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Using partial agonists/allosteric modulators to regulate and normalize the effects of double-edged nootropics

nicotine partial agonist nefiracetam

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#1 Cognizant

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Posted 16 August 2014 - 01:58 PM


Hey guys, 

 

It has been awhile since I have posted here, but I have been around for a long time. It's rare for me to post, as I would rather use this forum as a hub for the beginning of research ventures and take that out into journals, other forums, etc; however, I have a couple of things that I am wondering about. 

 

1) Have any of you ever used partial agonists in conjunction (though probably not concurrently) with certain nootropics/chemicals in order to normalize function and avoid some of the more long term side effects? For example, Nicotine seems as though it holds tremendous cognitive value, but it seems to fizzle out more long term due to receptor downregulation and other allosteric factors. A similar situation can be seen with Nefiracetam, where GABA receptor downregulation occurs, which can be undesirable. I have thought about these things in the past, but partial agonists for these receptors (specifically the alpha 7 nicotinic) were not readily available. 

It seems to me that if you took breaks (probably just a day to a few days) and took partial agonists to normalize receptor density and function, then it could be possible to make these drugs more manageable in the long term . This is especially of interest for instances like nicotine, where the alpha 7 partial agonists have cognitive benefit in themselves. 

 

2) Have any of you ever attempted to create your own sublingual drug delivery systems? In compared to where we started, back at the beginning of this forum and site, we have access to exceedingly more powerful and efficacious drugs that have their effects at the micro and milligram level. 

 

What I was thinking of was buying the make your own gum kits, which are very cheap, and making mint flavored gum. As the gum is hardening, I would add small doses of nootropics that I am interested in using (say 10-20 mg of Coluracetam). Then, I would use certain dyes for the gum to differentiate what drug, dose, etc. is there. Using the gum, you would be able to chew it and then, like nicotine gum, keep it below your tongue, near your gums, ect. in order to absorb the drug. This would be very efficacious for those of us who would like to redose these sort of drugs while we are working, in class, ect. but want to do so very discretely. 

 

Thanks for reading. 

 



#2 sativa

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Posted 06 November 2015 - 11:19 PM

Hey guys,

It has been awhile since I have posted here, but I have been around for a long time. It's rare for me to post, as I would rather use this forum as a hub for the beginning of research ventures and take that out into journals, other forums, etc; however, I have a couple of things that I am wondering about.

1) Have any of you ever used partial agonists in conjunction (though probably not concurrently) with certain nootropics/chemicals in order to normalize function and avoid some of the more long term side effects? For example, Nicotine seems as though it holds tremendous cognitive value, but it seems to fizzle out more long term due to receptor downregulation and other allosteric factors. A similar situation can be seen with Nefiracetam, where GABA receptor downregulation occurs, which can be undesirable. I have thought about these things in the past, but partial agonists for these receptors (specifically the alpha 7 nicotinic) were not readily available.
It seems to me that if you took breaks (probably just a day to a few days) and took partial agonists to normalize receptor density and function, then it could be possible to make these drugs more manageable in the long term . This is especially of interest for instances like nicotine, where the alpha 7 partial agonists have cognitive benefit in themselves.

Currently investigating alpha 7 nicotinic antagonists to upregulate alpha 7. Also, NGF and BDNF releasers - I believe it is TrkA & TrkB of interest here, NMDA antagonists, prolactin inhibitors (I'm male), opioid receptors and AChE inhibitors.

Antagonists in general also, especially with regards to 5-HT1A - Zinc is a 5-HT1A antagonist!

My approach also involves neuronal maintenance such as the periodical resetting of my tolerances (both to exogenous and endogenous compounds) which involves NMDA, opioid, dopamine and serotonin. Iboga is king for this.

Edited by sativa, 06 November 2015 - 11:33 PM.


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