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Stimulants of the Future II

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Every DAT re-uptake inhibitor that I have been able to get the pharmacological information on about it shows a greater NET re-uptake inhibitor affinity than DAT; has this been an unbroken rule? That every DAT re-uptake inhibitor universally is stronger at inhibiting the re-uptake of NET?
 
That is not true. Cocaine has a higher affinity for the DAT than it does the NET.

The case of ultra potent phenyltropanes are an even better example, such as this:

220px-Beta-CIT.png


Perhaps you are talking about release agents....
 
I was thinking of making arecoline from niacin (vitamin b3) not too long ago, sort of as a cognition enhancer. But, I have neither the reagents (aside from vit.b3) nor the expertise...
 
I was actually wondering about the potential for new nicotine, arecoline and anabasine-like chemicals as stimulants. I imagine something cocaine-like could come up. As far as I know, most of the research on nicotine analogues has been focused on their potential as insecticides.

The problem with things that work on that sort of cholinergic mechanism though is that they have to have a pretty high affinity for the brain, or else they can be very poisonous.
 
N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate: whats the chance of this having opioid binding?
 
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I'm wondering... l-tyrosine can be made extremely simply into tyramine, and tyramine is supposedly a DE/NA releaser albeit one that can't cross through the BBB due to the polar -OH group. And it survives MAO long enough apparently unlike say phenethylamine.

But what if you alkylate that hydroxy group (easy enough, look up williamson or something) to get something along the lines of 4-ethoxy phenethylamine or something? Or even acetic anhydride to get 4-acetoxy phenethylamine? I think those would be potent enough very easy to make stimulants.
 
what is it with converting amino acids and related amines into drugs? Here's a thought, why not decarboxylate tryptophan, and dimethylate the amine...
 
Nibiru said:
I was actually wondering about the potential for new nicotine, arecoline and anabasine-like chemicals as stimulants. I imagine something cocaine-like could come up. As far as I know, most of the research on nicotine analogues has been focused on their potential as insecticides.

The problem with things that work on that sort of cholinergic mechanism though is that they have to have a pretty high affinity for the brain, or else they can be very poisonous.
Click to expand...


Like remove the carboxylic acid ester part of arecoline & you have MPTP 8o

PS Do I have to remind everyone about no synthesis discussion?
 
You forgot about the phenyl ring. That makes quite a bit of difference.

It seems that there are about three different people here who can get whatever they want while everyone else can take what they can get.
 
So have there been any known synthetic stimulants made that work as muscarinic acetylcholine agonists like nicotine and arecoline do? All I ever find any info about is stuff like imonocarpid, which is a lot more toxic than what I'm wondering about.

I imagine there might be potential for a super-addictive euphoriant stimulant coming out of that category. Knowing well how bloody horrible both tobacco and betel can make me feel, I'd be pretty wary of trying any of it, though.
 
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