Mitragynine - Speedballing for lazy people
- the principal alkaloid situated in the leaves of Mitragyna speciosa Korth (Kratom, Biak-Biak), a rubiaceous tropical tree that is native to Southeast Asia
- people have been known to chew fresh leaves to acquire a numbing and stimulating effect, enabling them to fight fatigue and increase their tolerance to harsh working conditions
- acts like morphine via mu opioid receptors to produce analgesia, although the potency of this effect is only about one-fourth that of morphine, making it akin to less potent opioid analgesics such as codeine (Tylenol 3s, baby!) or methadone
- also produces a cocaine-like stimulating effect, likely due to it possessing a similar structure to yohimbine, an alpha2-adrenergic receptor antagonist that has stimulant activity and is best known for its alleged ability to treat erectile dysfunction (not an ad, I promise!)
- changing a carbon double bond to a single bond and adding a hydroxyl group gives you 7-hydroxymitragynine, which is also found in the aforementioned plant, albeit in fairly small amounts, but is significantly more potent than morphine and so is likely primarily responsible for the analgesic effects of the plant
http://en.wikipedia.org/wiki/Kratom
10 chemically inspired comments:
the fact that you included the words "erectile dysfuntion" will probably get you a bajillion hits from google. Not that you don't already have that problem, judging from your Google search posts, but funny anyways.
I'm glad you posted on this plant and its drugs. Fascinating. Unfortunately, the accessibility of the dried leaf (and fortified extracts) on the itnernet is creating an army of addicts. Like any mu opioid agonist, 7-hydroxymitragynine (and mitragynine) are extremely addictive! Painful, horrible withdrawal, escalating doses, etc...
I'm always looking to try new experiments with ethnobotanicals. I have been researching forever and cannot find info on hoe to synthesize 7-OH from mitragynine. any help please =)
FYI this really is a no-joke opiod, from the perspective of dose escalation and withdrawals. I didn't treat it as the real deal, and I paid dearly in terrible terrible withdrawal that lasted for close to 2 weeks. Be mighty careful with this one!
Plenty of "legal highs" out there (plants in the garden, research chemicals, plant extractions, inhailants), but I would like to see more scientific research before I ever concidered experimented. SO far anything proven to make you feel good is illegal or controlled by the governement.
I don't quite agree with the second comment made. Mitragynin and 7-OH are not terribly addictive. Whilst 7-OH is more potent than Morphine (probably on par with hydromorphone), the administration of the whole plant reduces the overall addictive potential due to the other alkaloids present, one of which acts as a partial mu-agonist, another as a full antagonist at mu and yet another as an NMDA-antagonist. Additionally, withdrawal symptoms have been described as being milder than that of morphine, and shorter in duration. Whilst tachyphylaxis is expected of most mu-agonists, 7-OH-mitragynine is selective for mu-1, not mu-2.
Good article by the way. I enjoyed reading your blog :)
Many of these legal highs contain analogues of controlled substances. No proper clinical testing has been done and we have only anecdotal reports to go on. The biggest danger lies not with the herbs (since some of these have had a long history of indigenous use) but with the so called "Party Pills" and herbal ecstasy pills that contain anything from methamphetamine analogues to aporphine alkaloids like Glaucine. Not to mention that the manufacturers of these products make it a point to NOT reveal the ingredients of their pills let alone the quantity of the ingredients. I can agree how the use of such products could serve a purpose in Harm Reduction, but the very fact that the manufacturers do not reveal the contents of what they sell, poses a terrible risk to the consumer.
"Unfortunately, the accessibility of the dried leaf (and fortified extracts) on the itnernet is creating an army of addicts. Like any mu opioid agonist, 7-hydroxymitragynine (and mitragynine) are extremely addictive! Painful, horrible withdrawal, escalating doses, etc..."
Wrong, wrong and wrong. Compared to the more powerful opiate painkillers, the number of people addicted to mitragynine is extremely low. This substance is much less addictive than opiates, and the withdrawal syndrome, by all accounts, is much less severe. Please do your homework before posting.
I believe that mitragynine and its 7-th hydroxyl brother are indeed a very viable narcotic of the future our research indicated that those treated with fentanyl, oxycodone, and morphine have shown an acceptance to mitragynine's effects after being withdrawn from the phenanthrene series drugs such as morphine and codeine as well as semi-synthetics, hydro and oxy-morphones and codones, as well as fully synthetic agonists such as fentanyl and meperidine. However it should be noted methadone is a different creature all together, as well as its cousin LAAM which have a long duration of action(more research is necessary) as with all the natural opioids or the phenanthrene series and their corresponding semi synthetics. mitragynine is a very promising class of narcotic as i said before not like that awful tramadol, which the DEA even failed to schedule.
Methadone is by no means a weak opioid. At low doses it is about twice as potent, and as the dosage of methadone goes up, it's relative activity in comparasion to morphine only rises. 10 years of school in pharmacology and theraueputics, as well as 15 years of use of the various and sundry opioids give me a pretty good background of knowledge on which to draw upon when I make this comment. Thanks for an otherwise excellent adventure.
Kev
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