An important part of working productively is making sure that you are taking full advantage of your after work hours. You have to unwind and de-stress to help you reach your full potential during the day. To this end we bring you the Rest and Relaxation capsule.
The first compound in the capsule is Magnesium in the form of an Amino Acid Chelate to assist with absorption of the metal. There have been over a dozen small scale studies examining the efficacy of magnesium supplication for treatment and prevention of anxiety and stress. A metanalysis of these studies found that magnesium may be a viable treatment for stress stemming from general clinical anxiety and premenstrual syndrome.[i] The authors stipulate that further study is required to confirm the outcomes of these trials, but the evidence so far is promising. It is hypothesized that magnesium exhibits it effects due to its interactions with the GABA receptor, the primary inhibitory neurotransmitter receptor in the mammalian brain. The Mg2+ ion sits in the GABA receptor blocking it until certain biochemical conditions are met. This results in the closing of calcium channels into neurons which decreases neuronal activity having a sedative effect. Potentiating the magnesium’s sedative effects is Valerian Root Extract (std. to 0.8% Valerenic Acid). Valerian Root Extract has been used as an herbal medicine for decades due to its sedative effects. What makes this preparation special is its standardization to 0.8% Valerenic Acid. This is one of the compounds with Valerian root that has been proven through clinical trials to be a positive modulator of the GABAA receptor. It increases Cl– permeability of the receptor which alters the internal charge of the neuron, making it more difficult to fire, causing a sedative effect.[ii] Valerenic Acid is special in that it binds only to very specific version of the GABAA receptor, limiting the peripheral side effects that other more promiscuous drugs carry. It also functions as a partial agonist of 5-HT5A receptor, a serotonin receptor that is found mainly in a brain region that has been implicated in the sleep-wake cycle.[iii]
This capsule also contains pure GABA, the most important inhibitory neurotransmitter. While GABA has not been shown to cross the blood-brain barrier, it can still reach the parts of the brain that do not have a proper blood brain barrier having some yet un-characterized effect. These capsules also contain the minor ingredients Chamomile extract, Passion Flower extract (standardized to 4% flavonoids), Lemon Balm extract, and Hops extract. While research is scarce on these extracts they have all been reported to have varying degrees of sedative effects that can help the user relax and drift into a peaceful sleep.
The final major ingredient in this capsule is melatonin, a hormone produced in the brain by the pineal gland that regulates the day night cycle. As humans age, we become less efficient at producing melatonin, which can effect our sleep. When we supplement melatonin, it can make up that natural loss. Melatonin effects sleep by activating the MT1 receptor in correlation with the length of night. Because of this, you can recalibrate your bodies sleep cycle with the help of supplementing melatonin, a common practice for people who travel between time-zones frequently.
To cap off the capsule is BioPerine. It was isolated from black pepper and patented with the purpose of increasing absorption of other chemicals. BioPerine has been licensed from Sabinsa for use in this blend to further enhance its relaxant and sleep inducing effects. While the exact mechanisms causing it to enhance absorption are still under investigation it is currently thought that by inhibiting glucuronidation enzymes that it prevents compounds from being metabolized for a longer time, thus allowing them to exert their effects for a longer period of time. You can read more about BioPerine at the manufacturers website http://www.bioperine.com/index.php/mechanismsofactions
[i] Boyle NB, Lawton C, Dye L. The Effects of Magnesium Supplementation on Subjective Anxiety and Stress—A Systematic Review. Nutrients. 2017.
[ii] Luger D, Poli G, Wieder M, Stadler M, Ke S, Ernst M, Hohaus A, Linder T, Seidel T, Langer T, Khom S, Hering S (2015). “Identification of the putative binding pocket of valerenic acid on GABAA receptors using docking studies and site-directed mutagenesis”. Br. J. Pharmacol. 172 (22)
[iii] Dietz, B.; Mahady, G.; Pauli, G.; Farnsworth, N. (2005). “Valerian extract and valerenic acid are partial agonists of the 5-HT receptor in vitro”. Molecular Brain Research. 138 (2)