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  • BDD Moderators: Keif’ Richards | negrogesic

Stimulants Caffeine blocks GABAa receptors?

The Holy Quadruplty

The Holy Quadruplty

Bluelighter
Joined
Feb 9, 2022
Messages
660
I read that caffeine blocks GABAa receptors, and here's some of what I read...

with several mechanisms of action, such as non-selective antagonism of adenosine receptors, as the high-affinity A1 and A2A adenosine receptor (A1R and A2AR) subtypes, inhibition of cyclic nucleotide phosphodiesterases, mobilization of Ca2+ from the sarcoplasmic reticulum or inhibition of its reuptake, inhibition of monoamine oxidase and cyclooxygenase enzymes, and blockade of GABAA receptor.

Then I read that caffeine potentiates the release of GABA. So I'm confused, and would it effect my benzos at all? For the last couple years I've been trying to stay away from Caffeine, because of it's Adenosine antagonist effects, but haven't read that Caffeine blocks GABAa receptors that I can remember atleast.

What do you guys think about this? Does anyone know what caffeine really does to GABAa receptors?
 
Caffeine has an affinity for the gaba receptor. It acts as an antagonist, making the Gaba receptor not work as well when it is bound to the receptor. This means theoretically over time, with a high enough dose, caffeine upregulates GABA receptor density; which should make gabaergic function more sensitive to Gaba agonists and positive allosteric modulators.

In reality, it's not going to quite work that way. It would take a lot of caffeine, all the time, because it's not a significantly powerful antagonist.

What it doesn't mean is that caffeine stops Gaba agonists or positive allosteric modulators from affecting GABA receptors.
 
Ive tried reading about this for hundreds of hours and am just as confused as when I started.

The biggest things I found is caffeine gets metabolized to paraxanthine which is similar to caffeine changing my dosing timing

Adenosine prob main mechanism

Pdei might increase effects at very high doses via gaba interneuron and cgmp signaling in the striatum

Idk gaba interneurons and cgmp are beyond me good luck lol

I used Google scholar.
 
paranoid android said:
Ya me to i like having my clonaz with my morning cofee. Relaxes me and helps me focus
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That's because it's not very competitive.

You have to understand how they identify positive allosteric modulators of receptors and agonists of receptors. It's basically an evaluation of if they activate or change the receptor at all, it's not necessarily to the degree. For that you have to look at the binding affinities and a bunch of other stuff.

And it might be the case that the dosage of caffeine necessary to evidence the behavior they're talking about maybe higher than the LD50 of caffeine's in humans. I'm not sure that's the case, but it could be.
 
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shugenja said:
This means theoretically over time, with a high enough dose, caffeine upregulates GABA receptor density; which should make gabaergic function more sensitive to Gaba agonists and positive allosteric modulators.
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But not really if you are also on a high enough dose of gabanerics at the same time right? Theoretically.
 
Pissed_and_messed said:
50/50 love/hate
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Same.

I love it so long as I keep it to once in awhile. Soon as I start to use it daily it makes my life hell. I’ll be craving it and then once I drink it, makes me hazy, unmotivated and later I crash. Actually finally got free of that demon again. Been caffeine free for months now besides a couple cups.

-GC
 
G_Chem said:
Same.

I love it so long as I keep it to once in awhile. Soon as I start to use it daily it makes my life hell. I’ll be craving it and then once I drink it, makes me hazy, unmotivated and later I crash. Actually finally got free of that demon again. Been caffeine free for months now besides a couple cups.

-GC
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I think one cup puts you back to starting blocks but not sure.
 
pretty much. if not completely, I am then guaranteed to drink 5 of next 7 days and then it gets pretty hard to quit anymore.
 
new2drugs said:
Caffeine is a nice drug. Who else likes it?
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I hate caffeine, it comes with huge promises but delivers next to none. I instantly believe that it's a GABA antagonist, feels like one. Jitteryness, nervousness and a little wakefulness is all I get. Unfortunately it's the only stim I have readily available at the moment so I'm still drinking the occasional coffee ☕.
 
plumbus-nine said:
I hate caffeine, it comes with huge promises but delivers next to none. I instantly believe that it's a GABA antagonist, feels like one. Jitteryness, nervousness and a little wakefulness is all I get. Unfortunately it's the only stim I have readily available at the moment so I'm still drinking the occasional coffee ☕.
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I was told that one cup of coffee is worth about 3 teas in terms for caffeine strength.

I like a coffee when I'm out walking
 
new2drugs said:
I was told that one cup of coffee is worth about 3 teas in terms for caffeine strength.
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Possible. I always found tea 🍵 to be weaker than coffee. Some say it was due to the additiona l-theanine in there but I did multiple grams of l-theanine without feeling anything so I doubt it.

new2drugs said:
I like a coffee when I'm out walking
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I like a dissociative when I'm out walking xD
 
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