Neurotransmitters by
Ray Sahelian, M.D.
Definition of a
Neurotransmitter A neurotransmitter is defined as a chemical
messenger which is released from the synaptic terminal of a neuron at a
chemical synapse that diffuses across the synaptic cleft and binds to and
stimulates the post-synaptic membrane. In simple words, a neurotransmitter
is a chemical messenger released from one nerve cell which makes its way
to another nerve cell where it influences a particular chemical reaction
to occur. Neurotransmitters contro major body functions including
movement, emotional response, and the physical ability to experience
pleasure and pain.
The neurotransmitters that are most familiar to the
public are serotonin,
norepinephrine, dopamine, acetylcholine,
and GABA.
Types of
Neurotransmitters Neurotransmitters can be broadly classified
into several categories: Small molecule transmitters and neuroactive
peptides. Around 10 small-molecule neurotransmitters are generally
recognized: acetylcholine, 5 amines, and 3 or 4 amino acids, Purines,
(Adenosine, ATP, GTP and their derivatives). Fatty acids
Neuroactive peptides have been found, among them neuropeptide Y and
hormones such as leutenizing hormone. Single ions, such as the mineral
zinc are considered neurotransmitters by some. Gases such as nitric
oxide
Serotonin
Neurotransmitter Serotonin happens to be the most widely studied
neurotransmitter since it helps regulate a vast range of psychological and
biological functions. Serotonin (5-hydroxytryptamine or 5-HT) was first
identified in 1948. The wide array extent of psychological functions
regulated by serotonin involves mood, anxiety, libido, aggression, and
thinking abilities. Other brain neurotransmitters, such as dopamine and
norepinephrine, also influence mood and arousal. However, serotonin
generally has different effects. For instance, excess amounts of serotonin
cause relaxation, sedation, and a decrease in sexual drive. Prozac, a
common antidepressant of the SSRI type, elevates serotonin levels in the
brain. One of the common side effects of SSRIs is diminished sexual urge
and sensation. There is a nutrient called 5-hydroxytryptophan (5-HTP) that
is the immediate precursor to serotonin. When ingested as a supplement,
5-HTP converts in the brain into serotonin. The substance 5-HTP is often
used to treat depression and anxiety. I have noticed that 5-HTP
supplements decrease sexual interest.
Dopamine neurotransmitter Dopamine is one of the most important neurotransmitters
involved in the human sexual response. Dopamine has a significant effect
on sexual desire. Plus, elevation of dopamine levels often leads to an
improvement in mood and alertness. A number of psychiatric disorders,
particularly Parkinson's disease and mood disorders, are attributed to
imbalances in dopamine levels. Dopamine is made from the amino acid
tyrosine. Once produced, dopamine can, in turn, convert into the brain
chemicals norepinephrine and epinephrine. Some of the natural supplements
that increase dopamine levels include NADH and CDP-choline.
Acetylcholine
neurotransmitter Acetylcholine
was the very first neurotransmitter to be identified back in the early
1900s. It is made simply from choline, a natural substance found in
lecithin, and a two-carbon molecule called acetyl. Acetylcholine plays
numerous roles in the nervous system. In the brain, acetylcholine is
involved in learning and memory whereas in the genital organs,
acetylcholine is released by the parasympathetic nerves. Acetylcholine
helps in the release of nitric oxide, which leads to the relaxation of
smooth muscles and engorgement of the genital organs. Nutrients that
elevate levels of acetylcholine include choline and CDP-choline.
Norepinephrine
neurotransmitter and
Epinephrine In the flaccid state of the penis, frequent release
of norepinephrine from sympathetic nerves contracts the arteries in the
penis and also contracts the smooth muscles of the corpora cavernosum.
Therefore, in the normal state, norepinephrine keeps the penis soft. A
relative predominance of norepinephrine-induced contraction over nitric
oxide-mediated relaxation may contribute to erectile dysfunction. Two
amino acids phenylalanine and tyrosine, sold as supplements, are converted
into dopamine. Dopamine, in turn, is converted into norepinephrine, and
then epinephrine. The ingestion of these amino acids elevates dopamine and
norepinephrine levels, and hence will lead to alertness and mood elevation
and increased sexual interest. However, excess amounts of norepinephrine
and epinephrine may make it difficult to have erections. In addition, high
amounts raise blood pressure, increase heart rate, and cause anxiety,
irritability, and insomnia. Yohimbe, the natural sex booster from Africa,
facilitates erections by blocking the inhibitory action of norepinephrine
on the penis.
Nitric Oxide: Say Yes to
NO Nitric oxide (NO) is the most important neurotransmitter
involved in the engorgement of genital organs leading to erections. I will
mention NO several times Throughout this book, since some you will find
herbs and nutrients that help in the formation of this chemical. For
instance, the amino acid arginine can be metabolized into NO by an enzyme
known as nitric oxide synthase. This conversion is done in endothelial
cells, which are cells that line the inside of blood vessels. Ginseng, the
popular herbal aphrodisiac, is also thought to increase NO levels. NO
functions by activating an enzyme called guanylate cyclase. Guanylate
cyclase, in turn, helps form cyclic guanosine monophosphate (cGMP). cGMP
becomes the secondary messenger that causes smooth muscle relaxation,
resulting in venous engorgement and erections. Under normal conditions,
cGMP helps the smooth muscles surrounding the arteries of the penis and
the smooth muscles of the corpus cavernosum to relax. This allows blood to
easily flow into the penis. Any condition that interferes with the
signaling of these messenger enzymes can quickly lead to the breakdown of
the entire process and cause erectile dysfunction. Viagra works by
blocking an enzyme that breaks down cGMP, hence more of this chemical is
left to help dilate the genital arteries. Interestingly, having adequate
levels of androgen hormones in the body makes it easier for the genital
organs to respond to nitric oxide. Nitric
oxide is a biological messenger molecule produced by one of the essential
amino acids L-arginine by the catalytic action of the enzyme NO synthase
(NOS). The dual role of nitric oxide as a protective or toxic molecule is
due to several factors, such as; the isoform of NOS involved,
concentration of NO and the type of cells in which it is synthesised, the
availability of the substrate L-arginine, generation of guanosine
3,5'-cyclic monophosphate (cGMP) from soluble guanylate cyclase and the
overall extra and intracellular environment in which nitric oxide is
produced.
GABA
neurotransmitter In the adult central nervous system (CNS),
gamma-amino butyric acid (GABA) is a predominant inhibitory
neurotransmitter, and is involved in relaxation. Thus, dysfunction of the
GABA system is implicated in the pathophysiology of several
neuropsychiatric disorders, including anxiety and
depression. In mammals, 16 different
polypeptides (alpha1-alpha6, beta1-beta3, gamma1-gamma3, delta, epsilon,
pi, and theta) have been identified, using recombinant DNA techniques,
each of which is encoded by a distinct gene. The products of these genes
assemble in diverse combinations to form a variety of receptor subtypes
that have different sensitivities to a number of clinically relevant
compounds, such as the benzodiazepines (BZs). 2. Based on a number of
chromosomal mapping techniques, the majority of the GABA(A) receptor genes
have been localized, in man, in four clusters on chromosomes 4, 5, 15, and
the X. Furthermore, the genes that are present within these clusters have
a conserved transcriptional orientation. It has, therefore, been proposed
that the clusters arose largely as a consequence of two whole-genome
doublings that occurred during chordate evolution, and that the ancestral
cluster contained an "alpha-like," a "beta-like," and a "gamma-like"
subunit gene. Piracetam is a derivative of
GABA. Supplements of GABA are also available, however it is unclear how
effectively a GABA supplement can cross the blood brain
barrier.
Glutamate
neurotransmitter The role of glutamate receptors in synaptic
transmission and excitotoxicity in the nervous system is well established.
Recent evidence has emerged that glutamatergic mechanisms also exist in a
wide variety of non-neuronal cells. In the case of thymocytes and
lymphocytes, several types of glutamate receptor are expressed which can
induce functional changes. Glutamate may serve as a signaling agent
between the immune and nervous systems.
Histamine neurotransmitter
Histamine has many actions in both the periphery and in the
central nervous system. In the lungs, histamine acts the smooth muscle of
the smaller bronchioles to cause constriction, and reduced air flow. In
the stomach, histamine is involved in acid secretion.
Neurotransmitter testing A neurotransmitter test
is available to measure the levels of major neurotransmitters including
serotonin, norepinephrine, epinephrine, GABA and dopamine. This testing
can be done by urine, blood, or a spinal tap to measure neurotransmitter
levels in the spinal fluid. However, only in rare cases is it necessary to
do neurotransmitter testing. Even if we know the blood level of these
neurotransmitters, and we find a neurotransmitter deficiency, it offers
little help in guiding therapy since neurotransmitter levels and
neurotransmitter production fluctuates easily from day to day and hour to
hour. Neurotransmitter testing is not a reliable way to determine how a
person will respond to a particular medicines or supplement for conditions
such as depressions, anxiety, ADHD, etc. Neurotransmitter testing could
reveal a neurotransmitter imbalance that would be accurate for that
particular time period only. Neurotransmitter testing is appropriate in
cases of neurotransmitter imbalance or excess such as pheochrmocytoma and
other clear cut medical conditions.
Monoamine
neurotransmitter These include
serotonin, norepinephrine, GABA, glutamate, and dopamine. The monoamine
hypothesis holds that mood disorders are caused by a depletion in one or
more of these neurotransmitters.
Neurotransmitter
metabolism The process by which our bodies make, use, and break
down neurotransmitters is extremely complicated. When there is a
disruption within this process, abnormalities can occur in any of their
essential functions.
Acetylcholine is derived from Choline Serotonin
[5-Hydroxytryptamine (5-HT)] is derived from Tryptophan GABA is
derived from Glutamate Histamine is derived from Histidine
Epinephrine, norepinephrine and dopamine are derived from
Tyrosine Adenosine is derived from ATP Nitric oxide is derived from
Arginine
Neurotransmitter release Neurotransmitters are
responsible for transmitting information across the synaptic gap between
neurons. Neurotransmitters are stored in synaptic vesicles. When action
potentials are conducted down an axon, synaptic vesicles attach themselves
to the presynaptic membrane, then break open and spill neurotransmitter
into the synaptic cleft. Neurotransmitters in the synaptic cleft attach to
postsynaptic receptor sites and trigger an action potential in the
postsynaptic membrane. Some neurotransmitters attach to presynaptic
neurotransmitter receptors (autoreceptors) located on the membrane
(pre-synaptic membrane) of the cell that originally released
them.
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