Stimulants 3-FPO / 3FPO New Oxadiazol-based PEA

[Soulfake]

I got a G sample of this in the mail and wanted to ask what people think about this and if there are already faster labowls with experiences?

First reports sound a bit too good, something about similar to 3FPM and Amphetamine and derived from 4F-MPH although personally I can't compare both on the same level, 3FPM is very different from all Ephe/Amph/Cath stuff and feels really sedating for me, and after seeing how many possible metabolites this stuff can form, I really don't wonder about cardiovascular side effects that had been observed as well as why the non-halogenated one was used to stop hunger as there seem to be many metabolites with those "body building booster" thingy structures or how they are called, with those octopamine synephrine whatever pseudo-stims that mainly raise blood pressure etc.

Somehow I find those structures a bit scary with those extra nitrogens and older drugs with such configurations like Pemoline were as problematic as my gut feeling tells me, although others like Cyclazodone and Methyl-Cyclazodone seem to be less harmful but I wonder how they can state that without many studies and years of experience, usually it takes 15 years until a drug is really "researched" and further classified according to the severity of side effects and also the worldview of those deciding about it (just look at the sildenfinil situation where it gets more and more OTC in many countries as there simply haven't been any problematic effects been observed in healthy people so there is no reason to forbid adult people to put it into their body, but in Germany the buerorats instantly think "oh no that cannot be allowed people can't use it responsibly people are too dumb" (even though everyone can legally get a online prescription without any further questions etc., and everyone can put holes into his stomach legally with too many headache meds...)

5-((3-fluorophenyl)(piperidin-2-yl)methyl)-3-methyl-1,2,4-oxadiazol
FC=1C=C(C=CC1)C(C1=NC(=NO1)C)C1NCCCC1

SwissTargetPrediction

 

[4DQSAR]

I recall a team researching various methylphenidate derivatives a few years ago so I'm pretty sure it WAS tested. I belive it only ever underwent in vitro testing. So we have no way of knowing what the metabolism will be.

That meta fluoro moiety would have pushed up the synthetic cost so included to provide a specific activity or needed for the compound to demonstrate ANY activity?

If it hasn't undergone human trials - YOU ARE the human trial. The risk, I have always thought is that 99 people could consume something so novel and be fine - only to discover that due to genetic differences, the 100th person does have a negative reaction.

I would have gone for a para methyl or meta methyl first because it appears that a lot of enzymes will oxidize that methyl and produce a fairly reliable metabolic pathway. I mean over an example with no ring-substitution. But who knows? Maybe it was tried, maybe it wasn't.

I just use what I term 'defensive design' stratergy i.e. go for something where you can make a reasonable prediction of metabolism.

Still, interesting stuff.

 

[Esperighanto]

I'm excited to hear more about this, phenidates and relatives (phenylmorpholines, tricyclic compounds like pipradol and desoxypipradol, etc.) are some of my favorite compounds. Has anybody ever explored something like 2,5-dimethoxy-4-halogenated substitutions on the phenyl heterocycle? I suspect that since the same substitutions on phenmetrazine make a weak, though active psychedelic, perhaps something similar could some day arise in the world of phenidates.

 

[4DQSAR]

I, for one, would appreciate some reference for such a novel compound.

The closest I can find is: this:

Checking your browser - reCAPTCHA

EN300-37293661
2-[(4-fluorophenyl)(3-methyl-1,2,4-oxadiazol-5-yl)methyl]piperidine
CAS 2743442-63-7

The para fluoro positional isomer of the pictured compound. A few ligand suppliers offer it.

Now examples without that para fluoro AREN'T listed as far as I can tell. The meta fluoro isn't listed either. In fact, NO homologues are listed.

So why the meta fluoro? It appears the para fluoro compound was only added in 2022 but the meta fluoro isn't.

I checked Chemspider, Chemical Book, Molecule Finder & Chemsource as well and no further data was found.

EN300-37293660 | EnamineStore

View details for EN300-37293660 on EnamineStore.

www.enaminestore.com

Above is a link to a ligand supplier who doesn't sell to individuals so I think can be ruled out as a source. I enclose it because it includes the SDS of the positional isomer. I lack the technical skill to provide a link directly to that SDS. I'm hoping a mod can isolate that SDS so potential tasters have at least the best data I can find.

I would suggest someone invest in having GC-MS and NMR analysis carried out to see if it is the meta or if in fact it's the para. I mean, better safe than sorry and knowing for sure what you have is important in staying safe.

BTW that code name beginning with EN suggests that Enamine are the discoverrs of the para fluoro positional isomer.

 

[Esperighanto]

I lack the technical skill to provide a link directly to that SDS. I'm hoping a mod can isolate that SDS so potential tasters have at least the best data I can find.

I actually had a ton of trouble figuring out how to link to it, since it's not a separate download link as much as it's a page on a website. I wouldn't be super shocked if there's an analog being made of the para-fluoro isomer that is the meta-fluoro. It's probably weaker, and I'd be willing to bet that this is an attepmt to get around 4F-MPH bans in places like NL. Just my guess on the matter.

 

[4DQSAR]

@Esperighanto I really appreciate your feedback and I think you may well be right. My issue is that it's unclear to me what metabolic pathway(s) might be involved when the labile ester function is swapped for an aromatic.

I did search Google patents looking for Enamine patents but found nothing.

So I took the step of contacting Enamine asking for reference.

I SUSPECT that if a patent exists, if the compound only turned up in 2022 such a patent would still be in place. But the fact that they don't offer the meta fluro compound OR the unsubstituted parent compound MAY suggest that the para fluoro compound represents a 'small island of activity'. Or, equally possible, it's merely weaker and thus not as useful as a research ligand. Both make some sort of sense.

But I would love to see a GC-MS / NMR instrumental analysis of the product offered. Maybe they have something truly novel, Maybe not.

Only that analysis can confirm. I am not convinced that a simple 'druglikeness' webform in any way confirms utility or, more importtantly, safety. Legal comes a long way after 'safe' in my ethos.

I can't help thinking that there are things like pyrophenidone which is a bioisostere of pyrovalerone - the para methyl both increasing activity and reducing duration. If you simply MUST have crazy potent, JNJ-7925476 is part of a series and the interesting thing is that like the simple PEA-based compounds, various meta and para substituents were also tested so in theory, one can 'tune' the results in a subtle manner. While it has undergone in vivo models using rodents, I would still approach with great care. Sub nM affinity for the three monoamine transports makes for something that may be highly active... but as for human safety? None carried out as best I can tell.

But at least JNJ-7925476 HAS many academic papers and indeed patents thus we know a little biit more than we do with this stuff.

Quite honestly surprised that para ethynyl amphetamine was also offered as a research ligand and I'm honestly surprised that nobody has thought to try the beta ketone derivative. Why that and not the simple amphetamine? Metabolism. It would almost certainly be less potent but don't forget that while methadrone was reasoably non-toxic, p-TAP was mush more dubious. I had call to look at a cluster of deaths in and around Greater Manchester and some genius had figured out that mixing p-TAP with amphetamine estimated MDMA. But p-TAP appears to be an MAOI. Certainly it was misrepresented to consumers.

I hope my explaination is understandable to others.

It's been my experience that people under the influence of psychoactive sometimes make bad decisions. So in a way, you have to 'idiot proof' a design. If something is VERY potent, I don't think powder appropriate. Invest in a press and batch-test. At least that way know what they had and how much they had.

​

 

[4DQSAR]

https://www.erowid.org/archive/rhodium/pdf/cocaineanalogs.pdf#50

'The3â-(substituted phenyl)-2â-(3′-substituted 1 2′,4′-oxadiazol-5′-yl)tropanes (31,32a-f, 33; (Figure 9)) were designed becauset the1,2,4-oxadiazole ring is a bioisostereo of the carbomethoxy group and also stable to chemical and enzymatic degradation.'

The closest I can find is examples in which the methyl ester moiety found in cocaine was substituted with the 1,2,4-oxadiazole aromatic (page 938-940).

I note that all of the examples feature a para substituted benzene ring. It may just be a limitation of scope of research or may be important to activity. But that 3-methyl MAY be incorporated to provide a labile moiety for metabolism. But without data, that's just a guess. Equally they may increase activity or indeed do both,

So inching towards finding the data but so little is known, Well, 16+ hours of searching and this is all I have along with a couple of patents that MIGHT cover it but use click-chemistry and Markush structures so I can't be certain.

The 'elephant in the room' is the fact that che compound (whichever one it turns out to be) is chiral. I hope I don't need to remind people that the four enantiomers may have significantly different activity inclusing different metabolic fates. So any research would need to address that issue.

I just can't help thinking that homologues of Levophacetoperane AKA (R,R) Phacetoperane all appear to be legal BUT since the parent compound was used medically, at least we have data on that and one important detail is hidden in the name. It IS only a single enantiomer. Now, chiral synthesis costs more... but they did it anyway. So why?

 

[EnthusiastEclectic]

This stuff has reached clearnet providers, who even provide 10 mg and 20 mg pellets... Anybody tried those ?

 

[4DQSAR]

Well, question 1- why aren't the tablets white?

With a lot of RCs which came in tablet form, a colouring agent is sometimes to hide the fact that the product isn't white.

Now to be fair, some pure compounds are NOT white, but it's a minority.

I've always wondered why the term 'pellet' is used? Does US law mean using the term 'tablet' could leave a vendor open to 'misrepresenting' their product as a licenced pharmacutical' (or something along those lines)?

I would want to see independent instumental analysis as there are some synthetically simpler compounds and assuming the active was made in China, the Chinese are pragmatic, to whit 'if the market accepts the product, it's good enough'.

Getting the 98% purity required of licenced medications is hard and of course that other 2% has to be accounted for. If it's a non-toxic intermediate, no problem. If it's a reagent the workup didn't remove, it may be an issue. I'm not saying it will be, only that even if someone claimes 99.98% purity - if that 0.02% is abrin... that would be bad. Understanding how a medicine is licenced seems lacking. Just people producing a tiny, tiny (50mg) sample from repeated preparative chromatography that get sent to a tame 'independent' analytical laboratory.

If someone DOES order, I'm sure everyone would appreciate the sacrifice of one pellet to a HR unit who has instrumental analysis would, I'm sure, be appreciated by all.

 

[EnthusiastEclectic]

Well, question 1- why aren't the tablets white?

It is probably because they sell a lot of different substances with the same pellet form and their color is a practical way to differentiate...

The same clearnet provider sells also 4-MPO HCl

4-MPO HCl properties​

Synonym: 4-MPO, 4MPO, 5-[(4-methylphenyl)(piperidin-2-yl)methyl]-3-methyl-1,2,4-oxadiazole
IUPAC: 5-[(4-methylphenyl)(piperidin-2-yl)methyl]-3-methyl-1,2,4-oxadiazole
Molar mass: 307.82 g/mol
Purity: >98%

There's no picture for the HCl, so I do not know it's color

 

[4DQSAR]

Colour for the purposes of differentiation is depricated due to colour-blindness. That's why in developed nations medications are presented in patient-packs (which are sterile).

There is no associated CAS number for this compoiund or references so it's highly experimental. Sold as a research ligand for in vitro models.

Sci-Hub: are you are robot?

The aromatic substituted for the labile ester HAS been used in a wide variety of cases with no specific toxicity attributed to it's presence.

BUT as stated, that 2% needs to be qualified. The example I gave was obviously extreme but there are examples we can all point to. Recent cases where several common medications were discovered to contain nitrosamines. With any medicinal product, that 2% would be required to be qualified.

98% is fine, as long as we know what the other 2% is. After all, chronic toxicity is likely why the presence of nitrosamines was overlooked. No yellow cards from clinicians.

But, as I say, pop one tablet into the post - there are several highly respected HR agencies with access to instrumentation that provides for QUALATATIVE analysis.

These's days a GSL means a medication is in 'Stage V trials - pharmacovigilance' i.e. if yellow cards flood in the manufacturer is required to investigate.

I would be cautious as there are four stereoisomers and that means four chances of the product demonstrating side-effects.

Just an opinion but I would be especially keen on checking that the metabolism of the cis and trans isomers is the same. The bulky aromatic may prevent the oxidation of the para methyl.

 

[izo]

This 3-fpo is solid stuff. Works really Long and has a nice 3-fluoro feeling to it. But I find too expensive to really buy, there are man cheaper alternatives around…

 

[4DQSAR]

This 3-fpo is solid stuff. Works really Long and has a nice 3-fluoro feeling to it. But I find too expensive to really buy, there are man cheaper alternatives around…

Well, if you read my post - I noted that CHRONIC toxicity would be my concern, ESPECIALLY if there is a fluorine which may or may not have been addressed, since the thread begins with 3-FPO then announces the 4-MPO, which to be fair I did suggest was likely to be less problematic.

But unless a person sends of a tablet for quantitative and qualitative analysis (several HR agencies offer this service for free), who knows if someone simply renamed the same compound?

I'm not asserting it is toxic, in fact I did check and posted a paper on how widely the aromatic was being tested as an alternative to labile esters.

But saying you personally likewd whatever it was you were sent it appeal to anecdote - a logical fallicy.

 

[izo]

Well, if you read my post - I noted that CHRONIC toxicity would be my concern, ESPECIALLY if there is a fluorine which may or may not have been addressed,

Way should an aromatic fluorine be an toxicity concern? I See no reason…

 

[4DQSAR]

Way should an aromatic fluorine be an toxicity concern? I See no reason…

Because it ISN'T labile and it also lacks the labile methyl ester of methylphendiate.

In short - the metabolism is going to be far more complex and as stated there are four stereoisomers so think of it a 4 seperate drugs each of which could have their own metabolic pathways and potentially toxic metabolites.

People forget that - history is littered with medicines that WERE effective but could produce tarrible chronic toxicity. Often only in a sub-set of users. Aminorex is a good example.

Do you think the makers of methylphenidate haven't already experimented with the very same substitutions?

In my earlier posts you will note I found the para fluoro homologue and a link to examples where the methylester of cocaine and methylphendiate were swapped for a oxadiazole ring.

I've been supportive but you begin by altering ONE element, not two at the same time. It appears I was heard as I suggested the para methyl would at least offer a potentially labile moiety BUT because there is a second aromatic, it's not a given. One would need to locate the metabolites to ensure that like mephedrone, essentially 100% of it follows a very simple and non-toxic metabolic pathway.

I'm not asseting the compounds ARE toxic, only that they really are totally untested and appear to be sold only as reference ligands where toxicity wouldn't be an issue.

Put simply, it isn't for me to DISPROVE safety but for others to prove the fact. Hitchen's Razor.

I also noted that without sending off a sample pill for free indepedent testing, it's just another 'mystery powder game'.

I do have quite a lot of experience dealing with various 'fine chemical' suppliers and a person would need to be INSANE to trust their own instrumental data.

Elsewhere I've mentioned how someone was trying to sell what they claimed was the N-ethyl homologue of ketamine which was legal at the time. The NMR clearly showed that the chlorine was para, not ortho. When they finally admitted that yes, it was in fact a positional isomer they simply offered it for a lower price! We said 'no' but be honest, how many RC vendors these days would do the same? Would they even be able to spot it was the positional isomer? I have had DOZENS of such experiences so forgive me if I remind people that altruism is not how retailers operate.

We turned it down because it could have killed a lot of people and that's not good IF your plan is to sell the same produce for years. Now it seems vendors make a single batch and move on i.e. by the time the sky falls, they have moved on. I presume because stuff is banned so fast - but something being as dangerous as say aminorex isn't an 'if', only a 'when' and I would rather it not be BLers.

Now, vendors rely on people not checking. The Chinese manufacturers are totally pragmatic i.e 'it the marker accepts it, it's good enough'. If you have some, send a sample off - then, if I'm wrong, I'm wrong. The instrumental data will be on-line so every one of us can check.

 

[Chaurus]

Hey folks!

I just got the 10 10 mg 3-FPO pellets I ordered this week (in The Netherlands) this afternoon. How much should I take?

3-FPO Dosierung: Mengen in der Forschung – MODERNmind

3-FPO Dosierung: welche Mengen laut Berichten in der Forschung genannt werden, Formen wie Tabletten und Spray und worauf zu achten ist.

modernmind.eu

modernnmind.eu mentions the following doses:

Low dose: ca. 5 –10 mg

Medium dose: ~ 15 mg

High dose: ~ 30+ mg

 

[4DQSAR]

Hey folks!

I just got the 10 10 mg 3-FPO pellets I ordered this week (in The Netherlands) this afternoon. How much should I take?

3-FPO Dosierung: Mengen in der Forschung – MODERNmind

3-FPO Dosierung: welche Mengen laut Berichten in der Forschung genannt werden, Formen wie Tabletten und Spray und worauf zu achten ist.

modernmind.eu

modernnmind.eu mentions the following doses:

Low dose: ca. 5 –10 mg

Medium dose: ~ 15 mg

High dose: ~ 30+ mg

I would strongly encourage you to hold your water take one pellet to Jellinek or the DIMS network. Apparently the Amsterdam site now charges a nominal €2.50 in cash while the others remain free.

Since the synthesis is more taxing, there is more reason to question any instrumentation provided WITH the product and I have been fair, I haven't stated there is any reason to assume the product is misrepresented or dangerous, but then I'm not the one making the claims. Hitchen's Razor means the seller has to prove safety, skepticism is without that evidence, assume thee worst.

I'm reminded that aminorex reached market an only demonstrated chronic toxicity i.e. a person's may use and the toxicity only become symptomatic until after cessation, just like aminorex.

If nothing else, you can only make an informed choice if you KNOW what you are consuming.

 

[izo]

Dont but those pellets they are too overpriced.

 

[Chaurus]

I would strongly encourage you to hold your water take one pellet to Jellinek or the DIMS network. Apparently the Amsterdam site now charges a nominal €2.50 in cash while the others remain free.

Since the synthesis is more taxing, there is more reason to question any instrumentation provided WITH the product and I have been fair, I haven't stated there is any reason to assume the product is misrepresented or dangerous, but then I'm not the one making the claims. Hitchen's Razor means the seller has to prove safety, skepticism is without that evidence, assume thee worst.

I'm reminded that aminorex reached market an only demonstrated chronic toxicity i.e. a person's may use and the toxicity only become symptomatic until after cessation, just like aminorex.

If nothing else, you can only make an informed choice if you KNOW what you are consuming.

Can't promise a pellet will end up getting tested, also because I have no experience having my drugs tested, but I'm certainly considering it.

Dont but those pellets they are too overpriced.

Too late. What drew me in is that some of them were advertised as stims.

I miss RC-stims after the good ones were banned.

 

[izo]

miss RC-stims after the good ones were banned.

If youre in Europe you only have to Look, almost everything sold in recent years can still be purchased These days.