effects, reduce anxiety and promote sleep. Increase the pool of GABA available for use within the brain may be one mechanism which underlies the calming, anti-anxiety effects of fasoracetam.
How to Use
Fasoracetam is orally bioavailable and water soluble. This means that the compound can be taken with or without food. It can also be administered sub-lingually (under the tongue) for improved absorption.
Fasoracetam appears to be generally well-tolerated and safe for most healthy individuals when taken responsibly.
Some side effects of the racetam family of drugs include, mild fatigue, digestive discomfort and headaches. Some of these effects, such as headache, are by a depletion in choline supplies due to enhanced choline uptake induced by fasoracetam. These symptoms can be avoided by stacking fasoracetam with a nootropic which enhances the pre-cursor pool of choline (such as citicoline).
As with all nootropic drugs, it’s important to consult a doctor before adding them to your regime, especially if you’re taking other medications or have an underlying health condition.
In particular, since fasoracetam is metabolised by the kidneys, anyone with impaired kidney function should consult a doctor before taking the drug.
Pregnant and breastfeeding women should avoid fasoracetam as there is no current data regarding the safety of the compound during pregnancy or to infants.
Stacks well with
- Citicoline. Stacking fasoracetam with citicoline will reduce the likelihood of any negative side effects by ensure precursor choline stocks are high enough for the increase in cellular choline uptake.
Recommended Dose: 20mg-100mg
There has been no formal clinical research which gives a definite answer on the most effective and safe dose of fasoracetam.
Human clinical trials have ranged from doses of 50mg – 400mg. However, it’s important to remember, that high doses are often intended to treat specific problems. For someone seeking to improve normal cognitive function, a much lower dose between 20mg – 100mg is recommended.
Fasoracetam is a powerful compound, and users should also begin with the lowest effective dose. The dosage should only be increase if not effects are felt and increases should be made gradually.
Classification: Memory, Cognition, Mood
As with most racetam molecules, we’ve classified it as a powerful cognitive and memory enhancer. This is because fasoracetam can exert potent effects on a number of neurochemical systems which lead to more balance and optimal brain function. Subsequently, users of this substance appear to experience improved memory, cognitive and mental clarity.
We’ve also classified fasoracetam as a mood booster because of the calming and stabilising effects the compound can exert by boosting GABA activity within the brain.
References
- Elia, J., Ungal, G., Kao, C., Ambrosini, A., De Jesus-Rosario, N., Larsen, L., Chiavacci, R., Wang, T., Kurian, C., Titchen, K., Sykes, B., Hwang, S., Kumar, B., Potts, J., Davis, J., Malatack, J., Slattery, E., Moorthy, G., Zuppa, A., Weller, A., … Hakonarson, H. (2018). Fasoracetam in adolescents with ADHD and glutamatergic gene network variants disrupting mGluR neurotransmitter signaling. Nature communications, 9(1), 4. https://doi.org/10.1038/s41467-017-02244-2
- Fatuma Nageye & Samuele Cortese (2019) Beyond stimulants: a systematic review of randomised controlled trials assessing novel compounds for ADHD, Expert Review of Neurotherapeutics, 19:7, 707-717, DOI: 10.1080/14737175.2019.1628640
- Harmsen, Bram et al. 2017. A Study of Fasoracetam’s Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical. Journal of Pharmaceutical Sciences, Volume 106, Issue 5, 1317 – 1321
- Takashi Ogasawara, Yoshinori Itoh, Masaru Tamura, Takeshi Mushiroi, Yojiro Ukai, Masahiro Kise, Kiyoshi Kimura. 1999. Involvement of Cholinergic and GABAergic Systems in the Reversal of Memory Disruption by NS-105, a Cognition Enhancer. Pharmacology Biochemistry and Behavior. Volume 64, Issue 1, Pages 41-52, ISSN 0091-3057, https://doi.org/10.1016/S0091-3057(99)00108-2.
- Takako Shimidzu, Yoshinori Itoh, Michiko Oka, Tsuyoshi Ishima, Yojiro Ukai, Yoshiaki Yoshikuni, Kiyoshi Kimura. 1997. Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: Possible involvement of GABAB receptor up-regulation after repeated treatment. European Journal of Pharmacology, Volume 338, Issue 3, Pages 225-232, ISSN 0014-2999, https://doi.org/10.1016/S0014-2999(97)81925-5.
