• N&PD Moderators: Skorpio

Propargyl beta phenylethylamine

Neuroprotection

Bluelighter
Joined
Apr 18, 2015
Messages
1,265
Selegyline and rasagyline are two substances that inhibit the enzyme MAOb, enhancing the concentrations of dopamine by preventing its breakdown and protecting nerve cells against toxicity by oxidation from free radicals produced by the breakdown of dopamine. However many of the more important benefits of these compounds such as life enhancement and neural protection are caused by activation of pro survival and antiapoptotic pathways in cells via the propargylamine group rather than enzyme inhibition.
I am suggesting adding a propargyl group to the 2phenylethylamine molecule in the same way that selegiline is synthesised from methamphetamine.
My knowledge of chemistry and pharmacology is poor but my hypothesis is as follows. This compound should have the same benefits as the previous mentioned substances and given its structure should be able to access Monoaminergic Neurons and inhibit MAOb inside them if it exists there. It should also lack the stimulant metabolites and therefore the side-effect profile of selegiline. In addition this substance that should be rather cheap in comparison to the very expensive rasagyline which is it self much better than selegyline.
What do you think of this, if it already exists please post any information on it.
 
You definitely don't want to take something that prevents apoptosis. That's a fast track to cancer
 
Youvknow very little about chemistry but you want to synth your own maoib inhibitor sounds beyond dangerous
 
No offense you seem to have very high logic and reasoning but making your own drug is like saying I studied music theory never played guitar in my life but I want to play like van halen or jimi hendrix on the first try. Just because you have fhe mental capacity to do something doesnt mean you can so easily just do it. And with this you cant mess up
 
Im confused so someone proposing adding a propargyl group to phenylethylamine sounds very specific to me to just ask for hypothetical no reason.
 
Ahh my bad lol I am a chemistry nerd so I read everything in a skewed way. Anyway did you see my link for the 1phenylethylamine version of your molecule. It looks like you have two possible versions where the nitrogen is in the one position and the one your prob thinking of in the two position
 
Anyway did you see my link for the 1phenylethylamine version of your molecule.

Simply cut the "address" of the image in question, and hit the faint picture of the tree with the four dots around the border above the box you type your responding thread message in (next to the film strip) and put that address there and the picture shows up:

330px-Pargyline.svg.png


So are we talking:

HgJl2B.jpg


or possibly:

beT652.jpg
 
Last edited:
I dont see no tree or film strip what am I doing wrong ? im on mobile quick reply
 
^ who knows? Mobile browsers vary in their interface a lot.

ff4c82c5eb.png


I'm pretty sure that second compound has been tried and tested during development of selegeline ?
 
I dont see no tree or film strip what am I doing wrong ? im on mobile quick reply

Ah, my assumptions again, on a desktop browser, specifically Firefox but I think most others (IE etc.) would be the same. Yes sekio is right, you might not have the ability from your mobile.

I'm pretty sure that second compound has been tried and tested during development of selegeline ?

Speaking of L-Deprenyl, they say D-Deprenyl is active on its own and not simply active as a prodrug to amp & m-amp, does anyone have the affinity/potency of D-Deprenyl without regard to its metabolites, or more likely available, potency in its over-all with (amp & m-amp) metabolites considered.

But this is a good segue into the SAR of this type of compound, namely because I think with how well m-amp is widely rated subjectively, that D-Deprenyl must be severely under-rated / overlooked.
 
Last edited:
If you are going to start making (and designing) your own drugs, and it *IS* a really, really interesting, fascinating and to boot, fucking well FUN thing to do, walk before you run, is my advice, start with something possessing less potential danger, produce a few analogs of known compounds and of course bury yourself deep deep deep, as do I, worming your way into pharmacology journals and textbooks. I look for everything, from psychedelcs to antibiotics to stimulants, sedatives and dissociatives. Dissociatives you must be extra careful with, as with if ever you seek them, methaqualone analogs, you do NOT want orthosteric NMDA, AMPA or kainate receptor analogs, allosteric modulators may be interesting, but glutamate binding site agonists are excitotoxic and permanently damaging. Avoid anything potentially MAOI and monoaminergic in the same molecule, there ARE exceptions to the rule that these are extremely dangerous and or outright poisonous, such as the weak MAO(a)I AMT, also quinol or quinone type monoamine derivatives, these, such as dihydroxydopamine, dihydroxytryptamines (even those not with with the two phenolic OH'es next to each other) and dihydroxyadrenaline or noradrenalines (having two OH on the Ph ring that is, not counting the sidechain here) these too possess potential for PERMANENT damage, things like 5,6 and 5,7-dihydroxytryptamine are used to selectively lesion animal brains as is the corresponding amphetamine and DA.
 
If you are going to start making (and designing) your own drugs, and it *IS* a really, really interesting, fascinating and to boot, fucking well FUN thing to do, walk before you run, is my advice, start with something possessing less potential danger, produce a few analogs of known compounds and of course bury yourself deep deep deep, as do I, worming your way into pharmacology journals and textbooks. I look for everything, from psychedelcs to antibiotics to stimulants, sedatives and dissociatives. Dissociatives you must be extra careful with, as with if ever you seek them, methaqualone analogs, you do NOT want orthosteric NMDA, AMPA or kainate receptor analogs, allosteric modulators may be interesting, but glutamate binding site agonists are excitotoxic and permanently damaging. Avoid anything potentially MAOI and monoaminergic in the same molecule, there ARE exceptions to the rule that these are extremely dangerous and or outright poisonous, such as the weak MAO(a)I AMT, also quinol or quinone type monoamine derivatives, these, such as dihydroxydopamine, dihydroxytryptamines (even those not with with the two phenolic OH'es next to each other) and dihydroxyadrenaline or noradrenalines (having two OH on the Ph ring that is, not counting the sidechain here) these too possess potential for PERMANENT damage, things like 5,6 and 5,7-dihydroxytryptamine are used to selectively lesion animal brains as is the corresponding amphetamine and DA.

Thanks for the advice. I was not really thinking of making this compound myself, but I can understand why you were a little concerned. It's funny you mentioned the weak MAOa IAMT, I think I came across it several days before seeing this post when researching tryptamine analogues. Is this the one with terrible effects at low doses and which has practically no euphoria?
 
I believe that would be 5-MeO-AMT. That sounds utterly vile.

AMT is, or can be a gem of a compound. Its essentially the tryptamine analog of amphetamine. And it is, in action in vivo with a human as the subject, a serotonin releaser (I'd guess, never looked it up or if I did I cannot remember, but thats unsurprising, I am to rain man what a pigeon is to design, construction and subsequent operation and maintenance of a thorium-cycle breeder reactor whilst riding a unicycle, masturbating and reading 'war and peace' backwards, transliterating it from the original russian to arafuckingmaic. By way of chinese. AFTER being decapitated, plucked, slathered in a bit of butter dressing b efore being out into an oven and having done to it what donald 'prize pillock' trump/fart/passage of gas through the anus derived from fermentative processes within the intestine/bronx cheer/guff desperately needs to have done to him for the good of all humanity and all politicians as well. God...its shocking isn't it, that a coarse, thuggish, greasy little dollop of foetid dog sewage could be voted in. Even if the alternative is hilary satan, shit, even the ambulant, by oozing, by extending amoeba-eque pus-pseudopods tide of Staph aureus& Streptococcus pyogenes-infested testicular pus dribbling from a necrotic knob sore on a paeophile infected with terminal politics.


Him, not even the strong entactogenic effects of AMT could make my (albeit [classic/aka 'severe' ewewewewwewwewew autism, the 'ew' being aimed at the term 'severe' its horrid] autistic wetware produce such as a fractional little shy, retiring, agoraphobic pathetic spineless squelch of an attomolar-sized squirt of oxyto(x/c)in for, if he were to be first forcibly made massively physically dependent on a huge dose of methadone, and fentanyl, tied by the wrists and first injected with a LOT of diprenorphine, slowly skinned alive, dusted with salt and calcium hypochlorite, before being dipped, millimeter by millimeter, feet first, into a large tank of concentrated caustic potash and left to shriek until either he had a fatal pulmonary haemorrhage from the effort of screaming or simply ended up liquifying high enough up until he got dipped far enough in that his abdomen corroded at a point where his organs could all drop out into the KOH:P

(NOT a happy bunny about that svinya winning. Thought of him with a thuggish meat-blob fist hovering over the nuclear button is a scary thought, and a nasty one too)


But, otherwise, AMT is both an excellent entactogen, of the MDxx type vein, 5-HT releaser, DA/NA releaser too, as well as a bona-fide 5HT2a agonist psychedelic. Not like how with MDMA one has strongly entactogenic effects with, especially at high doses, the beginnings of some trippyness. AMT is a full blown outright psychedelic that can knock your socks so jolly well far back off, that if a closet be open nearby, you've got one long ass trek through narnia to find them again. It is a powerful stimulant, and a long lasting drug in most of its respects, I'd say its (amphetamine like) stimulant effects are in my experience with using AMT, the longest, the psychedelic and entactogenic effects dropping off first, probably psychedelic effects first, then entactogenic, although its got a very long afterglow, and finally the stimulant effects.

Being the indolic analog of amphetamine, it IS amphetamine-like, there is bruxism, if not remedied, magnesium helps, and it goes lovely with a dash of an NMDA antagonist IMO, I LOVE it with methoxetamine or 4-methoxy-PCP. Very nice with some IV morphine now and then, and especially more opiates for the day or two after (I did say it was long. I've never yet had DOx, but its easily as long as I've read of DOM, DOB etc. lasting, and its a good idea to have a generous quantity available (whether or not one wishes to actually use any) of a nice strong sedative-hypnotic, a strongly hypnotic benzo, is a good choice, like nitrazepam. If it were me personally, PERSONALLY, and this is NOT advice, because it would be dangerous for most people, especially with opiates, and especially in someone who is not used to the drug and also on opiates longterm as am I, but the downer stack, opiates excluded that I choose if I may do so, is benzo-wise, nitrazepam first choice, if not, loprazolam (not lorazepam, I MEAN loprazolam) second choice, and chlormethiazole as its partner (its a barbiturate site agonist without the AMPA type glutamate receptor antagonist properties of barbs) and some MXE as dissociative, although I'd LOVE to try the combination using 3-hydroxy-PCP because the last, is a delightful dissociative. And some memantine dosed at the start due to its nice long duration of action to help nix the bruxism.

Its a full on psychedelic and can be rough going even strength wise, lower doses strongly stimulant still, pretty strong to moderate-strong entactogen and some medium psychedelia.

Best routes IMO are up the backside and up the schnozzle, best bypass the GI tract, I believe it a pretty strong 5HT3 agonist, this is the same target ondansetron is an antagonist at, the antiemetic, that is super super ripoff expensive for the NHS, wholesale pricing I mean, given usually as a surgical pre and post med to stop vomiting and aspiration whilst intubated, and mainly for cancer patients on the nastier chemo regimes. I get it on rx, although I have neither cancer nor am having surgery. And it is astonishingly powerfully effective. Its had me (when hospital gave it me IM once) from first vomiting my stomach contents out, liquid all out, acid etc. then vomiting, curled up in the foetal position in agony and unable to help myself refrain from screaming in pain, spewing bile, foam, billious foam and blood therein every 2-3 minutes or so, to sitting up and reading my hastily thrown together bag of scientific journal literature within the time it took for the IM dose to take effect.

And when I get GI issue flareups its even better than the only other of my large collection of prescription GI drugs to approach it in efficacy, cyclizine, and that when extracted, and plugged (I've yet to render my cyclizine HCl into an injectable prep), and even then ondansetron leaves cyclizine up the asshole sucking an ondansetron-shaped dust trail and the shockwave left behind in the wake of its sonic boom.

So presumably agonistic effects at the very much nausea-involved 5HT3 receptor are in a large part responsible for the gutbuster potential, especially in high doses for AMT. Best taken up the ass, it really is. Snorting works but stings and leaves you with a clogged nose later. Although a squirt or two of xylometazoline locally acting nasal decongestant (its a vasoconstrictor acting on adrenergic receptors.) reverses that pretty thoroughly, makes things a lot more comfy both after taking the AMT up the snout and later on now and then too.

Entactogen-wise, this is the drug, that in combination with low-dose (compared to the doses of AMT I was using) helped me address my at the time pretty severe PTSD. I won't go too far into why I ended up with it, for it could and would compromise my security)

I think, due to some of its effects when I've had it not exactly on its own, but whilst on opiates and the daily doses of chlormethiazole I take for seizure prophylaxis without at the time dropping extra of either, so am used to and not overly sedated by these. But I MUST have a portion of both to prevent withdrawal and seizures respectively.

I've had strong doses of AMT, despite being powerfully stimulant, also be strongly drowsy and delightfully mongy and sedate-ey, not hypnotic just munty stuff, drowsy and languid in the extreme, so I believe its probably quite a powerful 5HT releaser. Not looked at the numbers recently. A weak inhibitor of MAO-a and is one of those drugs that like tramadol (with which this stuff should NEVER be combined, could be dangerous, likewise DXM and wouldn't suggest people drop pethidine on it either.
 
AMT has been shown to act as a serotonin releaser. It is sort of the tryptamine equivalent of MDA, with alpha-ethyltryptamine being the tryptamine equivalent of MDMA. AMT is, however, much more psychedelic than MDA, but they have the same basic mechanism-of-action.

Its not clear how much MAO inhibition contributes to the effects of AMT. It can't be that important, otherwise AMT would tend to cause serotonin syndrome.
 
Top