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Entactogens/Entheogens of the Future.

How about...

abxcdeaxv1.png


Where R = any of these...
1) hydrogen
2) methyl
3) ethyl
4) phenyl

Same as amino indans / tetralins?
 
MattPsy said:
They've been tested by Nichols, terrible affinity IIRC.
Click to expand...

for SERT? I can understand the crap affinity for 5-HT2a, as all N-sub's seem to be, but remember this is a thread about entactogens.
 
Oh; not for SERT, sorry. Forgot which thread I was replying to, that'll teach me for having a screen's worth of tabs open :P .
Hmm, might be too sterically bulky to fit anyway.
Those cyclized structures (like MDAI) don't have significant DA/NE activity anyway, so even if it did fit SERT well, you'd need a coadministration of of dopamegenic drug to make it empathogenic and so worthwhile.
 
6 membered vs 5 membered N-alfa mono-N cyclo HCs.

5 membered thought to be significantly more likely than not to be more potent than 6 membered where 6 membered =s 3,4-MDO-Ph-1-CH2-(2)-piperidine and 5 membered version is 3,4-MDO-Ph-1-CH2-(2)-pyrrolidine.

Former active *(anonymous personal communication).
Later > or = to 95 % yes active IMO.
See also nicotine, conitine.

Des-[3,4-MDO]-6 known active (published).
Des-[3,4-MDO]-5 unknown.

Pampa.
Dream Operator.
 
MattPsy said:
Oh; not for SERT, sorry. Forgot which thread I was replying to, that'll teach me for having a screen's worth of tabs open :P .
Hmm, might be too sterically bulky to fit anyway.
Those cyclized structures (like MDAI) don't have significant DA/NE activity anyway, so even if it did fit SERT well, you'd need a coadministration of of dopamegenic drug to make it empathogenic and so worthwhile.
Click to expand...

you might be right about DA/NE transporter activity, but from a quick look at wikipedia, there are dopamine agonists with the cycloheptane structure attached to the benzene ring (see: SKF 38393, SKF 82958 and Fenoldopam).

notornotFMAN said:
5 membered thought to be significantly more likely than not to be more potent than 6 membered where 6 membered =s 3,4-MDO-Ph-1-CH2-(2)-piperidine and 5 membered version is 3,4-MDO-Ph-1-CH2-(2)-pyrrolidine.

Former active *(anonymous personal communication).
Later > or = to 95 % yes active IMO.
See also nicotine, conitine.

Des-[3,4-MDO]-6 known active (published).
Des-[3,4-MDO]-5 unknown.

Pampa.
Dream Operator.
Click to expand...

Is this a contribution to the discussion between me and mattpsy? If so, I haven't a clue what your talking about (with all the percentages etc.). If not, then nevermind this message. =D
 
No - he's discussing benzyl-(saturated ring) empathogens, like R-benzylpiperidine and R-benzylpyrrolidine. He is saying that the pyrrolidine is likely to be of higher activity.
So no, he's not contributing to our discussion.

Interesting bigmac - i'll think about this some more when I have time - I have uni now - back later :) .
 
MattPsy said:
No - he's discussing benzyl-(saturated ring) empathogens, like R-benzylpiperidine and R-benzylpyrrolidine. He is saying that the pyrrolidine is likely to be of higher activity.
So no, he's not contributing to our discussion.

Interesting bigmac - i'll think about this some more when I have time - I have uni now - back later :) .
Click to expand...

to be precise he is not contributing anything worthwhile to any discussion.
 
I was just wondering what the differences wuld b between substitutions @the 3 position rather than the 4, it seems the 4 has been thuroughly tested 4the most part but the only reference i hav for the 3 is fenfluramine appearantly it also metabolizes into m-C-Amp and p-C-Amp?
 
toxide said:
I was just wondering what the differences wuld b between substitutions @the 3 position rather than the 4, it seems the 4 has been thuroughly tested 4the most part but the only reference i hav for the 3 is fenfluramine appearantly it also metabolizes into m-C-Amp and p-C-Amp?
Click to expand...

fenfluramine metabolises into m-trifluoroamphetamine and m-trifluoromethylhippuric acid. the 3-position is similar to the 4 position in activity but as far as i can understand less potent, at least in terms of neurotoxicity. the most effective configuration is usually 3,4-diwhatever as far as halogen containing compounds. halogens in these positions on simple amphetamines seem to cause neurotoxicity, and with the cardiac fibrosis caused by fenfluramine, are probably nothing to fuck around with (peripheral 5HT2b agonists + CNS stimulantion = not good apparently!)

m-chloro-n-tert-butyl-cathinone (wellbutrin, bupropion) is an impotent NDRI. here's a neat paper about that and mCA: http://www.geocities.com/borg_aw/studies/FDALetter32001.htm
 
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