• N&PD Moderators: Skorpio | thegreenhand

  • Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

Stimulants of the Future III

Anyway, as a personal interest of mine, alpha-cyclohexyl-PEA's
Click to expand...

That's funny, I've also been thinking about alpha-cyclohexyl-PEA:s. Didn't know any of them were actually tested though. That's real interesting.

I'd also be interested if there's any made/tested with other rings in place of the cyclohexane, such as cyclopentane, tetrahydrofuran or tetrahydrothiophene. Tetrahydrofuran is already in zylofuramine but it lacks any n-substitution.
 
dread said:
Tetrahydrofuran is already in zylofuramine but it lacks any n-substitution.
Click to expand...

As long as the 'it' is zylofuramine, it contains an n-ethyl, which was found to be the most potent substitution.
 
Just to possibly clarify, there do seem to be multiple binding sites or at least configurations in DAT and NET. Look at competitive binding assays with nisoxetine vs. methylphenidate and cocaine. In some trials methylphenidate will displace nisoxetine but cocaine will not.
 
Hi, sorry for ungraving and old thread but I wanted to share a 3D optimized image about to isomers of 'Ampheracetam' (and old idea gotten by looking at carphedon in this post) in the hope of getting some opionions on which would be the more active enatiomer out of the 2 (there are arctually 4 but I've put the methyl in the dextro position since it's a cliche' for increased amphetamine activity.

The interesting thing about this compund is that it would be metabolized into methylphenibut possibly giving it GABAergic properties as well throughout it's metabolism.

amheracetam.png


Any guesses?
 
Last edited:
/navarone/ said:
The interesting thing about this compund is that it would be metabolized into methylphenibut possibly giving it GABAergic properties as well throughout it's metabolism.

amheracetam.png


Any guesses?
Click to expand...

Well I certainly doubt methylphenibut is a stimulant. This could potentially be a bad combo (a racetam and phenibut derivative). I combined phenibut and piracetam once and ended up with my first and only ever migraine. Light sensitivity, pounding headache, nausea, vomiting... not fun.
 
Funny, as phenylpiracetam(Carphedon) hydrolyses into phennibut and it is considered a potent nootropic with some stimulatory effect.

Sorry for your side effects.

EDIT:
BTW you missed the fact that the primary compound has an amphetamine structure hybridized with a racetam.
It is not a prodrug but it's major metabolite is methylphenibut which is a GABA analogue with nootropic, tranquillizing, and antistress properties (don't know if the methyl interfears with this, it might as well enhancee phenibut's efects, who knows).

Phenibut has also ben proven to stimulate dopamine receptors, I guess the alpha d-methyl might act as a potentiatior.

Do you get the picture?
 
Last edited:
I wonder, if one would methylate the carboxyl & amine of baclofen, would it be a DRI?
 
dread said:
I wonder, if one would methylate the carboxyl & amine of baclofen, would it be a DRI?
Click to expand...

I have my uncertainties on that...
Anyway it will be metabolized into it's parent compound rather quickly.
Baclofen has no DA NE 5-HT activity..only GABAb agonist effects.
 
I believe Redline energy drinks are a good long term investment.

Nothing that Shiva says should be interpreted as likely, credible, or possibly even true.
 
A substance that caught my interest was beta-keto-benzyl(2)piperazine, probably a more potent analogue of Methylphenidate.
 
Hammilton said:
Were you high when you wrote this? Of course they do. In fact, they're one of the more important aspects related to potency. Other factors are BBB penetrability and rate of metabolism, but binding affinity is inextricably linked to potency.
Click to expand...

Maybe what was meant is that there's a difference between affinity and efficacy, and that recent evidence has shown that receptor conformation in binding may have more importance than affinity for binding. To explain some mysteries in why high affinity structures are not as reinforcing as others with less that bind differently.
 
That would be a sick substitution pattern to add to tryptamine (ie, N,N-dicyclobutyltryptamine).
 
I know, tertiary amines don't get along with stimulants
Click to expand...

Sure they do. MDPV, most tropanes, lefetamine...

the structure looks primising
Click to expand...

How? I don't see how this structure fits any known SAR... (known to me, that is) So, what exactly makes it promising, in your opinion?


hmm, now that I look at it, it resembles aminotetralin a bit... and it is a phenethylamine, of course... but the rest don't make much sense to me... a fluorine and an amide on the phenyl ring? wut?
 
^ They're like those chromanamines, etc. Also a few anti depressants. Where is the reference?
 
You must log in or register to reply here.
Top