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New paper: HPBCD complexed DMT made 100% bioavailable sublingually under tongue


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#1 tregar

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Posted 15 April 2021 - 10:33 AM

There is a new paper out indicating that a 1:1 or 2:1 mix of HPBCD (hydroxy propyl beta cyclodextrin, on auction sites and elsewhere) to DMT can be made by placing for example 30mg freebase dmt on a spoon, add 30 to 60mg of HPBCD powder on top the DMT, add around 2 to 3 drops of water from a pipette, mix it all together for 20 seconds using a toothpick, then draw up liquid with pipette, place drops under tongue and hold for 10 minutes or so, the DMT will 100% completely dissolve into the bloodstream.

Strong effects at 5 minutes, intense rush & elevated heart rate, dilated pupils...neon colorful visuals/visions...peak at 30 to 45 minutes, duration 60 to 90 minutes.

Cyclodetrin to drug ratio is considered to be 1:1 or 2:1. So you can experiment with for example: 30mg HPBCD to 30mg DMT or 60mg HPBCD to 30mg DMT.

This was using DMT cleaned up using a sodium carbonate wash. PKA of DMT is 8.75 or so, so do not use a sodium bicarbonate wash -- it will eat up most of your DMT, as ph of bicarb is not high enough, it needs to be 1 to 2 points higher than PKA of DMT, at 11 or 11.5 or so is perfect, where 100% sodium carbonate PH is at, found in pool isle of home box store.

This would allow those who normally get nausea from oral preps to avoid the nausea. There is no burn under tongue, taste yes. I used this 4 times in one night over the course of several hours with THH, and my tongue was just fine, no burn or scarring. Felt just fine next day too. I experienced infinite beauty and visuals, very transcendent.

HPBCD is a new technology that allows freebase nonpolar drugs like DMT to be trapped by the cyclodextrin inner cavity which is composed of an inner "non-polar trap", and "outer polar cavity or cone" which allows the normally water insoluble DMT to be made 100% water soluble.

HPBCD is composed from a sugar molecule, it has been used to make (see table on page 1122) scores of other non-water soluble drugs 100% water soluble and reach peak activity as measurements of the drug in the bloodstream indicated that all of the freebase drug was absorbed effectively.

Other examples of non water soluble freebase non-polar drugs complexed with HPBCD made water soluble: hormones, pregnisolone, etc.

Apparently, this also makes the DMT absorb very well if taken orally as well, improving even the oral bio-availability by many factors when taken with RIMA's to activate it, etc.

Attached Thumbnails

  • HPBCD.JPG
  • HPBCD structure.JPG
  • HPBCD cone.JPG
  • freebase non-polar drugs made water soluble using HPBCD.JPG
  • pipette.JPG

Attached Files


Edited by tregar, 15 April 2021 - 03:25 PM.

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#2 newmoon

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Posted 15 April 2021 - 10:45 AM

Interesting; do you believe this allows sublingual DMT use without an MAOI?


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#3 tregar

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Posted 15 April 2021 - 10:54 AM

newmoon said:

Interesting; do you believe this allows sublingual DMT use without an MAOI?

Yes, absolutely. THH or tetrahydroharmine can be taken orally (100 to 200mg), my favorite in combo, while the DMT can be used sublingually, allowing the best of both worlds. Zero nausea. Have tried this in dreams several times, and it works extremely well, tryptamine rush felt around 5 or more minutes after sublingual application, peak at 30 to 45 minutes, like an extended sub-breakthrough, excellent for long lasting transcendental contemplation and work. Best to limit to once a week or so, so no tolerance.

professor8 (11/1/2010, he writes like a poet with special powers of imagination & expression):

Tetrahydroharmine (THH) has the ability to raise your vibration in a most powerful, yet subtle way. It brings a crystalline prismy texture to spice and adds a super clear watery dimension to Aya, like looking down through 10meters of shimmering Caribbean Sea on clear blue day. It brings a dimension of pure light to the entheogenic experience and encourages entities & intelligences of only the Highest Order. If one is not accustomed to perceiving these experiences with a spiritual perspective most of the nuances & subtleties THH brings on are overlooked and remain unseen and one would better enjoy Harmaline as a house painter chooses a roller over a brush, its about preference & choice.
 

Should add that music sounds quite incredible on a combo of 150mg or more of THH + DMT as tetrahydroharmine breaks down the filters or barriers in the mind, very similar to listening to music on cactus.

 

Don't forget that this should improve the ORAL BIOAVAILABILITY of dmt when combined with a RIMA as well -- by many factors -- this technology has been used to potentiate these freebase drugs ORALLY as well -- this could potentially mean a pharmahuasca experience that is very strong indeed!  :ohmy:  :smile: 


Edited by tregar, 15 April 2021 - 04:38 PM.

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#4 Chips101

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Posted 15 April 2021 - 08:57 PM

Will it also increase the bio activity of psilocybin or block it?

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#5 tregar

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Posted 16 April 2021 - 03:41 AM

Thanks newmoon and Chips101 for questions.

 

Chips101 said:

Will it also increase the bio activity of psilocybin or block it?

Great question Chips101. Psilocybin is an alkaloid that is already soluble in water, so its absorption into the bloodstream is not improved or enhanced by HPBCD's. HPBCD's is a technology used to greatly enhance the absorption of freebase or non-polar molecules, like freebase DMT. It makes it 100% water soluble.

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I strongly suggest taking 100, 150 or 200mg of THH or tetrahydroharmine first, then take the HPBCD complexed DMT under tongue around 30 minutes later. You can continue to take more HPBCD complexed DMT doses sublingually for several more hours. This results in a mind-expanding experience very similar to cactus -- music sounds incredible, infinite beauty is seen all around you, powerful spiritual insights and divine transcendence. THH has a half life of 10.5 hours, so for 5 hours you can enter this remarkable state of expanded divine consciousness.

 

You can alternately also combine the drops of HPBCD complexed DMT liquid with a warm to hot water solution of harmine and THH dissolved all together and ALL taken at the exact same time for a powerful pharmahuasca experience identical to true Ayahuasca. Freebase DMT complexed this way with HPBCD will dissolve into the bloodstream of the stomach very effectively when taken with harmine & THH, for a strong journey nearly identical to if you were to use strong water soluble psychotria leaf DMT actives, which is hard to find now days, with Hawaiian leaf nearly extinct.

 

Caapi contains tetrahydroharmine as it's second largest alkaloid, and contributes greatly to the experience in many postitive ways, besides it's visionary, brightening and coloring abilities, it goes way beyond that....it strongly inactivates barriers or filters in the brain (like LSD and cactus does) so that "mind at large" as coined by Aldous Huxley can be let loose a bit.

Mind at Large: https://en.wikipedia...i/Mind_at_Large

Tetrahydroharmine on it's own will also yield the same type visions as harmaline, it just takes more of it. For example, around 300mg of THH will yield the same visions as about 100mg harmaline...even if the THH dose is split in two over several hours, the visions will still be apparent some time after the 2nd dose takes effect, the doses are additive.

THH in the caapi also seems to strongly activate the right hand hemisphere of the brain-- the side that performs tasks that have do with creativity and the arts, feelings, visualizations, imagination, holistic thinking & intuition, empathy, spirituality & connectedness. Researchers found that the right side of the brain lit up in brain scans of people who took LSD, mescaline, or mushrooms. This includes tetrahydroharmine. The world is largely moving in the direction of the Left Brain: technology and science. What the world needs is to move in the direction of Right Brain development.

Quote from TIHKAL by Dr. Shulgin "More studies on tetrahydroharmine are absolutely imperative."

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This is why I suggest taking the DMT with tetrahydroharmine (as found in true Ayahuasca):

 

Thomas S. Ray, Psychedelics and the Human Receptorome (2010):
https://journals.plo...al.pone.0009019
hxxp://journals.plos.org/plosone/article?id=10.1371/journal.pone.0009019
Breadth of Receptor Binding, 4.00=max or "off the charts", 0.00=min

LSD: 5ht1a = 3.73, DMT: = 0.00, psilocin = 2.88, mescaline = 3.61, 5-meo-DMT: = 4.00 (make up >80% of brain 5-ht)
LSD: 5ht1b = 4.00, DMT: = 0.00, psilocin = 2.19, mescaline = 0.00, 5-meo-DMT: = 2.41
LSD: 5ht1d = 3.70, DMT: = 3.91, psilocin = 3.40, mescaline = 0.00, 5-meo-DMT: = 3.48
LSD: 5ht1e = 2.62, DMT: = 3.28, psilocin = 3.03, mescaline = 3.16, 5-meo-DMT: = 1.72
LSD: 5ht2a = 3.54, DMT: = 2.58, psilocin = 2.14, mescaline = 0.00, 5-meo-DMT: = 0.98
LSD: 5ht2b = 3.11, DMT: = 3.91, psilocin = 4.00, mescaline = 3.97, 5-meo-DMT: = 0.69 (sensual & entactogenic)
LSD: 5ht2c = 3.11, DMT: = 3.42, psilocin = 2.52, mescaline = 0.00, 5-meo-DMT: = 1.55
LSD: 5ht5a = 3.64, DMT: = 3.16, psilocin = 2.83, mescaline = 0.00, 5-meo-DMT: = 1.84
LSD: -5ht6 = 3.75, DMT: = 3.35, psilocin = 2.82, mescaline = 0.00, 5-meo-DMT: = 2.73
LSD: -5ht7 = 3.77, DMT: = 4.00, psilocin = 2.82, mescaline = 0.00, 5-meo-DMT: = 3.69 (novelty & new ideas)
LSD: ---D1 = 2.34, DMT: = 3.51, psilocin = 3.37, mescaline = 0.00, 5-meo-DMT: = 2.38
LSD: -A-2A = 2.93, DMT: = 2.75, psilocin = 1.36, mescaline = 2.92, 5-meo-DMT: = 0.00 (aesthetic/beauty adrenal a2a)
LSD: -A-2B = 0.00, DMT: = 3.53, psilocin = 1.57, mescaline = 0.00, 5-meo-DMT: = 0.86 (aesthetic/beauty adrenal a2b)
LSD: -A-2C = 0.00, DMT: = 3.53, psilocin = 1.03, mescaline = 4.00, 5-meo-DMT: = 1.57 (aesthetic/beauty adrenal a2c)

 

2011 Thomas S. Ray study: Breadth of Receptor Binding, 4.00=max, 0.00=min

LSD: 5ht1a = 3.73, DMT: = 0.00, psilocin = 2.88, mescaline = 3.61, 5-meo-DMT: = 4.00 (these serotonin filters/gates/barriers/doors make up >80% of brain 5-ht & are broken down when 5-ht1a is agonized)

 

Dr. Nichols (Heffter.org LSD paper):

LSD has very strong potency in blocking the action of serotonin. LSD is strongly "anti-serotonin". The morpholide lysergamide cousin had only about 1/10th the potency in blocking serotonin. Of the 5 diferent dialkylamides we studied LSD was the most potent and specific serotonin antagonist. 5-ht1a makes up >80% of brain 5-ht receptors.

As we go thru day to day life, the 5-ht1a brain serotonin filters (gates, or day to day survival filters as I like to call them) which make up over 80% of brain 5-ht are in place so that we will not be overwhelmed by the perception of the way things would appear to an un-filtered mind, or "Mind at Large" as Aldous Huxley describes it in "Doors of Perception" as "infinite or eternal". He also referred to the visions as coming from "the other world" in his book "Moksha". I prefer to think of it in similar terms as well "the spirit world" or "the other world".

5-ht1a inhibition by entheogens (in green above) theoretically cause this filter system to be lifted, and the infinite mind to manifest in combination with oral dmt with the tetrahydroharmine providing the 5-ht1a inhibition & additional adrenal system agonization (A2A thru A2C), just as bufotenine in snuff's provide the 5-ht1a inhibition combined with the dmt in the snuff's, resulting in a 3 hour experience ie both examples of Teamwork on how these entheogens are used traditionally in the Amazon.

Thomas S. Ray's study shows a value of 3.57 at SERT for Ibogaine (4.00 is max). Ibogaine has been shown to inhibit serotonin transporter (SERT) noncompetitively, in contrast to all other known inhibitors, which are competitive with substrate. Ibogaine inhibits both serotonin and dopamine reuptake transporters, it is an SDRI or serotonin & dopamine reuptake inhibitor. Tetrahydroharmine is a serotonin reuptake inhibitor, it is an SRI found in caapi. In other words, both are strong serotonin reuptake inhibitors which inhibit over 80% of brain 5-ht at 5-ht1a.

In contrast, as an example, Cocaethylene (coca leaf tea bags soaked in wine, the orally active & potent ingredient formed in the liver from cocaine + ethanol in the 1860's "Vin Mariani" wine popular with both Popes, Thomas Edison and scores of other famous people) increases the levels of serotonergic, noradrenergic, and dopaminergic neurotransmission in the brain by inhibiting the action of the serotonin transporter, norepinephrine transporter, and dopamine transporter. These pharmacological properties make cocaethylene a serotonin-norepinephrine-dopamine reuptake inhibitor [SNDRI; also known as a "triple reuptake inhibitor"].

Cocaethylene has a higher affinity for the dopamine transporter than does cocaine, but has a lower affinity for the serotonin and norepinephrine transporters. In McCance-Katz et alia's 1993 study cocaethylene "produced greater subjective ratings of 'High' in comparison with administration of cocaine or alcohol alone."

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The Ayahuasca closed eye visions using 100, 150 to 200mg tetrahydroharmine or THH and HPBCD complexed DMT (30mg on up) together surpass in magnificence anything I have ever seen in reality or in works of art.

With open eyes, all spiritual things such as nature, art, female form, beauty, joy, take on significant meaning with infinite beauty, just like with cactus or LSD. Extraordinary beauty is manifested with open eyes and with the visions one sees with closed eyes. Impossible neon-like colors are seen that don't exist on this Earth.

The existence of a higher spiritual plane is recognized to which insight can and must be gained, yet it does not reject the mundane reality as inferior or empty. This joyous embracement of the world of form leads to words like infinite pleasure, beauty and joy. This loving reappraisal of the worldly forms leads the way to higher divine planes.


Edited by tregar, 16 April 2021 - 04:45 AM.

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#6 tregar

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Posted 16 April 2021 - 12:12 PM

FYI: The THH is an SRI (serotonin reuptake inhibitor with significant adrenal activity at A2A thru A2C receptors, similar to mescaline in that regard), it has super weak MAOI activity (see Wikipedia on tetrahydroharmine).

I also looked up the data comparing RIMA activity of THH to harmine from a lab supplier who gave the data, and they referenced THH as only having around 1/100th the RIMA strength of harmine, practically non-existent strength as a RIMA. That would mean it would take 20,000mg of THH to equal 200mg of harmine in RIMA strength. Harmine & harmaline however have significant RIMA/MAOI activity.

P.S. I have not actually tried the sublingual DMT by itself, I always prefer it with THH taken orally about 1/2 hour before applying the sublingual HPBCD DMT under my tongue. THH will not activate the DMT at all, but the combo of the two (oral THH + sublingual complexed DMT) is my absolute favorite after trying this several times.

How to best describe THH or tetrahydroharmine:

THH alone (200 to 300mg) with open eyes = everything is brighter and extremely colorful, beauty enhancement is over the top...neon-diamondlike is my best description, like looking down thru several meters of clear blue ocean water on a bright sunny day, just like professor8 describes it. A study done once on the UDV found that brews with high levels of tetrahydroharmine were preferred over all other brews, they found the "dmt was not the main attraction" but actually brews high in THH, fascinating study.

With 250mg to 300mg THH, closed eye dream-like Ayahuasca visions actually form with closed eyes that begin with colored sparkles and geometric dots and ziggly lines in orange, green, and blue that dart around and then progress to the monochrome visions for 1.5 to 2 hours, These visions are WAY beyond 4k, and highly detailed. The DMT seems to add color and brightness to the visions. The DMT also of course adds strong psychedelic alterations & activity to the journey and enhances the quality of music in combo with THH, music sounds incredible as mentioned before for several hours, especially if you keep taking the sublingual DMT around once an hour for the next 3 hours.


Edited by tregar, 16 April 2021 - 05:52 PM.

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#7 newmoon

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Posted 16 April 2021 - 01:58 PM

This thread at the nexus suggests that this isn't a viable route for DMT alone. However, this led me to learn about complexing salvinorins with HPBCD, so I've ordered some and intend to try that with Salvia divinorum extracts. Thanks, tregar, for putting this interesting information here!


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#8 tregar

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Posted 16 April 2021 - 05:01 PM

Glad I could be of help Newmoon, let us know how it works. 
 
Attached another paper (see Table 2) showing various freebase non-water soluble compounds...notice the higher the non-water soluble compound was, just like the paper states, the greater it was taken up by the HPBCD complex...take testosterone for example in Table 2, It has only 0.026 mg/ml solubility in water, but when complexed with HPBCD, achieved 38mg/ml solubility in water! When HPBCD drug complex is held under tongue for around 10 minutes, absorption is full on. 

Attached Files


Edited by tregar, 16 April 2021 - 05:24 PM.

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#9 tregar

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Posted 16 April 2021 - 07:00 PM

A little off topic, but I think tetrahydroharmine is a pretty special compound, I've used 250mg of it to potentiate cactus to very strong levels, it makes a 12" medium san pedro cactus which may contain around 300mg mescaline feel like a large 12" thick san pedro cactus containing around 450mg mescaline. It makes a 12" bridgesii cactus feel like a 16" bridgesii cactus.

 

In the data I've seen for THH, it strongly blocks serotonin just like cactus, but also agonizes the adrenal A2A thru A2C receptors (the receptors associated with aesthetics & beauty), just like mescaline has been shown to do receptorome rise, explaining perhaps why they "overlap" so well. THH being able to make mescaline in cactus feel much stronger than it really is. Anyone who has ever taken cactus or high dose THH knows the beauty you see and experience is "over the top".

 

But you have to stagger the THH from the cactus by taking the tetrahydroharmine around an hour after the cactus is taken, that way any minor maoi's or rima's in the cactus won't interact with the SRI which is THH, which can result in a faster heartbeat for a few hours which has happened to me before...so long as you take it later, it potentiates the cactus quite incredibly...it feels like I've taken 450mg of mescaline containing cactus when it's really only 300mg mescaline containing cactus, and they both lasts around 6 hours with super strong activity, so they wear off at around the same time.

 

It works so well, I won't take cactus any other way from now on. I get much more mileage from cactus this way. Visuals and visions are insane, music is so good sounding, you would think you were an alien experiencing sound and music for the very first time, every instrument stands out on it's own, like hearing a track for the very first time.


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#10 tregar

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Posted 17 April 2021 - 05:17 AM

I underestimated the post right above, and since I could not edit, rewrote it again to give better descriptions of the experiences:
 
A little off topic, but I think tetrahydroharmine is a pretty special compound. I've used 250mg of it to potentiate cactus to very strong levels, it makes a 12" medium san pedro cactus tea which may contain around 250mg mescaline feel like an X-large 12" thick san pedro cactus containing around 400mg mescaline. It makes a 12" thick bridgesii cactus feel closer to a tea made with a 12" bridgesii cactus along with an extra 6" piece.
 
In the data I've seen for THH, it strongly blocks serotonin just like cactus, but also agonizes the adrenal A2A thru A2C receptors (the receptors associated with aesthetics & beauty), just like mescaline has been shown to do receptorome wise, explaining perhaps why they "overlap" so well. THH being able to make mescaline in cactus feel much stronger than it really is. Anyone who has ever taken cactus or high dose THH knows the appreciation for beauty experienced is "over the top".
 
But you have to stagger the THH from the cactus by taking the tetrahydroharmine around an hour after the cactus is taken, that way any minor maoi's or rima's in the cactus won't interact with the SRI which is THH, which can result in a faster heartbeat for a few hours which has happened to me before...so long as you take it later, it potentiates the cactus quite incredibly...it feels like I've taken 400mg of mescaline containing cactus tea when it's really only 250mg mescaline containing cactus, and they both lasts around 6 hours with super strong activity, so they wind down at around the same time. I have around 7 months experience combining the two, giving myself around 2 weeks apart from journeys.
 
It works so well, I won't take cactus any other way from now on. I get much more mileage from cactus this way. Visuals and visions are insane, music is so good sounding, you would think you were an alien experiencing sound and music for the very first time, every instrument stands out on it's own, like hearing a track for the very first time.
 
It's a game changer.

Attached Thumbnails

  • Solubility in water after HPBCD complexing.JPG

Edited by tregar, 17 April 2021 - 06:39 AM.


#11 tregar

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Posted 17 April 2021 - 08:20 AM

A litte bit more on sublingual & nasal HPBCD complexed pharmaceuticals:

Several years ago, before "prohormones" were banned, there was a company called "Ergopharm" ran by chemist Patrick Arnold that made HPBCD complexed solutions of prohormones in a nasal spray & in a HPBCD complexed powder that was administered under tongue.

In 2001 Arnold's company introduced the prohormone 4-Androstenediol, under the marketing name 4-AD. 4-AD is a prohormone that is easily converted by the body into testosterone, and it sold well. He is the chemist who created hydroxypropyl-beta-cyclodextrin complexed diols such as Cyclo-Diol™ and Cyclo-Nordiol™.

https://thinksteroid...rick-arnold-11/

https://en.wikipedia...-Androstenediol

I bought and used the nasal spray and it was very effective, had my testosterone level checked with a blood test at the local labcore one hour after administering the spray and it was 3,500 ng/dl ! when my normal level was 600ng/dl. Highest measured normal levels in men are around 1200 ng/dl. The blood test cost me $70.00. It had strong mental effects as well. The spray would cause the 4-ad to enter the bloodstream nasally, and convert to testosterone via enzyme activity.

Patrick Arnold also made a sublingual powder of HPBCD complexed 1-AD that could be grabbed from the bottle with a pre-measured scooper, and the powder held under tongue for 10 to 15 minutes, sold just as well as the nasal spray, I tried the sublingual product he sold, and that again was effective.
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In closing, the oral route using HPBCD complexed DMT in combination with a pharmahuasca RIMA/SRI combo (taken all at the same time in a hot water tea) holds much promise as well, for greatly increased absorption & strength.
 

Keep in mind that only a portion or "tail end" of the host molecule is needed to attach or fit into the cyclodextrin cone, and that's all that is needed to be "trapped". I attached a picture of this below. The cyclodextrins have toroidal shapes, with the larger and the smaller openings of the toroid exposing to the solvent secondary and primary hydroxyl groups respectively.

Attached Thumbnails

  • portion of molecule trapped in cyclodextrin.JPG

Edited by tregar, 17 April 2021 - 03:15 PM.

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#12 tregar

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Posted 17 April 2021 - 01:45 PM

IMPORTANT!!! -----------------------------------Major correction to 1st post:------------------------------------------------------

 

I remember pouring an excess of HPBCD onto the DMT. My chemist friend helped me in clarifying the molar ratio. I see that dmt molar weight = 188 g/mol and HPBCD has a molecular weight of between 1200 to 1500g/mol depending on what source you look at. Even though I weighed out twice as much HPBCD, I did go back into the tub of HPBCD and grab an even larger amount with end of dash weigher and poured that on top the DMT in the spoon as well, as I remember reading long ago some had used closer to 1:10 gram ratio for other really small gram weight molecules. I was unsure on how much to use exactly, but I did pour an excess on top the DMT way beyond the 60mg, several large drops did dissolve it all. I should have clarified that in first post. From now on I will use a 1:7 gram weight ratio of DMT to HPBCD in order to keep an equimolar ratio of DMT to HPBCD at 1:1. many thanks to my chemist friend! :smile:

 

From now on will use exactly 30mg DMT to 210mg HPBCD when dissolving on spoon.

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1st post re-written correctly:

 

I used a 7:1 gram weight ratio of HPBCD (hydroxy propyl beta cyclodextrin, molar weight between 1200 to 1500 g/mol), on auction sites and elsewhere, to DMT (molar weight = 188g/mol) in order to keep the molar ratio of cyclodextrin to host drug at a 1:1 molar ratio. What I did was place for example 30mg freebase dmt on a spoon, add 210mg of HPBCD powder on top the DMT, add several large drops of water from a pipette, mix it all together for 20 seconds using a toothpick, then draw up liquid with pipette, place drops under tongue and hold for 10 minutes or so, the DMT will dissolve into the bloodstream.

 

Most studies recommend a 1:1 equimolar ratio of HPBCD to host drug for complexing. 

 

My experience with the sublingual route: 10 minute duration of sublingual application under tongue, then 5 minutes after that, heart rate increased, very fast pulse, pupils dilated large when I looked in mirror, tryptamine buzz rush felt take over the body, neon colors & visuals very apparent, 60 to 90 minutes of pure bliss psychedelic state that overlapped the THH journey with precision, I could not have asked for more. I've taken Ayahuasca with Caapi & Hawaiian psychotria over 65 times at moderate to very strong doses over many years, and this was no different. I look forward to trying the oral HPBCD complexed route as well in future.

This was using DMT cleaned up using a sodium carbonate wash. PKA of DMT is 8.75 or so, so do not use a sodium bicarbonate wash -- it will eat up most of your DMT, as ph of bicarb is not high enough, it needs to be 1 to 2 points higher than PKA of DMT, at 11 or 11.5 or so is perfect, where 100% sodium carbonate PH is at, found in pool isle of home box store.

This would allow those who normally get nausea from oral preps to avoid the nausea. There is no burn under tongue, taste yes. I used this 4 times in one night over the course of several hours with THH, and my tongue was just fine, no burn or scarring. Felt just fine next day too. I experienced infinite beauty and visuals, very transcendent.

HPBCD is a new technology that allows freebase nonpolar drugs like DMT to be trapped by the cyclodextrin inner cavity which is composed of an inner "non-polar trap", and "outer polar cavity or cone" which allows the normally water insoluble DMT to be made 100% water soluble.

HPBCD is composed from a sugar molecule, it has been used to make (see table on page 1122) scores of other non-water soluble drugs 100% water soluble and reach peak activity as measurements of the drug in the bloodstream indicated that all of the freebase drug was absorbed effectively.

Other examples of non water soluble freebase non-polar drugs complexed with HPBCD made water soluble: hormones, pregnisolone, etc.

Apparently, this also makes the DMT absorb very well if taken orally as well, improving even the oral bio-availability by many factors when taken with RIMA's to activate it, etc.
----------------------------------------
THH or tetrahydroharmine can be taken orally (100 to 200mg), my favorite in combo, while the DMT can be used sublingually, allowing the best of both worlds. Zero nausea. Have tried this in dreams several times, and it works extremely well, tryptamine rush felt around 5 or more minutes after sublingual application, peak at 30 to 45 minutes, like an extended sub-breakthrough, excellent for long lasting transcendental contemplation and work. Best to limit to once a week or so, so no tolerance.

 

Professor8 (2010):

Tetrahydroharmine (THH) has the ability to raise your vibration in a most powerful, yet subtle way. It brings a crystalline prismy texture to spice and adds a super clear watery dimension to Aya, like looking down through 10meters of shimmering Caribbean Sea on clear blue day. It brings a dimension of pure light to the entheogenic experience and encourages entities & intelligences of only the Highest Order. If one is not accustomed to perceiving these experiences with a spiritual perspective most of the nuances & subtleties THH brings on are overlooked and remain unseen and one would better enjoy Harmaline as a house painter chooses a roller over a brush, its about preference & choice.

 

Should add that music sounds quite incredible on a combo of 150mg or more of THH + DMT as tetrahydroharmine breaks down the filters or barriers in the mind, very similar to listening to music on cactus.

Don't forget that this should improve the ORAL BIOAVAILABILITY of dmt when combined with a RIMA as well -- by many factors -- this technology has been used to potentiate these freebase drugs ORALLY as well -- this could potentially mean a pharmahuasca experience that is very strong indeed!


Edited by tregar, 17 April 2021 - 05:48 PM.


#13 Norman

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Posted 17 April 2021 - 02:33 PM

This thread at the nexus suggests that this isn't a viable route for DMT alone. However, this led me to learn about complexing salvinorins with HPBCD, so I've ordered some and intend to try that with Salvia divinorum extracts. Thanks, tregar, for putting this interesting information here!


That thread is over nine years old and went nowhere on the DMT Nexus, so no I agree that this isn’t likely a miracle sublingual route for DMT solo.
Salvia, on the other hand, or anything else orally active at dropwise doses might be interesting. Siebert wrote about sublingual salvia dosing using an acetone tincture, of all things. He’s tougher than me on that but ethanol might be an option or maybe this method would be a way around both without having the underside of your tongue scorched for ten minutes.

#14 tregar

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Posted 17 April 2021 - 04:47 PM

Norman said:

That thread is over nine years old and went nowhere on the DMT Nexus, so no I agree that this isn’t likely a miracle sublingual route for DMT solo.
Salvia, on the other hand, or anything else orally active at dropwise doses might be interesting. Siebert wrote about sublingual salvia dosing using an acetone tincture, of all things. He’s tougher than me on that but ethanol might be an option or maybe this method would be a way around both without having the underside of your tongue scorched for ten minutes

Newmoon and Norman, I read the complete DMT nexus thread (all 3 pages) from beginning to end and it was all just talk, Nobody and mean nobody even attempted to create a HPBCD complex of DMT.

FYI: Here is the thread Newmoon found from DMT nexus on "Complexing DMT freebase for sublingual administration"

https://www.dmt-nexu...g=posts&t=30071

As far as I know, I am the only one so far to have done this sucessfully. It is extremely easy. Back then when the nexus had that thread, commercial HPBCD was not even available on auction sites or anywhere else. I had bought mine from a bulk supplier on a whim over 12 years ago, and stored the whole tub in my closet, and just pulled it out the other day to use it for the 1st time on DMT, and I'm so glad I did! It does indeed work very well, and I plan to use if for the rest of my life.

Years ago, I took DMT freebase (70 to 90mg) with harmine and THH pharmahuasca at least a dozen times, and found it mild at best (on a Shulgin scale of 1 to 5, they were all +3 experiences). I even tried to dissolve it into coca cola and citric acid in hot water to make it absorb better as the salt, but it only slightly increased the strength.

The sublingual HPBCD complexed DMT tried the other day was all encompassing and strong at only 30mg, very impressed, I can only imagine where stronger doses will carry this psychonaut.

After that I switched to taking 30 to 35 grams of Hawaiian psychotria boiled down to a couple oz, then added the harmine + thh to the 2oz of hot pychotria tea....well that blew my mind CONSISTENTLY for many years, as I continued to use it over 65 times! Most of the experiences were +4 to +5, very strong indeed, much stronger than the freebase used dmt.

This agrees with what I read from clearlight:

Clearlight experiments that involved several people found the leaf brew form superior to extracted actives, they found the leaf brews very strong and powerful & clairavoyant (+5 Shulgin scale), while they mentioned that the extracted actives were mild (+3 Shulgin scale) at best, even up to 100mg. Again, this is poorly understood.


Even Jonathan Ott found that in his 20 experiments posted in his book "Ayahuasca Analogues", that none of his later experiments with extracted actives quite matched the power of his 1st actual Ayahuasca brewed with caapi and good real leaf (experiment #1), he had no explanation for this. He did however find 70mg to be close to it, but still not the same.

However, at this point, I have noticed that ALL the dried Hawaiian psychotria is extinct, and is no longer available. So I am looking forward in dreams to oral HPBCD complexed DMT at around 60mg on up, and hoping this will do the trick, I'm sure it will after having experienced what I really love with the 30mg sublingual HPBCD complexed DMT.

I have read HPBCD complexing these non-water soluble freebase drugs to make them orally 100% water soluble should make it absorb very effectively in the body, so I do believe it will be possible to once again achieve very strong journeys, similar to the ones I used to have using strong water soluble psychotria leaf.

I often found the oral DMT too short as it would wind down after 90 minutes of taking the pharmahuasca, and I am very glad I found this new complexing method so that I can take a "sublingual dose" if I choose at 90 minutes, to extend the journey at least another 90 minutes, to get a full 3 hours of strong activity out of it, that is my goal, and I feel I am one step closer after having experienced the 30mg HPBCD complexed DMT experiment that was successful.

 

"Sublingual mucosa as a route for systemic drug delivery" by Narang & Sharma 2010:

https://innovareacad...Suppl2/1092.pdf

-------------------------------------------------------------------------------------------------------------------------------------------------------------

With Insufflation, sublingual or rectal, DMT is not broken down by monoamine oxidase.
 
See above paper from Narang et al, Intl J Pharm Sci, Vol 3, Suupl 2, 2011, 18-22:
"With sublingual or "under the tongue", the mucosea thickness is only 100-200, high permeability with rich blood supply, much better than buccal or gingival & palatal, 200, 250, 500 micrometer respectively, shuttling the drug directly to bloodstream." The DMT is not broken down via monamine oxidase whatsoever this way. It avoids the liver and first pass metabolism. The drug is rapidly absorbed via the rich blood supply vessels under the tongue rather than being broken down in the digestive track via the enzyme monamine oxidase. According to paper: "Sublingually administered drugs reach directly in to the blood stream through the ventral surface of the tongue and floor of the mouth. The drug solutes are rapidly absorbed into the reticulated vein which lies underneath the oral mucosa, and transported through the facial veins, internal jugular vein, and braciocephalic vein and then drained in to systemic circulation."
 
According to paper, "the absorption of drugs through the sublingual route is 3 to 10 times greater than oral route and is surpassed by hypodermic injection. Peak blood levels of most products administered sublingually are achieved within 10 to 15 minutes, which is generally much faster than when those same drugs are ingested orally." This has been my experience as well, after 10 minutes of sublingual under tongue application, 5 minutes after the 10 minute sublingual absorption, the DMT rush is felt, followed by 60 to 90 minutes of entheogenic activity. According to paper, "sublingual absorption of drugs is efficient. The percent of each dose absorbed is generally higher than that achieved by means of oral ingestion."
 
Smoked: If DMT is smoked, the maximal effects last for a short period of time (5 to 30 minutes, dose-dependent). The onset after inhalation is very fast (less than 45 seconds) and maximal effects are reached within about a minute.
 
Insufflation & Sublingual absorption via Oral Mucosa (under tongue): When DMT is insufflated (snorted through the nostrils) or absorbed sublingually via the complexing of the drug with HPBCD to make it water soluble, the duration is markedly increased.
 
Injection: Injected DMT produces an experience similar to inhalation in duration, intensity, and characteristics.
 
Oral ingestion: DMT, which is broken down by the digestive enzyme monoamine oxidase, is practically inactive if taken orally, unless combined with a monoamine oxidase inhibitor (MAOI).
 
See post #11 on nasally and sublingually (under the tongue) delivered HPBCD complexed pro-hormones & testosterone, all very poorly water soluble like DMT, made water soluble with HPBCD.

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Edited by tregar, 17 April 2021 - 07:28 PM.

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#15 newmoon

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Posted 17 April 2021 - 09:11 PM

I'll give it a try once the HPBCD arrives.


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#16 tregar

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Posted 18 April 2021 - 06:54 AM

Newmoon said:
I'll give it a try once the HPBCD arrives.
1) Also, don't forget the MAJOR CORRECTION to the numbers from post #1, re-written in post #12.
 
You will want to use a 1:1 molar ratio of HPBCD to DMT, but this means using a 7:1 ratio in milligram weight which translates to 210mg of HPBCD placed on top the 30mg of DMT on the spoon, add many drops of water from a pipette, mash & stir for at least 20 seconds or more before placing under tongue -- hold for at least 10 minutes, I prefer 15 minutes. You will feel strong effects around 5 minutes after the 10 to 15 sublingual "under tongue" period is over, and it's been dissolved. 
 
2) Also, don't forget this makes HPBCD complexed DMT drops which can be added to a hot water tea that already has (around 180 to 220mg) harmine and (150 to 250mg) tetrahydroharmine dissolved in it (using added crushed vitamin C or similar to dissolve) for a SUPER POTENT ORAL pharmahuasca exeperience. Mix it all together and take at the exact same time, just as the Shaman's do. This is how I used to take the Ayahuasca over 65 times I made using same ingredients mixed into 2oz of hot psychotria leaf tea filtered and boiled down to 2oz. 
 
3) Don't forget the importance of tetrahydroharine or THH, which is 2nd highest ingredient in Caapi made Ayahuasca...you will want to experience real TRUE Ayahuasca, which is a brew high in it (from 150 to 250mg, 250 to 300mg for intense visions):
 
My last taking 300mg of THH, I saw the interior decorations of palaces, the checkered floors, the beautiful windows and furniture, the winding stair cases, I was blown away, I've seen sacred temples for religious worship, beautiful animals and super fine women, birds of all kinds, Caapi tells a story when you drink it with eyes closed, it teaches you things, the most beautiful "realistic visions" that no other entheogen comes close to showing you, these realistic visions go on for long periods.
 
THH with open eyes: everything is brighter and extremely colorful, beauty enhancement is over the top...neon-diamondlike is my best description, like looking down thru several meters of clear blue ocean water on a bright sunny day.
 
All of the closed eye visions for me begin with colored sparkles and geometric dots and ziggly lines in orange, green, and blue that dart around and then progress to the monochrome visions for 1.5 to 2 hours. These visions are WAY beyond 4k, and highly detailed. The DMT adds brightness and color to the visions, for example, animals seen will have colored patterning. It also adds strong psychedelic alterations to the journey. Music will sound very alien & incredibly good. 
 
In one past journey, saw three beautiful naked woman dancers twirling in front of stone pillars that rotated slowly. Jungle scenes lit up by the moonlight, full of snakes and palm trees by the beach and lots of people I had known in my life in floating bubbles that were to the left and right of the scene, drifting up into the sky. Elephants from India embellished with vibrantly colored jhools (saddle cloth) and heavy jewellery and sparkling anklets. Detached female faces of breath-taking beauty with freckles. Waterfalls in the middle of the jungle. 
 
With another session, saw barely dressed women wearing futuristic clothing and bikinis of some sort, dazzling in it's design. A spinning vortex made of blue color with closed eyes that opened up in front of me that looked like a wormhole of some sort, I travelled inside of it, and was dropped off on an island in the pacific with wooden Tikis all around the perimeter of a small culture. I saw a chalkboard full of mathematical equations and scientific discoveries drawn out. I flew like a bird for nearly a minute over what looked like Los Angeles, as I could see the homes with swimming pools and parks below me. 
 
I've seen pyramids adorned with gold sheen, architecture of the past and future, Egyptian scenery, vast landscapes, medieval scenery, it goes on and on. Everything is brand new as if newly created. Very similar to the Ayahuasca visions encountered by Benny Shanon in "Antipodes of the Mind". 
 
Stay true to yourself. Love, Peace & music

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#17 newmoon

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Posted 18 April 2021 - 05:30 PM

Reading a bit turns up suggestions that ethanol will likely work better than water as the solvent (evaporating it off at the end), and that complexing for a long amount of time with magnetic stirring might be worthwhile. So, I'll probably try that.

 

I'm curious to see if this will make DMT active sublingually by itself, without other compounds; at this point I'd rather use more traditional leaf/vine preparations for ayahuasca.


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#18 tregar

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Posted 19 April 2021 - 06:01 AM

Newmoon said:
Reading a bit turns up suggestions that ethanol will likely work better than water as the solvent (evaporating it off at the end), and that complexing for a long amount of time with magnetic stirring might be worthwhile. So, I'll probably try that.
 
I'm curious to see if this will make DMT active sublingually by itself, without other compounds; at this point I'd rather use more traditional leaf/vine preparations for ayahuasca.
 
Sounds good Newmoon. I have in the past done exactly like you and used 95% ethanol and stir mantel to the do the same. You should have fine results. I've been lifting weights since my early 20's. I bought my 1kg tub of HPBCD from a supplier of sports supplements long ago believe it or not, dirt cheap. Back in the early 2000's I learned weight lifters were doing fast and efficient complexing of prohormones with HPBCD, just by putting the prohormone on a spoon, adding the HPBCD on top, adding drops of water and stirring it for 30 seconds and letting it melt all together, by heating up the spoon a bit. It's fast and works well too (heating of spoon and melting is not necessary I discovered unless you prefer). I prefer simplicity since I tend to use 3 to 4 doses of this sublingual DMT over the course of a night with oral tetrahydroharmine taken earlier.
 
30mg of HPBCD complexed very clean DMT held under tongue for 15 minutes indeed resulted in a tryptamine "rush & buzz", dilated pupils super wide, increased heart rate and pulse greatly, and resulted in visuals with neon coloring. Narang and Sharma mention in their 2010 sublingual paper that under the tongue pharmaceuticals can be 3 to 10 times more bioavailable than oral.
 
FYI: Just so you all know I am not full of hot air, I was the one who introduced HPBCD complexing to 25i-nbome at the BL forum back in Jan of 2012, after that virtually every vendor in the world of the nbome's took my idea and begin marketing them as such. Some of my other topics have been how to convert 4-aco-dmt to 4-ho-dmt (actual psilocin). However, I am only into Ayahuasca and cactus. I regret the whole nbome thing, and threw all of mine out many, many years ago. I hate that nasty compound. Most of you have probably noticed I work with natural psychedelics, I avoid all man-made psychedelics. You can see where I introduced it in below link in 2012:

Edited by tregar, 19 April 2021 - 08:13 AM.

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#19 tregar

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Posted 20 April 2021 - 06:13 AM

Narang and Sharma mention in their 2010 sublingual paper that under the tongue pharmaceuticals can be 3 to 10 times more bioavailable than oral. HPBCD makes the non-water soluble DMT water soluble. It traps and delivers small molecules such as DMT extremely effectively across the mucosa membrane under the tongue, with it's high permeability (only 100 to 200 micrometers thick) and rich blood supply--shuttling the DMT directly to bloodstream.



#20 tregar

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Posted 22 April 2021 - 12:12 PM

IMPORTANT!: Post #1 corrected HPBCD to DMT mg ratio...and also added link to a paper at very bottom showing that even 50 to 100mg sublingual doses of pharmaceuticals shown to be very effective!
 
HPBCD complexed DMT made bioavailable sublingually under tongue, also improves oral bioavailability for pharmahuasca & Ayahuasca
 
I used a 7:1 gram weight ratio of HPBCD (hydroxy propyl beta cyclodextrin, molar weight between 1200 to 1500 g/mol) on auction sites and elsewhere, to DMT (molar weight = 188g/mol) in order to keep the molar ratio of cyclodextrin to host drug at a 1:1 molar ratio. What I did was place for example 30mg freebase dmt on a spoon, add 210mg of HPBCD powder on top the DMT, add many drops of water from a pipette, mix it all together for 30 seconds using a toothpick, then draw up liquid with pipette, place drops under tongue and hold for 10 minutes or so...I prefer 15 minutes. The DMT will dissolve into the bloodstream.
 
 Narang and Sharma mention in their 2010 sublingual paper that under the tongue pharmaceuticals can be 3 to 10 times more bioavailable than oral. HPBCD makes the non-water soluble DMT water soluble. It traps and delivers small molecules such as DMT extremely effectively across the mucosa membrane under the tongue, with it's high permeability (only 100 to 200 micrometers thick) and rich blood supply--shuttling the DMT directly to bloodstream.
 
 Most studies recommend a 1:1 equimolar ratio of HPBCD to host drug for complexing.
 
 Strong effects at 5 minutes after the end of the 10 to 15 minute sublingual drug delivery under tongue: tryptamine rush/buzz & greatly elevated heart rate & pulse, dilated pupils...neon colorful visuals/visions...peak at 30 to 45 minutes, duration 60 to 90 minutes.
 
 This was using DMT cleaned up using a sodium carbonate wash. PKA of DMT is 8.75 or so, so do not use a sodium bicarbonate wash -- it will eat up most of your DMT, as ph of bicarb is not high enough, it needs to be 1 to 2 points higher than PKA of DMT, at 11 or 11.5 or so is perfect, where 100% sodium carbonate PH is at, found in pool isle of home box store.
 
 This would allow those who normally get nausea from oral preps to avoid the nausea. There is no burn under tongue, taste yes. I used this 4 times in one night over the course of several hours with THH, and my tongue was just fine, no burn or scarring. Felt just fine next day too. I experienced infinite beauty and visuals, very transcendent.
 
 HPBCD is a new technology that allows freebase nonpolar drugs like DMT to be trapped by the cyclodextrin inner cavity which is composed of an inner "non-polar trap", and "outer polar cavity or cone" which allows the normally water insoluble DMT to be made 100% water soluble.
 
 HPBCD is composed from a sugar molecule, it has been used to make scores of other non-water soluble drugs 100% water soluble and reach peak activity as measurements of the drug in the bloodstream indicated that all of the freebase drug was absorbed effectively.
 
 Other examples of non water soluble freebase non-polar drugs complexed with HPBCD made water soluble: hormones, pregnisolone, etc.
 
 Apparently, this also makes the DMT absorb very well if taken orally as well, improving even the oral bio-availability by many factors when taken with RIMA's to activate it, etc.
 ---------------------------------------------------------------
 THH or tetrahydroharmine can be taken orally (100 to 200mg), my favorite in combo, while the DMT can be used sublingually, allowing the best of both worlds. Zero nausea. Have tried this in dreams several times, and it works extremely well, tryptamine rush felt around 5 or more minutes after sublingual application, peak at 30 to 45 minutes, like an extended sub-breakthrough, excellent for long lasting transcendental contemplation and work. Best to limit to once a week or so, so no tolerance.
 
 professor8 (11/1/2010, he writes like a poet with special powers of imagination & expression):
Tetrahydroharmine (THH) has the ability to raise your vibration in a most powerful, yet subtle way. It brings a crystalline prismy texture to spice and adds a super clear watery dimension to Aya, like looking down through 10meters of shimmering Caribbean Sea on clear blue day. It brings a dimension of pure light to the entheogenic experience and encourages entities & intelligences of only the Highest Order. If one is not accustomed to perceiving these experiences with a spiritual perspective most of the nuances & subtleties THH brings on are overlooked and remain unseen and one would better enjoy Harmaline as a house painter chooses a roller over a brush, its about preference & choice. 
 
Should add that music sounds quite incredible on a combo of 150mg or more of THH + DMT as tetrahydroharmine breaks down the filters or barriers in the mind, very similar to listening to music on cactus.
 
 Don't forget that this should improve the ORAL BIOAVAILABILITY of dmt when combined with a RIMA as well -- by many factors -- this technology has been used to potentiate these freebase drugs ORALLY as well -- this could potentially mean a pharmahuasca experience that is very strong indeed!
 --------------------------------------------------------------
 "Sublingual mucosa as a route for systemic drug delivery" by Narang & Sharma 2010:
 
 
As you can see from the bottom linked sublingual viagra study, even 50 to 100mg doses can be administered under the tongue, the authors noting that less of the drug was required, and that it began working in only one half the normal time of an oral dose:
 
"The start of pharmacological activity after sublingual administration of sildenafil citrate in 30 patients affected by erectile dysfunction." by Siati & Franzolin 2003. 
 
------------------------------------------------------------------------------------------------------------------
Here are a few of my other topics in case you are interested:
 
 13,000 views:
 Positronic Ayahuasca brewing
 
12,000 views:
Receptorome study: how traditional Ayahuasca & snuffs differ from dmt
 
6,000 views:
New research: Morning glory contains 5 stimulating LSD-like drugs, soluble only in wine/alcohol, only sparingly soluble in water

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Edited by tregar, 22 April 2021 - 05:18 PM.





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