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Article from "Whole Earth Review" No.57 Winter 1987 MAY YOU NEVER SLEEP - Cognition Enhancing Drugs by R.U. Sirius INTELLIGENCE INCREASING DRUGS might be labeled "Cognitive Enhancers," "Memory Enhancers," or, in some cases, "Psychic Energizers." What many of these drugs and nutrients have in common is that they produce effects similar to effects people are seeking from popular stimulants such as caffeine, amphetamines and cocaine. These popular drugs temporarily enhance cognition and memory, and amp up the user's energy levels only to leave the user depleted. Cocaine and amphetamines might properly be labeled as short-term intelligence-increase drugs and long-term intelligence-decrease drugs. However, the drugs and nutrients discussed in this review are all believed to create long term improvements in memory and cognition. Some of them also provide the short-term high-energy states associated with the stimulant drugs. Also, there is virtually no tendency towards the kind of weirdness and darkness of the spirit which so often accompanies even the occasional speed or cocaine high. It seems that while the illicit stimulants cause short-term release, but long-term depletion of norepinephrin, many of the memory-enhancing drugs and nutrients work on the noradrenergic nervous system in a different way, apparently modulating nerve cell control mechanisms so that the cellular response is neither too great nor too little. This is a gross oversimplification. More precise information on each of these cognitive enhancers is easily available to the serious researcher. Accurate and concise information for the layperson is easily available through the popular written works of Durk Pearson and Sandy Shaw who, whatever one might think of their bucket-of-pills-a-day personal regimen, do carefully monitor all of the research in this field. This survey deals primarily with the short-term experiential effects of these compounds, since I only have the experience of a relative and imprecise ongoing use of one drug, Pemoline, and no scientific proof of any intelligence increase on my part. Besides, a three-hour play can be realistically reviewed. Reviewing a life is a somewhat more dubious prospect. In consideration of all this, I hereby present a review of intelligence-increasing drugs. May you never sleep. VASOPRESSIN - Definitely the most euphoric of the memory-enhancing intelligence-increase drugs outside of the one being called "Euphoria" (more on Euphoria later), Vasopressin is marketed as Diapid, a prescription drug made by our old friends Sandoz. It can also be ordered as Vasopressin through chemical supply houses by those who know the ropes. I had five squirts of Vasopressin out of a nasal inhaler. I was surprised by how strong the effects were. I had that charged-up hyperconfident rush that one experiences with cocaine, but combined with much clearer ideation and without the numbing and discomfort or the strange and disquieting hard edges which often accompany even the more euphoric coke highs. It didn't last very long, about two hours, most of which unfortunately spent riding the BART and walking. By the time I got home, the experience had pretty well dissipated. I did not have an opportunity to experience Vasopressin as a work/writing drug. It was clear, however, simply from reading (I was reading "Gravity's Rainbow" at the time and I consider that a fairly challenging test of comprehension) on the BART ride home, that Vasopressin is an excellent tool for rapid learning and comprehension of complex systems of thought. The only other time I had Vasopressin, it was in the form of Diapid. I had only two squirts at a party late at night on top of fairly substantial amounts of marijuana and alcohol. It didn't noticeably cut through the depressant effects of those drugs. However, I did experience an intensified and prolonged orgasm! HYDERGINE - The invention of one Dr. Albert Hoffmann of Sandoz Laboratories. I know of many people who got their hands on buckets of this stuff and I know of nobody who continues to take it. The effects are said to be cumulative rather than immediate and everybody seems to lose interest. "I forgot to take my Hydergine" is a term which one often hears from chagrined "intelligence agents," fully cognizant (even without Hydergine) of the ironies involved. This probably says more about the people that I hang out with than about Hydergine as an intelligence increase agent. Incidentally, Dr. Hoffmann told a friend of mine that one can get exactly the same effects one gets from daily megadoses of Hydergine by using 25 micrograms of LSD daily. I have not experimented with subthreshold acid as an IQ substance, so I cannot comment. LECITHIN, CHOLINE with INOSITOL, PHENYLALANINE (with VITAMIN C and B6) - While perhaps less intriguing and glamorous to technophilic reality hackers, most of these easily available cognitive enhancers have a substantially perceptible effect. LECITHIN seems to be the exception. Even at "Durk and Sandy" dosage levels there was no noticeable enhancement of focus, recall, etc. CHOLINE and INOSITOL, at about three grams each, produce mild but definite results with no discomfort and can be used daily. I did this once for about a month and found myself losing my sense of humor. However, if you're already humorless you might just as well give this a go. PHENYLALANINE is quite speedy. While it can be used for creativity and focus, it tends to make one irritable. For emergency use only. DEANER - This is getting really popular with the "health food set." Experientially, the effect is very subtle but noticeable. I've tried this a few times and what I've found is that if I already have a task to do, I will do it and, in retrospect, I will realize that I sustained my attention for an unusually long time without flagging or needing a break. However, if I use this (as I often do with other cognitive enhancers) without a precise sense of what the task at hand is, it doesn't clarify and help to motivate activity. This is an important point. Drugs such as Vasopressin, Pemoline, Euphoria and THA can actually cut through confusion and ennui and help invoke will. My guess is that most of these substances also work, to varying degrees, on the pleasure centers of the brain, provoking one's natural 'joie di vivre' and thereby provoking enthusiasm for creative and organizational activities. PEMOLINE (usually combined with Magnesium) - The information most frequently passed around in reference to MAGNESIUM PEMOLINE was published by the Church of the Tree of Life some years ago in their publication "Bark Leaf". It recommends taking "Mag-Pem" at 50-100 mgs. every day for two months in order to substantially increase your I.Q. OUCH! This program is a sure ticket to severe headaches and extreme nervousness. However, in the 20-30 milligram range, I've found that this can be used twice weekly with excellent results. The lift is very substantial and noticeable. I, and several of my friends, find it particularly good for writing, both creative and functional. For rapid-fire associations and grand synthesis just combine it with moderate amounts of Cannabis (Sativa, if possible). It lasts about twelve hours, coming on slowly and having its greatest effect at around the fifth through the tenth hours. Clarity and verbal acuity are the strong points here. At times, the sheer mass of information, new thoughts and connections can overwhelm and put one into a rather confused state, particularly if one is not applying oneself to something. When this occurs I find that I can slow down my thoughts to a point where there is coherence simply by verbalizing them or writing them down. Unlike its close cousin "EUPHORIA," Pemoline is emotionally bland. It is not a pleasure drug. WARNING: from my observations, approximately one in every ten people get nothin' but headaches from even small doses of Pemoline. EUPHORIA - Well, someone took Pemoline, twisted it around a little bit and put a whole lot of pleasure into the equation. This might be a Dangerous drug! There are lot of different things that seem to happen with Euphoria. The first time I took it (40 milligrams - I've learned since that 25 mg. is considered your basic dose) I got really charged up. This is definitely a High and it comes on suddenly (about 45 minutes after ingestion). My first response upon coming on to it was an experience of an intense rush of perceived personal power. I found myself goosestepping down the busy Berkeley streets thinking about how good I felt, how successful I was destined to be, and knowing that the world was my oyster. After about 15 minutes of this as I found myself leaping down the BART escalator, I had to tell myself to slow down for fear that I would be completely drained later on. Although I didn't really slow down at all during this experience, I did bring myself into a somewhat more humane mindset and I spent the subway ride having an almost methoxylated amphetamine (MDMA, MDA, etc.)-type ideations. In other words, I wasn't just feeling good about myself, I was feeling good about most everybody else. The world was everybody's oyster. Arriving at my office, I immediately found myself doing organizational work at about three times the normal rate with far more self-assurance and fewer mistakes than usual. Simultaneously, I was entertaining perspectives on the nature of my true will and making important phonecalls which I had put off for some time. I did about thirty hours worth of work in about ten hours. I literally could not stop. I tried to make myself take a break for about ten minutes. Within a minute, I found my hand going into a drawer to pull out another file which needed reorganizing. Believe me, this is very unusual behavior. I hate organizational work. This all might sound like the first blushes of an amphetamine high, but he emotional overtones and the mentation under this substance is of a softer and more inwardly whole (less alienated) quality. As I've already indicated, the Euphoria high seems to have a slight methoxylated amphetamine quality to it. All in all, this was a very powerful experiencing of clarity, self-assurance and cognitive ability. The following day, I experienced the same sort of effects at about one-third the intensity. There was no burnout at all in aftermath. Subsequent experiments have shown Euphoria to be predictable as an effective tool for organizing binges, brainstorming sessions and radio talk-show appearances. It also seems to induce ongoing personal growth in terms of clarity of personal will. (I've received three other testimonies in this same direction.) As a writing tool, I've found Euphoria to be variable. It seems that verbal acuity comes on strong but the verbal circuits burn out quickly from intensity of use and one has to move on to less verbally oriented tasks. In other words, this is generally good for creative flashes and outlining grand syntheses but not too good for actual completion of written work. It gives one an impatience for minutiae and the kind of careful faceting that it takes to bring a work to completion. In terms of appreciation and comprehension of aesthetics and information, this seems the opposite of its close cousin Pemoline. The accessing mode favored is visual. One wants to explore a painting or photograph or watch a movie rather than read a book. My only complaint about Euphoria is that it lasts 16 hours, which feels about 4 hours too long. In two of my five experiences, the last four hours were spent feeling slightly "headachy" and weary, although there was still no burnout following sleep. I would say, at this point, that Euphoria should not be used more often than once a week since it is so powerful and so much energy is expended in the experience. This is easily the most Fun of the intelligence increasers and, as such, is probably the most likely to be abused. PRL-8-53 - Untried by your reviewer at this time. However, Durk Pearson is quoted in 'High Frontiers' as saying that "PRL-8-53 is a terrific memory enhancer. Normally you can memorize about seven or eight digits just by looking at them for a second. PRL-8-53 gives the average person a memory span of about 21 to 22 digits." He also reported that one amnesia victim was cured with one dose. THA - Untried by your reviewer at this time. Again, Durk Pearson, this time in 'High Frontiers/Reality Hackers Newsletter:' "In combination with arecoline, THA has been found to be remarkably effective as a memory improver ... it's important that the dosage be individualized ... too much will actually impair memory and produce sweating, excessive muscle tone and mouth-watering." The standard dosage is "1 to 2 mg." however, Durk recommends that you start with a quarter of that every two to four hours and work up - if you get those side effects, back off. =========================================== Letter to the Editor in response to the R.U.Sirius article above. From the Summer 1988 issue of "Whole Earth Review" --- IF THESE DRUGS HAD BOTTLES, HERE'S WHAT THE WARNING LABELS WOULD SAY I have been a big fan of your magazine for many years now, and I am a firm believer in the principle that the free exchange of information is a necessity to the survival and progress of our species. I commend you for your efforts in this area. Unfortunately, when it comes to psychopharmacology the old saying, that a little knowledge is far more dangerous than none at all, is quite often true. Specifically I am referring to the article of winter '87 on page 56, "Cognitive Enhancers." I am not upset that you would print this sort of information; there is both interesting and important research going on in this field right now. What I object to is the uncritical, inaccurate, and incomplete information given in an area that has Serious implications on your reader's health. Here are some errata and addenda for that article, most of this information is available in the "Physician's Desk Reference" and the "Merck Index". VASOPRESSIN - It is a naturally occurring peptide that can cause a wide variety of effects beyond those mentioned in the article. It strains the heart by reducing the heart's food and oxygen supply and increasing the heart's workload by increasing blood pressure. In individuals with hidden or overt heart problems, this can mean a heart attack. In addition vasopressin can cause a dangerous elevation in brain fluid pressure, leading to stroke, coma, or death. Also it can produce vertigo, circumoral pallor, pounding headaches, cramps, diarrhea, gas, nausea, vomiting, urticaria, difficulty breathing, anaphylactic shock, and normal shock. It is dangerous to use in people with a history of epilepsy, migraine, asthma, heart failure, or poor kidney function. Vasopressin can have dangerous interactions with most stimulants, including pemoline, caffeine, diet pills, and cold medications. Overall vasopressin is a real Pandora's Box, but fortunately there is ongoing research to develop safer and more effective alternatives. CHOLINE, INOSITOL, VITAMIN B6, PHENYLALANINE, and DEANER - These compounds are both basically safe and effective if not spectacular. I would add a few notes though. Use caution with these if you have a history of epilepsy. Choline may be more effective when taken with inositol. B6 is more effective and better for you when taken in wide-spectrum mega-B vitamin supplements. PHENYLALANINE is neurotoxic and can cause brain damage in about 2% of the population [uploader's note: the 2% with the metabolic disorder PKU, that is], and it's probably not good in large doses for anyone. TYROSINE on the other hand is not toxic and is a more effective substitute. DEANER can be made more effective by combining it with METHIONINE, but be cautious of large doses of methionine if you have a history of psychosis. In addition, there are other nutrients that are save and effective in increasing psychological energy in most people, INOSINE, CYTOCHROME C, LYSINE, and GINSENG. HYDERGINE - It is an ergot alkaloid, the same chemical class as LSD, but with no psychedelic or immediate effects. It is currently prescribed to help alleviate some of the symptoms of Alzheimer's disease, but, despite the tremendous numbers of people with this affliction, Hydergine is not widely used, mainly because it is only effective in about 1/3 of the people using it. As a matter of fact it worsens cognition in about 1/3 of people. It is dangerous to use in individuals with any history of psychosis, low or high blood pressure, heart disease, pregnant women (at any point in pregnancy), or a history of migraines. Hydergine has caused rashes, drug fever, headaches, dizziness, vision problems, appetite loss, nausea, vomiting, cramps, fainting, sluggishness, drowsiness, emotional withdrawal, apathy, nervousness, hostility, confusion, depression, weakness, collapse, and coma. EUPHORIA - The section on Euphoria is really in a muddle. First of all it is not clear what Euphoria is. The chemical structure shown is the article is MDA (methylenedioxy amphetamine), a drug rejected long ago by both psychologists and users as inferior to MDMA (XTC); it is also Highly Illegal. The other name given for Euphoria was 3,4-Methylenedimethoxy Methamphetamine. This is an impossible chemical structure. Technically speaking, a chemical structure can contain a methylenedioxy group or have 2 methoxy groups; there is no such thing as a methylenedimethoxy group. None the less I can guess about Euphoria's toxicology from the effects R.U.Sirius describes and the class of drugs to which he claims it belongs. Like crystal methedrine it is almost certainly capable of precipitating paranoid psychosis, even in psychologically stable people. Though Sirius noticed no crash, he may have just been lucky. Amphetamines almost always have a crash. In general they also create tremendously large egos, and over confidence, so No judgement on mental improvement made by people under their influence can be trusted. Finally Euphoria is relatively untested, both scientifically and on the street. Its long and short term health effects are unknown by based on its chemical structure it would not be unreasonable to expect it to cause heart damage, brain damage, or cancer. I do not expect Euphoria to be any better than Coke or Speed, in the long run. I don't mean to sound cruel or cynical, but let some lab rats die before you put your neck on the line. PEMOLINE is an interesting drug at the center of some current research. Unfortunately, it is not known how the drug works. If it was, a safer alternative could be found. Pemoline has caused fatal liver failure, still births, La Tourette's Syndrome, seizures, hallucinations, uncontrollable movements of the tongue, lips, face, eyes, and extremities, depression, delirium, dizziness, irritability, headaches, drowsiness, insomnia, anorexia, nausea, and cramps. Caution should be used when combining it with any other drug because it is known to have strong dangerous interactions with many drugs. Finally, pemoline, a controlled substance, is recognized by the government as having an abuse/addiction liability. PRL-8-53 - I could find no information on this, even in the most up to date references. The fact that it still is referred to by its code number probably means that it is still highly experimental; they may not even know what its structure is yet. It might be safe, but you are playing neurochemical roulette. THA - This is potentially very dangerous. It is an acetylcholinesterase inhibitor making its actions closely related to Nerve Gas, Pesticides and Strychnine. BE CAREFUL! I wish you all good luck in your quest for personal growth. I am sure in the near future science will come up with many things to help you. Please do not let enthusiasm interfere with accuracy and safety Name withheld upon request ========================================================================== Uploader's Notes: The previous letter is interesting in that the writer makes an erroneous assumption about the structure of Euphoria based on an erroneous and mislabeled diagram in the original R.U.Sirius article. Euphoria is NOT related to the methamphetamine class of drugs as this writer assumes! Euphoria IS however related to Pemoline (as R.U.Sirius implies in the text of his article), so the warnings above about Pemoline may well apply to Euphoria. The writer of this letter also makes a wrong assumption about PRL-8-53; namely, that it is so new that there's no info about it available yet. At the end of this file, there's an article out of "The Daily Breeze" Newspaper (which I don't have a date for, but it was published in either 1980 or 1981) that explains the origin of PRL-8-53. Strangely, R.U.Sirius didn't identify the chemical structure of PRL-8-53 either, even though he knew it was being investigated by Durk Pearson! ======================================================================== Yet More Letters to the Editor in response to the R.U.Sirius article above. From the Winter 1988 issue of "Whole Earth Review" --- NO EUPHORIA ABOUT CHEMICAL STRUCTURE In your Winter '87 issue, you ran an article by 'R.U.Sirius' entitled: "May You Never Sleep" dealing with personal use(s) of experimental or FDA licensed materials which your article collectively termed 'cognitive enhancers.' Some of these are prescription only drugs, others come from underground chemistry. Psychedelics generally have continued to receive erroneous, confused & even hysterical press stemming from the LSD chromosome scare of the mid-sixties through & into today's supposedly better informed press & reporters having, among other things, computer technology to aid in getting the facts straight. Or so one would think. Or at least hope. However, I'm sorry to say that 'Whole Earth Review' has perpetuated this same disregard for the facts of the matter not in one issue (Winter 1987) but again in your Summer 1988 issue, surrounding the same subject - U4Euh (Euphoria). In Sirius' original piece, he presented a completely False chemical identification diagram re: U4Euh, showing instead that if MDA, a completely different substance altogether. We all make mistakes, but Sirius AGAIN put his foot in his mouth, appearing in the June issue of 'Whole Mind" & calling U4Euh N-Methyl Aminorex, which is again false. In the Summer WER there is a letter of rebuttal to Sirius' article which attempted to once & for all (I suppose) set the facts straight, particularly about U4Euh. Here again, an attempt at correction dis-information IN ACTUALITY ends up spreading further myths surrounding U4Euh & psychedelics. The letter writer states: "finally, U4Euh is relatively untested, both scientifically & on the street, etc...." OK. Let's get some facts straight & clear up a lot of confusion about this substance U4Euh. U4Euh (4-Methyl Aminorex) was 1st discovered by a research group headed by Georde Poos at McNeil Laboratory in Ft. Walsh, PA. in the early 1960's. The 1st published report appeared in 'The Journal of Med. Chem." in 1963 [1] & several other patents were issued in Belgium, France & the US [2,3,4]. Three other papers were published regarding U4Euh in 1963 & 1966 [5,6,7]. In the mid 1980's, U4Euh was resurrected within the underground & noncontrolled experiments were carried out on humans. The substance's new spokesman was named The Friendly Stranger & samples were studied at, among other places, the Continental Rainbow Gatherings. Both instructional manuals as WELL as ongoing research results were distributed to those having interest & concern about U4Euh & its effects. There are two forms of U4Euh currently available via the underground - the free-base & the hydrochloride. Prices range from $75 pre gram for the hydrochloride upwards to $150 per gram for the most powerful free-base. This substance (4-Methyl Aminorex) was placed on schedule I by the DEA & the FDA in 1987. The resultant scheduling report presented by the DEA shows a Death associated with its use (or abuse). Unfortunately psychedelics or 'cognitive enhancers' remain the legendary, obscurely attractive sources for 'bad press' - & are kept illegal - BECAUSE false, misleading, obtuse or hysterical reporting (like that perpetuated in your WER) outweighs the true facts of the matter. I hope that author R.U.Sirius & WER continue to provide insightful articles in the area(s) of drug use/abuse. However, some attempt must be made to provide accurate reporting, especially in areas already worked over by too much of the same. Best wishes, Thomas Lyttle, Publisher, Psychedelic Monographs and Essays References: [1] Journal of Medicinal Chemistry 6, 266 (1963) [2] Belgian Patent 628,803, June 16, 1963 [3] French Patent M2448, May 4, 1964 [4] U.S.Patents 3,161,650 Dec 15, 1964 and 3,278,382 Oct 11,1966 [5] Archives Int. Pharmacodyn. Ther. 164(2) 412-18 (1966) [6] Journal of Pharm. & Experim. Therapeutics 140: 367-374 (1963) [7] Ibid. 141:180-84 (1964) [8] Journ. Clin. Pharmacology 7:296-302 (1967) [9] Science 1982 218(457)487-490 [10] Annual Reviews of Med. Chemistry 1965 51-58 (1966)44-47 The above mentioned references were provided by 'Psychedelic Monographs & Essays' from an upcoming piece entitled: "A Chemical and Pharmacological Review of Euphoria or Intellex" by 'The New Age Chemist'. This piece will appear in the Autumn 1988 (vol.4) issue of PM&E. --- ANOTHER ALCHEMIST WHO AGREES Dear Friends, I read with interest the article in issue #57 on intelligence drugs by "R.U.Sirius." I also read the same author's letter correcting the depicted structure and identification of "Euphoria" in issue #58. I too noticed that the chemical structure on page 58(#57) was that of 3,4-methylene dioxymethamphetamine (mistakenly spelled as "3,4-Methylene Dimethoxy Methamphetamine"). while it was incorrectly labeled as "EUPHORIA." The label was meant to say "chemically related to MDA." The label was however, correct in stating that it was "Ecstacy." In "Sirius's" letter (#58, page 140) correcting his article in issue #57, he (?) states that "Euphoria is N-Methyl Aminorex and looks like this - C6H5 O NH2 \/ \/ | || [uploader's note: THIS IS THE CORRECT U4EUH.] |___N / CH3 Well, this structure is not that of N-Methyl Aminorex. It is correctly called 4-Methyl Aminorex. Aminorex has the structure: [Diagram of Aminorex] And the structure of N-Methyl Aminorex is as follows: [Diagram of N-Methyl Aminorex] I am not yet sure what the correct chemical structure of "Euphoria" is but I am sure of the above information. Perhaps this will help clear up the misunderstanding. "Sirius," maybe you could try again to enlighten us? What is the correct structure and name of "Euphoria"? Yours sincerely, The Alchemist Vashon, Washington =========================================================================== Article from "The Daily Breeze" newspaper, published around 1980 or 1981 Chemical Found to Improve Memory OMAHA (AP) - Creighton University researchers say they have discovered an organic chemical compound which apparently improves memory and intellectual performance that normally deteriorate with aging. Dr. Nikolaus Hansl, associate professor of medical chemistry and a member of the team of scientists, said the compound, known as PRL-8-53, counters the destruction of certain chemical pathways in the brain by "making up the slack chemically." In a clinical study at Creighton, Hansl said, 58 college students performed better on intellectual tasks when they were given the compound, which he described as similar to an amino acid. In another study published in 1978, researchers compared the compound's effects on performance of college students with that of persons who were over 30. The participants were asked to remember lists of "nonsense syllables," geometric objects and other tasks, Hansl said. "The older group showed a 130% to 140% improvement in memory over the college students," he said. He said the effect of the compound lasted about seven hours, and added that even after the effect faded, memory was better. "Experiences from the past that were fading were recalled better" with no detectable side effects, he said. Hansl said the compound could help "the geriatric population - anyone over 30 - such as the elderly man who forgets his glasses or loses a thought in midsentence. I would like to make them more self-sufficient." Another use, he said, could aid those "in intellectual stress situations, such as a businessman or student, to perform tasks better." But Hansl added there have been no indications that people with brain damage could benefit from the compound. He said the research team is working on a related compound which could produce even better results. They are now evaluating the clinical effects of the compound. Hansl, who had been involved in the research project for more than 15 years, said the chemical is one of a new group of compounds that were studied in the search for a new tranquilizer that would not slow down intellectual functions. ============================== Uploader's Note: On the back of the above news clipping I wrote: "PRL-8-53 is 3-(2-benzylmethylamino ethyl) benzoic acid methyl ester" I don't recall where I found that piece of info, but I suspect it was from an item in "Science News". The Reader's Guide to Periodic Literature lists the following reference to PRL-8-53: "Learning and Memory Improvment Through Chemistry: Dream or Reality in the Offing." (PRL-8-53) by Nicolas Hansl & A.B. Hansl in the "Phi Delta Kappan" 61:264-5 December 1979 But I haven't been able to get a copy of that article yet. --- Finally, the magazine "Reality Hackers/High Frontiers" which R.U.Sirius edits is available from: Fun City MegaMedia/Mondo 2000 PO Box 49271, Berkeley, CA 94704 (415)845-9018 And the "Whole Earth Review" is available from: Whole Earth Review PO Box 15187, Santa Ana, CA 92705-9913 --- ========================================================================= ENHANCER.TXT 14-JUL-90 NEW DRUGS THAT MAKE YOU SMART by John Morgenthaler from MONDO 2000 - issue #2 The term nootropic comes from the Greek word meaning "acting on the mind." Since the invention of Piracetam by UBC laboratories in Belgium, other drug companies have been scrambling to develop their own nootropics. Some of them being researched now include; Vinpocetine, Aniracetam, Pramiracetam, and Oxiracetam. As yet, there is no nootropic drug that is FDA approved for sale in the United States, but there is plenty of motivation on the part of the drug companies to get that approval - financial analysts expect the U.S. market for cognitive enhancers - smart pills - to soon be in excess of one billion dollars per year! Nootropics are very interesting because of their lack of any demonstrable toxicity. They are not, however, the only substances that increase intelligence. There are over 30 chemicals that have been shown to improve animal and/or human intelligence (learning and data processing of particular types of tasks.) Here I propose to present a practical, drug-by-drug guide to the use of the most interesting of these cognitive enhancement compounds, and where you can get them. Disclaimer: This article should not be interpreted as medical advice or an attempt to encourage the use of cognitive enhancement dru... uh, compounds. You must consult with a licensed physician for such medical advice. We don't even want you to EXPERIMENT WITH THESE COMPOUNDS. Nor do we wish to imply, in any way, that you should try to INCREASE YOUR INTELLIGENCE or MAKE YOURSELF INTO A SUPERBEING. Heaven forfend! --------------- CENTROPHENOXINE (Trade Name: Lucidril) Centrophenoxine is an intelligence booster and also an effective anti-aging therapy. It has been shown to cause improvements in various aspects of memory function and a 30% increase in lifespan of laboratory animals. One of the most widely recognized aspects of aging is the buildup of lipofuscin in brain cells (lipofuscin is the stuff that age spots are made of.) Centrophenoxine removes lipofuscin deposits from brain cells and reduces its rate of accumulation in young brain cells. It also rejuvenates the synaptic structure - the area where the actual transfer of information takes place between nerve cells. PRECAUTIONS: Centrophenoxine should not be used by persons who are easily excitable, people with severe arterial hypertension, or those subject to convulsions or involuntary musculoskeletal movements. The drug also should not be used by nursing mothers. Adverse effects are rare, but include hyperexcitability, insomnia, tremors, motion sickness, paradoxical drowsiness, and depression. There is no toxicity of Centrophenoxine at therapeutic doses. DOSAGE: Take 1000 to 3000mg per day. Centrophenoxine takes effect very quickly. You'll notice an increase in alertness and a slight stimulating quality. SOURCES: Centrophenoxine is not sold in the United States. It can be purchased over the counter in Mexico or by mail from the address below. -------------- CHOLINE / LECITHIN: Choline can be found in several forms including choline bitartrate, choline chloride, or phosphatidyl choline. Phosphatidyl choline (PC) is the active ingredient of lecithin. All of these forms of choline will produce memory boosting effects, but PC has some unique effects as well. Choline compounds, including PC, are able to pass through the blood-brain barrier, where the brain utilizes the choline to make acetylcholine (a neurotransmitter that plays an important role in memory). Thus, choline enhances memory by increasing the amount of acetylcholine available for memory and thought processes. PC has some other important health benefits. It functions as a source of structural material for every cell in the human body, particularly those of the brain and nerves. It also aids in the metabolism of fats, regulates blood cholesterol, and nourishes the fat-like sheathes of nerve fibers. PRECAUTIONS: Any compound that acts like a precursor to acetylcholine such as choline, PC, or DMAE should not be used by people who are manic depressive because it can deepen the depressive phase. Choline bitartrate and choline chloride can sometimes cause a fishy odor or diarrhea. PC, however, does not have either of these effects. DOSAGE: Take 3 grams of choline per day in three divided doses. If you're taking lecithin you need to take a lot more because only part of the lecithin is choline. Often the label will provide information on the quantity of choline per tablespoon. All forms of choline should be taken with one gram per day of vitamin B-5 so that the choline can be converted into acetylcholine. SOURCES: Choline and lecithin are considered nutritional supplements and can be found at health food or drug stores. Commercial lecithin usually contains other oils and phosphatides besides phosphatidyl choline. Look at the label before you buy and make sure the product contains more than 30% phosphatidyl choline. Also, you should taste your lecithin and make sure it does not taste bitter (this indicates rancidity). Much lecithin on the market is rancid. The best form of lecithin I know is Twin Labs brand "PC 55" - it contains 55% PC and is always very fresh. ------------ DHEA: Dehydroepiandosterone (pronounced dee-hi-dro-epp-ee-an-dro-ster-own) is a steroid hormone produced in the adrenal gland. DHEA is the most abundant steroid in the human bloodstream. Research has found it to have significant anti-obesity, anti-tumor, anti-aging, and anti-cancer effects. DHEA levels naturally drop as people age and there is a good reason to think that taking a DHEA supplement may extend your life and make you more youthful while you're alive. Additionally, DHEA may be an important player in cognitive enhancement. DHEA is involved in protecting brain neurons from senility-associated degenerative conditions like Alzheimer's disease. Not only does the neuronal degenerative condition occur most frequently at the time of lowest DHEA levels, but brain tissue contains more DHEA than is found in the bloodstream. In an experiment with brain cell tissue cultures, Dr. Eugene Roberts found that very low concentrations of DHEA were found to "increase the number of neurons, their ability to establish contacts, and their differentiation." DHEA also enhanced long-term memory in mice undergoing avoidance training. Perhaps it plays a similar role in human brain function. DOSAGE of DHEA ranges from 50 mg to 2000 mg per day. There is no solid information indicating an optimal dosage for humans, but, if you want to get serious, you can get your DHEA levels checked every few months (for about $65), each time raising the amount of DHEA you take. When your blood levels reach what is normal for a 20-year-old human, then you're taking enough. SOURCES: DHEA is now being used by many people with AIDS because of its immune enhancement and antiviral effects. DHEA is not FDA approved but AIDS buyers groups are able to sell it to members because the FDA has a policy of looking the other way when it comes to the activity of these groups. Try contacting these buyer's groups: Alliance 7, 617/281-5360 in San Diego; or Healing Alternatives Foundation, 415/626/2316 in San Francisco. ---------- HYDERGINE (ERGOLOID MESYLATES): Research in other countries has shown that Hydergine improves mental function, prevents damage to brain cells, and may even be able to reverse existing damage to brain cells. Hydergine acts in several ways to enhance mental capabilities and slow down or reverse the aging processes in the brain. Its wide variety of effects include the following: 1. Increases in blood supply to the brain. 2. Increases the amount of oxygen delivered to the brain. 3. Enhances metabolism in brain cells. 4. Protects the brain from damage during periods of decreased and/or insufficient oxygen supply. 5. Slows the deposit of age pigment (lipofuscin) in the brain. 6. Prevents free radical damage to brain cells. 7. Increases intelligence, memory, learning and recall. 8. Normalizes systolic blood pressure. 9. lowers abnormal high cholesterol levels in some cases. 10. Reduces symptoms of tiredness, dizziness, and tinnitus (ringing in the ears). One way that Hydergine may enhance memory and learning is by mimicking the effect of a substance called nerve growth factor (NGF). NGF stimulates protein synthesis that results in the growth of dendrites in brain cells. Dendrites facilitate communication throughout the central nervous system and are necessary for memory and learning. New learning requires new dendritic growth. PRECAUTIONS: If too large a dose is used when first taking Hydergine. it may cause slight nausea, gastric disturbance, or headache. Overall, Hydergine does not produce any serious side effects, it is non-toxic even at very large doses, and it is contraindicated only for individuals who have chronic or acute psychosis. DOSAGE: The US recommended dosage is 3 mg per day; however, the European recommended dosage is 9 mg per day, taken in three divided doses. Most of the research has been done at levels of 9 to 12 mg per day. It may take several weeks before you notice the effects of hydergine. SOURCES: Hydergine is available in the United States and you can buy it if you have a doctor's prescription, but keep in mind that your doctor may not be familiar with the uses I have discussed. It can also be purchased over the counter in Mexico or by mail from overseas (see below). ---------- SULBUTIAMINE (ARCALION): Sulbutiamine is a new compound that has been described as being like Hydergine only better. It has been shown to facilitate wakefulness, improve long-term memory, speed up reaction time, decrease anxiety, and increase overall resistance to stress. DOSAGE: To combat fatigue take two 200mg tablets per day, always with breakfast or an AM meal, for a period of 20 days. Do not exceed three tablets at any time as this very powerful substance may cause severe headaches. Other than this, Sulbutiamine has no known adverse side effects. SOURCES: Sulbutiamine is not sold in the United States. It can be purchased by mail order from the address below. --------- VASOPRESSIN (DIAPID): Vasopressin is a brain hormone that is released by the pituitary gland. It improves attention, concentration, memory retention, and recall (both short-term and long-term). Vasopressin facilitates more effective learning by helping to "imprint" new information in the memory centers of the brain, a function which cannot be achieved without the action of vasopressin. Cocaine, LSD, amphetamines, Ritalin, and Cylert (pemoline) cause a release of vasopressin. Frequent use of these drugs can deplete levels of vasopressin with a result of making you slow and dopey. If you feel burnt out, a whiff of vasopressin can transform your experience in about 10 seconds because it is a direct application of the specific brain chemical that has been depleted. Alcohol and marijuana, however, inhibit the release of vasopressin. A whiff of vasopressin when using these drugs will compensate for much of the dopiness caused by them. Vasopressin is very useful in situation where there is a large amount of new information to learn. It increases your ability to memorize and recall specific factual information. PRECAUTIONS: Vasopressin usually produces the following side effects: runny nose, nasal congestion, itch or irritation of the nasal passages, headache, abdominal cramps, and increased bowel movements. Vasopressin has not been proven safe for use during pregnancy. DOSAGE: Vasopressin usually comes in a nasal spray bottle. Most studies showing memory improvement have been done with a dose of 12 to 16 USP per day or about two whiffs three or four times per day. Vasopressin produces a noticeable effect within seconds. SOURCES: Vasopressin is available in the United States. You can buy it if you have a doctor's prescription, but keep in mind that your doctor may not be familiar with the uses I have discussed. It can also be purchased over the counter in Mexico or by mail from overseas (see below). ------------ VINPOCETINE (CAVINTON): Vinpocetine, like Piracetam, is a nootropic drug and a powerful memory enhancer. It facilitates cerebral metabolism by improving cerebral microcirculation (blood flow), stepping up brain cells' production of ATP (the cellular energy molecule), increasing the brain's use of glucose, and increasing the brain's oxygen utilization. Vinpocetine is often used for the treatment of cerebral circulatory disorders such as memory problems, aphasia, apraxia, motor disorders, dizziness, and headache. PRECAUTIONS: Adverse effects are rare, but include hypotension and tachycardia. It has no drug interactions, no toxicity, and is generally very safe. DOSAGE: One or two 5 mg. tablets per day. SOURCES: Vinpocetine is not sold in the United States. It can be purchased by mail from the address below. ----------- MAIL ORDER: A little known FDA ruling now allows the importation of a three-month personal supply of drugs as long as they are regarded as safe in other countries. Ordering safe but unapproved drugs is now legal under the new FDA pilot guidelines, Chapter 971. This compromise was made under pressure from AIDS political action groups because the were being denied access to potentially life-saving substances. INTERLAB, a mail order pharmacy in England, was established in response to this new FDA ruling. INTERLAB carries a wide variety of drugs for cognitive enhancement, life extension, and the treatment of AIDS which are not available in the United States. They even carry Retin-A for the skin. All of the drugs I have discussed here can be purchased without a prescription from them. You can request a price sheet by writing to: INTERLAB, PO Box 587, Newport Pagnell, Bucks MK16 8AA, England. Their prices are reasonable and, on some items, quite low. If you want to order right away send a personal check for the amount of the item(s) you want plus $6 for shipping (or $10 for accelerated shipping).