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Tramadol related Opioid Agonists

Gaz_hmmmm

Gaz_hmmmm

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Tramadol (C16H25NO2) as we all know is kinda weak when it comes to getting high.

I was wondering if anyone one has any experience or knows if the following related substances are any good when it comes to analgesia, euphoria and also for weaning when opioid dependant ...

(-)-(1S,2S)-O,N-Di-desmethyl Tramadol HCl (C14H21NO2 . HCl)
(-)-(1S,2S)-O,N-Di-desmethy.gif


(+)-(1R,2R)-O,N-Di-desmethyl Tramadol HCl (C14H21NO2 . HCl)
(+)-(1R,2R)-O,N-Di-desmethy.gif


O,N-Di-Desmethyl Tramadol HCl (C14H21NO2 . HCl)
O,N-Di-Desmethyl-Tramadol-H.gif


O-Ethyl Tramadol (C17H27NO2)
O-Ethyl-Tramadol.gif


If anyone has any info' on these please do put it here as I can't find much about them other then they're not controlled substances and I don't think they're used medically at the moment, but I could be wrong about them (some)! :\
 
any n-demethylated tramadol-like molecules aren't active as opioid-agonists.
so far concerning your first 3 examples.

o-ethyl-tramadol should be similar to ethylmorphin and thus be of the same activity as tramadol itself.
 
Gaz, activity falls when the alcoholic function is esterified, while having a delta-1,2 double bond shortens duration, without effecting potency that much. Tramadol's cis analog is a VERY WEAK analgesic, if at all, and all non-phenolic analogs of tramadol reported thus far have been inactive. The importance of the phenolic function suggests that tramadol type is closely related to morphine, and orientation of their basic group aromatic features mimics that of the alkaloid. Concerning M-1 (0-desmethyl), if you transposition the aryl and one of the alpha hydrogens of the aminomethyl side chain with each other, you get quite an active compound (ciramadol). It is about 2X morphine in standard rat tail flick test, but is partial agonist/antagonistic. Even though it is more potent than tramadol, it produces very little euphoria. For those who properly metabolise tramadol, psychic effects can be the pinnacle of the opioid experience (even rivaling ketibemidone).

O-desmethyl more potent, but dimethylamino grp is needed to retain potency. N-O-didesmethyltramadol, with just the methylamino grp nitrogen, is much less active. Has this answered your question?
 
The M1 metabolite (o-desmethyl) is the active drug. Tramadol is a cut-down codeine analog so it's only really active when that ether is removed. I had the chance to sample the M1 metabolite and it's a LOT stronger. Snorting gives a similar hit to morphine (but more speedy). You may ask how? Well, a LONG time ago Grunthenthal asked for volenteers to test this group of pain-killers out. I signed up and they very stupidly left vials of solution unlocked. I pocketed some vials of the M1. I took it home, dried it & snorted it. 30mg gives a great hit!
 
If you wanted to find something interesting, I would suggest swapping the N,N dimethyl for something else. Piperidine or morpholine would be obvious canidates looking at the modified 3,3 diphenyl heptanone class of opiates. Methadone -> dipipanone or dextromoramide.
 
I guess you must have had that rareexotic M1 from multiple sources Mr. Gummy Bears ;)

haribo1 said:
The M1 metabolite (o-desmethyl) is the active drug. Tramadol is a cut-down codeine analog so it's only really active when that ether is removed. I had the chance to sample the M1 metabolite and it's a LOT stronger. Snorting gives a similar hit to morphine (but more speedy). You may ask how? Well, a LONG time ago Grunthenthal asked for volenteers to test this group of pain-killers out. I signed up and they very stupidly left vials of solution unlocked. I pocketed some vials of the M1. I took it home, dried it & snorted it. 30mg gives a great hit!
Click to expand...

27-01-2007, 20:48 #7
haribo1
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Join Date: Nov 2006
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Offline: I've tried desmethyl tramadol from Sigma-Aldrich. It's more or less half way between morphine & codeine. Snorted it kicks in at about 3 minutes. Very euphoric and long-lasting. It caused me some hyperthermia but that was the only side-effect off 100mg of the HCl salt.
 
Just watch out that if you wake up from your tramadol nod to go to the bathroom, that you don't bump into things;) hehehe
 
sarbanes said:
27-01-2007, 20:48 #7
haribo1
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Join Date: Nov 2006
Posts: 3,082
Offline: I've tried desmethyl tramadol from Sigma-Aldrich. It's more or less half way between morphine & codeine. Snorted it kicks in at about 3 minutes. Very euphoric and long-lasting. It caused me some hyperthermia but that was the only side-effect off 100mg of the HCl salt.
Click to expand...

No mate, Gruntenthal used Sigma-Aldrich material for some reason. Now you know HOW I 'aquired' it. ;)
 
haribo1 said:
No mate, Gruntenthal used Sigma-Aldrich material for some reason. Now you know HOW I 'aquired' it. ;)
Click to expand...

But you claimed to have ordered it from Sigma Aldrich (you even said the price), and you also said you stole it from Gruenthal when they left out the vials. No offence, but I'm curious what your going to say next;)

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haribo1
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I've tried desmethyl tramadol from Sigma-Aldrich. It's more or less half way between morphine & codeine. Snorted it kicks in at about 3 minutes. Very euphoric and long-lasting. It caused me some hyperthermia but that was the only side-effect off 100mg of the HCl salt.

haribo1
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This is going back a decade! 1g was about $200. Yes it was freebase but that's hardly difficult to sort out.

01-05-2007, 06:39 #4
haribo1
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Join Date: Nov 2006
Posts: 3,129
Offline:
The M1 metabolite (o-desmethyl) is the active drug. Tramadol is a cut-down codeine analog so it's only really active when that ether is removed. I had the chance to sample the M1 metabolite and it's a LOT stronger. Snorting gives a similar hit to morphine (but more speedy). You may ask how? Well, a LONG time ago Grunthenthal asked for volenteers to test this group of pain-killers out. I signed up and they very stupidly left vials of solution unlocked. I pocketed some vials of the M1. I took it home, dried it & snorted it. 30mg gives a great hit!
Quote:
Originally Posted by sarbanes
27-01-2007, 20:48 #7
haribo1
Bluelighter


Join Date: Nov 2006
Posts: 3,082
Offline: I've tried desmethyl tramadol from Sigma-Aldrich. It's more or less half way between morphine & codeine. Snorted it kicks in at about 3 minutes. Very euphoric and long-lasting. It caused me some hyperthermia but that was the only side-effect off 100mg of the HCl salt.

No mate, Gruntenthal used Sigma-Aldrich material for some reason. Now you know HOW I 'aquired' it.

So, haribo1, what really happened? Also, the freebase is an oil. Did you convert to the HCL salt on your own (just one gram?) hehehe. Heh, if your lying its ok, but might as well come clean now;) no offence, and best. Sb
 
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Oh well, in any event, don't attempt to snort the FB, it will burn to high hell! Remember its a lipophyllic oil. Will numb you.
 
fastandbulbous said:
^ Thought someone was on about snorting me for a second there (I get rather uppity if someone tries to do things with razor plades to me!!)
Click to expand...


Lol, I see that now! Nah, if I was going to say that, would have said FAB (not just FB). Because you look so FAB in that leather S&M mask, hehe;)

Didn't even think| F=fast, B=Bulbous when I was initially writing. BTW, FAB, I got a few books you might be interested in (not floating around on internet anywhere). One is the Bentley book, Chem of the Morphine Alk. Other is "Opioid Analgesics, Chem & receptors", by Casy and Parfitt. Also, have the main Arckander books (Perfume and Flavor Chemicals, vol 1&2), and "Perfume and Flavor Materials of Natural Origin"

I photographed the ones I dont have hard copy of, cause its the most time effective way for me to quickly do hundreds of pages. Got my digital camera mounted on a ring stand with two clamps, making a T. The Casy book is only one I own the hard copy. Was lucky to get it for $26!

Best,
S
 
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