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"Legal" RC synthetic opiods?

I wonder what's the simplest l-tyrosine derivative you can get that's an opioid agonist- the hydroxy group on l-tyrosine is very important for binding, and it's the first amino acid on all the endorphin peptides... Basically I'm wondering how many rings of levorphanol you can decyclicize before it loses too much activity.

I couldn't find any 3d pictures of endorphin (mu agonist) but here's enkephalin, (delta agonist):
enkephalin.gif
 
What's the binding profile difference of met enkephalin vs. leu enkephalin? I'm too lazy right now.

I wonder what's the simplest l-tyrosine derivative you can get that's an opioid agonist- the hydroxy group on l-tyrosine is very important for binding, and it's the first amino acid on all the endorphin peptides... Basically I'm wondering how many rings of levorphanol you can decyclicize before it loses too much activity.
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This is something I've talked about before. I think we go to lefetamine to answer the question. Open the alpha phenyl ring, and you have no opioid. close it, you do.

I have trouble finding documentation, but I'm nearly certain that the para-hydroxy analogue of lefetamine would be more potent. Probably lots more potent.

What I really want to look at though would be 4-hydroxy-alpha-(cyclohexan-4-one)-N,N-dimethylphenethylamine. I would be amazed if that wasn't at least 10x more potent an agonist than lefetamine.
 
That's interesting, I guess that's about the simplest that you can get.. It's nice that nitrogen doesn't have to be cyclicized to piperidine or whatever...

Would the cyclohexane (or cyclohexan-4-one, which would be more potent?) ring on your compound be lipophilic enough to carry the compound to the brain right? Because for example tyramine (4-hydroxy phenethylamine) is a DE/NA releaser but can't cross the BBB obviously.
 
now this is very intresting.. wow

n thats fucked really, if there was a widely available opiate rc.. rc's would be no mo..
 
Hammilton said:
You're thinking about aromatic amines, which are quite toxic. nitro aromatics don't have these issues. I'm having trouble finding any connection between toxicity and the latter.
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Well try uncoupling phosphorylation of ADP to ATP. Lots of munitions workerss in WW2 suffered from such poisoning from handling TNT, picric acid (trinitrophenol) etc

And they can be reduced in vivo to produce the aromatic amine...
 
Yeah, nitrobenzene and family are all pretty nasty.

Oxyfluorfen, pendimethalin, dintro-o-cresol, dinoseb, dinoterb, parathion/thiophos, and fluorodifen are all suspected carcinogens...
 
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Exactly! Although I don't think that parathion is feared much for its potential to cause cancer but rather for its acute toxicity.

Anyway, although this seems to be a lesser known issue (in contrary to primary aniline's toxicity), I have to insist: Aromatic nitro-compounds are definitively nasty stuff. It gets even worse if there's one or more halogens added to the ring... :\

- Murphy
 
Isn't the oil from nigella sativa seed supposed to have some mild opiate activity?

Not an "RC", but most certainly legal. Rather easy to grow and pretty too, with edible, spicy seeds.
 
MurphyClox said:
Exactly! Although I don't think that parathion is feared much for its potential to cause cancer but rather for its acute toxicity.
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Most organophosphates are by and large horrible for anything that lives.

My mother was working on farms in the days when they were still using guthion in BC, and she broke out in sores and couldn't breathe while sleeping for weeks without sitting up in a chair. A lot of the research that led to the development of organophosphate pesticides started with research on nerve agents like sarin. Because of this, anybody would be hard-pressed at convincing me that organophospate pesticides are nontoxic to humans, and it's a wonder people are even still allowed to use them. Their acute toxicity and environmental persistence outweighs their benefits by far, in my opinion.
 
Acute toxicity is obviously not an issue para-nitro-methopholine. There are so many nitroaromatics that are fine. I'm not aware of many aromatic amines that are fine.

Has any study of the metabolism of this been had?
 
Nibiru said:
Isn't the oil from nigella sativa seed supposed to have some mild opiate activity?

Not an "RC", but most certainly legal. Rather easy to grow and pretty too, with edible, spicy seeds.
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Meh...I suppose you could get away with calling this an opioid, but I couldnt possibly overstate how mild it is.
Taken on its own, any opioid effect could easily be attributed to placebo.
I will admit though, that a few tablespoons of nigella sativa oil on top of a traditional opioid, really does have some solid potentiating effects.

Anyone else experience this?
 
Oh, O-desmethyltramadol has been found in a product purported to be kratom, called "krypton kratom", a metabolite which is far more potent than tramadol. I wonder if it is enantiomerically pure, probably not, but potentially...
 
I wonder if they start making desmethyltramadol the same way they make morphine from codeine...

And the next step... Homebake tramadol: O-acetyl-desmethyltramadol?
 
O-Desmethyltramadol is now available on the market. Does anyone know how doses of this would compare to tramadol? Or in other words, how much O-Desmethyltramadol is produced when tramadol is metabolized?
 
negrogesic said:
Oh, O-desmethyltramadol has been found in a product purported to be kratom, called "krypton kratom", a metabolite which is far more potent than tramadol. I wonder if it is enantiomerically pure, probably not, but potentially...
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Wow, really? Where did you come across this information?
 
MescalitoBandito said:
O-Desmethyltramadol is now available on the market. Does anyone know how doses of this would compare to tramadol? Or in other words, how much O-Desmethyltramadol is produced when tramadol is metabolized?
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it is about 3 times as potent as tramadol, mentioned here
 
MescalitoBandito said:
O-Desmethyltramadol is now available on the market. Does anyone know how doses of this would compare to tramadol? Or in other words, how much O-Desmethyltramadol is produced when tramadol is metabolized?
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As with tramadol itself, the O-desmethyl metabolites can be categorized into a primarily a analgesic one (+ enantiomer; has also 5HT-reuptake inhibiting activity) and a primarily NE-reuptake inhibiting one (- enantiomer). Please note that tramadol is usually employed as racemate.
(Ref: J Pharmacol Exp Ther 2003, 305, p.710)

- Murphy
 
the reported O-desmethyltramadol going on sale just now is mentioned to be racemate.
 
is O-Desmethyltramadol the first opiod rc to hit the market or have there been others before?!
 
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