Good quality, uninterrupted sleep is integral to
achieving optimal health. Without it, we fall prey to
a cascade of physiologic dysfunction that results
in increased body mass index (BMI), a decline in
cognitive performance1, increased risk of heart
disease and diabetes, hormonal imbalances,
immune system dysfunction, depression and
anxiety, and even vitamin D deficiency.
Stages of Sleep
Sleep is a complex phenomenon constituted by two
types of sleep patterns: non-REM (also called Slow
Wave Sleep) and REM. In an ideal sleep pattern, a
person experiences stages of sleep in non-REM and
REM phases. Slow Wave Sleep (non-REM) presents as
a high voltage slow wave electroencephalographic
pattern (alpha and delta waves), while REM sleep
exhibits a low voltage fast wave pattern (theta wave)
accompanied by eye movement. If either phase
is disrupted, sleep disturbance results. Although
stages of sleep accompanied by calming brainwave
activity is the natural circadian rhythm, 70% of
American adults report that they obtain insufficient
sleep at least one night a month, and 11% report
insufficient sleep every night. It is estimated that
sleep-related problems affect 50 to 70 million
Americans of all ages and socioeconomic classes.2
Because sleep deprivation is linked to increased
health risk, sleeplessness has become a public
health concern.
Root of Sleeplessness
At the root of impaired sleep quality may be a
number of underlying issues. Neurochemical
balance is key to achieving optimal sleep patterns.
However, the following may be contributing to a
neurochemical imbalance:
• Imbalance in neurotransmitter function
(GABA, serotonin and dopamine)
• Lack of precursors to make neurotransmitters
• Excess glutamate
• HPA-Axis Dysregulation
• Anxiety and stress
• Environmental factors
• Electromagnetic fields
Anxiety can be an instigator for sleepless nights
and seems to be the result of an imbalance in
neurotransmitter (GABA, serotonin and dopamine)
function. Excess glutamate, the main excitatory
neurotransmitter in the brain, results in low
gamma-aminobutyric acid (GABA), essential for
limiting the excitation of neurotransmitters and
fundamental for good-quality sleep.
Electromagnetic fields and blue light also play a
role in decreased melatonin production,3 necessary
for normal sleep cycles. Stress, common to 79%
of all Americans⁴, can yield excess cortisol or
insufficient cortisol production, both of which tip
the hormonal balance to wakefulness in the night.
Although each person’s neurochemistry is unique,
Alpha-Theta Ultra PM™ and Alpha-Theta PM™
are somnotropic formulas that incorporate key
nutrients recognized to induce calming brainwave
activity and promote the onset and duration of
high-quality sleep for most people by supporting
GABA receptor function, and healthy levels of
serotonin and dopamine.
Well-researched anxiolytic botanicals and nutrients
include L-theanine (Suntheanine®), Baikal Skullcap
(Scutellaria baicalensis), Lemon Balm (Melissa
officinalis), Passionflower (Passiflora caerulea), 5-HTP,
and Melatonin.
L-Theanine (Increases GABA and Dopamine Levels)
L-theanine (γ-glutamylethylamide) is an amino acid
found in green tea. A derivative of glutamic acid,
it is one of the most important neurotransmitters.
Fat-soluble, it is easily absorbed and crosses
the blood-brain barrier resulting in increased
dopamine and GABA levels in the brain⁵, and
increased production of calming brain alphawaves.
L-theanine has been shown to support
improved sleep quality not by sedation but
through anxiolysis.⁶
Protection Against Glutamate Toxicity
There is some evidence L-theanine offers
neuroprotective benefits partly due to the
antagonistic action of theanine on glutamate
subtype aMPA and kainite receptors. By acting
on the glutamine (Gln) transporter, it inhibits the
incorporation of extracellular Gln into neurons,
suppressing the conversion of glutamine to
glutamate by glutaminase.⁷ This antagonistic
activity plays a role in neuroprotection against
glutamate toxicity.⁸,⁹,1⁰
Optimizes Stress Response
In one study where subjects were given L-theanine
and a placebo and exposed to stressors to test
cortisol levels, the salivary cortisol response
was significantly reduced in the subjects taking
L-theanine when compared to the placebo.11
In another study, L-theanine intake resulted
in a reduction in heart rate (HR) and salivary
immunoglobulin A (s-IgA) responses to acute stress
relative to the placebo due to its effect on the
sympathetic nervous system. Overall, L-theanine
has been shown to cause “anti-stress effects” via the
inhibition of cortical neuron excitation.12
Increases Alpha Waves
L-theanine has been found to significantly increase
activity in the alpha frequency band, which is
associated with relaxing the mind.13
Boosts Brain-Derived Neurotrophic Factor (BDNF)
BDNF plays a central role in neural development
and cell survival and is essential to the molecular
mechanisms of synaptic plasticity. In one study,
L-theanine was found to increase expression
of BDNF protein in the hippocampus due to
its antagonistic action on the NMDA receptor,
one of the three glutamate receptors. Therefore,
L-theanine has been positively associate with
BDNF, a protein that increases neural plasticity
and promotes neurogenesis (dopaminergic and
serotonergic).1⁴
Improves Overall Sleep Quality
When evaluating L-theanine’s effect on sleep
quality, one study looked at boys diagnosed with
ADHD and found higher sleep percentage and
sleep efficiency scores, compared to those in the
placebo group.1⁵
Baikal Skullcap (Improves Overall Sleep Quality)
Scutellaria baicalensis Georgi, or Chinese skullcap,
has been widely used for its health-supporting
properties for thousands of years in China.
Flavones such as baicalin, wogonoside and their
aglycones baicalein wogonin are the major
bioactive compounds extracted from the root of S.
baicalensis.1⁶ Baicalin reports anxiolytic effects by
acting on the GABA(A) receptor site and exerts this
effect through the alpha2- and alpha3-containing
subtypes.1⁷,1⁸,1⁹ In addition, the neuroprotective
effects of S. baicalensis have been studied using
both in vitro and in vivo models yielding positive
results.20,21
Lemon Balm (Melissa officinalis)
Lemon balm is a perennial herbaceous plant in the
mint family that has been shown to improve sleep
quality.22 In a study of children with sleep bruxism,
Lemon Balm was administered, with and without
Phytolacca decandra. A significant reduction of
sleep bruxism was observed using the Visual
Analogic Scale, demonstrating increased calmness
during sleep.23 In another study, Lemon Balm
increased self-ratings of calmness and alertness,
mitigating the effects of stress, often the source of
sleeplessness.²⁴ These findings are also consistent
with the German Commission E recommendations
regarding the approval of Melissa officinalis L.
extract use for nervous insomnia.²⁵
Passionflower (Passiflora caerulea)
Passiflora caerulea, also known as blue
passionflower, is one of the most vigorous
and tender members the passionflower genus
Passiflora. Native to South America, its traditional
use has been as an anxiolytic. According to the
American Botanical Council, the components of
the fruit and flower that confer therapeutic benefits
include maltol, coumarin derivatives, flavonoids
(vitexin), and small amounts of essential oils.
Much of the evidence supports the anxiolytic and
sedative effects of Passiflora caerulea are due to
its high chrysin content.2⁶ Another animal study
demonstrated that the combined aqueous extract
of Melissa officinalis and Passiflora caerulea reduced
plasma corticosterone, the most important
biomarker associated with stress.27
5-Hydroxytryptophan (5-HTP)
5-HTP is the intermediate metabolite in
the biosynthesis of serotonin.28 L-theanine,
tryptophan and 5-hydroxytryptophan (5-HTP) all
are reported to promote relaxation by acting as
GABA receptor agonists, thereby boosting GABA
levels.29 In animals, 5-HTP is decarboxylated to
form serotonin, which is then either acetylated
to N-acetylserotonin or it is methylated to form
5-methoxytryptamin; these products are either
methylated or acetylated to produce melatonin,
which aids in sleep.
Melatonin
Melatonin functions in the regulation of sleep,
modulation of circadian rhythms and enhancement
of immunity, while retaining its ability to reduce
oxidative stress by processes that are, in part,
receptor-independent. This multifunctional
hormone mediates the body’s response to light
availability and signals its production in times
of darkness to prepare for sleep. Production of
melatonin decreases with age, which contributes
to sleep difficulties associated with aging.
Alpha-Theta PM™ is a powerful natural sleep aid
with all the benefits of Alpha-Theta Ultra PM™
without the melatonin.
Vitamin B6
Vitamin B6 is a cofactor in the tryptophan-serotonin
pathway. When using 5-HTP to enhance serotonin
and melatonin production, the activated form
of vitamin B6 helps to catalyze the conversion of
5-HTP to serotonin.
