The Big and Dandy 4-AcO-DMT thread - New incarnation

[Shambles]

there really isn't any proof that 4-aco-DMT crosses the BBB. Even if it did it would, in all likelihood be deacetylated in the brain before it could bind.

I know sod all about the BBB really but this rings a bell from earlier discussions... from what I recall of them the fact that 4-AcO-DMT is highly active used IV suggests that it does cross the BBB and is not simply a prodrug for 4-HO-DMT. I think. I may well be completely wrong though.

Also, it feels much more akin to DMT (or maybe a mushroom/DMT mashup as mentioned above) than mushrooms in my limited experience - definitely not the same feel as shroomies for me.

 

[Xorkoth]

To me, 4-AcO-DMT begins working slightly FASTER than 4-HO-DMT (yes I've had both as pure chemicals), and the AcO feels significantly different, in visual character, emotional character, and mental character. The AcO feels much closer to DMT than it does to mushrooms, for me. Also, the AcO produces virtually zero anxiety, whereas the HO tends to be among the most anxiety-producing of psychedelics for me (though not as much as mushrooms). I also find the HO to be much more intensely mentally psychedelic/godly.

I would be very surprised if 4-AcO-DMT was simply a prodrug of 4-HO-DMT. Very surprised indeed. I am convinced it crosses the BBB on its own, and is also converted to 4-HO-DMT, and that the variance in effects between users is due to differing rates of it crossing the BBB before being converted. It seems that for some 4-AcO-DMT is basically an elongated mushrooms trip, and for others it's more like it is for me, a quick, DMT-like journey.

 

[any major dude]

I know sod all about the BBB really but this rings a bell from earlier discussions... from what I recall of them the fact that 4-AcO-DMT is highly active used IV suggests that it does cross the BBB and is not simply a prodrug for 4-HO-DMT. I think. I may well be completely wrong though.

Also, it feels much more akin to DMT (or maybe a mushroom/DMT mashup as mentioned above) than mushrooms in my limited experience - definitely not the same feel as shroomies for me.

I agree that its subjectively different, however why is still a mystery to me. I just don't think IV usage proves its not a prodrug for 4-HO-DMT.

I know this isn't a perfect analogy, but it seems pretty valid. IV heroin works pretty instantly, however diacetylmorphine doesn't bind to opioid receptors. It is deacetylated in the brain (apparently almost instantly) into morphine and 6-monoacetylmorphine, which bind to a couple opioid receptors causing the subjective effects. If there are enough deacetylation enzymes in the brain to do this, I don't see how 4-Aco-DMT could make it to a receptor site with the acetyl group, and that's just via IV usage. I really can't understand how it would survive the oral rout intact, with the first pass metabolism before reaching the brain with its abundant deacetylazation enzymes. IV heroin users I'm sure would notice a difference in effects from injecting morphine and heroin, and that is likely due to the increased lipid solubility of heroin due to the acetyl groups, and possibly some potentially unknown pharmacological properties of some of the minor & hence lesser studied metabolites. Though the larger differences would likely be mostly due to the increased lipid solubility.

To me, 4-AcO-DMT begins working slightly FASTER than 4-HO-DMT (yes I've had both as pure chemicals), and the AcO feels significantly different, in visual character, emotional character, and mental character. The AcO feels much closer to DMT than it does to mushrooms, for me. Also, the AcO produces virtually zero anxiety, whereas the HO tends to be among the most anxiety-producing of psychedelics for me (though not as much as mushrooms). I also find the HO to be much more intensely mentally psychedelic/godly.

I would be very surprised if 4-AcO-DMT was simply a prodrug of 4-HO-DMT. Very surprised indeed. I am convinced it crosses the BBB on its own, and is also converted to 4-HO-DMT, and that the variance in effects between users is due to differing rates of it crossing the BBB before being converted. It seems that for some 4-AcO-DMT is basically an elongated mushrooms trip, and for others it's more like it is for me, a quick, DMT-like journey.

I definitely agree with it being much less manic & anxiety inducing than shrooms, however, I've never had pure 4-HO-DMT. I rarely ever take mushrooms anymore because of the social anxiety they were causing me when I stopped regular usage, but I find 4-aco practically anxiety free as well. I would speculate this could be, when take orally anyway (or possibly rectally as well), due to it not reaching the brain all at once due to it not passing the BBB until its been deacetylized. However, while there isn't any proof that it does cross the BBB, there isn't really any proof that it doesn't either. Quite the conundrum...

I suppose its also possible that the Aco makes the molecule a bit sturdier and less of it is destroyed before reaching the brain, and that could potentially account for some people experiencing longer duration. If these two things were true, that would be a potentially viable explanation for the subjective differences if 4-aco were a psilocin prodrug. Its all semi-informed speculation on my part though. And it also wouldn't account for some people's shorter, more DMT-like experiences. Unless through some odd quirk in heredity the enzymes in some peoples brains knock everything off the 4 position in a substantial amount of the substance... Though I don't know if that's even possible. Anyway, certainly interesting stuff. I hope I live long enough to see these chemicals studied thoroughly enough to provide a definite answer. I'd venture a guess that it has something to do with the likely increased lipid solubility of 4-Aco-DMT as compared to 4-HO, and that may well account for the decreased comeup time you, and others mention, but in all honesty I have absolutely no clue.

 

[Captain.Heroin]

I find it annoying that the trip itself is only ~3 hours but i cant get to sleep untill ~8 hours after ingesting it.

I never really got the scatterbrain effects you mentions. usually it a pretty smooth transition from tripping to sobriety. I hardly notice it.

But i do get residual stimulation which i find annoying.

So if the trip lasts roughly 3 hours anyways, dosing it IV won't dramatically reduce the length of effects?

Sounds good!

 

[Shambles]

IV lasts well under an hour from memory, Cap'n. It's a completely different experience to oral dosing - ridiculously intense, euphoric, disorientating and dissociating. Kinda like how I'd imagine IVing a substantial dose of ket and DMT together would be like. On mushrooms. Potent medicine indeed

 

[psood0nym]

^How much did you IV? According to this post IV lasts quite a while, at least with a high dose. It wouldn't surprise me if there is a lot of variation in duration with the IV route though, given the drastic differences in duration reported by other users.

For me, 25mg IV gives me a 20 minute or so intense DMT-like rush, followed by a few hours of tripping.

For my friend who is mentioned above, I guess it had different effects (it WAS a fully immersive 2 hour DMT-like experience). It was also his first time IV'ing 4-ACO-DMT or any tryptamine. He was caught completely off guard, he said. I think it affects different people differently.

I've IV'ed up to 30mg before and not gotten anywhere near where my friend did. I get the 30 min. pleasurable rush, followed by a nice trip. And my other friend who's done 25mg a few times gets similar effects as me, it is still very intense and pleasurable though (it really is worth it, and 25mg IV seems to be perfect for me and my other friend. I know it's a high dose, but there are NO negative side effects that I notice). I would recommend starting with at least 15mg IV if you try it. It only takes a SMALL amount of heat to dissolve in water, so do not boil it.

My friend got so lucky, and I am so jealous.... And no, we don't use MAOIs. I would say my friend's total duration was more like 6 hours total (he said he felt like he ate an eighth for a few hours after he "came to").

I don't find IV duration to be much shorter than oral, but it is a completely different experience, almost like a different drug. Although, I thoroughly enjoy both routes.

If there are enough deacetylation enzymes in the brain to do this, I don't see how 4-Aco-DMT could make it to a receptor site with the acetyl group, and that's just via IV usage.

If we accept that a large amount of 4-AcO used IV can be converted to 4-ho in the brain very quickly, then doesn't it follow that for any dose sufficiently small to be entirely converted by endogenous deacetylizing enzymes in the brain that 4-AcO used IV, and I assume IM, should have the same duration as psilocin used IV or IM? I've used both at similarly intense dosages IM, and the duration is radically different, with 4-ho tappering off in just 1.5 hours and the AcO lasting well over 3.

Also,reports of different 4 sub AcO and ho tryptamines indicate that for most people AcO doses are about 50 percent heavier than ho doses for similar intensity of effects (I can only assume the same holds for IM or IV administration of these other 4 sub trypts). I'm pretty sure the weight of the cleaved off portion of AcOs is nowhere near 50 percent of the total weight of these AcO tryptamine molecules (psilocin mol. mass = 204.27 g/mol and 4-AcO-DMT's = 246.3049 g/mol). So if both versions cross the blood brain barrier quickly (which they must to be so quickly active by the IV route) and get converted quickly in the brain (similarly to heroin), shouldn't we expect the dosages for similar effects to be far closer by weight (in the case of 4-ho/AcO-DMT around 20 percent)?

This is all assuming IV or IM, to factor out the additional complications of first-pass.

 

[ASquishyApple]

anyone know if this would show up on a standard drug test? and if so how long after taking it would it be detected?

 

[Delta-9-THC]

It will definitely not show up on any standard drug test. I'm sure it is possible to test for but I don't see it ever actually happening unless someone had a specific reason to look for that chemical and used more advanced testing techniques.

 

[Shambles]

^How much did you IV? According to this post IV lasts quite a while, at least with a high dose. It wouldn't surprise me if there is a lot of variation in duration with the IV route though, given the drastic differences in duration reported by other users.

I've IV'd various doses from 5-20mg or so (again from memory) and was really surprised when I read the post you quoted and a few other reports of higher dose, significiantly longer experiences. My notes on it (posted between shots) are here. The gist of it being that it's insanely intense and maddeningly short. Does seem to be very much in the YMMV realm this one. With the debate about BBB and so on, maybe different people metabolise it significantly differently cos some of the reports like the one above bear almost no relation to my own experiences really.

The micon-filter thing should be a given... I am still a reckless boy though

The IV route was profoundly dissociative, euphoric and obscenely visual for me. Also extremely brief... although the eternity I lost between posts would suggest otherwise subjectively :D

There was an initial - near overwhelming - onslaught of a rather lush rush of the swirly ilk followed by a plateau of profound dislocation which was far from unpleasant then a sudden drop to near-baseline. So brief yet still eternal. If ever there was a candidate for being hippy crack this would have to be high on the list - takes you so high and then leaves you begging for more

 

[highandrolling]

4aco is simply put, one of the best drugs out there. Orally and insufflated are both great routes. Anybody else like 15mg oral doses too?? Of course I really like 20 and 25mg, but this is one of those that can be appreciated in small doses for sure! Can't wait to get my hands on some more!

 

[any major dude]

its definitely one of my faves. i'll have to get some more of it and some more 4-Aco-MET to truly decide my favorite 4 sub tryptamine though

 

[any major dude]

If we accept that a large amount of 4-AcO used IV can be converted to 4-ho in the brain very quickly, then doesn't it follow that for any dose sufficiently small to be entirely converted by endogenous deacetylizing enzymes in the brain that 4-AcO used IV, and I assume IM, should have the same duration as psilocin used IV or IM? I've used both at similarly intense dosages IM, and the duration is radically different, with 4-ho tappering off in just 1.5 hours and the AcO lasting well over 3.

Also,reports of different 4 sub AcO and ho tryptamines indicate that for most people AcO doses are about 50 percent heavier than ho doses for similar intensity of effects (I can only assume the same holds for IM or IV administration of these other 4 sub trypts). I'm pretty sure the weight of the cleaved off portion of AcOs is nowhere near 50 percent of the total weight of these AcO tryptamine molecules (psilocin mol. mass = 204.27 g/mol and 4-AcO-DMT's = 246.3049 g/mol). So if both versions cross the blood brain barrier quickly (which they must to be so quickly active by the IV route) and get converted quickly in the brain (similarly to heroin), shouldn't we expect the dosages for similar effects to be far closer by weight (in the case of 4-ho/AcO-DMT around 20 percent)?

This is all assuming IV or IM, to factor out the additional complications of first-pass.

Well, psilocin is substantially more fragile than its Aco counterpart. I'd assume that some of it my fall victim to dehydroxylating enzymes or bacteria before it gets to the brain, but I could well be totally wrong about that. Does anyone know if 4-Aco would have more resistance to being broken down by MAO? Also, there's a chart somewhere with comparable dosages for different 4-sub-trypts and their respective salts, and i didn't think the difference was that great. I'll have a look for it a bit later

 

[ASquishyApple]

It will definitely not show up on any standard drug test. I'm sure it is possible to test for but I don't see it ever actually happening unless someone had a specific reason to look for that chemical and used more advanced testing techniques.

but since its converted to psilocin. would it still be the same case?

 

[Delta-9-THC]

I've never heard of psilocin being tested for. Especially not on a standard test.

 

[any major dude]

detecting psilocin in urine would be prohibitively expensive, and would have to occur within 48hrs of ingestion, if not sooner. I've never heard of it before either

 

[psood0nym]

Well, psilocin is substantially more fragile than its Aco counterpart. I'd assume that some of it my fall victim to dehydroxylating enzymes or bacteria before it gets to the brain, but I could well be totally wrong about that. Does anyone know if 4-Aco would have more resistance to being broken down by MAO? Also, there's a chart somewhere with comparable dosages for different 4-sub-trypts and their respective salts, and i didn't think the difference was that great. I'll have a look for it a bit later

If the AcO is a prodrug, for it to last so much longer at a similar intensity must mean that, compared to dosing psilocin directly, lots more 4-ho-DMT is working in the brain but spread out over time, kind of like time released psilocin. Let's assume both that the AcO is a prodrug and that some psilocin is destroyed before it gets to the brain, but that 4-AcO does not get destroyed before the brain because it's a more durable molecule. Also, assume that the dosage weights for the ho and AcO are, as you suggest, closer than I suggest for similar intensity of effects (say, the AcO is 20 percent heavier for equal effect- which is about the difference between the versions in g/mol).

So, assuming all else is is equal - deacetylizing enzymes are quickly active in the brain, etc. - for a similar intensity of effect 10 mg psilocin and 12 mg 4-AcO used IV or IM should feel about the same if no psilocin is destroyed in the blood since about 2 mg of the AcO is cleaved off in the brain. However, because we're assuming psilocin is destroyed in the blood it suggests that the psilocin dose should be >10 to be equivalent to 12 mg of AcO used IM to make up for the loss during breakdown in the blood. If for the sake of illustration we say 1 mg of psilocin from the 10 mg psilocin dose is destroyed in the blood that means 9 mg is available to the brain. If the AcO survives intact in the blood that means 12 mg of AcO is available to the brain, but since around 2 mg of the weight is removed on conversion to psilocin about 10 mg of psilocin is ultimately available to the brain. So if the end result of our dosing these amounts is 9 mg in the brain for the original 10 mg psilocin dose and about 10 mg of psilocin in the brain for the original 12 mg AcO dose (very close), then why should the AcO dose last so much longer while maintaining a similar intensity level? On these assumptions doesn't it make more sense to think the AcO is active on its own in the brain but it's not as potent and has a longer duration?

Despite this, I'm inclined to believe 4-AcO is a prodrug or at least that it doesn't reach receptors as 4-AcO, simply because, as you've stated, there is good pharmacological reason from the example of heroin to believe the standard explanation. I'm still not seeing how it adds up, though.

 

[ASquishyApple]

thanks for the info.

i believe i read something about this causing increased mucus production during the come-up but can't really find what i read again so i may be thinking of something else. i seemed to experience an increase in phlegm in my throat but it my have just been psychosomatic. has anyone else experienced this? and have you found a good way of dealing with it? i figure taking diphenhydramine would work but i'd be afraid that would end up putting me to sleep on an already relaxing drug. i take an antihistamine every morning as it is so i'm not really sure if this is necessarily some sort of mild allergy or something else all together. i have only experienced this once out of the four times taking it.

 

[any major dude]

if you sometimes have allergy trouble, and you sometimes take strange drugs, occasionally the two will occur simultaneously. I have allergy problems sometimes myself, nothing too serious, just uncomfortable mucous issues mostly, but i haven't noticed much of an effect on psyches from a standard dose of OTC antihistamines. I find cetirizine to be the most effective and to have pretty much nil in the peripheral effects department.

Also, strange sidenote here, I have dosed LSD, 4-Aco-DMT and mushrooms (separately) while having uncomfortable sinus congestion and during the duration of the trip the allergy issues cleared up completely. I'd say that its possible I just was too high to be aware of them, but I had been having to blow and wipe my nose incessantly and surely someone would've told me had there been snot running down my face the whole time... surely.

I know that LSD and some trypts are a bit promiscuous when it comes to receptor affinity and some of them to bind to histaminergic receptors, but I don't know if they have enough of an affinity to actually have an effect on allergies. Any info on this would definitely be appreciated.

If the AcO is a prodrug, for it to last so much longer at a similar intensity must mean that, compared to dosing psilocin directly, lots more 4-ho-DMT is working in the brain but spread out over time, kind of like time released psilocin. Let's assume both that the AcO is a prodrug and that some psilocin is destroyed before it gets to the brain, but that 4-AcO does not get destroyed before the brain because it's a more durable molecule. Also, assume that the dosage weights for the ho and AcO are, as you suggest, closer than I suggest for similar intensity of effects (say, the AcO is 20 percent heavier for equal effect- which is about the difference between the versions in g/mol).

So, assuming all else is is equal - deacetylizing enzymes are quickly active in the brain, etc. - for a similar intensity of effect 10 mg psilocin and 12 mg 4-AcO used IV or IM should feel about the same if no psilocin is destroyed in the blood since about 2 mg of the AcO is cleaved off in the brain. However, because we're assuming psilocin is destroyed in the blood it suggests that the psilocin dose should be >10 to be equivalent to 12 mg of AcO used IM to make up for the loss during breakdown in the blood. If for the sake of illustration we say 1 mg of psilocin from the 10 mg psilocin dose is destroyed in the blood that means 9 mg is available to the brain. If the AcO survives intact in the blood that means 12 mg of AcO is available to the brain, but since around 2 mg of the weight is removed on conversion to psilocin about 10 mg of psilocin is ultimately available to the brain. So if the end result of our dosing these amounts is 9 mg in the brain for the original 10 mg psilocin dose and about 10 mg of psilocin in the brain for the original 12 mg AcO dose (very close), then why should the AcO dose last so much longer while maintaining a similar intensity level? On these assumptions doesn't it make more sense to think the AcO is active on its own in the brain but it's not as potent and has a longer duration?

Despite this, I'm inclined to believe 4-AcO is a prodrug or at least that it doesn't reach receptors as 4-AcO, simply because, as you've stated, there is good pharmacological reason from the example of heroin to believe the standard explanation. I'm still not seeing how it adds up, though.

I'm pretty lost on this as well. Though I don't know that I, or some others, find 4-Aco to have the same intensity level as psilocin. The former seems much smoother & more relaxed where as the latter is IME, a bit more manic, and inconsistent throughout the experience. With psilocin I'll have a few moments of sobriety, or more accurately coherence, then spiral into weirdness for a bit, rinse & repeat. With 4-Aco I get a much smoother ride, maintaining a similar level of weird throughout the experience. I'm not sure how analogous this is to others' experience though

 

[ASquishyApple]

does anyone have any idea what the threshold dose for this is? i've never gone lower than 10mg but from the effects of 10mg it seems like half that would at least do something.

 

[any major dude]

I would expect some activity around 3-5mg, though not much.