RCs The AH-7921 (Ah7921) Megathread (v1)

[Bupe20mg]

Im not interested in its recreational value just its analgesic value. I am on 20mg norspan but nowhere near strong enougnh and they wont put me up. so I buy as many subutex and suboxone tabs and films as possible. cant get enough to store away. I break/cut it up for breakthrough pain and thats every day. use extra 4-6mg a day. I dont take any other opioids/opiates ofcourse due to both bupe and noloxone. the noloxone works jusy as well for me as subutex and its about 1/2 the price. got 15 more subutex 8mg coming I will be using up the suboxone starting with the strips first then tabs before I switch back to tabs.
many people on Transdermal Buprenorphine doing this for break though pain ans Australia doesn't alowe this in the subutex 200ug sub tabs as some countries do. got a 70ug/h ultram on its way I was going to try this once and they get them all the time if they do. any idea's

Australia

 

[Aleph]

The worst of the AH-7921 is not their utility for pain is that it produces dysphoria and hallucinations in a suspiciously similar to many agonists kappa.
See for example the resemblance of this molecule and Spiradoline

 

[mydrugbuddy]

The worst of the AH-7921 is not their utility for pain is that it produces dysphoria and hallucinations in a suspiciously similar to many agonists kappa.
See for example the resemblance of this molecule and Spiradoline

Ive had a few anxiety attacks from it. About once evry ten days of taking it. I thought maybe id got some cannabinoids mixed up into it, but judging from Aleph, it can just give bad effects occasionally. A simillar thing happens to me with speed, usually i feel on top of the world, but occasionally i can be plunged into the foulest of moods. Its all very mysterious.

 

[THCified]

Dunno what your guys problems are with this?

It's a damn functional opioid with zero side-effects when used properly. I've never taken it 10 days straight, just as i wouldn't take any other compound. When i take AH 7921, it always offers a decent long-lasting buzz without making me too distracted to do whatever's on that specific days schedule.

That said, after taking some beloved MXE yesterday, i took a buzz off of just 25mgs via sublingual route It's a shame this isn't available via prescription.

 

[Poelster]

What would your normal dose be?

 

[THCified]

It varies, but i've never gone above 100mgs (in staggered doses).

 

[QUARE]

I dont know for you guys, but for me AH-7921 cause serious skin eruption and rash, mainly in the face and little in the back. I also get some invulontary movement while withdrawal. The withdrawal is real pain too, like potent opioids.

Another weird thing that happen with that chemical, is that when I take it before going to sleep. When I wake up, half of my hands are completly numb like if I would have sit on it for a while and no blood where able to go to the hands. What is really weird is that HALF of the hand is numb. I take Quetiapine (Seroquel) for sleep, meaby it is cause by the mix, I dont know, but I was scared the first few time it happened.

 

[knock]

I dont know for you guys, but for me AH-7921 cause serious skin eruption and rash, mainly in the face and little in the back. I also get some invulontary movement while withdrawal. The withdrawal is real pain too, like potent opioids.

It can certainly produce a strongish histamine release, I took some two days ago and spent most of yesterday scratching away. And agree the wds can be unpleasant.

Another weird thing that happen with that chemical, is that when I take it before going to sleep. When I wake up, half of my hands are completly numb like if I would have sit on it for a while and no blood where able to go to the hands. What is really weird is that HALF of the hand is numb. I take Quetiapine (Seroquel) for sleep, meaby it is cause by the mix, I dont know, but I was scared the first few time it happened.

If your little and ring finger are numb but your other fingers are OK then it's probably a compressed ulnar nerve. It's happened to me before. I mentioned this to my doctor and they told me that drunks used to get it all the time because of the wooden seats in drinking establishments, they would get drunk, pass out and sit/slouch in one position on these hard seats and get pinched nerves.

If it is this, then it's because you're falling asleep in a bad position, and not moving in your sleep.

edit: It's not an issue once or twice but a damaged ulnar nerve can leave you with serious problems.

 

[sekio]

knock, how long would you say a 200mg dose lasts for?

Back of the napkin calculations based on LogD lead me to suggest, maybe 4-6 hours? Half an hour to an hour oral onset?

NSFW:

LogD@pH 7.4 (Chemspider predicted fat solubility, larger=more fat soluble=longer duration)
Clonazepam = 2.5 (8hours+)
Methadone = 2.2 (roughly ~8-12 hours)
Levorphanol = 1.7 (~6-8 hours)
Pethidine = 1.6 (2-4 hours, metabolically labile ester)
AH = 1.5
Oxycodone = 1.2 (~4 hours)
Morphine = 0 (~3 hours)

And, does this little doodle look right?

The claim of "80% potency of p.o. morphine" actually means that it's only ~27% as strong (orally) as an equivalent IV dose. So with oxycodone at "1.5x morphine" and 90% BA, worst case... it's only 17% as potent as oral oxycodone, by weight

At least on paper. I'd like to be corrected. Given a 5 kg rhesus monkey and the quoted dose of 14mg/kg for pain control, that's a reasonable dose of 70mg oral AH per monkey. (If one naively assumes that the same figure applies to a 60kg human, one would need a whopping 850mg of AH for pain control. Seems a little... much.)
If we assume monkeys and humans share similar responses to equal doses of opioids instead, doses between 50 and 250 mg then seem about right for a back-of-the-napkin calculation. (fudge factor of 0.7x to 3.5x)

 

[knock]

A lot longer than that! I took 250mg at 11pm on Tuesday and was still feeling it on Wednesday evening. This stuff last for hours and hours. Stuff I have anyway. In me! Oral onset is about 45 minutes when consumed in water solution. I've been in the habit of dosing with a gelcap but that can take a couple of hours to get started Think the gelcaps I have stick in my gullet.

And yeah I would say that there is analgesia at 250mg. I don't (consciously) take it for pain control, but I have cervical spondylosis that can be painful and it doesn't bother me much on 250mg of AH.

 

[DickTate]

I dont know for you guys, but for me AH-7921 cause serious skin eruption and rash, mainly in the face and little in the back.

That is interesting since I too had a lot more skin irritations, small pimples etc but no rashes. Mainly in the mouth sorrounding area.
I always wondered if it was due to the AH I took back in the days.

Another reason for me to stay abstinent I guess^^

knock: I never had a big histamine reaction on doses between 50 and ~125mg sublingual.

€: So oral consumed AH-7921 has only a potency of ~0,17? Did I get that right?^^

 

[sekio]

oral consumed AH-7921 has only a potency of ~0,17? Did I get that right?

the freebase is about 17% as potent by weight relative to a dose of oral oxycodone HCl. (27% to IV morphine).

any idea about differences in bioavailibility? my gut sense tells me this is well absorbed orally. the patent specifies both oral and parenteral (IV/IM) doses between 5 and 500 mg.

i want to punch whoever wrote that.

 

[DickTate]

Oh thanks sekio. I didn't read that properly.
So its potency is about 0,27 which explains the relatively high doses needed via oral ingestion. Interesting.

Now I'd really like to know the BA for the sublingual ROA 8)

 

[sekio]

I don't think the BA of sublingual is any higher than that of oral; TBH - just that the onset is faster. But this is just based on anecodtes from the internet, I haven't actually seen anyone compare them.

 

[DickTate]

From my experience and comparison trials it is higher. But I only can estimate, maybe around 40%. And there is the undeterminable absorption factor of cause.
This stuff is generally weird. Not bad, but for me tolerance to the (limited) recreational effects occured pretty quick.
On the other side 75mg sublingual could hold me through 1 1/2 pretty pleasant days, so yeah

But it is an efficient painkiller and taper tool as well as a neat toy for those with little to no tolerance.

 

[JJ-180]

After only a few months regular use I broke out in weeping eczema round my eyes and my hands ended up looking like crocodile skin.The eczema cleared up during my w/d from it and despite (very)occasional use since, has not recurred.

 

[knock]

DickTate, does sublingual dosing not burn? I'd be very happy to use smaller doses as it would save money, but every ROA I've tried other than oral has caused extreme irritation. And when I've made a solution and drunk it, I've felt burning on my tongue.

 

[QUARE]

DickTate, does sublingual dosing not burn? I'd be very happy to use smaller doses as it would save money, but every ROA I've tried other than oral has caused extreme irritation. And when I've made a solution and drunk it, I've felt burning on my tongue.

I use this chemical insufflated, and it is very smooth, no burn at all and it gives me a much better effect then those of oral.
BUT,
The first batch a got from a vendor burned alot it was like snorting capsaicain.

I dont know why but between the batch from the first vendor and the one I get from the vendor I use now is very different in that matter. The first one burned really bad and that one is very smooth, no burn at all.

 

[knock]

Hmm. And some people report difficulty dissolving while I have no problem. Would salt/freebase explain this?

 

[sekio]

Yes, that's exactly what's happening. Unfortunately it seems there are not only a lot of vendors mislabeling the freebase as the HCl and vice versa, there seems to be quite a lot of confusion as to what exactly it means to be a "salt" or a "freebase".

The freebase is an alkaline compound which is totally insoluble in water, hot or cold, unless an equimolar amount of acid is added. Since it's basically insoluble in water (less than 0.5mg/ml when in 1:1 ethanol/water) you won't measure the pH of the compound; it will appear at 7 all the time because there's very little dissolving in the water.

Freebase is soluble at a few mg/ml in solvents like DMSO, ethanol. Probably THF, dichloromethane, chloroform, dioxane, maybe even ether too. Practically insoluble in water, soluble in acidic water (turns into a salt). You will probably be able to force some amount of AH into solution with very vigorous heating and stirring but what I'm trying to get at here is: don't try to dissolve the freebase in water, if you get it dissolved it won't stay that way for long.

The HCl salt is a slightly acidic compound produced by neutralising the alkaline free base. As knock pointed out, should be almost instantly soluble in water, and should stay that way. The pH of a solution of this should be much more tolerable, too - but it will eventually corrode metals and stuff like any salt would. Don't store it in a steel spoon overnight.

People reporting problems dissolving the compound in water and "this burns on insufflation", "this tastes corrosive", "can't get it to stay dissolved" etc... you probably have the freebase. For your own good stop putting it on your rather sensitive mucous membranes. (Not that the salts won't burn either - they will be a hell of a lot smoother) And also, don't inject it!!

See, for instance comparisons of amphetamine sulphate (a white, crystalline, water soluble, slightly acid powder) versus amphetamine freebase (a corrosive alkaline water-insoluble organic liquid that stinks like piss).

The usual methods exist for turning one compoud to the other.

Salt --> Freebase.
Dissolve salt in water, add some sodium carbonate (as a solution, preferably) to raise the pH to about 10-11, and then filter off the freebase that's crashed out.

Freebase --> Salt.
Dissolve the freebase in a solvent of choice (probably dichloromethane, chloroform.. somethin polar but aprotic - hexanes, etc won't work very well cuz ah freebase has shit solubility) and add a solution of e.g. citric acid also dissolved in a solvent, or gas with HCl, or add HCl in solution and recover the water layer with your HCl salt dissolved in it and evaporate to dryness.

You can also just boil the shit out of the freebase in a solution of e.g. vinegar, or 1% HCl. Eventually it will all dissolve, then just evaporate the water off.

Oh, the HCl to Freebase conversion rate for AH7921 is 0.90.