Epitalon (Epithalon, Epithalone)

Description:

Foitalon is a peptide derived from epithalamin, a hormone produced in humans by the pineal gland. It is an experimental agent, used most prominently in the area of anti-aging science. In animal studies, done with older lab rodents and monkeys, epitalon prolonged life span by more than 12-13 percent,1 increased insulin sensitivity2 and endurance,3 lowered body temperature,4 inhibited carcinogenesis,5 improved the digestion of whole foods,6 increased the uptake of glucose and amino acids,7 reduced DNA damage,8 and increased melatonin levels and decreased cortisol levels.9 In in vitro studies epitalon increased the vitality of cells, 10 increased the amount of times human cells can divide,11 made old cells function as young ones,12 and increased the quantity of protein old cells are able to manufacture.13 Epitalon’s working mechanism is unknown, but scientists suspect the drug interacts with an unidentified and universal receptor in cell membranes. We are not aware of human studies that have been published in peer reviewed scientific literature.

Human users report the healing of injuries that date from years back, improvement of sleep and mood, increase energy, and smoothening of wrinkles and lines in the face. Older athletes incidentally report an increase of strength and improvement of endurance.

History:

Epitalon was discovered by Russian anti-aging researchers from Saint Petersburg University. It was found by analyzing the potential bioactive compounds of the biological pineal extract Epithalamin, which has been used in Russia since the nineties. The Russians reported their discovery in 1999 at the Pan-American Congress on Gerontology and Geriatrics in San Antonio.14 Though early research has been promising in many regards, this remains a research product only.

How Supplied:

Epitalon is not available as a pharmaceutical product. No standard dosage information is available.

Structural Characteristics:

Epitalon is a peptide – a tetrapetide, to put it more precisely. Its molecule consists of a sequence of the amino acids Ala-Glu-AspGly.

Side Effects:

Epitalon has not been approved for use in humans. Its Safety and propensity for side effects may not be well understood at this time. We have not been able to find anecdotal reports of serious side effects by human users.

Administration:

As epitalon has not been approved for use in humans. Prescribing guidelines are unavailable. In animal studies epitalon has been administered orally and by subcutaneous and intramuscular injections. In most animal studies researchers administered epitalon subcutaneously. The human equivalent of the subcutaneous dosage used by scientists is approximately 0.8 micrograms/kilograms/day. The human equivalent of the oral dose is approximately 30 micrograms/kilograms/day. Underground experts, however, typically advise much higher doses. In most experiments, the Russians used epitalon for a limited period of 5 days, up to one month. Underground experts often advise users to take epitalon during a 2-3 weeks cycle.

Availability:

Epitalon in oral or intranasal products are available as ‘grey market’ supplements. Injectable versions, mostly powders that have to be reconstituted with bacteriostatic water, are sold as research chemicals. These injectables are available on the black market in underground-manufactured products only. At room temperature epitalon powder can be kept for 3 months, in the refrigerator for 2 years. Reconstituted epitalon can be kept in a refrigerator for 20 days. Epitalon should not be frozen.

1 Anisimov VN, Khavinson VKh, Popovich IG, Zabezhinski MA, Alimova IN, Rosenfeld SV, Zavarzina NY, Semenchenko AV, Yashin Al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology. 2003;4(4):193-202.

2 Goncharova ND, Vengerin AA, Khavinson VKh, Lapin BA. Peptide correction of age-related hormonal dysfunction of the pancreas in monkeys. Bull Exp Biol Med. 2004 Jul;138(1):80-3.

3 Vingradova IA, Iliukha VA, Fedorova AS, Khizhkin EA, Unzhakov AR, lunash VD. Age-related changes of exercise capacity and some biochemical indices of rat muscles under influence of different light conditions and pineal preparations. Adv Gerontol. 2007;20(1):66-73.

4 Anisimov VN, Khavinson Vkh, Zavarzina Nlu, Zabezhinskii MA, Zimina OA, Popovich IG, Shtylik AV, Arutiunian AV, Oparina TI, Prokopenko VM. Effect of pineal peptide on parameters of the biological age and life span in mice. Ross Fiziol Zh Im IM Sechenova. 2001 Jan;87(1):125-36.

5 Anisimov VN, Khavinson VKh, Popovich IG, Zabezhinski MA. Inhibitory effect of peptide Epitalon on colon carcinogenesis induced by 1,2dimethylhydrazine in rats. Cancer Lett. 2002 Sep 8;183(1):1-8.

6 Morozov AV, Khizhkin EA, Svechkina EB, Vinogradova IA, Ilyukha VA, Anisimov VN, Khavinson VKh. Effects of Geroprotectors on Age-Related Changes in Proteolytic Digestive Enzyme Activities at Different Lighting Conditions. Bull Exp Biol Med. 2015 Oct;159(6):761-3.

7 Khavinson Vkh, Egorova W, Timofeeva NM, Malinin W, Gordova LA, Gromova LV. Effect of Vilon and Epithalon on glucose and glycine absorption in various regions of small intestine in aged rats. Bull Exp Biol Med. 2002 May;133(5):494-6.

8 Rosenfeld SV, Togo EF, Mikheev VS, Popovich IG, Khavinson VKh, Anisimov VN. Effect of epithalon on the incidence of chromosome aberrations in senescence-accelerated mice. Bull Exp Biol Med. 2002 Mar;133(3):274-6

9 Khavinson Vkh, Goncharova N, Lapin B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro Endocrinol Lett. 2001 Aug;22(4):251-4.

10 Khavinson VK, Kvetnoii IM. Peptide bioregulators inhibit apoptosis. Bull Exp Biol Med. 2000 Dec;130(12):1175-6.

11 Khavinson VKh, Bondarev IE, Butyugov AA, Smirnova TD. Peptide promotes overcoming of the division limit in human somatic cell. Bull Exp Biol Med. 2004 May;137(5):503-6.

12 Chalisova NI, Linkova NS, Zhekalov AN, Orlova AO, Ryzhak GA, Khavinson VKh. Short peptides stimulate skin cell regeneration during ageing. Adv Gerontol. 2014;27(4):699-703

13 Khavinson VKh, Lezhava TA, Monaselidze JR, Jokhadze TA, Dvalishvili NA, Bablishvili NK, Trofimova SV. Peptide Epitalon activates chromatin at the old age. Neuro Endocrinol Lett. 2003 Oct;24(5):329-33.

14 Khavinson, V.Kh., Morozov V.G., 1999. Novel approaches to the prevention and treatment of age-associated pathology using peptide bioregulators-epithalamin and thymalin. Abstract of the Pan-American Congress on Gerontology and Geriatrics, San Antonio, p. 46.