Because the assay on human subjects was the only test at our disposal for the detection of the active extract fractions, we had no other choice than to perform the testing on ourselves if we wanted to carry on the work and bring it to a successful conclusion. In the self-experiment just described, a strong reaction lasting several hours was produced by 2.4 g dried mushrooms. Therefore, in the sequel we used samples corresponding to only one-third of this amount, namely 0.8 g dried mushrooms. If these samples contained the active principle, they would only provoke a mild effect that impaired the ability to work for a short time, but this effect would still be so distinct that the inactive fractions and those containing the active principle could unequivocally be differentiated from one another. Several coworkers and colleagues volunteered as guinea pigs for this series of tests.
Psilocybin and Psilocin
With the help of this reliable test on human subjects, the active principle could be isolated, concentrated, and transformed into a chemically pure state by means of the newest separation methods. Two new substances, which I named psilocybin and psilocin, were thereby obtained in the form of colorless crystals.
These results were published in March 1958 in the journal Experientia, in collaboration with Professor Heim and with my colleagues Dr. A. Brack and Dr. H.
Kobel, who had provided greater quantities of mushroom material for these investigations after they had essentially improved the laboratory cultivation of the mushrooms.
Some of my coworkers at the time—Drs. A. J. Frey, H. Ott, T. Petrzilka, and F.
Troxler—then participated in the next steps of these investigations, the determination of the chemical structure of psilocybin and psilocin and the subsequent synthesis of these compounds, the results of which were published in the November 1958 issue of Experientia. The chemical structures of these mushroom factors deserve special attention in several respects. Psilocybin and psilocin belong, like LSD, to the indole compounds, the biologically important class of substances found in the plant and animal kingdoms.
Particular chemical features common to both the mushroom substances and LSD show that psilocybin and psilocin are closely related to LSD, not only with regard to psychic effects but also to their chemical structures. Psilocybin is the phosphoric acid ester of psilocin and, as such, is the first and hitherto only phosphoric-acid-containing indole compound discovered in nature. The phosphoric acid residue does not contribute to the activity, for the phosphoric-acid-free psilocin is just as active as psilocybin, but it makes the molecule more stable. While psilocin is readily decomposed by the oxygen in air, psilocybin is a stable substance.
Psilocybin and psilocin possess a chemical structure very similar to the brain factor serotonin. As was already mentioned in the chapter on animal experiments and biological research, serotonin plays an important role in the chemistry of brain functions. The two mushroom factors, like LSD, block the effects of serotonin in pharmacological experiments on different organs. Other pharmacological properties of psilocybin and psilocin are also similar to those of LSD. The main difference consists in the quantitative activity, in animal as well as human experimentation. The average active dose of psilocybin or psilocin in human beings amounts to 10 mg (0.01 g); accordingly, these two substances are more than 100 times less active than LSD, of which 0.1 mg constitutes a strong dose. Moreover, the effects of the mushroom factors last only four to six hours, much shorter than the effects of LSD (eight to twelve hours).
The total synthesis of psilocybin and psilocin, without the aid of the mushrooms, could be developed into a technical process, which would allow these substances to be produced on a large scale. Synthetic production is more rational and cheaper than extraction from the mushrooms.
Thus with the isolation and synthesis of the active principles, the demystification of the magic mushrooms was accomplished. The compounds whose wondrous effects led the Indians to believe for millennia that a god was residing in the mushrooms had their chemical structures elucidated and could be produced synthetically in flasks.
Just what progress in scientific knowledge was accomplished by natural products research in this case? Essentially, when all is said and done, we can only say that the mystery of the wondrous effects of teonanácatl was reduced to the mystery of the effects of two crystalline substances—since these effects cannot be explained by science either, but can only be describe.
A Voyage into the Universe of the Soul with Psilocybin
The relationship between the psychic effects of psilocybin and those of LSD, their visionaryhallucinatory character, is evident in the following report from Antaios, of a psilocybin experiment by Dr. Rudolf Gelpke. He has characterized his experiences with LSD and psilocybin, as already mentioned in a previous chapter, as "travels in the universe of the soul."
Where Time Stands Still
(10 mg psilocybin, 6 April 1961, 10:20)
After ca. 20 minutes, beginning effects: serenity, speechlessness, mild but pleasant dizzy sensation, and "pleasureful deep breathing."
10:50 Strong! dizziness, can no longer concentrate .
10:55 Excited, intensity of colors: everything pink to red.
11:05 The world concentrates itself there on the center of the table. Colors very intense.
11:10 A divided being, unprecedented—how can I describe this sensation of life?
Waves, different selves, must control me.
Immediately after this note I went outdoors, leaving the breakfast table, where I had eaten with Dr. H. and our wives, and lay down on the lawn. The inebriation pushed rapidly to its climax. Although I had firmly resolved to make constant notes, it now seemed to me a complete waste of time, the motion of writing infinitely slow, the possibilities of verbal expression unspeakably paltry - measured by the flood of inner experience that inundated me and threatened to burst me. It seemed to me that 100 years would not be sufficient to describe the fullness of experience of a single minute. At the beginning, optical impressions predominated: I saw with delight the boundless succession of rows of trees in the nearby forest. Then the tattered clouds in the sunny sky rapidly piled up with silent and breathtaking majesty to a superimposition of thousands of layers—heaven on heaven—and I waited then expecting that up there in the next moment something completely powerful, unheard of, not yet existing, would appear or happen -
would I behold a god? But only the expectation remained, the presentiment, this hovering, "on the threshold of the ultimate feeling." . . . Then I moved farther away (the proximity of others disturbed me) and lay down in a nook of the garden on a sun-warmed wood pile—my fingers stroked this wood with overflowing, animal-like sensual affection. At the same time I was submerged within myself; it was an absolute climax: a sensation of bliss pervaded me, a contented happiness—I found myself behind my closed eyes in a cavity full of brick-red ornaments, and at the same time in the "center of the universe of consummate calm." I knew everything was good—the cause and origins of everything was good. But at the same moment I also understood the suffering and the loathing, the depression and misunderstanding of ordinary life: there one is never "total,"
but instead divided, cut in pieces, and split up into the tiny fragments of seconds, minutes, hours, days, weeks, and years: there one is a slave of Moloch time, which devoured one piecemeal; one is condemned to stammering, bungling, and patchwork; one must drag about with oneself the perfection and absolute, the togetherness of all things; the eternal moment of the golden age, this original ground of being—that indeed nevertheless has always endured and will endure forever—there in the weekday of human existence, as a tormenting thorn buried deeply in the soul, as a memorial of a claim never fulfilled, as a fata morgana of a lost and promised paradise; through this feverish dream