La Valentonine : la véritable hormone du sommeil ?

Valentonin: the true sleep hormone?

What is valentonin?

Valentonin, or N-acetyl-3,4-dihydro-β-carboline, is a molecule believed to be derived from melatonin, a hormone naturally produced by the pineal gland. It belongs to the beta-carboline family, like its two sister molecules: melatonin and 6-methoxy-harmalan (6-MH). According to Professor Fourtillan's discovery, revealed in 2015 at the Academy of Pharmacy in Paris, valentonin is actually the true sleep hormone — challenging the role previously attributed to melatonin. LaNutritionHolizen

The nocturnal biochemical cascade

To understand valentonin, we must start with tryptophan, an essential amino acid obtained through diet. In the pineal gland, between 10 p.m. and 6 a.m., the biosynthesis of the three hormones occurs from serotonin, with successive formations of melatonin, 6-methoxy-harmalan, and then valentonin. These transformations take place through a cascade acetylation via N-Acetyl-Transferase (NAT). Professeur JoyeuxValentonine

The diagram is as follows:

Tryptophan → Serotonin → Melatonin → 6-Methoxy-Harmalan → Valentonin

These three hormones constitute a "biochemical cascade": they are formed successively from serotonin by three successive enzymatic acetylations, and secreted simultaneously by the pineal gland during the eight hours of sleep. Professeur Joyeux

Three hormones, three distinct roles

Melatonin (MLT) — the neuroprotective hormone

Melatonin is the neuroprotective hormone: it essentially "cleans" neurons that have been highly stimulated during the day. According to Fourtillan, it is therefore not the sleep hormone strictly speaking, but rather prepares the neurological ground for sleep to occur. Professeur Joyeux

6-Methoxy-Harmalan (6-MH) — the wakefulness hormone

6-methoxy-harmalan is the wakefulness hormone, preponderant and active during periods of wakefulness. It is the true agent of psychoses in case of excess — the dopaminergic hypothesis, although criticized but still current, should, according to Fourtillan, be abandoned. FamillessantepreventionProfesseur Joyeux

Valentonin (VLT) — the sleep hormone

Valentonin is the sleep hormone, preponderant and active during sleep. From 10 p.m. onwards, valentonin concentrations are higher than those of 6-MH. From 6 a.m. onwards, 6-MH concentrations again become higher than those of valentonin within a few minutes — triggering waking. FamillessantepreventionValentonine

Proposed mechanisms of action

The patents filed by Prof. Fourtillan (European patent EP3253378A1, international patent WO2016124688A1) detail the supposed actions of valentonin on the body.

During the period of valentonine prevalence over 6-MH, sleep results from the allosteric activation of 5-HT2c serotonergic receptors by valentonine. Furthermore, during nocturnal sleep, valentonine allosterically activates central α2 adrenergic receptors, which reduces blood pressure and heart rate during the rest period, as well as D1 and/or D2 dopaminergic receptors, leading to muscle relaxation. Homelie

Physiological sleep is recognizable by characteristic EEG patterns. It includes restorative deep slow-wave sleep and REM sleep, which is important for memory. Artificial or anesthetic sleep is entirely different: its EEG pattern mainly consists of light fast-wave sleep, which is not restorative, with little deep sleep. AgoraVox

An important particularity: valentonine, like most endogenous compounds, cannot be administered orally, so its administration must be transdermal. STM Cairn.info

Valentonine in animals: a universal vertebrate hormone

This is one of the most fascinating aspects of Fourtillan's theory: valentonine is not a strictly human hormone, but a mechanism shared by the entire vertebrate animal kingdom.

The two hormones 6-MH and VLT constitute the sleep-wake system that ensures the total regulation of the psychic and vegetative lives of the organism for 24 hours in all mammals and higher vertebrates. Famillessanteprevention

In humans and all nocturnal-sleeping mammals, such as dogs, the pharmacokinetic properties of valentonine and 6-methoxy-harmalan are perfectly adapted to maintaining the organism in sleep mode between 10 p.m. and 6 a.m., and then in wake mode between 6 a.m. and 10 p.m. Valentonine

Studies in dogs

Dogs played a central role in Fourtillan's experimental research, because, like humans, they are nocturnal-sleeping animals. Professor Fourtillan successfully synthesized valentonine and tested it on dogs, which, like us, are diurnal animals. Salud y Bienestar Natural

As always, the discoverer first experiments on animals to verify the effects of their discovery, comparing sleep with either a placebo or drugs considered to be sleeping pills, such as Stilnox and Valium, then with valentonine at different doses, using the intravenous route. The results are positive, reported on pages 63 to 71 of his book "The Pineal Gland and the Sleep-Wake System". Valentonine

These results were then confirmed by comparative EEG recordings, visible in the presentation video published on valentonine.fr, showing the comparison of electroencephalographic sleep recordings in dogs with a placebo, Zolpidem (Stilnox), Diazepam (Valium), and valentonine. Valentonine

It is highly probable that the values of pharmacokinetic parameters, both for the elimination kinetics of valentonine and 6-MH and for their distribution kinetics, are identical for humans and all nocturnal-sleeping animals, such as dogs. Homelie

Experiments in chickens

Poultry were also used in Fourtillan's early work. Professor Fourtillan explains in his book "The Pineal Gland and the Sleep-Wake System" (pages 56 to 62) the demonstration of valentonine's action on the sleep of chickens subjected to different lighting conditions. Le Quotidien du Médecin

This choice is not trivial. The pineal gland begins to function erratically when a light source enters the chicken coop. A lack of adequate pineal hormone secretion reduces egg production, disrupts the circadian rhythm, and leads to a wide range of behavioral alterations. The chicken is therefore a study model particularly sensitive to disturbances of the pineal system. Holizen

The Pineal Gland in the Animal Kingdom: An Ancestral Structure

To understand why valentonin would concern all vertebrates, one must grasp the antiquity of the pineal gland. In some reptiles and birds, the pineal gland, located just beneath the surface of the skull, directly senses external light intensity and thus allows for the adjustment of the animal's circadian rhythm — earning it the occasional designation of the "third eye" of primitive vertebrates. La-voie-de-l-ayurveda

In mammals, the pineal gland appears to have lost its function as an autonomous circadian pacemaker, a function it has retained in reptiles and birds. However, according to Fourtillan, it retains its function of secreting the three hormones of the sleep-wake cycle, common to all mammals. Valentonine

A remarkable case: in several species of whales and certain cetaceans, the pineal gland is said to be absent or non-functional, and certain genes associated with the production or action of melatonin are inactive — which could explain their ability to sleep with only one half of their brain at a time, without a fixed nocturnal cycle. Valentonine

Pathologies associated with valentonin deficiency

The most common neurological disorders — primary insomnia, sleep disorders, reactive and endogenous nervous depressions, and neurodegenerative diseases such as Parkinson's and Alzheimer's — are said to be due to quantitative deficits in the VLT/6-MH system, which should be restored. LaNutrition

Conversely, an excess of 6-MH during the day would be responsible for psychotic disorders, for which valentonin administered alone could play a corrective role.

It should also be noted that human beings are not equal in terms of the secretion of the three hormones by the pineal gland: a very high variability in melatonin secretion has been observed, with a factor of 13 between extreme pineal secretions. Since melatonin is the marker of overall secretion, this implies that the amount of valentonin produced varies just as much from one individual to another. Valentonine

Pathologies associated with valentonin deficiency

The most common neurological disorders — primary insomnia, sleep disorders, reactive and endogenous nervous depressions, and neurodegenerative diseases such as Parkinson's and Alzheimer's — are said to be due to quantitative deficits in the VLT/6-MH system, which should be restored. LaNutrition

Conversely, an excess of 6-MH during the day would be responsible for psychotic disorders, for which valentonin administered alone could play a corrective role.

It should also be noted that human beings are not equal in terms of the secretion of the three hormones by the pineal gland: a very high variability in melatonin secretion has been observed, with a factor of 13 between extreme pineal secretions. Since melatonin is the marker of overall secretion, this implies that the amount of valentonin produced varies just as much from one individual to another. Valentonine

The transdermal patch

Given the impossibility of administering valentonin orally, Fourtillan developed a system in the form of an adhesive patch. A two-reservoir transdermal patch containing valentonin and 6-methoxy-harmalan is applied at bedtime and removed upon waking in the morning to treat sleep disorders, depression, and neurodegenerative diseases. For psychotic disorders, a single-reservoir patch containing valentonin is applied upon waking in the morning and removed during the day before 10 p.m. Professeur Joyeux

Treatment for sleep disorders involves applying a two-reservoir transdermal patch at bedtime, which delivers approximately 50 micrograms of 6-methoxy-harmalan and 200 micrograms of valentonin over about 8 hours. Professeur Joyeux

What official science says

In the interest of transparency, it is necessary to recall the position of the scientific community. The existence of valentonin and/or its effects is highly contested: no studies or other scientists confirm it, and the scientific community is surprised that Jean-Bernard Fourtillan's research has not been published in peer-reviewed journals, but only as patent applications. Wikipedia

His work on melatonin, however, has been published in international journals (American Journal of Physiology, 2001; Dialogues in Clinical Neuroscience, 2002), which attests to recognized methodological rigor in this field. This also helps us understand that some researchers must use curiosity to push the rigid framework of current science to continue producing research. In our time, one must dare to go where few people have gone to make real discoveries. Valentonine is one such discovery, and like the story of "water memory," it opens up new horizons and debates for the common good.

Conclusion

Valentonin is a beta-carboline molecule proposed as the third link in a nocturnal biochemical cascade in the pineal gland. Far from being a purely human curiosity, it fits, according to Fourtillan's theory, into a universal hormonal system shared by all mammals and higher vertebrates — which experiments on dogs and chickens have sought to demonstrate. Its deficiency would explain a wide range of neurological disorders ranging from insomnia to Parkinson's and Alzheimer's. What is missing to date is confirmation by published independent studies — an indispensable step for this molecule to fully enter the field of evidence-based medicine.

At NaturaSounds, we believe that science sometimes advances off the beaten path, and that any serious hypothesis deserves to be known, discussed, and rigorously examined. We have been able to demonstrate on several occasions, particularly with water frequencies and especially our advances on the resonance frequencies of the 4th state of water, that there is still a tremendous amount of research to be done and produced for the common good.


Find the Valentonine therapeutic tuning fork by clicking on the image:


Sources:

Back to blog