GABAiclin is a trademarked extract of Scutellaria baicalensis, standardized for 30% of the main active baicalin. Baicalin is a positive allosteric agonist for your GABAA receptors. -aminobutyric acid, aka GABA is your main inhibitory neurotransmitter that essentially tells your brain it’s time to get ready for sleep. Once baicalin binds to your GABAA receptor, it activates the receptor and elicits sedative, hypnotic, muscle relaxant and anxiolytic(anti-anxiety) properties. This is the same mechanism and receptor that a class of sleep medications known as benzodiazepines interacts with. Baicalin has been shown to increase slow-wave sleep(deep sleep), as well as REM(rapid eye movement) sleep. REM sleep is extremely valuable to your body, as it releases growth hormone(GH) to help aid in recovery.
MagnaSleep is an extremely potent form of magnolia bark extract(MBE), standardized for 90% of two powerful active phenolic compounds: magnolol and honokiol. These two bioactives also act on your GABAA receptors to help reduce anxiety and prepare your body for sleep. MBE has been used for thousands of years in Chinese and Japanese tradition medicine for help promote sleep and reduce anxiety. Magnolol and Honokiol both have very high binding affinity to your GABAA receptors, specifically interacting with the benzodiazepine binding site. This binding potentiates the sleep inducing-effect of baicalin. Since magnolol and honokiol can quickly be metabolized via glucuronidation, a hefty 25mg dose of BioPerine(black pepper extract) was added to inhibit this process.
Cussonia zimmermannii is an African herb that has been studied for bioactive constituents that modulate your GABA receptors to induce sleep. The rootbark extract of C. zimmermannii has some very unique compounds known as polyacetylenes that have an extremely high affinity to GABAA receptors. These compounds have been shown to promote restfulness sleep, as well as staying asleep longer.
Hesperidin is one of the main bioactive compounds from citrus peel extract. It is a polyphenolic compound that has been shown to induce sleep, but does not act on the GABA receptor or benzodiazepine binding site. Studies show hesperidin interacts with your extracellular signal-regulated kinases 1/2(ERK1/2), located in the cortex and cerebellum. Hesperidin inhibits the activity of ERK1/2, which may be linked to sedation. Studies show that hesperidin can induce sleepiness and enhance sleep, and may potentiate other sleep-promoting compounds that activate your GABAA receptors.
Apigenin is a polyphenolic flavonoid that is one of the most abundant and well-studied. Apigenin’s mechanism of action is not directly on the GABA-benzodiazepine receptor, but does modulate its’ activity. Studies show it has a synergistic effect when combined with GABAA agonists, like baicalin, magnolol and honokiol. It has been shown to reduce locomotor activity, which prevents restlessness and may help induce sleep. One study showed subjects taking apigenin slept for longer durations vs the placebo. Apigenin is also subject to glucuronidation, so absorption is critical. With 25mg of BioPerine added to prevent this metabolism, you can be sure that the large dose of apigenin will be absorbed and utilized.
I formulated SLEEP because I have had sleeping issues all of my adult life. I have tried countless over-the-counter sleeping aids, melatonin, as well as 11 different pharmaceuticals. This combination of ingredients at clinical doses has dramatically improved my ability to fall asleep, my biggest issue, as well as stay asleep, my 2nd biggest issue. I scoured papers to look for natural sleep-enhancing compounds and I truly believe this formula will help anyone looking to get more restful sleep to help fully recover not only from exercise but from mental stress, as well.
Read The Studies On The Ingredients Below
1. Chang HH, Yi PL, Cheng CH, et al. Biphasic effects of baicalin, an active constituent of Scutellaria baicalensis Georgi, in the spontaneous sleep-wake regulation. J Ethnopharmacol. 2011;135(2):359-368.
2. Shi, Yuan, et al. "Herbal insomnia medications that target GABAergic systems: a review of the psychopharmacological evidence." Current Neuropharmacology 12.3 (2014): 289-302.
3. Ai, Jinglu, Xiaomei Wang, and Mogens Nielsen. "Honokiol and magnolol selectively interact with GABAA receptor subtypes in vitro." Pharmacology 63.1 (2001): 34-41.
4. Squires, Richard F., et al. "Honokiol and magnolol increase the number of [3 H] muscimol binding sites three-fold in rat forebrain membranes in vitro using a filtration assay, by allosterically increasing the affinities of low-affinity sites." Neurochemical research 24.12 (1999): 1593-1602.
5. Chen, Chang-Rui, et al. "Magnolol, a major bioactive constituent of the bark of Magnolia officinalis, induces sleep via the benzodiazepine site of GABAA receptor in mice." Neuropharmacology 63.6 (2012): 1191-1199.
6. Senn, Martin W. Structures and evaluation of biologically active constituents of" Cussonia Zimmermannii" harms. Diss. University_of_Basel, 2006.
7. Martínez, M. Cecilia, et al. "Hesperidin, a flavonoid glycoside with sedative effect, decreases brain pERK1/2 levels in mice." Pharmacology Biochemistry and Behavior 92.2 (2009): 291-296.
8. Fernández, Sebastián P., et al. "Synergistic interaction between hesperidin, a natural flavonoid, and diazepam." European journal of pharmacology 512.2-3 (2005): 189-198.
9. Fernández, Sebastián, et al. "Sedative and sleep-enhancing properties of linarin, a flavonoid-isolated from Valeriana officinalis." Pharmacology Biochemistry and Behavior 77.2 (2004): 399-404.
10. Salehi, Bahare, et al. "The therapeutic potential of apigenin." International journal of molecular sciences 20.6 (2019): 1305.
11. Kim, Jae-Wook, et al. "Enhancement of pentobarbital-induced sleep by apigenin through chloride ion channel activation." Archives of pharmacal research 35.2 (2012): 367-373.
Gazola, Andressa C., et al. "Involvement of GABAergic pathway in the sedative activity of apigenin, the main flavonoid from Passiflora quadrangularis pericarp." Revista Brasileira de Farmacognosia 25.2 (2015): 158-163