• N&PD Moderators: Skorpio | thegreenhand

Ketamine salts solubility

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The next Foxy???
noname45.jpg
 
Anyone care to guess about the pharmacology and dosing of this MPMI derivative? It is available from multiple sources.

I would love to guinea pig this but it's expensive. I would expect a dose to be similar to MPMI but I cannot find dosing information for MPMI only 4-HO-MPMI and 5-MeO-MPMI. @AlsoTapered do you know anything about MPMI dosing?
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Like I say - paste the SMILES into PubChem and it will show you all similar compounds. If it's know, it's activity is given.
 
Likely facile and active. Likely more toxic than MDPV which I presume it closely mimics. If you know the general pathway to 'bath salts' then I'm sure you can see it's not complex. But p-halogenated seems to have been avoided by the people making 'bath salts'. So ask why?
 
They thought all halogenated Amphetamines and congeners were toxic, based on highly ambiguous diction in an early study, which claimed pCA wipes out the entire 5-HT system.

But I've Tried Some, And They Are Quite Active. Halogens deactive the benzene ring and were more likely to cause pupillary constriction, kinda like heroin, rather than dilation when I was being a willing Guinea pig.
 
Oh they are. But so is MDPV so it makes little difference.

The original medical product pyrovalerone is by far the best. VERY smooth indeed and that p-CH3 is a perfect sacrificial moiety. It increases activity AND the body can readily hydroxylate it to remove it from the body. If memory serves, the French made a heap of analogues and pyrovalerone and PPP were the best. The latter has no p-Me but the entire pyrrole ring is cleaved so again, we know where it's going.

Often designers keep on adding things they perceive to add potency but in fact, they usually just increase LogP and slow metabolism.
 
I read an article about the toxicity of clephedrone and meta-clephedrone recently. Both are apparently considered neurotoxins these days.

It doesn't exactly make me want to jump on the bandwagon. I held off on both 4-CMC and 3-CMC due to concerns over neurotoxicity and now I'm kind of glad I did.

I'm sure pCA is a great high too a few times, but you might pay a heavy price for it later.

I've seen both 4-cmc and 3-cmc wind up supposedly sold as 4-mmc so I haven't been trying to buy that either.

I could see clephedrone being a nice high, though. I liked flephedrone better than para-fluoroamphetamine.

I have seen para-bromoamphetamine listed for sale but I'm fairly certain it's neurotoxic and a potent maoi so I haven't been tempted.
 
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1-(3,4-methylenedioxy-5-methoxyphenyl)-2-amino-1-oxopropane.png


PUMPKIN_SPICE
1-(3,4-methylenedioxy-5-methoxyphenyl)-2-amino-1-oxopropane

Why is that substitution pattern, the 3,4-MDO-5-MeO-phenyl, so rarely seen?

1-(3,4-methylenedioxyphenyl)-2-amino-1-oxopropane.png


SPODEE_BOY
1-(3,4-methylenedioxyphenyl)-2-amino-1-oxopropane

bk-amps like to dimerize but still can be synthed
 
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@paracelsius what do you think about this one? It's α-PPP with the sidechain from mexedrone constrained into a ring.

I think it would at least be a functional stimulant. It might not knock your socks off. who knows?

I give you 3-pyrrolidin-1-yl-4-chromanone
3-pyrolidinyl-4-chromanone.jpg
 
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Can you please put the SMILES string as text so I can cut and paste.

O=C1c2ccccc2OCC1N1CCCC1

Is the above. And what a surprise, it's in PubMed.

 
l would love to try 5,7-dimethoxy-chroman-3-amine.

It's on pubchem but not the activity..
It's a ring constrained TMA-6.

5-7-dimethoxy-chroman-3-amine.jpg

smiles=COc1cc(cc2OCC(N)Cc21)OC
 
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OK, find phenylethylamine on PubChem and using the 3D viewer, compare the 2. I make the benzene ring look like a flat line so I'm looking down the length of the molecules. You will notice with PEA and amphetamine and related that the nitrogen is offset. If the aromatic isn't in an appropriate relative position to the amine (actually it's the nitrogen's lone pair but that's a detail),

I use this technique to decimate (the technical meaning) searches.
 
Yes, I can see that the nitrogen will be in a slightly different position. I would still be interested in trying the 5,7-dimethoxy-chroman-3-amine. It would be interesting to see how potency would be affected.
 
Try it with ALL the stimulants and 5HT2a ligands. They ALL have that offset.

Try cocaine, try phenmetrazine, try aminorex, amfonelic acid..... the relative position of the benzene ring and basic nitrogen is ALWAYS in exactly the same relative position.
 
The nitrogen is also offset quite a bit differently on the 3d model of TMA-6 vs amphetamine and phenethylamine.
 
BTW note that the nitrogen in the 'magic position' in amfonelic acid is part of a pyridine ring. the SECOND nitrogen is in the same relative position as the one found in all SSRI drugs like sertraline.

You have to ditch thinking about drugs as 2D structures, they are (almost) all 3D (a few are planer).
 
The nitrogen is also offset quite a bit differently on the 3d model of TMA-6 vs amphetamine and phenethylamine.

It's on the other side because it's a 5HT2a ligand. Stimulants are (R) and 5HT2a ligands are (S) (sinister). But TMA-6 is still the amphetamine scaffold with bits bolted on.

They represent the simplest class of all to build a training-set for.

Try it with opioids!

'The Morphine Rule' is common to over 90% of them and says:

1)Aromatic system
2)Quaternary carbon
3)2 methylene spacers
4)tertiary amine

But then you get tilidine, dezocine and a stack of exceptions. This is because it's NOT the nitrogen itself BUT the location and direction of the nitrogen's lone-pair.

I believe 1 training set defined

1)Aromatic system (pi bonds)
2)positively ionizable function
3)2 x oxygen lone-pairs
4)1 x nitrogen lone pair.

BUT their is also a specific site for a a second aromatic (e.g. fentanyl) and yet another that also binds via pi bonds e.g. allylprodine & 14-cinnamyloxycodone.....

That's why I study opioids. Nobody has yet found a set of rules that will include all opioids but exclude all non-opioids.
 
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