• N&PD Moderators: Skorpio | thegreenhand

Post about novel RCs you would like to see on the scene.

Anything messing with NMDA receptors or possibly even AMPA ones as long as it's not overly toxic or turns you into a psychopath (as some AMPA antagonist anti-epileptic apparently is able to do) ...

More weird GABAergics a la pagoclone ...

Mixed dissociatives / psychedelics. Granted, you don't need them in one single molecule, I just want to finally experience these colorful visuals on a disso trip too.

Non-stimulant stimulants. Nootropics that work, etc. Sigmaergics.
 
Post about novel RCs you would like to see on the scene.
This is coming from a 100% "enduser" POV, not a big brained, lookit-me-and-how-clever-I-am one 😉 but, for those of us who've reached their "100 trip limit" with DXM, decades ago, and had whatever liver enzyme William White talked about (??WW's paper still respected??) that put us in the 33% that were psychopharmacologically able to benefit from this substance, as opposed to the 33 odd % that got ill and remainder who just experienced "typical, mediocre, under-the-counter drug high" without the 4+ hour dissociative state / 4th & 5th plateau / life-changing affects with incredible, speedy, after-the-hole comedown that was a 12 hour speed trip and slow, slow thing usually lasting 12+ hours depending what parachute you took (for me? O.E. & brown frown lol). Anyways, good times. And, all of that available any time day or night for about 15 dollars per God Tier 4 hour hole / most incredible Astral Projection / OOBE eva (as detailed above) down the street at your nearest grocery store. 24/7. Ahh, but those were different times. Anyways, did anyone figure out the liver magic or whatever behind the 100 trip limit with DXM and way around it? I've now waited 20 years...zero DXM use and even after all that time, no joy in the holing department when I've recently imbibed ye olde max strength cough gels. So sad. And so, to wrap up, a novel RC that I would like to see is a harmless little thingie with zero-to-little psychoactive activity itself (and so of no interest to the nosey, boring, backwards-facing feds) but that allows activation of other substances (like DXM and dissociative, which, by and large, are my favorite substances).
 
Too easy. Opioids are so dull.

First
Direct Stereospecific Synthesis of Unprotected N-H and N-Me Aziridines from Olefin

Science 03 Jan 2014:Vol. 343, Issue 6166, pp. 61-65
DOI: 10.1126/science.1245727
https://science.sciencemag.org/content/343/6166/61.full

There are many other ways to do this and newer variations of this specific reaction using for example different nitrene sources and there are other alkene aziridination methods.

then

Kumar, M., Gandhi, S., Singh Kalra, S., & Singh, V. K. (2008). Efficient Ring Opening of Aziridines with Carboxylic Acids. Synthetic Communications, 38(10), 1527–1532. doi:10.1080/00397910801928723

Without doing any real thinking there are 5 or 6 other ways to do this even starting from phenylcyclopentene. The key is to deal with the stereochemistry, as the amino is cis to the phenyl, which means the route needs to deal with possible racemization at the benzylic position. Which might require something more clever.


But why bother? You are totally correct about the people who could do this are simply not interested in doing it.

I have to say I am impressed, N-(2,4-Dinitrophenoxy)methanamine is obviously the compound to produce the N-methylaziridine as the patent states. I couldn't find much on the synthesis of this compound. It is presumably made from 2,4-dinitrophenol. Did you notice how the original paper doesn't QUITE explain how to make the nor compound? I even tracked down the guy whose name is on the patent.

Your note on stereospecificity. In the tramadol patents, the cis pair are removed using a zinc complex. The trans pair were transformed to the cis thermally.

You MAY like the effects of nortramadol (or indeed isonotramadol). As I mentioned, it is quite unique because it is stimulating at lower doses and rather trippy at higher doses. Some people on Land de Traume got hold of grams and gave pretty comprehensive reports. The cost of the precursors for nortramadol make it VERY expensive. I believe someone in China got hold of Tramadol (legal in that nation) and removed an -CH3 using Br as per tramadol patents.

The compound was quite a surprise to me. I provided some technical help to one guy who sent me a small sample in return.
 
O-(2,4-dinitrophenyl) Hydroxylamine is the actual droid you are looking for.It is not the most stable compound in the world. There are reagent equivalents which substitute for O-DNPH.
 
Hydroxylamine is way more dangerous. Plain vanilla hydroxylamine.

Potassium hydride is not a reducing agent, it is a strong base.

As clubcard correctly pointed out earlier those that have the skill and knowledge do this simply aren't interested.
 
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Potassium hydride is not a reducing agent, it is a strong base.

Metal hydrides tend to have an inflexible lattice, which makes H- transport difficult, so the researchers turned to oxyhydrides where oxygen and hydrogen share the same lattice sites. Another challenge is the high electron-donating properties of H-, which means that the electrons will dissociate from the H- to produce protons and electrons, giving rise to electron rather than hydride-ion transport. As a result the team sought a system containing cations that were more electron-donating than the H-.
 

Maybe someone already made this but I know the police have a specific acronym for isophenidine. Adding a p-Me to the 2-aryl increases the DRI activity making it almost identical to MXE in dose and action. I take nothing away from Kevin, MXE was his baby and he did a great job... but it was kind of hard to make and in the end I think that the Chinese ripped him off. To lose ones cat, life-partner and sanity in a 2 week period would upset any right thinking man. If one of my cats died, I don't know HOW I would deal with it, but drugs, certainlly.
 
Hydride acts as a strong base it is the conjugate base of hydrogen which is a very very weak acid.
 

Maybe someone already made this but I know the police have a specific acronym for isophenidine. Adding a p-Me to the 2-aryl increases the DRI activity making it almost identical to MXE in dose and action. I take nothing away from Kevin, MXE was his baby and he did a great job... but it was kind of hard to make and in the end I think that the Chinese ripped him off. To lose ones cat, life-partner and sanity in a 2 week period would upset any right thinking man. If one of my cats died, I don't know HOW I would deal with it, but drugs, certainlly.
you mean police or forensics? the police will have some dumb as fuck name like ippydippy or meow meow.
Forensics seem to use NPDPA for N-Isopropylphenidine.
 
Hydride acts as a strong base it is the conjugate base of hydrogen which is a very very weak acid.

Yeah, it can't exist in water solution because it reacts to form KOH and H2. Measuring a standard electrochemical potential for it would require dissolving it in liquid ammonia or something like that.
 
Oh I'd love to try isophenidine and nortramadol ...

Why the fuck is a substance that never has been marketed really on *legal* RC shops known in forensics?? Guess it can't be that deadly either, given it's a disso.
 
Well, diphenidine was part of a patent for NMDA rnatgonists. Kevin (FastandByulbous) came up with MXE but UK law controlled any arylcyclohexylamines so something new had to be tried. So diphenidine was first. Then some dicks tried to add an o-F or o-Cl but couldn't so added an o-OCH3 and it killed people.

Isophenidine was so very like MXE in terms of DRI and NMDA antagonism. That p-Me on the 2-aryl gives the body a convenient place to oxidize(so duration comes down) and increases the DRI activity. We tried the N-methyl, N-ethyl & pyrrolidine rings.We quickly worked out pyrophenidineis nigh on identical to pyrovalerone in effects and the N-isopropyl homologue of the series was way, way better. Now that was interesting because it showed that the series was more similar to PCP than to MXE.

But F&B did to an amazing job. I wasn't too keen on desoxyprpridrol because a speed-slized line lasted 3 days. I tried out the morpholine analogue which was smoother (more specifically DRI) but I never got to try out the thiomorpholine because I'm guessing that the S2+ could be oxidized thus lowering duration.

I seem to remember talking to Kevin and when he said he was going to invade Russia, I replied by saying I would invade Poland. I've never even VISITED Poland nor do I hold any negative views of it's people. The stuff just unbalanced you.

IF someone wanted to make $$$ then a 2:1 mix of p-Me aminorex : m-Me aminorex is like MDMA on steroids BUT you cannot get ring-closure using KOCN so it's BrCN or other mad materials.
 
Yeah these methylated aminorex derivates are gold... want to have 4,4'-dmar (14 days of low-dose XTC. Stopped voluntarily, not cause of side effects, and then my fucking ex flushed the rest...) again so bad and probably your mix might be even better ...

@polymath, guess I really under-estimated the amount of energy some people put into this subject ...
 
Yeah these methylated aminorex derivates are gold... want to have 4,4'-dmar (14 days of low-dose XTC. Stopped voluntarily, not cause of side effects, and then my fucking ex flushed the rest...) again so bad and probably your mix might be even better ...

@polymath, guess I really under-estimated the amount of energy some people put into this subject ...

I did ask Dr. Dave about the 4MAR series as compared to the AR series. He was concerned that the former may have MAOI activity which is 1 reason went with the synthetically less friendly ring-substituted aminorex. Those -CH3 groups give the body a convenient point to oxidize so duration was on par with MDMA.. I know who made the p,4-DMAR i.e. DR. Zee. I am not a fan. His furan analogues (benzo fury) are lifted from a patent and p,4-DMAR is purely an SRI so has little activity along. It is not exactly rocket science to know that p-Me amphetamines are SRIs whereas m-Me amphetamines are DRIs so the ONLY guess was the ratio.

Oh, and the 125mg dose unit was not arrived at because the tester knew of Shuldin's work. She just took increasing doses (of the 2:1) over successive weekends. I think she's a pretty good chemist but I am biased, I married her. Interesting to note that she was a bit of a fiend with the excess of m-Me aminorex.

We went through 3 itterations before arriving at pyrophenidone i.e. 1-(1,2-Diphenylethyl)pyrrolidine -->1,2-Diphenyl-2-(1-pyrrolidinyl)ethanone --> 2-phenyl-2-(pyrrolidin-1-yl)-1-(p-tolyl)ethanone

I'm not a big stim fan but she also likes coke and when I mentioned that some ladies find that coke (and indeed pyrophenidone) act as aphrodisiacs... so she hastily agreed and dragged me into our bedroom :)

I'm proud of her. In truth, it was her who worked out the 2:1 mix.... and the dose unit for pyrazolam. I asked for something around 5mg of diazepam and she went with 0.5mg. To be fair, it does seem to be a lot less sedating and dependence forming. I owe her a lot.
 
They're not exactly novel, but I'd love to give jimscaline, 2c-b-Ind and its 5-alkylated derivatives 2c-d-Ind, 2c-e-ind etc a go. I thought these would have made the rounds long ago...
 
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Like to see more experimental compounds on the market. Hell even the nootropic folks are more into experimenting than the RC vendors. Things like the sigmaergic PRE-084 (which I still couldn't sample, thanks rigid EU) or some compound hitting only a subunit of the NMDAr, which was investigated but thrown as a rapid acting antidepressant. Also the vendor threw it quickly again as it had no recreational potential.. guess it indeed was either too short acting or sth like a P-GP substrate but it had an interesting rush..

I don't refer to crazy experiments but more so things out of medical research which were thrown because of psychoactive side effects, of business decisions etc.. but of course contributions like mephedrone or MXE are welcome too :)

Oh, and I'd absolutely love to have a weak partial MAOI which could safely be combined with RI/RA. Would take a whole lot of their problems I guess, like transmitter depletion or rebound.

But in conclusion I think we'd have enough interesting things to research for a long time if they would just follow the UN's statement of the war on drugs being a catastrophal failure. These people are so stupid not to realize that banning well researched compounds will always lead to dangerous experiments (just look at countries w/o or w/ very strict opioid maintenance programs. Krokodil anyone?).

--

Other than that, dissociatives. Subunit selective, peripherally selective, etc.. guess they are still somewhat of the least explored and researched drug groups currently known as until very recently nobody's seen any therapeutical value other than anesthesia for which K is pretty good choice* and psychedelics which happened to have a bigger fangroup probably?

* strange enough that all the dissociative are anesthetics when K has some additional (channel blocking??) properties which in some papers were specified as being responsible for anesthesia ... for sure it'd be fascinating to abolish the memory inhibition of these compounds without increasing toxicity or interfering with the experience for example. Or as said before, things like different versions of memantine, e.g. one without or with less dopamine agonism.
 
Well, while I'm here, before I have to feed the kitties, I might as well put in my twopennethworth. 5-methoxy-6-(2-aminopropyl)-2,3-dihydrobenzofuran fulfills a lot of desirable qualities wanted for a phenethylamine psychedelic. The dihydrofuran ring is held planar, making it an ideal candidate for 5HT2a agonism. It also holds the two lone pair groups, on the oxygen atom rigid, meaning it has the property of making the SERT run in reverse (like entactogens). Where the furan ring connects to the benzene ring fulfills the requirement of a psychedelic to be hydrophobic, to fit into the pocket of said 5HT2a receptor. The 5-methoxy group allows for maximal activity at the 5HT2a receptor, by allowing appropriate changrs in electron density of the aromatic ring. Finally, the 2-aminopropyl (alphamethylethylamine) group prevents degredation of the amine function by MAO.
All in all, it's a combination of the MMDA-2/DOM molecule, which means it should be a much reduced stress version of DOM, by nature of it's entactogenic activity. I mean, isn't that what's needed? A wonderful psychedelic like DOM, but with the stress/fear reducing properties of MDA/MDMA like drugs (from experience, LSD & MDA is a very comfortable combo). From the profiles of MDA like drugs and of psychedelic amphetamines, it should be active in the 10-20mg range.

Right, have to go now, as the kitties are getting very insistant, for food!! :)
 
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