Conformationally Constrained Analogues of Stimulants?

[jahh]

And the N-ethyl group has the lowest toxicity/ highest theraputic ratio (N-methyl deriv of fcf is twicve the toxicity). The N-ethyl group is very popular in anorectic/stimulant compounds eg diethylpropion, fencamfamine, fenfluramine etc, so seemed like the natural choice if treating fencamfamine as the model for the drug

This one looks very interesting%) F&B!!
Is it worth a try?
Even just the cypenamine?

 

[fastandbulbous]

it does require higher doses than amphetamine which may be a problem in itself, I think there were some reports about it here.

Not exactly advanced, but my experience of N-rthylamphetamine is that it is incredibly smooth in action, but lacks a lot of methamphetamines crazy potential. It also has the weird property that the two optical isomers have different half lives yet the same activity. As to neurotoxicity, it's bound to have some asd the N-alkylated amphetamines all seem to have some serotonogic activity, though nowhere near that of meth.

Basically it's a very nice drug, shame it's a class C ion the UK.


On another topic, some of the constrained amphetamines look dodgy as fuck, like the isoquinolines (the amphetamine equiv being 3-methylisoquinoline)

 

[Limpet_Chicken]

Interesting about the half lives of the isomers.

Why is this, oh speedy, yet enlarged one?

And what of the isoquinolines?

 

[fastandbulbous]

Not a clue as to why isomers have different half lives. As to the isoquoinolines, I've read some ddgy toxicology reports of closely related compounds (hyperthermia seems to be a common theme to them)

 

[Limpet_Chicken]

Pretty common theme with all dopaminergic releasers isn't it? and I would guess at DARIs also, but not sure.

DARI/DRA activity seems to go hand in hand with noradrenergic activity usually, as well as the fact that DA gets metabolised eventually into NA, inducing vasoconstriction which whilst making one feel subjectively colder, would inhibit loss of heat through the skin surface due to less bloodflow, is there a central action at play there also with stimulant induced hyperthermia (excluding the serotonergics such as MDxx etc)?

Most stimulants seem to increase body temperature, is it particularly nasty with the isoquinolines? does this include diclofensine? that one looked interesting to me.

 

[hugo24]

Not a clue as to why isomers have different half lives.

Must be because they're different compounds

 

[fastandbulbous]

^ Slaps own forehead in a moment of clarity!

Actually it's probably because the size of the N-alkyl group starts to fuck with the action of the metabolic enzyme (a quick trial with N-propylamphetamine would confirm/deny this)