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Stimulants of the Future III

ha !
by chance i ran into another student who actually could run the Pea-nBOMe through the 3D-QSAR with the GPCR modeling for the 5ht2a receptor.

it has very minor 5ht2a binding and is pretty lipofile.
but it cannot show how it reacts on other parts of central nervous systems...

conclusion (for now) :
we can't tell ....so probably not worth persueing
we'll have to wait for more receptor models.

kiss kiss

your ex.
 
Im hy guess the future best stims will be a mix of selective agonist antagonist drugs in order that dependin on the individual the different componets can be dosed at wish.

Or maybe even a miracle molucule that seems the general stream being a cool D2 and substype agonist while also having 5-HT1a agonism, 5-HT1b partial agonism, 2-HT2a agonism, 5-HT2b antagonism, 5-HT2c antagonism. 5-HT3 antagonist, probably some 5-HT7 activity and weaker adrenergic, NMDA and opioid activiy.

But this is just a far painted dream though possible with with a balanced dose all the new highly selective drugs being researched in laboratories.

Monoamine release seem to fishy for as do SRI's DARI's and generally TRI's.
 
Is NE receptor antagonism with DA transporter reuptake inhibition a possibility in one molecule if the 'discrimination ratio' for reinforcement and reward really is a NE to DA contrast? If so, such a mechanism of action would be my "stimulant of the future". Comments?
 
I think NA release is likely to be responsible for most, if not all, of the rush effect, as well as the 'tweakyness' and definately peripheral stimulation.

Going from my recent use of desoxypipradrol, which is a potent DARI, but as far as I know, not a releaser of NA, but a reuptake inhibitor, there are no signs at all of peripheral stimulation, other than than a slightly elevated heart rate (haven't taken my BP), even when plugged there is no rush whatsoever at the highest dose I have tried, 5mg (and I don't intend to take more than that, due to its long duration of action, and 5mg didn't really feel any better than 2)

Depending on the adrenoreceptor antagonised by such a hypothetical drug, it could be dangerous, if it were to be a beta-adrenoreceptor antagonist but remaining an agonist at alpha receptors that could cause, if were also to be a NA releaser, (or just have high affinity for alpha receptors regardless of releasing ability) dangerous degrees of vasoconstriction.

Antagonists at alpha2 adrenoreceptors are awful, anxiogenic, causing release of NA, as alpha2 is the autoreceptor and agonism there causes release of NA, and seem to cause akathisia. Would cause lots of peripheral stimulation, very unpleasant. Yohimbine is a good example of an alpha2 antagonist, and its definately not euphoric or to the best of my knowledge, reinforcing.

A DARI/alpha2 adrenoreceptor agonist on the other hand could be good, although I can't see the two coming together, don't know of any imidazoline-based DARIs, and all the alpha2 agonists I can think of, clonidine, tizanidine, lofexidine etc, are imidazoline-based. Can't think of any that are not, in fact.
 
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Recenetly got to try the N-methyl analogue of fencamfamine, like it's ethyl brother, it is devoid of peripheral activity and feels like an entirely central stimulant. No jaw grinding, dry mouth etc, just a lovely stimulation (sadly devoid of any sexual overtones, like MDPV; maybe that's a blessing though!) reminicent of amfonelic acid. Smoother than smooth stimulation, in the words of Homer Simpson "I give it 11 thumbs up"!
 
IS this one (fencamfamine analog) commercially available!!!!!!!!!!!!!!!
Sounds like a keeper. Hopefully somebody starts a thread, real soon
 
GBR 12935 is not recreational. I bought it and took 50mg orally. I will try amfonelic acid in a couple of weeks.
 
IIRC 3,4-dichloro-PVP was not marketed (instead they chose MDPV) because it was too potent. Personally, I think a-PVP is great.
 
Camfetamine was pretty good when I tried it, one of the better stimulants I have tried, by quite a long way.
 
According to Swedish news reports, police have detected a substance called N-ethyl-1-phenyl-2-butylamine in a (now withdrawn) sports supplement after a hospital visit by a user. Any thoughts? It is also speculated to contain N-Benzyl-2-Phenethylamine.
 
That's the alpha-ethyl analog of N-ethyl-amphetamine. Probably an OK stimulant, more NE than DA though.
N-benzyl-PEA is probably next to inactive though
 
N-ethyl-aephetamine? That might be interesting. Amphetamine is more NE than DA, so that's not very useful.

It's probably not as enjoyable as mephedrone, but I'd suspect it's still quite good. N-ethyl doesn't do a lot for potency, but it doesn't drop it down much, either. IIRC, Aephetamine was supposed to be fairly smooth if not very strong. The N-ethyl homologue is probably about the same. Perhaps more serotonergic, based on the increase of 5HT release from amp to methamp. don't know if it increases further from methamp to ethamp, but if it does, this might be pretty good, actually.

5, 4, 3, 2, 1.... counting down until someone says 3,4-Methylenedioxy-N-ethyl-Aephetamine! lol
 
AFAICT, going from a-methyl to a-ethyl increases affinity for NET and moves the cmpds closer to things like prolintane and away from amphetamine.
 
I'm curious what people think about dimethocaine with a fluorine or chlorine in the 4-position of the phenyl rather than the amine. If the SAR from the phenyltropanes applies then the compounds would have higher DAT affinity than dimethocaine proper, however 4-fluorococaine seems to have mysteriously high SERT activity which could apply to the dimethocaine analogs assuming they bind in a similar manner.

These compounds wouldn't be anything particularly difficult or expensive to prepare..
 
Fuck it: bring on the substituted aminorices and phenmetrazines. We could use an expansion in the palette of available monoamine releasers from substituted phenethylamines (and...I guess...BZP and propylhexedrine...eeeew).

ebola
 
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