• N&PD Moderators: Skorpio | thegreenhand

dimethocaine, good dopamine reuptake inhibitor?

asecin

Bluelighter
Joined
Apr 13, 2005
Messages
1,725
it was accidental that i read about dimethocaine being second to cocaine in some similar action and it shocked me i havent heard of this for all those years trying to find coke alternative and it seems NOBODY TALKS ABOUT THIS hence why i didnt know for so long! googling it and checking this forum goes far back as 10 years ago and nothing new has come up. why is that?? can someone tell me why is this not more popular among people who enjoy cocaine???
 
It's nowhere near as potent as cocaine, and is reportedly worse for your heart, two good reasons there.
 
If you swap the p-amino for a (pseudo)halogen then you get something as potent as cocaine. The problem is the solubility. The idiots who introduced 'nitrocaine' made the hydrochloride which smokes like crack, but is so insoluble that snorting it is like snorting ground glass. The sulphate is somewhat more soluble but if someone does find a highly soluble addition salt, it is surprisingly like cocaine. I have used several analogues orally and it was very like oral cocaine. Much smoother than snorting or (god forbid) smoking it. I'm not sure it is absolutely safe but I've seen people smoke grams of nitrocaine in an evening.

The p-NO2 has the advantage that the body (generally an oxidative instrument) reduces the nitro to an amino so the LogP crashes and the body produces the gluconate that is removed by the kidneys. The p-NO2 wasn't covered by the seminal paper that covers (almost) all known CNS stimulants. The authors name eludes me but I think he is of Indian extraction. For those seeking to make a product identical to cocaine, the p-nitro benzoic acid ester of pseudotropine fits the bill. You need to make the dihydrogen monophosphate salt to provide solubility so that their is no 'burn' when snorted. It's local anesthetic qualities then ensure that further lines are OK.

But to put it into context. If you love cocaine then this scaffold has some very similar analogues. Even the hydrochloride melts at <120?C so you don't need to freebase it to smoke it. If you use the semi-rigid pseudotropine derivatives, you can certainly emulate cocaine. The only difference is a slightly slower onset and slightly longer duration. Now I hate cocaine but I have seen people fiend crack and that is a terrible affliction that damages not only the user but everyone else in their circle. This class of drug seems to being out the worst in people. When I say 'it's like cocaine', I mean 'it feels identically unpleasant' but others who tried the p-NO2 benzoic pseudotrophine ester did say it was like cocaine.

Be careful - the hERG activity of many of this class has not been researched and a death toll is not an acceptable way to trial a new compound. I have seen someone drop dead after snorting cocaine and no amount of effort could bring them back. We did all we could but as it turned out, the coroner noted both congestive heart failure & a previous medical showed that the victim suffered from pulmonary hypertension. I don't know if it was suicide, devil-may-care or ignorance but I think most people would take on board the fact that their drug of choice could strike them down at any moment.

That was in 1999 and it still haunts me.
 
"The p-NO2 has the advantage that the body (generally an oxidative instrument) reduces the nitro to an amino so the LogP crashes and the body produces the gluconate that is removed by the kidneys"

This makes it feel even more dangerous to me, this undergoes same pathway as those toxic "aromatic amines" metabolic pathway
 
I thought dimethocaine failed because it was a relatively weak DAT ligand in comparison to its sodium-channel blocking activity i.e. it's effectively like sniffing benzocaine.
 
That was my understanding as well. Remember reading it was like 25% the potency of cocaine, along with the heart dangers.
 
well, you can add heart medicine to the mix to prevent damage to the heart as long as it does have some good dopamine boost, i think it should be tried
 
I almost bought some when I saw how cheap it was. I could buy 20 grams for the price of 1 gram of real coke. But I decided against it. I would also be interested in hearing experiences though.
 
you can add heart medicine to the mix to prevent damage to the heart

I think the big issue is that dimethocaine is a much stronger sodium channel blocker (anesthetic) than dopamine reuptake inhibitor. Same issue as cocaine has, and also any local anesthetic - the sodium channel blockade if taken too far causes seizures and cardiac conduction issues. People have OD'd on lidocaine before and the Na blockade is why. And derivatives of procaine are used to modulate heart output.

And unfortunately there's no "heart medicine" to reverse excessive sodium channel blockade causing heart arrythmia. It's not fixable through beta blockers because it's not caused by excessive adrenergic stimulation; you're actually blocking the electrical circuitry of the heart.
 
If you swap the p-amino for a (pseudo)halogen then you get something as potent as cocaine. The problem is the solubility. The idiots who introduced 'nitrocaine' made the hydrochloride which smokes like crack, but is so insoluble that snorting it is like snorting ground glass. The sulphate is somewhat more soluble but if someone does find a highly soluble addition salt, it is surprisingly like cocaine. I have used several analogues orally and it was very like oral cocaine. Much smoother than snorting or (god forbid) smoking it. I'm not sure it is absolutely safe but I've seen people smoke grams of nitrocaine in an evening.

The p-NO2 has the advantage that the body (generally an oxidative instrument) reduces the nitro to an amino so the LogP crashes and the body produces the gluconate that is removed by the kidneys. The p-NO2 wasn't covered by the seminal paper that covers (almost) all known CNS stimulants. The authors name eludes me but I think he is of Indian extraction. For those seeking to make a product identical to cocaine, the p-nitro benzoic acid ester of pseudotropine fits the bill. You need to make the dihydrogen monophosphate salt to provide solubility so that their is no 'burn' when snorted. It's local anesthetic qualities then ensure that further lines are OK.

But to put it into context. If you love cocaine then this scaffold has some very similar analogues. Even the hydrochloride melts at <120?C so you don't need to freebase it to smoke it. If you use the semi-rigid pseudotropine derivatives, you can certainly emulate cocaine. The only difference is a slightly slower onset and slightly longer duration. Now I hate cocaine but I have seen people fiend crack and that is a terrible affliction that damages not only the user but everyone else in their circle. This class of drug seems to being out the worst in people. When I say 'it's like cocaine', I mean 'it feels identically unpleasant' but others who tried the p-NO2 benzoic pseudotrophine ester did say it was like cocaine.

Be careful - the hERG activity of many of this class has not been researched and a death toll is not an acceptable way to trial a new compound. I have seen someone drop dead after snorting cocaine and no amount of effort could bring them back. We did all we could but as it turned out, the coroner noted both congestive heart failure & a previous medical showed that the victim suffered from pulmonary hypertension. I don't know if it was suicide, devil-may-care or ignorance but I think most people would take on board the fact that their drug of choice could strike them down at any moment.

That was in 1999 and it still haunts me.

Sean, was it you who went on about the para-nitro descarbmethoxy phenyltropane as a simple and easy "synth" that emulates cocaine from colloquially attested 'testers'?

Anywho; taking away the local anesthetic, the phenyltropane class has the most therapeutic value as seen from how many have been synthed, the most potent appears to be:

183px-Davies_11f.svg.png


^DAT/SERT/NET
0.03 +- 0.01 / 0.23 +- 0.07/ 2.05 +- 0.9

different data set, but that's compared to cocaine with DAT @ 249 +- 37, and that's the best of the three MATs (smaller the number, better the affinity)

I am still interested in the allosteric modulation found in some coke-ish skeletons:

260px-3%E2%80%B2-methoxy-8-methyl-spiro%288-azabicyclo%283.2.1%29octane-3%2C5%E2%80%B2%284%E2%80%B2H%29-isoxazole.svg.png


tropanyl-Δ(2)-isoxazoline: interconverts the conformational state of MAT, selective for SERT (and a slight derivative does the same selectively with DAT) from the occluded position so that MAT re-uptake ligands will bind. Possibly a large factor of tolerance overcome there.
 
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well, im still curious to read about experiences with this stuff, beyond just people sharing their theory on how it works
 
Sean, was it you who went on about the para-nitro descarbmethoxy phenyltropane as a simple and easy "synth" that emulates cocaine from colloquially attested 'testers'?

Anywho; taking away the local anesthetic, the phenyltropane class has the most therapeutic value as seen from how many have been synthed, the most potent appears to be:

183px-Davies_11f.svg.png


^DAT/SERT/NET
0.03 +- 0.01 / 0.23 +- 0.07/ 2.05 +- 0.9

different data set, but that's compared to cocaine with DAT @ 249 +- 37, and that's the best of the three MATs (smaller the number, better the affinity)

I am still interested in the allosteric modulation found in some coke-ish skeletons:

260px-3%E2%80%B2-methoxy-8-methyl-spiro%288-azabicyclo%283.2.1%29octane-3%2C5%E2%80%B2%284%E2%80%B2H%29-isoxazole.svg.png


tropanyl-Δ(2)-isoxazoline: interconverts the conformational state of MAT, selective for SERT (and a slight derivative does the same selectively with DAT) from the occluded position so that MAT re-uptake ligands will bind. Possibly a large factor of tolerance overcome there.

No mate. I know who did, but it wasn't me. I have sampled the stuff I mentioned, but I didn't come up with the idea. Well, in fact the stuff is covered in that HUGE paper on classes of CNS stimulants so I suppose it would be simple. It would also be pretty expensive. The prices demanded were a piss-take and you know who shuttled between my costings and their demands. They were told to stop taking the piss. The 2-carbon aminoketones WAS a great idea and I can't take anything from him for coming up with that one but even in the hit and miss world of making 'euphoric' or 'relaxing' or 'weirding' the mind is as tricky as finding an antidepressant that works in man ;-) The very WORST miss was isophenidine i.e. the N-isopropyl analogue of diphenidine. The mono-substitution meant that it had more DRI activity and the isopropyl moiety conferred the highest NMDA affinity of the class. The sulphate salt was also soluble. That meant a snortable MXE-like compound. Do you know why it didn't turn up? They insisted that only thermal dehydration was possible. You tell me, I had the exact paper with a 1-pot RT synth and they ignored it... they had to build-in costs to up the price...

I guess the E-like, booze-like and suboptimal K-likes were the ones the cohort liked. I might add they weren't good enough to make the pyridinyl benzos: those were part of a previous project with some truly amazing chemists. Best instrumentation, best routes and anybody who keeps going until they find the 24th solvent system works are tenacious.

Still, that was then, this is now. The Eunoia disk is around if you ask - a full DVD of patents and papers all in directories and subdirectories. That was 2 years, 7 days a week, 12 hours a day using Reaxys. It's the full set. Every paper on every (recreational) psychoactive. Science has moved on so Belgium might be the place to look for new stuff (I hope that is sufficiently vague; 13 million people is quite vague).
 
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Isophenidine? That IS interesting. And just when there happens to be some diphenylacetic acid hanging around waiting for a use. This is the N-monoisopropyl substituted analog of diphenidine? thanks for that.

Edit-I would be REALLY really REALLY interested in isophenidine. Presumably it lacks opioidergic type effects as per lefetamine etc. given that it is a secondary rather than tert. amine? but still, anything you can tell me at all, chemical, biological, anything, I'd love to know. More DRI and the highest NMDAr antagonistic profile in the series of related analogs, that sounds like a real winner to me. And a 1-pot synthesis? very nice. I can't see why that would be passed up! diphenidine was lovely, as was MXP, although MXP had greater solubility, whilst for the likes of IM use it had literally to be boiled in a spoon/shot-cooking pan in about 5ml of water first, and then it'd dissolve. (in the case of diphenidine that is), which really is a big nonpolar greasy zit of a molecule, waxy almost and it is to dissolution in H2O what donald bloody trump and that slagchops stygian whore we brits unfortunately have for a prime monstrosity..ahem..minister... are to politics being conducted in as sensible a manner as a society which permits politicians whatsoever could be =D

MXP had the disadvantage though that with that there methyl ether present, that presented, unlike with diphenidine, a nice easy metabolic 'handle' for the body to latch on to, presumably hydroxylate and conjugate to glucuronide or sulfate in order to get rid of it, so it didn't have that lovely long duration of effect that diphenidine does. Never tried snorting diphenidine, I saw how nonpolar it obviously was, and thought better of it. Dosed either by dissolving in boiling water and IV/IM once it had cooled, or else liquefying it likewise and sticking it up my theresa may once it was of a tolerable heat for a trip up the chocolate starfish.

If you have any information you would share, I'd be immensely grateful to hear it, and if any of it needs to be PM'ed, then you know my username and where to find me :)

Out of interest were any other branched-chain analogs tested, like iso- or sec-butylphenidine, and how did, if tested, n-propylphenidine perform if known?

Oh man, this is just what I wanted to be finding out actually, right about now, diphenidine and lefetamine chemistry. So anything you could share, I'd be immensely grateful:)

LC.
 
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I don't know what to say. Anyone will tell you it's a 1-step RT synth BUT the trick was making it soluble. Yet another person had to mess around with that bit and voila, sulfate and the monophosphate don't burn much. It's pretty much identical to MXE. The affinity to mu receptors I don't know. You can reduce the T? and increase DRI activity by adding a p-Me onto the 2-benzene. That lone methyl is an easy target for the MAOs so rather than 3-4 hours it's more like 90-100 minutes. Onset faster than MXE but it's the DRI/NMDA ratio that gives the subjective experience so I would stick with the simpler one.

It's literally just ephenidine with an extra methyl on the amine moiety. The 1,2-DEA class is closer in QSAR to PCP than K. The 2-MeO did increase affinity but the 2-F was much better. Guess what? Too hard to make. Idiots. So, thinking as I type, the o-F with the 'p-Me would possibly keep the DRI/NMDA ratio the same while increasing potency and decreasing duration.

That was the 'problem' with diclazepam. People went for the shortest acting and thus most addictive derivatives. Diclazepam was a specific design as a 'methadone' for people who got themselves into trouble with the others. I know, it took 18 months to get down from 24mg/day to nothing. I did it and it wasn't too rough. I tried to think ahead. As Happy Brand says 'good business is not the most profit NOW, it is long-term trust and fair dealing'.
 
No mate. I know who did, but it wasn't me. I have sampled the stuff I mentioned, but I didn't come up with the idea.
By "went on about" I meant mentioned it here is all, friend. ;-j

(I hope that is sufficiently vague; 13 million people is quite vague).

Anybody not privy to those in the circles like you know: wouldn't know, and that's all that should matter. ;-)
 
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Maybe, I honesty don't remember so if I did, I do apologize. Those circles are tiny, but the cohort of people on this site was sizable. I didn't ask anyone. I'm of the opinion that the designer has to be the first into man. If it kills someone, it should be the designer. Others handed round the invitations to eunoiapharmacopia. I was against it - for certain things especially.
 
Do you mean burn as in on insufflation? or with respect to attempting vaporization and inhalational delivery, I.e physical pyrolysis?

Definitely will keep these in mind. Any papers on lefetamine analog SAR would be appreciated if you have any. I know more about PCP etc. SAR than I do about ket and its analogs, and little on lefetamine specifically. Although its not been one I've looked into deeply, its only by chance and of late that the diphenylacetic acid became available, 30g to play with though, and lefetamine itself has always been an intriguing drug, due to its triple-whammy of psychostimulant, NMDA antagonism and MOR opioidergic effects.

That sounds to me very much like a 'whats not to like' and 'potential winner' right there, with regards to lefetamine.
I've never tried it, not yet at least. But I have tried diphenidine and methoxphenidine, although not ephenidine and I LOVED both, diphenidine especially.

Also, DECREASING duration of effect? unless that expense is to be a cost paid for much improved subjective 'flavour' then why? why would anybody want to do that? I find short-acting dissociatives to be all the more compulsive redosers compared to something with a nice few hours at least (and something really long like very high dose IV memantine, now that hits the spot. i've always wanted to try MK-801, as well as a combination of MK-801 and a small amount of some sort of dopaminergic reuptake inhibitor just because MK-801 is so selective, but, on the whole, I don't think I've ever met an NMDA antagonist I didn't take to like a blowfly takes to a fresh, juicy steaming turd=D)

Do I like my NMDA antagonists? yes, yes I do. At recreational doses, one of my favourite classes of all drugs, especially with a little cannabinoid action added from whatever happens to be available; and at what one would probably call therapeutic dosing regimes, then NMDA antagonists seem somehow to 'normalize' something that was mis-configured in my original factory settings. And as an added subjective bonus, if this makes sense, then they almost....its as if they make me 'feel', subjectively speaking, 'more autistic' (I was born classically/kanner's autie. And I like it that way. I find the thought that I might not have been born that way nothing short of a nightmarish proposition if I'm quite honest. Doesn't mean I hate NT people, I don't. Well, not all NT people, and not BECAUSE they are NT, met plenty NT assholes, but thats on an individual basis, although some common factors do often occur as comorbids in their cases. Although I'm not one of the autistic supremacist types who thinks of ours as the 'master race'; not looking for a position as the first ReichsFuhrer of Autia. Although if the post came up for grabs, I'd take it to prevent others doing so because I'd probably do a better job and avoid as much butchery or/and deportations of NTs as humanly and humanely possible (yes, there are people who would at least split up families and deport the NT-born at age 18. I'm not, however, one of them)

NMDA antagonists though do definitely make me feel 'more' autistic. What some (NTs, naturally, the curebie ones in particular, would call 'severely', but I personally, prefer the term 'profoundly', because profound is what to experience being autistic is, in so many ways. There might be downsides, but for me, the upsides overrule those by a long shot, and a profound experience of life is exactly what I have been fortunate enough to be blessed with. I'd not give that away for love, nor money, nor the best damn analytical electronics for my lab that both put together could bring me. Not in a thousand lifetimes. I'd sooner die than wake up tomorrow and find I had been magically cursed to lose my being autie. I don't think I could live without it, having spent all my life with it. I'd not be ME anymore. And its deep, profound, all-encompassing, touching every aspect of life and beautiful:)

Curebies don't see that of course, they never will. I wish there could be a pill, a shot, depot implant etc. that could allow people to transition from NT to autie or to aspie according to preference for a given time, a week, a month, a year. I could really see such a pharmaceutical temporary cure for NT-ism selling like hot cakes and cold beer to a famine-beset third world country. And if it were something short acting, the fentanyl of autie/aspie-shots/pills/transdermal patches then that'd be like crack cocaine to a crackhead. Once an NT tried one, they'd be back pawning their shoes and possibly even their internal organs (not that one can PAWN an innard as such, thats more of a one-way transaction of course=D).....but they'd be back for more, mark my words, given a taste, the NTs would be back in such numbers begging for more that the pharm companies would need to have dedicated facilities for production of just the autism-transition pill, and begging for a permanent NT-ceptive for making sure their kids were too.

I know, I know, it isn't ever likely to happen. But a man can dream, can he not? and in this case of sharing something good with the world, not only the Scrooge McDuck-esque gold coin-filled swimming pools to roll around in and stim with some wall and ceiling mounted lights at the sparkly things.... That would just rock so much.. (and flap, spin, twist and bounce and twirl......=D)
 
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