Russian 'novelties' - Fabomotizole, Mebicar (anxiolytic), Mesocarb (dopaminergic)

[dopamimetic]

Besides the better-known things like phenibut, phenazepam and phenylpiracetam (Carphedron) - all of which were mostly unknown to the western countries until some RC / nootropic vendors started to selling them - the Russians have some more very interesting compounds. Probably there are quite a few more that yet need to be documented in English.

Mebicar
An anxiolytic that modulate GABA, increases serotonin levels, decreases noradrenaline with no effect on dopamine and no anticholinergic activity. Is said to be non-addictive, non-sedating and does not impair motor skills. Sounds pretty good?

Fabomotizole
Another one with GABAergic, NGF- and BDNF-release-promoting and sigma-agonistic properties. Seems to involve serotinin too.

Emoxypine
A pyridoxine derivate antioxidant and anxiolytic, that increases dopaminergic transmission, lowers cholesterol levels and stabilizes cell membranes. Possibly promotes regeneration of peripheral nerves. Afaik this one has already reached the nootropic market.

--

Last but not least, a pretty old drug but somehow one of my favorites: Mesocarb
A dopamine reuptake inhibitor and anticonvulsant(!) with slow onset and long duration, stated to lack significant potential for abuse. ADHD treatment. And it's a weird oxazoline derivated structure (very) distantly related to Pemoline / Aminorex - the class of stimulants that greatly fascinates me. Sadly it's banned nearly worldwide, but a legal derivate shouldn't be too hard to make...?

 

[clubcard]

I've often wondered if that urea-bridge & second benzene make it a prodrug. I also wonder about possible MAOI activity.

 

[aced126]

I read about mebicar a while back and wondered why more people haven't tried it. Seems like the perfect drug. In fact, it could probably substitute well for alcohol as a social drug. There must be a catch...

 

[dopamimetic]

This is around the only statement I've found about mesocarb (and this paper - fulltext anyone?)

It was widely used in USSR, decades ago, and was taken off due to problems of abuse in early 90s. Until 2006 it was precribed by psychiatrist, it was an only stimulant in Russia. After 2006 the only factory i St. Petersburg was closed and now here is no Mesocarb.
As for effects it was prone to stimulant psychosis, for example if you use amphetamine for 5 days then on a fifth day you'll get no euphoria from same dose - only dirty stimulation, but Mesocarb is another thing, it will give your all positive effects of a stimulant, but also chances of a psychosis are skyrocketed. It was manufactured in a 5 mg pills.

Sounds indeed like an oxazoline. 'Non-depleting' stimulant, relative lack of locomotor potentiation / peripheral stimulation, selective and potent but also dangerous if overused.

I really wanna try this one (as well as pemoline and it's derivates). I've used quite some 4,4'-dimethylaminorex with no problems at all to limit the consumption, getting enough sleep at night etc - and I'd say it was one of the most impressing drugs I've ever done. So crisp, clear, calm, natural - really enhanced my psychic potential far over the normal limits and in a nearly nootropic way. Also it worked on and on again every day for weeks (low dosed, maybe 25mg). If just the danger of pulmonary hypertension and heart valve damage wouldn't be so imminent.

There are some russian online pharmacies selling mebicar among others. If I find a reputable one (and manage to get these pills through customs) I'll try the mebicar for sure, and will report !

 

[clubcard]

Russian chemists originally discovered this in the 1950s:

Which is 1/2 the potency of morphine. Researchers in the US rediscovered it in 1969.

Discussion of QSAR J Med Chem. 1969 Nov;12(6):994-7 - Analgesics. II. Relationship between structure and activity of some β-Amino Ketones J Med Chem. 1969 Nov;12(6):994-7

Interesting that it's conformal isomerism that makes it active. Overlays prodine. It would appear that a ketone can replace esters in quite a few examples of this class.

 

[blueberries]

Oh I love Russian drugs!!

I've tried Emoxypine ('Russian coke' we dubbed it), SEMAX (hands down best nootropic I've ever tried), Carphedon & Noopept (of course but still probably the best -racetams (disregarding Colur- & Faso-)), Bromantane (wonderful anxiolytic) and Afobazole (another wonderful anxiolytic!). Each one is just miles ahead of the competitors.

Honestly the stuff to come from the (ex-)Soviets is incredible. It's another level of pharmacology. I thought Japanese drugs were 'out there' but this is something else. I swear everything they touch turns to gold...except Phenazepam. That went a little awry but the UK sold it by the gram so it's not surprising.

That Fabomotizole looks like a proper gem. Plus the compound from clubcard looks just amazing too. I mean it's so damn simple. I'd never heard of them before today but dammit I'm going to research the shit out of them now!

)Sounds indeed like an oxazoline. 'Non-depleting' stimulant, relative lack of locomotor potentiation / peripheral stimulation, selective and potent but also dangerous if overused.

It may act like an Oxazoline and almost has the structure of it, removing one of the nitrogens from the pyrolle and reducing the bridge by a few carbons, that ketone, the amines and reducing the double bond, but it isn't! It's still a very interesting structure though but I really don't think it could be as powerful as say 4-MAR or even Phenmetrazine, though it would almost certainly make up for it with ingenious Russian modifications. It'd be like Russian amphetamine. All of the bonuses, none of the negatives!

EDIT: Ok, one of the negatives! If used responsibly I don't think it could be an issue though.

Sadly it's banned nearly worldwide, but a legal derivate shouldn't be too hard to make...?

Just put a para-methyl on one of the phenyl rings. Job done.

 

[dopamimetic]

Honestly the stuff to come from the (ex-)Soviets is incredible. It's another level of pharmacology

Oh yeah. Really makes me think again what the hell our western pharmacology industry does with all that billions of $$$ ... in recent times, more true novelties seem to come from clandestine RC chemists and nootropic scientists than from all the big companies together. Granted, most of them are at least based on research done at universities or companies. But nevertheless.

The Russians also seem to have a working anti-influenza drug. Something apparently nobody else has been able to come up with (Tamiflu etc..)

Semax is actually the first nootropic that really amazed me. It has some edgy sides, but it does a good job for someone with negative responses to all those racetams.

Fabomotizole and Mebicar should be on their way hopefully reaching me. Bromantane too, but not the original Russian product.
So Emoxypine is worthy to try too?

 

[clubcard]

Pyrazolam is an example of a compound that improves on medical benzos - excreted unchanged. Not great for getting wasted, but loved by the Social Anxiety forums.

I think people had better start pushing protons around the -1,2,3-oxadiazol-3-ium-2-ide. Charged (small) molecules cannot pass the BBB. So many medications use this fact from Buscopan to Methylnaltrexone. I'm betting that the carbamate bridge to the benzene is lost. Hydrolysis would produce something that is likely to be active.

 

[dopamimetic]

You- thanks for the U47700. Pity you killed someone with it.

How do you mean that?

 

[clubcard]

Ask Herbivore... ask anyone from Eunoiapharmacopia.com

 

[dopamimetic]

While experimenting with SEMAX - the first nootropic that really hits me (the racetams were more or less dysphoric, anxiogenic and overstimulating) - I begin to feel that it is somewhat a double edged sword. The first administration led to a pronounced stimulation, including elevated heartbeat, but also very clear and mind-centered. After some time, this faded away. Maybe four hours later I experienced a true crash, feeling overwhelmed by sensory input and thoughts maybe comparable to an overdose of a very dopamine-selective stimulant like isopropylphenidate. At this point I had to lie down in a dark room and listen to calming music. After another hour or so, this had passed too.

The morning after I noticed that I woke up earlier and with more energy than usual. Not positive but not negative either.
In the following days I did not notice much acute effects anymore, but a tendency to clarity of mind and long forgotten drive / energy continued.

Somehow it is a very unpredictable chemical. The overall effects are positive, I feel that it has true potential to lift that "therapy resistent" depressive brain fog I've lived with for years. But in the last days I noticed that it might be addictive. It lasts only a few hours and then comes a light, but annoying crash- that can be alleviated by redosing, and/or (re)dosing a -phenidate.

Also there is a good synergy with phenidates (in therapeutic dosages for ADD, I usually stay below 20mg per day). I take magnesium citrate, citicoline, an omega 3-6-9 supplement and memantine 30mg/d, as well as clonidine as needed from 25-150mcg (mostly to sleep). So this is not representative at all, but I've read in a German forum from someone else who seemed to be quite addicted to semax (as with all internet reports, I take this with a grain of salt of course.)

 

[clubcard]

http://bitnest.ca/external.php?id=%7DbxUgP%5BCnxfi%7B%7F%04%04W%5BT%04V

Mesocarb is listed as a prodrug for amphetamine. Both animal and human studies found amphetamine as a metabolite. I would say, a VERY Russian prodrug. I think that there are 2 steps. Firstly hydrolysis yields a syndone (and the trade name is Syndocarb) and then the second step is a bit of a mystery. It's still carrying a displaced charge so won't pass the BBB so I think (dex)amphetamine is the only active. I put (dex) because various sources disagree, but for a medicine, I would HOPE they made the active isomer (it's got a lot less body load).

This intermediate isn't excreted while 35% exists as hydroxylated mesocarb metabolites so it appears that this second step occurs in short order. Maximum doses are given as 100-150mg/day and that would equate to about 1/3rd as much amphetamine. I guess it's an interesting prodrug and from what I can glean from Russian papers, synthesis isn't from amphetamine. Even so, I wouldn't trust it to make a legal prodrug. Of 0.1% degrades to the active, you will be tried for the full weight.

 

[aced126]

I agree with club that the charged version of mesocarb ain't crossing the BBB. Could the molecule not however be protonated for example in the stomach, where the -ve nitrogen attacks a proton and the double bond attacks another proton, making the molecule neutral? Or is the molecule more stable as it is in charged form? On another note can anyone speculate on the role of oxazoline in these types of compounds? Is it simply acting as a bioisostere instead of the carbon spacer, which isn't easily metabolised by MAO? Or could it have more interactions on its target?

Edit: the oxazoline has 5HT2b properties as well, so that is at least one extra interaction.

 

[clubcard]

That's the great mystery. What it does in the stomach is of little import, it what it does in the blood. None of the syndone is excreted while 35% is excreted unchanged or hydroxylated. Amphetamine with a hydrazine is known, but I think it's an MAOI. certainly something major is happening - that ring is destroyed leaving an amine behind. I WOULD be an interesting experiment and technically it would be legal but like I said, if a tiny amount breaks down to amphetamine, any prosecution will try for the whole mass to be considered to be amphetamine with a cut.

The net charge is 0 so it could well be that the 1,2,3-oxadiazole is formed when the carbamate bridge is broken. Just move the double bond. It would be fascinating to find that an aromatic bearing the nitrogen is active.

 

[clubcard]

OK, I'm going to suggest that the imine kept the compound charged so it couldn't enter the brain. Then hydrolysis replaced it with a =O, the double-bond shifts so no charge. Since it's not found as a metabolite, either it then quickly breaks down to amphetamine and/or the MAOs get it while it's bound to the receptor. The fact that amphetamine is a substantial part of the metabolites, I don't believe it's a PURE dopamagenic.

 

[Nagelfar]

Oh I love Russian drugs!!

...Emoxypine...SEMAX...Carphedon & Noopept... Bromantane...Afobazole...

Does the Russian Federation make use of a lot more peptides than we do further west or what? I still think they should start putting DAMGO into all the Rx opioids.

 

[dopamimetic]

Is DAMGO orally active?

It's a really fascinating drug, an opioid that actually reverses tolerance.. (is anything known about how far this goes... will it stop at baseline or does sensitization occur with continued use, what could become dangerous?) I've read about some obscure opioid peptides before that were researched for possible lack of tolerance development, but with DAMGO it seems to be a proven thing.

Unfortunately, the interest in tolerance alleviating doesn't seem that big. Memantine is proven to help with opioid tolerance and every doc could prescribe it off-label.

 

[dopamimetic]

Forgot to post about the impressions of some of them:

Bromantane: This is a real winner. Why can't coffee be like this!? It's stimulating in such a calm, clear, natural way that I wouldn't call it a stimulant at all. More of a wakefulness-promoting 'normalizing agent' with some hints of positive mood. If this shows to be sustainable (which it probably won't, or many people would be taking it daily), then just wow.

Emoxypine: Unnoticeable when taken alone, but possibly of great benefit when taking stimulants. It's too early to claim anything, but I'd say that it nearly erases the comedown and hangover from isopropylphenidate (which is already much easier than MPH, but with one 125mg emoxypine pill with every dose it's a new level.) Might be effective in alleviating dopamine (auto)oxidation.

 

[asecin]

very very good and informative thread. any updates recently? im actually interested in sources to buy some of the things mentioned here, specifically mesocarb, any ideas?

 

[clubcard]

Besides the better-known things like phenibut, phenazepam and phenylpiracetam (Carphedron) - all of which were mostly unknown to the western countries until some RC / nootropic vendors started to selling them - the Russians have some more very interesting compounds. Probably there are quite a few more that yet need to be documented in English.

Mebicar
An anxiolytic that modulate GABA, increases serotonin levels, decreases noradrenaline with no effect on dopamine and no anticholinergic activity. Is said to be non-addictive, non-sedating and does not impair motor skills. Sounds pretty good?

Fabomotizole
Another one with GABAergic, NGF- and BDNF-release-promoting and sigma-agonistic properties. Seems to involve serotinin too.

Emoxypine
A pyridoxine derivate antioxidant and anxiolytic, that increases dopaminergic transmission, lowers cholesterol levels and stabilizes cell membranes. Possibly promotes regeneration of peripheral nerves. Afaik this one has already reached the nootropic market.

--

Last but not least, a pretty old drug but somehow one of my favorites: Mesocarb
A dopamine reuptake inhibitor and anticonvulsant(!) with slow onset and long duration, stated to lack significant potential for abuse. ADHD treatment. And it's a weird oxazoline derivated structure (very) distantly related to Pemoline / Aminorex - the class of stimulants that greatly fascinates me. Sadly it's banned nearly worldwide, but a legal derivate shouldn't be too hard to make...?

The problem is, the majority of these have no English language articles on interactions so while they may well be safe alone, someone on an SSRI for example. One of those looks like a RIMA to me. Interesting, but find the patent, find the paper(s) and find metabolism. Only then can you be reasonably sure it's safe. If you can order from Russia and translate the patient information leaflets then it would be interesting, but without that, I wouldn't go near them - don't want to hurt anyone.