Ethcathinone

[Ham-milton]

ethylamphetamine has to have less neurotoxicity than amphetamine proper.

Are there any papers discussing the neurotoxicity issues with the various 4-subbed amps like PCA, PMA, 4FA. It's my understanding that 4-methylthio-amphetamine blows even PCA out of the water in this respect. No?

 

[hussness]

How is the ability of a drug to function as a monoamine transporter substrate quantified? Is it by competition with labeled DA, NE, or 5-HT? I know that DAT blocking can be measured by competition with a high-affinity ligand, but since substrates for these transporters need to have moderate affinity how is this measured?
I remember F&B speculating that part of the reason why fencamfamine was such a nice stimulant was because it had a near perfect substrate to reuptake inhibitor ratio. I did a brief scan for literature and haven't come up with anything. Any thoughts?

 

[immad]

Zombie bump, but does anyone have some more data on the neurotoxicity of ethcat?

 

[tadfish]

I very much like it. You can snort, smoke and eat it. What dose's ya all using?

 

[tadfish]

does it turn into cathinone in ya stomach?

 

[fastandbulbous]

I've been wondering in what way ethcathinone affects the brain, if it's a releaser and reuptake inhibitor like plain cathinone and methcathinone seem to be or if it's mainly a reuptake inhibitor, like wikipedia seems to suggest? As a novice, I don't really believe that sticking one extra CH2 at the methyl destroy's the releasing properties of MCAT.

Here's some figures from a paper (Monoamine transporters & psychostimulant drug, Eur J. Pharmacology; 479(1-3): 23-40)

Laid out as follows

Drug/DA release EC50/DA reuptake inh Ki/NE release EC50/NE reuptake Ki/5HT release EC50/5HT reuptake Ki (all figures in nM)

N-ethylcathinone/>1000/>1000/99.3/360/2118/3840

Diethylpropion/>10000/>10000/>10000/>10000/>10000/>10000/

and for comparison

(+)Amphetamine/24.8/34/7.1/38.9/1765/3830

(+)Methamphetamine/24.5/114/12.3/48/736/2137

 

[shibireru]

Here's some figures from a paper (Monoamine transporters & psychostimulant drug, Eur J. Pharmacology; 479(1-3): 23-40)

Laid out as follows

Drug/DA release EC50/DA reuptake inh Ki/NE release EC50/NE reuptake Ki/5HT release EC50/5HT reuptake Ki (all figures in nM)

N-ethylcathinone/>1000/>1000/99.3/360/2118/3840

Diethylpropion/>10000/>10000/>10000/>10000/>10000/>10000/

and for comparison

(+)Amphetamine/24.8/34/7.1/38.9/1765/3830

(+)Methamphetamine/24.5/114/12.3/48/736/2137

Ewwwwww.... Fucking worthless serotonin. That shit doesn't do ANYTHING useful near as I can tell (unless you dislike having emotions and a libido).

So, is this why amphetamine is such a worthless aphrodisiac for me? It actually diminishes libido when I take it.

/BTW, what's the standard recreational dose? Maybe that's my problem. The most I've taken at any one time was 15 mg of dextroamphetamine. I couldn't go any higher because it makes me extremely aggressive and irascible; I found myself screaming at people, especially my father, at the top of my lungs. Then there's the anxiety, edginess, increased apathy and dysphoria, insomnia, confusion, increased competitiveness, decreased working memory capacity, poorer word recall, and generally just decreased intellectual capacity... (I have a little baseless pet theory that says that amphetamines and so-called "amphetaminergics" produce little to no recreational effect unless mu-opioid receptors are already being stimulated to a considerable degree - that is, that they synergistically produce euphoria.)

 

[shibireru]

Okay. I'm going to go to harm myself by taking a randomly large dose of my dexies here, if you don't answer my questions soon.

Reduce my harm!

 

[nuke]

Ewwwwww.... Fucking worthless serotonin. That shit doesn't do ANYTHING useful near as I can tell (unless you dislike having emotions and a libido).

So, is this why amphetamine is such a worthless aphrodisiac for me? It actually diminishes libido when I take it.

Those are EC50 values.

The term half maximal effective concentration (EC50) refers to the concentration of a drug or antibody which induces a response halfway between the baseline and maximum.[1] It is commonly used as a measure of drug potency.

So lower amounts refer to greater amounts of potency in those areas. This makes ethcathinone a poorer serotonin releaser than amphetamine (but higher doses of ethcathinone are usually required).

It's interesting that we found a selective NE releaser/reuptake inhibitor and people like it so much!

 

[tadfish]

Here's some figures from a paper (Monoamine transporters & psychostimulant drug, Eur J. Pharmacology; 479(1-3): 23-40)

Laid out as follows

Drug/DA release EC50/DA reuptake inh Ki/NE release EC50/NE reuptake Ki/5HT release EC50/5HT reuptake Ki (all figures in nM)

N-ethylcathinone/>1000/>1000/99.3/360/2118/3840

Diethylpropion/>10000/>10000/>10000/>10000/>10000/>10000/

and for comparison

(+)Amphetamine/24.8/34/7.1/38.9/1765/3830

(+)Methamphetamine/24.5/114/12.3/48/736/2137

I would like to see those for all those cathinones like 4mmc and methylone and ethylone. pls

 

[shibireru]

So lower amounts refer to greater amounts of potency in those areas. This makes ethcathinone a poorer serotonin releaser than amphetamine (but higher doses of ethcathinone are usually required).

Okay. I figured that that might be the case, since everything I've read suggests amphetamine to be only modestly serotonergic. Sorry for being such an ignorant asswipe.

It's interesting that we found a selective NE releaser/reuptake inhibitor and people like it so much!

That is interesting.


Thanks for indulging me who don't really belong in ADD with my idiotic questions and complete ignorance. (I don't feel that I quite belong in BDD, either, though.)

 

[immad]

Here's some figures from a paper (Monoamine transporters & psychostimulant drug, Eur J. Pharmacology; 479(1-3): 23-40)

Laid out as follows

Drug/DA release EC50/DA reuptake inh Ki/NE release EC50/NE reuptake Ki/5HT release EC50/5HT reuptake Ki (all figures in nM)

N-ethylcathinone/>1000/>1000/99.3/360/2118/3840

Diethylpropion/>10000/>10000/>10000/>10000/>10000/>10000/

and for comparison

(+)Amphetamine/24.8/34/7.1/38.9/1765/3830

(+)Methamphetamine/24.5/114/12.3/48/736/2137

Thanks a lot, I guess that implicitly answered my question. Is it safe to assume that ethcath isn't neurotoxic, since dopamine isn't boosted, so it's highly unlikely that dopamine is take up by serotonintransporters when serotoninlevels are low (MDMA like neurotoxicity)? No dioxy-metabolites either.

Those are EC50 values.



So lower amounts refer to greater amounts of potency in those areas. This makes ethcathinone a poorer serotonin releaser than amphetamine (but higher doses of ethcathinone are usually required).

It's interesting that we found a selective NE releaser/reuptake inhibitor and people like it so much!

Indeed, it's pretty strange. I remember it to be not that bad at euphoria. Not as good as for example cocaine and more "wired" in the body, but quite pleasant overall.

 

[tadfish]

Whats everyone dose for this i wondering cause i have high tolerance and don't want to have heaps and have too much cause i dind't get the effects my mate was asking how much should he have and he is a lightweight i was saying i think 50mg nasal and 100mg orally. But he didn't trust me cause of massive amounts of stuff i take and my crazy ways.

Anyone found this goes well with any other caths? maybe a combo with 4mmc might be really good.

 

[fastandbulbous]

^ Dont know about nasal as nothing goes up there (except my finger! ), but rectally I've dosed at between 50-100mg; 100mg was a bit much (churning guts), but 50 & 75mg were quite good. Orally I'd say 75-150mg depending upon body weight, but as the most I've ingested orally is 120mg, I can't vouch for 150mg not giving a bad gut

PS I seem to require larger than average doses of stimulants due to weight (90kg) & from years of (ab)using them,

 

[nanobrain]

seems to be sex-specific d/r-wise. in general, females appear to be at least 3x more sensitive and comment on its entactogenic and euphoriant properties...

 

[nuke]

This compound may be neurotoxic as well. Apparently it is the metabolite of Diethylpropion that likely most contributes to the 5HT toxicity of the drug.

 

[Refluxer]

Nuke: Can you please elaborate? That comment was not very meaningful.

 

[nuke]

Nuke: Can you please elaborate? That comment was not very meaningful.

Diethylproprion is a poor stimulant in and of itself (in fact it has no DA/NE/5HT releasing properties and high micromolar reuptake properties). It's theorized that Ethcathinone is the active metabolite, as the other metabolites are very poor reuptake inhibitors/releasers.

I had thought I recalled it was a 5HT-styled neurotoxin, but all I really have to go on the neurotoxicity aside from a study not particularly revealing from Ann N Y Acad Sci. is the Wikipedia entry for DEP which claimed that in unpublished data the stimulant was neurotoxic. It would actually be a very interesting thing if it caused NE or 5HT (or even DA) neuronal toxicity as it's not a DA releaser.

I guess it'll remain a mystery for now unless someone can come forth with the data.

 

[Solipsis]

I find ethcathinone to be smooth as hell, somewhere it reminds me a bit of dexamphetamine.
In any case I agree stuff like MDPV and also alpha-PPP (both pyrrolidines) are much more yucky and I am not likely to every try one of those again.
It is in a way compelling to take it once more if you get the hang of it (doesn't take long either). I'd suspect it to have something to do with the brains reward center and the fact that NE levels are heightened? This is pretty much saying it's addictive, it probably would be even much more so if it were more rushing. It's satisfactory, I might have ordered it again if a source hadnt dried up.

 

[tadfish]

yeah i find ethylcath was pretty safe on the mind and body, well didn't notice much side effects compared to other stims.