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Stimulants of the Future

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There are many very potent dopamine/monoamine reuptake inhibitors which have no recreational value whatsoever. Mazindole and bupropion are good examples. And just because a compound has a stimulant effect in mice or rats doesn't mean it has recreational value. I've made quite a few compounds which are stimulants for rodents but are useless for humans. Finding good new stimulants isn't as simple as it might seem.
 
I'm surprised nobody mentioned amfonelic acid yet. It's a well documented, potent stimulant. One publication even concludes that it's more addictive than morphine.
 
Finding good new stimulants isn't as simple as it might seem.

I totally agree. Deutsch predicts on the basis of discrimination ratios (binding affinity / uptake inhibition) that dichlororitalin is the most addictive of all ritalin analogs. However it could easily turn-out that dichlororitalin is a piece of shit, we just dont know that in advance on the basis of tests conducted on rats & theoretical models alone.
 
There are many very potent dopamine/monoamine reuptake inhibitors which have no recreational value whatsoever. Mazindole and bupropion are good examples. And just because a compound has a stimulant effect in mice or rats doesn't mean it has recreational value. I've made quite a few compounds which are stimulants for rodents but are useless for humans. Finding good new stimulants isn't as simple as it might seem.
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Well I'd geuss bup is no fun because it has slow distribution kinetics, and it is too DAT selective (and possible has too low SERT affinity)... While Madizanol, I'm not sure why it's not fun... maybe its TOO NET selective...

It would seem to me, that for a reuptake inhibitor to be fun, it needs to be quite equal SERT/NET/DAT...

While amphetamines need to be leaning towards NET/SERT.
 
I don't think it's a matter of selectivity. The best explanation I've found so far is this:

Mol Pharmacol. 1994 Feb;45(2):312-6.

Release of dopamine via the human transporter.

Eshleman AJ, Henningsen RA, Neve KA, Janowsky A.

Research Service, Veterans Affairs Medical Center, Portland, Oregon.

A human dopamine transporter cDNA was cloned and transfected into COS-7 cells, a cell line that lacks vesicular storage and release mechanisms. Cells expressing the dopamine transporter acquired the capacity to take up and release dopamine via the transporter. Ionic conditions that stimulate inside-out transport in vivo, such as depolarizing concentrations of K+ or low concentrations of extracellular Na+, were found to stimulate Ca(2+)-independent release of [3H]dopamine from transfected COS-7 cells. Dopamine uptake inhibitors had one of three effects on transporter-mediated efflux. Some drugs, in addition to inhibiting uptake, inhibited spontaneous release of dopamine. Drugs in this class included mazindol, GBR-12935, bupropion, nomifensine, and benztropine. All of the drugs with the potential for abuse by humans either enhanced release (methamphetamine, amphetamine, and ethanol) or had no effect on release (phencyclidine, cocaine, and WIN 35,428). The ability to define classes of uptake blockers based on their effects on human transporter-mediated dopamine efflux may lead to the identification of structural features of the transporter that differentiate abused from nonabused drugs.

PMID: 7906856
 
It would seem to me, that for a reuptake inhibitor to be fun, it needs to be quite equal SERT/NET/DAT...

While amphetamines need to be leaning towards NET/SERT.
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BilZ0r, I was under the impression that the affects on dopamine are the primary reason why amphetamines are "fun." Could you explain why you say that it "need to be leaning towards NET/SERT?"
 
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Because it seems that there is either low DAT expression and/or function in the prefrontal cortex.

Also, if you just block a single transporter, it seems that the monoamine is taken up by the others, you still get an increase, but not anywhere near as big.

Check out this little review on the subject.
 
bump

i heardd the wordd from da lord, and da lord said, fellow lord that mdpv stuff might return but there's probably a hundred DA uptake inhibitors possible that are selective and similar, but more euphoric and less higher dose side effects, and maybe easier and cheaper to make too. I'd eat some. Yum.
 
Riemann Zeta said:
Phenmetrazine is too hard to synthesize. It requires nor-ephedrine, which was banned in 2000. Same goes for 4-methylaminorex (4-MAX), which is why both are as rare as it gets in the drug world.
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Real pitty. I remember the day I went to he druyg store and the cold meds section was "missing". The day they pulled phenylpropanolamine off the shelves. I don't know why there wasn't more 4-methylaminorex on the market when PPA was so readily available. I guess there wasn't an easy synthesis known at the time. I've read that going by the same route, but using psuedo(ephedrine) produces an aminorex derivative that has some negative effects on humans. Does anybody know more about this? Because 4-methylaminorex is one of the easiest synths out there, if you have access to PPA/nor-ephedrine. And ephedrine is still readily available, it would be great if one could cyclize your ephdrine and make something effective and non toxic. I'm pretty sure that the synthesis wouldn't need any major tweaking to produce the (un)desired aminorex. I'm sure there are other people that have thought about many other aminorex analogues, probably largely academics. Personally, I would love something that lasted about 3 times less long than 4-mar. I remember one of the first times I took 4-mar (I don't know which isomer) but I was up for 3 days. One dose, no binging. There wasn't ever a second in those three days that I wanted to do more. There were times where I wished I had done less. but wow. Long lasting.
i think something that I'd like in a stimulant is the property like this: After your dosed, you can sleep after 3-4 hours. Cathinone is a winner for that one. Too bad you have to take so much of it.
 
Anyone have any info about the different isomers of 4-MAR and comparisons to their subjective effects? I tried the cis isomer a while back, thats one wierd stimulant... and yep lasts a looong time.
 
yaesutom said:
Anyone have any info about the different isomers of 4-MAR and comparisons to their subjective effects? I tried the cis isomer a while back, thats one wierd stimulant... and yep lasts a looong time.
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Yeah, I've got a link to some discussion about the different effects of the differing isomers. But the bookmarks aren't on the computer I'm on now. I'll send them when I have a chance. in this discussion they also discuss the ephedrine analogue of 4-mar. I know that's not very clear. basically they discuss what you would get if you substituted ephedrine for phenylpropanolamine. I'll look it up.
 
So I read through, and I really enjoyed this thread and the wonderful collection of knowledgeable folks here on bluelight... but, still, one nagging question remains...

h0w culd i make meth? & lsd???
 
watch said:
So I read through, and I really enjoyed this thread and the wonderful collection of knowledgeable folks here on bluelight... but, still, one nagging question remains...

h0w culd i make meth? & lsd???
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lol. you could not if you have to ask how.
i wonder how long you're going to stay here on bluelight 8)
 
It's a joke, my friend. I felt the thread was lacking without the "teach me how 2 make drugs" post.

It's a beautiful contrast, don't you think?
 
My dog mentioned to me that the vet prescribed her PPA pills for her uncontrollable bladder
 
Does anybody know N-Ethylamphetamin?Information appears extreme sparse on this one.
 
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