• N&PD Moderators: Skorpio | thegreenhand

Why ARE ephedrine, cocaine, or amphetamines so much more potent than caffeine?

As caffeine is an adenosine antagonist, I'm curious about the effects of adenosine agonists alongside with stimulants/ephedrine/etc. Might be a stupid idea, but feel like potential of abolished anxiety stuff. The benzodiazepine antidote flumazenil is possibly only tolerable (it even aids somewhat against PAWS apparently) because it's an adenosine agonist too..

How long does coca tea last? Only 1-2h like cocaine or longer?
 
I haven't taken cocaine before but ADHD meds in America and ephedrine once from my bodybuilding friend. I have to say that it blows caffeine out of the water.

I might be suffering from sleep apnea/ADHD/narcolepsy so that's why caffeine doesn't work on me but compared to these two drugs, it's fucking shit. When I took Adderrall, I went 14 hours without feeling tired or taking a nap. This never happened on caffeine. I used to feel a bit energized and then fall asleep two/three hours later.
caffeine is a stimulant, not a drug.
 
Caffeine has kind of two main mechansims of action. Like ions said it is a purine, and it acts as an antagonist of the adenosine A2A receptors. These receptors normally mediate feelings of tiredness when activated, so blocking them causes wake fullness (this is different than stimulation, which comes from increased dopamine and norepinephrine signalling, which is the primary mechanism of action of all the drugs you listed.

Second caffeine is a phosphodiesterase inhibitor. When G alpha coupled g protein coupled receptors (such as beta adrenergic receptors or D1 dopamine receptors), the molecule adenosine mono phosphate (AMP) gets converted to cyclic adenosine mono phosphate(cAMP) by the enzyme adenylyl cyclase. cAMP acts as a second messenger sequential to (Gs) receptor activation, which activates many enzyme targets in the cell to exert it's effects. cAMP is broken down by phosphodiesterase, to terminate this signal (cells have loads of phosphodiesterases to break down a wave of cAMP, so that its timing is precise).

Caffeine inhibits phosphodiesterases that break down cAMP, so the effects of any Gs coupled receptor will be magnified. Some of the actual stimulation works through increasing the "gain" on existing norepinephrine and dopamine signaling.
Didnt know this so thanks
 
There were some more potent analogues of caffeine around, yet never had the desire to research them, sounds like jittery nightmare to me.. Ephedrine too is just different, not necessarily stronger as you can overdose on plain coffee too ... as has been said, these PEAs are different, working on different systems ... just that PEA itself gets immediately broken down by MAO-B so you need to add like an a-methyl in amph.

We have thingies like methylated aminorex derivates which blow amphs out of the water :)
I looked up methylaminorex, it said it was about equal to meth, what was your experience with it
 
I'm curious to know why the α-methyl group results in the substance bypassing MAO.
 
Theacrine should be incorporated into this conversation.





So you're saying ephedrine gives you anxiety, but caffeine doesn't? For me it's the opposite.

Theacrine wasn’t bad, I was actually fairly impressed with it. I’ve used it a number of times for the extra duration it provides.

-GC
 
I'm curious to know why the α-methyl group results in the substance bypassing MAO.

Easy answer: The enzyme catalyzes a specific reaction on a specific part of a range of molecules, and the addition of α-methyl changes the molecule so that this specific part no longer exists on the molecule.

In this particular case i think the enzyme needs an amine group connected to a methylene group, and the further branching of carbons changes this.
 
Theacrine wasn’t bad, I was actually fairly impressed with it. I’ve used it a number of times for the extra duration it provides.

-GC

Would you say the effect is more comparable to caffeine or to other stimulants?
 
Never having drank coffee n only having the odd cup of tea I don't have much experience with caffeine or needing a coffee upon waking to function.
I've drank red bull vodkas all night on nights out n felt wired n jittery from the caffeine overload. But I imagine if you were able to and brave enough to IV caffeine I think it would be up there with amphetamine in terms of a stimulating kinda high.

And to answer the question if ephedrine is euphoric an stimulating or just the latter in my experience (ex bodybuilder of over 20 yrs) its not at all euphoric its very stimulating and keeps you awake an alert but in terms of feeling great loving everyone an the world . Nope! I used to neck a few before a night out of id had a busy day/week at work to keep me awake which they did. Id still end up with a bag of coke alongside though
 
It's funny how variable this is. For me, caffeine, cocaine, and methylphenidate gave me jitters and anxiety and no positive feeling at all. But I always felt great on methamphetamine.
If you didn't test your cocaine, I'd say it's serotonin which makes the difference. Meth is a SNDRA (serotonin-norepinephrine-dopamine releaser) while methylphenidate and caffeine don't touch serotonin as well as cocaine cuts tend to be 'speedy' which means norepinephrine/dopamine focused. Meth indeed is nice the first times but when using daily the serotonin compound fades quickly, also it caused a strong rebound depression when stopping. That's the thing about serotonin, while e.g. dopamine is able to re-achieve homeostasis within a day or so, serotonin takes weeks.

I never really used cocaine because it's just too expensive for the short duration most of but the few samples I dabbled with were from the deep web, probably high quality and gave mostly a relaxed high but there are also heavily anxiety inducing 'cocaine' variants out there.

I fucking love aminorex variants. 4,4'-dimethylaminorex was great, this stuff inhibits its own metabolism by blocking MAO, which makes it as good as dangerous. Mephedrone wasn't bad as well, too a serotonin releasing agent. Then we have naphyrone, the serotonergic cousin of metyhlphenidate - its naphthyl moiety makes it a possible cancerogen, which might be the reason why it never got mainstreamed.

Yeah people IV at least meth and probably then amph as well but a good upper doesn't require needles to be good. Imho when you're chasing the initial rush instead of the high as such, you're lost.
 
You misinterpreted my above post. 'Can you IV pure amphetamine salts?' is just the title of the thread.
 
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