Sciencemadness Discussion Board

4-anilino-N-phenethylpiperidine 2-furanamide

chemrox - 28-1-2016 at 15:03

Through methods I can't publish I have discovered that 4-anilino-N-phenethylpiperidine-2-furanamide is a partial mu agonist/antagonist that potentiates other mu agonist/antagonists such as buprenorphine and possibly etorphine. I don't care for killing mice. I left med chem for that reason (they were using dogs in my department). So how to publish the results or properly document.

Nicodem - 30-1-2016 at 07:51

Clearly, if you have scientific evidence, you can publish it in scientific journals, assuming it is relevant enough to be worthy of acceptance. Since the chemical name you gave is invalid, I can't say much about scientific relevance. In principle, it is unlikely to be accepted if all it is about is just one compound that fit the current SAR theory. It would lack any novelty. In general, no journal would publish information just about a single compound, unless there is some solid biological activity study in addition to that (like animal or clinical experiments, etc.). If it would be a new lead compound, without further lead optimization, it might be accepted in some less relevant journals, assuming there is at least some proper biological data with it. If at least the synthesis would have been challenging, like requiring the development of new strategies or synthetic methods, then perhaps you can publish it as chemistry.

If the evidence is based on belief, you can post it on some theological internet forum. They might mistake you for a troll, but at least you would get it published. Alternatively, you can disclose such information in a pub.

If you only have circumstantial evidence, for example, by subjectively believing based on a human biological assay on yourself, that some compound is "a partial mu agonist/antagonist" and does this and that, you can publish it on some internet forum dedicated to narcotically inclined people. I googled for keywords "opiates forum" just to be shocked about how many such forums there are!

If you got the circumstantial evidence by doing illegal biological assays on nonconsenting subjects, or consenting but unapproved by the ethics commission, or through any any such methods that might have given you the feeling that you can't publish about, then you can still publish it in one of those narcotics forums, but anonymously, or you can find some forum for criminally inclined and publish it with your real name.

zed - 30-1-2016 at 15:52

Are you suggesting that the material is substituted at the 2-position of the piperidine ring?

Or, is it the furan-2-carboxamide of 4-anilino-N-phenethylpiperidine?

It is a big world. What might bring trouble here in the U.S., via publication.....might be completely hunky-dory to publish elsewhere.

Plenty of Journals are starving for decent submissions, though from what I understand, some may charge a hefty fee for such submissions.

Got some journals in India, would probably like to have the info.. No questions asked. From there, the information will spread everywhere.

In lots of parts of the world, scheduling is kind of a theoretical endeavor. Opiates are technically illegal, but of course, if you need some opium, you can just go down to the farmers market, and buy a little bit. Not a big deal.



[Edited on 31-1-2016 by zed]

AvBaeyer - 30-1-2016 at 19:36

Nicodem,

You cracked me up! Great!

AvB

semesa - 3-2-2016 at 00:02

You want to publish results based entirely from "methods I can't publish"?

Beyond the fields of Psychology and religion, I think success is extremely unlikely.

zed - 3-2-2016 at 15:48

Hunh? Albert Hoffman published. He was accidentally exposed to an extremely potent research chemical; it got him high as a kite, and he didn't die. The rest is history.

A fella could accidentally insufflate a research chemical, when he had meant to reach for the snuff. He could even accidentally inject himself with a dangerous opiate. It happens all the time.

Read the cautions for working with M99. A guy is trying to prep a dart, to immobilize a rhino, and whoops! A scratch, or an accidental injection. In fact, yer supposed to start first aid, if you so much as touch the needle itself.

Chemrox seems to have a worthwhile story to tell. Let the world hear it.

Dr.Bob - 3-2-2016 at 18:34

Not quite sure of the structure either, but this is a forum for publishing data, so let 'er rip. If nothing else, you can present an abstract of what you want to publish more formally.

By potentiate, do you think it acts allosterically, blocks the metabolism of other drugs, or changes the expression of the receptor?

I have had lots of work that never saw the light of day from previous projects, that is a risk of working for a corporation. Even academic places sometimes don't publish data that they don't think leads to a grant. And negative data is hard to get journals to publish as well.

chemrox - 3-2-2016 at 20:49

Quote: Originally posted by zed  

Or, is it the furan-2-carboxamide of 4-anilino-N-phenethylpiperidine?

[Edited on 31-1-2016 by zed]

Yes.

chemrox - 3-2-2016 at 20:57

@Nicodem. I appreciate the comments. The issue hinges on "biological activity.." I don't do rat torture. Shulgin published accounts of friends tasting his beverages so to speak but not in the scientific literature. Nichols has his students and colleagues giving feedback on his materials but these accounts are not published and he resorts to animal torment or delight as the case may be .. I can hardly say I gave the stuff to an opiod user and he threw up whereas a naive person experienced relief from chronic back pain. 1) insufficient data- not nearly enough and 2) non-pc methods. 3) my license doesn't permit human trials.

chemrox - 4-2-2016 at 12:29

Quote: Originally posted by semesa  


Beyond the fields of Psychology and religion, I think success is extremely unlikely.

Maybe those are the realms to approach with it. On the other hand, why publish at all? The reasons are to get the information to those who could benefit. Why did Shulgin publish PiKHAL? To make the discoveries of psychedelics more available. Also to attack the prevalent notion that drugs are bad. One of my friends here shared that opinion. His living in Thailand may have had a lot to do with the attitude. Thailand was an oasis of peace and equanimity in region plagued by war and politics. Western culture brought the disease of mendacity with it's common cogener: methamphetamine. Formerly Thais used opium and alcohol for occasional respite from the aches and pains of daily life. Mostly they used meditation. The advent of long working hours, ambition and hyperactivity brought meth and bad temper along with them.

chemrox - 4-2-2016 at 13:43

4-(p-fluoroanilino)-N-phenethylpiperidine-(2furanoylcarboximide). I'm having trouble here with nomenclature but I could draw it.. It could be called "furanoyl-P-fluorofentanil." [substitution of "y" with "i" in fentanyl seems to be in the literature.] The compound was tested by: 1 junky, 2 (legal) opioid users and 2 chronic pain victims. Of these 1 was given buprenorphine as "suboxone" which contains naltrexone an opiate antagonist. Buprenorphine is an opioid mixed agonist/antagonist. The results are as follows: the junky got sick, the pain victims experienced reduction of pain, the buprenorphine patient got high and had additional pain relief. The only way to publish results (with much additional experiential data) would be to make an erowid "vault." Is that still available? For very good reasons this is NOT a drug forum. However these experiments may provide help to people who need pain relief and 'happiness' to folks on suboxone. It would be *irresponsible* to disseminate the information on "bluelight" or other drug related forums. The stuff is very strong. I believe it is much less toxic than fentanyl. But I don't have proof of that yet and am not sure how to proceed without killing small rodents. Besides I no longer have access to rats and mice or the torture methods they'd be subjected to. This is new analog recently synthesized and tested. The new aspect is the p-fluor substitution. The consensus was that the p-fluoro version was a little stronger and more pleasant. In any case P-fluoroaniline is less toxic than aniline and may not be carcinogenic. Thus the synthesis is safer. NB: 2 furyl chloride is very hard on the eyes and throat (hood).

@ Doc Bob: replacement and allosteric (as a WAG) ;^)

[Edited on 4-2-2016 by chemrox]

chemrox - 8-2-2016 at 16:23

uncorrected m.p. 252-3 for the HCl. soluble in hot 2-propanol further data indicates unlikely to be an agnonist/antagonist as the aniline version was

zed - 10-2-2016 at 13:04

I have a real aversion to needless killing. Killing always makes me sad, needed or not.

Still, stuff has to be tested. In China, I suppose the government would allow prisoners to take their chances. In fact, the way I remember it....we used to let prisoners take their chances here. I don't suppose it would be hard to get certain prisoners to volunteer

halogen - 10-2-2016 at 14:15

Medical ethics get complicated. While on the first look it's perfectly sane to experiment on a condemned man, especially in return for a pardon, the factor to be aware of is that this creates, potentially, and industry which brings with it an incentive. An incentive is one of the most powerful, subtle, perhaps insidious things you can create. I don't know if you read Freakonomics, but this is popular and amusing book which illustrates. In the case of the creation of an industry - a need for prisoners to test things on, people unconstrained by ethics (this is a phenomenon which exists!) will use deceit to create them for profit. As you can see, a perverse situation develops.

Another case of the principle in action is allowing prisons to profit from accumulating... accreting I should say, in the manner of a black hole... prisoners, which is puzzlingly only starting to gain public attention.

In the time of the kings, monarchs, nobility and so on, the lower classes were valued as dog food just about, even if they weren't criminals. So in old times the objection meant so little.

[Edited on 10-2-2016 by halogen]

zed - 10-2-2016 at 15:04

Ahh. I was cut off.

I meant to say: " I don't suppose it would be hard to get certain prisoners to volunteer, to test out opioids." Har, Har!

I can imagine lotterys and fist fights.... and long lines of hopeful volunteers.

Stuff leaves me cold. But, lots of folks live and die for the high.

Crap. What would you want a pardon for? Not a required incentive. Three squares, and being a subject for opioid testing? Some guys would be trying to get into prison, to get a deal like that.

halogen - 10-2-2016 at 15:37

Oh, I meant, and read, in place of execution, as in testing the toxicity up to fatal/near-fatal level as is done with rats, mice etc.

[Edited on 10-2-2016 by halogen]

JJay - 10-2-2016 at 15:39

Quote: Originally posted by chemrox  
Through methods I can't publish I have discovered that 4-anilino-N-phenethylpiperidine-2-furanamide is a partial mu agonist/antagonist that potentiates other mu agonist/antagonists such as buprenorphine and possibly etorphine. I don't care for killing mice. I left med chem for that reason (they were using dogs in my department). So how to publish the results or properly document.


I don't care for killing mice either, but if a few mice have to die to save a human life... it's a small price to pay. I'm not sure how valuable this compound is to medical science.

zed - 11-2-2016 at 15:06

Don't like the idea of using dogs in drug trials. Foremost, they aren't very much like us. Moreover, I like dogs, and after researchers have had their way with them, they aren't generally paroled....they are flushed.

I've always felt, there are an over-abundance of animal trials, to no great end. Were all of these trials designed to gain important information, they might be justified. Sadly, many animals are sacrificed, I mean tortured, for dubious reasons.

JJay - 11-2-2016 at 16:11

Quote: Originally posted by zed  
Don't like the idea of using dogs in drug trials. Foremost, they aren't very much like us. Moreover, I like dogs, and after researchers have had their way with them, they aren't generally paroled....they are flushed.

I've always felt, there are an over-abundance of animal trials, to no great end. Were all of these trials designed to gain important information, they might be justified. Sadly, many animals are sacrificed, I mean tortured, for dubious reasons.


I actually don't think there is an over-abundance of animal trials... there are shocking numbers of incredibly common compounds for which insufficient information is available to hazard more than a guess at LD50 and safe workplace levels. We don't even know for sure if styrene is a carcinogen. If anything, not enough animal trials are carried out.

On the other hand, there has been a tremendous amount of research on the effects of compounds with activity at mu opioid receptors, so I'm not sure there is any good reason for animal trials of the particular compound mentioned by the OP.