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Valerian Root Extract: Complete Nootropic Guide

December 19, 2017

Valeriana officinalis or valerian is a flowering plant that has been use for thousands of years to help sleep and soothe the nerves. It is one of the oldest known natural remedies for anxiety in Europe, and it's use has been noted at least as far back as the ancient Greeks, where the roots of the plant were brewed into a valerian tea.

 

The medicinal anxiolytic (anti-anxiety) and sleep enhancing properties of the valerian plant come from its ability to enhance GABA (gamma-Aminobutyric acid) neurotransmission. 
 
GABA is the brain's natural sedative and reduces neural activity.

 

Valerian has been well-studied and we have a decent and reliable understanding of how the components of Valerian interact with GABA receptors.

 

Valerian is also one of our top herbs for anxiety.

Contents

 

Valerian Root Infographic
Biochemical Composition

Neurological Mechanisms

          GABAergic Mechanisms

          Dopaminergic Mechanisms

          Serotonergic Mechanisms

          Cholinergic Mechanisms

          Melatonergic Mechanisms

How to Take

          Standardisation

          Valerian Root Dosage

          Synergistic Compounds

Conclusion

Biochemical Composition

 

There are a large number of compounds in Valerian Root extract that may have bioactivity. The three main classes are:

 

Sesquiterpenes (valerenic acid, hydroxyvalerenic acid and acetoxyvalerenic acid).

 

Monoterpenoids (valtrate, isovaltrate, didrovaltrate and acevaltrate).

 

Flavanoids (hesperidin and 6-methylapigenin).

Neurological Mechanisms

 

GABAergic Mechanisms

 

Most of the relaxation effects of Valerian Root extract a due to valerenic acid.

 

Valerenic acid is a sesquiterpene, which is part of a class of organic compounds that generally have strong smells and are often produced by plants to attract larger animals that would remove the threat of small herbivores that eat such plants.

 

Valerenic acid is positive allosteric modulator of GABAA receptors. [R] Also called "PAMs", such compounds bind to GABA receptors but instead of directly activating them, they make them more sensitive so that they are more easily activated by other compounds, generally by the neurotransmitter GABA.

 

Secondary to valerenic acid, two flavanones in Valerian Root also have GABAergic action.

 

6-methylapigenin appears to have weak positive modulation effects on GABAA receptors, and hesperidin is a GABAA receptor agonist, although it is found in very low concentrations. [R]

 

These GABAergic functions make valerian root for anxiety very effective.

 

Dopaminergic Mechanisms

 

Valerian Root extract does not appear to have affinity for either the dopamine transporter nor any dopamine receptors.

 

Serotonergic Mechanisms

 

Valerian Root extracts and valerenic acid also appear to have some serotonergic effects, though this may occur at higher doses.

 

Specifically, it appears to be a fairly strong partial agonist of the 5-HT5A receptor, a very weak agonist of the 5-HT2B receptor, and also have a very weak affinity for the serotonin transporter. Molecules that displace neurotransmitter transports inhibit neurotransmitter re-uptake[R]

 

The 5-HT5A receptor is involved in the sleep-wake cycle, so Valerian's serotonergic effects may be related to it's ability to improve sleep quality.

 

Cholinergic Mechanisms

 

The sesquiterpines and one monoterpenoid in Valerian Root appears to have acetylcholinesterase inhibiting properties, and therefore may increase acetylcholine concentration and have some anti-dementia bioactivity. [R]

 

Melatonergic Mechanisms

 
Valerian root extract does appear to have affinity for the ML2 receptor in vitro but this effect is very weak and is unlikely to be relevant to supplementation. [R]

 

These effects on melatonin receptors are not likely the main cause for the effectiveness of valerian root for sleep.

​How to Take

 

Standardisation

 
Valerian root extracts are normally standardised to contain between 0.5% and 1.0% of the main active compound, valerenic acid.
 
0.5% is on the low end of this however and we recommend an extract standardised to contain at least 0.8% valerenic acid.

 

This usually means a 4:1 extract, where 4 kg of raw valerian root gives 1 kg of the concentrated extract.
 
Valerian root extract should also be taken with a small meal.

 

Valerian Root Dosage

 

When taking valerian for sleep, a single dose of 450 mg is recommended, about 1 hour before going to bed.

 

When taking valerian for anxiety, the recommended dose is 300 mg taken 2 or 3 times per day.
 
When combining with synergistic substances a lower dose may be sufficient.

 

Synergistic Compounds

 

Valerian root primarily acts as a positive allosteric modulator of GABAA receptors, meaning that it enhances the receptivity of GABAA receptors to an agonist.

 

Therefore, all GABAA agonists will be synergistic with valerian root extracts.

 

In respect to this, the herbal supplement that valerian root is most synergistic with is chinese skullcap, commonly called scutellaria baicalensis.
 

This plant contains two GABAA receptor agonists.

 

Our endogenous GABAA agonist is, of course, GABA itself, so all compounds that increase GABA concentrations will also be synergistic with valerian.

 

In respect to this, the herbal supplement that valerian root is most synergistic with is melissa officinalis, commonly called lemon balm. This plant contains a GABA transaminase inhibitor, which increases GABA concentrations.

Finally, "synergistic potentiation of anti-anxiety activity by valerian" has been found when used in conjunction with licorice root extract. The underlying mechanism at work is thought to be an increase in the absorption and bioavailability of valerian root extract.

 

If you want to find more supplements similar to valerian root extract, you can read this article on the best supplements for anxiety.

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