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Opioids O-Desmethyltramadol

Here is an article discussing the seizure potential of tramadol and its metabolites.

The fact that one of the enantiomers of tramadol might be particularly
potent (potency in terms of seizure potential) was not found to be the case; the (+)- and
(–)enantiomers were about equipotent to tramadol. The
fact that the M1 (aka o-desmethyltramadol) metabolite or its enantiomers might be particularly potent was also not found to be the case. M1 and
its (+)- and (–)enantiomers were less potent than tramadol
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http://jpet.aspetjournals.org/cgi/reprint/325/2/500.pdf
 
In provoking seizures.

Ki for human mu opioid receptors (nM)

Tramadol (racemate): 17,000
Tramadol (+): 15,700
Tramadol (-): 28 800
O-Desmethyltramadol (racemate): 3190
O-Desmethyltramadol (+): 153
O-Desmethyltramadol (-): 9680
Morphine: 7.1

Less is more, as these are the required concentrations to displace a known substrate.

Lai J, Ma SW, Porreca F, Raffa RB. Tramadol, M1 metabolite and enantiomer affinities for cloned human opioid receptors expressed in transfected HN9.10 neuroblastoma cells. European Journal of Pharmacology. 1996 Dec 5;316(2-3):369-72.

And, with this inclusion of this substance in their catalogue, I would wager mucho that this place will not be around much longer.
 
moniorojo said:
So in the end it is LESS potent than tramadol?!?!?!
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less potent in it's seizure inducing potential, meaning you're less likely to get a seizure with this stuff than you are with regular tramadol.

No word yet as to its potency (as in dose).
 
In provoking seizures.

Ki for human mu opioid receptors (nM)

Tramadol (racemate): 17,000
Tramadol (+): 15,700
Tramadol (-): 28 800
O-Desmethyltramadol (racemate): 3190
O-Desmethyltramadol (+): 153
O-Desmethyltramadol (-): 9680
Morphine: 7.1

Less is more, as these are the required concentrations to displace a known substrate.
Click to expand...

thanks for the info
so those numbers have nothing to do with potency?
wouldn't it be logical to think its between tramadol and morphine in potency (closer to the potency of tramadol)
 
My guess is, probably, but as it seems to be a strong opioid I'd proceed carefully. That it is a NET substrate also concerns me, as it may give the illusion of wakefulness similar to combinations like speedballs while you proceed perilously towards dosages that may suppress the respiratory system enough to kill you.
 
as it may give the illusion of wakefulness similar to combinations like speedballs while you proceed perilously towards dosages that may suppress the respiratory system enough to kill you.
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I'm a low dose person and don't really re-dose (except for mephedrone which I have decided to stop using). I just want an idea of the potency but I guess starting at 10 mgs would be safe enough right?!
 
^Fuck no, I know nothing about this drug but 10mg is WAY too high to start titration of an unknown substance. Seriously, if you go around taking drugs you know nothing about at doses like that you will fuck yourself up bigtime. What if you did that with fentanyl, or LSD, or DOx, or benzos? You would be fucked in the head or in the cold hard ground. If you're making an educated guess then I apologise for this reaction, but if you think that 10mg is a safe starting dose with anything then you need education as a matter of urgency.
 
Jamshyd said:
as almost miraculous affects on stopping any kind of desire to drink alcohol. Just writing this brings me to tears because for those of us who can use it for this purpose, the tramadol itself presents a big addiction problem as well. Please be careful. I would never want to see you suffer what I did :(.
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Very much noted, and with thanks for your kindness. I have started halving the 50 mg pills, of which I have a reasonable supply for a slow taper, and I notice absolutely no w/d still. I think I picked the right time and am doing it the right way. I do not want to be a slave to psych meds forever, and now that my depression has largely alleviated (simply due to life improvements) I see no need to keep going with it as an antidepressant. I can certainly see taking it for occasional knee aches (old injury, mildly arthritic) or menstrual cramps (mainly) but that's on an as-need basis.

I'm interested as hell in Tianeptine as both an anxiolytic and antidepressant, but that is another thread entirely.

I would not elect to try any opiate analogues at this point, after someone I cared for deeply died as a result of a fentanyl analogue. I believe the lab, not the human body, is the place to attempt to titrate safe doses.
 
nuke said:
In provoking seizures.

Ki for human mu opioid receptors (nM)

Tramadol (racemate): 17,000
Tramadol (+): 15,700
Tramadol (-): 28 800
O-Desmethyltramadol (racemate): 3190
O-Desmethyltramadol (+): 153
O-Desmethyltramadol (-): 9680
Morphine: 7.1

Less is more, as these are the required concentrations to displace a known substrate.

Lai J, Ma SW, Porreca F, Raffa RB. Tramadol, M1 metabolite and enantiomer affinities for cloned human opioid receptors expressed in transfected HN9.10 neuroblastoma cells. European Journal of Pharmacology. 1996 Dec 5;316(2-3):369-72.

And, with this inclusion of this substance in their catalogue, I would wager mucho that this place will not be around much longer.
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agreed
 
so what is the best method of taking it?
is 10mg a good starting dose?

is it ok to take while on Mirrtazapine?
 
Work it up. Start with 1mg and double your dose until you find activity, maybe trialling it every other day.
 
I remember Haribo1 talking about this a couple years ago. I believe he mentioned dosage in the thread. I can't seem to find it, yet.
 
Swerz said:
I remember Haribo1 talking about this a couple years ago. I believe he mentioned dosage in the thread. I can't seem to find it, yet.
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please, post the link if you find it.
If there are no reports by saturday I think I'll be giving it a try anyway.
 
Wait, I found it:

http://www.bluelight.ru/vb/showthread.php?t=305427&highlight=tramadol

http://www.bluelight.ru/vb/showthread.php?t=289848&highlight=tramadol

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!
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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.
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haribo though is not the best source for reliable infos...
 
I tried M1 today, sniffed two little lines, no more than 10mg total , very nice subtle opiate effect.
Woot! First one to try it!
 
^^^Give updates regarding duration, etc...

Did it cause pupillary constriction?
 
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