Amazing research article on Mitragynine and 7-HydroxyMitragynine in lab mice: The liver's metabolic role of converting weakly analgesic Mitragynine into very potent 7-HydroxyMitragynine.

      A picture is worth a thousand words. 

  This one shows that the analgesia on the receptor sites of the lab mouse's brain are not activated by Mitragynine directly, but by liver's CYP3A enzymatically mediated conversion of Mitragynine into 7-HydroxyMitragynine, an active metabolite that is 50 times more potent.🐭

   Now for those 1000 words that I spoke of:  Grab a cup of the favorite tea of your choice 🍮☕🍲🍯 ...and cuddle up with your lab mouse to this amazingly enlightening, yet so unnessesarily complex article right here:

📥 https://www.ncbi.nlm.nih.gov/p...

  Don't fret if it became too confusing with all of the sciencey mumbo~jumbo. Just skip over the terminological inexactitudes and indeterminate specificities, 'cuz there be more gooder stuff 'tween them thar maths.

  

    Short abstract:

  Mitragynine is the major active alkaloid of Mitragyna speciosa (kratom). This compound is converted by the liver into a potent active metabolite, 7-hydroxyMitragynine, which mediates its analgesic effect via the mu-opioid receptor. 😀😆😂🤯

            ~~<Translation so that Petey's ever shrinking brain can comprehend>~~

   Natural kratom leaf, by weight, has 1~2% moderately potent Mitragynine, and a tiny fraction of 1% of VERY potent 7-HydroxyMitragynine (or 7-OHM for short). The natural level of VERY potent 7-OHM, that exists in the leaf, is insufficient to cause the observed levels of analgesia (pain relief) that were encountered. 

  🍂In the leaf, Mitragynine is more abundant but not very powerful, however the research theorizes that enzyme CYP3A metabolizes the weaker Mitragynine into potent 7-OHM, after it's first pass through the liver. This increases the available levels of potent 7-OHM  and explains the high level of analgesia (pain relief) observed in the lab mouse.  🐁

  Perhaps growers and enthusiasts alike should be more concerned with good levels of Mitragynine that naturally occur, and let our liver do the hard work of synthesizing 7-OHM.  🤔

  Now aren't you glad that you read the article instead.

                           Cheers! 🍻

          (not sorry for the emoticons) 😇

     ps.     I wish I was a lab mouse.  🐀

  


last edited by peteypyro
SubstanceTheSqid liked this

Cue list of CYP3A inducers for increased conversion and excretion for faster/stronger onset and shorter overall duration. Or Preload with a 3A inducer and post load dose with an inhibitor for increased duration. 

Without looking, I bet piperine/curcumin have potent enzymatic activity along these lines... 

last edited by SubstanceTheSqid

@SubstanceTheSqid  Some dark humor...

                       Lethal Injestion?


Cue the potentiator slideshow: 

   There are some interesting potentiator combos that require care, especially with traditional opioids, most of which depress respiration...

Note that Kratom has been shown to NOT depress respiration, like traditional opioids or opiates do.

     Death by Piperine & Curcuminoids? 

     Or maybe the dangerous potentiator  grapefruit?

Medication interactions:

"Furanocoumarins in grapefruit have other biological effects as well. For example, in humans, bergamottin and 6',7'-dihydroxybergamottin are responsible for the "grapefruit juice effect", in which these furanocoumarins affect certain P450 liver and gut enzymes, such as the inhibition of CYP3A4 which either activates or deactivates many drugs, thus leading to higher or lower levels in the bloodstream. Furanocoumarins have various effects which can specifically increase or decrease (depending on the drug) the blood levels of many pharmaceuticals in ways that can be life-threatening and so FDA approved drugs will include warnings for grapefruit."

It's a scary world out there.....

          And in my garden/farm.  🤯

last edited by peteypyro

For those without gooble handy and concerned about grapefruit contraindications, fresh lemon juice is a great replacement.  Sweeten to taste, of course.  

@roadkill  I'll revisit this topic of 7-ohm enhancement again soon. I need to research the existing bentuangie papers and both videos on the fermentation and drying processes.  

      ◇◇ work-in-progress◇◇

last edited by peteypyro

also we are going to send out this as the featured post along with what users have missed to everyone who has created an account here.

I'm looking forward to reminding those folks that we are here.