More and more people are asking about the Phenibut GABA connection. How does Phenibut affect your GABA receptors? What is GABA? If you’ve ever wondered about these questions, then this article has the answers for you.
We’ve answered some of the top questions about Phenibut and GABA in a way that (we hope) is easy to understand and also informative. As people around the world are beginning to understand the potential benefits of Phenibut, so more and more people are wondering about how it actually works. Phenibut is a potent GABA agonist that promotes calm and relaxation.
Phenibut and GABA are both known to improve relaxation and promote feelings of calmWhat Is GABA?
Gamma-Aminobutyric acid (GABA) is a hormone and a neurotransmitter in your body. It binds to receptors in your brain called GABA receptors. The effects of GABA are known as depressant effects because GABA reduces the signals from your Central Nervous System (CNS). GABA also has a very important role in regulating muscle tone in humans. [1]
Although it has depressive effects on your CNS, the subjective effects of GABA are the total opposite. GABA helps your mind and body to relax, and it is known to help counter the effects of stress. It also helps to regulate sleep and mood. GABA is the polar opposite to another neurotransmitter called glutamate, which is a stimulating hormone and strengthens signals from the CNS. The two neurotransmitters are highly regulated in your brain and body to maintain your health. [2]
Many substances use GABA receptors as their targets. Researchers and scientists have developed a number of chemical agents that activate GABA receptors. These substances are generally used as calming and anti-stress compounds, often with tranquilizing or sedative effects. Phenibut is a great example of a compound that was developed to promote calm and reduce stress by interacting with GABA receptors. [3]
How Does GABA Keep You Calm?
Research has shown that GABA has very important functions in your body and mind. Hence, the importance of the Phenibut GABA connection. There are two main types of GABA receptors: GABA-A and GABA-B receptors. There are also GABA-C receptors, but these are less prevalent and have fewer functions. The best studied receptors are the GABA-A receptors, which are known to be involved in relaxation and sedation, and also to have tranquilizing effects. [4]
When GABA or other substances (called GABA agonists) bind to GABA receptors, the receptor proteins change their structure. This structural change causes a cascade of biochemical reactions. The ultimate result of this chemical cascade is that signals from your central nervous system (CNS) are reduced. *Find out the difference between Phenibut HCl and Phenibut FAA!
Over-stimulation of the CNS is associated with stress and the fight-or-flight response. Glutamate is a substance that stimulates the CNS. GABA helps to counteract this through its depressive effects. By reducing the signals from the CNS, GABA promotes calm and relaxation. It is also useful in promoting healthy sleep and maintaining a healthy mood. [5]
How Effective are GABA Supplements?
GABA is such an important neurotransmitter and has such beneficial effects that many people have considered using it as a dietary supplement. Numerous pharmacological substances have been developed to mimic GABA’s effects in your brain. You can purchase GABA supplements in most health stores or from vendors online.
However, GABA supplements are actually not very effective, for a number of reasons. Firstly, your body is highly developed to reject excess GABA. As a result, GABA has a very low permeability across the blood-brain barrier. In fact, scientists have shown that as much as 80% of GABA is prevented from crossing the blood-brain barrier. [6] This means that you would need to take a very large quantity of GABA to actually feel any effects.
Furthermore, your body’s ability to reject GABA is around 16 times stronger than its ability to ‘accept’ GABA. In fact, your body has a specialized efflux system in place that is activated when it detects excess GABA. Once this is activated, your brain will not accept any more GABA. This is thought to be linked to the importance of maintaining homeostasis between GABA and glutamate in your brain. [7]
Therefore, GABA supplements are not considered to be very effective. However, scientists have long understood the importance of GABA receptors in managing symptoms of stress and helping to promote sleep. As a result, many different GABA agonists have been developed with better abilities to cross the blood-brain barrier than GABA supplements. These substances are able to activate GABA receptors in a similar way to GABA, but are much more potent and are often more specific as to which type of receptor they activate. [8]
Calmness and relaxation are important in our fast-paced societyHow Does Phenibut Affect GABA?
Phenibut has powerful effects on your GABA receptors. In fact, the effects of Phenibut and GABA are intertwined. Phenibut was initially developed in Russia as an anti-stress compound that would allow people to improve their focus and maintain applied mental activity. Phenibut is sometimes called a Nootropic compound because of its ability to influence learning, memory, and attention. [9]
Phenibut works by activating the GABA-B receptors. It acts primarily on GABA-B receptors, but also activates some GABA-A receptors. Phenibut is also thought to stimulate dopamine receptors and to reduce Beta-PEA activity. Phenibut has similar effects to baclofen and diazepam – both in terms of its mechanism of action and its subjective effects. [10]
Different compounds affect GABA receptors in different ways. Substances that positively influence GABA receptors are called GABA agonists. This helps to explain the Phenibut GABA connection. For more information about Phenibut, take a read through our Top 20 Questions about Phenibut FAQ!!
Some GABA-A agonists include:
- Alcohol
Alcohol is a powerful GABA-A agonist - Baicalin
- Benzodiazepines
- Barbiturates
- GABA
- Kava
- Phenibut
- Picamilon
- Valerian [11]
Some GABA-B agonists include:
- Baclofen
- GABA
- Gamma-Hydroxybutyric acid (GHB)
- Phenibut
- Picamilon [12]
What are Other Supplements that Affect GABA?
1. L-Theanine
Liftmode’s L-Theanine, 99% Purity 5 GramsL-Theanine is a constituent of tea and is also found in some species of mushrooms. L-Theanine is a potent relaxing and calming supplement of natural origins. It was originally extracted from tea plants but is now produced in laboratories.
L-Theanine has numerous benefits, which you can read about in our article on the Top 6 Benefits of L-Theanine. These include the ability to promote a calm, relaxed mood; to reduce stress; to help improve sleep quality; and to promote a healthy state of mind.
Furthermore, L-Theanine has a great synergistic relationship with caffeine. Together, the two substances boost mental alertness and focus more than either alone. L-Theanine also helps to reduce some of the negative effects of caffeine, such as headaches and raised blood pressure.
L-Theanine acts on GABA indirectly, by increasing the levels of GABA in your brain. Most GABA agonists work directly on GABA receptors. L-Theanine, however, simply promotes the production of extra GABA in your brain. As a result, the effects are calming and relaxing. L-Theanine also stimulates production of serotonin and dopamine. [13]
2. Magnolia Bark Extract
Liftmode’s magnolia bark extract: 99% purityMagnolia is a tree that grows in Asia. The bark has been used in Traditional Chinese Medicine for hundreds of years. In the past, Magnolia Bark was used against wind-stroke, cold, headaches, qi issues, blood impediments, and to treat dead muscles. Today, Magnolia Bark Extract can be purchased online as a dietary supplement to improve relaxation and promote calm. [14]
Scientists have found that Magnolia Bark Extract is especially effective at reducing stress and promoting relaxation because of its interactions with GABA receptors. Magnolol is one of the main actives chemical constituents of Magnolia Bark Extract. Researchers have found that Magnolol is great at activating GABA-A receptors. [15]
3. Oleamide
Liftmode’s Oleamide: 99%+ purityOleamide is a derivative of oleic acid – found in high concentrations in olive oil. Oleamide is produced naturally in your brain. It has potent calming effects and is wonderful at promoting relaxation. Oleamide is used by your brain to help promote healthy sleep. In fact, Oleamide concentrations are known to increase by 3-4 fold after just a few hours of lack of sleep. [16]
Oleamide has interesting effects on the GABA receptors in your brain. Oleamide doesn’t seem to interact directly with GABA receptors, nor does it stimulate the production of extra GABA. Oleamide’s method of action is to increase GABA signaling. When GABA or another substance binds to a GABA receptor, a signal is sent through your Central Nervous System. GABA is thought to increase the signal transduction, therefore improving the action of the GABA system. [17]
4. Baicalin
Baicalin from LIftmode, 98+% purityBaicalin is an active compound that is found in the Blue Skullcap plant species. It was originally used in Traditional Chinese Medicine to promote vitality and produce relaxation. In modern times, Baicalin has been researched for numerous benefits. These benefits may include pain relief, producing a calm mental state, powerful anti-inflammatory effects, and antioxidant support. [18]
Studies have shown that Baicalin activates GABA-A receptors in a similar way to alcohol and benzodiazepines. However, Baicalin has specific binding capabilities that allow it to produce pain-relieving effects without sedation or loss of motor-coordination. Furthermore, researchers have found that Baicalin may be able to produce feelings of well-being and to support a healthy mood. [19]
Can You Take Too Much GABA?
The GABA hormone is not well absorbed by your body and does not effectively cross the blood-brain barrier. As a result, if you want to feel effects from using GABA as a dietary supplement, you’ll need to take excessive amounts. Your body has highly effective mechanisms for eliminating excess GABA. There are currently very few side effects associated with taking GABA as a dietary supplement, even at high doses. [20]
Side effects from GABA usually come from interactions between various substances. Since many substances and supplements activate your GABA receptors, it is quite possible to take two substances at the same time that affect the GABA system. This can cause dangerous interactions through overstimulation of the GABA receptors.
GABA receptors have a depressive effect on your central nervous system. They reduce the electrochemical signals flowing through neurons in your brain. Overstimulation of GABA receptors can therefore be very serious. It is not recommended to use two substances that activate GABA receptors at the same time.
Symptoms of over-stimulation of GABA receptors can include:
One of the top benefits of Phenibut is to promote healthy sleep- Excessive tiredness
- Loss of motor-coordination
- Dizziness
- Nausea
- Loss of consciousness
- Weak breathing / Respiratory failure [21]
To prevent the possibility of experiencing these adverse effects, simply avoid using multiple substances that affect GABA at the same time. Additionally, do not exceed the recommended dosages for GABA substances.
Conclusion: The Phenibut GABA Connection
In conclusion, GABA is a natural hormone and neurotransmitter used to regulate signals in your central nervous system. It has depressive effects on the CNS. Its polar opposite is glutamate – a stimulating neurotransmitter.
GABA supplements are somewhat ineffective due to their inability to cross the blood-brain barrier, as well as your body’s natural efflux system for excess GABA. Researchers have developed a number of substances that work in a similar way to GABA and activate various GABA receptor subtypes.
An example of such a substance is Phenibut – a Russian developed compound aimed at promoting calm and reducing stress, while maintaining mental focus and attention. Phenibut may also be associated with improved learning and memory, and is sometimes referred to as a Nootropic substance. People online are searching for the Phenibut GABA connection.
There are also a number of naturally-derived supplements that activate GABA receptors. Examples include L-Theanine, Magnolia Bark, Oleamide, and Baicalin. These are all available for purchase online.
Taking multiple substances that activate GABA receptors at the same time can be dangerous and is not recommended. Interactions between GABA-agonists can cause overstimulation of GABA receptors and excessive depression of CNS signals. Do not exceed the recommended dosage for substances that affect GABA receptors.
Phenibut and GABA are great at helping to maintain a calm, relaxed state of mindReferences:
[1] M Watanabe et al., “GABA and GABA Receptors in the Central Nervous System and Other Organs” International Review of Cytology, Volume 213, 2002, Pages 1–47, A Survey of Cell Biology
[2] “GABA”, Examine.com, accessed May 16, 2017
[3] EA Ziablintseva, IV Pavlova, “[Influence of GABA agonist phenibut on the neuronal activity and interaction in hippocampus and neocortex in emotionally negative situations]”, Ross Fiziol Zh Im I M Sechenova. 2009 Sep;95(9):907-18.
[4] RG Paredes, A Agmo, “GABA and behavior: the role of receptor subtypes”, Neurosci Biobehav Rev. 1992 Summer;16(2):145-70
[5] F Petty, “GABA and mood disorders: a brief review and hypothesis”, J Affect Disord. 1995 Aug 18;34(4):275-81.
[6] H Al-Sarraf, “Transport of 14C-gamma-aminobutyric acid into brain, cerebrospinal fluid and choroid plexus in neonatal and adult rats”, Brain Res Dev Brain Res. 2002 Dec 15;139(2):121-9.
[7] OA Petroff, “GABA and glutamate in the human brain”, Neuroscientist. 2002 Dec;8(6):562-73.
[8] G Bartholini, “GABA receptor agonists: pharmacological spectrum and therapeutic actions”, Med Res Rev. 1985 Jan-Mar;5(1):55-75.
[9] GI Shul'gina, EA Ziablitseva, “[Effect of the GABA derivative phenibut on learning]”, Vestn Ross Akad Med Nauk. 2005;(2):35-40.
[10] I Lapin, “Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug”, CNS Drug Rev. 2001 Winter;7(4):471-81.
[11] P Krogsgaard-Larsen et al., “Specific GABA(A) agonists and partial agonists”, Chem Rec. 2002;2(6):419-30.
[12] “GABA Receptor Agonist”, Wikipedia.org: The Free Encyclopedia, accessed May 16, 2017
[13] PJ Nathan et al., “The neuropharmacology of L-theanine(N-ethyl-L-glutamine): a possible neuroprotective and cognitive enhancing agent”, J Herb Pharmacother. 2006;6(2):21-30.
[14] “Magnolia officinalis”, Examine.com, accessed May 16, 2017
[15] CR Chen et al., “Magnolol, a major bioactive constituent of the bark of Magnolia officinalis, induces sleep via the benzodiazepine site of GABA(A) receptor in mice”, Neuropharmacology. 2012 Nov;63(6):1191-9
[16] “Oleamide”, Examine.com, accessed May 16, 2017
[17] CS Yost et al., “Oleamide potentiates benzodiazepine-sensitive gamma-aminobutyric acid receptor activity but does not alter minimum alveolar anesthetic concentration”, Anesth Analg. 1998 Jun;86(6):1294-300.
[18] “Scutellaria Baicalensis”, Examine.com, accessed May 16, 2017
[19] F Wang et al., “GABA A receptor subtype selectivity underlying selective anxiolytic effect of Baicalin.” Neuropharmacology. 2008 Dec;55(7):1231-7
[20] “GABA”, WebMD.com, accessed May 16, 2017
[21] RW Olsen, “GABA-drug interactions”, Prog Drug Res. 1987;31:223-41.
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