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Thebaine

nabollocks

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Has anyone ingested thebaine on purpose?

Lots of people are taking small amounts of thebaine in their PPT, and I am interested in peoples experiences with this substance.

It is supposed to be a opiate stimulant. (And convulsant at large doses) I can see that this might be good for some people?

I cant find much on thebaine as a recreational drug, but I did find this reference from pubmed.

Stereoselective mu- and delta-opioid receptor-related antinociception and binding with (+)-thebaine.

In vivo and in vitro binding studies with natural thebaine and its enantiomer, (+)-thebaine were conducted to elucidate further their interactions with the opioid system. (-)-Thebaine a key intermediate in the biosynthesis of morphine in the poppy plant (Papaver somniferum) and in mammalian tissue, was poorly effective antinociceptively in mice at doses to 30 mg/kg. Its principal behavioral manifestation was lethal convulsions. Naltrindole, at doses of 1 and 10 mg/kg did not block either the convulsions or lethal effects, suggesting that the delta-opioid receptor system was not involved in this action. Surprisingly, the dextrorotatory isomer exhibited significant antinociceptive activity in the tail-flick [ED50 = 8.9 (3.4-22.1) mg/kg], hot-plate [ED50 = 22.9 (10.9-48.1) mg/kg] and phenylquinone [ED50) = 1.9 (1.6-9.5) mg/kg] assays. Studies with opioid receptor-subtype antagonists, beta-funaltrexamine, nor-binaltorphimine and naltrindole, indicated that antinociception was associated with mu- and delta-opioid receptors. Results of displacement experiments supported the in vivo data. Significant competition for [3H]diprenorphine binding with both isomers for cloned mu- and delta-opioid receptors was observed. However, (-)-thebaine was more effective at the delta-opioid receptor (Ki = 1.02+/-0.01 microM) whereas (+)-thebaine was more effective at the mu-opioid receptor ( Ki = 2.75+/-0.01 microM). Opioid-induced antinociception associated with unnatural thebaine raises the possibility of additional mu- and delta-opioid receptor sites.

Any ideas or discussion is welcomed.
 

nabollocks

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It would also be helpful if someone could get these papers for us to look at:


I now have a copy of this document.
Science in drug control: the alkaloid content of afghan opium.
Remberg B, Sterrantino AF, Artner R, Janitsch C, Krenn L.
PMID: 18816533

Narcotic alkaloids of four papaver species from Iran.
Salehi P, Sonboli A, Zavareh AF, Sefidkon F, Dayeni M, Cheraghi B.
PMID: 17425099
 
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Sturnam

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i got the first one, no luck on the second. if you need anything else though i have lots of journal subscriptions through university.

PM me your email?
 

Sturnam

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The morphine content of the samples ranged from 5.1 to 24.8% (average 14.4% ),
the codeine content from 2.6 to 9.7% (average 5.9% ), thebaine content from 0.7 to
9.3% (average 4.0% ), and papaverine content from below the limit of determination to
9.3% (average 2.8%; see Table 2).

I'll see if I can find any other references for stuff on thebaine more specifically.

edit: found that the CD50 (convulsive dose) is about 17mg/kg for mice

also, for anecdotal evidence, the one time i had poppy seed tea, there seemed to be some stimulation factor that kept both me and my girlfriend awake far longer than I would have expected, even after most of the euphoria was gone.

hmmmm, found more, and this is interesting
Monkeys given 23 hrs/day continuous access to 1.0 mg/kg/inj thebaine did, however, self-administer the drug at rates significantly higher than those maintained by saline, but not as high as those supported by 2.0 mg/kg/inj codeine. Two animals self-administering thebaine did not show any signs of withdrawal when injected with 0.1-1.0 mg/kg of naloxone or when saline was substituted for thebaine. A third monkey showed a severe reaction leading to death following an injection of 1.0 mg/kg naloxone.
from: Behavioral effects of thebaine in the rhesus monkey. Pharmacol Biochem Behav 1981; 14:805-9.

so, seems like, at least with this study, that thebaine produced no dependence. hmmmm. maybe thebaine could slow tolerance to other opiates? Anyone with regular PPT use, do you notice that your tolerance goes up slower for PPT than other opiates?
 
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Hammilton

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Okay, so here's the question that springs to mind:

Why is it that (-)-thebaine, having the same configuration as (-)-morphine not bind to the mu receptor, but (+)-thebaine (which has the same configuration as DXM and dextorphan (ie: dextromorphine))



(image courtesy of murphy, (c) 2008 all rights reserved, patents pending, etc etc)
 
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MurphyClox

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I read the opening post like that the natural isomer of thebaine doesn't have any µ-agonistic properties, but the enantiomer does. This is indeed strange. Just made a fast overlay of energetically minimized structures:




They look practically identical?! So how can one explain this? Do the 2 ethers disrupt µ-agonism THIS effectively?


Peace! Murphy

Edit: LOL! Double-posted pic...
 
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nabollocks

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What is a normal dose of PPT? 20 pods? 10 pods?

Just trying to work out approx how much thebaine people are ingesting without any percieved side effects from the thebaine.

How heavy were those monkeys in the quoted study Sturnam?

Here is Table 2 from:
Science in drug control: the alkaloid content of afghan opium.
Remberg B, Sterrantino AF, Artner R, Janitsch C, Krenn L.
PMID: 18816533
 

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LuxEtVeritas

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it says it is MORE effective at delta, not that it does not bind or has no effect of note on mu...and the unnatural enantiomer is likely the reverse

at an avg of 4% it is likely not expressing any effect in either capacity to any substantial degree,...

i would not htink in any real capacity it is having any effect to note
 

Hammilton

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(-)-Thebaine a key intermediate in the biosynthesis of morphine in the poppy plant (Papaver somniferum) and in mammalian tissue, was poorly effective antinociceptively in mice at doses to 30 mg/kg.
Surprisingly, the dextrorotatory isomer exhibited significant antinociceptive activity in the tail-flick [ED50 = 8.9 (3.4-22.1) mg/kg], hot-plate [ED50 = 22.9 (10.9-48.1) mg/kg] and phenylquinone [ED50) = 1.9 (1.6-9.5) mg/kg] assays.

If (-)-Thebaine has any affinity for mu it is substantially weaker than (+)-thebaine.

The question is why the unnatural enantiomer has HIGHER affinity than the natural enantiomer. Or, actually, why the unnatural enantiomer has ANY affinity at all.

I can't find a single (+)-morphinan that has substantial mu affinity, much less *higher* affinity than the (-)-enantiomer.
 

nabollocks

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LuxEtVeritas said:
at an avg of 4% it is likely not expressing any effect in either capacity to any substantial degree,...

i would not htink in any real capacity it is having any effect to note

What makes you think that?

At 4% Thebaine per poppy, you are consuming approximately 3:1.5:1 ratio of morphine:codeine:thebaine.

And in the experiment quoted by Sturnam:
Monkeys given 23 hrs/day continuous access to 1.0 mg/kg/inj thebaine did, however, self-administer the drug at rates significantly higher than those maintained by saline, but not as high as those supported by 2.0 mg/kg/inj codeine. Two animals self-administering thebaine did not show any signs of withdrawal when injected with 0.1-1.0 mg/kg of naloxone or when saline was substituted for thebaine. A third monkey showed a severe reaction leading to death following an injection of 1.0 mg/kg naloxone.

Thebaine:Codeine was administered at 1:2, suggesting that thebaine is twice as potent? I know this is not science, but it is definately something to think about.
 

vecktor

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I don't think it is very helpful to use data for afghan poppies and extrapolate it to western grown poppy pods or imported decorational pods, the alkaloidal proportions are known to vary from region to region and from variety to variety there are specific high thebaine varieties grown in places like tasmania, so what the concentration of thebaine is in a sample of poppys is not known unless it is analysed.
 

nabollocks

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vecktor said:
I don't think it is very helpful to use data for afghan poppies and extrapolate it to western grown poppy pods or imported decorational pods, the alkaloidal proportions are known to vary from region to region and from variety to variety there are specific high thebaine varieties grown in places like tasmania, so what the concentration of thebaine is in a sample of poppys is not known unless it is analysed.

Obviously Americans drinking PPT are not getting Tasmanian Poppies. And as far as I know Tasmania is the only place that has that variety.

The study with the percentages is pretty helpful in representing ratios. I was not really interested in the exact mg/poppy but the ratio of thebaine to morphine.

And we found that in general poppies contain 3 parts morphine, 1.5 parts codeine, and 1 part thebaine. That is obviusly going to change depending on where they are grown, but at least we have a guide.

Now, at what level does thebaine become a convulsant in humans?

And, has anyone found any literature to back up the 2mg:1mg Thebaine:Codeine argument?

Here is a bit more evidence to support the ratios. A little different, but much the same.
 

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nabollocks

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Seems it has been used to aid w/d. Now we need to know the dose.

Opium Culture: The Art and Ritual of the Chinese Tradition
By Peter Lee, Page 49-50
Published by Inner Traditions / Bear & Company, 2006
ISBN 1594770751, 9781594770753
 

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Sturnam

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Hmmm, this seems to contradict it being used for w/d

However, thebaine not only failed to suppress the morphine withdrawal signs in monkeys physically dependent on morphine, but served to precipitate the signs as well.
T. Yanagita, "An experimental framework for evaluation of dependence liability of various types of drugs in monkeys", Bulletin on Narcotics , vol. 25, No. 2 (1973), pp. 57-64.

But also,
In the first experiment, thebaine or naloxone were given to morphine dependent and non-dependent dogs. Thebaine did not precipitate morphine withdrawal signs. Thus, unlike the findings reported for the rhesus monkey, in the dog the physical dependence potential of thebaine was found to be very low and its antagonistic action lacking.
P. E. Gilbert and W. C. Martin, "The pharmacology of thebaine in the chronic spinal dog", Drug and Alcohol Dependence , vol. 3, 1978, pp. 139-142.

These were both from the WHO's report on the dependence liability of thebaine in 1980.

and here has many different opium alkaloids by %, although they're strictly from Korea.
http://www.unodc.org/unodc/en/data-and-analysis/bulletin/bulletin_1970-01-01_2_page008.html

this seems to say that the ratio for alkaloids is 10:3:1 for morphine, codeine, and thebaine, respectively. but they did talk about how the morphine and codeine content was higher for most of the samples, so your original estimate of 3:1.5:1 could be pretty close.
 

nabollocks

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Sturnam said:
However, thebaine not only failed to suppress the morphine withdrawal signs in monkeys physically dependent on morphine, but served to precipitate the signs as well.

Buprenorphine would do the same thing... that does not mean that it has no place in w/d.

This is really interesting, and I cannot wait to get to the bottom of it.
 

Jabberwocky

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why would you want to take this thing? A stimulating crappy opiate most likely?

I always assumed this was the stuff in pod tea that made it suck donkey balls (dizziness, stimulated crap peripheral effects, etc).
 

nabollocks

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The point is that most PPT drinkers are taking it unknowingly, and I want to know what the dangers of doing so are... call it HR if you will.
 
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