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Stimulants of the Future

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I suspect that without closing off the ring and getting propylhexedrine, you can't get better.
 
4-methylpentan-2-amine may be an active analogue.

n-methylgeranamine might be interesting, who knows.
 
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I got this idea for a stimulant/opioid. It resembles fencamfamine, but also fits to the morphine rule. Anyway, it's synthesis should be entirely possible.
 
Without the methylamine on the side it would just be a mPPP-type opioid. By adding the methylamine it resembles fencamfamine, with the norbornan changed into an azabicyclooctane and methyl instead of ethyl on the amine.

Ever since I first heard about Lefetamine I have been intrigued by the idea of a drug that would be a stimulant and an opioid agonist at the same time...

But yeah, what about the toxicity? What makes you think so?
 
MPP+ proper? Probably not. An N-methyl derivative, quite possible. An analogue with the ring opened and then fully saturated (as with MPTP --> MPP+), seems possible.

4-phenylpiperidine derivatives aren't smart to be ingesting, imho. The 4-phenyl-4- ester piperidine analogues are much safer. But bingo- they're already DARIs with opioid affinity.
 
Well, check out the ring structure of the azabicyclooctane... It's quite different from piperidine when you look it in 3d. It kinda looks like a bird cage. To me it looks like a stable molecule, there shouldn't be too much strain to force it to open... however this is just a gut feeling. Someone should look into the metabolism of azabicyclooctanes.

Actually, I just did, a bit... I found a drug, azasetron, which contains the same ring structure, azabicyclooctane, and by everything I read the only metabolism that occurs on the azabicyclooctane ring is N-oxidation of the tertiary amine. Nothing I read indicated that the ring structure would open or metabolize into something harmful.

Azasetron:

220px-Azasetron.png
 
a quaternary amine is exactly something dangerous with that motif. Gets passed the BBB, then is metabolized and can't get back out.

That's exactly what makes dangerous.

It might be totally fine- it's just a matter of whether or not the quaternary amine analogue of that structure would have similar neurotoxic effects. It's quite possible, and I think you'd be hard pressed to find anyone willing to risk that on themselves.

Considering that rodents aren't a viable research subject, you need primates. Makes it rather difficult to test this.
 
Well the structure is actually quinuclidine, which from memory is not subject to any sort of ring opening. Also, I'd imagine most people can think of at least one drug containing a quinuclidinyl structure ie BZ aka 3-quinuclidinyl benzilate
 
dread said:
fcanalog.gif


I got this idea for a stimulant/opioid. It resembles fencamfamine, but also fits to the morphine rule. Anyway, it's synthesis should be entirely possible.
Click to expand...

Not really as fencamfamine is an alicyclic compound (non-aromatic ring structure) whereas quinuclidine is a heterocycle (ring structure containing a non carbon atom) and as such a lot more different. Also, just because it fits the 'morphine rule' doesn't mean that it's a mu receptor agonist. There is a quinuclidine based stimulant, namely 3-phenyl-2-methylquinuclidine, which is a dopamine reuptake inhibitor (basically in essence a phenmetrazine type of analogue)
 
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