N&PD Moderators: Skorpio
You should upgrade or use an alternative browser.Stimulants of the Future II
I would like to see some evidence of this cited before I can agree fully with your claim.
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.
Also consider sibutramine. Actually, thats only been around since 1997.
http://www.cognitiveliberty.org/shulgin/adsarchive/acacia.htm
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
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.LabRatNW
Bluelighter
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Its okay... there's lots of stuff out there thats less than credible. I still
you anyway, shith3ad.
But Vecktor is a smart dude... he's got an excellent BS sniffer.Nagelfar
Bluelight Crew
dread
Bluelighter
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...?Hammilton
Bluelighter
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.
http://www.chemograph.de/en/list2009.html
...
There's some interesting bioassays in hyperreal by user name Demonic. For example topic Naphthalenic pyrovalerone analogues.fastandbulbous
Bluelight Crew
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
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.phase_dancer
Bluelight Crew
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.