Oilahuasca Activation

Version 1.24

IMPORTANT

Many people around the world are actively contributing to expanding the science of Oilahuasca. It has not been perfected yet. What's presented here works very well for some individuals. However, countless tests have shown that there are individuals who simply cannot get effects from any allylbenzenes no matter which set of known activators they use. The exact reason for this is currently unknown. We are still searching for Oilahuasca activation formulas that will work for more people.

For 24 hours prior to using oilahuasca you must follow the Oilahuasca Diet restrictions.

For a list of herbal formulas, supplements, and dietary restrictions known to be effective in obtaining psychedelic effects from allylbenzenes please see the article Oilahuasca Activators.

THIS PAGE EXPLAINS THE OILAHUASCA THEORY. MANY FACTS ARE PRESENTED TO SUPPORT THE OILAHUASCA THEORY. HOWEVER ALL SECTIONS ON THIS PAGE SHOULD BE TREATED AS THEORETICAL UNLESS STATED AS FACT.

THIS IS A WORK IN PROGRESS. IT WILL BE UPDATED AS NEW DATA IS AVAILABLE. TO LEAVE FEEDBACK FOR THIS PAGE USE THE DISCUSS LINK AT THE BOTTOM OF THIS ARTICLE.

Table of Contents

THE FACTS BEHIND OILAHUASCA

THIS SECTION IS BACKED BY SCIENTIFIC FACTS

BASIC OILAHUASCA THEORY

THIS SECTION IS THEORETICAL

THE OILAHUASCA ACTIVATION SEQUENCE

The theoretical activation sequence given in this example applies to all allylbenzenes (myristicin, safrole, etc.). In this example we use the allylbenzene elemicin.

There are two distinct sequences which are believed to lead to activity.


OILAHUASCA ACTIVATION VIA ENZYME MANIPULATION

This section details all the known enzymes to induce and inhibit in order to optimize the psychedelic and/or stimulant actions various allylbenzenes are capable of producing when fully activated. In some people allylbenzenes are extremely difficult to activate. Failure to follow these guidelines completely can lead to little or no effects from the various allylbenzenes available.

The single most important enzyme to induce is Estradiol 17beta dehydrogenase type 2 (17bHSD2). This enzyme is required. If 17bHSD2 is inhibited by drinking tea or consuming other drinks, supplements, or food items that inhibit 17bHSD2, then allylbenzenes activation will not take place. Without the action of 17bHSD2, allylbenzenes cannot form alkaloids in vivo.

For additional information on inducers and inhibitors used successfully by several individuals see the article: Oilahuasca Activators

The major human enzymes to induce (+) and inhibit (-) for Oilahuasca Activation.

SSAO 17bHSD2 ADH ALDH UGT1A9 UGT2B7 SULT1A1 SULT1A3 GST
- + + - - - - - -
Cytochrome P450 Enzyme Subfamilies
1A1 1A2 1B1 2A6 2B6 2C19 2C8 2C9 2D6 2E1 2J2 3A4
- - - + - +/- ? - - + - -

TRANSDERMAL USE VERSUS ORAL USE

THIS SECTION IS BASED ON ANECDOTAL DATA ONLY

Tests performed by several individuals have shown that topical application of these allylbenzenes can produce effects that are 5-10 times stronger than that of oral use. When used topically, the onset of the effects are also quicker and the overall duration of the effects are shortened as well. With topical use there are also less side effects.[5]


ALLYLBENZENE POLLS

After hundreds of votes have been made, the allylbenzene polls have consistently shown the same results year after year. As of May 2015, a total of 689 votes have been collected for the 2 polls. The results show very clearly that one of the three oils is by far the most effective in most people. It's interesting to note however, that the votes are not unanimous. The fact that the least effective essential oil is also the most effective essential oil for a minority of the people polled, shows just how different people are in how they are affected by these essential oils.

The nutmeg poll found in the article Nutmeg gives very strong evidence that the Oilahuasca theory is correct, which states that the allylbenzenes must be activated in the body before they can become psychedelic. If they were psychedelic without needing activation, they would be psychedelic in everyone all the time, but they clearly are not. The nutmeg poll results have been running for several years and the results are the same year after year. They show that most people find nutmeg to be psychedelic sometimes. However, not everyone does. A large minority finds nutmeg is never psychedelic.

The difficulty of activating elemicin, methyl chavicol, or myristicin varies from person to person. Some people can only easily activate one of these and have great difficulty trying to activate the others. Few people are able to easily activate all three. Many people have difficulty even activating just one of these. Hopefully, in the future, the Oilahuasca theory will advance enough to change this reality, making all three easy to activate in all people. Right now, that is not the case.

One major problem in advancing the Oilahuasca theory is finding people who are unable to get any hallucinogenic effects from allylbenzenes who are also willing to take part in the study. These people, because they don't initially get any results, are usually skeptics and right it all off as nonsense and aren't willing to further advance the Oilahuasca techniques. This is unfortunate. These are the very people who need to help advance the Oilahuasca theory. Their bodies are especially resistant to Oilahuasca techniques. If the reason for this resistance could be determined, it could greatly advance the Oilahuasca techniques for everyone. Currently, most of the individuals working on advancing Oilahuasca techniques are people who are already occasionally getting it to work.

To view the results of these polls, you need to cast your vote.

These polls are live polls hosted by www.pollsnack.com and are 100% anonymous. You don't need to log in to vote.


ALLYLBENZENE P450 ENZYME SPECIFICS


OILAHUASCA DIET

For 24 hours prior to using oilahuasca you must follow the Oilahuasca Diet restrictions.

Human diet is a major factor in getting oilahuasca working. Many people consume food, drinks and supplements known to inhibit 17bHSD2. Drinks as commonplace as tea and grapefruit juice potently inhibit 17bHSD2. These and other detrimental dietary items explained in this article must be avoided for at least 24 hours prior to using oilahuasca if psychedelic effects are desired. Failure to adhere to these dietary guidelines can completely prevent oilahuasca from working. The 17bHSD2 enzyme is critical for oilahuasca to work. If this enzyme is inhibited by drinking tea or ingesting similar 17bHSD2 inhibitors, it can be impossible to get oilahuasca working. This has been verified by several people. Please adhere to these diet guidelines if you want any success with oilahuasca.


SUPPLEMENTS AND FOODS TO AVOID

Oxidative 17bHSD2 Inhibitors to Avoid

All inhibitors of oxidative 17bHSD2 will prevent activation of allylbenzenes. This enzyme must be induced, not inhibited. It's the single most important enzyme to induce. If oxidative 17bHSD2 is not functioning, allylbenzenes cannot produce psychedelic activity.[5]

Several tests using the potent 17bHSD2 inhibitor quercetin orally in human test subjects have proven that quercetin can completely inactivate allylbenzenes for 3-4 hours if taken prior to taking allylbenzenes.[5] For this reason all sources of quercetin and other potent inhibitors of 17bHSD2 must be avoided.

Naringenin also potently inhibits 17bHSD2. Grapefruit contains large amounts of naringenin, and also prevents the psychedelic action of allylbenzenes if taken before allylbenzenes. Inhibition lasts approximately 4-8 hours.

Galangin, kaempferide, and kaempferol also inhibit 17bHSD2 and need to be avoided.

Here's a list of all known 17bHSD2 inhibitors that should be avoided 4-8 hours prior to using allylbenzenes:

See the articles 17bHSD2, Quercetin and Naringenin for more details and references to the facts stated above.

CYP2A6 Inhibitors to Avoid

CYP2E1 Inhibitors to Avoid

  • Disulfiram
  • Garlic EO
  • Kava

Dimethylamine Boosters to Avoid in Some Cases

It's not known which metabolites of the allylbenzenes are the preferred alkaloid metabolites. Avoid these substances if you specifically want to avoid making too many dimethylamine metabolites.

Anecdotal reports indicate that supplementation with piperidine sources improves activation, and supplementation with dimethylamine sources reduces psychedelic activity. The exact reason for this is currently unknown. Some reports indicate that methyl eugenol and myristicin can be inactive in some cases unless used with piperidine supplements.

The dimethylamine alkaloid metabolites of allylbenzenes are probably more easily destroyed by MAO-A or MAO-B or both. The piperidine metabolites, although probably not psychedelic, may act to protect the dimethylamine metabolites from enzyme destruction.

See the articles Choline, Dimethylamine and Piperidine for more details and references to the facts stated above.


BENEFICIAL SUPPLEMENTS

These have been found to be beneficial based on anecdotal reports. For more details see the article Oilahuasca Activators.

Berberine

Berberine is one of the most powerful activators tested. It potently inhibits CYP2D6, and inhibits CYP2C9 and CYP3A4, while leaving CYP2E1 active. There may be other unknown actions at play. When used with caffeine (inhibits CYP1A2) and steviosides (theorized to inhibit UGT2B7), it's been able to activate elemicin at doses smaller than any other activator tested. It works better than black pepper tea, and produces a cleaner experience. Black pepper has sedative effects in the doses used, and colors up the experience.

It's believed that berberine's lack of sedative effects and it's potent inhibition of CYP2D6 and it's inaction on CYP2E1 are why it's more effective than black pepper. CYP2D6 appears to be extremely detrimental to activation and CYP2E1 appears to be vital. Piperine found in black pepper has been shown to inhibit CYP2E1[19] to some degree in humans, which is not good.

Black Pepper Tea

Black pepper tea appears to greatly increase the activity of most allylbenzenes. It's not known how this works.

Black pepper tea provides piperidine. Piperidine is known to condense with the 1'-oxo metabolites of allylbenzenes to form piperidine alkaloids such as 1'-oxoelemicin-piperidine, 1'-oxoestragole-piperidine, etc. But it's not known if the piperidine alkaloids are active. Another action by black pepper may be at play.

To supplement with piperidine from black pepper, make black pepper tea from about 5-10 grams of black pepper. Brew with 1 cup of hot water. Then filter out the solids. This will provide a substantial amount of piperidine. To make the black pepper tea more palatable, one can use the hot black pepper tea to make Cup Noodles soup.

Note that black pepper contains piperine and other alkaloids in addition to piperidine. Piperine inhibits CYP3A4 which is good, but it also has some other actions, such as inhibiting CYP2E1[19] to some degree, which is not good. More tests need to be performed on isolated piperine to determine it's effectiveness. When making black pepper tea, filtering out the solids removes a lot of the piperine. Piperine’s solubility in water is only 9.4 mg per cup. However, piperine is potent, and 10-20 mg of piperine can inhibit CYP3A4. 5 grams of black pepper contains about 500 mg of piperine, but only 9.4 mg will be extracted into 1 cup of water. The rest remains in the solid black pepper grounds. 1 cup of water can hold all the piperidine in black pepper.

See the articles Black Pepper, 1'-oxoelemicin-piperidine, 1'-Oxoestragole-Piperidine, and Piperine for more details and references to the facts stated above.

Gallic acid

Gallic acid induces 17bHSD2, an essential enzyme required for activation. It also induces SULT1A1 and SULT1A3 and must be pared with potent inhibitors of SULT1A1 and SULT1A3, such as EGCG.

See the articles Gallic acid and 17bHSD2 for more details and references to the facts stated above.

Genistein

Genistein induces 17bHSD2, an essential enzyme required for activation. It also inhibits UGT, SULT, and GST. Genistein is still being researched. It's effectiveness has been called into question. Until more data is available, it might be better to avoid genistein. Kudzu, from which it is extracted, was found to reduce psychedelic action by interacting with 5-HT1A, 5-HT2A, and 5-HT2C receptors.

See the articles Genistein and 17bHSD2 for more details and references to the facts stated above.

Glycerol

Glycerol induces CYP2E1.

Glucosamine

Acts as an SSAO inhibitor. When using glucosamine to inhibit SSAO it's probably best use it 1 hour before and then again combined with coffee at the time the allylbenzenes are ingested, and a few times periodically throughout the experience to boost the psychedelic effects. Doses of 1500 mg glucosamine HCl have been tested along with coffee producing very good results. Its possible that lower doses are effective but they have not been tested. Glucosamine has a half life of approximately 15 hours. It's SSAO inhibition is likely to last at least 15 hours or more.

See the articles Glucosamine and SSAO for more details and references to the facts stated above.

L-Lysine (causes piperidine formation in vivo)

Piperidine is naturally found in the human body. Piperidine is made mostly in the large intestine (colon) from excess L-lysine. Some people are low in this amine.

Theoretically the body uses piperidine to make piperidine alkaloids from allylbenzenes.

Piperidine supplementation appears to greatly increase the activity of most allylbenzenes. It's not known how this works. Piperidine is known to condense with the 1'-oxo metabolites of allylbenzenes to form piperidine alkaloids such as 1'-oxoelemicin-piperidine, 1'-oxoestragole-piperidine, etc. While these piperidines are probably not psychedelic, they may act as enzyme inhibitors protecting the actual psychedelic metabolites of allylbenzenes from rapid enzyme destruction.

It can take 3 or more hours for food to reach the colon (this varies dramatically from person to person, and depends highly on other contents in the digestive system). For this reason L-lysine supplements should be take several hours before taking allylbenzenes.

To supplement your piperidine levels using L-lysine, take at least 1000 mg or more of L-lysine approximately 3 or more hours before using the allylbenzenes.

See the articles L-Lysine and Piperidine for more details and references to the facts stated above.

Niacinamide

Niacinamide supplementation increases NAD+ in humans. The 17bHSD2 enzyme uses NAD+ as a cofactor. Without NAD+, 17bHSD2 is not effective.

Steviosides

Steviosides is theorized to act as a competitive inhibitor of UGT2B7. See the article on Steviosides for more details.

Vitamin D3

Vitamin D3 induces 17bHSD2, an essential enzyme required for activation. It also induces glutathione and should be pared with a good depleter of glutathioine such as cinnamon oil (which contains cinnamaldehyde).

Vitamin A

Vitamin A induces 17bHSD2, an essential enzyme required for activation.


THE OLD OSWALD AND PEELE ALLYLBENZENE ACTIVATION THEORY


See Also

Important New Oilahuasca Activators

Related Allylbenzenes

Other Related Links


Bibliography
1. E.O. Oswald, L. Fishbein, B.J. Corbett, M.P. Walker. Metabolism of naturally occuring propenylbenzene derivatives : II. Separation and identification of tertiary aminopropiophenones by combines gas—liquid chromatography and chemical ionization mass spectrometry. Journal of Chromatography A, Volume 73, Issue 1, 8 November 1972, Pages 43-57 (web link)
(Download Attached PDF Document)
2. E.O. Oswald, L. Fishbein, B.J. Corbett, M.P. Walker. Identification of tertiary aminomethylenedioxy-propiophenones as urinary metabolites of safrole in the rat and guinea pig. Biochimica et Biophysica Acta (BBA) - General Subjects, Volume 230, Issue 2, 23 February 1971, Pages 237-247 (web link)
3. E.S. Oswald, L. Fishbein, B.J. Corbett, M.P. Walker. Urinary excretion of tertiary amino methoxy methylenedioxy propiophenones as metabolites of myristicin in the rat and guinea pig. Biochimica et Biophysica Acta (BBA) - General Subjects, Volume 244, Issue 2, 19 August 1971, Pages 322-328
(web link) (Download Attached PDF Document)
4. E.S. James D. Peele Jr., Edward O. Oswald. Metabolism of naturally occurring propenylbenzene derivatives III. Allybenzene, propenyl benzene, and related metabolic products. Biochimica et Biophysica Acta (BBA) - General Subjects, Volume 497, Issue 2, 27 April 1977, Pages 598-607
(web link)
5. Unpublished scientific research performed by members of herbs.maxforum.org.
6. Handbook of phytochemical constituents of GRAS herbs and other economic plants
Duke, James A. 1992. Boca Raton, FL. CRC Press (Dr. Duke's Phytochemical and Ethnobotanical Databases Online)
7. Content of Potentially Anticarcinogenic Flavonoids of Tea Infusions,
Wines, and Fruit Juices Michael G. L. Hertog, Peter C. H. Hollman, and Betty van de Putte. 1993. DOI: 10.1021/jf00032a015
8. Carcinogenic and mutagenic activities of safrole, 1'-hydroxysafrole, and some known or possible metabolites.
Wislocki PG, Miller EC, Miller JA, McCoy EC, Rosenkranz HS. PubMed PMID: 192464
9. 1'-Hydroxysafrole, a proximate carcinogenic metabolite of safrole in the rat and mouse.
Borchert P, Miller JA, Miller EC, Shires TK. http://www.ncbi.nlm.nih.gov/pubmed/4347718 4347718]
10. Safety evaluation of certain food additives; Prepared by the Sixty-ninth meeting of the Joint FAO/WHO Expert Committee on Food Additives (JECFA); World Health Organization, Geneva, 2009; ISBN: 978-92-4-166060-0
11. METHYLEUGENOL;
IARC MONOGRAPHS – 101 Download Attached PDF Document
12. Douglas W. Bristol, Ph.D., Study Scientist
NTP Technical Report on the 3-Month Toxicity Studies of Estragole; National Toxicology Program, Toxicity Report Series, Number 82; NIH Publication No. 11-5966; National Institutes of Health, Public Health Service, U.S. Department of Health and Human Services Download Attached PDF Document
13. Evaluation of human interindividual variation in bioactivation of estragole using physiologically based biokinetic modeling.
Punt A, Jeurissen SM, Boersma MG, Delatour T, Scholz G, Schilter B, van Bladeren PJ, Rietjens IM. PubMed: 19920071
14. Glucuronidation of 1'-hydroxyestragole (1'-HE) by human UDP-glucuronosyltransferases UGT2B7 and UGT1A9.
Iyer LV, Ho MN, Shinn WM, Bradford WW, Tanga MJ, Nath SS, Green CE. PubMed: 12657745
15. Immunochemical identification of hepatic protein adducts derived from estragole.
Wakazono H, Gardner I, Eliasson E, Coughtrie MW, Kenna JG, Caldwell J. PubMed: 9705747
16. Copper-mediated oxidative DNA damage induced by eugenol: possible involvement of O-demethylation.
Sakano K, Inagaki Y, Oikawa S, Hiraku Y, Kawanishi S. PubMed PMID: 15576237
17. Yun CH, Lee HS, Lee HY, Yim SK, Kim KH, Kim E, Yea SS, Guengerich FP
Department of Genetic Engineering, Pai-Chai University, 439-6 Doma-dong, Seo-ku, Taejon 302-735, South Korea. Toxicology Letters [2003, 137(3):143-150]; Roles of human liver cytochrome P450 3A4 and 1A2 enzymes in the oxidation of myristicin; DOI: 10.1016/S0378-4274(02)00397-1 PubMed PMID 12523956
18. Amunom I, Dieter LJ, Tamasi V, Cai J, Conklin DJ, Srivastava S, Martin MV, Guengerich FP, Prough RA.
Cytochromes P450 catalyze the reduction of α,β-unsaturated aldehydes; Department of Biochemistry and Molecular Biology, The University of Louisville School of Medicine , Louisville, KY 40292, USA; Chem Res Toxicol. 2011 Aug 15;24(8):1223-30. doi: 10.1021/tx200080b. Epub 2011 Jul 29; PubMed PMID: 21766881
19. Effect of piperine on CYP2E1 enzyme activity of chlorzoxazone in healthy volunteers.
Bedada SK, Boga PK. Xenobiotica. 2016 Sep 27:1-25. PMID: 27670974; DOI: 10.1080/00498254.2016.1241450

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