Fasoracetam

A newer racetam that uniquely upregulates GABA-B receptors, making it potentially useful for people who have developed tolerance to GABAergic substances like Phenibut or benzodiazepines. It also enhances glutamate and acetylcholine signaling. Being studied in clinical trials for ADHD in adolescents with specific glutamate receptor gene mutations.

Dosage

Standard: 20-100 mg sublingually or orally, 1-3 times daily. Many users find 20-40 mg effective. Clinical trials for ADHD used 100-400 mg twice daily.

Dosages shown are for research reference only. Always consult a qualified healthcare provider.

Half-Life

1.5-2.5 hours

Administration

Oral or sublingual. Sublingual may provide better absorption.

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Mechanism of Action

Fasoracetam upregulates GABA-B receptor (GABA-B1/GABA-B2 heterodimer) expression and function, which is unique among racetams — this receptor upregulation is potentially beneficial for restoring GABAergic sensitivity after prolonged benzodiazepine or phenibut use. It enhances group II metabotropic glutamate receptor (mGluR2/mGluR3) signaling, which modulates presynaptic glutamate release and reduces excitotoxicity. Fasoracetam increases acetylcholine release in the cerebral cortex via modulation of choline acetyltransferase activity and vesicular acetylcholine transporter function. It may also modulate the glutamatergic system through mGluR5. The combination of GABAergic (GABA-B-mediated inhibition), glutamatergic (mGluR modulation), and cholinergic enhancement provides anxiolytic effects alongside cognitive enhancement. Clinical trials focus on ADHD patients with GRM (glutamate receptor) gene variants.

Regulatory Status

Investigational drug — in Phase 2/3 clinical trials for ADHD (Aevi Technologies/Neurofix). Available as a research compound.

Risks & Safety

Common

Headache, fatigue, mild digestive discomfort.

Serious

Limited long-term human safety data.

Rare

Low mood, brain fog, loss of motivation at very high doses.

Compare Fasoracetam With

Research Papers

5
Fasoracetam. LAM 105, NS 105.

Published: August 22, 1999

AI Summary

Abstract too short to summarize.

Fasoracetam in adolescents with ADHD and glutamatergic gene network variants disrupting mGluR neurotransmitter signaling.

Published: January 15, 2018

AI Summary

NFC-1 treatment resulted in significant improvement. Parental Vanderbilt scores showed significant improvement for subjects with mGluR Tier 1 variants (P < 0.035).

Beyond stimulants: a systematic review of randomised controlled trials assessing novel compounds for ADHD.

Published: July 25, 2019

AI Summary

Given the high effect size found in RCTs of stimulants in terms of efficacy on ADHD core symptoms, it is unlikely that these novel agents will show better efficacy than stimulants, at the group level. However, they may offer comparable or better tolerability.

A Study of Fasoracetam's Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical.

Published: May 18, 2017

AI Summary

Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C.

Molecular authentication, metabolite profiling and in silico-in vitro cytotoxicity screening of endophytic Penicillium ramusculum from Withania somnifera for breast cancer therapeutics.

Published: March 8, 2024

AI Summary

Pharmacokinetic profiling revealed that Baptifoline, Odorinol, and Thyronine depicted an excellent therapeutic profile of druggability. These findings collectively substantiate the anticancer activity of bioactive metabolites synthesized by P. ramusculum SVWS3.

Frequently Asked Questions

What is Fasoracetam used for?

A newer racetam that uniquely upregulates GABA-B receptors, making it potentially useful for people who have developed tolerance to GABAergic substances like Phenibut or benzodiazepines. It also enhances glutamate and acetylcholine signaling. Being studied in clinical trials for ADHD in adolescents with specific glutamate receptor gene mutations.

What are the side effects of Fasoracetam?

Common: Headache, fatigue, mild digestive discomfort. Serious: Limited long-term human safety data. Rare: Low mood, brain fog, loss of motivation at very high doses.

How is Fasoracetam administered?

Fasoracetam is administered via oral or sublingual. sublingual may provide better absorption..

What is the half-life of Fasoracetam?

The half-life of Fasoracetam is 1.5-2.5 hours.

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