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Ketamine salts solubility

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BO-PMMA??

Do you mean bk-PMMA?

It's still an MAOI so still makes the user feel poisoned but if the dose of bk-PMMA dose isn't to high, it should be OK. Do not forget that these p-monosubstituted homologues tend to mimic chemicals normally in the body and so high BP, high PR and such is likely.

I mean, I would try a low dose but I would much rather go for the p-Me (which the Russians did).
 
I guess if you are going to put a beta-ketone then you may as well go for an pyrrlidine for the N (as seen in MDPV). There was a medical stimulant which just had a p-Me on the benzene ring )so I expect it's a good choice) BUT who says go for an N-pentyl? The 1,2-diphenylethylamine homologue was made and was good i.e. pytophenidone.

The REASON why a p-Me was chosen over a p-MeO or an MD ring or a cyclopentane ting was SIMPLE. The body can oxidise that p-Me (alkane--->alcohol---> aldehyde--->carboxylic acid. OK it leaves the CNS as soon as it's hydroxylated but the whole point was:

a)to make it DAT selective
b) make it easy for body to metabolise & remove

I should add that the second benzene ring could be ANY aromatic. Just as long as it's space-filling. We didn't have to do it but ANY 5 or 6 membered aromatic ring will work (see zylofuramine).

We could not see any advantage of one aromatic over another but that is not to say that their are not a few that have an advantage. An O containing ring will lower LogP so lover potency but also lower duration.....

Of course, then diphenidine and all of the 1,2-diphenylethylamine NMDA antagonists are close by.

The idiots we had doing chemistry could not place a '2-Cl (so it overlays K) so they made the o-MeO which was toxic. NOT my idea.

The PERFECT would be the 2-Cl,5-MeO derivative (not made, too complex in spite of Janssen actualy patenting it in 1977).

But maybe you would like a TOYALLY new ligand for you? Ring substituted 8A-PDHQ & PD-137889 derivatives seem the obvious place to look.
 
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arrall said:
You gotta look at how low those probabilities are. The odds of it binding to more than one or two of those receptors well enough to produce a significant effect are very slim. It could very well be inactive.
Click to expand...
It has a low, but definite possibility for all the receptors.
 
Feretile said:
BO-PMMA??

Do you mean bk-PMMA?

It's still an MAOI so still makes the user feel poisoned but if the dose of bk-PMMA dose isn't to high, it should be OK. Do not forget that these p-monosubstituted homologues tend to mimic chemicals normally in the body and so high BP, high PR and such is likely.

I mean, I would try a low dose but I would much rather go for the p-Me (which the Russians did).
Click to expand...
I meant BO. Shulgin named the beta methoxy 2C series BOx. Like BOD and BOB aka beta methoxy 2C-D and beta methoxy 2C-B.

According to SAR studies I've read about MAO, beta keto and beta methoxy basically abolish an amphetamine's ability to inhibit MAO.

For instance, pMA is a potent MAOi. Beta keto or beta methoxy pMA would be less potent MAOi's than plain old amphetamine is though.

For some reason beta hydroxy retains MAOi activity yet beta keto and beta MeO do not.

www.frontiersin.org

Frontiers | Amphetamine Derivatives as Monoamine Oxidase Inhibitors

Amphetamine and its derivatives exhibit a wide range of pharmacological activities, including psychostimulant, hallucinogenic, entactogenic, anorectic, or an...
www.frontiersin.org www.frontiersin.org
 
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