Nootropics Review: Gerovital (GH-3)

Gerovital is a nootropic made by Dr. Ana Aslan in Romania in the 1940s. Around that time, Aslan had been administering a procaine – an anesthetic to patients suffering from arthritis so they can achieve joint pain relief. The majority of her patients ended up with enhanced memory, decreased depression, improved skin tone, more energy, hair color restoration, and overall well-being. These significant results allowed her to conduct further studies to test out effects of procaine to individuals [1].

Gerovital (GH-3) Aslan found that by incorporation benzoic acid as a preservative and potassium metabisulfite as an anti-Oxidant, the molecule of procaine became balanced, and the procaine effects were even more dramatic. She named her enhanced procaine version as “Gerovital” [2].

Gerovital is one of the many widely known rejuvenation products in the globe today. The nootropic is said to provide a potent long-acting anti-depressant properties. Aslan’s test findings have been met with heavy skepticism, and further research outside Aslan’s lab received yielded mixed results [1] [2].

Inhibition of MAO

Gerovital has been proven to hinder MAO (monoamine oxidase); an enzyme found within the brain. MAO is primarily responsible for breaking down the neurotransmitter such as that of serotonin, norepinephrine, and dopamine. As individuals become older, the activity of MAO increases, causing a breakdown of these neurotransmitters. Dopamine, norepinephrine, and serotonin are responsible for feeling of calmness and pleasure. Individuals are taking in the nootropic report of enhanced energy levels, awareness, and mood. Such effects may be due to the inhibition of the MAO [2] [3].

Research Studies

A single study indicated that procaine enhanced the use of oxygen within the brains of older rodents to levels equivalent to that of younger rats. This suggests that this could be another approach that Gerovital can achieve its effects [4].

Gerovital has been given approval by the Romanian government for treating the body’s aging effects. These could include neuralgia, atherosclerosis, neuritis, arthritis, and others [5].

Recent clinical studies reported Gerovitals effects in a varying medical conditions, which include mental retardation, Alzheimer’s, and Parkinson’s disease. Multiple studies conducted compared the effectiveness of the nootropic to Piracetam, leading to similar improvements within the central nervous system processes. Another study led to further improvements in cognitive function when Piracetam was mixed with another drug, Aslavital [1] [6].

There have been other studies that failed to carry out similar findings of the nootropic. The majority of these studies was claiming Gerovital to be false utilized Procaine instead of the actual Gerovital preparation. Researchers believe that Procaine has similar properties to Gerovital. But developers of the nootropic claim the ingredient traces are essential [7].

Side Effects:

There have been no reports of significant negative effects of Gerovital except for very rare allergic reactions [1].

Drug Dosage

A Gerovital tablet can be taken once a day for 25 days. No tablets are ingested for a period of five days prior to the start of another round. Via injectable, the nootropic can be administered once every third day of the month then resting for one prior to the next round. Such complex plan intake was made by Aslan to let the enzymes restore the Procaine breakdown, while desensitizing the Procaine effects. The schedule may be present a challenge for patients to follow. One or two weekly injections on a consistent basis offer an equivalent effect [8].

Purchase

In the United States, Gerovital can only be bought in Nevada. It’s typically available over-the-counter in Romania, in the majority of European countries, and in Mexico [7].

References:

  1. http://www.smart-publications.com/books/full-text/smart-drugs-and-nutrients/smart-drugs-and-nutrients-sec-5/smart-drugs-and-nutrients-sec5-gerovital-gh-3
  2. http://www.ageless.co.za/procaine.htm
  3. http://www.emaxhealth.com/1275/banned-antiaging-drug-gerovital-h3-makes-comeback
  4. http://books.google.com.pk/books?id=UKgfDsRffnkC&pg=PA371&lpg=PA371&dq=procaine+enhanced+the+use+of+oxygen&source=bl&ots=GYC5Jor3wD&sig=UANj8dR0ckFYrFPdY6xJItyGLtk&hl=en&sa=X&ei=08FTVIu8BdbsaPGcgfAH&ved=0CB0Q6AEwAA#v=onepage&q=procaine%20enhanced%20the%20use%20of%20oxygen&f=false
  5. http://intelegen.com/nutrients/dmae_and_paba_an_alternative_to.htm
  6. http://www.zalmo.com/scientificstudies.pdf
  7. http://en.wikipedia.org/wiki/Gerovital
  8. http://www.drugs.com/npp/kh-3.html

Nootropics Review: CILTEP

CILTEP is a nootropic and supplement made to enhance and maintain brain capabilities in terms of motivation, memory, and concentration. It’s a new nootropic made from a mixture of forskolin and artichoke extract, and it functions in conjunction with choline-enhancing nootropic stacks.

CILTEP basically stands for Chemically Induced Long-Term Potentiation. It enhances learning and memory by optimizing and giving support to the levels of intracellular second messengers [1].

Benefits and Targeted Users

CILTEPMost users say the nootropic creates a potent effect similar to that of Modafinil, another known nootropic. CILTEP works ideally for individuals who are struggling to learn new content, and concentrating on a series of tasks that can last for several hours.

CILTEP processes are precious to nootropic users for a number of reasons. It has a powerful and positive effect in memory. Since long-term potentiation aids in our ability to utilize and store new information, it can be useful for studying and learning a new set of skills. Another positive effect of the nootropic is its amplifying activity of neurotransmitters such as that of dopamine, and acetylcholine. This leads to a significant improvement in cognition and overall learning speed.

Certain individuals may look into CILTEP as a way of enhancing athletic capabilities since it also improves particular sensitivity in some hormones. This could be useful in workouts and recovery time by biologically manipulating the chemistry of the body [2] [3].

Stack Ingredients

An interesting aspect of the CILTEP stack is that you don’t have to utilize certain ingredients in order for it to remain useful or for it to work. The mechanisms of CILTEP happens with synergy of several pharmacological chemical classes. — each consisting of a factor in aiding the other [4].

cAMP Increase

Typically, the CILTEP effects are made by spiking the cyclic adenosine monophosphate levels, or cAMP. cAMP is a basically a molecule that conducts second messaging, which involves signal transmission from the outer and internal cellular parts. In a precise manner, cAMP lets certain hormones (glucagon and adrenaline for instance), to influence their mechanisms on cells and triggering protein kinases. When you utilize more of it, the neurotransmitters efficiently function since their signals on the cells act proficiently [5].

PDE4 Inhibitor

Increasing cAMP directly may be the most limited flexibility of the CILTEP equation since forskolin is utilized. But a significant factor responsible for increasing cAMP is the inhibition of PDE4, a chemical largely responsible for its natural breakdown. Since there is a plethora of chemicals that inhibit PDE4, it’s deemed to be an all-around substance within the stack.

One notable option is Rolipram, an unpopular Racetam drug that has been utilized to inhibit PDE4. It’s rarely used in practice due to its side effects, among them being vomiting and nausea.

The PDE4 inhibiting properties from CILTEP is sourced from an artichoke extract in luteolin form. Such substance functions as an immunity booster and an anti-oxidant aside from its inhibition characteristics [6] [7].

CILTEP Sources and Effects

The contents required for CILTEP are easy to find. They can be selected from a shop or ordered via the internet in the form of powder or capsules. No standard dosages are indicated for each stack part, but it’s advisable to take a standard dose per ingredient to gain the appropriate CILTEP effect. It can take as long as a week to feel its effects.

Side effects of the nootropic are minimal since it’s practically safe to slightly increase cAMP levels. It’s important to take note that PDE4 inhibitors are notorious for causing nausea at high concentrations.

References:

  1. http://www.ncbi.nlm.nih.gov/pubmed/16672292
  2. http://www.powdercity.com/pages/artichoke-extract-forskolin-ciltep-stack
  3. http://nootriment.com/ciltep-stack/
  4. http://www.smarternootropics.com/2014/03/ciltep-stack-review-a-week-with-ciltep/
  5. http://www.ncbi.nlm.nih.gov/pubmed/20969573
  6. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2704616/
  7. http://www.ncbi.nlm.nih.gov/pubmed/9844008

Nootropic Review: Selank

Selank is an anxiolytic heptapeptide and a nootropic made by the Institute of Molecular Genetics of the Russian Academy of Sciences. It has been widely considered as a nootropic with anxiolytic effects. Selank is a synthetically analog of the peptide Tuftsin. It’s known for enhancing and altering the immune system in a positive manner. This have led the nootropic to be classified under the immunomodulatory category.

Selank

Semax, along with another heptapeptide nootropic, was made by researchers at the Molecular Genetics of the Russian Academy of Sciences. The substance is very much related to Selank and has been approved for use in humans in Russia and Ukraine. A number of reports from users and researchers showed that Selank is far more efficient choice than Semax. The nootropic, however, recently wrapped up the third stage of clinical trials in Russia. It’s now waiting a green light for public use [1] [2].

Dosages

Selank dosageIn general, a 250 to 500 mg of the drug should be taken at once or twice daily. Selank isn’t bio-available orally since it’s a peptide that is hydrolyzed and broken down into amino acids within the gut. As a result, both methods of intake are either through subcutaneous injection or intranasal. If you happen to have purchased freeze-dried Selank powder, it should remain stable for three months although it’s recommended to store it in the fridge as much as possible.

Meanwhile, a lyophilized Selank will entail a reconstitution with bacteriostatic water prior to intranasal or subcutaneous injection [3].

Mechanism

From a pharmacological point of view, the nootropic mimics a majority of its results from Tuftsin – that is a peptide where it’s sourced upon. Such effects involve balancing T-helper cells and a modulation expression of the Interleukin-6.

Furthermore, there’s increasing evidence suggesting Selank may be able to modulate the expression of the neurotropic factor.

Selank’s action processes are believed to be related to serotonin increase. Serotonin is primarily responsible for influencing a person’s appetite, positive mood, and regulation of the wake and sleep cycle. It’s also proven that a state lacking serotonin can lead to painful sleep, depression, and lack of hunger.

A study done on mice showed the Selank effects on monomines and their metabolites. It showcased a significant difference in dopamine, norepinephrine, and serotonin content as well as levels in the frontal cortex, hippocampus, and hypothalamus. Additional research supports Selank’s serotonin-increasing capability.

Selank and Tuftsin were also indicated to provide serotonin levels even though rodents were pre-tested with a serotonin synthesis inhibitor, p-chlorophenylalanine. Metabolism of serotonin was improved within half an hour of nootropic administration while Tuftsin remained incapable of raising 5-HIT levels.

Rodents who were exposed to 6-hydroxydopamine, a neurotoxin that destroys the catecholaminergic system, had their cognition processes restored via Selank [4] [5].

Benefits

A mice study that were purposely bred to suffer depression showed the nootropic’s capability in fighting anhedonia and bring back pleasure-seeking behavior. Selank administration led to an increase in sucrose content and less immobility during a forced swim test.

A study that involved 62 patients with a General Anxiety Disorder (GAD) wanted to compare the nootropic to benzodiazepine. 30 patients were given a Selank treatment while the remaining 32 had benzodiazepines. Surprisingly, the effectiveness of both drugs were strikingly similar, but scientists found that the nootropic possessed anti-fatigue effects. Complete study details were hard to extract since it was experimented in Russia, and a sole abstract only indexed by PubMed.

Another study experimented with the immunomodulatory effects of the nootropic given by the fact that its peptide relative Tuftsin has an immune function capability. Selank was given to patients suffering from GAD for two weeks, after which, it was observed Selank have the suppressed depression in patients while leaving healthy participants unaffected. T-helper cells have been modulated with patients who have GAD [6].

Cognitive Enhancing Properties

A study performed on an animal compared Selank to a saline placebo during a food-reward test that featured memory and learning. While certain study details remain unclear, since the test was done in Russia, scientists concluded that the nootropic enhanced memory consolidation. This mainly occurred via an increase in serotonin.

A study conducted in adult rats showcased Selank to compensate hypoxia-induced cognitive deficit while lowering noradrenaline and serotonin levels [6] [7].

 References:

  1. http://en.wikipedia.org/wiki/Selank
  2. http://nootropicsupplementreview.com/selank
  3. http://www.ironmagazine.com/2012/nootropics-selank-peptide-explained
  4. http://www.ncbi.nlm.nih.gov/pubmed/11550013
  5. http://www.ncbi.nlm.nih.gov/pubmed/18454096
  6. http://www.smarternootropics.com/selank
  7. http://www.europsy-journal.com/article/S0924-9338%2812%2975281-1/abstract

Nootropic Review: Vitamin B6

Vitamin-B6Vitamin B6, in a number of forms, is a water-soluble vitamin and a natural nootropic found in a wide range of foods [1]. It plays a significant role in more than one hundred enzyme mechanisms associated with lipids, amino acids, neurotransmitters, and carbohydrate metabolism. Its properties are linked to many health benefits [2]. Furthermore, it is constant found in meats, non-citrus fruits, and vegetables. The nootropic is also found in a number of multivitamins, but it can also be utilized as a separate dietary supplement [3].

Mechanisms

The tone of  action of  Vitamin B6, in terms of nootropic qualities, entails some discussion. The nootropics so widely availability in the body’s functions that extract a correlation between Vitamin B6 intake and specific treatment of a particular condition has been nothing but a challenge [4].

A general scientific theory is that, Vitamin B6, often working hand in hand with other B Vitamins can minimize brain atrophy and cognition impairment by reducing homocysteine levels within the blood. Demonstration of studies indicates that while ingesting Vitamin B6 and other vitamins can lessen homocysteine levels and reduce the chances of brain atrophy, it’s not effective in curbing or curing impaired cognition [5] [6].

Benefits

With Vitamin B6 being involved in a number of enzyme reaction, advantages of ingesting the nootropic frequently visible in a wide range of health concerns. Furthermore, it is safe in normalization of  homocysteine level and slowing the process of cognitive degeneration to curb cardiovascular problems. It has been indicated to lessen colorectal cancer risks in a study involving postmenopausal women while normalizing blood sugar levels, and treating nausea. There are plenty of other advantages and application with the nootropic, both for health and in treating particular developed conditions [7].

Dosages

Vitamin-B6-DosageFor the majority of adults, the recommended daily intake of Vitamin B6 is at 1.3 mg [1]. Such amount can easily be taken from a healthy and balanced diet which include legumes, meat, whole grain, and poultry [7].Taking a 100 mg of the nootropic daily is considered to be safe. No adverse effects have been observed when taking 200 mg of Vitamin B6 daily [8].

Toxicity Reports

Since Vitamin B6 is a passively delivered, potential toxic dosages can be absorbed. Repetitive high dosages can lead to nerve damage, skin lesions, ataxia, and sensitivity to light. At the same time, deficiency of Vitamin B6 can also possess a number of adverse effects which include confusion, mouth sores, depression, and less immune system efficiency to fighting off infections [9].

References:

  1. http://www.nlm.nih.gov/medlineplus/ency/article/002402.htm
  2. http://en.wikipedia.org/wiki/Vitamin_B6
  3. http://www.mayoclinic.org/drugs-supplements/vitamin-b6/background/hrb-20058788
  4. http://www.nutritionj.com/content/5/1/6
  5. http://www.ncbi.nlm.nih.gov/pubmed/17848650
  6. http://www.ncbi.nlm.nih.gov/pubmed/20838622
  7. http://www.drweil.com/drw/u/ART02763/vitamin-b6.html
  8. http://www.ncbi.nlm.nih.gov/pubmed/16320662
  9. http://ods.od.nih.gov/factsheets/VitaminB6-HealthProfessional

Nootropic Review: Pyritinol

Pyritinol is a nootropic that has been patented by Merck in 1961. It’s recognized to be one of the oldest nootropics still being used today. Pyritinol generated a number published research in 1980s and 1990s during its early study period, and this is likely due to its wide number of uses, efficiency, and safety of the nootropic. The majority of the study done on the drug has been published in a number of Czech, Swiss, German, French, and British journals [1].

The nootropic is virtually not popular in the United States and has been ignored by the FDA and AMA. Pyritinol is also named as pyridoxine disulfide and Pyrithioxine [2] [3]. The nootropic’s molecule involves two pyridoxine sulfide molecules conjugated to create two sulfur atoms [3]. The drug has been widely used to enhance memory and to treat individuals with learning disorders, dementia, and rheumatoid arthritis [2]. Furthermore, Pyritinol has been classified as nootropic since the 1990s [1].

Pyritinol

Dosages of Pyritinol

The half-life of the nootropic is around two and a half hours. Most common daily intake are within the 400 to 600 mg per day although it’s still no unusual to take in 100 mg or as much 1,200 mg daily. The drug is frequently sold in tablet form with labels that indicate ingesting the supplement with food. An average lethal dosage for oral intake is around 300 mg per kg for mice, 980 mg per kg for rats, and up t0 3,200 mg per kg for rabbits [4] [5].

Mechanisms of Pyritinol

Pyritinol facilitates more blood flow to the cerebrum of the brain via nerve cell enhancement. It’s also capable of moving intracellular choline from the choline kinase pathway to synthesize Acetylcholine, a known neurotransmitter. Acetylcholine hosts a number of functions in the nervous system as well as memory retention, muscle movement, and alertness sustainability [6].

Observed Benefits

The nootropic was utilized in France as a modifying drug that interrupts the progress of rheumatoid arthritis. It’s also capable of treating cognitive disorders by increasing the functions of the brain and learning capabilities [7] [8].

A study that involved 12 volunteers compared performance on a number of psychological tests found that subjects provided with Pyritinol doses showed enhance performance on a choice reaction time experiment to an extended degree than those taking a placebo. However, memory tests didn’t offer big differences in the performance of both groups [5].

A small group study gave support to a theory that Pyritinol doses taken during alcohol intake may lessen hangover-related symptoms [2].

Toxicity Issues

Pyritinol has a reputation for being safe. But in small and reported cases, the nootropic may be responsible for cholestatic hepatitis [9]. A study that compared the drug’s effectiveness with that of Auranofin (an anti-rheumatic drug) noted serious muscle and gastrointestinal effects in patients although such effects also surfaced in users of Auranofin as well [10].

References:

  1. http://en.wikipedia.org/wiki/Pyritinol
  2. http://examine.com/supplements/Pyritinol/#ref2
  3. http://nootriment.com/pyritinol
  4. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC381054
  5. http://www.ncbi.nlm.nih.gov/pubmed/2135070
  6. http://www.smarternootropics.com/table-of-contents/pyritinol
  7. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC381054
  8. http://www.ncbi.nlm.nih.gov/pubmed/23120794
  9. http://www.ncbi.nlm.nih.gov/pubmed/15001508
  10. http://www.ncbi.nlm.nih.gov/pubmed/8495257

Nootropc Review: Coluracetam

Being one of the new members of the Racetam family, Coluracetam made its first registration with PubChem back in 2005 via the Mitsubishi Tanabe Pharma Corporation, which was given to Brain cells Inc.later. Brain cells did a majority of testing on the nootropic including its Phase 2A trials, which wrapped up in 2010 for treating Major Depressive Disorder with Generalized Anxiety Disorder. No significant results were shown for individuals possessing one of the two conditions [1] [2] .

Mechanism of Coluracetam

Coluracetam structureColuracetam seems to have completely defined processes; the first involving increase affinity choline uptake and the potentiation of AMPA. As in cases with a few Racetam members, the nootropic has been proven to facilitate AMAP potentiation, which is known to enhance memory, learning, and wakefulness [3].

What’s particularly interesting with Coluracetam is its functionality in terms of high-affinity choline uptake. Choline uptake plays a significant role in the synthesis mechanism of Acetylcholine within the brain by functioning as “rate limiter.” The step of rate limiting gives the brain a chance to convert Choline into Acetylcholine within the neuron. With increasing choline uptake, the mind is ready to convert the choline into Acetylcholine. By enhancing the capability of converting the choline to Acetylcholine, in theory, it should enhance alertness, attention, and memory in humans [4].

Notable Benefits

The initial observed benefit of Coluracetam is in its ameliorating influence of glutamate neurotoxicity. Cortical cultures were extracted from fetal mice treated with a chemical that triggers glutamate toxicity. The cultures were treated via the nootropic for 12hours to one day. After a period of exposure, it was observed that Coluracetam ameliorated the effects of exposure [5].

Another benefit observed with the nootropic was minimizing the learning deficits in rates via the Morris Water Maze test. Adult rats within the experimented group were given a cholinergic neurotoxin. The controlled group involved healthy rats. With the group, Coluracetam significantly minimized learning deficits related with neurotoxin administration without triggering any serious side effects such as hypothermia, drooling, or tremor. It seems that from such study, the nootropic had little effect on the healthy rats than it did with the experimented group [6].

The last well-known benefit of the nootropic signifies long-term improvement in individuals with learning impairment. Rats were treated with a cholinergic neurotoxin AF64A and administered repetitive dosages of Coluracetam for 8-straight days at 3 mg per kg per day. Scientists concluded that after72 hours of the last administration of the nootropic, rats with learning impairment still showcased improvements in the Morris Water Maze test [6] [7].

During the experiment, scientists also conducted a test as to whether or not Coluracetam can be detected in the body of rats at the time of the test. They found that while the rats were showcasing positive effects from its previous administration, Coluracetam content within their systems were negligible [6] [7].

Dosages of Coluracetam

COLURACETAMOf the experiment conducted in adult rats, the dosage schedule ranged from 1 mg per kg to 10 mg per kg daily. At the high-end dosage range, the dose in average human adult is equivalent to 2.9 mg per kg.This is around 203.5 mg/day for an average human weight [6].

Just recently, BrainCells Inc., concluded the Phase2A trials of Coluracetam, going under the monikerBCI-540, where they administered up to 80 mg thrice daily of the drug for adult humans suffering from a  Major Depressive Disorder. 36% of the participants showcased improvements in their scores on the drug test [1].

Toxicity of Coluracetam

Phase 2A trials done by Brain Cells Inc. indicated that 80 mg of the nootropic given thrice daily showed no side effects. At that time, it was deemed the highest dosage schedule for the drug [1].

References:

  1. http://www.smarternootropics.com/coluracetam/
  2. http://en.wikipedia.org/wiki/Coluracetam
  3. http://www.ncbi.nlm.nih.gov/pubmed/18461273
  4. http://www.ncbi.nlm.nih.gov/pubmed/18446264
  5. http://www.ncbi.nlm.nih.gov/pubmed/9541286
  6. http://www.ncbi.nlm.nih.gov/pubmed/8740080
  7. http://examine.com/supplements/Coluracetam/#summary3-0

Nootropic Review: Semax

Semax is a nootropic created by the Institute of Molecular Genetics, Russian Academy of Science. The nootropic was developed within the early 1908s to 1990s and later gained authorization to be marketed to the public [1]. Within Russia, the substance was utilized for treating brain stroke, brain damage after ischemia, optic nerve diseases, and other cognitive disorders. Furthermore, the nootropic has been shown during a private human study to improve cognitive capabilities effectively while positively managing EEG bands [2].

Enhancement in Cognition

A 2-day clinical study done of Russian power plant employees tested the effectiveness of the nootropic through a number of memory-related tasks. The test lasted for 15 minutes where the first half was done at the start and the other half at the end of employee shift on the first and second day respectively.

A 1 mg dosage was given via the nasal cavity on the first day one hour before testing and the second day shortly after the morning tests were conducted.A placebo group was also asked to conduct the same task.

Semax significantly minimized the number if erroneous responses on the first and last day while the error rate from the placebo group surged. The substance also attenuated a dip in proper performance scores compared to those taking a placebo [3].

Mood Aspects

Animal studies done showcased Semax to have the potential for enhancing mood and minimizing anxiety [4]. A recent rat study indicated the nootropic to be capable of minimizing CCK-4 induced depression and stress while not affecting rats given a placebo.

CCK-4 is a powerful neuropeptide that triggers anxiety in animals and human. So much so, the chemicals utilized to trigger panic attacks when scientists are seeking for treatment choices. Such study mostly indicated that rats offered nothing or with Semax was in the same state of mood while rats given CCK-4 were further depressed and anxious on a maze and swim test.

Mixing Semax and CCK-4 back to levels of placebo particular mood parameters, indicate Semax to be capable of treating individuals who are depressed or anxious, while leaving the healthy state as is [5].

An abstract study done featured within the International Journal of Psychophysiology talked about how Semax, combined with Selank, were capable of triggering sedation effects and relieving certain effects of mental health in animals [6].

The Semax was found to minimize severe psychotic disturbance times (at 1 to five days) compared to placebo (at 1 to nine days) when given a dosage of 0.6mg daily via inhalation. With subsiding acute symptoms of Semax given at 0.3 mg per day, enhanced cognitive function, and minimal asthenic disorders were observed compared to placebo [7].

Mechanism of Semax

Semax structureWithin the glial cell structures, both levels of NGF and BDNF increased eight times than normal and gave more after being exposed to Semax. In rats, the nootropic was shown to increase levels of BDNF and trkB levels by up to 1.6 times. Comprehensive research done indicated the nasal intake of Semax promotes an increase in BDNF of rats brains [8] [9] [10].

Alpha Brain Wave Activity

Semax was indicated to alter EEG in human cognitive and hyperventilation tests. During the cognitive test, the chemical dramatically decreased the activity of a delta brainwave and enhanced alpha and beta brain rhythm [11] [12].

Safety Aspects

Semax appears to be completely non-toxic and safe. In Russia, the drug is headed under the list of essential and required drugs where it received approval for treating medical conditions such as migraine, stroke, and other cognitive disorders. At the same time, it has comprehensively been tested and included in numerous clinical trials with no reports of hormonal changes or side effects [1] [13].

References:

  1. http://old.img.ras.ru/semax1-e.htm
  2. http://www.ncbi.nlm.nih.gov/pubmed/11569188
  3. http://onlinelibrary.wiley.com/doi/10.1002/%28SICI%291520-6769%28199609%2919:2%3C115::AID-NRC171%3E3.0.CO;2-B/pdf
  4. http://link.springer.com/article/10.1007%2Fs11064-005-8826-8#page-2
  5. http://www.ncbi.nlm.nih.gov/pubmed/20387390
  6. https://www.deepdyve.com/lp/elsevier/the-cerebroprotective-effects-of-Semax-and-selank-in-primates-at-gHqfNvoDEw
  7. http://www.google.com/patents/US20100222286
  8. http://www.ncbi.nlm.nih.gov/pubmed/18756821
  9. http://www.ncbi.nlm.nih.gov/pubmed/19662538
  10. http://www.researchgate.net/publication/26724475_Comparison_of_the_temporary_dynamics_of_NGF_and_BDNF_gene_expression_in_rat_hippocampus_frontal_cortex_and_retina_under_Semax_action
  11. http://brain.bio.msu.ru/research_e.htm
  12. http://www.researchgate.net/publication/237217244_Synthetic_ACTH_analogue_Semax_displays_nootropic-like_activity_in_humans
  13. http://en.wikipedia.org/wiki/Semax

Nootropic Review: Phenibut

phenibutCreated in the Soviet Union back in the 1960s, Phenibut (also referred to as Phenybut or Noofen) is naturally observed within the GABA, the body’s primary neurotransmitter) [1]. The nootropic has been indicated to offer anti-stress, anti-anxiety, and a soothing effect on the body similar to another substance, Baclofen [2]. Phenibut has been observed to offer nootropic mechanisms not only for its neuroprotective properties but also for minimizing amnesia and aiding in sleep [3].

The nootropic was deemed such a tremendous success from the Russian cosmonaut’s medical team that they made a decision to make it a mandate in their medical kits. Phenibut is a replacement in other tranquilizers since they didn’t make cosmonauts sleepy. At the same time, it helped lower their stress levels without any adverse effects in their cognitive abilities [4] [5].

Phenibut is a recommended inhibitory compound since it aids users to wind quickly down if any mild insomnia is observed. The nootropic is beneficial since it enhances the normal sleep cycle for improved sleep and better cognitive capabilities the next day [6].

Primary Findings of Phenibut

  • Effective in alleviating fear, tension, depression, and anxiety [7]
  • Effective in fighting against alcohol toxicity
  • Features anti-oxidant properties
  • With anti-amnesic and neuroprotective mechanisms [8]
  • Protection from decreased cognition after lack of sleep

Details of Phenibut

Phenibut is a substance that is said to fight anxiety and stress. Comprehensive studies have shown the drug to possess neuroprotective and anti-amnesic mechanisms. Widely known in Russia for its nootropic effects, the drug crept its way into the country’s medical practice for its sedative properties compared to traditional tranquilizers.

Many Russian cosmonauts found Phenibut helpful since it lacked sedation and cognitive impairment unlike that of other medications. Such qualities are essential since levels of stress are high during years of travelling in space. The compound is required to alleviate stress without interrupting cognitive performance [9].

Phenibut has been utilized in Russia for a number of applications which include relief from fear and tension, and enhanced sleep in neurotic or psychosomatic patients. Stuttering and post-traumatic stress disorders also involved the use of Phenibut.

The compound has been indicated to exhibit anti-amnesic effects when scopolamine-amnesia is triggered. It even surpassed the same anti-amnesic properties of Piracetam. Phenibut showcased anti-oxidant effects when experimented on the spleen. Such health benefit is further pushed when studies showed that the nootropic efficiently curbed brain injury after an alcohol intake as well as preventing induced hypoxia damage [10] [11].

Mechanisms of PhenibutPhenibut structure

Being a GABA derivative, Phenibut has been shown to function as an agonist to the metabotropic GABA receptor. It also has an agonist process to the GABA A receptor at larger dosages. Such process lets the nootropic offers an inhibitory and calming effect on the brain.

Further studies have also shown how the compound lessens norepinephrine levels found in the hippocampus thereby minimizing unnecessary stimulation. Anti-anxiety and anti-depressant properties are a result of increased neurotransmitter metabolites observed after ingesting the nootropic [12] [13].

References:

  1. http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2001.tb00211.x/pdf
  2. http://www.raysahelian.com/phenibut.html
  3. http://www.ncbi.nlm.nih.gov/pubmed/11830761
  4. http://www.phenibutforanxiety.com/thescienceofphenibut.php
  5. http://corpina.org/complete-guide-responsible-phenibut-use
  6. http://nootriment.com/phenibut-sleep-aid
  7. http://www.ncbi.nlm.nih.gov/pubmed/23391959
  8. http://www.fasebj.org/cgi/content/meeting_abstract/26/1_MeetingAbstracts/672.6
  9. https://www.erowid.org/references/refs_view.php?ID=8524
  10. http://www.ncbi.nlm.nih.gov/pubmed/3609269
  11. http://www.dr-bob.org/babble/alter/20040815/msgs/384573.html
  12. http://www.ncbi.nlm.nih.gov/pubmed/22232912
  13. http://www.ncbi.nlm.nih.gov/pubmed/15776965

Nootropic Review: Adrafinil

AdrafinilAdrafinil is a nootropic belonging under the “eugeroic” category. It’s later broken down into Modafinil when it reaches the liver resulting to a number of beneficial effects. Both Adrafinil and Modafinil are nootropics with wakeful-enhancing properties. But unlike that of Modafinil, Adrafinil isn’t regulated in the United States and requires a private purchase.With that mind, the nootropic is said to offer unpleasant side effects, so caution is a must [1] [2].

Mechanism of Adrafinil

While the precise mechanism of the nootropic isn’t completely confirmed, there a host of theories regarding its effects. One widely known theory indicates that it enhances hypocretin, a brain neurotransmitter. Hypocretin aids in appetite, wakefulness, and arousal. Through increasing such neurotransmitter within the hypothalamus, it’s been thought to increase dopamine, histamine, and norepinephrine levels. A surge in these chemicals is said to be the primary mechanism of Adrafinil [3].

Another theory regarding its process that is less known than what was mentioned is that the nootropic activates the glutamate pathways while halting the GABA pathways. That is said to promote wakefulness and alertness [4].

Benefits of Adrafinil

Adrafinil carries some benefits inherited by Modafinil. Some indicate that the nootropic is a weaker version of Modafinil. Others believe Adrafinil isn’t as effective as that of Modafinil. But nevertheless, the nootropic is recommended for increasing alertness with lesser side effects compared to stimulants that depend on monoaminergic systems [4].

Individuals who have ingested Adrafinil say it does an excellent job in enhancing memory and learning. It can be utilized in cases where high mental demand is needed to aid in alertness and focus. There’s proof that the nootropic can assist with concentration and even help people with ADHD symptoms. The supplement should never be, in any way, be taken without the advice from a physician [5].

Adrafinil Safety

Adrafinil carries certain risks. The compound may place additional strain on the heart, and while it is unconsidered as strenuous as that of amphetamines, there are risks involved. Individuals with a healthy heart shouldn’t but worried, but it’s highly recommended not to ingest Adrafinil if one currently or has had heart-related problems. Combining Adrafinil with other stimulants further increases risks to heart complications [6].

Adrafinil Interactions

Adrafinil structureAdrafinil can be mixed with stimulants and functions in a synergistic manner. This may be a concern if you combine the nootropic with substances that increase blood pressure or heart rate. There have been evidence that Modafinil can hinder some birth control products to be effective. It’s still not clear if Adrafinil carries the same mechanism, but it’s believed to carry a similar action [7].

Hepatotoxicity of Adrafinil

When the nootropic is broken down in the liver, it places a strain on the organ and increases liver enzymes. If an individual is connotative of high liver enzymes, it shouldn’t be recommended to ingest Adrafinil because it can damage the liver or cause liver failure. It’s advised to have a blood test done prior to taking the compound [8].

Tolerance/Withdrawal of Adrafinil

Adrafinil has a lower risk to addiction compared to other stimulants, but it can still be addictive in some ways. Any compound involving dopamine carries an increased addiction risk. Unfortunately, the nootropic falls into such category. Adrafinil has less euphoric effects compared amphetamines and has lesser abuse potential. If utilized properly to promote alertness, there’s a slight chance of developing an addiction [7] [9].

Ingesting the nootropic, usually can lead to drug tolerance over time and that is likely the case if ingested for a longer period. Cycling the drug can help eradicate such problem [9].

References:

  1. http://examine.com/supplements/Adrafinil/
  2. http://pubchem.ncbi.nlm.nih.gov/compound/adrafinil#section=Top
  3. http://nootriment.com/adrafinil/
  4. http://www.ncbi.nlm.nih.gov/pubmed/11191710
  5. http://pubchem.ncbi.nlm.nih.gov/compound/adrafinil#section=Chemical-Vendors
  6. http://www.smart-publications.com/articles/adrafinil-alertness-without-stimulation
  7. https://www.erowid.org/smarts/adrafinil/adrafinil_info1.shtml
  8. http://livertox.nih.gov/ModafinilArmodafinil.htm
  9. http://nootropicsreview.org/how-to-use-adrafinil

Nootropic Review: Sulbutiamine

sulbutiamineSulbutiamine or commonly referred to as Arcalion, is nootropic that possesses a synthetic lipophilic derivative of thiamine. The supplement is capable of entering the blood-brain barrier swiftly and quietly [1]. The nootropic was created in Japan with an attempt to seek for a chemical capable of transporting thiamine to the brain to treat individuals with cerebral chronic fatigue [2].

At present, Phenylpiracetam is the only primary treatment for such condition and when ingested, offers mild stimulation. The Sulbutiamine is claimed to inherit a number of nootropic characteristics. It’s also known to treat individuals suffering from erectile dysfunction based on latest clinical studies [3] [4].

It’s recommended to not ingest Sulbutiamine in the middle of the day since it may lead to insomnia. It’s advised to not ingest the supplement daily since it can quickly lead to tolerance. The maximum benefit that can be done is only to take it when mental concentration and energy is extremely required for better performance [5] .

Primary Findings of Sulbutiamine

  • Significantly enhances mood
  • Effective treatment for long term fatigue
  • Improves learning and memory
  • Heightens focus and boosts overall energy
  • Effective treatment for erectile dysfunction

Details of Sulbutiamine

Primarily made for treating chronic fatigue, the nootropic offers mild stimulation which lead to mental concentration, motivation, and alertness. It has also been showcased to enhance overall cognition and memory by increasing Acetylcholine levels. For such reason, it has been utilized in enhancing memory especially for individuals suffering Schizophrenia and Alzheimer’s [6].

An improvement of memory is observed due to the potentiation of reward centers, glutamatergic, and cholinergic delivery of Sulbutiamine. Animal studies done indicate an increase in operational conditioning and adequate recognition of objects [7].

Latest studies have shown that the nootropic is becoming more efficient in minimizing the dizocilpine effects seen in individuals with schizophrenia. People suffering Alzheimer’s showed remarkable daily improvement in activities when Sulbutiamine is administered simultaneously with any Acetylcholinesterase inhibitor [8].

In addition, studies found that Sulbutiamine is every effective in treating erectile dysfunction. 16 out of 20 patients were treated from erectile dysfunction symptoms. As an affordable and cheaper alternative to ED meds, many claims that Sulbutiamine is an excellent therapeutic advancement [4].

Mechanisms of Sulbutiamine

Sulbutiamine structureThe nootropic is capable of stimulating the body by functioning as a releasing medium for Glutamate in the central nervous system. Glutamate is one of the body’s primary neurotransmitters that let the central nervous system be stimulated while playing a critical role in learning and memory [9].

Sulbutiamine quickly enters the blood-brain barrier since it’s a lipophilic molecule. This makes it possible to be readily absorbed in the brain than thiamine. This is particularly handy since the nootropic is transformed into thiamine and provides a batter administration path. Thiamine is internally converted into Acetylcholine and GABA [6].

It’s been indicated that Sulbutiamine adds density to the D1 reward receptors found in the prefrontal cortex. This is done by minimizing the release of the reward neurotransmitter [10].

References:

  1. http://examine.com/supplements/Sulbutiamine
  2. http://www.smartdrugsforthought.com/what-is-sulbutiamine
  3. http://nootriment.com/sulbutiamine-side-effects
  4. http://www.ncbi.nlm.nih.gov/pubmed/15776829
  5. http://corpina.org/sulbutiamine-treatment-chronic-fatigue-syndrome
  6. http://en.wikipedia.org/wiki/Sulbutiamine
  7. http://www.ncbi.nlm.nih.gov/pubmed/4059305
  8. http://www.ncbi.nlm.nih.gov/pubmed/15951087
  9. http://www.researchgate.net/publication/230897996_Effect_of_Sulbutiamine_on_glutamate_transporters_%28EAAT1SLC1A3_and_EAAT2SLC1A2%29__nee_cell__Astrocyte_metabolism
  10. http://www.ncbi.nlm.nih.gov/pubmed/10996447
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