• N&PD Moderators: Skorpio

Stimulants of the Future II

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so nothing is to come out of the acacia trees??
too much work? not worth it ?
 
Sure,

the FDA refused for 20 years to approve bupropion for sale in the US b/c of the aromatic chlorine on a cathinone issue, but during this time period bupropion was being widely used by Europeans.

Today Wellbutrin/Zyban is a blockbuster drug in the US too, and has been for years.

Hope that's the elaboration you were looking for.
I would like to see some evidence of this cited before I can agree fully with your claim.

Also consider sibutramine. Actually, thats only been around since 1997.
 
looks like a little more than that in those trees.....lol



Amines and alkaloids from A. berlandieri (ppm)

Phenethylamine 991.3 1390.0
N-Methylphenethylamine 1702.7 3742.2
N,N-Dimethylphenethylamine 99.1 604.4
N,N,N-Trimethyl-β-phenethylammonium hydroxide nd 23.6
Amphetamine 3.1 10.1
Methamphetamine 20.1 11.5
N,N-Dimethyl-α-methylphenethylamine 45.6 229.7
p-Hydroxyamphetamine 8.0 7.3
p-Methoxyamphetamine nd 35.7

Amines and alkaloids from A. rigidula (ppm)

Phenethylamine 872.3 1135.7
N-Methylphenethylamine 2314.6 5264.8
N,N-Dimethylphenethylamine 123.6 724.5
Amphetamine 6.7 11.8
Methamphetamine nd 12.4
N,N-Dimethyl-α-methylphenethylamine 57.6 394.2
p-Hydroxyamphetamine 2.1 6.9
p-Methoxyamphetamine nd 15.7
 
the two papers are in the bullshit category as far as I am concerned, unless of course someone credible replicates the results.
I understand the authors wouldn't discuss or defend the (somewhat surprising) results.

acacias as a genus usually contain tryptamines.

the list looks like the kind of crap one would find in a liner or old column in an analytical lab that had been doing forensic stuff.
 
:(

Its okay... there's lots of stuff out there thats less than credible. I still <3 you anyway, shith3ad.

But Vecktor is a smart dude... he's got an excellent BS sniffer.
 
one can hope...... iuf they can clone people.....they could make some sort of plant if it doesnt exist......who knows
 
Might phenylpiperidines become the new lefetamine? Nocaine is not far away from pethidine, in structure.

200px-Nocaine.png
200px-Pethidine.svg.png


I'm sure it wouldn't be impossible to develop a related chemical which would be both, a DRI with mu-agonism... or is this just wishful thinking...?
 
What would the holy grail stimulant be considered? A purely CNS experience with little to no PNS stimulation? I havent read much material that suggests many of these novel chemicals are as potent as pure D-amp or D-methamp (or as rewarding) with a similar or lower ratio of cns/pns stimulation.
 
You're not searching very hard, I guess. Amfonelic Acid looks as if it will fit the bill as it has very little pns effect and seems to be extremely selective for DA.


Speaking of which: I'm trying to find something, but I'm getting nowhere. Is anyone aware of any sort of SAR investigation into AFA and derivatives? It'd be interesting to see 7-benzyl-1-ethyl-1,4-dihydro-1,8-naphthyridine or even just 2-benzyl-5,8-dihydroquinoline. Or hell, just 2-benzylquinoline would be interesting.

I would be surprised if the first two didn't have some activity. It'd be interesting to know if the hydrogen binding of the carbonyl oxygens is necessary. Or even important. Since there's no such element in methylphenidate and the like, I would suspect not, but I've not seen any phenethylamine derivatives that have much beyond the amine besides small alkyl groups. Only the N-benzyl's, and that's still entirely different even.
 
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Yes, any info on amfonelic acid past what's already been posted here would be greatly appreciated!
 
Might phenylpiperidines become the new lefetamine? Nocaine is not far away from pethidine, in structure.

200px-Nocaine.png
200px-Pethidine.svg.png


I'm sure it wouldn't be impossible to develop a related chemical which would be both, a DRI with mu-agonism... or is this just wishful thinking...?


The one you're thinking of might be the prodine alalogue made using a tropinone ring rather than piperidine (3-phenyl-3-propionoxytropane) or it's pethedine/demerol reverse ester equivalent. Can't be bothered (off to folks for Dad's birthday in nex 5 mins) to find a pictorial representation of it's structure, but I'm sure someone will oblige - there generally a nice bunch in here! :D
 
Sibutramine is a good place to start thinking about what new analogs could be made.

Stuff like pyrovalerone is the mouse droppings but it isnt exactly "challenging" chemistry.

Think about the difference between phentermine and chlorphentermine.

It would be easy to switch stuff around assuming that the SAR is understood fully.

Even something as mild-mannered as changing the chlorine for a fluorine might be expected to work favorably?

How the fuck do they even construct the cyclobutane ring? Does that come from a beta-keto precursor?

Infact, if one wanted they could just make a ketal.
 
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Also consider tametraline is in no way regulated.

If anybody can get some info for this and sibutramine who has access to Scifinder etc?
 
How the fuck do they even construct the cyclobutane ring?

A gem of a book which covers this subject in great depth is

The Chemistry of Cyclobutanes Edited by ZVI RAPPOPORT The Hebrew University, Jerusalem
and JOEL F. LIEBMAN, The University of Maryland, Baltimore County

was available as a torrent at one stage.
 
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