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Picamilon

picamilon

Picamilon (nicotinyl-y-aminobutyric acid) is a combination of vitamin B3 (niacin) and GABA that is capable of providing anxiolytic and vasodilatory effects.  First developed in the early 1970s in the Soviet Union, picamilon (alongside phenibut) is an “enhanced” form of GABA that is capable of crossing the blood brain barrier when taken as a supplement.

Inside the brain, picamilon is rapidly hydrolyzed into its constituent parts; niacin and GABA. Niacin helps to enhance brain blood flow through its vasodilatory properties while is an inhibitory neurotransmitter that provides a calming effect.

As with any nootropic that directly affects receptors, tolerance should be expected with prolonged use, picamilon is best cycled.

Virtually all of the research on Picamilon has been conducted in Russia and is only available in abstract form, as such It’s difficult to go into great depth. Many of the abstracts are not available in NCBI but have been archived by third party sites including the life extension foundation.

Other Names

4-(Pyridine-3-carbonylamino)butanoic acid , nicotinyl-y-aminobutyric acid, nicotinoyl-GABA, pycamilon, pikamilon, picamilone

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Important Information

Picamilon Dosage

The Russian drug encyclopedia RLSNET recommends 20-50mg taken 2-3 times per day for cerebrovascular purposes and up to 200mg-300mg per day for a 4-6 week period for calmative purposes (1). One study advised 60-120mg in 24 hours for modest depressive effects in the elderly (2) All of the Russian recommendations for picamilon have time frames attached to them, as such it’s probably best to view picamilon and a nootropic that should be cycled.  The effects of picamilon are felt around an hour after dosing.

Picamilon Nootropic Stack Advice

Picamilon’s mechanisms of action are though enhancing brain blood flow and increasing brain GABA concentrations. As covered in our nootropics stack guidelines it’s probably unwise to “stack” compounds that share too similar an effect. Phenibut and vinpocetine (being gabaeric and vasodilatory respectively) are very similar and probably shouldn’t be stacked with Picamilon. Anxiolytics that operate through different mechanisms such as magnesium, bacopa and aniracetam could be considered.

Another potential use for picamilon is to help take the “edge” off of a stimulant and enhance a “clean” feeling of energy (similar to the idea of a theanine and caffeine stack). A picamilon + stimulant such as caffeine or modafinil could be a powerful combination.

Relevant Articles

  1. Designing your own stack – 3 important guidelines.

Picamilon Absorption

In animal studies Picamilon has been found to cross the blood brain barrier (3). Peak blood concentrations are around 20 minutes after dosing (3). It’s often mentioned that picamilon is hydrolysed into its constituent parts GABA and Niacin once inside the brain, though research confirming this is unavailable.

Oral GABA supplements are thought to be poorly absorbed and don’t cross the blood brain barrier to any great degree. In animals radiolabel GABA wasn’t able to cross the BBB (4). However, there is clearly some degree of GABA absorption in the brain as it’s known to increase growth hormone release via neurological mechanisms (5)

In any event, the addition of Niacin to the GABA molecule to form picamilon ensures it crosses the blood brain barrier with greater efficacy than GABA alone.

Picamilon Benefits

Non-Muscular Relaxant

Picamilon is unique to most sedatives in that it specifically only seems to affect the brain and act in a non-sedative manner. Indeed a Russian study (abstract only available) comments that picamilon is recommended for sportsmen by causing relaxation without affecting muscle tissue (8) Another Russian review comments that “picamilon acts as a tranquilizer without the sedative component of myorelaxation” (2) A third Russian study comments that picamilon helps to support sporting activity under conditions of extreme stress (9).

Picamilon, Niacin and GABA molecules

Picamilon, Niacin and GABA molecules

Enhancing Brain Flood Flow

In Russia, picamilon is listed as a treatment for migrane, ischemia and cerebrovascular conditions (2). Picamilon is a vasodilator (14) and the niacin portion of picamilon is most likely responsible for these effects.  A study of 28 patients showed picamilon to be effective for the vast majority suffering with chronic cerebral insufficiency, (17)

Learning

One study involving rodents showed picamilon (56mg/KG) prevented electroshock related amnesia and improved water maze navigation when compared to piracetam (200mg/KG). A dose of 10mg/KG was also found effective at radial maze navigation (6).

Anti-Stress / Normalizing Effect

A translated Russian journal entry shows research conducted with picamilon and rodents placed under chronic stress (7).  To generate a stressful state the Jouvet method of stress generation was employed; this involves sleep deprivation by not allowing the rodents to drop into REM sleep.  This method is sometimes called the “flowerpot technique” and involves the animals being placed on a narrow circular platform surrounded by water.

In the event the animal drops off to sleep, they essentially fall into the water and re-awaken.  The animals become deprived of REM sleep and develop chronic stress as a result.

Flow

Flowerpot Test

This study divided 100 rodents into 5 groups;

  • Control,
  • Stress (sleep deprived group)
  • Stress + picamilon,
  • Stress + piracetam
  • Stress + B-44 (A novel gaba derivative).

After the 4 day period, animals brains were analysed for various biomarkers of stress including endogenous antioxidants (superoxide dismutase and catalase) and malonic dialdehyde (a marker of lipid peroxidation).  Study results below:

picamilon stress study

The authors found that stress increased lipid peroxidation (measured by MDA level) by 70% where endogenous antioxidants were significantly lowered.  Picamilon (results above) was found to be highly protective of stress related changes, researchers noted “the effect of picamilon was so strong that the parameters studied during stress were virtually identical with levels in the intact group.

Picamilon Mechanism Of Action

Picamilon is a combination of GABA (a neurotransmitter) and Niacin (a vasodilatory B Vitamin). It’s reasonable to assume that the effects of increased stress tolerance are related to GABA’s ability to reduce neuronal excitability and act as a sedative (10)(11).

Niacin is well known for it’s vasodilatory properties (12). Picamilon has been shown to increase cerebral bloodflow in animals, almost certainly due to the niacin present in the molecule (13). Further research confirms picamilon causes blood vessel dilatation and and increase in cortex blood flow in rabbits and rats.  (14)

Picamilon Safety

Picamilon seems relatively free of side effects in theraputic doses. Three available abstracts comment that human patients were free from side effects (15,16,17). The russian drug encyclopaedia lists nausea, headache, lightheadedness, and (paradoxically) anxiety and agitation and possible side effects. This nootropic is contraindicated in patients with kidney disease (2)

References:

1.  http://www.rlsnet.ru/tn_index_id_5545.htm

2.  http://www.lef.org/prod_hp/abstracts/picamilon.html#3

3.  http://www.ncbi.nlm.nih.gov/pubmed/1884802

4.  http://www.sciencedirect.com/science/article/pii/002839087190013X

5.  http://www.ncbi.nlm.nih.gov/pubmed/7419665

6.  http://link.springer.com/article/10.1007%2FBF02446941

7.  http://link.springer.com/article/10.1007%2FBF00839928#page-2

8.  http://www.lef.org/prod_hp/abstracts/picamilon.html#43

9.  http://www.lef.org/prod_hp/abstracts/picamilon.html#42

10. http://www.ncbi.nlm.nih.gov/pubmed/2884549

11. http://www.ncbi.nlm.nih.gov/pubmed/12467378

12. http://www.annualreviews.org/doi/abs/10.1146/annurev.pharmtox.48.113006.094746

13. http://www.ncbi.nlm.nih.gov/pubmed/2707413

14.   http://www.lef.org/prod_hp/abstracts/picamilon.html#10

15.   http://www.lef.org/prod_hp/abstracts/picamilon.html#38

16.   http://www.lef.org/prod_hp/abstracts/picamilon.html#41

17.   http://www.lef.org/prod_hp/abstracts/picamilon.html#29