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  #1  
Old 03-21-2015, 05:00 PM
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Epithalon, Epithalamin, Epithalone polypeptide

Epithalon, Epithalamin, Epithalone
Epithalon (A,G,A,G - Ala-Glu-Asp-Gly)

Epithalon (also known as Epitalon or Epithalone) is the synthetic version of the polypeptide Epithalamin which is naturally produced in humans. This pineal peptide preparation is secreted in the epithlamium-epiphyseal region of the brain. Its more prominent tasks are: to regulate metabolism in the epiphysis, increase the sensitivity of hypothalamus to its natural hormonal influences, normalize the function of the anterior pituitary, regulate the levels of gonadotropins and melatonin in the body. Epithalamin increases a person's resistance to emotional stress and also acts as an antioxidant.

Epithalamin was first discovered in the late 1980's by Prof. Vladimir Khavinson from St. Petersburg, Russia. It has been studied extensively ever since. It is known by several names, including Epitalon, Epithalon, Epithalone, Epithalamin and Epithalamine. Since all the patents are held by the Russian inventor there is not much interest for this tetra-peptide from the western big pharma industry. This makes the substance fairly unknown in the west due to the absence of marketing usually seen with big pharma products. In Russia it is currently in clinical studies and shows prospective results as treatment for liver disorders, neuropathology, psychiatry and geriatrics.

Human life extenssion via Telomerase activation and elongation of Telomeres

Epitalon is one of the very few substances which are able to activate Telomerase (telomere terminal transferase) enzyme in humans. Telomerase renews (elongates) the telomeres, which are responsible for protection of the human DNA from damage and cancer causing errors.

Treatment of aging cells in culture with Epithalon induced elongation of telomeres to the size comparable to their length during the early cell divisions. Epitalon treated cells with elongated telomeres made 10 extra divisions (44 passages) in comparison with the control and continued dividing. Thus, Epithalon prolonged the vital cycle of normal human cells due to overcoming the Heyflick cell division limit. (reference: V. Khavinson et all. in Bulletin of Experimental Biology and Medicine. June 2003, PMID: 12937682)

Epitalon used for Anti Aging

Epitalon decreases the age-related changes in immune and neuroendocrine systems, reduces the incidence of recurrent infections and chronic diseases. Long term clinical trials have shown that in patients with age-related pathology Epithalamin eliminates imbalance in prooxidation and antioxidation systems. (reference: N. Anisimov et all. Neuroendocrinology Letters, 2011, PMID: 11335874)

Results of 12-months treatment with Epithalon in patients with signs of accelerated aging showed normalizing effect on metabolism and condition of various functional systems. Elevated uric acid, alkaline phosphatase and cholesterol in elder patients returned to normal after 10 days of treatment, and remained stable in a several months peroid afterwards.

Epitalon effects

Experimental and clinical studies of Epitalon showed the following pharmaclogical properties of Epithalamin (Epitalon):

Telomerase activation (consequently, elongation of Telomeres)
regulates neuroendocrinous system
increases the hypothalamic sensitivity to the endogenous hormonal effects
decrease or suppression of proliferative changes in vaginal epithelium and endometrium in anovulatory phase
normalization of gonadotropic hormones levels (FSG, LG, prolactin)
positive influence on peripheral haemodynamics: improvement of blood rheology, decrease of intravessel thrombogenesis
regulation of the levels of reactants in the acute inflammation phase (c3-component of the complement, pre-albumin, C-reactive protein, alpha-orosomucoids
normalization of T-cell immunity
normalization of aqua-electrolyte balance indices
normalization of uric acid levels
normalization of Cholesterol
rejuvenation / strengthening of the immune system
inhibition of spontaneous and induced carcinogenesis (tumor prevention)


Epitalon side effects

There have been no reported side effects of Epithalon in any of the clinical and experimental trials. Likewise there are no reports of any Epithalamin adverse reactions on various internet forums, where people have been documenting repeated courses every 10-15 days for several years.

Epithalon dosage and course (cycle) duration

Dosage depends on the purpose and severity of the damage which is treated. Epitalon can be used orally (less effective and large dose) or injected intramuscularly or under the skin (more effective at much smaller dose).

1. Oral Epithalon use (least effective):
duration: between 10 - 20 days
dosage: between 400 - 600 mg of Epithalon per day
daily frequency:200 mg per serving, between 2 - 3 servings per day (depending on the dosage)

2. Epithalon as nasal spray or drops (medium effectiveness):
duration: between 10 - 20 days
dosage: between 15 - 30 mg of Epithalon per day
daily frequency:total daily dosage split into 3 servings throughout the day

3. Injectable Epithalon use (most effective):
duration: 10 - 20 days
dosage: between 5 - 10 mg per day (20 mg intravenous for terminal patients)
frequency of injection:1 injection per day for low dose, 2 injections for higher dose (divided between morning and late afternoon injection)

Each 10 - 20 days course of Epithalamin is followed by 4-6 months pause before repeating the course again. Epitalon treatment can be repeated indefintely.

Reconstituting (dissolving, mixing) Epitalon:

Plain sterile water for injection is the most suitable diluent for freeze dried Epithalamin (Epitalon). Alternatively it can also be reconstituted with bacteriostatic water (0.9% sodium chloride), normal saline (0.9% NaCl) or water containing 0.9% (9 mg/mL) of benzyl alcohol. It all works the same, but you probably want to use the least amount of aditives in the water - therefore plain sterile water.

Lyophilized (freeze dried) Epitalon usually comes in 10 mg vials. Gently inject 1 to 2 ml of water into the vial. Let it sit in refrigerator for 10 - 15 minutes. If there are any undissolved particles left after 15 minutes, gently rotate the vial between your fingers until all of the powder has dissolved and you are left with clear liquid.

Injecting Epitalon

Epithalon has a systemic effect regardless of the injection spot. It can be injected subcutaneously (under the skin) or intramuscularly (into the muscle). People usually inject it into the shoulder, tigh, buttocks or under the skin in the stomach fat area.

Proper storage of Epitalon:

If possible, always store both the freeze dried powder and the mixed solution in refrigerator (do not freeze).

Before mixing (lyophilized / freeze dried Epitalon powder):
refrigerated between 2 - 8 degrees celsius (36 - 46 Fahrenheit) it can be used for 24 months
at room temperature (up to 37 degrees Celsius or 98.6 Fahrenheit) it can be used for over 90 days

After reconstitution (liquid Epithalon):
liquid Epithalamin should be refrigerated between 2 - 8 degrees celsius (36 - 46 Fahrenheit) at all times. It should not be frozen.
once reconstituted, the Epitalon should be used within 20 days

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  #2  
Old 03-21-2015, 05:07 PM
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Epitalon (50 mg)
"Also known as Epithalon Tetra Peptide is a peptide used to regulate the cell cycle through up-regulation of telomerase activity (repairing of chromosomes).
The sequence of amino acids in the peptide is Alanine-Glutamate-Asparagine-Glycine. Animal studies have been done on the effects of Epithalon on suppression of spontaneous mammary tumors and spontaneous carcinogenesis. Studies have shown that the mode of action of Epithalon involves suppression of oncogene expression and modification of telomerase activity.

Science has shown that Epitalon is the most powerful factor ever found to stop the aging of the human body and to rejuvenate it. This is the only product that is scientifically proven in clinical studies in humans and in laboratory studies on cells.

The daily injection of 1-3 mg epithalon for ten days or several weeks every six months, to the elderly, namely the older members of the eminent Russian Academy of Sciences, has enabled many of them to increase their longevity. Mortality in this assembly was reduced by 30 to 50% over seven years in those who took it. Researchers of the St. Petersburg Institute of Bioregulation and Gerontology of the North-Western Branch of the Russian Academy of Medical Sciences and the Institute of Gerontology of the Ukrainian Academy of Medical Sciences (Kiev) clinically assessed the geroprotective effects of thymic (Thymalin) and pineal Epithalamin (Epitalon) peptide bioregulators in 266 elderly and older persons during 6-8 years both peptides were given at 10 mg daily for ten consecutive days once every 6 months. The bioregulators were applied for the first 2-3 years of observation. The obtained results convincingly showed the ability of the bioregulators to normalize the basic functions of the human organism, i.e. to improve the indices of cardiovascular, endocrine, immune and nervous systems, homeostasis and metabolism.

Homeostasis restoration was accompanied by a 2.0-2.4-fold decrease in acute respiratory disease incidence, reduced incidence of the clinical manifestations of ischemic heart disease, hypertension disease, deforming osteoarthrosis and osteoporosis as compared to the control.
Such a significant improvement in the health state of the peptide-treated patients correlated with decreased mortality rate during observation: 2.0-2.1-fold in the Thymalin-treated group; 1.6-1.8-fold in the Epithalamin-treated group; 2.5-fold in the patients treated with Thymalin plus Epithalamin as compared to the control. A separate group of patients was treated with Thymalin in combination with Epithalamin annually for 6 years and their mortality rate decreased 4.1 times as compared to the control.

Khavinson and others study abstract:
Twenty-five years of study have shown a wide spectrum of high biological activity of the pineal peptide preparation epithalamin (epitalon). Long-term exposure to epithalamin was followed by an increase in the mean and maximum life spans and slower rates of aging of rats, mice, and D. melanogaster.

Epithalamin increases pineal synthesis of serotonin, N-acetylserotonin, and melatonin and night pineal secretion of melatonin in adult and old rats. The pineal preparation decreases the luteinizing hormone and prolactin levels in adult male rats as well as the threshold of the hypothalamopituitary complex to feedback inhibition by estrogens in old female rats; it slows dawn age-related cessation of estrous function in rats and induces the recurrence of estrous cydes and fertility in old, persistently estrous rats.

Epithalamin increases the levels of triiodothyronine and decreases thyroxine in serum of adult rats. It further decreases the levels of corticosterone in the serum of mice and increases the susceptibility of the hypothalamo-pituitary complex to the homeostatic inhibition of adrenocorticotropic function by glucocorticoids in old rats. Serum insulin and triglyceride levels in rabbits are decreased by epithalamin and the tolerance to glucose and diuresis are increased.

With respect to immune function, it was found that T and B cell-mediated immunity in adult and old mice as well as the titer of thymic serum factor and the titer of thymosin-like compounds in old mice are stimulated by the pineal peptide preparation in the same way as the colony-forming activity of splenocytes in pinealectomized rats.

Epithalamin inhibits spontaneous and induced carcinogenesis and is a potent antioxidant, decreasing lipid peroxidation and stimulating the activity of CuZn superoxide dismutase.

The obtained results demonstrate a high efficiency of epithalamin therapy for prophylaxis of age-related pathology, including cancer, showing a new physiological way to slow down pathological processes and to extend human life spans.
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