• N&PD Moderators: Skorpio | someguyontheinternet

DMT and opiate activity

fastandbulbous

Bluelight Crew
Joined
Jul 29, 2004
Messages
21,333
Location
that rainy little island off europe
The following is an extract from NIDA monograph 149 - Hallucinogens; an update

The negative melatonin data are inconsistent with DMT’s biological effects being mediated by nonspecific stress rather than by selective serotonin receptor subtype activation. The rise in beta-endorphin seen in this study is more than twice that seen after a 28.5 mile mountain race in which daytime melatonin levels doubled (Strassman et al. 1989).

0.05 mg/kg: One-third of the subjects mistook this dose for placebo. Those who were able to distinguish the dose from saline remarked on its uniformly relaxing, comfortable, and warm physical effects. One former heroin user likened it to the “soft cotton batting” of heroin. There were no perceptual (auditory or visual) effects at this dose.

These seem to indicate that low doses of DMT have characteristics that are also common to opiate drugs; but would seem to go against the use of hallucinogens by opiate users, some actually equating the effects of psychedelic agents to a withdrawl syndrome.

The thing I was wondering was, is this something specific to DMT (and 5-methoxy DMT possibly due to their endogenous role as a neurotransmitter/neuroendocrine agent) or is it something common to all psychedelic agents acting via 5HT mechanisms, and if not, is this linked to DMT's ( and 5-methoxy DMT) agonist action at the 5HT1a receptor
 
Hmm, very interesting.. - as I love DMT, i'm not an opiate fan though, but DMT makes me feel... real good.
 
That's plasma beta-endorphin levels... it will have been anaylsied with a single anti-body type test... it's quite likely it's not beta-endorphin at all... but as your first quote says, it's likely to just be a side effect of the mental and cardiovascular stress..

Theres this paper, which I don't quite get... serotonin increases beta-endorphin release, only when the animal has a working serotonergic system... which means it's a presynaptic effect... on serotoninergic neurons... which would be to reduce serotonin release... but that doesn't make sense because any effect of reduced serotonin release would be swamped by exogenous 5-HT...

I don't like this study, cause again it's looking at plasma endorphin, BUT they show its 5-HT1A, 2A and 2C mediated... all receptors DMT has fun with....

Repeated here.
 
In order to test those observations given above, I decided to try an experiment for myself regarding low doses on tryptamines with 5HT1a agonist activity, only with some differences

1/ As I did not have any DMT to carry out this experiment with, I used 5-methoxy DMT, which differs slightly from DMT in terms of qualitative effects, but is also a potent 5HT1a as well as 5HT2a agonist (dose adjusted accordingly). The 5-methoxy DMT was material that had been recrystallizede from methanol, then dissolved in sterile saline (actually for cats, but the same make up/osmolarity as saline for human use)

2/ As I have no experience of how to give IV doses, I have had to use the IM route. For this purpose, I used 3 times the IM dose regeime that would have been used for IV administration.

To ensure no issues with any possible tolerance, I also left at least 2 hours between doses


0.3mg (300ug equiv to 100 ug IV)

Not much happened, could feel something, but too vague not to be put down to placebo

0.75mg (750ug equiv to 250ug IV)

Definitely something, it feels quite relaxing, but not particularly psychedelic in nature, although there is a tendancy to be more concerned with inner mental processes, rather than external stimuli (other than background music)

1.5mg (equiv to 500ug IV))

Aha! This is more familiar, a certain psychedelic nature to the experience, but quite mild compared to the intense onslaught of smoked material. Still characterized by a relaxed, laid back onset of intoxication.

3.0mg (equiv to 1.0mg IV)

Pretty much more of the same as 1.5mg, except nowhere near as relaxed; even had the odd moment of feeling the onset second by second. Time dilation is noticable now

4.5mg (equiv to 1.5mg IV)

Right, that's my lot. This is characteristic of 'normal' 5-methoxy DMT onset, except that instead of the sudden 'whoosh' of the smoked experience, this was more of feeling my ego and intergrated sense of self being slowly (in comparison to smoking onset) dismantled. The onset was a much more anxious affair, and I kept finding myself partaking of stereotyped movements (leg rubbing mostly) that I recognize as being one of the things I tend to do with early stage onset anxiety of large doses of psilocybin and other oral psychedelics with a fairly rapid onset. The whole thing lasted about 45 mins, and the first 10 mins in no way resembled anything like a relaxed opiate onset. Somebody said that they'd never try snorting 5-methoxy DMT because of the uncomfortable onset; I think that this method lies somewher between smoking and snorting, but I'm not keen to repeat theis dosage and method.

It does seem to be the case that small doses have some sort of very relaxing psychological effect, similar to opiates, but I think it's most probably also got a lot to do with the MDMA type anxiety reducing effects as well.

PS. A couple of hours after the last dose, I developed a tension headache, possibly due to the subconcious anxiety generated by the two higest doses. Took 2, 500mg paracetamol tablets and 5 mg of diazepam at least 45 mins to get rid of it (just in case anyone intends to repeat the above)
 
Where was the injection site?

Do you think different areas of IM administration would lead to a different onset / duration / experience?
 
If the theory is that 5-HT1A agonists cause this, then wouldn't bupropion be really fun?
 
I have noticed a "warm feeling" from a variety of tryptamines (prototypical: psylocybin) and phenethylamines (prototypical: MDMA), especially during onset.

I personally suspect the warmth experienced is due to the "inward-looking" nature of psychedelics, and natural endorphin release from excitement and anticipation, rather than through any opioid-mediated action of the psylocybin. The former heroin user's quote sounds very reminiscent of the onset of psilocybin, and the spike in endorphin levels can probably be attributed to the "thrill" of having an adventurous doctor inject a mysterious experimental drug into your arm in a relatively spiritual setting (read Rick Strassman's book if you haven't yet).
 
Where was the injection site?

The gluteus maximus (buttocks). I don't like needles and I don't have to watch to inject this site, just cover with isopropanol, then inject without having to look.

Do you think different areas of IM administration would lead to a different onset / duration / experience?

Yeah, a different rate of onset & duration, but it's not going to change the receptors etc that it binds to (if anything, I'd say IM would be more unpleasant - as described with the 4.5mg IM experiment)

If the theory is that 5-HT1A agonists cause this, then wouldn't bupropion be really fun?

Honestly, I'm not sure; I just wanted to confirm that report as it really seemed unusual. I'm not sure how the response comes about, just that it does (and that's my limit of volunteering with injecting tryptamine psychedelics - any more is for people with access to PET/NMR scanning facilities!). I've read that possibe tolerance to the effects of psychedelics is mediated via 5HT1c receptors so is it possible they're involved? (I'm not actually too familiar with the whole range of receptors that N,N-dialkyltryptamines bind to)

the spike in endorphin levels can probably be attributed to the "thrill" of having an adventurous doctor inject a mysterious experimental drug into your arm in a relatively spiritual setting

I would have though that a double blind trial would have been able to discriminate between this an drug, as some heroin addicts (and ex addicts) have a needle fetish - even saline gets them off.

I admit that my apprehension at using needles may have produced an endorphin spike (no pun intended!), but I would get that from just injecting plain saline (I don't, I did try that after reading your post - it just made me feel uncomfortable from using a needle again).

PS. A lot of the chapter about tryptamines, from the NIDA monograph, was referenced to Rick Strassman, but I will get the book in the near future (it is DMT, the spirit molecule, isn't it - all the refs were to papers, not the book)
 
Last edited:
In my experience with opiate dependency and psychedelics I have noticed no real blocking of physical withdrawal symptoms while on LSD or psilocybin. I have never tried this combination with DMT. While taking LSD or mushrooms during withdrawal can be a very rewarding experience, you still will be shitting your pants.

I wonder if DMT might temporarily suspend withdrawal something like ibogaine.
 
ketamine and dihydrocodeine were a fantastic help to me when withdrawing from a 2 year habit.
 
Yeah, opiates sure do help when you're having opiate withdrawal...

?
 
they worked excellently to get me off a gram aday smack habit.why do you think they are proscribed?its a lot easier to reduce on dhc than it is heroin.i thought you moderators were supposed to know stuff like that.use the dhc to combat just about all heroin sickness,but you dont get a buzz.within a week the dose of dhc you were on at the start will flatten you.then reduce the dose to nothing after another week.if desperate for an instant buzz, snort some k.ive actually weened myself off heroin a few times like this.think before you type.
 
>>they worked excellently to get me off a gram aday smack habit.why do you think they are proscribed?its a lot easier to reduce on dhc than it is heroin.i thought you moderators were supposed to know stuff like that.use the dhc to combat just about all heroin sickness,but you dont get a buzz.within a week the dose of dhc you were on at the start will flatten you.then reduce the dose to nothing after another week.if desperate for an instant buzz, snort some k.ive actually weened myself off heroin a few times like this.think before you type.>>

We were talking about the potential of psychedelics to suspend opiod withdrawl (and exploring possible pharmacological mechanisms thereof), not the efficacy of various opiod agonists for running a taper. Your post was largely off topic, and I think that's what B1lz0r was getting at. He can be terse, but he's rarely mistaken.

ebola
np: converge
 
5-HT1C? You mean 5-HT2C....

Actually, no. There's a discussion of the possible role of 5HT1c receptors in the development of tolerance/downreg in the same monograph that I found the quote about DMT and subjective feelings akin to opiates that's in the 1st post of the thread.

I'm trying to find the actual bit, but 5HT1c receptors are very very similar in terms of amino acid sequence of the protein sub-units, and hallucinogens show similar relative affinities (though weaker) for the 5HT1c as they do for the 5HT2a receptors.

When I find the part I'm on about I'll post it, but the similar relative affinities quote is from page 279 (the whole thing is over 300 pages)

The classical hallucinogens bind at 5-HT1C receptors with affinities comparable with the affinities for 5-HT2 receptors. Indeed, there is less
than a tenfold difference in 5-HT1C versus 5-HT2 affinities for a large
series of DOB-related analogs (Glennon et al. 1992). Thus, any drugreceptor
model developed for 5-HT2 receptors should possess those (or
structurally analogous) features found in 5-HT1C receptors.

The Glennon ref is:

Glennon, R.A.; Raghupathi, R.; Bartyzel, P.; Teitler, M.; and Leonhardt,
S. Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2
serotonin receptors: Evidence for a lack of selectivity. J Med Chem
35:734-740, 1992.
 
There is no 5-HT1C receptor any more... the 5-HT1C receptor was renamed the 5-HT2C receptor when the 5-HT2 receptor was renamed the 5-HT2A receptor.

Meanwhile, my point was "wow an opiate helped you with opiate withdrawal" (said in a completely sarcastic tone), along the same lines as someone saying "Valium really helped with my Xanax withdrawal" or "GBL really helped with my GHB withdrawal"... aka, it's not surprising that Drug X helps with Drug Y withdrawal, if drug X and Y are essentially the same.
 
Aha, explains it then (it's nearly twenty years since my days of academia, and I'm not up to date with everything - well quite a few things actually!)

When I start making a case for phrenology, somebody will put me out of my misery...
 
This isn't spectacularly relevant but I have recently used IV heroin and smoked ultrapure DMT in combination (surprisingly the IV heroin wasn't really all that noteworthy or even more-ish), and the two had a very unique synergy. I found the transition to hyperspace to be faaaaar more comfortable than it would have been otherwise, with a conspicuous lacking of the mental cloudiness one would expect while smoking DMT on smack. It was also the first and only time I have ever met mantids in hyperspace.
 
Sometimes it is hard for one to let go of certain areas of one's Self.. opium has always been utilized by alchemists to help one relax and let go..
 
Top