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Overview of drugs that affect GABA

gaba

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#31 medievil

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Posted 08 March 2013 - 08:43 PM

Baclofen inhibits calcium channels GHB induces them, prob makes up alot for the differences, induction induces glutamate release and stuff.

#32 Thorsten3

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Posted 08 March 2013 - 08:48 PM

Is it weird to know that when I take ephedrine (30mgs) and have a coffee, the crash I experience that occurs just about an hour before bedtime helps me fall asleep faster than on a day that I don't take such a combo before my workout?


Haha, sounds like your brain has fried and cannot give any more, lol.

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#33 Thorsten3

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Posted 08 March 2013 - 09:01 PM

Baclofen inhibits calcium channels GHB induces them, prob makes up alot for the differences, induction induces glutamate release and stuff.


I rememeber reading somewhere that GHB increases glutamate release. Also, it's supposed to interact with acetylcholine levels quite considerably (in some mysterious manner), IIRC (god knows where I saw that paper, going to try and dig it up). It intrigues me though, because the craziest dreams i ever had was when I was on piracetam + GHB. Jesus! The word 'weird' doesn't even describe it. GHB either increases acetylcholine acutely or it gets increased substantially during the withdrawal process. I can't remember. I'll have a look for the paper.

It's interesting that acutely, GHB induces glutamate release, but IIRC, the withdrawal (or 'rebound' effects) also increase glutamatergic tone, too. That might not be correct 100%, but it has always been my opinion, based on what I've read from the literature. I always found that a more plausible explanation than the 'dopamine rebound effect' - which is garbabge, IMO. I suppose the downregulation of GABAB is overall going to play a pretty major part in the withdrawal process. I still remember those intensely nervous, impending sense of doom, states of mind, that I went through (on my many occasions) when withdrawing from G. Thank God I was never stupid enough to get a benzo addiction and go through that.

Edited by Thorsten2, 08 March 2013 - 09:03 PM.


#34 medievil

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Posted 08 March 2013 - 09:04 PM

I went trough benzo withdrawal for half a week, its far from as bad as phenibut but lasts forever lol, thats what makes it worse, gabab depletes glutamate and ghb receptor induces it, during effects the ghb overpowers but afterwards gabab downregulation causes induced glutamate release and withdrawals.

The da rebound is indeed a stupid theory lol.

lol at gbl dreams so realistic its odd.

#35 medievil

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Posted 08 March 2013 - 09:50 PM

I wonder why plants and pharm company's dont make many gabab agonists, i smell a conspiracy, possible involvement of the inuits and the metal industry.

#36 xsiv1

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Posted 09 March 2013 - 01:54 AM

Is it weird to know that when I take ephedrine (30mgs) and have a coffee, the crash I experience that occurs just about an hour before bedtime helps me fall asleep faster than on a day that I don't take such a combo before my workout?


Haha, sounds like your brain has fried and cannot give any more, lol.


No, no. Perhaps I didn't provide enough information. Its completely normal to feel a crash from an ephedrine/caffeine combo hours after ingestion. If I take the combo at 3:30pm and workout at 4-4:15 for an hour, eat, get stuff done, and chill...I'll end up being relaxed enough to fall asleep easier than I would without taking that combo earlier in the day. The crash inherent to the combo is timed perfectly to elicit a faster onset of sleep that evening for me. I'm just unsure if others experience the same thing. Than again, maybe my brain is fried and I just need rest. Full time work, two little kids, high intensity workouts, meal prep, cleanup, bathtime etc leads to one worn out Dad by the end of the night.

I've went through my own GHB era. I'm 40 now so I didn't even know what GBL was until I looked it up. I remember the horrid withdrawals from it as well. Glad those days are long gone lol. Anyways, I have extensive personal experiences with just about any Gaba agonist. I'm quite sure 40-50mgs of Baclofen in one shot before bed would cause some positive effects the next day. That's kind of a hefty dose for only trying it a few times. I'm quite aware of it's dependence risks along with that of Phenibut. I still think any and all of the aforementioned (despite their negative ramifications when misused) have therapeutic effects but need to be used sparingly for the vast majority of people.

#37 Thorsten3

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Posted 17 March 2013 - 03:13 PM

GHB would be amazing it it wasn't so abusable, but that's the reason it's a no goer, I suppose. Even if you weren't in withdrawal, you'd still be mentally craving it. Just having the bottle there, looking at you, smiling, giving you a wink. My first thought, upon seeing the bottle, was always 'fuck it, I'm having some fun'. And that's how it pulls you in. Just one dose isn't enough, because of the shitty half life (especially GBL). And the more you take, the harder you crash at the end.

Is it weird to know that when I take ephedrine (30mgs) and have a coffee, the crash I experience that occurs just about an hour before bedtime helps me fall asleep faster than on a day that I don't take such a combo before my workout?


Haha, sounds like your brain has fried and cannot give any more, lol.


No, no. Perhaps I didn't provide enough information. Its completely normal to feel a crash from an ephedrine/caffeine combo hours after ingestion. If I take the combo at 3:30pm and workout at 4-4:15 for an hour, eat, get stuff done, and chill...I'll end up being relaxed enough to fall asleep easier than I would without taking that combo earlier in the day. The crash inherent to the combo is timed perfectly to elicit a faster onset of sleep that evening for me. I'm just unsure if others experience the same thing. Than again, maybe my brain is fried and I just need rest. Full time work, two little kids, high intensity workouts, meal prep, cleanup, bathtime etc leads to one worn out Dad by the end of the night.

I've went through my own GHB era. I'm 40 now so I didn't even know what GBL was until I looked it up. I remember the horrid withdrawals from it as well. Glad those days are long gone lol. Anyways, I have extensive personal experiences with just about any Gaba agonist. I'm quite sure 40-50mgs of Baclofen in one shot before bed would cause some positive effects the next day. That's kind of a hefty dose for only trying it a few times. I'm quite aware of it's dependence risks along with that of Phenibut. I still think any and all of the aforementioned (despite their negative ramifications when misused) have therapeutic effects but need to be used sparingly for the vast majority of people.


It may have been 40-50mg, or it may have been 20mg. I honestly couldn't tell you, for sure. I just remember the positive effects that would follow, the day after.

Edited by Thorsten2, 17 March 2013 - 03:14 PM.

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#38 xsiv1

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Posted 18 March 2013 - 12:41 AM

It may have been 40-50mg, or it may have been 20mg. I honestly couldn't tell you, for sure. I just remember the positive effects that would follow, the day after.

Yeah, they do come in 20's..so that would have been enough to help you sleep and boost mood the next day...otherwise, it's just a meh feeling for me. As for GHB, I read somewhere (I'm sure it was a second hand account) that their are people trying to combine it clinically with small dose naltrexone to remove any of it's addictive qualities in a sense. IF one was able to use it say, once or twice a day and be content with that, I can see it being very therapeutic but that was pretty impossible for me back in the day. I think we're talking late 90's when you could buy kits and make it on your own ensuring it's pure and the PH was right. Still glad it's not in my life lol..I liked it too much since it felt, well, perfect. I distinctly remember that it did produce significant fat-burning effects while I retained muscle. During that time, a bunch of us went to Acapulco (of all places nowadays) back when it was still a hotspot for March Break and I'd say I was the leanest I've ever been and I never did cardio...just heavy weight training. Some memories of it are still fond.

#39 maxwatt

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Posted 18 March 2013 - 01:49 AM

Dihydromyricetin binds to the GABAA receptor, blocking alcohols intoxicating effects thereon.

http://www.ncbi.nlm....pubmed/22219299

But I suspect this is the opposite of what you guys are looking for.

#40 xsiv1

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Posted 20 March 2013 - 10:26 PM

What a unique compound though.

#41 Olon

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Posted 21 March 2013 - 06:41 AM

Baclofen sucks compared to phenibut, imo because it blocks calcium channels and depletes glutamate a property wich phenibut hasnt got im guessing as it feels more like GHB, so i was researching how to hijack that calcium channel blockade.


4-AP opens calcium channels,
but I have my doubts whether schizophrenia patients with low or no dopaminergic medication really have the low glutamate problem.
http://www.ncbi.nlm....pubmed/22213769
http://www.ncbi.nlm....pubmed/22432602
http://www.ncbi.nlm....pubmed/20970118

#42 xsiv1

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Posted 21 March 2013 - 09:31 PM

What I don't get is how a calcium channel blocker like Gabapentin or Lyrica can feel so nice during its short honeymoon period in normal doses. I've made no attempts to abuse them but when used quite sparingly, they're pretty good social lubricants for me. I know there's a lot of people who hate their effects.

#43 Galaxyshock

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Posted 28 March 2013 - 05:33 AM

I wonder why plants and pharm company's dont make many gabab agonists, i smell a conspiracy, possible involvement of the inuits and the metal industry.


Muscimol:

http://www.ncbi.nlm....pubmed/10998126

I probably wouldn't go eating those mushrooms for the GABAB-agonism though lol

#44 medievil

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Posted 09 April 2013 - 11:12 AM

GHB would be amazing it it wasn't so abusable, but that's the reason it's a no goer, I suppose. Even if you weren't in withdrawal, you'd still be mentally craving it. Just having the bottle there, looking at you, smiling, giving you a wink. My first thought, upon seeing the bottle, was always 'fuck it, I'm having some fun'. And that's how it pulls you in. Just one dose isn't enough, because of the shitty half life (especially GBL). And the more you take, the harder you crash at the end.

Is it weird to know that when I take ephedrine (30mgs) and have a coffee, the crash I experience that occurs just about an hour before bedtime helps me fall asleep faster than on a day that I don't take such a combo before my workout?


Haha, sounds like your brain has fried and cannot give any more, lol.


No, no. Perhaps I didn't provide enough information. Its completely normal to feel a crash from an ephedrine/caffeine combo hours after ingestion. If I take the combo at 3:30pm and workout at 4-4:15 for an hour, eat, get stuff done, and chill...I'll end up being relaxed enough to fall asleep easier than I would without taking that combo earlier in the day. The crash inherent to the combo is timed perfectly to elicit a faster onset of sleep that evening for me. I'm just unsure if others experience the same thing. Than again, maybe my brain is fried and I just need rest. Full time work, two little kids, high intensity workouts, meal prep, cleanup, bathtime etc leads to one worn out Dad by the end of the night.

I've went through my own GHB era. I'm 40 now so I didn't even know what GBL was until I looked it up. I remember the horrid withdrawals from it as well. Glad those days are long gone lol. Anyways, I have extensive personal experiences with just about any Gaba agonist. I'm quite sure 40-50mgs of Baclofen in one shot before bed would cause some positive effects the next day. That's kind of a hefty dose for only trying it a few times. I'm quite aware of it's dependence risks along with that of Phenibut. I still think any and all of the aforementioned (despite their negative ramifications when misused) have therapeutic effects but need to be used sparingly for the vast majority of people.


It may have been 40-50mg, or it may have been 20mg. I honestly couldn't tell you, for sure. I just remember the positive effects that would follow, the day after.

naltrexone abolishes GHB abuse while retaining therapeutic effects in alcohol addicts in several case reports of Italy where its used for alcohol addiction.

Baclofen sucks compared to phenibut, imo because it blocks calcium channels and depletes glutamate a property wich phenibut hasnt got im guessing as it feels more like GHB, so i was researching how to hijack that calcium channel blockade.


4-AP opens calcium channels,
but I have my doubts whether schizophrenia patients with low or no dopaminergic medication really have the low glutamate problem.
http://www.ncbi.nlm....pubmed/22213769
http://www.ncbi.nlm....pubmed/22432602
http://www.ncbi.nlm....pubmed/20970118

The glut hypothesis is crappy indeed, hypoactivity does play a big role but its not really the "actual cause" wich is more a combo of things.

#45 medievil

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Posted 09 April 2013 - 11:19 AM

As an aside, seems like swithing to etizolam works solid to withdrawal of benzo's, did this twice after switching i could stop eti wich only caused weirdness for couple days then im fine.

In rodents it barely causes tolerance and withdrawals too.

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#46 123apk

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Posted 16 January 2016 - 10:37 AM

Seems like ppl did it before, wonder how much i could yield out one extraction, wont bother if its not worth it.

There is some wonderfully intelligent chemists on herbsmaxforum or something like that. I'm sure a moderator there named Toastus would know. They've devised a unique way to extend PEA's effects for far longer than what you'll typically find reading anecdotal reports like combining it with Selegline or Quercetin etc. Anyways, it's something to consider. I myself reacted very positively to Phenibut and it lasted for quite some time..taking it with Piracetam mostly. Sharpness personified. It pooped out and I had to taper off. I've tried Baclofen on several occasions and hate it. It seems like it lacks any of the dopamine agonism that Phenibut possesses. Makes you kind of just flat and dull feeling if not dysphoric. For me, it's completely void of any recreational or nootropic value. It will relax your muscle and possesses anxiolytic qualities. You may not develop the tolerance to it..as phenibut has a very steep tolerance ramp. Unfortunately, unless used sparingly - like Phenibut, Baclofen also possesses dependence qualities and must be tapered off. The one thing about Baclofen, if you're getting it from a pharm, is you typically know it's clean and void of heavy metals etc..otherwise it's crap. It may work nicely when combined with DLPA or the CILTEP regimen, otherwise meh.

The dopamine agonism of Phenibut is one of the main things that "poops out" when you've been on it for some time.
After a while for me it became purely sedating and anti-anxiety, but as you describe baclofen - made me feel a bit dull and flat.
But what I found was as Phenibut's dopamine effects were weakening over time that Tyrosine was able to bring them back to an extent. Not the huge effects from Phenibut when you're new to it, but enough of the energy and motivation back that Phenibut doesn't dull you down like a benzo. And it also seems to make the anti-anxiety effect a bit more extended.

I'm not sure why this is, maybe Phenibut has depleted dopamine receptors and Tyrosine fills the gap. Tyrosine is very under estimated though. In a normal person there probably wouldn't be too much effect, but in a person with dopamine receptor damage (in my case probably from Phenibut) it can keep them functional.





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