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Ketamine salts solubility

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But if there would be a hydroxyl moiety left from picamilon hydrolysis, wouldn't it produce GHB instead of GABA?

Cay29397-1_600x600.png


If it's indeed the case that a hydroxyl is left, then how about this? I guess this double-ketone thing wouldn't work?

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If it'
 
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It would indeed produce GHB but the hydrolysis isn't instant so it's just a way of making an inferior prodrug.

Your second image is more interesting but if I were looking to improve pregabalin, I would simply produce 4-methyl pregabalin which is apparently almost identical in it's subjective effects but is several times more potent.

I mean, I PRESUME you are looking for a legal pregabalin alternative. The higher potency makes it's more facile but all of the optimized routes to pregabalin I've seen cannot be modified to produce the chiral 4-methyk derivative and it's unlikely that the patent route will be optimal.
 
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HIGH_ROLLER_GIRL
1-(1-thiaindene-5-yl)-2-aminopropane

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HIGH_ROLLER_BOY
1-(1-thiaindene-6-yl)-2-aminopropane
 
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Yes, I know about the 4-methyl analogue, I'm just thinking in general terms about how you could change some structures and use the same principles for others too.

What about esters of different active substances? For example a 1:1 combination of desmethyl-tramadol and pregabalin is very nice, why not combining them into one molecule? If it would be possible, which OH moiety of the tramadol would make more sense to connect both molecules?





What about some Pregadrone or Pregamphetamine?


And here some really random things that got weirder as the night got longer



edit: just realized, that after separation the pregabalin molecule would probably tend to close into the lactame, maybe some carbamate analogues would make more sense if you can use the NH moiety of the tramadol to connect the carbamate, losing one of the carbons wouldn't have to be a problem I guess, as the single carbon metabolite is said to be active, although I couldn't find any binding data etc.
 
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Tramadol and even 4-methyl tramadol are active at quite different ranges so either one will be inactive OR a person would overdose on one to reach an active dose of the other,

As for producing a polymer of pregabalin - exactly how would you ensure you ended up with a single product? Have you 3D modelled an discovered that a cyclic polymer containing 12 pregabalin monomers will form?
 
I didn't went in that deep to 3d model it, really just a random molecule. I was thinking of those big polypeptide compounds and stuff like Semax and if one could make similar stuff with pregabalin. After all it's just an amino acid, so basically you should be able to do most things that you can with other amino acids, too?

I guess those esters and even carbamate conjugations of different drugs would probably be already banned by most analogue acts in the US and Europe, otherwise it would be too simple and obvious to not have been done yet, as I can't see any big problems or overly dangerous uncertainties arising from using such methods. At least I would feel somewhat safer ingesting an ester or carbamate of two known drugs instead of those really crazy analogue (d)evolutions we have seen over the years, especially with cannabinoids it's getting into really strange territories and those cathinones are getting quite creepy, too.

Although I could imagine that some compounds could have new effects on their own and in the worst case you could end up with some unexpectectly high potent agonist or antagonist, or toxic lactames and other alterations, and even just slight differences in metabolism leaving a hydroxyl instead of an amide could result in much more toxic compounds as it's the case with phenibut vs. "phenibot", which is phenyl-GHB and can cause convulsions at low doses (the compound is on the european market and can be researched if anyone dares)

If a 1:1 ratio of odT : pregabalin wouldn't fit for someone than maybe a 1:2 ratio will do ^^ and it doesn't have to be the perfect substance in terms of recreational value, but having something relatively nice at all would be good enough in todays conditions, and the line between self medication, supplementing, self-improvement/neurohacking and recreation gets more blurry anyways, so compounds of all kinds are interesting I'd say, just depends on how many people would research them and how complicated they are to create.

 
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It has been done. If memory serves someone mated a barbiturate with a carbamate long ago. I presume at a time when it wasn't appreciated that they bind to the same site.
 
Someone I know has serious fear for Alzheimer. Age 67 (she has skin Lupus to), another family member is 96 (cognitively still ok) but IMO also a good candidate.
At 50 my own body is showing Liverspot's, so I'll experiment on myself too.
To bad Centrophenoxine is not used by dr's over here, its not mentioned in their drug bible like many nootropic's.

The Lipofuscin removal/ anti Alzheimer effect do they still stand or has that been proven wrong. Anyone knows? I did search, but you are my knowledge database.

Is it worth to try, the fact its for someone else worries me as I ain't no dr. and never took it.
Should they tell there dr's. Has it interaction's with prescription medication's that you must be beware of.
 
It may be worth your time to watch (or indeed read the original book) 'The Case of the Frozen Addicts'.

Near the end it was suggested that in the future an MRI scan would detect those likely to develop Alzheimer's and those who were at risk would simply be prescribed meclobemide (if memory serves) which is an MAOI.

It's interesting that centrophenoxine displays MAO activity and is structurally similar to meclobemide.

Now, that 'future' never happened. I don't know why.

But it does seem that maintaining neuroplasticity is an important defence. People with quite advanced forms of dementia (from a structural point of view) who maintain patterns of learning do appear to survive and more importantly remain mentally aware for longer.
 
AlsoTapered said:
It may be worth your time to watch (or indeed read the original book) 'The Case of the Frozen Addicts'.

Near the end it was suggested that in the future an MRI scan would detect those likely to develop Alzheimer's and those who were at risk would simply be prescribed meclobemide (if memory serves) which is an MAOI.

It's interesting that centrophenoxine displays MAO activity and is structurally similar to meclobemide.

Now, that 'future' never happened. I don't know why.

But it does seem that maintaining neuroplasticity is an important defence. People with quite advanced forms of dementia (from a structural point of view) who maintain patterns of learning do appear to survive and more importantly remain mentally aware for longer.
Click to expand...

A future that relies on a simple MAOI (especially an old one) isn't profitable, even if it can slow the decline.

emkee_reinvented said:
Someone I know has serious fear for Alzheimer. Age 67 (she has skin Lupus to), another family member is 96 (cognitively still ok) but IMO also a good candidate.
At 50 my own body is showing Liverspot's, so I'll experiment on myself too.
To bad Centrophenoxine is not used by dr's over here, its not mentioned in their drug bible like many nootropic's.

The Lipofuscin removal/ anti Alzheimer effect do they still stand or has that been proven wrong. Anyone knows? I did search, but you are my knowledge database.

Is it worth to try, the fact its for someone else worries me as I ain't no dr. and never took it.
Should they tell there dr's. Has it interaction's with prescription medication's that you must be beware of.
Click to expand...

You can try it. It tends to be rather expensive though, particularly if you're planning to take it for years or decades. No particular interactions I can think of. Can make you feel a bit nauseous at higher doses, though nothing like homotaurine.
 
Yeah - MONEY. That hit's the nail on the head.

The thing is meclobemide was on-patent at the time (Hoffmamn la Roche from 1977) and experience has taught me that pharmaceutical companies have an almost supernatural ability to retain patent control on a medicine if they choose to do so.

One has to suspect HlR had another candidate in the pipeline.
 
AlsoTapered said:
It may be worth your time to watch (or indeed read the original book) 'The Case of the Frozen Addicts'.

Near the end it was suggested that in the future an MRI scan would detect those likely to develop Alzheimer's and those who were at risk would simply be prescribed meclobemide (if memory serves) which is an MAOI.

It's interesting that centrophenoxine displays MAO activity and is structurally similar to meclobemide.

Now, that 'future' never happened. I don't know why.

But it does seem that maintaining neuroplasticity is an important defence. People with quite advanced forms of dementia (from a structural point of view) who maintain patterns of learning do appear to survive and more importantly remain mentally aware for longer.
Click to expand...
"The case of the Frozen Addict's" is that a book you'll find in a library? Bizar title btw. Thanks for the pointer.

Meclobemide, assuming you mean Moclobemide the MAO-inhibitor prescription anti depressant, in other word's fat chance they will be able to get it. Way to many side effect's and interaction's and which dr. would be prepared I wonder.

But does it also remove Lipofuscin from the brain and Liverspots a.o.

Agreed on the last paragraph. Doing anything pleasureable, creative anything new is supposed to stimulate neuroplasticity. I noticed that myself, it was 3 year's ago 3 Epileptic seizures kinda stopped my life. And that together with more stress and sleepless night's. No good, better just to keep going. Luckily the Hippocampus is very neuro plastic.

But the Centrophenoxine is not for me so that's another story. I take L-Acetyl-Carnitine to repair my Hippocampus. Centrophenoxine is contradicted for Epileptic's.
 
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emkee_reinvented said:
Meclobemide, assuming you mean Moclobemide the MAO-inhibitor prescription anti depressant, in other word's fat chance they will be able to get it. Way to many side effect's and interaction's and which dr. would be prepared I wonder.
Click to expand...

Yeah moclobemide. It's not available in the US but it is in Europe. For all intents and purposes, there are very few side-effects. Doctors have this thing about MAOIs because an obese docker in Liverpool eons ago ate some ripe cheese once while taking an irreversible MAOI and had a heart attack from a (suspected) OD on catecholamines, but most don't actually understand how they work (or indeed how any medications work). Moc is a RIMA, and despite the package inserts, you can eat a very healthy quantity of tyramine and it still has little (if any) affect on BP or HR.

To be fair though, the MAOI that did/does seem to be more effective against Parkinsons and (in theory) dementias or brain injuries of all types is selegiline (taken for years). And that does have more side-effects, and is much harder (depending on where you live) to persuade anyone to prescribe. I secured Moclobemide very easily just by speaking to a psychiatrist, but selegeline was a no-no under any conditions.

emkee_reinvented said:
But the Centrophenoxine is not for me so that's another story. I take L-Acetyl-Carnitine to repair my Hippocampus. Centrophenoxine is contradicted for Epileptic's.
Click to expand...

Maybe add GlyNAC (glycine and NAC) to your arsenal if you're looking for an insurance policy against both physical and mental maladies of all kinds? It's cheap, easy to buy, and there's a fairly bulky - and growing - body of research that suggests it may help. You can read my short thread on what supps I'm giving my Mum with dementia down in LAVA if you want some more off-the-shelf ideas.
 
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iso-PCP
1-(1-piperidinyl)-2-phenylcyclohexane

Expected to be a stimulant, but I don't know.
 
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Selegiline is most likely a better option.

It DOES concern me that people mention this medicine and consider taking other stuff on top... well, maybe it will be OK and maybe it will not but their is such a thing as 'survival bias' in which various BLers will inform you that they took drug X with drug Y and were FINE. Not recognizing that the minority for whom it was not 'fine' are not in a position to post.

So yes - I think selegiline is very likely a medication that reduces the incidence of dementia BUT I know 30, 40 and even 50 year studies are ongoing and I'm sure we would all love a peek at the data... But a study is a study.
 
The LAVA points to different thread's, its a bit confusing.

You are presumably not dosing your Mum with LAVA right?

No way I am dosing my parents with Moclobemide or Selegiline, maybe myself. But that are presription's not nootropic's. So not avaiable.
 
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