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Coluracetam Nootropics Racetams Reviews

Coluracetam Review: A Nootropic With Antidepressant Properties

The drug piracetam is often regarded as the first truly nootropic drug, due to its ability to promote healthy brain function and cognition without potentially debilitating side effects. The family of nootropics that are structurally related to piracetam, known as racetams, have also been held in high esteem by the nootropics community. Coluracetam is one of the many members of this nootropic drug class, but it has some unique properties that set it apart from the rest.

Introduction

ColuracetamColuracetam is a fairly new addition to the racetam category of nootropics, being developed and initially researched in the mid-1990s.[1] Coluracetam, known also by its research names of MKC-231 and BCI-540, was initially developed and researched by the Mitsubishi Tanabe Pharma Corporation in Japan as a potential treatment for Alzheimer’s disease. Coluracetam has also seen some limited research concerning its potential use for treating Major Depressive Disorder and Generalized Anxiety Disorder.[2]

Mechanism of Action

When ingested, coluracetam becomes present in nerve tissue within 30 minutes of administration. The concentration in the body begins to decrease about 3 hours after ingestion.[3]
The most definitive mechanism through which coluracetam works is high-affinity choline uptake (HACU). HACU is a crucial step in the process of the body’s converting of choline into acetylcholine, a vital neurotransmitter for cognition processes. [4] In essence, this means that an increase in HACU (caused by coluracetam) will also increase the activity level of acetylcholine in the nervous system. This is the basis for coluracetam’s ability to enhance cognition

My Experience with Coluracetam

My trial run for NootropicsDepot’s coluracetam lasted for one week, due to the fact that coluracetam’s effects seem to all take place rather quickly. In other words, the effects do not appear to be cumulative like some other nootropics. Typically, I took 30 mg orally in the morning, along with another 30 mg in the afternoon. If necessary, I took another dose later on in the day. Dosage recommendations for coluracetam range anywhere from 3 mg up to 100 mg or more, but this dose seemed to work just fine. Having experimented with coluracetam briefly a few months ago, I had a general feel for what dose might work.

Coluracetam powder nootropicDuring the time of this trial, I was not taking any prescription medications. In the morning, I was taking Vitamin B12, Vitamin D, potassium gluconate, fish oil, and turmeric. The effects I experienced from taking coluracetam have been very positive. However, bear in mind that this is only a subjective experience. The placebo effects cannot be ruled out (although I am convinced it was the coluracetam I felt), and experiences will vary between individuals. That being said, I will now go into what I felt are the major benefits of coluracetam:

  1. Motivation enhancement
    Right off the bat, coluracetam seems to provide a decent increase in motivation to engage in productive work. I felt a stronger desire to work on school work that I don’t find very interesting. It made it much easier to push through to get things done, leaving a very satisfactory feeling when things were accomplished.
  2. Stimulation
    This effect goes somewhat hand-in-hand with motivation enhancement. Coluracetam has the effect of making me feel more awake and alert. It seems to help me feel more ready and able to get work done. It didn’t make me feel “jittery” either – I felt quite relaxed the whole time.
  3. Reduction in fatigue
    Coluracetam appears to help alleviate both physical and mental fatigue. There were a few instances when taking it where I went from being exhausted and drained to energized and ready to go.
  4. Enhanced cognition
    This effect is very important for any nootropic compound. After all, it is the main thing that nootropics are purported to influence. Within half an hour of taking coluracetam, I felt much more able to formulate thoughts and translate them into writing. I also felt more able to connect ideas in my mind and get a better idea of the “bigger picture.” I also felt more naturally able to hold conversations with others, feeling much more engaged and fluent.
  5. Music enhancement
    While this is mostly unrelated to the topic of cognitive enhancement, listening to music while on coluracetam was very pleasant. The music itself felt more full, interwoven, and immersive than usual. Individual pieces of melody and minor details became more distinguishable than usual.
  6. Mood Boost
    After taking coluracetam, I can understand why it is being researched as a treatment for depression. It helped me remain more positive and upbeat throughout the day. I also seemed to make things more enjoyable in general.

Drawbacks

Coluracetam seems to be a very promising nootropic in terms of its multiple benefits and few side-effects. I did not experience any apparent increase in tolerance during the week I was taking it, even with multiple doses in one day. Experiments in which rats were given coluracetam for 14 days at a time seems to reinforce this.[5] The only possible side-effect I experience was mild to moderate headaches, which occurred throughout the week. This should be taken with a grain of salt because I am normally fairly prone to headaches in the first place. I’ve also heard that taking choline can alleviate headaches that come with racetam supplementation, so that could be a potential remedy.

Conclusion

All things considered, I was very pleased with the effects of coluracetam. I will certainly be implementing it into my nootropic stacks, as it is one of the most noticeable and useful nootropics I have personally taken. It seemed to have a real impact on my motivation, energy, and cognition. Everyone is bound to react differently to coluracetam, but I strongly encourage nootropics users to give it a try.

You can buy Coluracetam powder and capsules at NootropicsDepot.

Coluracetam
7.5
Focus
8.5
Mood
8
Memory
7.5
Stimulation
7
Relaxation
8
Safety
Reviewer 8.4
Summary
I highly recommend coluracetam for anyone who needs to spend extended periods of time working on demanding mental tasks. The cognitive boost and mental stimulation was extremely useful.

References   [ + ]

Categories
Nootropics

The 14 Best Nootropics for Anxiety

As we collect evidence provided to us by our ever-expanding group, we’ve come up with a few good remedies. Anxiolytic drugs are known to “relieve anxiety”.[1] Many of us suffer from anxiety ranging from slight to severe impairment. It is wise to note that some drugs, such as Bacopa, have enhanced efficacy after chronic administration.[2] Others, such as Tenoten, are applied sublingually and can be used to treat acute anxiety.[3] Any of the information here is not to be used or substituted for medical advice.

Bacopa

4 out of 5 stars
Bacopa monnieri nootropics for anxiety
Bacopa monnieri

Bacopa monnieri (also known as Brahmi) is one of the most important herbs in Ayurvedic medicine. It has been used for centuries as a mental tonic originating in India.

Bacopa has been shown in studies to relieve anxiety, improve cognition, and enhance memory formation.[4] [5] In a rat study, Bacopa increased the levels of serotonin and enhanced the gene expression of serotonin transporters[6]. Studies have shown a relationship between high levels of serotonin and positive mood.[7] [8]

Bacopa also appears to have an adaptogenic effect by reducing the biochemical effects of stress.[9]

To fully appreciate the positive effects of Bacopa, it needs to be taken consistently. Studies have shown more improvement as time passes. [10]

Ashwagandha

4 out of 5 stars

Withania somnifera, commonly known as Ashwagandha, is a popular herb used in Ayurvedic medicine. In Sanskrit, Ashwagandha means “the smell of a horse”, because of its unmistakable smell. It is also believed to give vitality and the “strength of a stallion”.

Ashwagandha is believed to act as a neuroprotector, anxiolytic, anti-inflammatory, thyroid-booster, and libido enhancer.

Ashwagandha activates GABA-A receptors, the mechanism of action responsible for its anxiolytic and sleep-inducing effects.[11]

It has been shown to be as effective as fluoxetine for obsessive-compulsive disorder (OCD) in a mice study.[12]

L-Theanine

3 out of 5 stars
Matcha
Matcha is a Japanese green tea with a very high Theanine content

L-Theanine is a natural amino acid contained in green tea. Most store-bought teas contain minimal amounts of L-Theanine, however, concentrations are greater in teas such as matcha, gyokuro, and kabusecha.

L-Theanine is structurally similar the neurotransmitters glutamate and GABA.[13] L-Theanine is also a neuroprotective agent[14] which increases the amounts of serotonin, dopamine, and GABA in various areas of the brain.[15] It’s commonly used with stimulants, — like caffeine or amphetamines —, to reduce side effects, but it is also effective by itself.

Inositol

3 out of 5 stars

Inositol is a sugar involved in cellular signaling and as a component of cell membranes. There are nine different inositol molecules. The most abundant of these being myo-inositol.

Inositol was once considered a B vitamin (formerly Vitamin B8). It was later found to be producible by the human body, disproving it as an essential nutrient. It is naturally found in small quantities in milk products, fruits, and vegetables.

Research shows high dose Inositol supplementation (18 g) was as effective as fluvoxamine (150 mg) in decreasing the number of panic attacks[16] and reducing the symptoms of obsessive-compulsive disorder (OCD). [17]

Phenibut

5 out of 5 stars

Phenibut is a gamma-aminobutyric acid (GABA) derivative.

GABA is the major inhibitory neurotransmitter in the brain. The mechanism of action of conventional anxiolytics, hypnotics, and sedatives (such as benzodiazepines, barbiturates, and alcohol) increase GABA levels. This is what gives them anti-anxiety, sleep-inducing, tranquilizing, and anticonvulsive effects.

Phenibut was developed in the Soviet Union in the 1960s as a non-sedative alternative to benzodiazepines. Phenibut is part of the Russian cosmonaut medical kit as a treatment for stress.

Phenibut activates GABA-B receptors[18] and boosts dopamine levels.[19]

Picamilon

2 out of 5 stars

Picamilon is another Russian nootropic made by combining niacin (vitamin B3) and GABA. This allows Picamilon to cross the blood–brain barrier[20] and have anxiolytic and vasodilating[21] effects.

It is used in Russia as a treatment for anxiety, depression[22], alcoholism[23], and brain damage.[24]

Aniracetam

3 out of 5 stars

Aniracetam (known as Ampamet in Europe) is a compound of Racetam family. It is a fat-soluble derivative of Piracetam.

Aniracetam modulates AMPA receptors. AMPA is one of the main three excitatory neurotransmitters (the other two being NMDA and kainate receptors). Compounds that act on AMPA receptors are called AMPAkines.

AMPAkines are substances which exhibit neuroprotective and cognition enhancing effects[25]. Some of these have been investigated as treatment for Alzheimer’s disease and other neurodegenerative conditions[26]. Aniracetam is also a potential anxiolytic[27] and antidepressant.[28] Anecdotal evidence states that Aniracetam is effective in some individuals, while others are non-responders.

Coluracetam

4 out of 5 stars

Coluracetam is a relatively new Japanese nootropic drug with little clinical backing. Unlike Piracetam, Coluracetam directly affects High Affinity Choline Uptake.[29] It was shelved after failing to demonstrate efficacy for Alzheimer’s.

Phase IIa clinical trials have demonstrated efficacy for comorbid MDD with GAD (Generalized Anxiety Disorder).

Anecdotal reports state Coluracetam is responsible for a sensation of “HD Vision” as well as lowered anxiety.

Fasoracetam

3 out of 5 stars
Fasoracetam, a novel nootropic
Fasoracetam, a potent and novel nootropic which shows promise to relieve anxiety, as well as reduce ADHD symptoms.

Fasoracetam, also referred to as NS-105, is a novel cognitive enhancer. Fasoracetam is a high-affinity choline reuptake inhibitor, similar to Coluracetam.[30] Many refer to this particular mechanism of action as “HD vision”.

Fasoracetam can act as a sustainable anxiolytic since long-term administration upregulates GABA-B receptors.[31] Anecdotal reports have noted both acute and chronic anxiolytic effects.

Treatment of ADHD, by NS-105, is mediated through modulation of mGluR glutamate receptors.[32] In other words, those suffering from ADHD and/or anxiety may benefit from Fasoracetam’s purported effects.

Tianeptine

5 out of 5 stars

Tianeptine is a tricyclic antidepressant (TCA) developed in France circa 1960. Tianeptine embodies a unique mechanism of action, unlike other TCAs.

Tianeptine was originally believed to be a Serotonin Reuptake Enhancer. Recent research suggests its antidepressant effect is due to the activation of μ-opioid and δ-opioid receptors[33] as well as modulation of AMPA and NMDA receptors.[34]

Tianeptine efficacy is comparable to fluoxetine, amitriptyline, and imipramine (with significantly fewer side effects).[35]

Tenoten

2.5 out of 5 stars

Tenoten is a simultaneous nootropic and anxiolytic with novel properties. Unlike GABA agonists, Tenoten treats anxiety “based on antibodies to the brain-specific protein S-100B”.[36]

“Testing at the Russian Institute of Molecular Biology and Biophysics indicate Tenoten was as clinically effective as amitryptiline (Elavil), sertraline (Zoloft), and phenazepam (a benzodiazepine) for the reduction of anxiety but without sedation. It further recommended Tenoten for patients with moderate cognitive impairment”.[37]

“[Tenoten] demonstrated considerable improvement of the control over brain frontal compartment effector functions”.[38]

In a small trial group of 50 children, Tenoten showed efficacy for the treatment of ADHD symptoms.[39]

Selank

3.5 out of 5 stars

Selank, is an analog of the endogenous peptide tuftsin. Since tuftsin has innate immunomodulatory capabilities, Selank is also able to regulate T cell cytokines.[40] In this way, Selank can be seen as having immunomodulatory properties.

Unlike common anxiolytics, Selank does not cause sedation or cognitive impairment. It is non-habit forming and does not cause withdrawal symptoms.

Selank modulates monoamine transmitters[41] and catalyzes the metabolism of serotonin.[42] Selank causes rapid elevation of BDNF, solidifying its place as a cognitive enhancer.[43]

Although Selank’s mechanism of action is largely misunderstood, evidence suggests it lowers levels of tau(1/2) leu-enkephalin.[44]

Afobazole

3 out of 5 stars

Afobazole (also known by its scientific name Fabomotizole) is a Russian anxiolytic drug which does not possess sedative properties unlike most anxiolytics. Afobazole, similar to Fasoracetam, upregulates GABA receptors.[45] Afobazole restores GABA to healthy levels following ischemia.[46] This is widely regarded to be Afobazoles main anxiolytic mechanism of action.

Fabomotizole also induces BDNF and NGF release, agonizes MT3 receptors, and reversibly inhibits MAO-A [47] [48] [49] [50] [51]. Since Afobazole directly effects BDNF and NGF, it is also classified as a nootropic. Caution should be taken when combining Afobazole with other MAO inhibiting substances. Afobazole may also have an antidepressant effect.

Kava

4 out of 5 stars

Kava is a GABAergic drug which affects the GABA-A receptor in several ways. Kava exhibits reverse tolerance. It is a less-harmful alternative to common GABA-A benzodiazepine receptor agonists. The alkaloids chiefly responsible for Kava’s mechanism of action are called kavalactones.[52] It is becoming apparent that although Kava is confirmed to modulate GABA-A receptors, it may do so in a different method than direct agonism.[53] It appears Kava potentiates GABA-A through poorly understood means.[54] GABA-A receptor density increased following administration of Kava, suggesting both upregulating and sensitizing properties.[55]

A common concern for Kava usage lies in its purported hepatotoxicity. Hepatotoxicity of Kava is a direct result of the extract or plant matter obtained, suggesting quality is paramount to avoiding liver damage. “Risk factors included overdose, prolonged treatment, and comedication with synthetic drugs and dietary supplements”.[56] Indigenous tribes have been using Kava for centuries, with minimal consequences. One can assume toxicity is directly affected by the quality of the plant used.

Most, but not all, of clinical studies, have demonstrated Kava’s efficacy as an anxiolytic. Standardized extract demonstrated the highest efficacy versus placebo. 1 week of chronic administration may be necessary to feel its effects. Evidence suggests Kava may aid in the treatment of insomnia and sleeplessness.[57]

References   [ + ]

1. Definition of anxiolytic by Merriam-Webster
2, 10. Enhanced dendritic arborization of hippocampal CA3 neurons by Bacopa monniera extract treatment in adult rats.
3. The use of tenoten and tenoten (pediatric formulation) as a drug for premedication in adults and children during outpatients dentist visit.
4. Randomized controlled trial of standardized Bacopa monniera extract in age-associated memory impairment.
5. Bacopa monniera, a reputed nootropic plant: an overview.
6. Bacopa monniera leaf extract up-regulates tryptophan hydroxylase (TPH2) and serotonin transporter (SERT) expression: implications in memory formation.
7. Associations between whole-blood serotonin and subjective mood in healthy male volunteers.
8. Serotonergic function in the central nervous system is associated with daily ratings of positive mood.
9. Adaptogenic effect of Bacopa monniera (Brahmi).
11. Pharmacological effects of Withania somnifera root extract on GABAA receptor complex.
12. Influence of Withania somnifera on obsessive compulsive disorder in mice.
13, 14. Neuroprotective effects of theanine and its preventive effects on cognitive dysfunction
15. The neuropharmacology of L-theanine(N-ethyl-L-glutamine): a possible neuroprotective and cognitive enhancing agent.
16. Double-blind, controlled, crossover trial of inositol versus fluvoxamine for the treatment of panic disorder.
17. Inositol treatment of obsessive-compulsive disorder.
18. On neurotransmitter mechanisms of reinforcement and internal inhibition.
19. Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.
20. Pikamilon pharmacokinetics in animals.
21. The new cerebrovascular preparation pikamilon.
22. The results of clinical study of the drug Picamilon (analysis of data of neurologic and psychiatric clinics) – AP Huaichenko, RP Kruglikova-Lvova
23. Picamilon Application in Therapy of Patients with Alcoholism, – Novikov VE, Kovaleva LA
24. Picamilon Application in the Complex of Regenerative Therapy of Patients after Insultus
25. AMPA receptor potentiators for the treatment of CNS disorders.
26. Benzofurazan compounds which enhance AMPA receptor activity
27. Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism.
28. Antidepressant-like effects of aniracetam in aged rats and its mode of action.
29. MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice
30. Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer.
31. Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment.
32. A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture.
33. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist.
34. The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation
35. Tianeptine: a review of its use in depressive disorders.
36, 37, 38. Tenoten in the therapy of patients with moderate cognitive impairment.
39. Clinical efficacy of tenoten for children in treatment of attention deficit and hyperactivity disorder
40. Immunomodulatory effects of selank in patients with anxiety-asthenic disorders
41. Effects of heptapeptide selank on the content of monoamines and their metabolites in the brain of BALB/C and C57Bl/6 mice: a comparative study
42. Comparison of the effects of selank and tuftsin on the metabolism of serotonin in the brain of rats pretreated with PCPA
43. Intranasal administration of the peptide Selank regulates BDNF expression in the rat hippocampus in vivo.
44. Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia
45, 46. Effects of afobazole on the content of neurotransmitter amino acids in the striatum in global transient ischemia.
47. Clinical study of the selective anxiolytic agent afobazol
48. Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon
49. Effects of afobazole on the BDNF content in brain structures of inbred mice with different phenotypes of emotional stress reaction
50. Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons
51. Interaction of afobazole with sigma1-receptors
52, 57. Kava kava | University of Maryland Medical Center
53, 54, 55. Kavapyrone enriched extract from Piper methysticum as modulator of the GABA binding site in different regions of rat brain.
56. Kava hepatotoxicity–a clinical review.