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Stimulants of the Future

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morninggloryseed said:
4-MAR is 4-Methyl-Aminorex. What do you mean "plain MAR"? Do you mean Aminorex without the para-methyl?

With that in mind, there can be no such thing as "pFMAR" as aminorex can either have an para-alkyl or a para-fluoro...but it can't have both. I assume you mean 4-fluoro-aminorex.
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Sorry, not thinking, para-fluoro amino rex.
 
morninggloryseed said:
4-MAR is 4-Methyl-Aminorex. What do you mean "plain MAR"? Do you mean Aminorex without the para-methyl?

With that in mind, there can be no such thing as "pFMAR" as aminorex can either have an para-alkyl or a para-fluoro...but it can't have both. I assume you mean 4-fluoro-aminorex.
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The 4-methyl is on the oxazoline ring, not the phenyl. 4-Methylaminorex is the compound also known as U4EA. So there could welll be a 4'-methyl on tge phenyl ring. This would then be 4,4'-dimethylaminorex. The para-flouro compound would then be 4'-fluoro-4-methylaminorex.
 
haribo1 said:
I know this sounds dumb, but I REALLY enjoyed 4MAR but plain MAR is supposed to be about 4 times more potent. The strongest of the series (ED50) was the 4-fluoro. Now, I know 4-F amphetamine isn't quite as speedy but a bit more happy. Wouldn't pFMAR be worth giving the once over? That or possibly a pseudohalogen?
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I know somebody who synthed para-fluoro-4-MAR & he said the first time it had entactogen like properties, but subsequent doses just became unpleasantly stimulating (more psychosis & less fun), so all in all I don't think it's be worth the bother


Now you need to reduce the ketone to the alcohol, prepare the acetate, separate the isomers, and you get the well known stimulant levophacetoperane, which is sort of the reverse ester of methylphenidate.
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No, just leave it as the keto group - if you reduce the ket group of pyrovalerone you don't retain the dopamine reuptake properties, so it's probably be best to leave the keto group untouched here as well
 
fastandbulbous said:
I know somebody who synthed para-fluoro-4-MAR & he said the first time it had entactogen like properties, but subsequent doses just became unpleasantly stimulating (more psychosis & less fun), so all in all I don't think it's be worth the bother
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Fwiw, people who rave about entactogenic properties tend to dislike straight-up stimulants... so what this person said may not be valid for those of us who DO enjoy "plain stimulation." In other words, it may be worth the bother.
 
^ No he's the same one who synthed a series of alpha-amino alkanones & had a liking for plain out & out stimulants as well (he really rated 1-phenyl--2-(N-methylamino)-1-butanone and ended up consuming quite a bit of the stuff) - he said that it simply wasn't too pleasant after the initial experience with it. Strangely he never got around to synthing the methylenedioxy analogue of 4-MAR, which I had a feeling would have been a definite entactogen considering all the aminorex derivatives are effctively N-methyl derivatives, with the methyl group also attached to the beta-substituted oxygen, which also tend to retain entactogen activity (a la methylone).

As regards pure stimulants, I was always under the impression that the meta-fluoro substituted compounds were the best of the bunch, not the para-substituted (ie that 3-fluoroamphetamine is a much better stimulant than 4-fluoroamphetamine). I may be wrong though (my memory has bloody big holes in it due to moments of excessive drug intake - not quite Swiss cheese, but not watertight either! =D)
 
1-phenyl-2-(N-methylamino) butane

F&B. I know a Dutch chap who made the 1-phenyl-2-(N-methylamino) butane & optically purified it. He also made methamphetamine & optically purified that. He reckoned that the butane analog was BETTER than the propane version. His explanation was that it crossed the BBB better (or something). It's a shame because he was a 'problem user' i.e. he suffered mental illness due to excessive stimulant abuse. He truly believed that there was a worldwide conspiricy against him and EVERYONE was involved. He said he was still friends with me because he thought I was a 5th columnist of the 'company' who had a soft spot for him and was putting in good words to keep him out of trouble. I flipped. I figured if/when something bad happened, he would believe I had let him down or worse, grassed him up!
Anyway, back to the plot. What does that 1-one do to the binding? I was told by people that methcathinone was inferior to methamphetamine but methylone is very similar indeed to MDMA but what about things like MDPV (or 3,4 dichloro PV for that matter). Are the amines as well as the amino ketones active? If the butanones are active, then while MBDB is controlled, 3,4 methylenedioxy 5 methoxy WOULD be legal in the UK AFAIK? I quite liked it when I tried the 3 carbon primary version.
 
Yeah, I know someone who produced a whole series of alkanone derivatives and his favourite was 1-phenyl-2-methylamino-1-butanone. I think it's that it has a small amount of noradrenergic activity coupled with a lot of dopaminergic activity, which seems to be the right combination for maximum euphoric effects
 
I was told by people that methcathinone was inferior to methamphetamine but methylone is very similar indeed to MDMA
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Methcathinone is definitely very inferior to methamphetamine. In fact, it downright sucks (in my experience).
 
fastandbulbous said:
Yeah, I know someone who produced a whole series of alkanone derivatives and his favourite was 1-phenyl-2-methylamino-1-butanone. I think it's that it has a small amount of noradrenergic activity coupled with a lot of dopaminergic activity, which seems to be the right combination for maximum euphoric effects
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Of this series which stereochemical configuration about the alpha-alkyl corresponds to the more active enantiomer? Do they happen to follow the configurational rules for amphetamine (even though they probably don't share a similar mechanism)?
 
hussness said:
Of this series which stereochemical configuration about the alpha-alkyl corresponds to the more active enantiomer? Do they happen to follow the configurational rules for amphetamine (even though they probably don't share a similar mechanism)?
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That is a VERY good point. What isomer of MBDV was more active? This 1-one thing is becoming more and more fascinating. I always assumed that ring-substitution was required to make the PEAs dopamagenic but it seems not. That would certainly be interesting from a CsA POV. It LOOKS like one drug but ACTS like another. Like FSDoA pointed out about bemigride; looks like a barb but its a stim, not a downer...In fact, has anyone considered bemigride analogs?

imgsrv.fcgi


And this, I believe, is the strongest substitution pattern for a barb

s4_1_19.gif


Maybe its worth trying? I do suspect its a general CNS stimulant so nothing 'nice' but who can say...
 
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In fact, has anyone considered bemigride analogs?

http://pubchem.ncbi.nlm.nih.gov/imag....fcgi?cid=2310

And this, I believe, is the strongest substitution pattern for a barb



Maybe its worth trying? I do suspect its a general CNS stimulant so nothing 'nice' but who can say...
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Like a general CNS convulsant trigger - that's especially true of drugs based on the barbiturate structure
 
Going further with the SARs of cathinone analogs does annulation of the nitrogen (like with MDPV) really do anything significant to alter the properties of the drug?
 
Well there's a German patent for it as an appetite supressant (somewhere in Chemical Abstracts - don't ask I can't remember) and it's a better stimulant than diethylpropion, with less side effects, but beyond that there's nothing that major to recommend it - with the beta ketones the CNS stimulant activity incresaes with chain length, reaching a max with the hexanone derivatives then tailing off quite sharply
 
Dondante said:
How about a muscarinic agonist like arecoline?
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Arecoline mostly just makes you sweat, you get a little bit wired but its more like nicotine than anything else. Tried both fresh betel nuts and concentrated extract, the extract is stronger but they both taste nasty and don't do that much.

Strangely enough though betel is one of the most widely used drugs in the world on a population basis, literally hundreds of millions of people in south east asia chew betel nuts every day, but you hardly even hear about it in western countries. I guess arecoline must be fairly addictive when its used regularly but in my experience there wasn't really any high to speak of.
 
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