Question about binding affinities. Kratom vs Oxycodone

[GeisterxFahrer]

Does anyone know how competitive the active alkaloids of Kratom are in regards to their affinity to the mu receptors compared to that of oxycodone? I have taken my prescription already today (20mg Oxycontin) and I just received some Ultra Enhanced Indo Kratom and was wondering if it would even work right now or if it would kick the oxycodone out and take over essentially taking away the 12 hour effect. Does anyone know where I can find information like this?

 

[sekio]

http://pdsp.med.unc.edu/pdsp.php is a good resource. Also PubMed/Google Scholar searches.

pKi = -log(Ki)

Mitragynine pKi = 8.14 +/- 0.28
7-OH-mitragynine pKi = 7.87 +/- 0.16
Oxycodone pKi = 7.74

Mitragynine and friends out-compete kratom, so you're fine. Bigger pKi = smaller Ki = tighter binding.

(source: Studies on the Synthesis and Opioid Agonistic Activities of
Mitragynine-Related Indole Alkaloids: Discovery of Opioid Agonists
Structurally Different from Other Opioid Ligands, Takayama et al.)

 

[GeisterxFahrer]

woa! thank you! now I have to figure out what all this means.

Im a noob with this site.. How do i find the info that you found?

 

[sekio]

1. Figure out what receptor you want activity figures at
2. Find the chemical in the PDSP database and lookup its Ki or pKi. Also note the "Hot" ligand - the reference standard for receptor binding that the chemical is assayed against. For mu-opioid receptors this is usually something like [3H]DAMGO or [3H]endorphin. The ligand should stay the same across all pKi/Ki values you are comparing. Don't compare an affinity vs Damgo for an affinity vs Endorphin. Also note where the ligand was tested (e.g. cloned human cells or rat brains).
3. If it's not in the database Ilinked to, do a Google/PubMed search for it and see fi you can find a Ki or pKi.
4. Compare them! Smaller Ki = tighter binding = larger pKi. Also of note is the EC50 figure or an activation % or something of the like to tell if it is a functional agonist or antagonist.

 

[GeisterxFahrer]

Thanks sekio. Now I can start making my list

 

[Mugz]

I'm going to move this to OD, as this isn't basic drug discussion, also I thought that since you are the one answering the questions sekio, you would maybe rather have this thread in your own forum If not, then send it back

 

[Woodsong]

Couldn't tell ya for oxy, but from my experience, kratom will definitely kill a hydrocodone or poppy tea buzz for me...
It also makes my tolerance skyrocket...

 

[GeisterxFahrer]

Couldn't tell ya for oxy, but from my experience, kratom will definitely kill a hydrocodone or poppy tea buzz for me...
It also makes my tolerance skyrocket...

Hey i am really close to Decatur GA I think. anywho, Oddly enough, for me at least, Kratom seemed to lower my opiate tolerance. I do not know how often it does this in people. I just received a supposed 7OHM extract. if the site gave the real information (which I think they did, they are very reputable) then my calculations of equal analgesia should be correct. I posted the math on another thread but based on availlable research and assuming its correct, I calculated that this 1 gram I ordered would have the equivelent of 300 doses of 15mg oxycodone IR. I calculated that it is active at a mere 3.34 mg. I will soon test it, and also I will see how it affects the oxycontin I took earlier.