What is the mechanism of action of Kava on the GABA receptor.
- Thread starter calma
- Start date
Here’s what we know so far.
Kava Fact of the Day - Kavain acts as a positive allosteric modulator (PAM)
Kavain as a Positive Allosteric Modulator Today we’re going to return to one of our old topics to fill in some gaps. GABA-A. In the past I’ve described kavalactone’s binding ability to GABA as “enhancing” natural GABA to bind to its receptor. After further research, while accurate in simple...
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More research is needed, especially in vivo, but it’s looking like a positive allosteric modulator with specificity to some subunits over others.
Plantacious
Kava Enthusiast
I've always wondered if if was safe to combine Kava with Phenibut.
If I'm not mistaken Kava binds to GABA-A, while Phenibut is to GABA-B.
Hence, they probably wouldn't do much harm taken together, would anyone agree ?
Phenibut will also bind to GABAa at extremely high doses. Fluoro-phenibut binds to not only GABAb, but also your calcium voltage channels. Like gabapentinoids.
You know the reverse tolerance? I somehow think the binding to GABAa has something to do with it. I have been on benzodiazepines for two decades so my tolerance is insanely high, but I took 1 tbsp then 2 tbsp 30 minutes later of Kalm with Kava and I was unable to even open my eyes. That was the first time I ever used kava. It was the micronized type. I’ve had 3 shells tonight, 5 tablespoons total. Feel amazing. But I’ve only had 8 shells in my whole life.
My PTSD is so bad. This takes away all problems. Nothing but psychedelics can do that. It’s insane to me how well it works. People who say it does work just need to keep trying, because of the reverse tolerance. Eventually it’ll work. It works so heavily for me. It heals me. It keeps me sane.
How the heck would it not work for them too? It’s so powerful to me. I don’t get it. So I do believe GABAa tolerance has something to do with it. It slowly builds up a tolerance to GABAa and eventually the kavalactones kick in too.
Since I already had a GABAa tolerance, I think I bypassed the “reverse tolerance” part of it. Kava is a miracle to me. Buying that 2 oz jar of micronized Vanuatu Borongoru was the best purchase I’ve ever made. It changed my life.
And to answer your question, yes it would be. Both have very mild effects on the CNS. You won’t stop breathing. But do NOT drink alcohol. Alcohol with kava alone is dangerous to the liver, add phenibut and you’re overloading your GABAb receptors which keeps both the drugs in your system longer, potentiating both, and that can be deadly. However, kava and phenibut should be just fine. I’m using benzodiazepines and kava since I have to take them (prescription). I’ve used it on phenibut too.
I know it’s mostly anecdotal, but I did go to school for pharmacology. I see no true danger in taking a reasonable size dose of phenibut and combining it with kava. Just don’t use alcohol or f-phenibut (even though I use 800 gabapentin 5x daily. No respiratory distress whatsoever).
You know the reverse tolerance? I somehow think the binding to GABAa has something to do with it. I have been on benzodiazepines for two decades so my tolerance is insanely high, but I took 1 tbsp then 2 tbsp 30 minutes later of Kalm with Kava and I was unable to even open my eyes. That was the first time I ever used kava. It was the micronized type. I’ve had 3 shells tonight, 5 tablespoons total. Feel amazing. But I’ve only had 8 shells in my whole life.
My PTSD is so bad. This takes away all problems. Nothing but psychedelics can do that. It’s insane to me how well it works. People who say it does work just need to keep trying, because of the reverse tolerance. Eventually it’ll work. It works so heavily for me. It heals me. It keeps me sane.
How the heck would it not work for them too? It’s so powerful to me. I don’t get it. So I do believe GABAa tolerance has something to do with it. It slowly builds up a tolerance to GABAa and eventually the kavalactones kick in too.
Since I already had a GABAa tolerance, I think I bypassed the “reverse tolerance” part of it. Kava is a miracle to me. Buying that 2 oz jar of micronized Vanuatu Borongoru was the best purchase I’ve ever made. It changed my life.
And to answer your question, yes it would be. Both have very mild effects on the CNS. You won’t stop breathing. But do NOT drink alcohol. Alcohol with kava alone is dangerous to the liver, add phenibut and you’re overloading your GABAb receptors which keeps both the drugs in your system longer, potentiating both, and that can be deadly. However, kava and phenibut should be just fine. I’m using benzodiazepines and kava since I have to take them (prescription). I’ve used it on phenibut too.
I know it’s mostly anecdotal, but I did go to school for pharmacology. I see no true danger in taking a reasonable size dose of phenibut and combining it with kava. Just don’t use alcohol or f-phenibut (even though I use 800 gabapentin 5x daily. No respiratory distress whatsoever).
Have you tried GABA as food supplement? It is safer than phenibut for everyday use, even if you use medical dose of the latter 250 mg / d.
If you can sleep after drinking kava, no comments. If you can't then I suggest heady kavas in the morning.
Neurosteroids that interact with GABAA are various. In my experience, allopregnanolone does not cause anxiety, at least not in heroic doses.
pubmed.ncbi.nlm.nih.gov
One more thing. You can check your cortisol levels. If these high on the spectrum, you might be interested in researching food supplements that lower cortisol.
If you can sleep after drinking kava, no comments. If you can't then I suggest heady kavas in the morning.
Neurosteroids that interact with GABAA are various. In my experience, allopregnanolone does not cause anxiety, at least not in heroic doses.
Neurosteroids and GABA-A Receptor Function - PubMed
Neurosteroids represent a class of endogenous steroids that are synthesized in the brain, the adrenals, and the gonads and have potent and selective effects on the GABAA-receptor. 3α-hydroxy A-ring reduced metabolites of progesterone, deoxycorticosterone, and testosterone are positive modulators...
One more thing. You can check your cortisol levels. If these high on the spectrum, you might be interested in researching food supplements that lower cortisol.
describes how Kavain works and how other Kavalactones work On the GABA receptors
?
Pzk
Kava Enthusiast
I don't know if the conclusion from your post could be right, that kava resets also the Benzo tolerance which went up by time a lot, when you take kava? Or do I connect things wrong?
I always thought Kava acts on Gaba-B, but now after reading some latest infos, this isn't true, it seems to be Gaba-A - but in a different way that benzos act on that rezeptors.
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