Opioids PEPPP 1-phenethyl - 4-phenyl - 4-propionoxypiperidine

[soluti]

HI
I saw a company which sells new Rc drug: 1-phenethyl - 4-phenyl - 4-propionoxypiperidine. I bought 1 g and I have a few question:
Mayby someone try this compound and can tell me something about this drug ?
I don`t trust this company and mayby someone from Europe have access to lc-ms and want to test this compound?
I read on wikipedia that in 80`s acetyl esters of this compound with a shost name PEPAP was quit popular maybe someone will know about it?
I use only codeine in quite high doses and a small doses of u-47700 and I looking something in this type, and i afraid its can by to strong for me. I don`t want take something like fentany and risk overdoses.
If someone want i can sand a msds card.
Sorry for my english I`m not a native speaker
Discription and tabel copy from the vendor page:


"It is research chemical of opioid analgesic drug class from prodine group. It is a potent ? full agonist of opioid receptor. It shows 4-5 times as potent as morphine in animal study. Same research has shown lower tendency to cause respiratory depression than morphine. This compound shows duration of action up to 5 hours. It is also a powerful local anesthetic."
[COLOR=rgba(0, 0, 0, 0.87)]Results of tests on animals

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[COLOR=rgba(0, 0, 0, 0.87)][COLOR=#424242 !important]All experiments were performed on brown rat (Rattus norvegicus).[/COLOR]
[/COLOR]
[COLOR=rgba(0, 0, 0, 0.87)]

Compound	Receptor affinity K (nM)	ED 50 mg/kg mice hot plate test
Morphine	3	1.2 (0.9-1.3)
PEPPP	0.73	0.3 (0.1-0.4)

[/COLOR]

 

[Speed King]

Sounds like an interesting compound. I couldn't find any real info on it. Will be interesting to find out more.

 

[Dr. Extract]

Would this be phenethyl desmethylprodine? Probably not, but I think the closest to that RC thats ever been used or tested is desmethylprodine.

 

[kleinerkiffer]

Yeah, MPPP (1-Methyl-4-phenyl-4-propion-oxy-piperidin) seems to be the closed RC to this one. Iirc if you fuck up the synthesis of MPPP an impurity is MPTP, the metabolite MPP+ will cause irreversible symptoms similar to Parkinsons disease.

 

[soluti]

I found one article about this compound:
Alpha- and Beta-Prodine Type Compounds
http://chemistry.mdma.ch/hiveboard/rhodium/pdf/alpha-beta.prodines.pdf
and in this article written that have potency about 3,45 more than morphine.
My friend have acess to gc fid chromatograph maybe this tell me something , if i get acess to gc-ms or lc-ms it should dispel doubts
I read on wikipedia about MPTP and there is written that MPTP is converted to toxic MPP+ by MAO-B enzym. I think it may be protected by taking selegiline to inhibit MAO-B enzyme.

 

[Speed King]

I would tread lightly with maoi’s until you know the substance.

 

[soluti]

Hi
My friend do some research by this compound and I think can be useful to someone.
Photo of sample: https://postimg.org/image/78ut7njpn/
Colour: beige
Smell: slightly like organic solvent and vinegar

TLC method
chloroform/methanol 95/5 (v/v) plus one drop of NH3 aq
Spot reagent: Liebermann reagent 10% sodium nitrite in cocnc H2SO4
photo of tlc plate : https://postimg.org/image/p2qb92siz/
2. pure sample disolved in methanol plus one drop of NH3 aq
1. sample first hydrolized by concentration NH3 and then extraction by chloroform
3. sample heated by flame in test tube then ad methanol and one drop of NH3
Description
Green area shown pure PEPPP.
Pink area shown hydrolized PEPPP to alcohol.
Red area shown dehydratation product to PEPTP.
conclusions:
1.The tested sample does not contain potentially toxic PEPTP
2. Testing sample was very pure contain only a bit of alcohol ( It can arise in sample by reaction with NH3)
3. PEPPP hydrochloride heated very hard is decomposed to PEPTP in around 10%

Gas chromatography
1. The same sample was decomposes to PEPTP HCL in gas chomatography injector 270C-350C peak purity 95%
2. After hydrolize with NH3 created alcohol can by analyzed by GC with good results
Conclusion:
GC is not a good method to analize PEPPP
I lost photo of GC results but if i find it i host it
So i think this sample is safe to use.
In this weekend I and my more experiences friend will test it
If you have any questios of sugestion please ask.

 

[soluti]

We finally tested it!
At the beginning we carried out an allergy test. Each of us sniffed 5 mg. After about 10 minutes the first effects were visible, I felt the pleasant warmth on my face. Then i take 15mg rectaly. After that i felt very well, moderate sedative effect and strong feeling of bliss. This lasted about 2 hour and began to slowly decline. After another 3 hours I felt already sober. PEPPP causes moderate release of histamine and strong anesthesia of mucosa.
My friend take 15 mg I.V. And he told me that is somethink betwene U4770 and morphine. And that it is more similar to morphine but have less euphoric entry than it. He estimated duration time for around 3 hour.
So i think is a very interesting substances for someone who like substances without strong entry and probably will be a good substantion for withdrawal from hard opioids.
In next weekend i test it orally.


Backfromthebring Now that I know what it means, this word also makes me laugh.
Steady Scootin Thank you for your attention.
It is not easy to describe feelings in not native language. I have edited a bit for better readability.

 

[Steady Scootin]

Not clear on a lot of what you said there. Felt already cautious? No clue what you or your friend consider mild or whathave you euphoria. Light climate?

 

[Backfromthebrink]

someone who like substances without stong entry

Please don't be offended as I know it's difficult when trying to explain something in a foreign language, but that sentence made me lol for some childish reason

 

[DemonSeed]

Yeah, MPPP (1-Methyl-4-phenyl-4-propion-oxy-piperidin) seems to be the closed RC to this one. Iirc if you fuck up the synthesis of MPPP an impurity is MPTP, the metabolite MPP+ will cause irreversible symptoms similar to Parkinsons disease.

I would be kind of worried buying MPPP since it could possibly contain MPTP as an impurity, shouldn't I? I recently came across the Wikipedia article of MPTP, as it neurotoxicity was hinted when a chemist synthesized MPPP. Here's the full story:

Discovery in users of illicit drugs

The neurotoxicity of MPTP was hinted at in 1976 after Barry Kidston, a 23-year-old chemistry graduate student in Maryland, US, synthesized MPPP with MPTP as a major impurity, and self-injected the result. Within three days he began exhibiting symptoms of Parkinson's disease. The National Institute of Mental Health found traces of MPTP and other pethidine analogs in his lab. They tested the substances on rats, but due to rodents' tolerance for this type of neurotoxin nothing was observed. Kidston's Parkinsonism was treated with levodopa but he died 18 months later from a cocaine overdose. Upon autopsy, Lewy bodies and destruction of dopaminergic neurons in the substantia nigra were discovered.

In 1982, six people in Santa Clara County, California, US, were diagnosed with Parkinsonism after having used MPPP contaminated with MPTP. The neurologist J. William Langston in collaboration with NIH tracked down MPTP as the cause, and its effects on primates were researched. After performing neural grafts of fetal tissue on three of the patients at Lund University Hospital in Sweden, the motor symptoms of two of the three patients were successfully treated, and the third showed partial recovery.

I won't be messing around with that drug personally.

 

[soluti]

Yes i think contamination may be dengerous but I test this stuff by TLC and any traces of PEPTP were not detected. I've been waiting for results of analisys over a month. I was also interested because of the price of it. It`s almost 3 time cheapest than codeine. But most importantly I would not have to buy in many pharmacies and do extractions . I live in small town where is only 5 pharmacy and it`s a significant problem.

 

[Scrofula]

If this really is PEPPP (the propionoxy and not acetoxy PEPAP) then there's no risk of MPTP.

So this compound is an anologue of desme-prodine (MPPP), that's true. But where that compound has a single methyl group on the pyridinium nitrogen, this one has a phenethyl group instead. That means the starting reagent MPTP is never used, and the toxic form, MPP+, would never occur.

I would distrust this guy's TLC experiment simply because there's no reason to do it. Like, the whole point is there's no MPTP.

Instead you're left with PEPAP, alleged to be 6-7x the potency of morphine, or a more lipophilic desme-prodine/MPPP.

I don't know what all the advantages to MPPP were, but this is the no-risk-of-toxic intermediate, plus whatever-you-get-with a fatty tail analog.

 

[soluti]

Scrofula you have got right. I found a interesting article:

It is unlikely that the tetrahydropyridine byproducts that may be formed during the synthesis of PEPAP are neurotoxic in the same way as the MPPP byproduct MPTP. It appears that the N-methyl group of MPTP is required for neurotoxic activity. In animal experiments, only MPTP analogues that preserved the N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine structure were active as dopaminergic neurotoxins. Most structural changes, including replacing the N-methyl group with other substituents, abolished neurotoxicity.[3]

• Youngster, SK; Sonsalla, PK; Sieber, BA; Heikkila, RE (1989). "Structure-activity study of the mechanism of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurotoxicity. I. Evaluation of the biological activity of MPTP analogs". The Journal of Pharmacology and Experimental Therapeutics. 249 (3): 820–8. PMID 2786564.

So it`s 100% safe

 

[Scrofula]

It's pretty simple to know: Was MPTP a reagent used or not? Someone would have to grab a bottle that said "MPTP" on it at the beginning of the synth--it's not shrouded in mystery.

They wouldn't though. They'd grab a bottle that said 1-phenethyl-PTP instead. Ok, probably not in reality, but that's the equivalent starting compound.

It doesn't ever sneak in on its own.

ETA:

So it`s 100% safe

Meant to just say, "It's probably 100% safe from MPP+ toxicity. Still might kill you."

 

[soluti]

From the beginning I knew that this sample does not contain MPTP. The most important thing was to find out something about PEPTP, which may have been present as an impurity or formed during vaporization. This article dispelled doubts. So PEPPP can by vaporised without worries about dopamine neurotoxic. Dopamine neurotoxic not only shows MPTP but also nine analogs were found to be neurotoxic. All ow it contain N methyl group and orto/meta substitution in phenyl ring.

I spoke too hastily about safety. Any drug aren`t 100% safe in particular opioids.

 

[Neopunk]

The synthesis neither requires MPTP nor PEPTP, they're just impurities that are formed due to high temperatures or to acidic conditions, but soluti already explained the situation.
I read some papers on this topic and it seems, that substituents larger than propyl are required, too small substituents cause the compounds to remain substrates for MAO-B.
It's not safe to assume PEPTP isn't a neurotoxin just because of one paper.. Look at Haloperidol: The key pharmacophores are the same and the substituent at the nitrogen is even bigger than the phenethyl in PEPAP and PEPPP and we all know that Haloperidol isn't exactly what is called a non-toxic compound..
So better be careful..

@soluti: Can you please update on this topic? I'm still interested in some more details. Thanks in advance

 

[Scrofula]

What we do know is that MPTP, which is a precursor for desmeprodine, can form a toxic radical, MPP+. That causes Parkinson's Disease-type symptoms by killing dopaminergic neurons. Both of those compounds are related to another suspected toxic compound, the insecticide paraquot. Just think, they spray this shit into open air.

There is no way no how a person would ever use this for synthesizing a phenethyl- version of prodine. It would be like trying to attach a semi trailer to your car, but there's already a fifth-wheel attached.

So MPTP and MPP+ are not concerns with this compound. No one ever said that renders it safe for consumption, though, or that who ever made this particular lot knew what they were doing, or won't just sell you some crushed Vicodin instead. Or I guess, chalk with some fentanyl analogue squirted on.


Speaking of fentanyl, it--and most of its analogues--has the exact same N-substituent as this compound (and is part of the same pharmacophore, unlike haloperidol, which has a different target). Those fent analogues aren't exactly safe for home use (outside of patches) but I don't think there's any reports of toxicity at prescribed doses.

 

[Neopunk]

MPTP is not a precursor for Desmethylprodine. What does make you think so? Those drugs are made with 4-Piperidone by alkylation with the alkylhalide, following a Grignard with the aryl bromide and subsequent acylation of the tertiary alcohol. And that's where the elimination reaction happens: propionic acid liberates and MPTP or PEPTP is produced as a side product. No one would start with MPTP or PEPTP, not only because it's dumb to choose such a toxic reagent, no, it's absolutely impractical.

And it's irrelevant if Haloperidol acts on different receptors than PEPAP/PEPPP/MPPP, the toxicity comes from the methyl pyridinium metabolite, which is a cation and not a radical btw.
As I mentioned in my previous post, it's all about the affinity to MAO-B, like you said, Paraquat acts the same way and is of course not an opioid.

 

[Limpet_Chicken]

Yeah, from what I've read, an N-methyl substituent is requisite for DAergic neuron toxicity. Although that wouldn't mean I'd not get an NMR done on any sample of the stuff if I were to make it or buy it before it went into me or anybody else I liked.