For any chemical to qualify as a spirit molecule, it must at least possess psychedelic effects. Does melatonin’s striking chemical similarity to DMT and 5-methoxy-DMT mean that it also is profoundly psychoactive?
Some early studies suggested that melatonin has mind-altering properties. For example, administering high doses before bedtime seemed to induce vivid dreams. However, it is difficult to interpret those older studies. They were not looking for, nor did they measure, psychedelic effects of melatonin. There was only one way for me to find out if melatonin was psychedelic, and that was to administer it to my own human volunteers.
After completing my psychiatric residency, I spent a year in Fairbanks, Alaska, working at the local community mental health center. My experience in the Arctic introduced me to the new field of “winter depression.” This syndrome revitalized interest in the human biology of the pineal gland and melatonin. Research into their role in winter depression held promise for helping us understand and treat a wide range of seasonal human syndromes. This astonishing coincidence provided me a context for beginning to probe the pineal’s mysteries. However, I knew little about human research, so I sought ways to further my training.
I moved to San Diego to take up a year-long fellowship in clinical psychopharmacology research at the University of California. I learned how to write scientific proposals and grants, design experiments, and administer research drugs in a clinical environment. I gave and scored rating scales, collected blood and other biological samples, and analyzed and wrote up data.
Following a San Diego colleague, Jonathan Lisansky, M.D., to Albuquerque, I began working under the guidance of Glenn Peake, M.D., a pediatric endocrinologist. Glenn was the Scientific Director of the University of New Mexico’s General Clinical Research Center, an outstanding research site funded by the U.S. National Institutes of Health. Glenn, Jonathan, and I performed a comprehensive three-year study of melatonin effects in normal human volunteers. Out of this emerged the first, and so far only, documented role for melatonin in human physiology: melatonin contributes to the early morning drop in body temperature.
There is a daily rhythm in many biological functions in humans. One of the most robust is body temperature, in which there is a sharp dip at 3 A.M. This also is when melatonin levels are highest.
We studied nineteen male volunteers who stayed awake all night in light that was bright enough to prevent any melatonin formation. The drop in body temperature was not nearly as deep as normal in these melatonin-deprived men, and we wondered if the lack of melatonin was responsible. Administering melatonin back to the volunteers caused body temperature to fall in a typical manner. From these results, we proposed that melatonin plays a major role in the early morning temperature drop found in all of us.10
Most important to me were results from several rating scales that measured the psychological properties of melatonin. My reading led me to hope for some profound mind-altering effects of this pineal product. However, we found that melatonin produced little more than sedation and relaxation.
I was disappointed by the lack of significant mind-altering effects of melatonin. So, toward the end of this project, when I got a call late one night from the research unit telling me that one of our volunteers accidentally received about ten times the normal dose of melatonin, it was difficult to mask my excitement. This might be very interesting. If low doses of melatonin had such timid effects, this accident might breathe some life into my pursuit of its psychological properties.
I listened carefully to the research nurse’s description of how the staff miscalculated the delivery rate of melatonin. It seemed an honest mistake. In addition, the volunteer’s heart rate and blood pressure were holding up fine. It was his state of mind, however, that drew most of my concern.
“How’s he doing?” I asked.
“Well,” she yawned, “I’m having an awfully hard time keeping him awake to fill out his rating scales. He can’t keep his eyes open.”
“He’s not hallucinating or anything?” I offered hopefully.
“No such luck for you, Dr. Strassman,” she laughed in reply.
“No, no, I’m glad he’s fine,” I said, quickly returning to a more professional tone.
This event, more than any other, convinced me that melatonin was not psychedelic. However, my reading continued to persuade me that the pineal gland was the prime site in which to search for a spirit molecule. Let’s turn to that information, and the ideas that developed while pondering it. In doing so, we’ll begin to consider a DMT-forming function for the pineal gland.
4
The Psychedelic Pineal
Even before I began the melatonin study, my review of the literature indicated it might not be the spirit molecule. I wondered if the pineal gland made other compounds with psychedelic properties. However, while still in the early stages of my career, and well before I began outlining my DMT project, I quickly discovered how controversial these ideas could be.
In 1982 I undertook a year of clinical psychopharmacology research training at the University of California in San Diego. While I concentrated mostly on the relationship between the thyroid gland and mood, I also learned everything I could about the pineal gland.
One of my teachers was Dr. K., an authority on biological rhythms, melatonin, and sleep. Halfway through my fellowship training, I decided to share with him some of my nascent ideas about a psychedelic role for the pineal. We were walking along one of the innumerable halls of the San Diego Veterans’ Administration Hospital. Our conversation was rambling and wide-ranging. There was a pause, and I took the chance.
“Do you think,” I offered, “that the pineal might produce psychedelic compounds? It seems to have the right ingredients. Maybe it somehow mediates spontaneous psychedelic types of states—psychosis for example.” I was hesitant to get much deeper than this and avoided mentioning my more controversial ideas about the pineal—that it played a role in more exotic states, such as near-death or mystical experiences.
Dr. K. stopped in his tracks and turned on his heels. His brow furrowed and he peered at me intently through his glasses. A palpable menace glinted from his eyes. “Oops,” I thought.
“Let me tell you this, Rick,” he said very slowly and firmly. “The pineal has nothing to do with psychedelic drugs.”
That was the last time that year I said the words pineal and psychedelic in the same breath to anyone.
Nevertheless, I continued examining the literature and began developing some of the theories that inform this book. Further study of other scientists’ work, and the results of my own later melatonin research, added to the body of evidence upon which I drew in formulating the following proposals.
These hypotheses are not proven, but they derive from scientifically valid data combined with spiritual and religious observations and teachings. Many of these ideas are testable using available tools and methods. The implications of these theories are profound and disturbing but also create a context of hope and promise.
The most general hypothesis is that the pineal gland produces psychedelic amounts of DMT at extraordinary times in our lives. Pineal DMT production is the physical representation of non-material, or energetic, processes. It provides us with the vehicle to consciously experience the movement of our life-force in its most extreme manifestations. Specific examples of this phenomenon are the following:
When our individual life force enters our fetal body, the moment in which we become truly human, it passes through the pineal and triggers the first primordial flood of DMT.
Later, at birth, the pineal releases more DMT.
In some of us, pineal DMT mediates the pivotal experiences of deep meditation, psychosis, and near-death experiences.
As we die, the life-force leaves the body through the pineal gland, releasing another flood of this psychedelic spirit molecule.
The pineal gland contains the necessary building blocks to make DMT. For example, it possesses the highest levels of serotonin anyw
here in the body, and serotonin is a crucial precursor for pineal melatonin. The pineal also has the ability to convert serotonin to tryptamine, a critical step in DMT formation.
The unique enzymes that convert serotonin, melatonin, or tryptamine into psychedelic compounds also are present in extraordinarily high concentrations in the pineal. These enzymes, the methyltransferases, attach a methyl group—that is, one carbon and three hydrogens—onto other molecules, thus methylating them. Simply methylate tryptamine twice, and we have di-methyl-tryptamine, or DMT. Because it possesses the high levels of the necessary enzymes and precursors, the pineal gland is the most reasonable place for DMT formation to occur. Surprisingly, no one has looked for DMT in the pineal.
The pineal gland also makes other potentially mind-altering substances, the beta-carbolines. These compounds inhibit the breakdown of DMT by the body’s monoamine oxidases (MAO). One of the most striking examples of how beta-carbolines work is ayahuasca. Certain plants that contain betacarbolines are combined with other plants that contain DMT to make this psychedelic Amazonian brew, which allows the DMT to become orally active. If it weren’t for the beta-carbolines, MAO in the gut would rapidly destroy this swallowed DMT, and it would have no effect on our minds.
It is uncertain whether beta-carbolines by themselves are psychedelic. However, they do markedly enhance the effects of DMT. Thus, the pineal gland may produce both DMT and chemicals that magnify and prolong its effects.
Under what circumstances might the pineal gland make DMT instead of the minimally psychoactive melatonin? For this to happen, there needs to be an overriding of one or more of the following constraints normally preventing pineal DMT production:
The cellular security system around the pineal gland;
The presence of an anti-DMT compound in the pineal gland;
The low activity of the methyltransferase enzymes that produce DMT; and
The efficiency of the monoamine oxidase enzymes’ breakdown of DMT.
The guiding principle of the first wave of human DMT research was to compare DMT and schizophrenic states. Therefore, this was the context in which scientists studied these four different elements of the human DMT system. From these psychosis studies, we can extract data supporting my hypotheses about how the pineal may make DMT.
My emphasis on the relationship between DMT and psychosis, therefore, is not because I believe that this is the only role for endogenous DMT. Rather, psychosis is the only naturally occurring altered state of consciousness for which we have any real data. I believe that other “spontaneous psychedelic” conditions, such as near-death and spiritual experiences, also share a similar relationship with endogenous DMT. Those studies, however, have yet to be performed.1
Most likely, the primary factor inhibiting excessive pineal DMT production is the supremely efficient pineal security system discussed in the last chapter. The best-known example of this defense is the difficulty we encounter when trying to stimulate daytime melatonin production.
Adrenaline and noradrenaline, the neurotransmitters that stimulate nighttime melatonin formation, collectively are called catecholamines. Nerve cells nearly touching the pineal gland release these catecholamines, which activate specific receptors on pineal tissue and thus initiate melatonin synthesis.
The adrenal glands also produce adrenaline and noradrenaline, releasing them into the bloodstream in response to stress. However, when blood-borne adrenal catecholamines approach the pineal, the nerve cells around the pineal immediately take up and dispose of them. Therefore, circumstances in which adrenal catecholamine release occurs, such as in times of stress or during exercise, don’t stimulate daytime melatonin formation.
We performed a research study that demonstrated this quite clearly. Elite athletes ran a high-altitude marathon, spending much of it above 10,000 feet. We measured melatonin before and after the race. For many of the runners, this was “nearly” a near-death experience. Yet melatonin levels in these athletes rose only to those observed at night during normal sleep—hardly an explosion of brain chemistry! Nevertheless, we did see that it is possible to override the pineal’s defense shield if the stress is great enough.2
Neuroscientists believe this barrier to pineal activation exists because it would be problematic for an animal to experience its environment as “dark” during daylight hours. Since the pineal normally releases melatonin only at night, daytime melatonin release would “feel” as if it were dark at the “wrong” time, and the animal would be disoriented.
However, this explanation is weak. Daytime melatonin secretion is hardly “dangerous” enough to merit such a complex and efficient security system. Melatonin effects are not immediate, but rather take hours to days to materialize. In addition, daylight almost instantly suppresses melatonin production to near zero, returning the system to baseline before any internal disruptions occur.
However, consider what might happen if stress easily triggered the pineal to produce DMT, rather than melatonin. DMT is physically immobilizing and produces a flood of unexpected and overwhelming visual and emotional imagery. Certainly, frequent bursts of DMT release would be much more dangerous for an animal than would be those of melatonin.
It may be that melatonin is so hard to make during the day because any breach in the pineal security system is intolerable. The pineal erects a barrier to inordinate stress that protects equally everything behind it. So, one set of circumstances in which pineal DMT may form is when stress-induced catecholamine output is just too great for the pineal shield to withstand.
It also is possible that the pineal security system does not function normally in psychotic individuals. There are strong indirect data supporting this idea. Stress worsens hallucinations and delusions in psychotic patients. DMT levels in those patients are related to the degree of psychosis—the more intense the symptoms, the higher the levels of DMT. We know that DMT also rises in animals exposed to stress. More common levels of stressinduced catecholamines may overwhelm inadequate pineal defenses in psychosis, thus producing too much DMT. This DMT then brings on or worsens symptoms in psychotic patients.3
Another factor normally protecting the body from pineal production of psychedelic amounts of DMT resides within the pineal gland itself. A particular kind of small protein, first discovered in blood, has been shown to interfere with the activity of the DMT-forming enzymes. The pineal has quite high levels of this protein, a sort of “anti-DMT.” If this inhibitor itself were blocked, DMT formation is more likely. Where better to provide an anti-DMT for preventing potentially dangerous excessive DMT formation than where it is made—in the pineal gland?
Data from psychosis research also support this contention. Individuals with schizophrenia received pineal gland extracts as an experimental treatment in the 1960s. Their symptoms improved markedly. The explanation for this finding was that the pineal extracts provided patients with an additional dose of the anti-DMT that their own pineal glands lacked. Thus, they were better able to combat pathologically high levels of DMT, and their psychotic symptoms improved.4
Two other possible brakes on DMT production in the pineal relate to enzymes: those that produce and those that break down the spirit molecule within the body.
Researchers have found that the methyltransferase enzymes that form DMT are more active in schizophrenia than in normal conditions. This would raise production of DMT. Scientists looked at many human tissues for the source of this abnormal enzyme function, but unfortunately did not study the pineal gland.5
Finally, if the MAO system normally destroying DMT were defective, more DMT might linger and produce “psychedelic”/psychotic symptoms. MAO is less efficient in schizophrenics than in healthy volunteers, and it may be that schizophrenics do not clear DMT quickly enough from their systems. This also would result in DMT levels too high for normal mental function. While researchers examined MAO activity in several human tissues, they unfortunately did not assess pineal MAO activity in schizophrenia.
Let’s now con
sider less pathological, but also relatively common and naturally occurring, altered states of awareness in which pineal DMT may play a role. Dream consciousness is one of these.
The most likely time for us to dream is also the time at which melatonin levels are highest, that is, around 3 A.M. Since melatonin itself has such mild psychological effects, it suggests a role for another pineal compound whose levels parallel those of melatonin. DMT is a likely prospect for such a substance. However, no one has looked at 24-hour DMT rhythms in normal volunteers in an attempt to relate DMT levels to dream intensity or frequency.
Jace Callaway, Ph.D., has suggested that pineal derived beta-carbolines may mediate dreams. While the uncertain psychological effects of the beta-carbolines shed some doubt on this hypothesis, pineal beta-carbolines certainly could, by virtue of their DMT-boosting effects, indirectly stimulate dream production.6
Meditation or prayer also may elicit deeply altered states of consciousness. Pineal DMT production could underlie these mystical or spiritual experiences.
All spiritual disciplines describe quite psychedelic accounts of the transformative experiences, whose attainment motivate their practice. Blinding white light, encounters with demonic and angelic entities, ecstatic emotions, timelessness, heavenly sounds, feelings of having died and being reborn, contacting a powerful and loving presence underlying all of reality—these experiences cut across all denominations. They also are characteristic of a fully psychedelic DMT experience.
How might meditation evoke the pineal DMT response?
Several meditative disciplines bring about an intense fine-tuning of attention and awareness; for example, one-pointed focus on the breath. The brain’s electrical activity, as measured by the electroencephalogram, reflects this synchronization, or bringing together, of brain activity. Many studies have reported that experienced meditators produce brain wave patterns that are slower and better organized than those found in everyday awareness. The “deeper” the meditation, the slower and stronger the waves.
DMT: The Spirit Molecule: A Doctor's Revolutionary Research into the Biology of Near-Death and Mystical Experiences Page 8