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Tryptamines HPBCD DMT very bioavailable sublingually under tongue, combo with tetrahydroharmine, Ayahuasca

tregar

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2 minute formed HPBCD DMT liquid very bioavailable sublingually under tongue & outperforms DMT salts orally by many factors in personal trials, combo with tetrahydroharmine, Ayahuasca.

HPBCD DMT very bioavailable sublingually under tongue, combo with tetrahydroharmine, Ayahuasca - Pharmahuasca - Welcome to the DMT-Nexus

Part 1: HPBCD complexed DMT experimental dosage, effects & duration
Part 2: receptorome chart & explanation
Part 3: Tetrahydroharmine (THH) effects
Part 4: Tetrahydroharmine receptorome similarities to mescaline; potentiates cactus & safety note
Part 5: chemist Patrick Arnold's HPBCD prohormones & bloodwork studies
part 6: Dr. Narang: "with sublingual" or "under the tongue" better than buccal, gingival & palatal
part 7: a little bit on my 70 Ayahuasca experiences, doses & visions
part 8: New research: Morning glory contains 5 stimulating LSD-like drugs, soluble only in wine/alcohol, only sparingly soluble in water.
part 9: 20 minute visionary visit from a dead Aztec Shaman
part 10: One way to make tetrahydroharmine

Latest experimental findings:

part 10: update 5-12-21 see post #57, ORAL AYAHUASCA REPORT: 70mg DMT complexed to 490mg HPBCD in 10 drops very hot water formed clear 0.500ml solution after 2 minutes of kneading/mashing on a spoon: clear solution mixed into 2oz hot water solution of 200mg harmine + 250mg THH resulted in +5 Shulgin scale :oops: experience IDENTICAL to 30 grams potent Hawaiian psychotria brew (Having taken 30 to 40 grams of Hawaiian psychotria with Caapi over 70 times over a period of many years).

70mg HPBCD DMT absorbed several factors better than oral freebase DMT or DMT salts (all were mild +3 :( experiences in a dozen trials, due to poor oral body absorption). The HPBCD DMT out performed and absorbed better than the dozen DMT salt experiments (70 to 120mg) I performed years ago. The results are similar to several papers I have read in which HPBCD was used to enhance the absorption of oral pharmaceuticals over their normal oral absorption by many factors.

Example: HPBCD improves oral absorption profile for Ofloxacin, a second generation fluroquinolones by 54 to 89 percent.(y)

part 11: 60mg sublingual DMT complexed to 420mg HPBCD with 10 drops very hot water on a spoon with 2 minutes of mashing & stirring: PHENOMENAL strength, active for 90 minutes, profound open eyed beauty, heavy CEV imagery, music incredible, very euphoric. See post #64.

Experienced PHENOMENAL strength, active for 90 minutes, profound open eyed beauty, heavy CEV imagery, music incredible, very euphoric.

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Part 1: HPBCD complexed DMT experimental dosage, effects & duration
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I found a thread from 2012 entitled "Complexing DMT freebase for sublingual administration" After reading all 3 pages, I learned that no user in the thread attempted HPBCD complex to DMT, so I did an experiment to find out if it works.

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 30mg freebase dmt on a spoon, add 210mg of HPBCD powder on top the DMT, add 5 drops (less than 0.250ml) of VERY HOT near boiling water from a pipette, this was water that was pre-heated up in microwave in coffee cup. I knead/mash & mix it all together using end of a spoon for 2 minutes, it turns into a clear sticky solution, then draw up liquid with pipette, place drops under tongue and hold for 15 minutes. The DMT will all dissolve into the bloodstream.

210mg of HPBCD may look like alot when laid out, but when even just a few drops of hot water is added to it, it shrinks into a tiny sticky clear mass as it is derived from a sugar molecule, perfect for "under the tongue" use.

Strong effects at 5 minutes after the end of the 15 minute HPBCD DMT 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. 250mg tetrahydroharmine taken orally 3 hours earlier, transcendent combination, music sounded heavenly, the spiritual power of music.

I would imagine this might allow those who normally get nausea from oral preps to avoid the nausea. There is no burn under tongue, taste yes. I used this 3 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 profound beauty and had visuals, very transcendent. Zero nausea.

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.

This was using DMT cleaned up using a sodium carbonate wash. PKA of DMT is 8.75 or so, so please 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.

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, possibly improving even the oral bio-availability substantially when taken with RIMA's to activate it, etc.

THH or tetrahydroharmine can be taken orally (100, 150 to 200mg), my favorite in combo, while the DMT can be used sublingually, allowing the best of both worlds. No nausea felt. Have tried this in dreams several times in one night, 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, so that "mind at large" can be let loose, very similar to listening to music on cactus.


In TIHKAL, 300mg of tetrahydroharmine (THH) is equated by one psychonaut to the closed eye visionary (CEV) power of 100mg harmaline, but without all the nausea and dizziness. I totally agree. It glows blue under blacklight, like LSD or psilocin & has a metallic-like lingering taste with a 10.5 hour half-life.

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 this 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.

 
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tregar

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Thanks G_Chem & Delsyd.

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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Part 2: receptorome chart & explanation
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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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Part 3: Tetrahydroharmine effects
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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.
 
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pupnik

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I want some of this aya premixed in a drop bottle like this water soluble THC prep, my current fave.

 

tregar

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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.

Actually Delsyd, 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.

There is another paper entitled "2-Hydroxypropyl-B-cyclodextrin: Properties & uses in Pharmaceutical Formulations" by Loftsson, Brewster, Derendorf & Bodor showing various freebase non-water soluble compounds...it shows that the higher the non-water soluble compound was, 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.
 
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SKL

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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.

[...]

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.
So does it work without the THH or not? If it doesn't, then how distinct are the sublingual effects from different RoAs?

First of all you're not getting 100% BA. 100% BA is achieved by intravenous administration and by definition means all the drug is circulating. Also by definition is pretty much impossible for other ROAs. Plus HP-β-cD actually probably isn't doing much of anything for you. I'll get into why a little bit below. And to round things out adding THH as a confounding variable just confuses things further. So, for now, I'm at "don't believe the hype." You're making some interesting claims in your post but they require evidence that you're just not providing.

Now that that's out of the way the subjective description reminds me a lot of intramuscular DMT, which I was quite fond of but which is a pain in the ass and potentially dangerous. This makes sense as the rates of absorption into the bloodstream are rather similar between i.m. and s.l.. As far as RoAs go, though, i.m. is a bit more involved than this (converting into a salt to make it dissolve at all, then, unless you're OK with a big abscess, making sure your pH is not off the charts, then wheel filtering.) IM DMT was kind of shroomy with a DMTish headspace but not as fierce as smoking or IV. No nausea or anything, quite benign. As I said I liked it a lot, more than smoking (with or without MAOI, although the latter felt in the same category) or i.v. injection but it was something that I'd always be wary of recommending to anyone as far as harm reduction practices go. I am not experienced combining DMT with β-carbolines although I have smoked it with moclobemide which also felt reminiscent of what you are discussing. Both smoking w/moclo and i.m. admin have a similar timeline (although smoking obviously with faster onset) to what you describe but I'd say last rather less than 90 minutes total.

But firstly, how much of the quality of the experience you describe is attributable to THH? I'm not convinced it's not an MAOI, by the way, there is plenty of literature that says it is, even if less potent than other β-carbolines, although it's SSRI activity and potential psychoactivity in and of itself (especially combined with a/nother MAOI?) are both interesting. See here, the paper is quite old but they even figured out an EC50 for it inhibiting MAO.

I looked around on a few forums for info about people taking sublingual DMT (mostly crudely converted acetate or citrate; I couldn't find anyone getting any success with unconverted freebase, a few people mentioned fumarate being better) and the results were unimpressive. I'd like to see the difference between your method and various salts of DMT. Now, what you're doing sounds like it could be increasing s.l. BA of DMT which is exciting. However a few points: DMT's MW is 188.27 g/mol, HP-β-cD's is a whopping 1387 g/mol. A 1:1 molar ratio would be the minimum to make good use of all the DMT and several sources I checked suggest a higher one. Your suggested ratio of HP-β-cD to fb DMT is not enough. If HP-β-cD is dramatically increasing BA, it seems to follow that you could significantly increase enhance potency by increasing the amount of HP-β-cD, which seems to have a high solubility in H2O.

Experimenting with this alone could tell you how well the HP-β-cD is working. In fact, unfortunately, just going on some of your subjective experiences, your DMT doses are not so much larger than equipotent i.v. doses to suggest that you could in fact get that much mileage out of it by increasing the molar ratio. That naturally suggests to me that HP-β-cD isn't actually doing as much as you think it is or that you are running into some hard limit I'm not thinking of. Either way what you're getting out of it now is certainly not 100% BA but not bad, however the very fact that it's not bad with such a low molar ratio suggests that the HP-β-cD isn't that much of a factor. I'd suggest that a lot of what you're getting out of this is attributable to THH potentiation with possibly a small assist from complexing. I don't think THH potentiates DMT enough to invalidate my argument about equipotency with i.v. adminstration, either.

So I would greatly like to hear three things:
(a) what complexed s.l. DMT is like without THH;​
(b) what complexed s.l. DMT is like with a higher molar ratio of HP-β-cD; and​
(c) less extraneous material and especially less New Age stuff.​
Until then, color me skeptical. HP-β-cD, however, is definitely exciting, especially as it does form complexes very readily in kitchen-sink type scenarios without a lot of equipment. If it substantially increases s.l. BA then that is very cool and would have wider implications but I'm not seeing evidence of that yet. What it definitely does do is render a freebase water soluble without converting it into a salt which could have some other applications. It might be a better way to convert freebases like DMT or crack into a solution for injection, although I'd be wary of doing so on anything that wasn't well filtered and pretty pure as HP-β-cD could complex other shit that you don't want in your body. Also these applications may run into a limit due to the weight of HP-β-cD although it is very water soluble. Depends on the doses of the drug involved.

You've piqued my curiosity on the subject generally, though. HP-β-cD is pretty neat:

Structure


Here's how it works, basically:




... which looks something like this ...


Here is a relevant paper: the melatonin-sulforaphane derivative ITH12674, a tryptamine as you can see, is not very soluble in water. They used HP-β-cD to make it both water soluble and more stable:


ITH12674 is a multitarget drug, designed to exert a dual “drug-prodrug” mechanism of action, able to induce the phase II antioxidant and anti-inflammatory response for the treatment of brain ischemia. However, its physicochemical properties limit its potential preclinical development due to its low water solubility and instability towards heat and pH variations. In order to improve its properties, we prepared the inclusion complex of ITH12674 with 2-hydroxypropyl-β-cyclodextrin (HP-β-cD) by the freeze-drying method. The formation of the inclusion complex was confirmed by FT-IR spectroscopy, PXRD, DSC, 1H NMR and SEM techniques. Experimental results showed that the inclusion complex enhanced its water solubility and stability against heat, acidic and basic conditions. Furthermore, the inclusion complex, prepared in water solution, exerted the same potency to induce the phase II antioxidant response as the pure ITH12674. Thus the formation of the inclusion complex with HP-β-CD is a very effective method to stabilize and solubilize the active compound for its future preclinical development.


Here is their method, obviously more involved than the one mentioned in OP involving stuff you probably can't do at home but are still rudimentary if you have access to the appropriate tools. Important takeaway is they're doing a 1:1 molar ratio which you don't approach, not nearly. And here is a paper that suggests you will often want to go beyond equimolar to get the best complex formation (although the curve starts to slope downward again if you have too much HP-β-cD.

We simply need a lot more before anyone should start getting excited about this.
 
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tregar

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Part 4: Tetrahydroharmine receptorome similarities to mescaline; potentiates cactus & safety note
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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.
 
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Skorpio

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Thomas S. Ray


I think that Thomas Ray has some very interesting ideas, his evidence is rather sparse for the magnitude of his claims.

I am biased, I feel like he creates his own terminology, which makes his ideas harder to integrate with the larger milieu of psychedelic/cognitive research.

A lot of his comparisons rely on self reported subjective experiences, which do not always mirror what I (and folks I know who enjoy knowing and loving compounds) have felt.

I do like the general concepts he puts down but I feel they should be viewed as a lens rather than gospel/an accurate depiction of reality.
 

tregar

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Thank you Ismene2. Yes, I agree Skorpio, the comments on receptorome actions should be used more as a Lens.

-------------------------------------------
Part 5: chemist Patrick Arnold's HPBCD prohormones & bloodwork studies
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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(TM) and Cyclo-Nordiol(TM).



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 around 10 minutes or so, sold just as well as the nasal spray, I tried the sublingual product he sold, and that again was effective.
--------------------------------------------------------------------------------------------------------------------------------------------------
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.
 
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Bagseed

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So does it work without the THH or not? If it doesn't, then how distinct are the sublingual effects from different RoAs?

First of all you're not getting 100% BA. 100% BA is achieved by intravenous administration and by definition means all the drug is circulating. Also by definition is pretty much impossible for other ROAs. Plus HP-β-cD actually probably isn't doing much of anything for you. I'll get into why a little bit below. And to round things out adding THH as a confounding variable just confuses things further. So, for now, I'm at "don't believe the hype." You're making some interesting claims in your post but they require evidence that you're just not providing.

Now that that's out of the way the subjective description reminds me a lot of intramuscular DMT, which I was quite fond of but which is a pain in the ass and potentially dangerous. This makes sense as the rates of absorption into the bloodstream are rather similar between i.m. and s.l.. As far as RoAs go, though, i.m. is a bit more involved than this (converting into a salt to make it dissolve at all, then, unless you're OK with a big abscess, making sure your pH is not off the charts, then wheel filtering.) IM DMT was kind of shroomy with a DMTish headspace but not as fierce as smoking or IV. No nausea or anything, quite benign. As I said I liked it a lot, more than smoking (with or without MAOI, although the latter felt in the same category) or i.v. injection but it was something that I'd always be wary of recommending to anyone as far as harm reduction practices go. I am not experienced combining DMT with β-carbolines although I have smoked it with moclobemide which also felt reminiscent of what you are discussing. Both smoking w/moclo and i.m. admin have a similar timeline (although smoking obviously with faster onset) to what you describe but I'd say last rather less than 90 minutes total.

But firstly, how much of the quality of the experience you describe is attributable to THH? I'm not convinced it's not an MAOI, by the way, there is plenty of literature that says it is, even if less potent than other β-carbolines, although it's SSRI activity and potential psychoactivity in and of itself (especially combined with a/nother MAOI?) are both interesting. See here, the paper is quite old but they even figured out an EC50 for it inhibiting MAO.

I looked around on a few forums for info about people taking sublingual DMT (mostly crudely converted acetate or citrate; I couldn't find anyone getting any success with unconverted freebase, a few people mentioned fumarate being better) and the results were unimpressive. I'd like to see the difference between your method and various salts of DMT. Now, what you're doing sounds like it could be increasing s.l. BA of DMT which is exciting. However a few points: DMT's MW is 188.27 g/mol, HP-β-cD's is a whopping 1387 g/mol. A 1:1 molar ratio would be the minimum to make good use of all the DMT and several sources I checked suggest a higher one. Your suggested ratio of HP-β-cD to fb DMT is not enough. If HP-β-cD is dramatically increasing BA, it seems to follow that you could significantly increase enhance potency by increasing the amount of HP-β-cD, which seems to have a high solubility in H2O.

Experimenting with this alone could tell you how well the HP-β-cD is working. In fact, unfortunately, just going on some of your subjective experiences, your DMT doses are not so much larger than equipotent i.v. doses to suggest that you could in fact get that much mileage out of it by increasing the molar ratio. That naturally suggests to me that HP-β-cD isn't actually doing as much as you think it is or that you are running into some hard limit I'm not thinking of. Either way what you're getting out of it now is certainly not 100% BA but not bad, however the very fact that it's not bad with such a low molar ratio suggests that the HP-β-cD isn't that much of a factor. I'd suggest that a lot of what you're getting out of this is attributable to THH potentiation with possibly a small assist from complexing. I don't think THH potentiates DMT enough to invalidate my argument about equipotency with i.v. adminstration, either.

So I would greatly like to hear three things:
(a) what complexed s.l. DMT is like without THH;​
(b) what complexed s.l. DMT is like with a higher molar ratio of HP-β-cD; and​
(c) less extraneous material and especially less New Age stuff.​
Until then, color me skeptical. HP-β-cD, however, is definitely exciting, especially as it does form complexes very readily in kitchen-sink type scenarios without a lot of equipment. If it substantially increases s.l. BA then that is very cool and would have wider implications but I'm not seeing evidence of that yet. What it definitely does do is render a freebase water soluble without converting it into a salt which could have some other applications. It might be a better way to convert freebases like DMT or crack into a solution for injection, although I'd be wary of doing so on anything that wasn't well filtered and pretty pure as HP-β-cD could complex other shit that you don't want in your body. Also these applications may run into a limit due to the weight of HP-β-cD although it is very water soluble. Depends on the doses of the drug involved.

You've piqued my curiosity on the subject generally, though. HP-β-cD is pretty neat:

Structure


Here's how it works, basically:




... which looks something like this ...


Here is a relevant paper: the melatonin-sulforaphane derivative ITH12674, a tryptamine as you can see, is not very soluble in water. They used HP-β-cD to make it both water soluble and more stable:


ITH12674 is a multitarget drug, designed to exert a dual “drug-prodrug” mechanism of action, able to induce the phase II antioxidant and anti-inflammatory response for the treatment of brain ischemia. However, its physicochemical properties limit its potential preclinical development due to its low water solubility and instability towards heat and pH variations. In order to improve its properties, we prepared the inclusion complex of ITH12674 with 2-hydroxypropyl-β-cyclodextrin (HP-β-cD) by the freeze-drying method. The formation of the inclusion complex was confirmed by FT-IR spectroscopy, PXRD, DSC, 1H NMR and SEM techniques. Experimental results showed that the inclusion complex enhanced its water solubility and stability against heat, acidic and basic conditions. Furthermore, the inclusion complex, prepared in water solution, exerted the same potency to induce the phase II antioxidant response as the pure ITH12674. Thus the formation of the inclusion complex with HP-β-CD is a very effective method to stabilize and solubilize the active compound for its future preclinical development.


Here is their method, obviously more involved than the one mentioned in OP involving stuff you probably can't do at home but are still rudimentary if you have access to the appropriate tools. Important takeaway is they're doing a 1:1 molar ratio which you don't approach, not nearly. And here is a paper that suggests you will often want to go beyond equimolar to get the best complex formation (although the curve starts to slope downward again if you have too much HP-β-cD.

We simply need a lot more before anyone should start getting excited about this.
tregar has a history of making wild and anecdotal claims about such things, see his threads a couple of months ago. unfortunately he just keeps ignoring people who are skeptical and try to debate his topic. Kudos to you for giving discussion a go but he probably won't reply to any of that. but your post was pretty informative in my opinion. :)

in his last threads, people like sekio with massive drug chemistry knowledge kept debunking his claims, but he never cared to actually participate in the debate.
 
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SKL

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Kudos to you for giving discussion a go but he probably won't reply to any of that. but your post was pretty informative in my opinion. :)

in his last threads, people like sekio with massive drug chemistry knowledge kept debunking his claims, but he never cared to actually participate in the debate.
Thanks! I claim no chemical/pharmacological knowledge to rival those guys but I try my best.

I was asked to explain my objection to the OP in less technical terms so here goes. It's really pretty easy to understand if I explain it without them. All of this is high school chemistry but people can be forgiven for forgetting that.
  • Molecular mass is what it sounds like: the mass per molecule of a substance, which is a function of the different atoms in it. It is expressed in grams per mole. A mole means about 6.02x10[super]23[/super] molecules, which is how many carbon-12 molecules it takes to weigh 12 grams. A mole of hydrogen molecules is about 2 grams. A mole of water (H2O) is about 18 grams. As you can see how much a mole of something weighs depends on molecular weight (or molar mass), so the unit of molecular mass is grams per mole. The larger/heavier the molecule the more grams 6.02x1023 of molecules is going to be.

    DMT has a molecular weight of 188.27 g/mol.



    HP-β-cD, as a much larger and more complex molecule, has an MW of 1387 g/mol.



  • One molecule of HP-β-cD (the "host") attaches to one molecule of another substance (the "guest") forming a "complex."
  • The number of molecules per gram for DMT and HP-β-cD is different, so an equivalent ("equimolar") number of molecules is going to result in the HP-β-cD necessary to bind to the DMT being considerably heavier.
  • @tregar used between 1-2 times as much weight, not moles, of DMT and HP-β-cD.
  • This means that only about 1/7 of the DMT bound to HP-β-cD.
  • Literature recommends using equimolar amounts of guest and host molecules, or up to twice as many host molecules.
  • With equal/double weight, not moles, of HP-β-cD, that means only 4-8mg of the 30mg DMT will bind to HP-β-cD.
  • 4-8mg, even with THH potentiaton, is not going to do anything. 22-26mg of DMT is going to remain unbound and in fact if it is the freebase, not even dissolved in water (it would dissolve with an acid, such as citric acid or acetic acid. Vinegar could be used to form a crude form of the latter.)
  • In order to get full complexing he'd need about 210-420mg of HP-β-cD. It's very soluble in water but I doubt that much would dissolve in as little water as he's using.
  • He claims to have gotten significant effect from sublingual administration.
  • Therefore, if he actually tried it and it worked, he's getting it mostly from regular freebase DMT (with THH potentiation.)
  • Therefore, the whole claim is bogus. Either the DMT was absorbed sublingually or some of it made it's way to the stomach (the latter is unlikely to have been responsible for all the effects if the onset was as quick as he says.
  • Other people online say they've gotten no effects from sublingual DMT freebase. So it's either all THH potentiation doing the work or it is a bunch of hot air.
 
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tregar

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Thanks SKL! I highly respect your chemistry skills & knowledge, I am in debt to you!

I remember pouring an excess of HPBCD onto the DMT. Thanks for 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. Thanks!

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

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". 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.

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.
 
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tregar

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As far as I know, I am the only one so far to have done this successfully. It is extremely easy. Back then when the nexus had that thread, most commercial HPBCD was not even available on auction sites or anywhere else. I had bought mine from a single 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.
 
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Zephyn

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interesting. so sublingual i imagine is broken down by monoamine oxidase as well, or wouldnt it not be? any why would hpbcd change that? ive never tried or read about sublingual dmt, but i know it works nasally
 

tregar

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Thanks for comments Zephyn.

-----------------------------------------------------------------
Part 6: Dr. Narang: "with sublingual or "under the tongue" better than buccal, gingival & palatal
-----------------------------------------------------------------

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 #13 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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