"The Holy Quadruplty"

[Skorpio]

Xanax is a GABA A positive allosteric modulator. It binds to a site on the receptor that causes the receptor to have a higher affinity for, and a higher response to the neurotransmitter GABA. This results in increased GABAergic signaling when alprazolam is bound.

Without any GABA, alprazolam will not cause any receptor activation.

An antagonist will block the binding of GABA, which will therefore result in a blockade of alprazolam's potentiation of GABA A signaling.

 

[plumbus-nine]

Not what I've read and saw, but I also heard that as well. I also heard lyrica doesn't bind to GABA at all just voltage gated calcium channels making more GABA essentially.

Pregabalin (Lyrica) induces an enzyme which converts glutamate into GABA and this makes it an indirect agonist. As the dosage increases, it also blocks glutamate reuptake, which mediates its stimulatory activity. The alpha2delta Ca channels are a subunit of NMDA ones btw which makes pregab an indirect dissociative as well. Just that the brain seems to react to this exceedingly fast, the tolerance is worse than any other drug and withdrawal feels like a mild narcotic WD.

Xanax was shown to be a dopamine D2 agonist as well, which makes it less sedating than other BZDs. Yeah, these are GABA-A PAMs.

 

[The Holy Quadruplty]

I think that's how you spell it, and what's it's called. The opioid growth factor like receptor 1 or something like that. Does anyone know anything about it?

 

[The Holy Quadruplty]

Pregabalin (Lyrica) induces an enzyme which converts glutamate into GABA and this makes it an indirect agonist. As the dosage increases, it also blocks glutamate reuptake, which mediates its stimulatory activity. The alpha2delta Ca channels are a subunit of NMDA ones btw which makes pregab an indirect dissociative as well. Just that the brain seems to react to this exceedingly fast, the tolerance is worse than any other drug and withdrawal feels like a mild narcotic WD.

Xanax was shown to be a dopamine D2 agonist as well, which makes it less sedating than other BZDs. Yeah, these are GABA-A PAMs.

Xanax binds to the alpha 2 delta calcium channels as well. Wouldn't Xanax binding to GABA receptors with agonist activity make it a GABA agonist like I've read from many sources? I think phenibut actually binds to GABA as well.

 

[Skorpio]

The alpha2delta Ca channels are a subunit of NMDA ones btw which makes pregab an indirect dissociative as well.

Alpha2delta calcium channels are a type of voltage gated calcium channel and a separate entity from NMDA channels, though they function downstream of any channels contributing to the rise in cellular voltage.

 

[plumbus-nine]

Alpha2delta calcium channels are a type of voltage gated calcium channel and a separate entity from NMDA channels, though they function downstream of any channels contributing to the rise in cellular voltage.

Well I once found a paper stating that NMDA mediates the anti-seizure effects of gabapentinoids, if not more. Posted this somewhere, I'll look it up. Thanks for clarifying this!

 

[The Holy Quadruplty]

Well I once found a paper stating that NMDA mediates the anti-seizure effects of gabapentinoids, if not more. Posted this somewhere, I'll look it up. Thanks for clarifying this!

It looks like gabapentinoids actually bind to GABAa GABAb and other GABA receptors, and also to serotonin receptors. I don't know what the Excitatory amino acid transporter 2 is, but Lyrica binds to it.

 

[The Holy Quadruplty]

That's because you're looking for the effects now and probably better at recognizing them, as opposed to when you're a kid, you're already jacked up on 3 bowls of fruity pebbles.

Some useless info.

Doesn't a chemical in chocolate metabolize into an amphetamine?

 

[The Holy Quadruplty]

What is the Excitatory amino acid transporter, and does it produce any recreational effects?

 

[The Holy Quadruplty]

Anyone have any information on this?

 

[plumbus-nine]

It looks like gabapentinoids actually bind to GABAa GABAb and other GABA receptors, and also to serotonin receptors. I don't know what the Excitatory amino acid transporter 2 is, but Lyrica binds to it.

EAAT-2 might be the same as GLT-1 (glutamate transporter)? Interesting that it binds directly to GABA and serotonin.

 

[jasperkent]

I'm 62 and I still LOVE dark roast coffee + good cannabis.....
BUT I only smoke two or three hits of bud at a time and and I'm a coffee fiend. I drink about 2 pots a day, so my caffeine tolerance is absurdly high. I can drink a cup right before bed and I sleep fine.

 

[tweakerguy]

Doesn't a chemical in chocolate metabolize into an amphetamine?

Heavens no, child. Chocolate would've been scheduled as a controlled substance before the Mayflower hit Plymouth Rock.

 

[thegreenhand]

Can anyone link me to any studies on the effects of buprenorphine with xanax?

you can find these yourself with some simple searches.

go to scholar.google.com and put in your search terms. another good one is pubmed.gov

asking people to find papers for you is a little lazy imo. find some papers first and then come back and ask any questions you have about them here.

 

[RandomClean3]

I appreciate that I'm feeling especially fragile this morning and all sorts of things are triggering me

There's no real difference once you get 65%+, well, it does explain some things, like why you need less methadone than the equivalent after you've been using morphine or oxy or h

 

[RandomClean3]

What is the Excitatory amino acid transporter, and does it produce any recreational effects?

With the limited knowledge I have of it, I wouldn't fuck with it. If cut the transport, which so far is the only thing we can do realibly with this thing, there is a very good chance your brain will drown in glutamate and you die a very horrific death. It's like drinking sarin to see what happens to your pupils. Now activation has been researched particularly in condition like addiction and dementia, as a neuroprotective agent, but there are very, very few agonists right now and their effect is to the entire brain, EAAT2 alone is more than 90% of the transport of glutamate, and glutamate is the most abundant excitatory neurotransmiter, so you're talking about something that affects pretty much your entire brain, think something way way smaller, like MAO inhibition and that can kill you very easily if not careful, now multiply that by 10, this is comparable to ChEIs, you're flooding or depriving most of your brain with the most essential excitatory neurotransmitter.

TLDR: Big nop

 

[The Holy Quadruplty]

Heavens no, child. Chocolate would've been scheduled as a controlled substance before the Mayflower hit Plymouth Rock.

I read it does, if I can find the source I will link it.

 

[The Holy Quadruplty]

With the limited knowledge I have of it, I wouldn't fuck with it. If cut the transport, which so far is the only thing we can do realibly with this thing, there is a very good chance your brain will drown in glutamate and you die a very horrific death. It's like drinking sarin to see what happens to your pupils. Now activation has been researched particularly in condition like addiction and dementia, as a neuroprotective agent, but there are very, very few agonists right now and their effect is to the entire brain, EAAT2 alone is more than 90% of the transport of glutamate, and glutamate is the most abundant excitatory neurotransmiter, so you're talking about something that affects pretty much your entire brain, think something way way smaller, like MAO inhibition and that can kill you very easily if not careful, now multiply that by 10, this is comparable to ChEIs, you're flooding or depriving most of your brain with the most essential excitatory neurotransmitter.

TLDR: Big nop

If that's true then I change my mind on wanting to be prescribed Lyrica, I'm not I was going to ask my doctor if he thinks it will work for me or not, but I don't want to if it really binds to that receptor. Good thing I asked about it!

 

[The Holy Quadruplty]

Btw I can't remember if it was caffeine, or a chemical in chocolate, actually I think it was phenylamine or whatever it's called that's in chocolate that supposedly binds to the GABAb receptor, I wonder if it would be an agonist or antagonist if so? You would think antagonist, but you never know, and the only time I consume any caffeine or chocolate is at night once in a while, but still sleep like a baby on the nights I do, although sometimes wake up in not as good of a mood.

 

[The Holy Quadruplty]

With the limited knowledge I have of it, I wouldn't fuck with it. If cut the transport, which so far is the only thing we can do realibly with this thing, there is a very good chance your brain will drown in glutamate and you die a very horrific death. It's like drinking sarin to see what happens to your pupils. Now activation has been researched particularly in condition like addiction and dementia, as a neuroprotective agent, but there are very, very few agonists right now and their effect is to the entire brain, EAAT2 alone is more than 90% of the transport of glutamate, and glutamate is the most abundant excitatory neurotransmiter, so you're talking about something that affects pretty much your entire brain, think something way way smaller, like MAO inhibition and that can kill you very easily if not careful, now multiply that by 10, this is comparable to ChEIs, you're flooding or depriving most of your brain with the most essential excitatory neurotransmitter.

TLDR: Big nop

Here it says Lyrica binds to it.