F-Phenibut (Fluorophenibut): Potent GABAnergic Compound Analysis

F-Phenibut represents a fluorinated derivative of phenibut with 5-10 times greater potency than its parent compound. F-Phenibut functions as a potent GABA-B receptor agonist with a binding affinity of 6.0±0.4 nM, producing anxiolytic and cognitive effects through its primary action on GABA-B receptors and secondary influence on GABA-A receptor systems.

F-Phenibut features a strategically placed fluorine atom that enhances blood-brain barrier penetration, resulting in a rapid onset of 15-30 minutes and shorter 5-7 hour duration compared to standard phenibut. F-Phenibut has gained attention for its potential applications in anxiety reduction and cognitive enhancement.

F-Phenibut comes in various forms including powder and capsules, making F-Phenibut a versatile option for those seeking cognitive benefits while requiring smaller dosages than regular phenibut due to its enhanced potency.

What is F-Phenibut?

F-Phenibut (also known as 4-Fluorophenibut, Fluorophenibut, Fluorobut, Baflofen, and CGP-11130) is a derivative of the popular nootropic supplement Phenibut. It is chemically similar to Phenibut but with an added fluorine atom at the para position on the phenyl ring.

This small change in structure, adding a fluorine atom, significantly increases its potency as indicated by lower EC50 values compared to Phenibut, but detailed information on its pharmacokinetic profile, such as absorption and duration, requires further research.⁽¹⁾

F-Phenibut offers cognitive enhancement, including memory, attention, and problem-solving skills. Users often seek these benefits to improve daily tasks or academic performance.

F-Phenibut is available in various forms, including potent powder and capsules, making it a versatile option for individuals seeking a high-quality nootropic supplement.

However, it is important for users to obtain this product from reputable suppliers, be aware of its potential for abuse and addiction, and consider the implications of substance use.

Pros:

• More potent than regular Phenibut with a higher potency, requiring a smaller dose
• Improves mood and provides feelings of well-being
• Effective at reducing anxiety symptoms

Cons:

• Less studied than Phenibut, with potential risks and long-term effects being less understood
• Potential for abuse and withdrawal symptoms

Mechanism of Action

F-Phenibut (Fluorophenibut) has a specific mechanism of action primarily centered around its influence on the brain’s neurotransmitter systems.

F-Phenibut functions by targeting your brain’s GABA receptors, acting as a GABAergic agent. These are the same receptors affected by alcohol and benzodiazepines.

By binding to these sites, F-Phenibut acts as an inhibitory neurotransmitter, which can calm nervous activity. This action is crucial for achieving the desired cognitive enhancement.

Here’s a closer look at how F-Phenibut works in the brain:

1. GABA Receptor Agonist: The primary mechanism of action of F-Phenibut is its role as a GABA(B) receptor agonist. GABA (gamma-aminobutyric acid) is the primary inhibitory neurotransmitter in the central nervous system. By acting on GABA(B) receptors, F-Phenibut enhances the inhibitory effects of GABA, leading to decreased neuronal excitability.
2. Effects on Dopamine: Some studies indicate that F-Phenibut might also have an impact on dopamine levels, a neurotransmitter associated with reward and motivation, although this effect appears to be secondary to its action on GABA receptors.⁽²⁾
3. Impact on Neurotransmitter Balance: The activation of GABA(B) receptors by F-Phenibut can influence the balance of neurotransmitters in the brain, particularly those involved in stress, anxiety, and mood regulation. This results in an overall calming effect on the brain.
4. Effects on Calcium Channels: Like Phenibut, F-Phenibut may also have effects on voltage-dependent calcium channels, particularly those in the alpha-2-delta subunit. This action can contribute to its anxiolytic and possibly analgesic effects.
5. Increased Blood-Brain Barrier Penetration: Due to the addition of a fluorine atom, F-Phenibut is believed to cross the blood-brain barrier more efficiently than Phenibut, resulting in more pronounced effects on the central nervous system. This makes F-Phenibut an efficient GABA(B) receptor agonist.
6. Longer Duration of Action: F-Phenibut is believed to have a longer duration of action compared to Phenibut, although the exact reasons for this are not fully understood. This could be due to a more sustained binding to GABA(B) receptors or a slower metabolic breakdown.
7. Reduced Tolerance Development: There is some evidence to suggest that F-Phenibut may lead to less tolerance development compared to Phenibut, although this is subject to individual variation and requires more research.

Nootropic Benefits of F-Phenibut

As a potent GABA(B) receptor agonist, F-Phenibut (Fluorophenibut) offers potential benefits for cognitive function and mental health.

These nootropic benefits of F-Phenibut include the below.

1. Improved Cognitive Function

As a nootropic, F-Phenibut enhances cognitive functions such as memory, attention, and executive function, potentially by impacting neuronal excitability and synaptic plasticity.

2. Memory Enhancement

Some users report improvements in both short-term and long-term memory, likely due to the compound’s influence on GABA and dopamine receptors in the brain.

3. Enhanced GABA Receptor Activity

F-Phenibut acts as a potent GABA(B) receptor agonist, which means it influences the GABAergic system in the brain. This action can lead to improved inhibitory neurotransmission, which is crucial for maintaining a balanced central nervous system (CNS).

3. Anxiolytic Effects

F-Phenibut may exhibit anxiolytic properties, helping reduce symptoms of anxiety and stress. This makes it a potential alternative to traditional anxiolytics like benzodiazepines.⁽³⁾

4. Reduces Depression Symptoms

Some studies suggest that F-Phenibut helps alleviate symptoms of depression by modulating neurotransmitter activity in the brain.

5. Blood-Brain Barrier Penetration

Due to its chemical structure, F-Phenibut is believed to cross the blood-brain barrier more efficiently than Phenibut, leading to more pronounced and rapid effects.

6. Better Sleep Quality

By potentially improving sleep, F-Phenibut can contribute to better cognitive function, since adequate rest is crucial for memory consolidation and brain health.

7. Neuroprotection

There is some evidence to suggest that Phenibut derivatives have neuroprotective effects, although more research is needed to substantiate these claims for F-Phenibut specifically.⁽⁴⁾

Uses of F-Phenibut

F-Phenibut is known for its various uses, primarily associated with its action as a GABA(B) receptor agonist and its potential influence on the central nervous system.

Here are some of the key uses of F-Phenibut:

1. Anxiety Reduction: F-Phenibut is commonly used for its anxiolytic properties, helping people manage anxiety symptoms and stress.
2. Enhancement of Cognitive Functions: As a nootropic, F-Phenibut is believed to potentially improve cognitive functions such as memory, focus, and concentration, although more research is needed to fully understand these effects.
3. Mood Improvement: Users often report a mood-enhancing effect, which might be attributed to its action on neurotransmitter systems.
4. Sleep Aid: F-Phenibut may be used to promote better sleep quality, particularly in individuals who experience insomnia or disrupted sleep patterns.
5. Stress Reduction: The supplement is sometimes used to manage stress, thanks to its potential to regulate the nervous system’s response to stressors.
6. Potential Treatment for PTSD: Due to its calming effects, there is interest in exploring F-Phenibut’s potential as a treatment for conditions like post-traumatic stress disorder (PTSD), although clinical evidence is still limited.
7. Alleviation of Depression Symptoms: F-Phenibut helps reduce symptoms of depression, but this area requires more clinical research for confirmation.
8. Withdrawal Management: F-Phenibut is used to ease withdrawal symptoms from certain substances, owing to its neurological effects, but this should be approached with caution and professional guidance.
9. Neuroprotective Properties: There’s ongoing research into whether F-Phenibut has neuroprotective properties, which are beneficial in the treatment of neurodegenerative diseases.

Where to Buy F-Phenibut

Before purchasing F-Phenibut, it’s crucial to verify the credibility of online suppliers and vendors.

Look for vendors with positive reviews and a solid reputation in the community. Reviews reflect other customers’ experiences and can guide your decision-making process.

A reputable, worldwide company is Science.bio.

This website is transparent about their products and they provide detailed information on sourcing and manufacturing processes, with third-party testing and to-your-door shipping!

Bulk purchasing options are available for those who want to pay a lower overall price per bottle.

F-Phenibut Dosage

Understanding the correct F-Phenibut dosage is crucial when you’re using nootropics like F-Phenibut. For new users, starting with a low dose is wise.

This might range from 50 to 100 mg per day. Experienced users may consume up to 250 to 500 mg daily.

You should monitor your body’s response carefully.

Signs that you need an adjustment include nausea or unusual fatigue.

If these occur, reconsider your current dosage.

F-Phenibut Side Effects and Safety

F-Phenibut is typically well-tolerated when used responsibly and in the correct dosages.

However, like most nootropics, F-Phenibut has some common side effects, including:

• Headaches
• Nausea
• Gastrointestinal discomfort

These are typically short-lived and disappear after your body adjusts to F-Phenibut.

Recreational use can lead to adverse outcomes such as insomnia, nausea, and more severe neurological side effects, including potential suppression of neuronal excitability as indicated by its effects on GABAB-expressing neurons. These risks underscore why you should approach F-Phenibut with caution.⁽⁵⁾

Combining F-Phenibut with other substances, particularly central nervous system depressants like alcohol, benzodiazepines, and opiates, increases risks due to potential synergistic effects that can amplify sedation and respiratory depression.

Avoid these combinations to reduce health risks significantly.

Note: If you decide that tapering off is necessary, create a safe plan. Consult with healthcare professionals before starting this process.

Summary

Through this exploration of F-Phenibut, you’ve gained insight into its potential as a nootropic and its mechanism of action.

The balance of benefits and risks has been laid bare, offering you a comprehensive understanding of what F-Phenibut can do, how it works, and the safety considerations it entails.

Armed with knowledge about dosages, where to source it, and its possible side effects, you are now better equipped to make informed decisions regarding its use.

Your journey with F-Phenibut doesn’t end here. Should you decide to incorporate it into your regimen, proceed with caution and always prioritize your health.

Stay informed, stay safe, and take the next step in enhancing your cognitive function with confidence!

Keep in mind: F-Phenibut, like its parent compound Phenibut, is not approved for clinical use in several regions, including the United States, European Union, and Australia.

FAQs

1. Irie, Tomohiko et al. “F-phenibut (β-(4-Fluorophenyl)-GABA), a potent GABA_B receptor agonist, activates an outward-rectifying K⁺ current and suppresses the generation of action potentials in mouse cerebellar Purkinje cells.” European journal of pharmacology vol. 884 (2020): 173437. doi:10.1016/j.ejphar.2020.173437↩
2. Borodkina, L E et al. Eksperimental’naia i klinicheskaia farmakologiia vol. 72,1 (2009): 60-3.↩
3. Lapin, I. “Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.” CNS drug reviews vol. 7,4 (2001): 471-81. doi:10.1111/j.1527-3458.2001.tb00211.x↩
4. Kupats, Einars et al. “Mitochondrial-Protective Effects of R-Phenibut after Experimental Traumatic Brain Injury.” Oxidative medicine and cellular longevity vol. 2020 9364598. 21 Nov. 2020, doi:10.1155/2020/9364598↩
5. Kupats, Einars et al. “Safety and Tolerability of the Anxiolytic and Nootropic Drug Phenibut: A Systematic Review of Clinical Trials and Case Reports.” Pharmacopsychiatry vol. 53,5 (2020): 201-208. doi:10.1055/a-1151-5017↩