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What potency, Ki ratio, IC50, LD50, EC50, ED50, or I generally suck at search thread.

Nagelfar

Bluelight Crew
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OK, I know it's out there, somewhere. But I can never find the damned potency of this or that opioid when I have a reason to know it. So I'm just making a general thread I'm going to post in whenever I need to ask this question, and others are welcome to as well, and it doesn't have to be limited to opioids, but what cannabinoid is a full or partial agonist, Ki values of stimulants, or just about anything that has to do with relative affinity or efficacy of any psychoactive substance you can work into a question and have somebody else do the work of finding it for you (hopefully when you've tried your damnedest yourself and are at the point of throwing your hands up in the air, but the reason for you needing to know still hasn't gone away)

I for one, am limited to my time online because I use 1-hour length library computers, so by the time I get into my groove of sifting through all the cruft a search engine usually spits at me, I get automatically logged off once I'm anywhere near the time I even get close to the meaty parts of the info I'm seeking.

So here is my question, so please, someone, humor me, take a moment (or maybe a couple wasted hours) of your time to try using your own secret backdoor of whatever chemistry archives or databases you've managed to hack into and keep secret to yourself (or, find in plain sight and become certain that I must be blind or otherwise, even if just relatively, cognitively disabled or impaired) and let me know this, most likely completely meaningless to you, tidbit of something you probably couldn't care less about.

I'm really just looking, right now, for the relative potency of oxycodone's synthetic intermediates, as in, the products of it (which ever different synthesis can be used) between codeine (possibly morphine or thebaine too) and it's final stage as oxycodone.

I believe what I'm looking for is the strength relative codeine (or morphine would be fine) of:
14-hydroxylcodeine
7,8-dihydrocodeine
carbonylcodeine (is there such a thing?)

...or what ever the names are of the potential intermediates of codeine, or even morphine, & oxycodone. I know someone knows, this is a basic and generally prevalent opioid whose synthesis probably has been elucidated at least several different ways. Some easier than others, but that doesn't concern me. I just want to know their strengths.

I already know that of codeinone (thank you, Wikipedia!), it's one third the strength of codeine (and is also used in the production of hydrocodone, but that is neither here nor there.)

Everyone always seems to have this sort of question be the dread of their day, and I always feel the fool for coming forth and asking it, but I've a reason (don't we all) so I beg your leniency and may one who needn't otherwise take the time please be gracious enough to educate me. I promise I'll remember it, and make it always part of the Rolodex of my implacable photographic memory and swear a blood oath to use it to the boon of everyone starved of such specific & specialized knowledge for the benefit of mankind whenever the need might arise to do so.

Thank you for your understanding.
 
Are you talking about biological potency as analgesics, or binding affinity?

There's a paper I can't get, but looks like it could be helpful:
The analgesic properties of some 14-substituted derivatives of codeine and codeinone
Journal of Pharmacy and Pharmacology Volume 16, Issue 3, pages 174–182, March 1964 W. R. BUCKETT, MURIEL E. FARQUHARSON and C. G. HAINING

From what I recall...
dihydrocodeine is anywhere from 150 to 200% as potent as codeine given orally
codeineone (= carbonylcodeine) only 1/3 as potent as codeine
14-hydroxycodeine and 14-hydroxycodeinone equal to or slightly greater than codeine.
 
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Are you talking about biological potency as analgesics, or binding affinity?

There's a paper I can't get, but looks like it could be helpful:
The analgesic properties of some 14-substituted derivatives of codeine and codeinone
Journal of Pharmacy and Pharmacology Volume 16, Issue 3, pages 174–182, March 1964 W. R. BUCKETT, MURIEL E. FARQUHARSON and C. G. HAINING

From what I recall...
dihydrocodeine is anywhere from 150 to 200% as potent as codeine given orally
codeineone (= carbonylcodeine) only 1/3 as potent as codeine
14-hydroxycodeine and 14-hydroxycodeinone equal to or slightly greater than codeine.

Thank you so much, sekio! Yes this is what I needed, the problem is I need citations (you know me, my Wikipedia-addiction; I have an edit in mind.) but I figured they were around said strength (I realized after I posted that codeinone was carbonylcodeine, since oxycodone only has three changes from being codeine.)

(...ironically, that link is, as you say, blocked; but the irony is it's by [a university]! lol)
 
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Thank you so much, sekio! Yes this is what I needed, the problem is I need citations (you know me, my Wikipedia-addiction; I have an edit in mind.) but I figured they were around said strength (I realized after I posted that codeinone was carbonylcodeine, since oxycodone only has three changes from being codeine.)
The actual location of the publication is: http://onlinelibrary.wiley.com/doi/10.1111/j.2042-7158.1964.tb07440.x/abstract

potency relative to morphine (morphine = 1.0), SC administration:
codeine = 0.17 (rats)
14-hydroxycodeine = 0.13 (rats), 0.12 (mice)
codeinone = potency could not be determined because it produced convulsions
 
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Thank you serotonin2A.

Why the edit to my post sekio, was some rule violated? There's no irony any longer to my observation, if that has to be done in the future please just remove the whole offending comment so I don't look like a stooge. ;-P Thanks.
 
I just forgot to snip a proxy URL that I shouldn't be posting (in the effort of minimizing personal information disclosure) sorry for any disruptions there :p
 
Gotcha...

...I also never got a proper response to what would be Loperamides potency relative morphine when I inquired elsewhere, I think the Ki binding values suggested to me half the potency of morphine (were it to effect the brain by readily & completely penetrating the BBB) by making assumptions based on Ki binding to the mu site. Though I'd like someone to confirm.
 
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