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Phenibut

 

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Important Information:

Phenibut Dosage:

Consider 500mg for sleep enhancement purposes. Social anxiety may benefit from doses up to 1gram. Phenibut is gabaergic and it’s effects are dramatically amplified when consumed with alcohol and certain medications, including benzodiazapenes. We don’t recommend taking phenibut with other gabaergic drugs.

Phenibut Tolerance;

Daily / frequent use of phenibut will result in tolerance which causes more problems than it solves. As a rule of thumb, do not consume more than twice a week.

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Background:

Phenibut was developed in the 1960s in Russia. A quick search for phenibut in pubmed reveals a wealth of information, most all of Russian origin making it obvious that there is something of value that the Russians see in this molecule.

Phenibut is, normally, referencing a racemic mixture of r/s-3-phenyl-4-aminobutyric acid. Each enantiomer does not have the same binding potential, it has been found that the R-isomer was two times more potent, with regards to locomotor activity, antidepressant and pain effects [2]. On the surface, phenibut is resemblant of γ-Aminobutyric acid (GABA) with the exception of a phenyl group 2 carbons from the amino group. This additional phenyl not only lends itself to the name Phenibut but also serves to augment hydrophobicity making travel across the blood brain barrier (BBB) all the more favorable.

Phenibut’s Mode of action:

In general, Phenibut acts almost identical to GABA, with the exception of increased ability to cross over the BBB. Thus its effects are attributed to hyperpolarization (a more negative cell potential) of neurons with either GABA(A) or GABA(B) receptors. This is achieved, upon receptor binding, by activating an influx of Cl- ions into the neuron or by opening outflowing K+ ion channels which results in a net effect of either ceasing or making signal propagation more difficult.

 

With respect to its antidepressant and antinocioceptive (pain relief) effects Phenibut seems to work by acting at the GABA(B) receptor. As simultaneous administration receptor-selective antagonist (3-aminopropyl)(diethoxymethyl)phosphinic acid (CGP35348) extinguished those functions [2].

Phenibut Benefits:

In rat studies under conditions of cerebral ischemia, phenibut was found to be superior to piracetam in reducing amnesia, degree of circulation drop and improved spontaneous movement [6]. If the studies conclusions are correct, then this implies that phenibut must be doing something to effect vascular functions under low oxygen conditions, since neurons have very high metabolism, they are very prone to injury when deprived of oxygen, even for a brief time.

Furthermore, with regards to metabolism, phenibut has been shown to reduce damage to neuronal mitochondria, in environments of edema [3][4]. This benefit, at first, may not seem practical because how often are you expecting to have brain edema in your lifetime? hopefully none. However, if the importance of a constant stream of energy to appease the high energy demand of neurons is underlined, then one can see that any protection you can award your mitochondria is one of the best things you can do for your brain. If this study is true, and phenibut reduces mitochondrial damage, it must mean that something is being done by the molecule that isn’t normally available.

In other rat studies, phenibut displayed the ability to increase transcallosal potential amplitude, even after a single administration of phenibut. This is very interesting, considering what the corpus callosum is:

The corpus callosum is a bundle of neurons that connect the two hemispheres of the brain, since certain functions of the brain are dominant to one side the importance of this set of neurons becomes obvious [1].

Other info:

Phenibut has been found to have interesting effects pertaining to motion sickness. In rabbits, one study found that phenibut seemed to alter blood flow to areas of the brain that resulted in increased vestibular stability [6]. Now all of that language is there to say that the snail like (see figure below) thing in the inner ear that communicates information about how gravity is affecting you is more stable, which could reduce sensitivity in those who are prone to motion sickness, or at least their rabbits.

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Sources:

  1. http://www.ncbi.nlm.nih.gov/pubmed/19334513
  2. http://www.ncbi.nlm.nih.gov/pubmed/18275958
  3. http://www.ncbi.nlm.nih.gov/pubmed/8205040
  4. http://www.ncbi.nlm.nih.gov/pubmed/1804695
  5. http://www.ncbi.nlm.nih.gov/pubmed/1884788
  6. http://www.ncbi.nlm.nih.gov/pubmed/16878492

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Average rating:  
 1 reviews
by Phenibut on
Works Perfectly - Tolerance Sucks

Basically phenibut does everything it promised me, i sleep like a king, i'm not anxious with my friends (i have mild SA) and it helps with my occasional public speaking. I give it 10/5 for it's effectiveness!

Tolerance is the main reason I give this an overall 3/5. I find I get tolerant within days and am tempted to up the dose (I haven't yet).

I take 500mg twice per week, if I take any more than that I find it loses effectivness.