• N&PD Moderators: Skorpio | thegreenhand

I Like to Draw Pictures of Random Molecules

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The first one 4-benzylpiperidine is an oddball, it sometimes gets 'good' when you take the dose up almost feels like the mao kicks in and theres too much DA. Its a weird one cause its 5 carbons away unlike most good stimulants there's always that PEA/amp pattern of benzene ring 3 carbons to the Nitrogen. I read somewhere (maybe here, don't remember if its reliable) that you could replace the N in ritalin with an O and it would be nearly the same. Wonder if you can do it with amphetamines?

Its been my dream to come up with a molecule that acts like ethylamphetamine but isn't. Maybe not exact but close enough.

In the last pic i meant "ethyl to hide the hydrogen" (could be methyl etc)


I was on some random chemical research site in the USA and they had 3-CF3-amphetamine for sale... what would happen? 3FA with one fluoro is pretty strong at dopamine release (feels like it). There's a high demand for a 2FA/2FMA substitute, I wonder what swapping for a Chlorine or Bromine might do.. make it less active there (there by making it more like standard amphetamine?)
 
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hard to say what happens... the carbonyl seems very sterically hindered which may slow down metabolism.
 
Are all endogenous ligands in the brain basically 'designed' to not pass the BBB? I mean: are there endogenous brain neurotransmitters known that could be active when administered, is the BBB made to transport some compounds unilaterally or would you never find any such administerable drug because it would leak out of the brain if it could also get in there / or get metabolized really quickly before it could get anywhere?

I don't think so much designed to 'not pass BBB' as just naturally respect the format as endogenous. For example, a lot of exogenous chemicals from plants serve to poison or otherwise dissuade animal predators, and are more of BBB crossing as an attack at the foreign target.
 
Most of these benzos are pretty obvious, but should all be active and probably enjoyable for people who like them, first some that are likely to have sane potencies:

n-methyl clonazepam - people like clonazepam and n-methyl 1,4 classical benzos are usually considered better than the desmethyl versions, potency should be a bit higher than clonazepam but still not insane like clonazolam

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n-methyl nifoxipam - this one has already been made and tested (it's in the same patent as nifoxipam), apparently it's stronger than flunitrazepam (so the potency is approaching the insane side but hey..) but has a higher ld50....

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the nitro analog of midazolam - should be pretty awesome, midazolam is already very well liked and replacing Cl with a nitro group tends to make things even better..... not sure about potency, oral midazolam has pretty low bioavailability and is thus relatively weak, the iv version however is a completely different ballgame, could likely work as a nasal spray which should be close to iv without any needles

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flualprazolam - a stronger and more hypnotic xanax, what is there more to say.... oh and since norflurazepam is a thing it should be a relatively straight forward synth (if you like working with dangerous chemicals anyway)

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None of these are anything spectacularly innovative but since they are all so close to well liked pharma benzos with small modifications to make them more enjoyable and/or potent they should all be good.
 
Few more

al-lah - a lysergamide allowed by the Koran, should probably be active too

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tfm-lad - probably a bitch to make, wonder if it's active

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2f-eth-lad - another bitch to make

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n-methyl clopremazepam - some more weirder benzos

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lol

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- Give me some of that new spice, I don't want any goddamn old spice
- Stop talking

ah 1992, the day people started extracting their own spice at home guided by subliminal messaging
 
lol

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- Give me some of that new spice, I don't want any goddamn old spice
- Stop talking

ah 1992, the day people started extracting their own spice at home guided by subliminal messaging

....and who said Columbus wasn't looking for new drugs?
 
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break the C-N bond, merge the pyrrolidine ring, replace the methylenedioxyphenyl by an indole, add a fluoro at the 7-position of the indole.. you get this:

uBp2aLm.png

Maniacamine! Now this compound is about 2000x more euforik than cocain! according to this patent .. guess that would be the LSD of stims.. would need blotter! .. Amazing!


edit: actually it is ONLY 200x .. here the SAR on this class
 
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Was it checked for being a MAOI or do those tend to be more analogous to releasers?
 
Yeah..It is a weak MAOI relative to MA activity: IC50 MAOI > 150x higher than IC50 for MAT so more likely no significant MAO inhibition within MAT doses range.

Releaser more pvpcoke-like than AMPH about 100x more potent than its congener pvp as SDNRA. But unlike pvp, it is not selective NDRA but SNDRA so it is more like a cross between mdma and pvp or coke! All the class regardless of the aryl as long as it is 2 or 3 -pyrrolidinyl..unlike pvp where all the congeners are pretty much all selective NDRA..Quite interesting!
 
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and replace it be a C.. you get this molecule: It is extremely potent NDMArA about 30x more potent than K as NMDAr antagonist (Ki 3HTCP binding = 27nM v Ket Ki = 860nm) according to this patent here. It doesn't look like any schedule dissociative at least the structure or can it be seen like ring restricted K analog or something?..but anyhow, it looks it might have an unbelievably long half life (>10 h???) considering there is no obvious "metabolizable" functional group to chew esaily by metabolic enzymes..But who knows?

WP article I just made for your bringing to my attention the above N-methylhexahydrofluorenamine
 
shhhttt! @Nag...That is a trade secret :!...just kidding!!! Actually, this and related compounds are from the Tricyclic class of NMDAr antagonists. They're pretty different from the arylcyclohexylamines, the adamantanes , the morphinans or the dipheylethylamines class of dissociatives NMDAr antagonists Maybe when you have time, you should create a separate WP entry for those if you're interested since they're pretty distinct class of NMDAr antagonists. More SAR data can be added later.

Here is the paper and reference on that particular compound with more NMDAr data on the whole series of related structures (the patent reference + the pubmed on WP). The most active compound discovered was the cis isomer ie cis-N-methylhexahydrofluorenamine with IC50 0.009uM almost 100x ketamnie. Maybe you should use that one on the WP page you setup and link up to the paper for analogs since it is the most optimized among the group.

Now having said that, this compound is insanely potent dissociative. It is in the range of the ridiculously potent NMDAr antagonist Dizocilpine aka MK-801, the standard NMDArA used to induce experimental full-blown schizophrenic dissociatives psychosis in lab rats!!..with doses in humans of 1mg or less (insane)!! But at this doses, there're is probably no aminergic ie no stim activity like with K, dck or 3meopcp..etc.. just pure dissociative!.
 
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for some reason, images I post on imgur.com dont show up here... Am I doing some wrong on that website imgur? may be they dont allow pic of "drugggg" molecules??
 
Imgur allows everything (legal-ish), you must have deleted it yourself. 50% of their traffic is hardcore porn, molecules are nothing lol

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doxdoxylamine
 
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