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Full-Text Excerpt of…

5-HTP:

The Natural Alternative to Prozac®

by John Morgenthaler & Lane Lenard, PhD
$3.95 - softcover, 40 pages (Out of Stock)

Is 5-HTP the Same as Tryptophan?

No, although they are closely related amino acids. In fact, 5-HTP is a metabolite of tryptophan. This means that nerve cells use tryptophan to make 5-HTP. Brain researchers refer to tryptophan as a precursor of 5-HTP. 5-HTP, in turn, is a precursor of serotonin (Fig. 1). In other words, in order to make serotonin, nerve cells (with the help of special enzymes, vitamins, and other "co-factors,") take some tryptophan, which normally comes from the diet, turn it into 5-HTP and then turn the 5-HTP into serotonin.

Just as you can enhance your available serotonin by ingesting more tryptophan, you can also increase your serotonin supply by ingesting supplements containing the next amino acid in the metabolic chain -- 5-HTP -- and let the brain finish the job of making serotonin.

As a means of enhancing serotonergic activity, supplemental 5-HTP appears to have several advantages over tryptophan:

5-HTP is probably a more effective antidepressant than tryptophan.
A given molecule of 5-HTP is more likely to be converted to serotonin, compared with a given molecule of tryptophan; the body can convert tryptophan to any one of several other substances, in addition to 5-HTP. This suggests that a given dose of 5-HTP is more likely to be converted to serotonin than a given dose of tryptophan, and might also cause fewer unwanted side effects.
5-HTP easily crosses the blood-brain barrier and therefore gets into the brain far more readily than does tryptophan. Tryptophan molecules that do not pass into the brain may increase serotonergic activity in other parts of the body, such as the gastrointestinal tract, which may result in unwanted side effects.

So why not just ingest serotonin? This seemingly logical solution turns out not to work, because serotonin has an even harder time getting into the brain than does tryptophan. Most of the serotonin found in the brain is produced there.

The 5-HTP and tryptophan used in supplements are also produced in very different ways. As noted earlier, tryptophan is synthesized in a laboratory by a fermentation process, not unlike that used to make beer or wine. 5-HTP occurs naturally in the seeds of a West African medicinal plant called Griffonia simplicifolia. Production basically involves extracting the 5-HTP from these seeds.

What does the FDA say about 5-HTP? They have tried to tar 5-HTP with the same brush they've used on tryptophan. Their questionable line of reasoning seems to go something like this: 1) We believe uncontaminated tryptophan may cause EMS in some people, but we don't know why. 2) Both tryptophan and 5-HTP raise serotonin levels. 3) Therefore, 5-HTP is suspect as well.

The FDA points to two or three isolated cases where 5-HTP may have been associated with EMS or, more likely, EMS-like changes in people or experimental animals. Close examination of these cases shows no clear causal connection, however. In two of the cases, the patients were also taking the drug carbidopa, which alters the metabolism of 5-HTP and tryptophan, increasing the amount that reaches the brain; one of these patients was also taking the drug flunitrazepam (an anti-anxiety drug related to Valium® and Xanax®).11, 12 In the third case, it is not certain that 5-HTP was even involved.13

Why is Serotonin So Important?

Serotonin was first identified 50 years ago, and ever since scientists have been finding more and more functions for this ubiquitous substance. Even though the body contains only a tiny amount of serotonin (about 10 mg) at any one time, it is clear that serotonin plays an important role in many different bodily functions or phenomena, as shown in the box.

What Serotonin Does

Scientific studies have found that serotonin plays a vital role in each of the following functions, behaviors, or mood states:

Depression
Mood
Anxiety
Sleep
Appetite control
Memory
Learning
Temperature regulation
Sexual behavior
Hallucinations
Cardiovascular function
Skeletal muscle contractions
Endocrine (hormone) regulation
Blood clotting
GI motility — contractions of the stomach and intestines that move food along and promote digestion

Given these widespread functions, it is not hard to understand why, if the serotonin system goes awry, there could be profound changes in the way we feel, think, and act.

Serotonin Up ... Serotonin Down

For the most part, reduced serotonin activity in the brain results in conditions such as insomnia, depression, anxiety, increased appetite, loss of impulse control, increased aggressiveness, and others. To the extent that they help bring serotonin activity back into normal balance, 5-HTP, as well as Prozac and other drugs, can be extremely effective in restoring normal behavior, feelings, and thought processes.

Enhancing Serotonin: Two Different Approaches

Prozac and 5-HTP differ markedly in the way they enhance serotonergic function. Whereas, 5-HTP provides the raw materials for the body to make new serotonin, Prozac and other SSRI drugs interfere with the normal metabolism of serotonin in the synapse, preventing excess serotonin molecules from being naturally deactivated. Either way, the amount of serotonin available to stimulate serotonin receptor sites increases. Figure 2 illustrates schematically some of the key elements in the synthesis, metabolism, release, and receptor binding of serotonin.

Tryptophan from the diet (eg, turkey, tryptophan supplements) is taken up by nerve cells (neurons) where it is converted by specific enzymes to 5-hydroxytryptophan. 5-HTP molecules, in turn, are converted to serotonin (5-HT) molecules. These are contained in microscopic bubbles called vesicles and stored in neuron terminals until they're needed.

When an electrical nerve impulse reaches the terminal, it causes a few serotonin laden vesicles to explode out into the synapse. Once in the synapse, serotonin molecules can have three possible fates:

First, they may float across the synapse and bind to a specific serotonin receptor, designed, like a lock for a key, to match up with serotonin molecules.
Second, they may run into the enzyme monoamine oxidase (MAO), the sole purpose of which is to inactivate serotonin (as well as other neurotransmitters). Drugs known as MAO inhibitors can increase the amount of serotonin available for receptor binding by blocking the activity of this enzyme.
Third, they may return to the neuron from whence they came via a recycling process known as reuptake. Prozac and the other selective serotonin reuptake inhibitors (SSRIs) increase the amount of serotonin available in the synapse by preventing reuptake.

Coordinating the Infinite Complexity of Daily Living

Who we are, how we feel, what we do, how our bodies function: these comprise the sum total of billions of neuroelectrical micro-events involving the actions and interactions of relatively few molecules of serotonin and other neurotransmitters within the cramped confines of a few billion synapses.

Under normal conditions, the brain is well-equipped to handle the infinite complexity of neurochemical events that accompanies the events of daily living. Alter their natural flow and balance, though, and things can start to change very quickly. Reductions from normal serotonin levels in the brain or an imbalance between serotonin and other neurotransmitters can cause symptoms ranging from mild anxiety and depression to overeating, alcoholism, aggressive behavior, hallucinations, delusions, paranoia, and suicide.

Researchers at the University of Texas Houston Health Science Center found that reducing serotonin levels can have a rapid and profound effect on human behavior. They gave a serotonin-lowering dietary formula (doses of 25 gm or 100 gm) to 10 healthy men in a controlled laboratory setting following 24 hours on a low-tryptophan diet. This regimen had previously been shown to significantly reduce serotonin levels in the brain. The men taking the 100-gm formula (resulting in lower serotonin) showed a significant increase in aggressive behavior (compared with their baselines). This behavior change occurred within only 5 hours of ingesting the serotonin-lowering formula. The 25-gm dose took 6 hours to produce the same effect.14

As we shall discuss in the chapters that follow, replenishing serotonin by supplying additional 5-HTP has been shown to have a wide variety of beneficial effects, the best-documented of which is relief of depression.

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