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The big thread on upregulating GABA activity "Naturally"

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#61 neurotropic

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Posted 17 October 2017 - 04:16 PM

Homotaurine and fasoracetam are supposed to be great for GABA B upreg. I've been taking homotaurine for awhile now but i think the dose is too low so I'm going to bump it up.



#62 Daniel Cooper

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Posted 17 October 2017 - 05:38 PM

Homotaurine and fasoracetam are supposed to be great for GABA B upreg. I've been taking homotaurine for awhile now but i think the dose is too low so I'm going to bump it up.

 

 

Are there any studies that show the above?  



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#63 airplanepeanuts

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Posted 17 October 2017 - 09:03 PM

Homotaurine and fasoracetam are supposed to be great for GABA B upreg. I've been taking homotaurine for awhile now but i think the dose is too low so I'm going to bump it up.

 

Do you get some kind of good effect of Homotaurin?



#64 gamesguru

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Posted 03 November 2017 - 11:40 PM

there definitely was a study concerning faso in the context of gaba-b restoration, and what's more, there were some guinea pig reports floating around in defense of things.  though one surely knows by now how enthusiasm follows suit to impressive findings, like froth on a river and how little it does to strengthen the academic claims  :sleep:

 

i just think it's too early to tell and this study only looks in a depleted state, not the whole picture.  for those nonetheless convinced of their thinking abilities and interested in reviewing the case, i've attached the study in question.  cheers on a friday night

 

Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: Possible involvement of GABA receptor up-regulation B after repeated treatment

Edited by gamesguru, 03 November 2017 - 11:45 PM.


#65 medievil

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Posted 07 November 2017 - 09:59 AM

KAVAKAVA upregulates GABAB, fasoracetam does so too, also ive read a anecdotal report of magnolia bark dramatically potentiating phenibut, aside from that NMDA antagonists like memantine could help although the anecdotes for gabab drugs have been inconsistent.



#66 normalizing

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Posted 07 November 2017 - 10:10 PM

i think gingko biloba does something to gaba as well just not sure which type and what exactly, but ive experienced something similar to sedation with it



#67 Daniel Cooper

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Posted 08 November 2017 - 04:59 PM



i think gingko biloba does something to gaba as well just not sure which type and what exactly, but ive experienced something similar to sedation with it

 

 

 

Terpene trilactones from Ginkgo biloba are antagonists of cortical glycine and GABA(A) receptors

 

 

Looks like ginko biloba antagonizes both glycine and GABA(A) receptors.  I would think the former would be anxiolytic while the later would be anxiogenic.  Net - net maybe they'd balance out?  Probably depends on the person.  This may be the effect responsible for people reporting that ginko biloba helps with recovering after benzo withdrawal.  Antagonizing GABA receptors (and hopefully upregulating them) while antagonizing gylcine receptors might be a good way to repair benzo induced damage while minimizing the anxiogenic effects.



#68 Daniel Cooper

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Posted 08 November 2017 - 06:55 PM

I stand corrected on the above.  Antagonizing glycine receptors should also I think be anxiogenic.

 

 

 


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#69 normalizing

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Posted 09 November 2017 - 03:37 AM

what if you just take glycine directly?


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#70 gamesguru

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Posted 10 November 2017 - 12:25 AM

what if you just take glycine directly?

 

then your approach lacks sophistication.


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#71 Kinesis

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Posted 10 November 2017 - 04:43 AM

This may not qualify as “upregulation”, but it definitely meets the “naturally” criterion. Interesting how Examine characterizes the cross-modulation of glutamate and GABA by the combination of melissa (lemon balm) and valerian:

Lemon Balm and Valerian are commonly used in conjunction with one another for the purpose of sleep, as Lemon Balm is able to inhibit the GABA transaminase enzyme weakly (which converts GABA into Glutamate) while Valerian bioactives also weakly stimulates Glutamate Decarboxylase (which converts Glutamate into GABA); this combination is thought to cause a two-pronged stimulation of GABA concentrations in the brain secondary to inhibiting breakdown and stimulating synthesis of GABA.[41]

https://examine.com/...sa-officinalis/



#72 normalizing

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Posted 10 November 2017 - 05:05 AM

well, glycine is used for sleep so i thought it must affect GABA in some positive manner. but when i did use it, i got to experience paranoia and anxiety. so whoever knows... it could have just been too high of dose. i used sublingual, which is much much more bioavailable

 

i wonder how rosmarinic acid works regard to GABA... ive been taking some pills with it and so far, it definitely seems more relaxing rather than stimulating


Edited by hazy, 10 November 2017 - 05:06 AM.


#73 Kinesis

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Posted 10 November 2017 - 06:04 AM

Makes sense, hazy. Sometimes people get a paradoxical anxiety response to things that are ordinarily relaxing; I forget what the term is but Mental Health Daily has cited it. Something to do with the calm sort of surprising the mind and inducing disquiet. I’ve experienced this myself; even a glass of wine taken in the wrong frame of mind has caused anxiety.

Rosmarinic acid by the way is one of the constituents of melissa.

Edited by Kinesis, 10 November 2017 - 06:17 AM.


#74 normalizing

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Posted 10 November 2017 - 07:00 PM

rosmarinic acid seems to be present in shitload of plants not just melissa, but i found this interesting https://en.wikipedia...inase_inhibitor as it contains few other things that work on GABA that i didnt know of and they are usually prescribed as drugs for other indications. interesting



#75 normalizing

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Posted 18 November 2017 - 08:39 PM

i found this interesting article; https://www.ncbi.nlm.../pubmed/2840912 it seems to be in vitro, i wonder how well it will work in vivo?

 

also i found similar reading here; https://books.google...ist buy&f=false

 

interesting book on naturally occurring benzos



#76 Galaxyshock

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Posted 27 November 2017 - 11:44 AM

KAVAKAVA upregulates GABAB, fasoracetam does so too, also ive read a anecdotal report of magnolia bark dramatically potentiating phenibut, aside from that NMDA antagonists like memantine could help although the anecdotes for gabab drugs have been inconsistent.

 

What's the evidence behind Kava upregulating GABA-B? Personally I didn't notice it to make Phenibut more effective. Although, sometimes the Kava euphoria resembles that of Phenibut which you initially get. One of the kavalactones works as MAOB-inhibitor which in theory could upregulate GABA-B by increasing levels of PEA (GABA-B antagonist) or maybe through some other mechanism. Kava even has affinity for cannabinoid receptors.



#77 normalizing

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Posted 27 November 2017 - 06:36 PM

i cannot feel kava. did you do the online powder forms or pills from your store? cuz the pills, didnt work for me in high doses even



#78 Galaxyshock

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Posted 27 November 2017 - 08:42 PM

i cannot feel kava. did you do the online powder forms or pills from your store? cuz the pills, didnt work for me in high doses even

 

I took powdered Kava king products vanuatu blend, I need 9-12 teaspoons to get a high from it (recommendation is 1-3 teaspoons). Yeah most commercial kava products are weak crap, you need to take whole bottle of those capsules to feel something or sometimes not even that does get the job done. Kava king is the only semi-decent one. I'm sure there are more authenthic ones somewhere (like nakamalathome), but I may not be able to order them to here in Finland. Kava is actually banned here, but people order so much from iHerb that I get those kava containing packets through.


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#79 tolerant

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Posted 28 November 2017 - 06:16 AM

 

i cannot feel kava. did you do the online powder forms or pills from your store? cuz the pills, didnt work for me in high doses even

 

I took powdered Kava king products vanuatu blend, I need 9-12 teaspoons to get a high from it (recommendation is 1-3 teaspoons). Yeah most commercial kava products are weak crap, you need to take whole bottle of those capsules to feel something or sometimes not even that does get the job done. Kava king is the only semi-decent one. I'm sure there are more authenthic ones somewhere (like nakamalathome), but I may not be able to order them to here in Finland. Kava is actually banned here, but people order so much from iHerb that I get those kava containing packets through.

 

 

I think I have the identical kava product to yours. Mine is a few years old though. Not sure how quickly it loses potency. The most I've dared try is about two heaped teaspoons and two regular ones -- so about six in total. Tried this dose the other day and no effect. Maybe that is what I was doing wrong. Did you have any effect at lower doses than 9-12 teaspoons you mention?

 

(Also tried two Thompson's tablets equal to 60 kavalactones and also to no effect.)



#80 Galaxyshock

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Posted 28 November 2017 - 09:20 AM

 

 

i cannot feel kava. did you do the online powder forms or pills from your store? cuz the pills, didnt work for me in high doses even

 

I took powdered Kava king products vanuatu blend, I need 9-12 teaspoons to get a high from it (recommendation is 1-3 teaspoons). Yeah most commercial kava products are weak crap, you need to take whole bottle of those capsules to feel something or sometimes not even that does get the job done. Kava king is the only semi-decent one. I'm sure there are more authenthic ones somewhere (like nakamalathome), but I may not be able to order them to here in Finland. Kava is actually banned here, but people order so much from iHerb that I get those kava containing packets through.

 

 

I think I have the identical kava product to yours. Mine is a few years old though. Not sure how quickly it loses potency. The most I've dared try is about two heaped teaspoons and two regular ones -- so about six in total. Tried this dose the other day and no effect. Maybe that is what I was doing wrong. Did you have any effect at lower doses than 9-12 teaspoons you mention?

 

(Also tried two Thompson's tablets equal to 60 kavalactones and also to no effect.)

 

 

Yup that's the product. Usually dry powders in sealed containers don't lose their potency. I think I tried low doses but the effects were weak if not placebo. But Kava has that reverse tolerance thing that in continous use lower doses may become effective. Personally I want to be sure that it hits me strong so I mix close to that dozen teaspoons of kava, several tablespoons of sugary cocoa powder and some rice milk and drink it fast. You know when it really works, you're hit with strong yet clearheaded anxiolysis and euphoria and feel like chatting people up or listening to music. Lasts about two hours and then you can redose a smaller amount to maintain the high but the sedative effects might start taking over at this point, whereas in start I definitely feel the stimulative euphoriant qualities more.

 

Most I've consumed in a day or setting was something like 35 teaspoons. The problem really is trying not to puke when consuming so much of that awful mud tasting plant matter.  :-D


Edited by Galaxyshock, 28 November 2017 - 09:28 AM.


#81 tolerant

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Posted 28 November 2017 - 09:40 AM

 

 

 

i cannot feel kava. did you do the online powder forms or pills from your store? cuz the pills, didnt work for me in high doses even

 

I took powdered Kava king products vanuatu blend, I need 9-12 teaspoons to get a high from it (recommendation is 1-3 teaspoons). Yeah most commercial kava products are weak crap, you need to take whole bottle of those capsules to feel something or sometimes not even that does get the job done. Kava king is the only semi-decent one. I'm sure there are more authenthic ones somewhere (like nakamalathome), but I may not be able to order them to here in Finland. Kava is actually banned here, but people order so much from iHerb that I get those kava containing packets through.

 

 

I think I have the identical kava product to yours. Mine is a few years old though. Not sure how quickly it loses potency. The most I've dared try is about two heaped teaspoons and two regular ones -- so about six in total. Tried this dose the other day and no effect. Maybe that is what I was doing wrong. Did you have any effect at lower doses than 9-12 teaspoons you mention?

 

(Also tried two Thompson's tablets equal to 60 kavalactones and also to no effect.)

 

 

Yup that's the product. Usually dry powders in sealed containers don't lose their potency. I think I tried low doses but the effects were weak if not placebo. But Kava has that reverse tolerance thing that in continous use lower doses may become effective. Personally I want to be sure that it hits me strong so I mix close to that dozen teaspoons of kava, several tablespoons of sugary cocoa powder and some rice milk and drink it fast. You know when it really works, you're hit with strong yet clearheaded anxiolysis and euphoria and feel like chatting people up or listening to music. Lasts about two hours and then you can redose a smaller amount to maintain the high but the sedative effects might start taking over at this point, whereas in start I definitely feel the stimulative euphoriant qualities more.

 

Most I've consumed in a day or setting was something like 35 teaspoons. The problem really is trying not to puke when consuming so much of that awful mud tasting plant matter.  :-D

 

 

I just had about 9 teaspoons and got drunk without clearheaded anxiolysis. Maybe I'm not one of those people who get clearheaded anxiolysis on kava. Or maybe I need to search for my dose more patiently. 



#82 Galaxyshock

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Posted 28 November 2017 - 10:03 AM

 

 

I just had about 9 teaspoons and got drunk without clearheaded anxiolysis. Maybe I'm not one of those people who get clearheaded anxiolysis on kava. Or maybe I need to search for my dose more patiently. 

 

 

I guess the effects tend to vary on different people, but also different times when and where it's ingested and so on. The clearheadedness was most prominent for me when I took kava before going out to a place with plenty of people at social setting, it felt really nootropic and my mind was sharp but at ease. Where as if I take it at home I sometimes get kinda groggy or drunken feeling. Maybe try a bit lower dose or simply the same dose again at different time.



#83 normalizing

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Posted 28 November 2017 - 06:22 PM

galaxyshock, what about liver problems? even though those crappy pills didnt do anything for me, i probably made the bad choice of mixing them with alcohol and i felt sick for a while could be liver issues. im not sure if by itself kava causes liver problems or only when mixed with other meds or alcohol??



#84 Daniel Cooper

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Posted 28 November 2017 - 06:34 PM

Has anyone here experienced the reverse tolerance effect attributed to kava?  Do we have any research that shows that this is a real effect and is this effect is in fact the result of upregulation of the number of gaba receptors?

 

 

 

 



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#85 Galaxyshock

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Posted 28 November 2017 - 07:07 PM

galaxyshock, what about liver problems? even though those crappy pills didnt do anything for me, i probably made the bad choice of mixing them with alcohol and i felt sick for a while could be liver issues. im not sure if by itself kava causes liver problems or only when mixed with other meds or alcohol??

 

Both kavalactones and alcohol are broken down by the same liver enzymes I believe, which can put some stress on it. Kava root shouldn't cause liver problems, only if the leaves are used.

 

Has anyone here experienced the reverse tolerance effect attributed to kava?  Do we have any research that shows that this is a real effect and is this effect is in fact the result of upregulation of the number of gaba receptors?

 

 

I'm still a bit unsure about the reverse tolerance, I feel like it's there but can't count out placebo. Some report that normal tolerance developes in that you need more.

 

This is another thread solely on Kava and its uses:

http://www.longecity...r-upregulation/

Increased binding GABA-A sites and densities were noted in studies.

 

There are different strains with different kavalactone profiles so a lot is still there to discover, but it definitely seems like a plant with good potential for both medical and recreational uses.






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