3. Fasoracetam Working principle and clinical research
Fasoracetam’s exact mechanisms of action are not entirely understood, but it is believed to work mainly by affecting the production and release of glutamate, GABA, and acetylcholine, three of the brain’s most important neurotransmitters.
Restoring Balance To The Glutamate System
Fasoracetam is known to modulate at least some of the brain’s receptors for glutamate, a crucial excitatory neurotransmitter essential for all aspects of brain function. Glutamate imbalances are associated with a variety of physical and mental disorders, including depressive disorder, ADHD, schizophrenia, epilepsy, and neurodegenerative disorders like Alzheimer’s disease.
Fasoracetam works on a specific group of glutamate receptors called metabotropic glutamate receptors, or mGluRs, which play a variety of roles in the body and brain but are mainly involved in learning, memory, and anxiety. The eight known mGluRs work together to maintain a delicate balance, with two acting to increase neural excitation and the remaining six reducing the risk of neurotoxicity by lessening neural excitation as needed.
In animal studies, Fasoracetam successfully restored the function of two inhibitory mGluRs, thus slightly lowering glutamate activity in the brain. However, it is thought that fasoracetam may well modulate all of the metabotropic glutamate receptors, restoring balance to the glutamate system as a whole. This may explain why fasoracetam may benefit individuals with ADHD, which is typically associated with low glutamate levels, without acting as an overall stimulant.
Glutamate is also the precursor to GABA, an important inhibitory neurotransmitter that is also associated with learning, but has calming effects and helps reduce anxiety and promote sleep. Fasoracetam has been shown to upregulate the activity of GABA-B receptors, making more GABA available in the brain and central nervous system.
This action, particularly in combination with the modulation of glutamate receptors, is at the heart of fasoracetam’s ability to alleviate depression and anxiety, decrease social inhibition, and increase motivation. In rat studies, this combined action was seen as key to the subjects’ ability to overcome learned helplessness after treatment with fasoracetam.
Increasing Available Acetylcholine
Fasoracetam is a powerful cholinergic, significantly increasing the uptake of choline in the cortex and hippocampus. The brain uses the additional choline to produce more acetylcholine, the neurotransmitter most strongly associated with learning, memory, and overall cognition.
This cholinergic action, which is typical of piracetam, aniracetam, and other members of the racetam family of nootropics, can create a significant improvement in virtually all aspects of cognition. However, it can also lead to swift depletion of the brain’s choline resources, which can result in headache, brain fog, and low mood. This effect can be largely countered by taking supplemental choline as part of any racetam stack.