• N&PD Moderators: Skorpio | thegreenhand

  • Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

I Like to Draw Pictures of Random Molecules

Status
Not open for further replies.
^ Quite unusual that this only has the N atom corresponding to the indole nitrogen... I tried to think of an ibogaine/harmala kind of derivative but you obviously can't build that from this compound.
 
Pawhuskin A is a cool compound, non-nitrogenous kappa receptor (mainly) blocker.

1574091111428.png

You could probably use that as an addition to a non-selective opioid agonist like the akuamma alkaloids, which bind more to kappa than mu receptors and therefore aren't very euphoric by themselves. Much like the "blue velvet" mixture of pentazocine and an antihistamine (I guess that mixture works because the sedative antihistamine potentiates only the mu agonist effect and not the kappa).

Edit: someone with any level of actual physical dependence to opioids probably shouldn't try balancing like that, tho...
 
Last edited:
Etifoxine/Flualprazolam hybrid
 

Attachments

  • e.png
    e.png
    22.7 KB · Views: 1
The 4-amino version of methylphenidate is significantly more potent than MPH itself, but can't know if it has aniline-like toxicity...

17784

The SwissTargetPrediction also gives it a slim chance of binding to mu receptor.

If someone were to make a non-amine MPH with the piperidine nitrogen removed or replaced with oxygen, it would be easier to purify if it had an amino group on the benzene ring.

Edit1: Also, making it a 4-aminoethylphenidate gives it a little bit more likelihood of binding to mu receptor, similar to meperidine SAR.

Edit2: And, by reducing the shit out of antibiotic chloramphenicol, you could obtain an equivalent 4-amino version of amphetamine.
 
Last edited:
The essential oil of aniba canelilla tree is unusual in containing a nitro compound, 1-nitro-2-phenylethane... That could be used in producing alpha-benzylphenethylamine, but unfortunately that compound doesn't seem to be an amphetamine-like stimulant.

www.sciencedirect.com

Pharmacological characterization of BNMPA (α-benzyl-N-methylphenethylamine), an impurity of illicit methamphetamine synthesis

α-Benzyl-N-methylphenethylamine (BNMPA), an impurity of illicit methamphetamine synthesis, has previously been reported to produce convulsions in mice…
www.sciencedirect.com www.sciencedirect.com

18404
 
A really dangerous idea:

make a quaternary ammonium compound from the antiglucocorticoid mifepristone, and take it as a peripheral glucocorticoid blocker with a huge dose of dexamethasone to get only the CNS effects of the latter.

20344

 
A compound that is both a kappa antagonist (Ki = 8.13 nM) and dopamine D2 and D3 agonist (Ki = 64.4 nM and 21.8 nM)... Maybe this could be some kind of an atypical antidepressant or ADHD medication. No chiral carbon atoms in there, so no confusion about the affinity of each isomer.


20851
 
3,4-dichloropemoline

21049

SwissTargetPrediction

www.swisstargetprediction.ch www.swisstargetprediction.ch

Nothing seems to be known about this. If its dosage in mg is like 10 times less that that of pemoline, it could have less liver toxicity, but that advantage disappears with stimulant tolerance.
 
polymath said:
The 4-amino version of methylphenidate is significantly more potent than MPH itself, but can't know if it has aniline-like toxicity...

View attachment 17784

The SwissTargetPrediction also gives it a slim chance of binding to mu receptor.

If someone were to make a non-amine MPH with the piperidine nitrogen removed or replaced with oxygen, it would be easier to purify if it had an amino group on the benzene ring.

Edit1: Also, making it a 4-aminoethylphenidate gives it a little bit more likelihood of binding to mu receptor, similar to meperidine SAR.

Edit2: And, by reducing the shit out of antibiotic chloramphenicol, you could obtain an equivalent 4-amino version of amphetamine.
Click to expand...

I've always mused about near methylphenidates that were also near fentanyls.

...

Wishing I had the specs to this one below, tried against the phenyltropanes.

Note the C1 position substitution, not a mistake, though maybe add a C2 position carbmethoxy
 

Attachments

  • mollynew.png
    mollynew.png
    4 KB · Views: 1
Last edited:
polymath said:
I drew some amine compounds like this in another thread:

View attachment 21584

It's a possible dopamine reuptake inhibitor and also looks a bit like fentanyl or meperidine, and a pharmacology app predicts it's a possible mu receptor ligand.
Click to expand...

Reminds me of Org 6582:

Org_6582.jpg


or Butyltolylquinuclidine:

Butyltolylquinuclidine.png


Really they all turn out to be Zoloft analogues, more or less.
 
No-one want to to comment on my "Hydrolicyclomethylamine" ??

**Got the nomenclature wrong in the first!**
 
ibuprofen-phenylephrine prodrug
(phenylephrine is garbage unfortunately)
PM3ZxRf.png


so why not
nrUhRiN.png

in the spirit of dibenzoylmorphine / dinicotinylmorphine, morphine di-acetylsalicylate aka morphine di-aspirinate
fix your headache "for real"
 
polymath said:
Those have a quite different connectivity, because the shortest distance between phenyl and nitrogen is only two carbon atoms. The compound in my post is more like 4-benzylpiperidine.
Click to expand...

Still reminds me of them. 4-BP is like a once lengthened phenmetrazine

P.S. would somebody direct me to a on phone free molecule renderer
 
Last edited:
Mo8rmQ0.png

Oxycodone 14-(3-phenylproprionate) is apparently some ~400x more potent than oxycodone, 14-pentanoyl 133x, 14-heptanoyl 200x, even the 14-acetyl is more potent by almost 10x.

Reading through Opiates by George Lenz... cool book.
 
Status
Not open for further replies.
Top