Fasoracetam upregulates GABA-B receptors and reduces learned helplessness

Mauritio

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Fasoracetam might be especially interesting for people that don't react well to the other racetams and stimulants in generel. I've found that phenylpiracetam can make me a bit irritable, but stacking it with something GABAergic alleviated that.
Or people dealing with anxiety, depression, irritability, insomnia, etc.

This study shows that overtime fasoracetam unregulates the GABA-B receptors . It also shows decreased learned helplessness in one of their tests on mice ,which indicates an anti serotonergic action.
This anti-serotonin effect might be indirect as they state that there's no effect on monoamines. My guess it's proably through increased GABA functioning and thus increased stress tolerance.


"We have previously found that a cognition enhancer [(+)-5-oxo-D-prolinepiperidinamide monohydrate] (NS-105) reversed the inhibition of cyclic AMP formation induced by the GABA(B) receptor agonist baclofen. The GABA(B) receptor has been implicated in the pathophysiology of depressive illness. The present experiment was designed to evaluate the antidepressant activity of NS-105 in the forced swimming and learned helplessness tests in rats. NS-105 (1-100 mg/kg, p.o.) significantly decreased immobility time in the forced swimming test, an effect similar to that of desipramine. Repeated administration of NS-105 also reversed the failure to escape in the shuttle-box test of rats previously exposed to inescapable footshock. Biochemical data showed that repeated administration of NS-105 increased the number of GABA(B) receptors in rat cerebral cortex without affecting the binding properties of beta-adrenoceptors and 5-HT2 receptors. In contrast to other antidepressants, NS-105 did not inhibit monoamine uptake in vitro, nor did it change monoamine concentrations in brain tissues or extracellular fluids. These findings suggest that NS-105, which lacks an effect on monoaminergic systems, has potent antidepressant activity, which may involve up-regulation of GABA(B) receptors after repeated administration.

@Hans you might wanna grab this one too if you haven't made your racetam purchase already:)
 
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Mauritio

Mauritio

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Hans

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Fasoracetam might be especially interesting for people that don't react well to the other racetams and stimulants in generel. I've found that phenylpiracetam can make me a bit irritable, but stacking it with something GABAergic alleviated that.
Or people dealing with anxiety, depression, irritability, insomnia, etc.

This study shows that overtime fasoracetam unregulates the GABA-B receptors . It also shows decreased learned helplessness in one of their tests on mice ,which indicates an anti serotonergic action.
This anti-serotonin effect might be indirect as they state that there's no effect on monoamines. My guess it's proably through increased GABA functioning and thus increased stress tolerance.


"We have previously found that a cognition enhancer [(+)-5-oxo-D-prolinepiperidinamide monohydrate] (NS-105) reversed the inhibition of cyclic AMP formation induced by the GABA(B) receptor agonist baclofen. The GABA(B) receptor has been implicated in the pathophysiology of depressive illness. The present experiment was designed to evaluate the antidepressant activity of NS-105 in the forced swimming and learned helplessness tests in rats. NS-105 (1-100 mg/kg, p.o.) significantly decreased immobility time in the forced swimming test, an effect similar to that of desipramine. Repeated administration of NS-105 also reversed the failure to escape in the shuttle-box test of rats previously exposed to inescapable footshock. Biochemical data showed that repeated administration of NS-105 increased the number of GABA(B) receptors in rat cerebral cortex without affecting the binding properties of beta-adrenoceptors and 5-HT2 receptors. In contrast to other antidepressants, NS-105 did not inhibit monoamine uptake in vitro, nor did it change monoamine concentrations in brain tissues or extracellular fluids. These findings suggest that NS-105, which lacks an effect on monoaminergic systems, has potent antidepressant activity, which may involve up-regulation of GABA(B) receptors after repeated administration.

@Hans you might wanna grab this one too if you haven't made your racetam purchase already:)
Lol so many things to grab. Honestly I have no issue with mental capacity (inc mood, confidence, restlessness, etc) so I'm not overly motived to try all the racetams. I feel that optimizing cellular function and energy production has the best effect on cognition and mood for me.
 
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Mauritio

Mauritio

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Lol so many things to grab. Honestly I have no issue with mental capacity (inc mood, confidence, restlessness, etc) so I'm not overly motived to try all the racetams. I feel that optimizing cellular function and energy production has the best effect on cognition and mood for me.
True . But it's good to know what it does in case you need it . Who doesnt have stress ?!
 

Hans

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True . But it's good to know what it does in case you need it . Who doesnt have stress ?!
Good point. However, if I do feel a little stressed, aspirin, B1, magnesium (my anti-serotonin stack) with pyrucet usually takes care of things.
 
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Mauritio

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Good point. However, if I do feel a little stressed, aspirin, B1, magnesium (my anti-serotonin stack) with pyrucet usually takes care of things.
Yeah its always good to go back to the basics . With that beeing said , i do love to experiemt. And the racetams seem like a very interesting group of supplements !
 
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Mauritio

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For anybody that's interested in the racetams .
The fulltext of this study is a great summary .

 

dukesbobby777

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If it upregulates GABA-B and increases number of receptors, does that mean it has an antagonistic effect there initially, I wonder. That’s usually how things work, what with homeostasis and whatnot.

Homotaurine also does the same thing apparently.
 
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Mauritio

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If it upregulates GABA-B and increases number of receptors, does that mean it has an antagonistic effect there initially, I wonder. That’s usually how things work, what with homeostasis and whatnot.

Homotaurine also does the same thing apparently.
Yes , i see it similarly. It activates one of the glutamate receptors, which makes the the body upregulate GABA-B receptors in return . This is why most people feel nothing initially as it takes some time (few days ) to have significant upregulation .
 

dukesbobby777

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Yes , i see it similarly. It activates one of the glutamate receptors, which makes the the body upregulate GABA-B receptors in return . This is why most people feel nothing initially as it takes some time (few days ) to have significant upregulation .

If that is the case it would be dodgy for somebody who has abused their GABA-B receptors (I would have thought), but seems to be lots of anecdotes on Reddit about people using it to come off their phenibut habit. It’s also been talked about as being useful (perhaps) for schizophrenia, so I don’t really understand what it’s actually doing at GABA-B. I might give it a try. I just hope it isn’t too cholinergic, as anything along those lines, for me, is pro-depressive. Most anecdotes talk of it being mostly mood enhancing though.
 
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Mauritio

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If that is the case it would be dodgy for somebody who has abused their GABA-B receptors (I would have thought), but seems to be lots of anecdotes on Reddit about people using it to come off their phenibut habit. It’s also been talked about as being useful (perhaps) for schizophrenia, so I don’t really understand what it’s actually doing at GABA-B. I might give it a try. I just hope it isn’t too cholinergic, as anything along those lines, for me, is pro-depressive. Most anecdotes talk of it being mostly mood enhancing though.
Yes exactly, pehnibut and other medication that agonizes the GABA-B receptor...

Yeah even phenylpiracetam, which is beeing studied for treating depression , causes depression in some. For me , all of its side effects or removed by a little bit of 5adhp ,which suggests it has to with allopregnanolone but that's another topic...
 
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Mauritio

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Homotaurine gave me a rebound BLISS effect, I will need to try it again. GABA-B Antagonism causes massive anxiety and tension acutely.
Have you tried fasoracetam though?
 

cjm

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For anybody that's interested in the racetams .
The fulltext of this study is a great summary .


Excellent!! Bookmarked.
 

dukesbobby777

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I tied it a few times and I did notice the sedation like effects, but it also definitely increased a ‘crabby’ like mindset which may have been down to cholinergic workings or glutamatergic mechanisms (all of which, alongside what Peat speaks of, antagonises my mood situations).

It’s a shame because as a former GBL abuser, I was hoping this could help restore my GABA-B neurons.
 

satsumass

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I tied it a few times and I did notice the sedation like effects, but it also definitely increased a ‘crabby’ like mindset which may have been down to cholinergic workings or glutamatergic mechanisms (all of which, alongside what Peat speaks of, antagonises my mood situations).

It’s a shame because as a former GBL abuser, I was hoping this could help restore my GABA-B neurons.
Can you tell me more about your GBL abuse? How frequently? Dose? Consequences? Positive effects? vs GHB? Why "former"---what led you to quit....asking for a friend...he's daily user (not 24/7, but most days from late afternoon through evening, sometimes through the night per the "pharmaceutical" use of GHB)...

Always interested in hearing ppls experiences...how ppl "discovered" GBL and what "problem it solved" for them...
 

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