• N&PD Moderators: Skorpio | someguyontheinternet

best ratio of DA and NE reuptake inhibition for methylphenidate and related compounds

black53

Bluelighter
Joined
Oct 27, 2013
Messages
1,439
Does anyone know what ratio would give the most recreational compound?

https://pdfshare.it/doc/7HVZ4KBAM has numbers for methylphenidate, ethylphenidate a isopropylphenidate. IPH appears to be much more focused on dopamine than the other two. Which of these would you think would produce the most 'fun' compound?
 
Interesting. I've also heard that recreational potential depends on not only the binding of reinforcing agents, and not only on brain regions stimulated or depressed, but importantly on the ratio of chemicals released. I'm not sure people know just what ratio of sympathomimetic amines creates euphoria, though. I'd imagine it lies parallel or concurrent to the ratio and type released during sex, though.
 
Assuming you are just going to drink on ritalin to convert it to ethylphenidate, I wonder if using extended release methylphenidate would help. Since the dosages are released at specific times you could just drink as you knew you were getting the next dose. A 36mg concerta is pretty much like 2 20mg's except instead of lasting for 8 hours, it goes for about 10-12. It would be more of a way to "experiment," until you knew how to dose the alcohol in relation to the time.
image.cfm
 
Last edited:
Doesn't ethanol + Ritalin actually convert to the the mostly inactive isomer of eph anyway? No, I was thinking of the research chemical market. They are now selling ethylphenidate. Would isopropylphenidate give a better compound or not? The duration should be longer according to the paper, so that's a +. Now I'm just not sure about the DA/NE ratio. Could IPH actually be so bad at NE reuptake inhibition that it wouldn't be fun (I know you need some for a good stimulant). Going by feel, ethylphenidate would be better with less NE....

I've found some data for amphetamine type compounds, d-meth has a lot of DA and not much NE and is considered the most fun. But since these act in a different way I'm not sure you can compare it directly.
 
d-meth has a lot of DA and not much NE

Actually, even meth has greater activity at NET than DAT, but it is less selective for NET than amp...there aren't really yet selective DA releasers.

ebola
 
Any sources for that? Not that I don't believe you, but would like to see the numbers for others too.

Besides, I don't think the amphetamine and methylphenidate numbers can be directly compared anyway because they work differently.
 
You're correct, RTI-229 is a reuptake inhibitor. I realized that right when I posted, tried to delete the evidence before anyone noticed, and failed miserably :)

I don't know of any selective Dopamine releasers.
 
there is some study going on about propyl and isopropylphenidate, I will dig them up if I can find them, supposedly if my memory serves me correctly longer the chain the lower the NE re-uptake and the higher the DA:NE re-uptake inhibition becomes.

throw some dapoxetine (fast acting SRI) in with some ethylphenidate and you have a triple re-uptake inhibitor similar to cocaine( minus the sigma agonism and local anesthetic action) but without cocaine's specific cardio toxic effects via sodium channel inhibition ( please correct me on the Na inhibition if I am wrong)
 
http://www.freepatentsonline.com/63555656.html <--- that one talks about phenidates in general and their possibilities, the other is the same study you have, and I

believe there is one more floating out there, there seems to be quite a interest in ''substituted phenidates''. the one above is not that in depth, but I find a ton putting

isopropylphenidate or propylphenidate into any major search engine so


sorry the link above does not seem to take you to the same spot as typing it in a search engine, will work on it!!
 
The binding affinity data for isopropylphenidate look pretty good--with reuptake inhibitors, you want selectivity for DAT with SOME affinity for NET. RIs entirely selective for DAT are more compulsogens than euphoriants.

ebola
 
I've read that ethylphenidate is so appealing because it has a better ratio of less NE:more DE than methylphenidate - also of course because ethylphenidate is unscheduled.
 
It would be very interesting to have: pure powder/crystalline Ethylphenidate(99.8%+ purity D- isomer) NEXT TO-

pure powder/crystalline Methylphenidate(99.8%+ purity D-isomer) NEXT TO-

pure powder/crystalline isopropylphenidate(99.8%+ purity D-isomer)

And have a blind study administrating each at same dosages to see the subjective differences in ''recreational potential'' or euphoria, compulsive re-dosing ect.

To see what ratio of DAT/NET is the preferred say- snorted powder @ 20mgs for recreational purposes or ADD or studying
 
>propylphenidate
Apparently already tested by a few rc vendors and found to be worse than eph.

> Is it "so appealing" though? It's getting quite mixed reviews...
I think it's one of those things you either like it or hate it. I like it and get mostly just the positive effects, but others react differently.

T9358, bet you could get a lot of volunteers here :)
 
It would be very interesting to have: pure powder/crystalline Ethylphenidate(99.8%+ purity D- isomer) NEXT TO-

pure powder/crystalline Methylphenidate(99.8%+ purity D-isomer) NEXT TO-

pure powder/crystalline isopropylphenidate(99.8%+ purity D-isomer)

And have a blind study administrating each at same dosages to see the subjective differences in ''recreational potential'' or euphoria, compulsive re-dosing ect.

To see what ratio of DAT/NET is the preferred say- snorted powder @ 20mgs for recreational purposes or ADD or studying

You want to use equi-potent doses not equi-weight. If one was less potent than the others you would underestimate the recreational potential of that compound because you're relatively underdosing.
 
Ethylphenidate high to me is more enjoyable than the methylphenidate one for sure. The increased NA release causes more unwanted peripheral effects (heart rate/pressure). As for drinking on methylphenidate, I seem to remember reading somewhere that only a fraction of the methylphenidate is converted to ethylphenidate in the bloodstream... Regardless of whether this actually changes the active compound or not, having a few drinks with either makes for a much more enjoyable high with less edgyness (methylphenidate being worse for that than ethylphenidate).
 
The binding affinity data for isopropylphenidate look pretty good--with reuptake inhibitors, you want selectivity for DAT with SOME affinity for NET. RIs entirely selective for DAT are more compulsogens than euphoriants.

ebola

Not aware of any compounds with more DAT action than NET activity.
 
Top