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interest in natural indole µ-opoid receptor agonists and other compounds for aide in opioid wit Options
 
entheogenic-gnosis
#1 Posted : 12/6/2015 3:41:58 PM
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P. nitida seeds contain a mixture of alkaloids producing antipyretic and antiinflammatory effects along with analgesia.[3][4] Several of these were shown to bind to opioid receptors in vitro, and two compounds, akuammidine and ψ-akuammigine, were found to be potent μ-opioid agonists, although not particularly selective. Surprisingly the main alkaloid from the seeds, akuammine, was found to be an opioid antagonist when tested in vitro and canceled out the effects of the active agonist components.[5] This finding contradicts the belief by some pharmacological scientists that there are no naturally occurring opioid antagonists.
https://en.m.wikipedia.org/wiki/Akuammine

Picralima nitida seeds are commercially available and are not scheduled, controlled or regulated. I have had much interest in natural µ-opioid delta and kappa opioid receptor agonists for the purpose of aiding opioid withdrawal, with compounds which include a prolonged withdrawal such as methadone in mind.

Mitragynine is a natural indole µ-opioid receptor agonist which I have looked into for this purpose as well, this compound is available as "kratom" extract sold in smoke-shops, and I believe that perhaps a mix of Mitragynine and related alkaloids derived from Mitragyna speciosa along with natural opioid receptor agonist from other plant sources such as P. nitida seeds, along with dextromethorphan and small amounts of harmala alkaloids may be a good place to begin.

Anyway, as Picralima nitida seeds contain an opioid receptor antagonist as their primary alkaloid (though this compound is likely eventually metabolized into an agonist in vivo)

I would be interested in learning about the process for extracting akuammidine and ψ-akuammigine from P. nitida seeds, while leaving behind any akuammine. Though I'm sure extracts may be commercially available, it could end up being more efficient and cost effective to preform an extract from the seeds themselves, provided the procedure is fairly simple ans requires common solvents and reagents.

I also believe that these natural indole opioids in combination with Racemorphan May be benneficial for aide in withdrawal. dextromethorphan is an over the counter opioid/NMDA receptor agonist and has been effective in opioid withdrawal, however the levatory enantiomer is a full µ-opioid receptor agonist, which leads me to believe that racemorphan would be optimal for this purpose, specially if combined with Mitragynine and akuammidine and ψ-akuammigine, perhaps even with small amounts of harmala alkaloids (which share structural similarity to ibogaine) added into the mix.

I'm still searching for novel compounds or novel combinations of compounds for aide in prolonged opioid withdrawal, such as from methadone. In this country ibogaine detox is not an option and most doctors will send an opioid addict to a methadone program before inpatient rehab. Methadone may reduce harm as in the addicts are not using needles or breaking the law, but it does nothing to treat addiction, methadone patients are still very addicted, they still must be concerned about enduring a hellish withdrawl if they miss even a single dose, they are still subject to the compounds narcotic effects and are still subject to serious physical and injury and other health issues as a result of their methadone addiction. Ibogaine May eventually make it to the states, but until that time I feel I may be able to devise some concoction of unscheduled compounds which will provide relief during tough withdrawal and prevent relapse.

The natural indole opioid compounds caught my attention simply because of my in depth study of tryptamines and other psychedelic indole compounds, however I'm open to researching any compound out there that may serve this purpose regardless of structure or natural availability.

-eg


 

Good quality Syrian rue (Peganum harmala) for an incredible price!
 
null24
#2 Posted : 12/6/2015 4:21:56 PM

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Is this academic or personal research?

I'm into month three free of methadone (the first extended period of opiate free life for mesince 1995). While I have concerns over long term damage done in such an extended period of addiction, I've found kratom very helpful.

Doesn't help me sleep, but allows me to stop perseverating on cravings. I don't use it daily as I don't want a dependency on anything.

My methadone taper occurred over 6 months, dropping 2-5 mg per week from 80. I stayed at 2 mg for over 10 days before walking, and I think rapid titration to as low a dose as one can handle (1-3) and the staying there for a period to allow the "backed up" 'done to excrete is the key.

That and extreme mental and emotional preperation.

entheogenic-gnosis wrote:
)
. Methadone may reduce harm as in the addicts are not using needles or breaking the law, but it does nothing to treat addiction, methadone patients are still very addicted




Many patients labor under the misconception that harm reduction refers to them, when the entity of concern is society at large. If it was addicts safety they were concerned with, ibogaine would be legal.
Sine experientia nihil sufficienter sciri potest -Roger Bacon
*γνῶθι σεαυτόν*
 
entheogenic-gnosis
#3 Posted : 12/7/2015 3:15:20 PM
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null24 wrote:
Is this academic or personal research?

I'm into month three free of methadone (the first extended period of opiate free life for mesince 1995). While I have concerns over long term damage done in such an extended period of addiction, I've found kratom very helpful.

Doesn't help me sleep, but allows me to stop perseverating on cravings. I don't use it daily as I don't want a dependency on anything.

My methadone taper occurred over 6 months, dropping 2-5 mg per week from 80. I stayed at 2 mg for over 10 days before walking, and I think rapid titration to as low a dose as one can handle (1-3) and the staying there for a period to allow the "backed up" 'done to excrete is the key.

That and extreme mental and emotional preperation.

entheogenic-gnosis wrote:
)
. Methadone may reduce harm as in the addicts are not using needles or breaking the law, but it does nothing to treat addiction, methadone patients are still very addicted




Many patients labor under the misconception that harm reduction refers to them, when the entity of concern is society at large. If it was addicts safety they were concerned with, ibogaine would be legal.


This is personal research, but it's well informed.

I don't tell others in my daily life I'm on methadone, on this forum only a few people know who I actually am in real life, so it's a little bit easier to talk about here, but still difficult. anyway I have great interest in novel methods for aiding in opioid withdrawal, and have great interests in discussing these potential methods and compounds involved with them, though I'm not particularly interested in discussing my personal struggles.

You make valid points, thank you for the response, I was a skateboarder when I was younger, and due to an injury involving a skateboard I was put on narcotic pain medication, eventually the doctors cut my prescription leaving me in pain, withdrawl and seeking other opioids for relief, after a struggle with illeagal opioids I was placed on methadone, which was fine until I tried to stop, your told "it's an easier withdrwal than heroin".... which is nonsense, methadone withdrwal last far longer and involves different but equally painfull symptoms.

When you said something to the effect of "they are protecting society, not the addicts" it made me think of the fact that methadone in no way reduces criminal behavior of its patients, a good deal of patients don't even stop using illicit opioids while on the program. it allows these people to be closely monitored, and it is a "study" between the DEA and the university, so statistical information as well as information on the addicts behaviors and habitts are collected, but other than that I find the justification for these programs to be ill-founded and questionable, in the end it turns into a form of making money, though when you make your money from the weakneses and suffering of others your technically profiteering...Or at the very least drug dealing...

But I'm getting off topic...novel compounds to aide in withdrawal was my focus here.

http://self.gutenberg.org/articles/Opioid

The link above is great for descriptions and scientific data of opioid compounds.

I'll post more as my research continues.

-eg
 
 
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