The Big & Dandy 25I-NBOMe Thread

[tregar]

Thanks Blowjay.

Had a fantasy dream, will recite it below:

Today prepared a HPBCD-complexed 2" x 3/8" wide blotter with 500ug of 25i-nbome, I sprinkled a thin layer of HPBCD on the blotter before applying the etoh dissolved drops of drug. allowed it to dry for 1/2 hour with a fan heater placed in front of it, the blotter suspended horizontally by two clothespins then placed on upper gum for 30 minutes, then removed.

I felt it kick in 1.5 hour later (the iodo takes a very long time to set in), by 2.5 hours, I was fulling full peak effects.

I am completely blown away by this dose, this higher dose is soooo much more to my liking, it feels equipotent to 150ug of acid or so....

I just had acid not but 2 days ago (once again) but promise to give a full 4 weeks before I take another psychedelic again.

I am experiencing an incredible empathogenic headspace with maginficient euphoria, I am enjoying this trip even more than my 175ug acid trip 2 days ago.

I am so in love with this molecule. I am getting visual activity very similar to that of acid trip, staring into an image on computer monitor, colors and patterns of the image begin to morph and almost change into other things, there are shadows everywhere, and afterimages everywhere. I am enraptured by the power and beautiful headspace of this substance. Watching movies I am sooooo into the characters and plot and visuals, I'm even in a better empathogenic headspace then even the acid trip days ago, way far ahead of it in fact...the euphoria is absolutely delightful as well. This a deep and meaningful molecule. The tracers are quite strong and looking into a mirror is an experience. I see patterns on actors and actress foreheads when watching them on TV, the headspace is deep and meaningful and incredibly empathogenic, the "human-ness" of this molecule is identical to the "human-ness" imparted by acid, strong glowing empathogenic quality with a great sense of humor. Every now and then I see "bursts of visual electric energy" shoot through the air, everything seems alive with electric energy...the visuals are just as powerful as those of acid, there is alot of visual stuff going on, I love the visual activity alot. Looking at a poster I see patterns on all of the skin of the actress, colors jump out and energy is everywhere. Music sounds glorious and has deep emotional impact. I saw intense strobe light flashes of pure energy and light go off in front of my visual field during the middle of the trip, I had never seen anything like that before on acid. I may even prefer this stuff to acid (in fact, I think I do), I place it ahead of acid in many respects. There is indescribable beauty all around me. This is a real Gem, just like Erny saids. Love, love, love this stuff.

I can't believe I am tripping this hard after having taken approximately 175ug of acid not but two days ago, how is this possible, perhaps it is the extrememly high affinity of this nbome molecule for the 5-HT2A receptor as compared to acid???

Well, whatever the case or mechanism, I am enraptured and place this experience among the best I have EVER experienced on psychedelics or empathogens.

p.s still no body load and absolutely no nausea at this higher dose, I will never go below this dose again, 500ug is where the magic happens! If I could cross acid with ecstasy, this is exactly what I would imagine it to be, the best of both worlds without the fatigue of ecstasy the next day.

This is no doubt my favorite psychedelic.

CEV's consisted of bright colorful fractals, which later progressed to see scenes of humans going about business, also saw women, some of erotic character, one of my favorite cev's was of a woman (face un-seen) with the most beautiful legs crossed wearing a short black miniskirt, later on saw clips of movie-like scenes, some of the visuals morphed and changed so fast in the beginning that I could not make them out completely, it wasn't until after I achieved a more meditative state that the visuals slowed down and advanced.

 

[tregar]

In a dream, 500ug of HPBCD-complexed 25i-nbome was given to female subject. Subject in the past was unable to take mescaline due to it causing heavy nausea in stomach for duration of trip. Subject applied 1.75" long x 5/16" filter paper blotter to upper gum and left on gum for 30 minutes, then removed. Subject tripped intensely for entire duration of trip. Subject remarked "enjoyed trip immensely". Subject had absolutely no nausea, no gastrointenstinal distress, no side effects. Subject had intense visuals, laughed hysterically for hours at funny situations on movies and TV, enjoyed music immensely. Subject replied material felt like a cross of acid and md**, had strong empathogenic mental effects and euphoria, subject also remarked the headspace felt much like that of acid as well. Subject also said trip was therapeutic and resolved some problems. Subject rated experience as 10 out of 10 and also commented that it was "very fun" and visuals were intense & some of the best visuals she has ever experienced before.

How prepared: A 1.75" long x 5/16" filter paper blotter (cut from a #103 filter paper disc) was suspended between two clothespins horizontally, and approximately 5 to 10mg of HPBCD powder was sprinkled on the surface of the paper, then the 1/2ml of 95% etoh dissolved pre-complexed drug was dropped back and forth over the entire surface of the powder on the paper from left to right, then right to left back and forth, allowed to dry for about 5 minutes with the fan heater blowing on it, then after most of the 95% etoh had evaporated, again more solution applied back and forth, all done with insulin syringe, the needle released the drops of fluid over the powder on paper, this was repeated over and over until all fluid exhausted. After all solution was applied, paper was allowed to dry in front of a heater fan on high setting for 45 minutes. Paper was 100% completely dry after 45 minutes and ready for application. Subject remarked after about 1/2 hour of the paper strip sitting on upper gum that a very faint "numbing sensation" could be felt on tongue and on different areas of gum and mouth surfaces, this is caused by the nbome apparently, as swim also remembers feeling the same faint numbing sensation in mouth as well in past and has read of others feeling the same after some time. Saliva was held in mouth only for the 1st 15 minutes, then swallowed, there was not huge amounts of saliva since the blotter was placed on upper gum.

 

[blowjay]

Have you experimented with different amounts of HPBCD? I am curious as to how you decided to settle on the amount you used. I would expect that a 1 to 1 molar equivalency would work fine as (by my limited understanding) HPBCD just holds the guest molecule inside of it.

I would love to hear more about HPBCD and if you think other cyclodextrins would also work. I am completely intrigued by HPBCD and all of its applications.

 

[tregar]

I stuck with using 9 times the amount of HPBCD to drug molecule while spinning them together (ie 900mg of HPBCD to 100mg of 25i-nbome) based on all the recommendations from cyclodextrin suppliers and past postings in the bodybuilding forums. I also had HPBCD complexed testosterone base back in the day (many many years ago), and it did work as advertised sublingually. I then added additional (5 to 10mg) of HPBCD to the blotter as a "double whammy" approach to make absolutely sure it absolutely complexed although this was probably un-necessary, but I did this based on the fact that some of the etoh may have competed for entrance to the cyclodextrin cavity while spinning with the drug based on the polar/nopolar properties of the etoh, but I wanted to use 95% etoh for storage of the molecule in solution in freezer because it evaporates from blotter so well when applied, and ease of storage (doesn't freeze as water would have). But other than that, have not experimented with various amounts of HPBCD, no.

The 500ug dose of 25i-nbome completely sent me on an intense trip with power visual, empathy, and acid-like headspace & great humor...was quite strong, so I'm completely satisfied with the buccal hpbcd-route, found to be equipotent to nasally applied same non-complexed amount.

I got tired of messing with nasal application because the spray bottles would keep breaking, it was difficult to evaporate off just the proper amount of etoh before adding water back in for nasal spray, it was just overall a pain in the butt, not to mention having girl subject try the stuff, nasal was not appealing to her, ROA with the HPBCD-complexed drug buccal strip was just as strong for her as it was for me., so we are happy as clams with the new buccal complexed route.

Keep in mind that it takes 1.5 hour with the heavier iodo (the most potent of the halogens however) to hit you (1.5 hour after you apply the blotter to upper gum), then you peak 1/2 hour to 1 hour later or so. This is with the buccal route. There is little saliva made by placing the strip on upper gum and it sits easily/practically invisible and is not in the least bit uncomfortable.

If you are interested in reading more on HPBCD, I quoted from 3 articles in one of my posts in the big and dandy 25c-nbome thread, good info from Dazed and others, blast from the past.

Testosterone is extremely hydrophobic with a solubility in water of something like 0.039mg per ml, practically in-soluble, however, when complexed to HPBCD, it becomes 100% water soluble. Guess what else is very hydrophobic (water-fearing)?, yes, that's right the nbome's, especially 25i-nbome. HPBCD can be thought of as like a "molecular condomn" that traps drug molecules in it's donut-shaped hole so that they can be delivered directly to surfaces of the mucosal cavities in the mouth with high effectiveness.

Dazed (bodybuilding expert on the use of HPBCD complexed hormones):

The conventional penetration enhancers like alcohols or polyethylene glycol act by disrupting the lipid layers of membranes.(3) That is a big source of irritation from the old formula, and this irritation can thus be avoided by the use of CD’s (cyclodextrins). Another advantage is, once administered, the steroid is rapidly absorbed sublingually. Nearly 95% of the steroid will be absorbed within 20 minutes. This also causes the need for multiple doses throughout the day.

1. Water

HPBCD is very soluble in water. Substitution of the hydroxyl groups of the BCD disrupts the network of hydrogen bonding around the rim of the BCD. As a result of disruption of the hydrogen-bonding network, the hydroxyl groups interact much more strongly with water resulting in increased solubility compared to BCD. Solubilities of HPBCD are typically listed at >60% at amnbient temperature. As the concentraion becomes higher, viscosity begins to increase and solubility determinations become difficult to perform due to slow filtration rates and at very high solids levels, slow dissolution because of high viscosities making mixing difficult.

Solvents

HPBCD is more soluble in solvents than BCD, but extensive work has not been done to characterize the solubility of HPBCD in solvents. The table below shows the solubility in selected alcohols.

Solubility (g/100ml)

95% ethanol 225g/100ml
isopropanol 152g/100ml

solubility of HPBCD in ethanol-water mixtures:

0% ethanol concentration: 360g/100ml
20% ethanol concentration: 340g/100ml
40% ethanol concentration: 320g/100ml
60% ethanol concentration: 295g/100ml
80% ethanol concentration: 265g/100ml
95% ethanol concentration: 225g/100ml

In any case, there are hundreds of research papers on the science of HPBCD, "Trappsol" and other fancy sounding brand names are currently used for the stuff these days it seems. Research elite chemist "Patrick Arnold" and his past company "Ergopharm" and his patented products "cyclodiol" etc. for even more info. There are many different methods you can use to complex, so explore and experiment to your heart's desire. The best thing about HPBCD is that when complexed to 25i-nbome, it makes the drug completely water soluble, imagine the possibilites, you can create very potent HPBCD-based nasal sprays, buccal blotter piece, etc.

 

[tregar]

Erny's posts were the inspiration for me getting interested in 25i-nbome in dreams, and I agree, his analysis was totally correct and descriptive. I pieced together fragments of his posts below to have them all together in one grouping.

Erny:

NBOMe-2C-I was the first of them I have tried myself and the first one to appear on an illicit market here under the brand name "Solaris", late summer 2007. Currently this name refers to any NBOMe on a glycine tablet (a common cheap innocuous medicine for sublingual administration).

David's NBOMe-2C-I is a true gem. Basically it resembles PEAs, but is much like acid in some of it's effects, especially in the emotional area. It is full with the deep glowing LSD-like empathy that is uncommon within phenylethylamines.

The activity of bomamines in humans are sometimes inverted: NBOMe-2C-I requires 500-1000 mkg for a trip. When insufflated or injected i/m, they need a full hour to come up, even 1,5 hours in the case of NBOMe-2C-I.

NBOMe-2C-I seem a little like DOI and a little like LSD, NBOMe-2C-C seem a little like DOC and a little like DOI, NBOMe-2C-B - a little like DOB, NBOMe-2C-N seem a little like DON and a little like DMT if you wish to know that.

I do not get what is 2C-I and DOI nastiness you are talking about, I see those two as a remarkable visual experience and something that is easy on the mind (not paranoid, not frightening etc), but little else than that. One may also find there some good humour and an an opened, euphoric state of mind good for social tripping, reminiscent of empathogens or acid. This effect is barely noticeable in these two however, and not really reproducible, but is the one that shines to its full extent in NBOMe-2C-I and makes it very special.

NBOMe-2C-I is amasingly positive and is a clear empathogen in an LSD manner, i. e. somewhat deeper and feeling more natural than things like MDMA. An overflowing, exuberant joy, yet not as jittery as MDMA is. This state of mind is uncommon in PIHKAL phenylethylamines and is much closer to a good LSD trip.

NBOMe-2C-I has very few side effects past the come-up, the fact that made me to regard all of them as chemicals that are easy on the body at first, unfortunatly this is not true. there is no heavyness to pull you down and pin to a single place, the body feels weightless. Like the rest, it doesn't suppress appetite, probably due to it's low affinity to 5-HT2C receptor. Yet it is mildly vasoconstrictive and thus may give you a headache shortly after returning to baseline, just like PIHKAL.

It is, of course, visually rich, like it's relatives with iodine in PIHKAL. NBOMes have less distinctive visual patterns that would repeat in every trip like those in PEAs. Besides simple visual "noise" I rarely pay attention to and don't remember well, visuals there are generally more variable. There is one distinctive visual effect, however - caleidoscopic images, like in a real caleidoscope, or, with a higher dose, true fractals, i. e. structures with self-similarity and not just any geometrical visual mesh. Those are present in NBOMe-2C-I as well, of course, and make this similarity with acid even greater.

If we are talking about 2C-I-NBOMe in regular doses, there is no anxiety at all and the overall discomfort is moderate to weak. Mushrooms are much more anxious during the come-up than 2C-I, even plain 2C-B is more anxious. Unless 2C-I is taken in a huge dose. 60 mg may make you anxious. Same is true for NBOMe-2C-I, or any other psychedelic, and taking into consideration it is much more potent not only in terms of dosage, you may guess now what was the real source of that anxiety.

I've heard such complaints about 2C-I, as well, as it's being a sort of "psychedelic speed", etc, but never heard anything like that about NBOMe-2C-I. The frequency of the appearance of negative reactions to this chemical seems to be much lower than that of any other well explored NBOMe molecule (those are B, C and N), and lower than with most of the DOX.

After-effects I was talking about are not real after-effects, it's just the chemical that haven't left the body completely. I was actually still tripping. With a regular dose you will feel almost normal yet not completely at the baseline during this time, and most probably will be able to sleep.

Question "Did you find this substance to be similar to 2C-I qualitatively?"

Somewhat. But more so to DOI in regard its CEV/OEV and LSD - in mindset.

Doses above one-two milligram(s) have produced ...some usual phenomena of an overdose mostly similar with that of any other psychedelic drug.

Doses of more than three milligrams may produce seizures and doses of less than ten milligrams may be fatal. Reality is a little more complicated of course. One of the reports on worryfying overdoses I was able to find was about a man who took 1 mg of NBOMe-2C-I by insufflation. He literally fell as if shot five minutes later, lost consciousness and had seisures.

But I also had a memorable overdose if we are talking on that subject now. At the beginning of it all in 2007 I couldn't killed myself with 30 milligrams (this isn't a typo and was accurately weighed) of NBOMe-2C-B i/m, when accidentally mislabeled packages. I was able to return to this plane of reality unharmed, without any lasting consequences of this misfortune to speak about. There were several lethal doses in it - if we are to estimate them the proposed way. Nevertheless, I am alive and feeling fine, and I can't do anything about this fact. What's worse, I am not at all unique in being so tough. There is a number of reports about similar accidents found at several russian thematic web-resourses. Their story is always the same: someone accidentially overdoses with 5-10 mgs of NBOMe-2C-C/B/I, and after suffering extreme DMT-like trip gets off with only a scare. People like me or these others who won't die from what was called a "lethal" dose in the citation aren't a rarity, it looks more like this is a norm (or one of several norms to be more precise). For us who are the toughest ones in this regard, NBOMe molecules are nearly as safe as the least toxic structures among 2C-X PEAs (that seem to be the safest psychedelic phenylethylamines I am aware of).

This shouldn't serve as a cause for optimism towards phentanyl-like structures we are talking about here. There are also people, who are also quite numerous, for whom their safety margin appears to be closer to that of DOX. For them a suicide by means of 20x-30x NBOMe-2C-X overdose isn't necessarily impossible. And there are also individuals, not as numerous (but it makes no difference; that they exist is just enough), who will find NBOMe-2C-X to have the safety closer to that of benzodifurans like bromo-dragonfly (it would probably be better to say they have no safety reserve at all). These latter individuals will be the first to get into dangerous or even lethal accidents, if we are to see such in the near future.

While there is no way to find out beforehand who is who, or what may happen if somebody will take one of these chems.

A true Gem indeed. It helped me break a powerful addiction as well....it seems to go straight for the therapeutic more-so than some other psychedelics I've tried. Even helped me break an addiction. The feeling the next day is one of total refreshness and clarity. as well, very powerful therapeutically.

 

[tregar]

Just as I suspected.....this is an important study (below) from the cyclodextrin mega-expert Dr. Joseph Pitha:

http://www.sciencedirect.com/science/article/pii/0378517392902816

hxxp://www.sciencedirect.com/science/article/pii/0378517392902816

"Effects of ethanol on formation of inclusion complexes of hydroxypropylcyclodextrins with testosterone or with methyl orange"

by Josef Pitha and Teruhiko Hoshinoa

aNational Institutes of Health, National Institute on Aging/GRC, Baltimore, MD 21224 U.S.A.
Received 21 June 1991;
revised 9 October 1991;
accepted 25 October 1991.
Available online 4 November 2002.

Abstract

Gradual additions of ethanol decreased and eventually abolished the formation of inclusion complexes of testosterone with hydroxypropylcyclodextrins in aqueous solutions. With hydroxypropyl-β-cyclodextrin this occured through two mechanisms. At low concentrations of ethanol (less than 30 percent), the solvent primarily acted as a competing guest compound; at higher concentrations the dissociation primarily occurred through non-specific solvent effects. With hydroxypropyl-γ-cyclodextrin only the dissociation through nonspecific solvent effects was observed. Surprisingly, when ethanolic solutions containing fully dissociated complexes were evaporated, the solid residues had properties characteristic of complexed species, i.e., they showed the rapid and complete dissolution characteristic of complexes prepared by freeze drying of aqueous solutions. That inclusion complexes were formed during the final stages of evaporation of ethanolic solution of components was confirmed by measurements of circular dichroic spectra of a methyl orange: hydroxypropyl-β-cyclodextrin combination. In this combination the spectra of included species were highly characteristic and were recorded both in aqueous solutions and in solid state after the evaporation of ethanolic solutions but not in concentrated ethanolic solutions.

Keywords: Cyclodextrin; Hydroxypropylcyclodextrin; Inclusion complexation; Solvent effect; Testosterone

I had read similar reports in the past of ethanolic solutions competing for entrance to the cyclodextrin cavity (along with the drug) due to the non-polar inner cavity of the cyclodextrin (CD)...normally, with a water solution of CD, the inner liphophilic cavity of the CD attracts hydrophobic molecules (such as testosterone or 25i-nbome)...the CD works by making "caging" or "trapping" these hydrophobic drugs inside them, then due to the CD's outer cone properties, allows them to dissolve in water so that they can deliver the drug to the surface of the mucosal membranes, where the CD then detaches but then transfers the drug through the mucosal membranes.

Earlier you may have noticed that I dissolved 100mg of 25i-nbome in 50ml of 95% ethanol (drinkable alcohol), and also dissolved 900mg of HPBCD in 50ml of 95% ethanol, doing this on two seperate magnetic stirrers, after 8 hours, the 50ml of 95% ethanol solution with the dissolved 25i-nbome was transferred via long 12" pipette over the course of about 20minutes (slowly) to the spinning 50ml of 95% HPBCD solution, then after that, the one remaining combined solution was allowed to stir for 12 to 24 hours.

The solution was stored in a jar in freezer where it would keep indefinately. The advantage to this, is that the 95% etoh solution will not freeze, so there is no need to "dethaw" it like you would have to do had you dissolved the HPBCD and drug in a water solution. Another advantage is that the etoh evaporates fairly fast (after about 1 hour, the blotter paper is completely dry) when applied to filter paper blotter, so long as a fan heater is kept pointed at the paper for the duration of evaporation.

Keep in mind that I also sprinkled about 5 to 10mg of additional HPBCD powder on the 1.5" x 5/16" wide filter paper blotter to cover the surface of it before I dropped the drops onto it via insulin syringe needle tip. I did this for "added insurance" that the complex would form as the etoh fully evaporated from the paper in the final stages.

In the study above we see that due to the competition of ethanol for the inner cone of the CD, we will not get a complex of 25i-nbome to the HPBCD until after the drops of solubized drug are transferred to paper blotter, and then allowed 45 minutes to 1 hour for complete evaporation of etoh from the blotter, finally leaving a complex of HPBCD to drug on the paper, this occurs only after all the etoh has evaporated,

so in essence, I have been on the right path, as I always applied the blotter after all the etoh had evaporated, when the paper was completely dry, then I would apply to upper gum, and it worked fantastic.

So in other words, the way I have been complexing has been working due solely to the HPBCD complexing to the drug as the etoh evaporates from the blotter paper, causing a complete complex in the end.

"Surprisingly, when ethanolic solutions containing fully dissociated complexes were evaporated, the solid residues had properties characteristic of complexed species, i.e., they showed the rapid and complete dissolution characteristic of complexes prepared by freeze drying of aqueous solutions. That inclusion complexes were formed during the final stages of evaporation of ethanolic solution of components was confirmed by measurements of circular dichroic spectra of a methyl orange: hydroxypropyl-β-cyclodextrin combination. In this combination the spectra of included species were highly characteristic and were recorded both in aqueous solutions and in solid state after the evaporation of ethanolic solutions but not in concentrated ethanolic solutions."

So you have a few choices when you complex HPBCD to 25i-nbome:

1. you can do it the way I did above, but remember that the HPBCD will not complex to the drug until the final stages of the ethanol has evaporated from the blotter, after the blotter is dried, then you will have HPBCD-complexed to 25i-nbome.

2. you can dissolve HPBCD powder in distilled water, then drop in your 25i-nbome drug and allow it to spin 12 hours or so, then the HPBCD will easily be complexed to the drug in solution, then just drop the appropriate amount of water drops on blotter, allow it to dry, and it's ready. This could also be used nasally (as HPBCD improves nasal absorption as well), if you add this solution to an empty metered nasal pump (such as the nasa*ort spray pum), then each spray of the nasal pump will equal approximately 0.100ml. To sterilize this solution, suck it up in a 100ml plastic syringe, screw a 0.22 micron whatman filter to the end of the syringe, and push the contents using your thumb to press on the plunger until the solution gets pushed thru the filter into a pre-alcohol washed empty metered nasal bottle. Then add say 5% (exact figure not known) of 95% etoh to the nasal bottle solution as well, to keep it from growing bacteria.

What are cyclodextrins?

Cyclodextrins are a form of linked carbohydrates. They're formed by an enzymatic synthesis that begins with starch. The enzymes, called transglycosidases, are derived from bacteria. What these enzymes do is couple the starch molecules together to form a truncated, conical, molecular structure with a hollow cavity inside.

The inside of this cyclodextrin "cone" is just about the perfect shape and volume to accommodate a steroid molecule. It's also a non-polar molecule, which means that it has some of the same properties as a fat or oil. The steroid molecule doesn't just sit inside the cone, it actually attaches to the inside of it. Also, it won't dissolve in water. However, while the inside of the cyclodextrin cone is non-polar, the outside is polar, which means that it will dissolve in water. What's the significance of all of this? When a steroid molecule and a cyclodextrin molecule hook up, they form a 1:1 complex. So, while the steroids themselves won't dissolve in water, a cyclodextrin/steroid complex will. The upshot is that steroid complexes become more absorbable through the oral mucosa.

A lot of clinical research has been published on the use of sublingual cyclodextrin complexes (SCCs) in humans. At the forefront of much of this research has been Josef Pitha of the US Department of Health and Human Services. Pitha has several patents on sublingual cyclodextrin complexes. He's also authored a journal article where he details the results of an SCC of testosterone on men. In a nutshell, Pitha found that an SCC containing 10mg of testosterone per tablet raised testosterone levels astronomically high (900% over baseline at one hour) and at two hours the levels were still elevated 485%. Compare that with another study that used regular testosterone at 20 times the dosage used in Pitha's study. Regular testosterone - not complexed with cyclodextrin - only raised testosterone around 500% at the peak.

Another study performed by Stuenkel et.al. showed that testosterone SCCs of 2.5 and 5.0mg raised testosterone levels in hypogonadal men 2341% and 4270% (absolute increases of 1765 ng/dL and 2406 ng/dL) respectively! It took an average of 20 to 30 minutes to achieve maximum blood testosterone levels, but even after eight hours post-dose, the testosterone levels were still elevated 126% for the 2.5mg dose and 195% for the 5.0mg dose. Interestingly enough, the peak levels for estradiol only increased 300% and 340% over baseline, respectively. Remarkable, considering that one usually sees estradiol levels increase proportionally with testosterone levels when other forms of administration are used (i.e. injectable esters and TU o

"Trappsol" and other fancy sounding names are used these days to name HPBCD/google the brand names, etc. to find probable outfits that have them.

 

[metalfaith]

Where could I find some HBPCD? I'm not aware of what these "auction sites" are.

 

[AustinJ]

This is awesome information, Tregar, thank you! I was trying to more fully understand how the drug complex is formed, and found this (from an admittedly non-technical source, although it does cite sources):

It is the interplay of atomic (Van der Waals), thermodynamic (hydrogen bonding), and solvent (hydrophobic) forces that accounts for the stable complexes that may be formed with chemical substances while in the apolar environment of the Cyclodextrin cavity. The complex exists in an equilibrium dependent upon the concentrations of the Cyclodextrin, the guest chemical and water. The rate at which the associated complex is formed is determined in large part by the accessibility of the guest molecule to the Cyclodextrin cavity and the magnitude of the net thermodynamic driving force.

Energetically favorable events make the thermodynamic contribution quite compelling:
**Return of hydrating water molecules to the larger pool
**Displacement of water from the hydrophobic Cyclodextrin cavity
**Removal of the hydrophobic guest molecule from the "hostile" aqueous environment
**Installation of the hydrophobic guest molecule into the apolar Cyclodextrin cavity.

This supports the idea that using distilled water to form the complex of 25I and HPBCD would be better than ethanol. Not only would the ethanol be competing with the 25I for entry into the HPBCD cavity, but it also makes a more 'friendly home' for the 25I, making it 'less eager', energetically, to escape the hostile aqueous environment and enter the cozy HPBCD cavity.

I believe the fact that the complex exists as an equilibrium means that a simple 1:1 molar ratio of HPBCD to 25I is not necessarily enough. The higher the relative concentration of HPBCD to 25I, the better chances of getting the 25I fully complexed. I'll be very curious to see what the actual numbers will look like for this, whether the 900mg HPBCD to 100mg 25I that Tregar has been experimenting with is higher than necessary or just right or what.

Also from that page:

Dissociation is usually an equally rapid process, most often caused by the sudden rapid increase in the number of water molecules outside the cavity. Even though there may be an initial energy barrier to dissociation, the concentration gradient created becomes overwhelming and the chemical is displaced. Unable to find relatively scarce Cyclodextrin molecules to reform the complex, the chemical exists free in solution or precipitates, depending on the amount of dilution and concentration of Cyclodextrin.

This seems to imply that using a smaller volume of water to create the complex will improve the rate/equilibrium. Not too sure about this, though.

I find this all fascinating, and it's making me miss my chemistry classes in school!

 

[hexagonsky]

Thank you for sharing all of this complexing info. Very good stuff.
If someone wanted to complex an nBOME and suspend it in a liquid solution that could be used directly out of a dropper, what would be the best way to go about that? How concentrated could you get it and how would you keep it sterile without worry of the alcohol getting inside the dextrin rings and leaving the nBOME with out a sugary protector?

 

[tregar]

Thanks for the comments/kind words AustinJ and hexagonsky. Keep in mind that these are research chemicals and not approved at all for human use, strictly for research purposes only.

Theoretically....

Cyclodextrins only improve the buccal or sublingual or nasal/rectal absorption of hydrophobic (water repelling) molecules (such as testosterone or this RC), it gives no improvements in absorption to hydrophilic (very water soluble) drugs. Judging from the earlier posts in this thread, it appears that this particular iodo RC is very hydrophobic (has a very difficult time dissolving in water). It appears to be much more hydrophobic then the 25c version from the reading of posts. CD's (cyclodextrins) also impart a bit of extra penetration enhancement as well as increasing water solubility substantially. The cyclodextrin acts as a "shaparone" of sorts that shuttles the molecule to the saliva for quick entry to the mucosal membrane, where the drug then partitions into the deeper lipohilic membranes, while the cyclodextrin itself does not. If you add for example testosterone base powder to water, it will not dissolve at all, but merely float on top the water, but if you were to add the powder to a pre-dissolved solution of HPBCD and water, the powder would instantly dissolve, becoming water soluble.

1. One method: a researcher could add 900mg of HPBCD to 50ml of 95% etoh (or similar alcohol like vodka), spin this for several hours to mix well, then slowly sprinkle in 100mg of RC over the course of about 5 minutes....allow this to spin a good 12 hours or more at medium speed on a magnetic stirrer, when done you would end up with a concentration of 200ug of 25i-nbome to each 0.100ml (1/10th of a milliliter). Only use a 1 ml insulin syringe or something even more exact (like a 3/10's insulin syringe). Use a tall graduated cylinder to measure out the 50ml of 95% etoh. This will be a dissasociated complex (non-complexed) but it will at least allow for storage in a freezer, etc for long periods of time, perhaps indefinately. Then use an insulin syringe to draw up 0.200ml (2/10's of a milliliter) which is equal to 400ug of the rc and slowly apply the drops from the tip of the insulin syringe to a piece of filter paper blotter paper cut for buccal or sublingual. Place fan heater in front of filter paper to allow it to dry for at least 1 hour, the drug will be "fully complexed" to the HPBCD on the paper (in this case you would have 400ug of the drug complexed to 3.6mg of HPBCD as a solid residue on the paper). Then and only then it is considered "complexed" when absolutely dry, when the last of the etoh has fully evaporated. It's a good idea to always use about x9 times (9:1) the amount of HPBCD as drug, that is the standard formula, but it's ok to use up to even x20 times the amount of HPBCD to drug (20:1).

P.S. In hindsite, I really don't see the need to sprinkle on "an extra 5 to 10mg of HPBCD powder" to the filter paper piece first before adding the drops of solution. The added insurance of extra HPBCD probably doesn't contribute anything as far as effectiveness is concerned as there is allready plenty of HPBCD mixed in with the RC to begin with.

2. Second method: a researcher could add 900mg of HPBCD to 50ml of distilled water, allow this to mix for several hours, then slowly sprinkle in 100mg of RC over the course of 5 minutes, then allow this to stir for around 12 hours or more, then your solution is fully complexed "as is" still in solution, it can be dropped onto a piece of filter paper blotter and allowed to fully dry for several hours. Sterilization process is described above in case of nasal app.

how would you keep it sterile without worry of the alcohol getting inside the dextrin rings and leaving the nBOME with out a sugary protector?

That's a good question, I don't know the answer to that. When etoh concentration is less than 30% of your solution, the etoh will indeed compete for entrace to the cavity. To keep your solution sterile you would probably need anywhere from 3% to 10% etoh, I don't know exactly how much you would need. Your best option in this case would be to expel the contents of the 0.22 micron filter into a pre-sterilized Vial with robber stopper allready crimped on it, attach an 18gauge needle to the end of the 0.22micron filter and poke the needle through the rubber stopper (rub with alcohol first) and expel the sterile contents into the pre-sterilized 100ml vial, it will stay sterile like this indefinately (no need to add any alcohol to it), however you would need to pull up the contents when needed with a clean sterile insulin syringe, then break off the tip of the needle, then depress the contents of syringe into nose for nasal absorption, etc. you get the general idea.

I really don't see the need for nasal application as sublingual (under the tonuge) or buccal (inbetween gum and cheek) offers tremendous horsepower as is imho. Just remember that the iodo applied buccally/sublingually takes a good 1.5 hours after application before anything is even felt, then it peaks about 1 to 2 hours later. It takes a long time, just be patient, it's well worth the wait in dreams. The "comeup" in other words starts at 1.5 hours after blotter applied, then the comeup will last approximately 2 hours, when peak effects are then felt, visuals/audial & mindtrip tend to increase at this point along with other enjoyable effects of the trip. With the buccal or sublingual ROA there is a longer time till the peak, but the effects of the trip are sustained for a longer duration.

Good Reading:
http://www.pharmainfo.net/reviews/cyclodextrins-drug-delivery-systems-update
hxxp://www.pharmainfo.net/reviews/cyclodextrins-drug-delivery-systems-update

http://www.aapspharmscitech.org/view.asp?art=pt060243
hxxp://www.aapspharmscitech.org/view.asp?art=pt060243

HPBCD Basics

By David Tolson

Introduction

One of the primary issues concerning steroids and prohormones is that of optimal delivery. While most drugs and supplements are taken orally, there are a number of reasons why this method is largely ineffective with most prohormones. When taken orally, these compounds are extensively metabolized in the liver, making the dose used much larger than the amount that gets through. This may also place undue stress on the liver, especially with certain substances. Because of this, other delivery methods, such as transdermal, sublingual, and intranasal, have all become popularized, and each has advantages and disadvantages. This article discusses the compound hydroxypropyl-beta cyclodextrin (HPBCD), which can be used to facilitate prohormone delivery in a number of ways.

Cyclodextrins are a group of compounds that are commonly used in medicine to increase the aqueous solubility of drug substances by complexation [1]. Cyclodextrins are cyclic oligosaccarides, or sugars, which contain alpha-1,4 linked glucopyranose units (in the case of beta-cyclodextrins, seven of these units) in a truncated cone shape [2]. This results in a molecule that has an internal cavity that is hydrophobic and easily forms a complex with a steroid/prohormone molecule, while the outer surface of the cyclodextrin is hydrophilic, and this makes the complex easily dissolvable in water [2-4]. This renders prohormones much more bioavailable, and cyclodextrins are capable of enhancing nasal, sublingual, and transdermal delivery [5-6], among others. Moreover, cyclodextrins will cause much less irritation than other methods [3, 7].

The cyclodextrin of choice for prohormone delivery is HPBCD. When compared to other testosterone beta-cyclodextrin complexes, HPBCD was 1,533 percent more soluble in water, while another study found that HPBCD-steroid complexes were effective while beta-cyclodextrin-steroid complexes were not [4]. HPBCD also has an excellent safety profile.

Sublingual delivery

Sublingual delivery (administered under the tongue) presents an attractive alternative to traditional oral administration. Because of the limited surface area, the amount of prohormone that can be absorbed at one time appears to be 25 milligrams or less. However, when compared to oral delivery, even this amount is advantageous. One study found that a cyclodextrin complex containing 10 mg of testosterone delivered sublingually raised testosterone levels by 900% over baseline, with a 485% elevation at the two hour point. In contrast, even 200 mg of oral testosterone only raises levels by around 500% at the peak. A study comparing oral and cyclodextrin complexed 4-androstenediol also found that the sublingual version lead to a 261% greater increase in testosterone with one quarter of the dose, with the peak levels at 40 as opposed to 90 minutes. [4]

All in all, sublingual delivery is much more effective than oral for the amount used, but it does require more frequent dosing. Sublingual prohormones are usually taken 3-5 times daily.

Intranasal delivery

Intranasal delivery takes the trend of sublingual delivery even further. It is doubtful that more than 20 mg at a time will be absorbed using this method, and blood levels quickly spike 15 minutes after delivery and then dissipate to baseline by 90 minutes. Running a cycle using this method is impractical, as one has to dose up to 10 times daily. However, bioavailability is further increased – intranasal delivery has the highest bioavailability of all prohormone delivery methods, short of injection [7]. Additionally, intranasal delivery provides the most direct route to the brain [6, 7]. For these reasons, this method has become popular for pre-workout stimulant purposes. Many people report increased workout intensity from intranasal prohormones. DHT precursors are best suited to this purpose, although some other prohormones may make effective pre-workout stimulants as well.

Conclusion

HPBCD complexes can allow for a number of novel effective prohormone delivery methods. Each one has unique advantages and disadvantages. For further information, as well as information on creating your own cyclodextrin complexed prohormones, I recommend the following article:

Alternative Steroid Delivery Systems, by Dazed

If you have any questions or comments regarding this article

No part of this article may be reproduced in any form without the permission of David Tolson or Mike McCandless.

References

1. Eur J Pharm Sci. 2003 Oct;20(2):197-200. Driving forces and the influence of the buffer composition on the complexation reaction between ibuprofen and HPCD. Perlovich GL, Skar M, Bauer-Brandl A.

2. Int J Pharm. 2003 Sep 16;263(1-2):173-81. The effect of beta-cyclodextrins on the permeation of diclofenac from supersaturated solutions. Dias MM, Raghavan SL, Pellett MA, Hadgraft J.

3. Mind and Muscle Magazine Issue #9. Alternative Steroid Delivery Systems by Dazed.

4. Super Andro: Cyclodextrin Technology Shatters the Absorption Barrier by Patrick Arnold and David Garrett.

5. Int J Pharm. 2003 Mar 6;253(1-2):1-11. Mechanistic studies of the effect of hydroxypropyl-beta-cyclodextrin on in vitro transdermal permeation of corticosterone through hairless mouse skin. Shaker DS, Ghanem AH, Li SK, Warner KS, Hashem FM, Higuchi WI.

6. Int J Pharm. 2002 Oct 10;246(1-2):25-35. The effects of water-soluble cyclodextrins on the histological integrity of the rat nasal mucosa. Asai K, Morishita M, Katsuta H, Hosoda S, Shinomiya K, Noro M, Nagai T, Takayama K.

7. The Scoop on Intranasal Prohormones by Patrick Arnold

Dazed:

The best tool available to make nasal and sublingual steroids are derivatives of beta cyclodextrins. The one that is most readily available is hydroxypropyl-beta cyclodextrin (HPBCD). (Note: Plain beta-cyclodextrin is of little use) In case you have not heard of these, cyclodextrins are cyclic oligosaccarides (sugars) that have a hydrophilic outer surface and a hydrophobic inner surface.(3)

They can be thought of as a doughnut, with the center capable of having a steroid molecule stuck inside it. The hydrophilic outer surface makes the cyclodextrin soluble in water, and when it is combined with a steroid, it can make the poorly water soluble steroid soluble as well.(3)

In addition to making steroids soluble, cyclodextrins have very other important properties that make them ideal for our purpose. Cyclodextrins are known to enhance steroid delivery through biological membranes.(3) The large CDs themselves are very bad at permeating biological membranes, but they deliver the steroid to the membrane, where it partitions into the membrane, leaving the CD on the outside of the membrane.(3)

The conventional penetration enhancers like alcohols or polyethylene glycol act by disrupting the lipid layers of membranes.(3) That is a big source of irritation from the old formula, and this irritation can thus be avoided by the use of CD’s. Another advantage is, once administered, the steroid is rapidly absorbed. Nearly 95% of the steroid will be absorbed within 20 minutes. This also causes the need for multiple doses throughout the day.

Complexation:
It seems that hardly anyone out there knows how to complex a steroid with a cyclodextrin. One procedure I saw on a different company’s steroid column was laughable. It was pretty obvious that whoever wrote that procedure knew very little about cyclodextrins. It is really fairly easy to do. There are multiple ways to do it, but I will tell you three methods to try, depending on what resources you have available. In all instances, you need a ratio of 9g of HPBCD to 1g of steroid. Complexation occurs because the steroid is more energetically stable inside the CD than outside of it. It is an equilibrium process, but the equilibrium lies much more on the side of complexation.(3) Water is essential for complexation to occur. It is removed from the inner cavity to allow for the steroid to enter, but even normal room humidity is sufficient for complexation if the mix is given sufficient time.(4)

Method1
For the first method we will formulate it for a total of 2g of steroid.
Dissolve 18g of HPBCD in 80ml saline in a beaker on a stir plate. Once this is dissolved, slowly add the 2g of steroid over about 5 minutes. Let this stir overnight. Filter out any insoluble particles. This provides a 25mg/ml solution.

Method 2
For the second method, we will formulate it for 1g of steroid.
Triturate (mix in a mortar with a pestle) 9g HPBCD with 1g steroid. Place this in a high humidity environment for 2-4 days. I have used a covered fish tank with water in the bottom, but anything that can create a humid environment will work. A syrup will form, and this is dissolved in 40ml saline and you have a 25mg/ml solution.

Method 3
For the third method, we will formulate for 4g of steroid.
Triturate 36g of HPBCD with 4g steroid. Let this sit at normal room temperature and humidity for a week. Complexation will occur, but takes time with this process Dissolve the powder in 160ml saline. This again makes a 25mg/ml solution.
These solutions can be made stronger by adding less saline, but the closer you get to 50mg/ml, the thicker the solution becomes. At 75mg/ml, the solution is too viscous to do anything with.

Editors Note: I am assuming he is talking about mg of actual androgen, not mg of androgen/cyclodextrin complex, because cyclos will dissolve just fine at 300mg/ml, which I think is ample, anyway.
If prohormones are used, you will probably want to filter the solution, since there are a lot of insoluble impurities in most of the prohormone powders out there.

Can I Inject?
I performed a little experiment with 4-androstenediol and HPBCD. I complexed some 4-Adiol with HPBCD as in example 1. I evaporated off some water until there was a 50mg/ml solution. This was sterile filtered this into a sterile vial and injected. These were the most painfree injections I have ever had with 4-Androstenediol. The cool thing about this formula is that it can be shot subcutaneously or intermuscularly, since it cannot crystallize and dissipates quickly because it is so water-soluble. Although I never tried, multiple daily shots would be needed to impart any kind of muscle building effect, and although you will never be limping because of a painful muscular injection, it would just be too much of a hassle. Another reason not to do this is because most HPBCD available is not endotoxin free, so you could be setting yourself up for a nice fever or illness, or possibly a very bad reaction that could cause death. That is always a good reason to avoid something.

Intranasal and sublingual delivery systems can be very useful. Not only do they work well, but the needle phobic and the human pincushion now have a way to add more steroids to their body. Those who want to get a boost in blood levels before a workout are now free to do so. As an added benefit, I can’t say I have ever heard of someone having their nasal inhaler confiscated to be tested for anabolic steroids. Enjoy!
Reference:

 

[metalfaith]

Anybody got any help for a noob? I am curious in beginning research with this RC, but without the HPBCD I can't do much.
Thanks in advance. You guys are the best, i'm learning infinite from this thread alone.

 

[JBrandon]

Reasd the entire 25C thread and you'll learn an infinitely more infinite amount.

 

[psykap]

Could somebody tell me one thing ? I made some blotters with 25I-NBOMe . As has already been said they are absorb very weak . How do you think if I soak ready blotters with 25I in HPBCD sollution cause it that they will be better absorbtion?

 

[tregar]

If you allready had some pre-soaked weak blotters, I suppose you could prepare a 50ml solution of 95% ethanol (or vodka), add 1000mg of HPBCD to the ethanol, allow it to stir for an hour, then drop about 1/4ml of the solution onto one piece of blotter, when all the etoh has evaporated from the blotter piece (say about 1 hour later), then and only then would the approximately 5mg of applied HPBCD have complexed to the drug. Alternately, you could sprinkle 5mg of HPBCD on the blotter piece, then drop 1/4 ml of 95% ethanol or vodka on the paper, allow it to dry for an hour, then it would most likely end up complexed to the drug as well.

As you can tell from reading the scientific study above, "Surprisingly" ethanolic solutions of HPBCD and hydrophobic drug form actual complete complexes during the final stages of etoh evaporation. It came as a "surprise" as it appears to work just as well as contemporary methods (ie the use of plain water, freeze drying, etc.).

Can I ask a question? Since I have never added the RC directly to water (only ethanol), what kinds of things do you observe when it is added to water? does it float on top or otherwise repel the water? Just how hydrophobic does it appear? There seem to be alot of problems with solubility into water from reading most of the earlier posts in this thread. If you are having to dissolve the stuff into alcoholic solutions (mixtures of alcohol and water) then this does absolutely mean the molecule is quite hydrophobic (which is good thing when you complex it to HPBCD, this is what you want).

Also, why is it that only Erny, Addam and myself have the only dream trip reports in this thread? Is the solubility causing this many problems in the past or is it just that it is hard to find/expensive, etc? What seems to be the problem? just curious. The 25c thread is 34 pages and this thread is not even off the ground, lol.

 

[Devourer]

I've been interested in this chem for quite some time, but the dose is what throws me off, I ordered an MG scale recently, but it's a cheapo and even when it gets here I feel as if it wont read the dosages I need.

I can prolly get away with doing the liquid solution, but I still feel as if I screw up I'm going to really jeopardize someone, or my own life.


Also the vendor I found this from sells it for the same price as the 2c's per gram,

I don't see how this is possible, I did the math and if you sold it you'd make ungodly amounts of money...
but once again, I feel like you'd kill a few people in the process.

 

[tregar]

You would need to weigh and re-weigh it over and over to make sure it is within as close as can be gotten to for example 100mg, then absolutely must be added to liquid, as liquid measurement is the only way it can be accurately measured out, there is no way to ever (even with an expensive milligram scale) weigh out accurate 1mg amounts accurate to within 1mg, you would need a thousand dollar/pound scale bolted to a perfectly flat table with windscreen all around, etc. etc. Liquid measurement is the only option. A tall graduated 50ml or so cylinder is the best way to accurately measure out exactly 50ml of solvent.

You might try to search for "trappsol" (a brand name given to hydroxypropyl beta cyclodextrin for research and investigative purposes only, not approved for human consumption).

Interesting tidbit:

How does Cyclodextrin Work for Feb*eze?
Feb*eze is an odour-eliminating product with modified β Cyclodextrin as one of its main ingredients. When Feb*eze is sprayed onto fabrics, the some-what soluble malodour molecules are dissolved in water. This is an essential part of the deodorization process. As a second step, when the solution dries, more and more malodour molecules complex with Cyclodextrin and are effectively retained to keep their concentration in the air low. This total process (water dissolution + complexation) decreases the volatility of the malodour molecules and causes odour elimination. The chemical equilibria involved in the deodorization process are as follows:
1 solubilization of the volatile compound (G)
2. complexation with the Cyclodextrin (C)
3 precipitation of the complex as item dries.

My Feb*eze bottle saids ingredients: water, alcohol, odor eliminator derived from corn, fragrance. I sprayed some of this on my hands and on a table, it does not leave behind any sticky residue, whereas an extremely sticky residue is left behind when you leave a puddle of HPBCD and water on your hands or on the table, this leads me to believe that there may not be HPBCD in Febreze, but rather some other derivative of cyclodextrin, it's just not sticky, whereas my HPBCD and water or when mixed with etoh and allowed to evaporate leaves a VERY VERY STICKY residue behind. So folks, I'm sorry but it looks like Feb*eze is just not a substitute. The sticky residue eventually gives way (once all the solvent & water has evaporated) to a "glossy looking solid state" with no stickiness.

amanitadine said:

There are. And there is one from Erny in the Trip Reports section here. Seems to be his fav N-Benzyl PEA....

Definately my favorite N-Benzyl PEA as well. I notice that Erny also talks about the hydrophobicity of this molecule and it's ability to reach the brain in a quoted statement on page 1 of this thread. Hydrophobic = loves lipophilic like fat & oils, nonpolar environments but repels water (which is polar).

 

[tregar]

I had totally forgoten that the book "Psychedelic Information Theory" by James Kent has a chapter on "Psychedelic Receptor Binding". He saids that the substances that have the most Hallucinogenic potency have very high 5-HT2A affinity as well as 5-HT2C affinity...

TABLE 1 from Kent's book

In this chart, a value of 4.00 indicates high affinity at that target; any value under 2.00 should be considered imperceptible. From Ray, 2010(3).

5HT--

2c-E = 1A (2.91), 1B (3.00), 1D (3.54), 1E (2.60), 2A (3.76), 2B (4.00), 2C [3.38], 5A (0.00), 6 (1.93), 7 (2.77), D1 (0.00)

2C-B = 1A (2.75), 1B (3.11), 1D (3.71), 1E (3.05), 2A (3.69), 2B (4.00), 2C [3.18], 5A (0.00), 6 (2.63), 7 (2.81), D1 (0.00)

LSD = 1A (3.73), 1B (4.00), 1D (3.70), 1E (2.62), 2A (3.54), 2B (3.11), 2C (3.11), 5A (3.64), 6 (3.75), 7 (3.70), D1 (2.34)

DOI = 1A (0.00), 1B (2.31), 1D (3.00), 1E (2.66), 2A (3.44), 2B (3.13), 2C (4.00), 5A (0.00), 6 (2.34), 7 (1.90), D1 (1.67)

DMT = 1A (0.00), 1B (0.00), 1D (3.91), 1E [3.28], 2A [2.58], 2B (0.00), 2C (3.42), 5A (3.16), 6 (3.35), 7 (4.00), D1 (3.51)

psilocin = 1A [2.88], 1B (2.19), 1D (3.40), 1E (3.03), 2A (2.14), 2B (4.00), 2C (2.52), 5A (2.83), 6 (2.82), 7 (2.82), D1 (3.37)

5meodmt = 1A (4.00), 1B (2.41), 1D [3.48], 1E (1.72), 2A [0.98], 2B (0.69), 2C (1.55), 5A (1.84), 6 (2.73), 7 (3.69), D1 [2.38]

DIPT = 1A (4.00), 1B (0.00), 1D (2.51), 1E (0.00), 2A (0.00), 2B [3.48], 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)

mescaline = 1A (3.61), 1B (0.00), 1D (0.00), 1E (3.16), 2A (0.00), 2B (3.97), 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)

MDMA = 1A (0.00), 1B (0.00), 1D (0.00), 1E (0.00), 2A (0.00), 2B (3.64), 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)

Ray, TS: "Psychedelics and the Human Receptorome". PLoS One. 2010; 5(2): e9019.

25iNbome has 0.044 affinity for 5-HT2A (the highest ever recorded for a psychedelic, higher than acid even) and 2.0 affinity for 5-HT2C (much higher than acid), this may help explain the wild visuals that I experienced.

In comparison, mescaline has no affinity for 5-HT2A or 5-HT2C, he saids this explains why it is largely considered a non-visual psychedelic, along with 5-meo-dmt, dipt, and mdma. To me, 25i-nbome is visually more spectacular than acid. I'll go ahead and paste his complete receptor chart table for all the popular psychedelics in just a bit.

From Nichol's paper:

The ligand 25i-Nbome had low affinity for most receptors, with the following reported Ki values (nM) for receptors where it had significant affinity: (remember the lower the number, the greater the binding):

5-HT2a (0.044)
5-HT2c (2)
5-HT6 (73, +/-12)
5-HT2B (231, +/-73)

u opiate (82, +/-14)
H1 (189, +/-35)
kappa opiate (288 +/-50)

LSD:

5-HT1A = 1.1
5-HT1B = 90
5-HT1D = 11
5-HT1E = 93

5-HT2A = 3.5
5-HT2B = 25
5-HT2C = 23

5-HT5A = 7
5-HT5B = 5
5-HT6 = 6
5-HT7 = 6

d1 = 27
d2 = 6.4
d3 = 261
d4 = 230
d5 =

adrenergic = 37
histamine H1 = 1083

The significance of 5-HT5A, 5-HT6, and 5-HT7 receptors are unknown, but psychedelic tryptamines such as psilocin or DMT do have significant affinity for 5-HT1A receptors.

From "Psychedelic Information Theory" by James Kent:

"Breadth of Psychedelic Receptor Binding

Table 1 lists the binding strength of popular psychedelic drugs at many 5-HT receptor sites, listed in order of 5-HT2A affinity.(3). This table should be an accurate representation of hallucinogenic potency of various psychedelics in descending order. From subjective reports all substances at the top of this list are very hallucinogenic, but DMT, which is often considered to be the most hallucinogenic, actually falls somewhere in the middle. If we also look at 5-HT2c affinity, which is implicated in hallucination, we can see that all substances at the top of the list also have high 5-HT2C affinity, with DMT and DOI having slightly higher affinity than the rest. 5-HT7 receptor affinity, which stimulates cAMP activity and the reward system, also seems to be implicated in overall transcendent psychedelic action, with the mystically popular DMT, 5-Meo-DMT, and LSD topping the affinity list for these receptors.

In contrast, there are four non-visual psychedelics at the bottom of the list, 5-Meo-DMT, DiPT, Mescaline, and MDMA. These substances have very poor 5-HT2A, 2C affinity, but all have a high 5-HT2B and adrenal affinity; this indicates they are effective at stimulating serotonin production, cardiovascular activity, and acute sensuality. 5-HT2B affinity is quite high for all samples in this list with the exception of DMT and 5-MeO-DMT, making 5-HT2B affinity a good indicator for purely sensual or entactogenic effects. It is interesting to note that DiPT, Mescaline, and 5-MeO-DMT all have a high 5-HT1A affinity, which is generally thought to work in contrast to 5-HT2A agonism to promote well-being and satisfaction. DiPT is unusual because it produces distinct audio hallucinationa and little or no visual hallucinations, and predictably does not bond with 5-HT2A, 2C receptors implicated in visual hallucination.

By analyzing this affinity table it seems possible to predict the relative potency and effect of any hallucinogen based soley on binding profiles, though the three control molecules at the bottom of the list (6-F-DMT, Lisuride, 4C-T-2) are reportedly non-hallucinogenic despite high 5-HT receptor promiscuity; this is likely because they are not active as agonists, they are antagonists, or their binding profiles are not synergistic and somehow cancel each other out.

Salvia divinorum interrupts kappa-Opiod tactile sensory pathways; these pathways mediate pain, gravity awareness, and sensation for determining physical orientation in space."

Interesting as 25i-nbome also agonizes u opiate and kappa-opiate to a small limited degree. This might have explaind my feelings of weightlessness when walking outside in a garden at the peak of one of my first trips.

 

[skillet]

In comparison, mescaline has no affinity for 5-HT2A or 5-HT2C, he saids this explains why it is largely considered a non-visual psychedelic, along with 5-meo-dmt, dipt, and mdma.

Bollocks, mescaline has a Ki of 360 (+/- 70) nM at [125I]DOI labelled r5-HT2A receptors, and similar at 2C, according to Nichols in the jimscaline paper. The Ray paper used results from the PDSP, who use antagonists to label the 2A and 2C receptors.

 

[tregar]

Thanks for the info skillet, I had my doubts as well...I've read receptor reports from 3 different sources across various popular psychedelics and there are definately differences reported from each study. This appears to be a gross error in Kent's book. Mescaline is plenty visual (at higher doses) to not only myself but lots of others.

 

[tryp2fun]

Here is the result of a recent experiment. 2.1 mg of recrystallized 25I-NBOMe hydrochloride was dissolved in 1 mL of water, which went slowly, since the compound was granular. 200 uL of this resulting solution (420 ug) was then applied sublingually with an oral syringe and held for 20 minutes without swallowing. Within 45 minutes, a strong and pleasurable +3 experience resulted. No need for cyclodextrin. Conclusion: The problems with solubility and activity reported above for 25I-NBOMe must be due to the supplier giving the free base instead of the HCl salt.