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I Like to Draw Pictures of Random Molecules

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(1R,2R)-2-[(dimethylamino)methyl]-1-(3-hydroxyphenyl)cyclohexyl propanoate

Would this act as a pro-drug for desmethyl-Tramadol?
 
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Yikes! (MPTP = indirect neurotoxin FYI - though you probably all know)

Oh no wait in this case it wouldn't be neurotoxic right? Since the cyclohexene can't be metabolized into a methylpyridinium containing MPP+ analogue since it is not a tetrahydropyridine, correct?

Soo esterifying the phenol moiety ("phenolyl" ??) instead would be the way to go for yielding in vivo M1 and possibly circumventing the iffy profile of tramadol itself?
 
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Oh no wait in this case it wouldn't be neurotoxic right? Since the cyclohexene can't be metabolized into a methylpyridinium containing MPP+ analogue since it is not a tetrahydropyridine, correct?
Click to expand...

It looks that way, yes. It still doesn't bode well for thermal stability of the compound.

I think desmethyl tramadol is already pretty good as a drug wrt pharmacokinetics.
 
Here's a picture of ToluenylPiperazine, or TNP.
nqabzc.png

Here's a picture of Neo-2C-D.
x5t6yo.png

The molecules will get ridiculous!
Here's WTH-19.
1238l12.png

Here's WTH-20.
34qll6f.png

Here's WTH-MD21.
b9glxw.png

Here's ZXS-BZ-14.
20g1daf.png

Here's ZXT-BZ-14.
2cymex0.png

Here's Super Fluorenol. This is just in case regular fluorenol causes sleepiness instead of wakefullness.
2zq5rg1.png
 
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The Neo-2C-D may be an interesting idea, I don't know if hooking up a beta oxy to the amine in PEAs works - maybe we should look at the efficacy of RMDMA (Thread here) to get an indication of that, especially if the N-desmethyl version of that would exist.

The ZXT's look potentially carcinogenic / teratogenic / mutagenic to me - polycyclic aromatics like that may intercalate between DNA grooves...

Some eugeroics like modafinil may indeed have paradoxical effects and cause sleepiness. Apparently consistently in rare individuals and incidentally in others (I've felt it at least once), not sure how that happens and how it can be avoided by modding structure and activity. :)

I'm interested in heterocyclic simply substituted PEA-like stimulants like the concept behind MPA. I also wonder about cycloheptatriene amph analogues for example. The cyclobutadienes like WTH-20, that is not stable is it? Antiaromatic..

Here's some phantasies of my own (#1-#5), I must admit I really wonder about the MET-type azetidine (#5)!! Never mind the chloro, bromo or if there are alkyl antlers, do you think it makes sense? Is it protected from MAO while potentially losing little of the specific DMT / MET character?
edit: Although the constitutional isomer pyrollidine tryptamine (Pyr-T) is apparently unpleasant if you refer to TiHKAL.


randomideas1_named.jpg
 
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I'd be really interested in bioassaying the azetidide MET homologue. That could really hold some promise I think. I would also be interested in sampling mescaline-piperidine, but I am inclined to believe that activity may be lost, given the comparison with 2C-B-BZP. Still, it is different enough to at least warrant exploration, although perhaps with a more potent substitution than the 3,4,5-trimethoxy pattern. GOOD ONES SOLIPSIS!!

For those interested in messing with the fluorene derivatives, you might want to have a look at these:

http://en.m.wikipedia.org/wiki/2-Acetylaminofluorene

http://www.ncbi.nlm.nih.gov/m/pubmed/8397005/

It seems that with very simple substitutions to the base fluorene moiety, it is possible to produce powerfully mutagenic compounds. This is not to say that such things will occur with other substitutions, and it seems to be related to substitutions at the 2- position, but still, it would be VERY wise to tread lightly indeed...
 
Oops, yikes apparently this has been thought of before:

Read in this thread here... http://www.bluelight.org/vb/threads/298517-Indolethyl-dimethylazetidine

Still, I wonder if the constrained DPT analogue (indolethyl '2,4-diethylazetidine) or the DET analogue (indolethyl '2,4-dimethylazetidine) could help elucidate which way the N-alkyl substitution antlers point best for binding - as was the whole point of designing LSZ...
Or even the trialkyl (vicinal)?

And yeah those look nasty, Seensofar!
 
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nj754 said:
Methylenedioxymichaeljackson (mdmj):

mdmj.gif


(methylenedioxypropofol)

I like the md-buckyball. That would have quite a bit of ring strain, though.
Click to expand...

I agree with all of this, although I would be curious to see how the methylenedioxy group would affect such a GABA agonist...atypical...almost reminiscent of the 'mdAi' meets propofol. Now, what if there were an amine were the phenolic hydroxyl group goes??
 
What about phenmetrazine analogues, I mean, Jesus, morpholine @ benzyl position...I think phenmetrazine is the preferrable phenethylamine-like structure from which to do analogues...
 
Cool molecules solipsis. Very MAO resistant it looks like.
In reply to the greenlighter with the m-eth question. the answer is probably DMAA.
Here's a list of fictional fluorenol prodrugs.
Fluorenol Modified D.
34illzk.png

Fluorenol Modified DO, or Stiminsomfinil.
4qn5me.png

Here's Fluorenol Modified DO2.
qx5kpg.png

Fladrafinil, based on Adrafinil.
10zpgeh.png

Last one, Flodafinil. based on Modafinil.
ztyety.png
 
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