Buccinazine (AP-237) and it's derivatives (AP-238 & AP-239)

[Fertile]

Buccinazine has been around since the 1960s and is supposed to be about ⅓ the potency of morphine.

A quick search of the patents shows that the team behind buccinazine went on to develop azaprocin (x30 the potency of buccinazine). But they also discovered that a simple substitution increased the potency by a factor of 2.5 i.e. addition of a p-NO2 i.e.

1 hosted at ImgBB

Image 1 hosted in ImgBB

ibb.co

It seems an obvious development. But if you seek a novel scaffold:

1 hosted at ImgBB

Image 1 hosted in ImgBB

ibb.co

Now I have found the above as a fragment of more potent opioids but unlike the phenylpiperidines, phenylbenzamides or others - their is no obvious way to increase potency and/or duration.

 

[negrogesic]

2-methyl-AP237 was more enjoyable than AP238. It has a nice initial euphoric flash due to rapid onset (even when taken orally), but it fades quickly, leading to compulsive redosing. Because of this flash, the pull to redose is stronger than anything I've seen from an opioid. It's like the synthetic cathinone of opioids.

Which I suppose would be fine if it wasn't also so simultaneously toxic feeling and intensely caustic. Once I tried it sublingually and it pretty severely burned some of the skin under my tongue. So much so that parts of it turned white (reminiscent of when you leave concentrated lemon juice on a piece of salmon for a long time). Some of the little flappy bits of skin under my tongue ultimately ended up falling off. It hurt for days. Now just imagine introducing that into your nasal passages or rectrum. Or circulatory system.

AP238 was slower acting with a muted flash, yet just about as toxic feeling.

 

[Fertile]

AP-238 is in fact 2,6-dimethyl AP-237. It's LogP is higher so duration should be longer. As for caustic - that's purely down to the addition salt the makers chose to use... most likely the hydrochloride.

But as you see from the diagrams and work of Cignarella et al, a p-nitro (and shortening amide by 1 methylene) seems to increase potency by a factor of 2.5 so it wouldn't require much in the way of synthetic modification to produce something in the range of morphine in potency.

I've never tried buccinazine or it's derivatives. Is the toxicity limited to 2-methyl AP-237?

If you look at azaprocin you will see that it's just AP-238 with a bridge between the 2 & 6 methyl groups. I DO question the optical purity of 2-,ethyl AP-237 which might explain toxicity.

But the dimethylamino[iva[enone is worth exploring. As I said - it turns up as part of the scaffold of some more potent opioids - ones that have not really been explored because their synthesis is rather complex.

Actually, some of the viminol analogues look like reasonable candidates because it's simple to make the chiral amine thus you get a mixture of inactive (50$) and agonist x7 morphine (50%). The more complex Z4349 is way complex to make unless someone has a more practical method of resolving isomers.

 

[SpiralusSancti]

As for caustic - that's purely down to the addition salt the makers chose to use... most likely the hydrochloride.

Are you sure about it?

Some examples that make me wonder -

I tried multiple salts of amphetamine for example and they feel very similarly when snorted (for the nose), with slight difference in potency ofc and possibly slight difference in how fast they absorb/in BA. All in all it’s not that bad to snort any amph salt.

But 2c-b HBr or Hcl are both fucking painful to snort.

Or H, water soluble form or not it’s just fine, almost pleasant to snort it.

And than I remember MT-45 and can’t imagine there’s salt of that drug that is snortable, unless you are not a heavy masochist. That’s substance that feels like it’s pure proto bitter thing from platonic plane. Like fucking weird psychoactive capsaicin of bitterness. Hell of a caustic and toxic, weird stuff. Still less toxic than 2-methyl-AP237 I imagine, didn’t and would not try that one.

 

[Fertile]

I believe 2CB was particularly nasty to smoke because most salts of it's aren't very soluble. It's snorting something with very little water solubility that makes it so nasty.

I would guess the sulfate or phosphate would be the most obvious places to look.

I know this from experience because diphenidine was intended to be snorted but the chemists made the hydrochloride (because it was the cheapest and easiest) which wasn't too nice to snort. But the sulfate salt was very good for snorting - the difference was the solubility.

If you have ever wondered why some medicines come in the form or really unusual salts (like methaqualone edisylate) it was specifically to get around solubility and stability issues.

MT45 poses some interesting questions. Are both of those basic nitrogen atoms bound to an addition salt or only 1 of them (when produced in a makeshift lab)? If one of them isn't salted, it's going to be basic and very nasty to snort.

It is worth considering that some compounds really were only intended for oral administration. Not everything is faster and/or more active if snorted (especially true for compounds without a basic nitrogen).

I've known of crazy people who inject clonazepam and such madness... but not many of them seem to reach retirement age.

 

[SpiralusSancti]

Thanks for clarification.

Yeah when you put it like that, 2c-b gave me significant drip for such a small dose needed. I like it orally a lot more anyway but would be delight to try really snortable salt.

I’m wondering, and vaguely remember reading about how in reality drug absorption on nasal membrane depends on more factors than just how water soluble it is. Maybe depends on how lipophilic it is too?

As non-water soluble H works just fine nasally and I also know few persons how preferred snorting etizolam but that maybe says more about them than about how effective ROA it is.

And amph, sulphate, phosphate, di-phosphate and HCl were kinda more different in how fast they absorb than anything else. Salts of amph that hurt nose less, usually hurt for longer. O yeah, even base can be snorted. Yeah I know it’s oil but it can be both vaped (pure) and snorted (if stupidly mixed with enough caffeine, works as good but hurts more and longer than salts mentioned ofc) but is best prepared for oral consumption in freebase form.

 

[AlsoTapered]

How well it's absorbed is a solubility issue. I suppose if the LogP is particularly high (far end of RO5) then it might slow the whole thing down a little.

But the very first samples of U-47700 worked just fine whereas we has to play with U-93951 a little more because it's LogP was technically JUST outside the RO5.

 

[AlsoTapered]

BTW the p-NO2 derivative of A-238 is as strong as H.