Article by Mike Arnold(a repost of a brilliant article)
One of the newer accessory drugs to hit the peptide & research chemical market in recent years is a nootropic, anxiolytic based drug known as Selank. This heptapeptide was originally developed by the Institute of Molecular Genetics of The Russian Academy of Sciences and is endowed with several potentially beneficial research applications, which may be applied for a variety of different uses. Currently, Selank has completed stage III clinical trials in Russia, with tentative plans to be released for human use in that region.
Using the spleen-produced, immunomodulatory peptide, Tuftsin, as the starting point in the creation of this nootropic, Selank is an analog of Tuftsin and shares with it multiple characteristics. It is closely related to the prescription drug, Semax, which was also developed by The Institute of Molecular Genetics and is approved for human use in Russia and the Ukraine. However, according to some user reports, Selank is considered the superior alternative when administered for like purposes.
While Selank is classified as a nootropic-anxiolytic type drug, it uses extend beyond the relief of anxiety and improved cognitive functioning alone. A few areas in which Selank may find itself useful are: stress reduction, the alleviation of depression, reversal of anhedonia, improvement in mood in emotionally stable individuals, and cessation of insomnia. Of course, with Selank being a nootropic-anxiolytic, it may also prove useful for the treatment of different forms of anxiety, such as G.A.D (generalized anxiety disorder), S.A.D (social anxiety disorder), Panic Disorder, as well as non-diagnosed bouts of anxiety. As a nootropic, Selank can help enhance mental sharpness, reduce mental fatigue, improve the ability to focus, improve cognitive functioning while in a sleep deficit, and enhance memory.
These effects are provided without the negative side effects typically associated with benzodiazepines, such as physical dependence, psychological addiction, and decreased motor ability. In fact, Selank is largely devoid of side effects, with the large majority of researchers claiming that it is a side effect free compound. This makes Selank more suitable for long-term use.
One of the mechanisms through which Selank is believed to derive its benefits is through an increase in serotonin, which is a neurotransmitter most commonly known for regulating mood, but also has effects on appetite and sleep. A deficiency in serotonin levels can lead to depression, lack of appetite, and difficulty sleeping. Selank also has significant modulatory effects on the bodys natural opioid system, leading to an increase in endorphin levels and a subsequent improvement in feelings of well being and overall mood. In addition, Selank works to increase dopamine levels, which is another neurotransmitter directly involved in many important functions, such as: cognition, motivation, mood, memory, sleep, and learning.
The general consensus, from those who have performed research with Selank, often say it leads to a mood stabilizing effect, in which the general overriding emotion is one of contentedness and wellbeing. This is not described as a sedating effect, in which the senses are dulled and physical aptitude is impaired (as experienced with benzodiazepines), but rather, it results in a calming effect, in which cognitive functioning and mental clarity is augmented. Periods of sleep deficiency are less likely to cause mental impairment and times of stress will be easier to cope with. For those who seem to have lost pleasure in activities or hobbies they used to enjoy, Selank may restore enjoyment in their participation.
Many reading this article may be BBrs or strength athletes and as such, they may find a unique use for this compound within their PED programs. It is no secret that some steroids lead to anxiety, the inability to sleep through the night, and other physical and mental-emotional issues. Not all individuals are affected equally when administering specific steroids, but there is no denying that certain drugs, such as trenbolone or heavy doses of androgens in general, may lead to an increase in anxiety, an inability to sleep, and excess excitability among other side effects. Selank can help to mitigate the intensity of these side effects, leading to a more normal emotional and functional state.
Another use for which Selank can prove valuable is for the alleviation of anhedonia, which is defined as the lack of pleasure or the inability to experience it. Many ex-drug users, particularly those who have abused amphetamine or opioid type drugs, often experience anhedonia for prolonged periods of time after discontinuance sometimes for several years on end. A portion of ex-addicts are negatively affected in this manner for the rest of their lives, never gaining a full recovery from the damage suffered to the brains pleasure centers. As a result, many have lost that natural spark; the inherent happiness which was present in their lives before damaging the bodys internal opioid system. Selanks ability to increase endorphin production may help to normalize levels of this critical chemical, making it possible for the individual to experience joy from everyday life.
The potential benefits dont stop there for ex-addicts, as many ex-drug users also experience several of the other ailments Selank is known to help alleviate, such as insomnia and anxiety. Unfortunately, the bodybuilding community is rampant with illicit drug use, including opiates and stimulant-based drugs. The addictive and risk-taking behavior of many steroid users has led them to explore drug use outside the confines of performance enhancing drugs, frequently leading to addiction to one or more of these substances. For those who have taken the necessary steps to abstain from illicit drug use, Selank may offer a multi-faceted approach in working towards the alleviation of ones post-drug use recurring ailments.
In terms of dosing, it was originally thought that 1-3 mg was the optimal dosing amount, but anecdotal evidence conflicts with these guidelines, as many users have stated that Selank can be effectively researched at 250-500 mcg with good effect. I suggest allowing personal research to determine ideal dosing guidelines. When it comes to toxicity, Selank is remarkably benign, with doses 500X the effective range shown to be easily tolerated by the human body. This should eliminate any fear of overdose with this peptide.
If you struggle with any of the issues listed above or would simply like to benefit from one or more of the effect(s) Selank provides, then this relatively inexpensive peptide is a good choice for your own personal research needs. The large majority of individuals who have used this drug report positive a experience, with many choosing to include it in their program long-term. There are many people in the BBing and strength communities who have not looked into this peptide seriously, simply because it does not lead to the direct accruement of muscle tissue or strength, but I believe that it would find a home in the regimens of many should it be given the chance.
[Effects of heptapeptide selank on genetically-based and situation-provoked symptoms of depression in behavior in WAG/Rij and Wistar rats, and in BALB/c mice].
AuthorsSarkisova KIu, et al. Show all Journal
Zh Vyssh Nerv Deiat Im I P Pavlova. 2008 Mar-Apr;58(2):226-37. Article in Russian.
A synthetic derivative of the endogenous peptide tuftsin heptapeptide selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) possesses an anxiolytic and psychostimulant effect, and represents a working element of a new peptide drug having completed the third phase of the clinical testing as a selective anxiolytic. The neurobiochemical spectrum of selank action combines mechanisms which are characteristics of antidepressants and psychostimulants: activation of the brain monoaminergic systems, dopamine synthesis and turnover, and modulation of the tyrosine hydroxylase activity. The aim of this study was to investigate the effect of selank in a new model of inherited (genetically-based) symptoms of depression in behavior of inbred WAG/Rij rats in comparison with its effect on situation-provoked symptoms of depression in behavior of BALB/c mice. Outbred Wistar rats constituted control group. Selank in high doses (1000-2000 microg/kg), after repeated injection counteracted symptoms of depression in behavior of WAG/Rij rats (increased immobilization in the forced swimming test and decreased sucrose intake or preference (anhedonia)). Selank in low doses (100 and 300 microg/kg) after single injection reduced the duration of immobility of BALB/c mice in the forced swimming test, but did not exert significant effect after repeated injection or after injection in high doses (600 and 900 microg/kg). Selank did not affect the level of general locomotor activity and anxiety in WAG/Rij rats, and did not exert substantial effect on the behavior of control Wistar rats. The results demonstrate the presence of antidepressant component in the spectrum of neuropsychotrophyc activity of selank and indicate the higher reliability of a new experimental model of depression (the WAG/Rij rats) as compared to the standard forced swimming test for the determination of antidepressant activity of a pharmacological drug
This medical study shows Selank has applications in anti viral medicine with regards to the flu. Wish I had this last week.
[Antiviral activity of immunomodulator Selank in experimental influenza infection].
AuthorsErshov FI, et al. Show all Journal
Vopr Virusol. 2009 Sep-Oct;54(5):19-24. Article in Russian.
The main objective of this study was to evaluate the antiviral properties of the glyproline Selank in both in vitro and in vivo against the influenza virus strain A/Aichi 2/68 (H3N2). The pronounced antiviral effect of the agent was detected in both systems. Selank added to the cell culture 24 hours before inoculation (a preventive use scheme) showed the highest efficiency, by completely suppressing viral reproduction. The in vivo studies also demonstrated that the highest survival of laboratory animals was observed when the agent was administered by the prevention scheme. The use of Selank in vivo induced the gene expression of interferon-alpha (IFN-alpha), without affecting that of interleukin (IL)-4, IL-10, or tumor necrosis factor-alpha (TNF-alpha). The findings suggest that the mechanism of the antiviral action of Selank may be due to its ability to modulate Th1/Th2/Treg cytokine equilibrium both directly and indirectly via the central nervous system. This is particularly promising if that the agent is synthesized on the basis of an endogenous peptide and that it has no negative effects is kept in mind.
Expression of inflammation-related genes in mouse spleen under tuftsin analog Selank.
AuthorsKolomin T, et al. Show all Journal
Regul Pept. 2011 Oct 10;170(1-3):18-23. doi: 10.1016/j.regpep.2011.05.001. Epub 2011 May 24.
Previous studies have shown that synthetic tuftsin analogue Selank causes a transcriptomic response in the rat hippocampus and in spleen cells and may participate in the regulation of inflammatory processes in the body. In this work we studied the effect of Selank and two of its fragments on the expression of genes involved in processes of inflammation. We analyzed the expression of 84 genes involved in processes of inflammation (e.g., chemokines, cytokines, and its receptors) in mouse spleen 6 and 24 h after Selank single intraperitoneal injection (100 μg/kg) using real-time PCR method. We found significant changes in the expression of 34 genes involved in inflammation processes. The detailed analysis of quantitative data showed that the Bcl6 gene, which plays a main role in the formation and development of the immune system, exhibited significant changes in its expression levels in response to injection of each of the peptides. Also, we observed expression changes for Bcl6 target and corepressor genes under the influence of Selank and its fragments. Our results showed that Selank and its fragments caused a number of alterations in the expression of genes involved in inflammation. The data obtained confirmed the participation of Selank in the processes of regulation of inflammation in the body. The complex biological effect of Selank may be partially determined by the systematic effect of this peptide on genomic expression.
In clinical trials, the drug has shown to provide a sustained nootropic and anxiolytic effect, which is useful for the treatment of generalized anxiety disorder (GAD). Selank has an advantage over traditional anxiety treatments, such as benzodiazepines, as it has no sedating or cognitive side effects and no associated addiction or withdrawal syndrome. Selank also has very low toxicity with an overdose proving harmless even up to 500 times the effective dose. When released, the drug will be used as a 0.15% aqueous solution which is applied to the nasal mucosa in drops. It is thought that this is the best method for absorbing peptide based drugs. The drug can be used to suppress feelings of fear and anxiety in people with anxiety disorders and to stimulate learning and memory in healthy people.
Selanks method of action is entirely unique of most other nootropics. It is thought to modulate the concentration of monoamine neurotransmitters. This may have incredible benefits for cognition. Another recognized benefit is its alleged effects on brain-derived neurotropic factor (BDNF)
The work presents results of study of role of heptapeptide Selank--an anxiolytic from group of biologically active peptides--in compensation of disturbed psychic and homeostatic functions in monkeys. New data have been obtained which indicate that an intranasal administration of Selank produces long-term changes of the monkeys' behavior disturbed during neurosis: elimination of fear and aggression and an increase of orientational-explorative activity as well as facilitation of handling reactions and communicational relations. It has been established that on the background of the Selank there occurs a long compensation of disturbed psychic functions (processes of memory) and of homeostatic parameters. It has been shown that unlike the earlier studied neurohormones (thyroliberin and ACTH4-10), the antistressor Selank effects do not depend on the type of neurotic disturbances and have long-term compensatory character. Comparison of the data obtained on monkeys with results of similar studies on the more low-organized mammals (rodents) allow suggesting that the new peptide preparation Selank is a promising agent for correction of various psychoemotional disturbances (alarm- and depression-like disorders).
[Experimental optimization of learning and memory processes by selank].
AuthorsSemenova TP, et al. Show all Journal
Eksp Klin Farmakol. 2010 Aug;73(8):2-5. Article in Russian.
The effect of selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro), which is a synthetic derivative of the endogenous tetrapeptide tuftsin (stable with respect to tissue peptidases), on the learning and memory processes and metabolism of serotonin (5-HT) have been experimentally studied on Wistar rats. The animals were trained with food reward in 30 trials per day. Selank (300 microg/kg) or saline were injected after the 10th trial. Elaboration of conditioned reflex with food reward was continued 30 min later. Retention was tested 24 h, 7 and 30 days after treatment. A single injection of selank activated the metabolism of 5-HT in the hypothalamus and caudal brain stem for 30 min to 2 h. It was established that selank induces an increase in memory trace stability during 30 days. These findings provide direct evidence that selank, when injected during consolidation phase, can enhance memory storage processes. Nootrope activity of the selank is probably caused by its obvious effect on the level of serotonin and its metabolite in the brain.
I interpret this study to be one of those old studies where they give a rat certain choices and if the rat makes the incorrect choice he is punished. This is what they mean by "conditined active avoidance reflex", if I'm not mistaken. This study shows that rats with below normal learning abilities improve rapidly post selank administration.
The optimizing action of the synthetic peptide Selank on a conditioned active avoidance reflex in rats.
AuthorsKozlovskii II, et al. Show all Journal
Neurosci Behav Physiol. 2003 Sep;33(7):639-43.
Abstract The actions of the synthetic heptapeptide preparation Selank on learning and memory processes in rats with initially low levels of learning ability were compared with those in normal rats, using a method based on acquisition of a conditioned active avoidance reflex, with repeated administration of peptide 15 min before the start of training sessions for four days. The effects of Selank (300 microg/kg) were compared with the effects of the nootrope piracetam (400 mg/kg). These experiments showed that Selank significantly activated the learning process in rats with initially poor learning ability, with effects apparent after first dose on training day 1. The effect progressively increased on repeated administration of Selank: the total number of correct solutions increased and the number of errors decreased (p < 0.05). The maximum optimizing activity of Selank on learning in normal rats was seen on day 3 of repeated administration and training, i.e., after formation of the initial consolidation phase. The dynamic features of the development of the activating action of Selank and piracetam were described. Comparison of the results obtained here with data on the anti-anxiety actions of Selank suggested potential for its use in optimizing mnestic functions in conditions of elevated emotional tension.
[Effects of the new peptide anxiolytic drug selank on the cardiovascular system functioning and respiration in cats].
AuthorsGan'shina TS, et al. Show all Journal
Eksp Klin Farmakol. 2005 Jul-Aug;68(4):33-5. Article in Russian.
The effects of the new heptapeptide anxiolytic drug selank (300 mg/kg, i.v.) on the arterial pressure (AP), cerebral blood flow, heart rhythm, respiration, and the AP depression induced by acetylcholine injections was recorded in narcotized male cats. Selank produced a 32 +/- 4.3% decrease in the AP for the first 1-3 min after injection. The drug also induced a 24 +/- 2.8% increase in the cerebral blood flow for the first 5 - 10 min upon injection and then the blood flow was gradually restored on the initial level. The heart rate and the respiratory rate were not affected by the drug injections. Nor did selank influence the AP depression in response to the acetylcholine introduction.
It was posted on another forum that Selank is helping remove withdrawal symptoms from a chronic pain suffer who is prescribed opiates. That's very interesting as anyone who has ever withdrawn from opiates knows it's pure hell!!!
[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia].
AuthorsZozulia AA, et al. Show all Journal
Zh Nevrol Psikhiatr Im S S Korsakova. 2008;108(4):38-48. Article in Russian.
Sixty-two patients with generalized anxiety disorder (GAD) and neurasthenia were studied. The effect of selank (30 patients) was compared to that of medazepam (32 patients). Patient's state was assessed with psychometric scales (Hamilton, Zung, CGI). Enkephalin activity in the blood serum was measured as well. The anxiolytic effects of both drugs were similar but selank had also antiasthenic and psychostimulant effects. The clinical-biological study revealed that patients with GAD and neurasthenia had the decreased level of tau(1/2) leu-enkephalin which was correlated with disease duration, severity of symptoms related to anxiety and asthenia and autonomic disorders. The increase of this parameter and stronger positive correlations with anxiety level were observed during the treatment with selank mostly in patients with GAD.
Selank-induced normalizing effects on the integrative brain activity and biogenic amine level disorders due to antenatal hypoxia.
AuthorsSemenova TP, et al. Show all Journal
Ross Fiziol Zh Im I M Sechenova. 2006 Nov;92(11):1332-8. Article in Russian.
The effects of Selank synthetic analog of Tuftsin, representing the heptapeptide forming Thr-Lys-Pro-Arg-Pro-Gly-Pro, on behavior and serotonin/noradrenalin concentrations in brain were investigated in adult rats exposed to hypoxia during 14-16 days of gestation. It was revealed that injection of Selank (300 mkg/kg, i/p) increased 2--3-fold (p < 0.01) the sensory attention, facilitated 1.5-fold the learning capacity (p < 0.01), normalized exploratory activity in the open field and hole board, and recovered the balance of serotonergic and noradrenergic brain system activity. The data obtained demonstrate the possibility of Selank to compensate for long-lasting negative effects of antenatal hypoxia on integrative brain activity and brain monoamine level.
The inhibitory effect of Selank on enkephalin-degrading enzymes as a possible mechanism of its anxiolytic activity.
Zozulya AA1, Kost NV, Yu Sokolov O, Gabaeva MV, Grivennikov IA, Andreeva LN, Zolotarev YA, Ivanov SV, Andryushchenko AV, Myasoedov NF, Smulevich AB.
Examination of patients with various forms of anxiety and phobic disorders (according to DSM-4 criteria) demonstrated a considerable shortening of enkephalin half-life and reduced total enkephalinase activity in the blood during generalized anxiety, but not during panic disorders and agoraphobia. This was probably related to low blood concentration of endogenous inhibitors of enkephalin-degrading enzymes in patients with generalized anxiety disorders. Heptapeptide Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro), which attenuates behavioral anxiety reactions and does not cause side effects typical of most anxiolytics, dose-dependently inhibited enzymatic hydrolysis of plasma enkephalin (IC50 15 microM). Selank was more potent than peptidase inhibitors bacitracin and puromycin in inhibiting enkephalinases. These results suggest that high efficiency of Selank in the therapy of anxiety and phobic disorders, including generalized anxiety, is due to its ability to inhibit enkephalin hydrolysis.
P-1114 - Rapid and slow response during treatment of generalized anxiety disorder with peptide anxiolytic selank
Heptapeptide Selank approved for the treatment of Generalized Anxiety Disorder (GAD). Studies revealed that Selank acts as an anxiolytic with stimulatory and cognitive enhancing properties. Though time to treatment response significantly varied in patients and this issue has not been studied.
Individual treatment response analysis in Selank-treated patients with GAD.
To compare clinical state and EEG changes in patients with different time to treatment response to Selank.
20 patients aged 2452 y.o. with GAD according to DSM-IV were included. Selank was administered at the dose 2700 μg/day intranasally. Study utilized valid clinical scales and pharmaco-EEG.
40% of patients were rapid responders (RR) and characterized by abrupt reduction of whole set of symptoms in first 13 Days. At the Day 3 Hamilton Anxiety Rating Scale (HARS) mean total score [SD] reduced from 20.3[11.9] to 7.0[2.9] (p < 0.01). 60% of patients responded gradually (conventional responders - CR). Clinically significant changes of mean HARS total score from 16.1[7.2] to 6.2[4.7] were achieved at Day 14, p < 0.01. In contrast to CR, RR demonstrated obvious EEG-reaction after single dose (900 μg) with increase of beta-rhythm, decrease of theta- and low frequencies of alpha-rhythm (all p < 0.05). Initially RR and CR significantly differed by the score of asthenic and cognitive symptoms (p < 0.05).
Data that peptide anxiolytic drug Selank in patients with GAD exert significant individual variability of therapeutic effect, including rapid effectiveness, confirmed. RR had more asthenic and cognitive symptoms and characterized by a higher EEG-reactivity than CR.
The neurobiochemical spectrum of selank action combines mechanisms which are characteristics of antidepressants and psychostimulants: activation of the brain monoaminergic systems, dopamine synthesis and turnover, and modulation of the tyrosine hydroxylase activity.