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Stimulants of the Future

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You can't find amphetamine in the USA, Canada, or Australia for a host of precursor supply, market demand, user preference, etc. reasons. You can't find methamphetamine in Europe for the same reasons.

P.S. if whoever reads this is an example of how I'm wrong, realize that you're in a tiny minority. I think getting clandestinely synthesized amphetamine outside of Europe is as easy as finding 4-methylaminorex.
 
Someone is looking closer into the class,note the year.To give an idea of dose,
"Pyrovalerone-HCl (I-HCl) [1147-62-2] in daily oral doses of 40-160 mg decreased the symptoms related to chronic fatigue in symptomatic human volunteers. "

1-(4-Methylphenyl)-2-pyrrolidin-1-ylpentan-1-one (Pyrovalerone) Analogs: A Promising Class of Monoamine Uptake Inhibitors. Meltzer, Peter C.; Butler, David; Deschamps, Jeffrey R.; Madras, Bertha K. Organix Inc., Woburn, MA, USA. Journal of Medicinal Chemistry (2006), 49(4), 1420-1432. Publisher: American Chemical Society, CODEN: JMCMAR ISSN: 0022-2623. Journal written in English. CAN 144:331200 AN 2006:83142 CAPLUS

Abstract

Dopamine, serotonin, and norepinephrine are essential for neurotransmission in the mammalian system. These three neurotransmitters have been the focus of considerable research because the modulation of their prodn. and their interaction at monoamine receptors has profound effects upon a multitude of pharmacol. outcomes. Our interest has focused on neurotransmitter reuptake mechanisms in a search for medications for cocaine abuse. Herein we describe the synthesis and biol. evaluation of an array of 2-aminopentanophenones. This array has yielded selective inhibitors of the dopamine and norepinephrine transporters with little effect upon serotonin trafficking. A subset of compds. had no significant affinity at 5HT1A, 5HT1B, 5HT1C, D1, D2, or D3 receptors. The lead compd., racemic 1-(4-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one, was resolved into its enantiomers and the S isomer was found to be the most biol. active enantiomer. Among the most potent of these DAT/NET selective compds. are the 1-(3,4-dichlorophenyl)- and the 1-naphthyl-2-pyrrolidin-1-ylpentan-1-one analogs.
 
C6H6 said:
There are many very potent dopamine/monoamine reuptake inhibitors which have no recreational value whatsoever. Mazindole and bupropion are good examples. And just because a compound has a stimulant effect in mice or rats doesn't mean it has recreational value. I've made quite a few compounds which are stimulants for rodents but are useless for humans. Finding good new stimulants isn't as simple as it might seem.
Click to expand...
I wonder what compounds he made? Bupropion is a bad example btw because it is weak.

Mazindol is potent though. However I also understand that it does have some positive effects even though it is not as strongly craved after as some of the more classical stimulants.
data.JPG
 
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hugo24 said:
Someone is looking closer into the class,note the year.To give an idea of dose,
"Pyrovalerone-HCl (I-HCl) [1147-62-2] in daily oral doses of 40-160 mg decreased the symptoms related to chronic fatigue in symptomatic human volunteers. "

1-(4-Methylphenyl)-2-pyrrolidin-1-ylpentan-1-one (Pyrovalerone) Analogs: A Promising Class of Monoamine Uptake Inhibitors. Meltzer, Peter C.; Butler, David; Deschamps, Jeffrey R.; Madras, Bertha K. Organix Inc., Woburn, MA, USA. Journal of Medicinal Chemistry (2006), 49(4), 1420-1432. Publisher: American Chemical Society, CODEN: JMCMAR ISSN: 0022-2623. Journal written in English. CAN 144:331200 AN 2006:83142
Click to expand...

interesting. this drug is already cheduled in canada (scheduled in 2003 with zolpidem and a few others)

has anyone thought about a methylenedioxy aminorex? seems like it'd be a good target.
 
i obviously know less than u guys but after reading pikhail i saw this veeeeery intrigueing substance.
I dont remember the name of it but it was a phenyethylamine and it had a few deuterium atoms attached to it instead of hydrogens.

Do u think that the introduction of deuterium or/and nitrogen isotopes could potentiate some of todays synthetic drugs, leading to a 'new' point of view on drugs?

deuterium is a rare isotope but it can easely be extracted from common water as heavy water (D2O).
 
I think isotopes of less abundance exhibit the same chemical reactivity, so I doubt it would potentiate anything. But they are useful for mechanistic studies.
 
Another Winner.

Sennokot is a laxative because ppl were discussion opiods under "Stimulants of the Future." Get it?

And while we're back on topic ("Stimulants of the Future"), may I also mention
Phenyl-ch2-(alpha)piperidine. Namely, des-(-COOMe)methylphenidate.
 
Well I couldn't find any articles on google for ANY of the compounds you've mentioned in any of your posts over the last few hours, want to quote some sources with some info on them?
 
The "piperidylamphetamin" is known,read some abstracts about it being a stimulant.But I would go for the pyrrolidino analog.

The des-COOMe phenidat looks interesting-has someone looked into it closer yet?I think it was mentioned in a thread before.
 
The sneat thing about this latter one [phenyl-ch2-(alpha)piperidine] is that it appears to be almost inert to bodily metabolism other than possibly
4-hydroxylation. And then there are the 3-chloro and the 3,4-methylenedioxy derivatives.
 
And the 3,4-dimethoxy and the 3,4-dichloro and the 4-methoxy and the
4-chloro and the 3-ethoxy and the 3-methoxy and the 4-ethoxy and the
4-propoxy and the 4-(n)-pentyl-2,5-dimethoxy derivatives....
 
hugo24 said:
The "piperidylamphetamin" is known,read some abstracts about it being a stimulant.But I would go for the pyrrolidino analog.

The des-COOMe phenidat looks interesting-has someone looked into it closer yet?I think it was mentioned in a thread before.
Click to expand...

Do you have any references for that? I couldn't find anything.
 
No, I thought of them (that is, the PMAPs) myself.

PhenylMethyleneAlphaPiperidenes.

I got the idea from Ritalin/methylphenidate.
 
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hiyall,

saw one of you speculating about 2-amino-tetralin and feel obligated to post
a warning story i heard from dear friend of mine:

it's absolutely vile stuff and should be avoided like the plague. yes the
rat studies look good, but no, humans are not rats and the data can not be
easily extrapolated.

my friends experimentation with this compound 8 years ago gave him a big life
lesson and he's lucky to still be here. now he's not so eager to test never
before been tried compounds. it's a fine line and i advise extreme caution
when working something up. some of my friends mishap was inexperienced
pilot error, after several days of ramping up slowly on seperate experiments,
he got impatient and boosted a double dose 3 hours after taking the first dose
(was getting slight effect from first dose and figured 3 hours was enough time
and should have peaked), then it all hit like a frieght train. very dysphoric,
nothing like amph, sedated, sick and wierd feeling, total agony. continued
accent and passed out completely unconscious at 4-5 hour point and came to
consciousness about 3-4 hours later completely surprized that he was still
alive. he was able to call friend for help at that point and seemed like was
leaving system slowly and was going to be OK. decided not to go to hospital to
avoid explaining situation and potential police inquiry.

friend took him to her
house and crashed in bed feeling sick and nauseous. some 6 hours later he
woke up middle of the night to go pee and on way into the bathroom passed
out completely (maybe due to low blood pressure) and did a face plant into
shower door slicing his face and severely breaking his nose. blood everywhere,
friend wakes up and sees him in pool of blood on the floor barely able to
maintain consciousness. was able to get bleeding stopped and then passed
out in bed from pain. awoke next morning in intense pain and found his nose
was on the wrong side of his face. required surgury, long recovery, etc. truly a
nightmare.

abandon hope all yee who enter here

sincerely,

purple heart
 
Well, thanks for the anecdote. That's interesting that it's so acutely toxic though; maybe mao inhibition?
 
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