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.
This is a supplement to the main article found here: Oilahuasca Activation.
The information presented in this article is mostly obtained from anecdotal reports. The data presented here needs to be verified by more individuals. If any data is missing from this article, or present in this article that is in conflict with other reports, please inform us by leaving a comment about it using the Discuss link at the bottom of this article.
Oilahuasca Activators are herbs and compounds found to help activate allylbenzenes in some but not all individuals. Some activators have been helpful in some people but detrimental in others.
Oilahuasca Diet
For 24 hours prior to using oilahuasca you must follow the Oilahuasca Diet restrictions.
Please note that the items in this article require that the Oilahuasca Diet is followed for 24 hours prior to using oilahuasca. If the Oilahuasca Diet is not followed Oilahuasca Activation can fail despite using the various oilahuasca activators given in this article.
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.[2]
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.[2] 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 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[Bibliography item PMID27670974 not found.] 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[Bibliography item PMID27670974 not found.] 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 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 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.
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.
Oilahuasca Enzyme Interaction
Most of the oilahuasca activators in this article are based on data pertaining to enzymes which interact with allylbenzenes. The chart below outlines several enzymes that need to be induced and inhibited.
17bHSD2 Induction
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
Estradiol 17beta dehydrogenase type 2 (17bHSD2) oxidative action needs to be induced. This enzyme creates phenyl vinyl ketones from allylbenzenes in their 1'-hydroxy form. For example, the phenyl vinyl ketone 1'-oxoestragole is proven to be created from the alcohol 1'-hydroxyestragole (a metabolite of the allylbenzene methyl chavicol) by the action of estradiol-17beta-dehydrogenase Type 2 (17bHSD2).[7] This metabolite is then proven to be capable of forming adducts with glutathione (GSH) leading to inactivation, or forming adducts with endogenous amines.[7] The latter action is believed to be required for the psychedelic effects of methyl chavicol and related allylbenzenes.
For information on 17bHSD2 inducers and inhibitors see the article here: Estradiol 17beta dehydrogenase type 2
UGT1A9 And UGT2B7 Inhibition
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
UGT1A9 and UGT2B7 are proven to inactivate allylbenzenes once in their 1'-hydroxy form. These add a glycosyl group to an available hydroxy position on hydroxylated allylbenzenes making them inactive. For example, it turns 1'-hydroxyelemicin into 1'-hydroxyelemicin glucuronide. Inhibitors must be used. UGT2B7 is more important to inhibit than UGT1A9. For information on inhibitors see their articles here: UGT1A9, UGT2B7.
The metabolite of methyl chavicol known as 1'-hydroxyestragole is proven to undergo glucuronidation primarily by the action of UGT2B7 followed by UGT1A9, with a very small amount carried out by UGT2B15.[8] These enzymes are assumed to be responsible for the glucuronidation of all related allylbenzenes.
Substrate |
UGT |
End Product |
1'-Hydroxyelemicin |
|
1'-Hydroxyelemicin glucuronide |
 |
|
 |
Cofactor |
|
Byproduct |
UDPglucuronate |
|
UDP |
SULT1A1 And SULT1A3 Inhibition
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
SULT1A1 and SULT1A3 are proven to inactivate allylbenzenes once in their 1'-hydroxy form. For example, the alcohol 1'-hydroxyelemicin becomes 1'-sulfoxyelemicin by these enzymes. Inhibitors must be used. For information on inhibitors see the articles here: SULT1A1, SULT1A3.
The metabolite of methyl chavicol known as 1'-hydroxyestragole is preven to undergo sulfation by the action of SULT1A1 and SULT1A3.[9] These pathways prevent 1'-oxoestragole from forming. These enzymes are assumed to be responsible for the sulfation of all related allylbenzenes.
Substrate |
SULT |
End Product |
1'-Hydroxyelemicin |
|
1'-Sulfoxyelemicin |
 |
|
 |
Cofactor |
|
Byproduct |
3'-phosphoadenylylsulfate |
|
adenosine 3',5'-bisphosphate |
GST Inhibition and Glutathione Depletion
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
Glutathione is proven to inactivate allylbenzenes once in their phenyl vinyl ketone form. For example, the phenyl vinyl ketone 1'-oxoestragole is proven to be inactivated by forming adducts with glutathione.[7]
GST adds glutathione to the 1'-oxo position of the phenyl vinyl ketones making them unable to form alkaloids. For example, it turns 1'-oxoelemicin into 3'-(glutathion-S-yl)-1'-oxoelemicin by the addition of glutathione preventing alkaloid formation by 1'-oxoelemicin.
It's not known to what degree glutathione S-transferase (GST) is involved in this inactivation.
Glutathione is proven to condense with phenyl vinyl ketones without the need for enzyme interaction (see the article 1'-Oxoestragole for more details). This means inhibiting glutathione S-transferase (GST) is not enough. We also need to deplete glutathione to prevent it from inactivating allylbenzenes (see the article Glutathione for details on ways to safely deplete glutathione).
There are several subsets of glutathione S-transferase (GST). The exact ones responsible for this action are currently unknown, as is there level of interaction in this adduct process. Inhibitors must be used. For information on inhibitors see the article here: Glutathione S-transferase.
CYP1A2, CYP2A6, CYP2C9, and CYP2E1
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
CYP1A2, CYP2A6, CYP2C9, and CYP2E1 play a pivotal role in 1'-hydroxylation of many allylbenzenes, creating alcohol. This is the first major step towards activation. However, this is not the only action each of these enzymes can perform. Many human based Oilahuasa tests have shown that CYP1A2 has undesirable effects on most allylbenzenes. CYP1A2 can perform ALDH-like activity, which is not good. CYP1A2 can also demethylenate myristicin, and probably other methylenedioxy allylbenzenes. Elemicin's non-psyechedelic "malatonin" effect appears to be primarily caused by the action of CYP1A2. The only allylbenzene believed to require CYP1A2 for 1'-hydroxylation is methyl eugenol. Very few Oilahuasca tests are being done with methyl eugenol currently. For all of the other allylbenzenes CYP1A2 appears to be very detrimental. And despite some tests showing that CYP1A2 is needed for 1'-hydroxylation of methyl eugenol, it's possible the tests are incomplelete, and another enzyme can also perform this in humans.
The alcohol 1'-hydroxyestragole is proven to be created from the allylbenzene methyl chavicol in human liver in vitro primarily by the P450 enzymes CYP1A2, CYP2A6 and CYP2E1.[6][7] However, several Oilahuasca tests with methyl chavicol have shown CYP1A2 to be detrimental.
In humans the alcohol 1′-hydroxymethyleugeol is proven to be created from the allylbenzene methyl eugenol by the P450 enzyme CYP1A2.[6] Some in vitro reports state that it is primarily catalyzed by both CYP1A2 and CYP2C9 and that CYP2C19 and CYP2D6 also play a minor role.[5] Human liver in vitro tests show that methyl eugenol is not metabolized by CYP2A6.[5]
The alcohol 1'-hydroxysafrole is proven to be created from the allylbenzene safrole by the P450 enzymes CYP2C9 and CYP2E1, and to a lesser degree CYP2A6 and CYP2D6 according to one human in vitro study.[4] Several Oilahuasca tests with safrole have shown CYP1A2 to be detrimental.
Substrate |
1'-hydroxylation |
End Product |
Elemicin |
|
1'-Hydroxyelemicin |
 |
|
 |
CYP3A4
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
CYP3A4 is proven to O-demethylenate the allylbenzene myristicin, an action that breaks the methylenedioxy group of myristicin, replacing it with 2 hydroxy groups.[11] The cytochrome P450 enzyme CYP1A2 plays a minor role in this action. Therefor CYP3A4 needs to be inhibited for myristicin and probably other allylbenzenes with methylenedioxy groups. All allylbenzenes that are O-demethylenated are not known to have psychedelic action. This enzyme may also have some undesirable effects on other allylbenzenes without methylenedioxy groups.
Substrate |
O-demethylenation |
End Product |
Myristicin |
|
Demethylenyl myristicin |
 |
|
 |
CYP2D6
THIS SECTION IS BACKED BY SCIENTIFIC FACTS
The allylbenzene eugenol is proven to be O-demethylated to hydroxychavicol by the action of CYP2D6 in vitro.[10] CYP2D6 performs this action on hundreds of compounds and very likely also performs this action on other allylbenzenes and should therefor be strongly inhibited. No allylbenzene that is O-demethylated is known to have psychedelic action.
Substrate |
O-demethylation |
End Product |
Elemicin |
|
Methoxyeugenol |
 |
|
 |
CYP2B6
THIS SECTION IS PARTIALLY BACKED BY SCIENTIFIC FACTS
CYP2B6, CYP3A4, CYP1A2, and CYP2J2 but not CYP2E1 can all perform ALDH-like activity.[12] They should therefor probably be strongly inhibited. ALDH-like action directly interferes with the two main activation theories presented on this page. For more details on this type of ALDH-like action of cytochrome P450 enzymes see the article here: Aldehyde Dehydrogenase
SSAO Inhibition
THIS SECTION IS BASED ON ANECDOTAL DATA ONLY
SSAO inhibitors appear to be greatly beneficial for
elemicin,
methyl chavicol,
methyl eugenol and possibly several other
allylbenzenes.
SSAO inhibitors work at any point during the effects, giving a very noticeable boost in effects for elemicin, methyl chavicol, methyl eugenol and possibly several other allylbenzenes. SSAO inhibitors can even bring back the effects if taken shortly after the effects of the allylbenzenes appear to have subsided.
The exact reason for potentiation by SSAO inhibition is unknown.
SSAO is not capable of deaminating dimethylamine, piperidine, or pyrrolidine alkaloids. It deaminates only simple amines such as mescaline, phenethylamine, methylamine and similar compounds. It's possible that some ammonia adducts form in vivo from allylbenzenes such as 1'-oxoelemicin-amine, or 1'-oxoelemicin-PEA, which could be substrates of SSAO.
For details on SSAO inhibitors and inducers please see the article found here: SSAO.
Alcohol Dehydrogenase (ADH)
THIS SECTION IS HIGHLY THEORETICAL
Alcohol dehydrogenase (as well as alcohol oxidase) should convert the 3-hydroxyl alcohol forms of allylbenzenes into their aldehyde forms which can then possibly be aminated to form dimethylamine, piperidine, and pyrrolidine alkaloids. CYP2E1 may also have the same action as alcohol dehydrogenase. For this reason alcohol dehydrogenase and possibly CYP2E1 should not be inhibited. Note that 17bHSD2 performs this action for phenyl vinyl ketones and might also perform this action on the aldehyde forms of allylbenzenes. There is currently no evidence showing which enzyme preforms this action on the aldehyde forms of allylbenzenes, although the action is proven to take place.
For details on alcohol dehydrogenase inhibitors to avoid see the article here: Alcohol Dehydrogenase
Aldehyde Dehydrogenase (ALDH)
THIS SECTION IS HIGHLY THEORETICAL
Anecdotal reports have shown that aldehyde dehydrogenase and similar enzymes (such as xanthine oxidase and aldehyde oxidase) which hydroxylate aldehydes into acids contribute to the inactivation of allylbenzenes.
CYP2B6, CYP3A4, CYP1A2, and CYP2J2 but not CYP2E1 can all perform ALDH-like activity and should therefor probably be strongly inhibited. ALDH-like action directly interferes with the two main activation theories presented on this page. CYP1A2 might be needed for the activation of certain allylbenzenes such as methyl eugenol. In this case it might be best not to inhibit CYP1A2.
For details on aldehyde dehydrogenase inhibitors see the article here: Aldehyde Dehydrogenase
BBSC Single Capsule Oilahuasca Activation Formula
Oilahuasca Activation formulas have been a work in progress since 2008. The latest BBSC formula from 2017 is a modification of the BBS formula. It was found to be much more effective.
Fill 1 size 000 capsule with:
Swallow with 1 cup of strong Colombian coffee (caffeine inhibits CYP1A2).
Note that calamus oil can be omitted, but the results will be much weaker. Beta-Asarone is a nootropic that is a powerful admixture for Oilahuasca, greatly improving the chances of a success. It's currently unknown why it's so effective.
Caffeine is essential. Without a source of caffeine, a "melatonin" effect from the elemicin is very likely to occur, which is void of psychedelic effects. Test results from multiple people suggest that CYP1A2 appears the be the main cause of the "melatonin" effect from elemicin.
It's also VERY IMPORTANT that the coffee be used at the same time as the elemicin, and never before it. Caffeine inhibits CYP1A2 for a short time, and then greatly induces it. If elemicin is taken while CYP1A2 is induced you are pretty much guaranteed to have the "melatonin" effect instead of the desired psychedelic effects.
Slightly better results can sometimes be had by pre-treating with vitamin A and glycerol, as is done in the original BBS formula.
BBS 2 Stage Oilahuasca Activation Formula
NOTE: 1 cup of coffee was always used in each test to swallow the capsules. This fact was previously omitted from this formula. The formula may not work well without a source of caffeine as a CYP1A2 inhibitor.
The BBS formula is primarily based on berberine,steviosides developed in 2016. This formula looks very promising. This formula takes advantage of all the latest known methods of boosting success rates for Oilahuasca Activation. This formula works by inhibiting several enzymes known to inactivate allylbenzenes and induces enzymes known to help activate allylbenzenes.
Oilahuasca Activation formulas prior to 2016 are less effective. As more research is made, it's becoming much clearer which enzymes need to be inhibited and which ones need to be induced to help activate allylbenzenes.
STAGE 1
T-4:00: ORAL: vitamin A, 55 mg. (induces Estradiol 17beta-dehydrogenase Type 2)
T-4:00: ORAL: glycerol, 5 ml. (induces CYP2E1)
STAGE 2
T-0:00: ORAL: 300 mg pure berberine hydrochloride (inhibits CYP2D6, CYP2C9 and CYP3A4)
T-0:00: ORAL: 100 mg pure steviosides (potentially inhibits UGT2B7).
T-0:00: ORAL: 200 mg elemicin (or an appropriate amount of another allylbenzene).
Berberine
Berberine has been tested by several individuals as an oilahuasca admixture. Doses tested were 300 mg and above taken as berberine hydrochloride. In one report as little as 20 mg of elemicin taken together with 1 cup of coffee (caffeine inhibits CYP1A2, 300 mg berberine hydrochloride and 100 mg steviosides, produced effects described as nearly equal to a 50 mg dose of mescaline hydrochloride. Larger doses of elemicin were also tested, with similar results, giving activated elemicin a potency roughly 250% the potency of mescaline.
Berberine is believed to help activate elemicin because it inhibits CYP2D6, CYP3A4 and CYP2C9, while leaving CYP2E1 fully active. CYP2D6, CYP3A4 and CYP2C9 can all theoretically O-demethylate elemicin into methoxyeugenol. By inhibiting these enzymes, elemicin is more likely to be attacked by CYP2E1. CYP2E1 is not known to O-demethylate allylbenzenes, but is known to 1'-hydroxylate them. By shifting attack of elemicin to CYP2E1, it is likely to prevent the formation of methoxyeugenol and favor the formation of 1'-hydroxyelemicin. The metabolite 1'-hydroxyelemicin can then theoretically form 1'-oxoelemicin (by the action of the enzyme Estradiol 17beta-dehydrogenase Type 2), which can then form alkaloids in vivo (see the article on oilahuasca for more details).
Steviosides
Steviosides are sold for use as sweeteners. They are extracted from the stevia plant. When used in conjunction with berberine, they where shown to help activate elemicin, a difficult allylbenzene to fully activate. Berberine appears to shift elemicin's metabolism to favor 1'-hydroxyelemicin over methoxyeugenol. 1'-hydroxyelemicin is theoretically a major step towards activation, but the next step can be blocked by the action of UGT2B7.
1'-hydroxyelemicin can form 1'-hydroxyelemicin glucuronide by the action of UGT2B7. This is a dead end.
1'-hydroxyelemicin can also form 1'-oxoelemicin by the action of Estradiol 17beta-dehydrogenase Type 2. This is theoretically the next major step towards activation. 1'-Oxoelemicin is the only metabolite of elemicin that's known to form alkaloids.
By inhibiting UGT2B7, the metabolite 1'-oxoelemicin is favored over 1'-hydroxyelemicin glucuronide.
Steviosides are potential inhibitors of UGT2B7 (see the article on stevioside for more details). Because the main metabolite of steviosides is proven to be almost exclusively steviol glucuronide in humans, even if steviosides do not technically inhibit UGT2B7 in humans, they should help divert UGT2B7 from attacking other compounds, especially in cases where they have a higher affinity towards UGT2B7 than the competing compounds.
Old Three Stage Oilahuasca Activation Formulas
This section contains old activation formulas prior to 2016. These formulas are not as effective.
These older Oilahuasca Activation formulas were created in 2013 based on research spanning only 5 years. Since these were created knowledge on Oilahuasca Activation has expanded, making these formulas obsolete.
STAGE 1 - DEPLETE GLUTATHIONE
For this cinnamon oil is taken used. The [cinnamaldehyde in cinnamon oil is used to deplete glutathione. This is a critical step to activating allylbenzenes. Cinnamaldehyde takes some time to deplete glutathione and should be taken before the allylbenzenes by at least 1 hour, and not with them. By taking it 2 days in a row it should be much more effective at depleting glutathione.
STAGE 2 - INHIBIT AND INDUCE ENZYMES
In this stage, taken 30 minutes after stage 1, herbs and supplements are taken that together inhibit CYP2D6, CYP3A4, UGT2B7, UGT1A9, SULT1A1, SULT1A3, and GST, and induce CYP2C9 and 17bHSD2. Is it very important that 17bHSD2 is strongly induced. If any food or supplements are taken that inhibit it, such as supplements, foods or drinks containing quercetin, then the allylbenzenes can not produce psychedelic effects.
STAGE 3 - AMINATION
In this stage we take the allylbenzenes together with a source of amines the allylbenzenes can condense with after they form 1'-oxo metabolites (such as 1'-oxoelemicin, 1'-oxoestragole, etc.). The amines should be taken in abundance with at least a 2:1 ratio or more, and should be safe to ingest at the doses used.
This formula is based on piperidine. It's currently not known how formulas based on piperidine actually work. The piperidine metabolites of allylbenzenes are probably not psychedelic themselves, but may possibly act as protectors of the true psychedelic metabolites.
This formula works with elemicin, dillapiole, myristicin, methyl chavicol, and methyl eugenol. In this example elemicin is used. If using other allylbenzenes you might need to adjust the dosage of the allylbenzenes used. In general most allylbenzenes are active in the dosage range of mescaline.
ELBP3 is used to describe the BP3 formula when used with elemicin, where the prefix EL means elemicin. Similarly use the prefix MC for methyl chavicol, ME for methyl eugenol, MY for myristicin, SA for safrole, DA for dillapiole, AP for apiole, GA for gamma-asarone, etc.
The ELBP3 three sage Oilahuasca Activation formula produced psychedelic effects in several individuals. The main effects lasted 8 hours, with residual effects lasting up to 16 hours. This formula is designed to theoretically create 1'-oxoelemicin-pideridine in vivo. Anecdotal reports indicate that the ELBP3 Oilahuasca Activation formula produces effects similar to mescaline with an LSD-like electric feel.
STAGE 1
T-25:00: ORAL: size OOO capsule filled with 230 mg of cinnamon oil (true cinnamon, not cassia) diluted with vegetable oil
T-1:00: ORAL: size OOO capsule filled with 196 mg of cinnamon oil (true cinnamon, not cassia) diluted with vegetable oil
STAGE 2
T-0:30: ORAL: size OOO capsules filled with 540 mg black seed oil, 208 mg 50% EGCG, 200 mg kudzu 200 mg, 61 mg valerian root oil from China, 0.8 mg vitamin B9 (folic acid), 201 mg pomegranate 40% ellagic extract, 100 mg rooibos 20% gallic acid extract, 50 mg vitamin B3 (nicotinic acid)
STAGE 3
T+0:00: ORAL: size OOO capsules filled with 100-350 mg 91% elemicin. This is consumed using 1 cup of filtered tea brewed using 5-10 grams of ground black pepper. The tea must be filtered. Do not consume the solids.
This formula works with elemicin and probably works with other allylbenzenes. In this example elemicin is used.
If using other allylbenzenes you might need to adjust the dosage of the allylbenzenes used. In general most allylbenzenes are active in the dosage range of mescaline.
ELPEA3 is used to describe the PEA3 formula when used with elemicin, where the prefix EL means elemicin. Similarly use the prefix MC for methyl chavicol, ME for methyl eugenol, MY for myristicin, SA for safrole, DA for dillapiole, AP for apiole, GA for gamma-asarone, etc.
The ELPEA3 three sage Oilahuasca Activation formula produced very long lasting psychedelic effects in several individuals. The main effects lasted 12 hours, with residual effects lasting up to 48 hours. This formula theoretically creates 1'-oxoelemicin-PEA in vivo. Anecdotal reports indicate that the ELPEA3 Oilahuasca Activation formula produces effects similar to a cross between mescaline and XTC.
STAGE 1
T-25:00: ORAL: size OOO capsule filled with 230 mg of cinnamon oil (true cinnamon, not cassia) diluted with vegetable oil
T-1:00: ORAL: size OOO capsule filled with 196 mg of cinnamon oil (true cinnamon, not cassia) diluted with vegetable oil
STAGE 2
T-0:30: ORAL: size OOO capsules filled with 540 mg black seed oil, 208 mg 50% EGCG, 200 mg kudzu 200 mg, 61 mg valerian root oil from China, 0.8 mg vitamin B9 (folic acid), 201 mg pomegranate 40% ellagic extract, 100 mg rooibos 20% gallic acid extract, 50 mg vitamin B3 (nicotinic acid)
STAGE 3
T+0:00: ORAL: size OOO capsules filled with 100-350 mg 91% elemicin, 300-700 mg phenylehylamine HCl, 200 mg rutin.
Oral Activators
In this section you'll find various herbs and supplements reported by individuals to help them activate allylbenzenes.
Latest Oral Activators
These activators are based on the latest ongoing Oilahuasca research. Current research is going against Oilahuasca Activation Sequence A (based on Oswald's theory) where allylbenzenes need to be 1-hydroxylated as a 1st step towards activation. CYP2C9 and CYP1A2 are prime enzymes for 1-hydroxylation of many allylbenzenes, but hundreds of tests have shown that these should be inhibited, not induced.
Current research is moving in the direction of Oilahuasca Activation Sequence B being a more accurate activation theory for humans. In this theory 3'-hydroxylation is the 1st step towards activation.
It's been determined that 2 of the primary activation enzymes are likely to be CYP2E1 and Estradiol 17beta-dehydrogenase Type 2. These fit the Oilahuasca Activation Sequence B theory quite well.
CYP2D6 appears the be a vital enzyme to inhibit. CYP2D6 is known to O-demethylate and O-demethylenate many compounds, and this is an action that is not good.
CYP3A4 appears the be a vital enzyme to inhibit. CYP3A4 is known to O-demethylate allylbenzenes.
Activator |
Effectiveness |
Dosage |
Notes |
Berberine |
Extremely Potent |
300-1000 mg |
Has been reported to be very helpful in activating elemicin. It is proven to inhibit CYP2C9, CYP2D6, and CYP3A4 in humans, but appears not to inhibit CYP2E1. |
Beta-asarone |
Extremely Potent |
1-2 drops |
This nootropic can activate elemicin stand alone in some people. Calamus oil from Nepal contains a large amount of beta-asarone. It's unknown why beta-asarone is so effective. Oil from India is vastly inferior, as it contains much less beta-asarone. |
Calamus EO from Nepal |
Extremely Potent |
1-3 drops |
It can activate elemicin stand alone in some people. Oil from Nepal is superior. It contains a large amount of the nootropic beta-asarone. It's unknown why beta-asarone is so effective. Oil from India is vastly inferior, as it contains much less beta-asarone. |
Caffeine |
Extremely Potent |
100-200 mg |
Caffeine inhibits CYP1A2. |
Coffee |
Extremely Potent |
1 cup of strong coffee |
It contains caffeine which inhibits CYP1A2. |
Glycerol |
Extremely Potent when used prior to berberine |
5 ml |
Used to induce CYP2E1. It works well in conjunction with berberine, but is not effective on it's own. |
Steviosides |
Very Potent when used with berberine |
100-1000 mg |
Used to potentually inhibit UGT2B7. It works well in conjunction with berberine, but is not effective on it's own. |
Vitamin A |
Extremely Potent when used prior to berberine |
55 mg |
Used to induce Estradiol 17beta-dehydrogenase Type 2. It works well in conjunction with berberine, but is not effective on it's own. |
Vitamin B3 (niacinamide) |
Extremely Potent |
50-100 mg |
Supplies NAD+ to fuel oxidative Estradiol 17beta-dehydrogenase Type 2 |
Older Oral Activators
These older activators have been in use for over 8 years by various individuals.
Activator |
Effectiveness |
Dosage |
Notes |
Aniseed (Anise) EO |
Potent |
5-10 drops |
Works very well for transdermal use. Ground aniseed is known to induce CYP2C9, however it's not known if the essential oil contains the active ingredient or not. |
Black Pepper Tea (solids removed) |
Potent |
5-10 grams |
Has been reported to be very helpful in activating methyl eugenol, dillapiole, elemicin, myristicin. Black pepper tea potently inhibits CYP2D6, and provides the amine piperidine for amination. |
Black Seed oil |
Potent |
500 mg |
It's used to potently inhibit CYP2D6 and inhibit CYP3A4 |
Cinnamon EO |
Potent |
200 mg (about 7 drops) used 1 hour before taking allylbenzenes |
Works for all allylbenzenes. The cinnamaldehyde in cinnamon OE depletes glutathione, a required step for boosting active alkaloid formation of allylbenzenes. |
EGCG |
Potent |
200 mg |
Used to potently inhibit SULT1A1 and SULT1A3 |
Glucosamine HCl |
Moderate |
700 mg (smaller doses not tested) |
Inhibits SSAO. Appears to boost the effects of most allylbenzenes. Other SSAO inhibitors such as coffee and phenylethylamine also have the same potentiating effect. It's not known how SSAO inhibitors interact with allylbenzenes or their metabolites. They possibly have some effect on theoretical ammonia based condensation products created in vivo such as 1'-oxoelemicin-Amine |
Kudzu |
Potent |
200 mg |
Used to potently inhibit SULT1A1 and induce 17bHSD2 |
L-Lysine |
Moderate |
1000 mg |
Provides piperidine. It appears to help activate all allylbenzenes if used several days in a row before using allylbenzenes. |
Pomegranate 40% ellagic acid extract |
Potent |
200-300 mg |
Used to induce 17bHSD2 (it normally contains gallic acid) and inhibit GST. Gallic acid induces 17bHSD2 but also induces SULT1A1 and SULT1A3 so it must be used with inhibitors of SULT1A1 and SULT1A3 |
Rooibos 20% gallic acid extract |
Potent |
100-200 mg |
Used to induce 17bHSD2. Gallic acid induces 17bHSD2 but also induces SULT1A1 and SULT1A3 so it must be used with inhibitors of SULT1A1 and SULT1A3 |
Rutin |
Moderate |
200 mg |
Used as an MAO-B inhibitor. It Appears to extends the effects of elemicin. |
Star Anise EO (Chinese not Japanese) |
Potent |
5-10 drops |
Works very well for transdermal use. Ground aniseed induces CYP2C9, and star anise EO contains many similar compounds, but it's not known if star anise EO also induces CYP2C9. |
Valerian root oil |
Potent |
3-5 drops |
Used to potently inhibit UGT2B7 and UGT1A9 |
Vitamin B9 (folic acid) |
Potent |
0.8-1.2 mg |
Used to induce CYP2C9 |
Miscellaneous Oral Activators
These have been found to be beneficial in most people. The exact mechanism at play is not known. These might not be effective in everyone.
Activator |
Effectiveness |
Dosage |
Notes |
Almonds |
? |
? |
Some reports suggest they help nutmeg |
Eggs |
? |
? |
Some reports suggest they help nutmeg |
German chamomile EO |
Moderate |
1-5 drops |
Can be helpful for elemicin |
L-Arginine |
? |
? |
More tests need to be done |
Star Fruit |
? |
? |
It has been used to activate methyl chavicol. It inhibits CYP3A4, and contains some inhibitors of MAO-B, SULT1A1, SULT1A3 and P-Glycoprotein. Because it contains some gallic acid it might also induce 17bHSD2 to some degree. |
Controversial Oral Activators
These help some people activate
allylbenzenes, but can delay the onset or weaken the effects in other people. The exact reason for this in unknown.
Activator |
Effectiveness |
Dosage |
Notes |
Black Pepper Powder |
Potent |
2 grams |
Very beneficial for nutmeg in some people. Some reports state that nutmeg is ineffective without it. It can delay the onset of the effects of elemicin by a few hours in some people, and weaken the effects. |
White Grapefruit juice |
Potent |
1-2 cups |
It has been reported to help some people get effects from nutmeg. It can greatly weaken and delay the onset of elemicin's effect for several hours in some people. |
Transdermal Activators
Activator |
Effectiveness |
Dosage |
Notes |
Aniseed (Anise) EO |
Potent |
1-2 drops |
Works very well for transdermal use with elemicin. Aniseed induces CYP2C9, but it's not known if the essential oil contains the active compound. |
German chamomile EO |
Moderate |
1 drop |
Can be very helpful for elemicin |
Calamus EO |
Potent |
1 drop |
It can activate elemicin stand alone in some people. It works very well transdermally |
Star Anise EO (Chinese not Japanese) |
Potent |
1-2 drops |
Works very well for transdermal use with elemicin. Ground aniseed induces CYP2C9, and star anise EO contains many similar compounds, but it's not known if star anise EO also induces CYP2C9. |
Bibliography
1. 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)
3. 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
4. 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
5. METHYLEUGENOL;
IARC MONOGRAPHS – 101
Download Attached PDF Document
6. 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
7. 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
8. 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
9. Immunochemical identification of hepatic protein adducts derived from estragole.
Wakazono H, Gardner I, Eliasson E, Coughtrie MW, Kenna JG, Caldwell J. PubMed:
9705747
10. 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
11. 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
12. 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