Amiflamine: Enctactogen with little tolerance

[MephedroneCandy]

The serotonin receptors required for the entactogenic effect do not generate much tolerance by themselves. Tolerance of entactogens is given by the depletion of serotonin reserves.

In addition to releasing serotonin and norepinephrine, amiflamine inhibits MAO-A avoiding the degradation of serotonin and giving the same effects as MDMA by releasing much less serotonin.
In addition, a useful peculiarity of the molecule is that of being selective for the MAO-A present in the surroundings of the serotonergic axons, not increasing the concentration of norepinephrine very much. This is a good thing because when I tried to inhibit MAOA with a selective inhibitor (methylene blue) I got effects that were attributable to excessive increases in norepinephrine relative to serotonin (although the serotonergic effects were also increased). In fact, MAO-A degrades much more norepinephrine than it does serotonin.

All this I think makes this molecule an excellent entactogen without too much tolerance or hangovers. Definitely on the list of molecules to try.

It must also be said that combining SRAs and MAOIs can cause serotonin syndrome, but since here the effects are all obtained with just one molecule, the risks are less since it is necessary to adjust the dosage of a single molecule, instead of finding the right ratios and the molecules with a compatible half-life between them.

 

[Skorpio]

I don't buy that it is safe. See 4-mta (flatliners), pma, 4-ma, shit even the 2CTs are way more dangerous than the non-MAOi compounds.

Also if it is more of a serotonin releaser than dopamine and norepinephrine, it will probably be quite mellow like mdai.

In general, I would need a lot of data to not view this drug as toxic.

 

[plumbus-nine]

Reminds me of 4,4'-dimethylaminorex, which too is a MAOI and SNDRA and caused substantially less tolerance than your usual empathogen would. I loved this stuff. Wonder about its safety but I had some residual venlafaxine in my system when I took the first dosage (back then nobody knew it was a MAOI) and I'm fine.

 

[MephedroneCandy]

Reminds me of 4,4'-dimethylaminorex, which too is a MAOI and SNDRA and caused substantially less tolerance than your usual empathogen would. I loved this stuff. Wonder about its safety but I had some residual venlafaxine in my system when I took the first dosage (back then nobody knew it was a MAOI) and I'm fine.

Where can I find the pharmacology of 4,4'-DMAR?

 

[MephedroneCandy]

I don't buy that it is safe. See 4-mta (flatliners), pma, 4-ma, shit even the 2CTs are way more dangerous than the non-MAOi compounds.

Also if it is more of a serotonin releaser than dopamine and norepinephrine, it will probably be quite mellow like mdai.

In general, I would need a lot of data to not view this drug as toxic.

Reading the reports 4-MTA and similars are responsible for deaths just because you can overdose them easily since you have infinite amount of serotonin available and so you have serotonin syndrome. But this same mechanism gives you a lot of benefits as written in the first post. With great power comes great responsability. One just needs to be responsible about the dosage.

I think it is fine if casual drug users that just wants to party some random night take MDMA since they can be irresponsible and MDMA is kind of safe if you overdose on it. But if an experienced user that knows safe practices etc... wants a drug that if used with caution has a better profile than MDMA, here is the answer.

 

[negrogesic]

I very much doubt the subjective effects resemble anything like the effects produced by MDMA, so I don't think "better profile than MDMA" is meaningful here.

Selective serotonin release are no fun, I learned that though my experiences with 4-fluoroethamphetamine. Produces a cold, somewhat empty feeling state. Without dopamine release these compounds are not enjoyable, and definitely cannot be compared to MDMA.

 

[plumbus-nine]

Where can I find the pharmacology of 4,4'-DMAR?

I think I read about it here on bluelight. Don't know where to look for pharmacology of rare compounds unfortunately.

But yeah if it's a selective serotonin releaser then this one won't be that enjoyable.

 

[MephedroneCandy]

It is noto so selective it also releases dopamine and noradrenaline. I want to find a SNRA with RIMA priorities to combine it with an allosteric D1 modulator.

 

[Skorpio]

I want to find a SNRA with RIMA priorities to combine it with an allosteric D1 modulator.

This is a bad idea, but I'm just on the Internet and can't force you to not do this.

Anybody else reading should be aware that serotonin releasers which inhibit MAO-A have much steeper dose response curves and are generally known for causing death.

 

[Fertile]

If memory serves, the first MAOIs were actually developed as a treatment for tuberculosis (when the outlook for sufferers was very poor) and researchers noted that while they were ineffective as antibiotics, many depressed patients saw their mood elevated.

The takeaway being that it was only accepted for the treatment for a disease that was likely to be fatal.

Abuse of DLRs seems like a bad plan. It's not as if acquiring better alternatives is a bit issue, is it?

 

[simstim]

According to a SAR study that I read beta ketone or beta methoxy substitutions greatly reduced maoi activity.

So perhaps the n-methylcathinone of amiflamine would be of value.

 

[plumbus-nine]

Anybody else reading should be aware that serotonin releasers which inhibit MAO-A have much steeper dose response curves and are generally known for causing death.

We have somebody here (always forgot the names) who binged 1g of 4,4'-dimethylaminorex in one night and is fine. Sheer luck? I know this substance had a death toll but I'm wondering why it appears to be safe unless combined with other SNDRA.

 

[Fertile]

Well, to be clear, it's more accurately p,4-dimethylaminorex. It was on the market for a while as 'Serotonia'. Now that p-Me provides a sacrificial moiety. It's required to make it selective to the SERT pathway and it's also easy for non-specific blood enzymes to oxidise. So yes, given that it's duration is about 4 hours rather than 16 hours, I can readily see someone taking 166mg every 4 hours.

When you put it that way, it isn't quite as crazy. Still not a GREAT idea.

But of the class, methylenedioxyaminorex is known and indeed is in the original patent of the aminorex class by George Ireland Poos.

We messed around and found that 80mg of p-Me aminorex + 40mg of m-me aminorex was a very good entactogen.

 

[fastandbulbous]

Well, to be clear, it's more accurately p,4-dimethylaminorex. It was on the market for a while as 'Serotonia'. Now that p-Me provides a sacrificial moiety. It's required to make it selective to the SERT pathway and it's also easy for non-specific blood enzymes to oxidise. So yes, given that it's duration is about 4 hours rather than 16 hours, I can readily see someone taking 166mg every 4 hours.

When you put it that way, it isn't quite as crazy. Still not a GREAT idea.

But of the class, methylenedioxyaminorex is known and indeed is in the original patent of the aminorex class by George Ireland Poos.

We messed around and found that 80mg of p-Me aminorex + 40mg of m-me aminorex was a very good entactogen.

Mixtures can work, but playing around in the dark can result in people ending up with toe tags.
The one Ifound useful was IAP and amphetamine (pref dexamphetamine); well until IAP became a class B...

 

[fastandbulbous]

If memory serves, the first MAOIs were actually developed as a treatment for tuberculosis (when the outlook for sufferers was very poor) and researchers noted that while they were ineffective as antibiotics, many depressed patients saw their mood elevated.

The takeaway being that it was only accepted for the treatment for a disease that was likely to be fatal.

Abuse of DLRs seems like a bad plan. It's not as if acquiring better alternatives is a bit issue, is it?

Nicotinic acid hydrazide, as I recall

 

[Fertile]

Every time I play a king, you play an ace.... damn you Geordie* chemist.

*I don't know if that's the correct term.