• N&PD Moderators: Skorpio | thegreenhand

Stimulants of the Future III

I stuck to insuffusion after being told that 1 x 25mg was about 1 x 5mg dexedrine. It's a little difficult to compare exactly because the physical is mostly absent & I enjoyed just sitting & being. My mind was going a mile a minute but it didn't seem to cause any locomotor stimulation.

For harm-reduction reasons I cannot really recommend injecting materials. I suppose plugging is a pretty efficient route for many compounds - just not pretty ;)

Of course, always start low! I was young and foolish and took advice off some 'Northern Soul' boys who had been serious fans of the stuff. Plus of course, the stuff was 25 years + old so I imagine it had lost at least SOME of it's potency (N-oxide formation?).
 
n-ethylation follows a drop in potency but in general doesn't seem to lessen the effects overall.

See MDMA -> MDEA

just a wild guess on the basis of two other chemicals with a similar structure and probably a similar mode of action
 
I seem to remember that the ED50 for ethylamphetamine was quite a bit higher than that of both amphetamine & methamphetamine. Potency is somewhere between the two others so it's probably a good choice. The best example I can think of right now is that the N-methyl analog of fencamfamine has an ED50 1/2 that OF fecamfamine.
 
Phenmetrazine is a lot nicer than amphetamine, but you need relatively a larger dose. It's a lot smoother and there isn't as much of a crash at the end of it. I obtained a dozen 25mg tablets from a 1960s prescription. We are going back 20 years here, so it's a little hazy, but it WAS better than dexedrine.

G-130 has the advantage of being more potent but the huge disadvantage of lasting such a long time. I think that tests revealed significant amounts of the material in test animals 72 hours later.

Bethedrone, ay. Well, N-ethyl seems a lot less toxic than N-methyl for the PEAs and many related classes (Fencamfamine, for example!). Maybe the law has actually made the market a bit safer? For some reason I thought that the mephedrone class had all been outlawed (although, TBH, I've not read the wording - anyone got a link?).

What about 4-methyl- phenmetrazine? I have a chemist offering me this stuff at the moment, but I don't know what its effects will be and I don't know if it is legal in the UK?
 
Serotonin-norepinephrine releasing agent, probably very low dopamine activity.

Out of curiosity... I have taken biochem and ochem1/2.

How can you tell by look at the structure that it will be a 5HT/NE releasing agent? We never learned this in class
 
because it's basically mephedrone with an ethyl in place of an N-methyl. not going to change it much, and you can probably assume it follows as the same path as N-methyl to N-ethyl amphetamine.
 
What about 4-methyl- phenmetrazine? I have a chemist offering me this stuff at the moment, but I don't know what its effects will be and I don't know if it is legal in the UK?

Well, looking at the MoDA it appears that it is legal. Phenmetrazine itself is class B drug and none of the class B 'catch all' paragraphs apply. I don't think the term 'structurally derived from phenylethylamine' in the class A 'catch all' would be applicable (the law was thinking of ring-substituted amphetamines) but I would doubt it. Mephedrone didn't fit, so it seems.

As for activity? Well it's very likely to be similar to phenmetrazine but with decreased duration & potency. p-TAP was very MDMA-like it seems, but mephedrone is much more like (meth)amphetamine. Structurally it's somewhere in between. Phenmetrazine itself is about 1/5 the potency of dexamphetamine although there are some relatives that appear stronger.

If your substituting for stimulant activity, a meta -CH3 will work, if your looking for increased serotonin activity then para -CH3 will most likely be better. In either case the body has an extra path to emimination.

Nobody has ever made it AFAIK, although it seems an obvious one to look into. Didn't F&B study this class of compound for his pHd? If anyone could make a prediction, he would be the one person...
 
if I didn't know already, the writing makes it obvious now. Can't stay away for long, huh?
 
Out of curiosity... I have taken biochem and ochem1/2.

How can you tell by look at the structure that it will be a 5HT/NE releasing agent? We never learned this in class

Analogy to related compounds. N-ethyls seem to decrease dopamine activity, as the N-ethyl compounds are generally less stimulating and less toxic than the N-methyls.
 
Guise run a search in this forum (but not for "bethedrone; that name is relatively recent and won't catch on). There has been prior speculation about...and tasting of... this compound.

ebola
 
I just wish that they could get away from the PEA structure entirely. Is it because people see that skeleton & in some way trust it?
 
Another very interesting long lasting potent stimulant which was first mentioned by Shulgin is 5-(2-Aminopropyl)indole aka 5-IT.
5-IT_structure.png

As Shulgin wrote:
5-(2-aminopropyl)indole or 5-IT, which, at 20 milligrams orally, is a long-lived stimulant producing increased heart-rate, anorexia, diuresis, and slight hyperthermia for about twelve hours.

Unfortunately very little information can be found about this compound.
 
I have spent quite a bit of time pondering in recent months over analogs related to sibutramine and pyrovalerone. In particular:

1. Changing the aromatic substituents
2. Changing the length of the alkyl chains
3 Swapping the pyrrolidine ring for a dimethylamine substituent.

My mood for the exact compound changes from time to time.
 
I didn't think that any other aromatic was useful for the Sibutramine class, not sure about the Pyrovalerone class. What about something a little bit further afield? If only the 5HT-2b activity could be reduced in aminorex, 4MAR was one of the only stimulants I ever enjoyed. It felt like a very smooth cross-over between MDMA & dexedrine. 25mg was too subtle, 50mg was just about perfect (as long as you have 12 hours to enjoy it).

Just a thought, anyway, I'm sure your reading an awful lot.

Of course, something totally non PEA would be the most interesting, but then again possible most risky in practice.
 
Look further afield! Why not something like N,N-diethyl-6-phenyltetrahydro-2H-pyran-2-amine or N,N-diethyl-2-phenyltetrahydro-2H-pyran-4-amine? Both of these align very well with cocaine and fit the pharmacophore model I put together, and matches those published (not that there's any real difference- it's not hard to visualize how how they all align).

N-ethyl-N-((2-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)methyl)ethanamine might be another one worth looking into, but my money is still on the first two.

I have a handful of others more removed from those two that look good, but those two are my personal picks.
 
Well, I admit I'm fascinated but won't those pyrans be a little complex from a synthetic POV? What is the predicted pKa of these two?
 
I was thinking some of the compounds Rothman utilized. 4-FA, 3-FA, 4-MeA, 3-MeA as well as PAL-287.

If any RC suppliers are reading this post, please add those compounds to your inventory.

Ive seen compounds such as 3,4-dimethylmethcathinone for sale recently. That's not what I want though.
 
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