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[OpenStrife]

I stumbled upon this molecules "JTP-4819" while researching into the mechanism of Pramiracetam.
Chemical structure and purchase(?)
http://acccorporatio...NEW0095673.aspx

-On a side note Pramiracetam works by modulating the enzyme prolyl endopeptidase which is one of the primary enzymes involved in regulating learning and cholingeric systems.


Anyways, when googling scholarly papers for prolyl endopeptidase, I came across JTP-4819

http://jpet.aspetjou...74/3/1370.short

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Microdialysis studies demonstrated that JTP-4819 caused a significant increase in ACh release in the frontal cortex and hippocampus of young rats at oral doses of 1 and 3 mg/kg, as well as in both brain regions of aged rats at a dose of 3 mg/kg. These results indicate that JTP-4819 potentiates neuropeptide functions inhibiting PEP, that it activates cholinergic transmission and that it enhances learning and memory.

There is very few information I could find on this molecule, nor could I find any place to purchase it for research purposes. Nearly all articles relating to this molecule go back in the 90's

If anyone knows anything about this or would like to help me look into it, then please do! It sounds very interesting and I don't think there's been much if any testing on humans.

I have a theory that, there are 2 potential side effects this substance could have on brain chemistry due to it's mechanism... just theories.
1)It could cause more of the enzyme prolyl endopeptidase to be released to make up for the inhibited ones... inevitably resulting in even higher levels of ACh.
2)It could cause ACh to be produced at an endless rate.

Now these are just optimistic shots in the dark, there could always be bad things that happen... but tests on rats show only positives. Though, in terms of how it affects the mind... testing on rats can only tell us so much. Really, how much can a rat learn about navigating a maze lol.

Some other papers on the substance:
http://www.mendeley....llesioned-rats/

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After the behavioral experiment, the choline acetyltransferase (ChAT) activity and 3H-pirenzepine binding (Kd, Bmax) in the residual hippocampus and cerebral cortex were analyzed. Neither parameter was significantly affected by JTP-4819. In conclusion, JTP-4819 can improve both learning and relearning deficits of spatial memory in DH-lesioned rats, postulating that enhancement of neuropeptide activity via PEP inhibition may be involved in the mechanism of action of JTP-4819.

A study on people:
http://onlinelibrary...0611.x/abstract

Quote

In the multiple–dose study, the cholinesterase activity was gradually increased and reached above the normal range on days 4 to 8 in all five subjects given JTP-4819 and gradually returned to normal range after completion of dosing. The elevation of plasma cholinesterase activity was considered to be an action of JTP-4819, but this remains to be verified. There were no other abnormal findings in objective symptoms and laboratory findings including blood pressure, heart rate, electrocardiogram, body temperature, haematology, blood chemistry and urinalysis.

Gradually returned...... sounds like it provides a boost and the brain slowly reverts back to it's previous state... but that's only from 4 days. By the sound of it's effects, this sound like it would be a phenomenal Nootropic! But how would it's effects and actions compare to that of Pramiracetam since they work on the same enzyme?

Edited by OpenStrife, 30 June 2012 - 07:35 AM.

[OpenStrife]

After doing some research and inquiry to chemical labs... I got some more information....

Quote

JTP-4819
98%, not in stock,
1g, 5800 USD
5g, 7000 USD
10g, 8500 USD
Lead time: 7 weeks

When I asked why the price is so high..

Quote

The compound is prepared in lab and not manufactured in large quantity. The cost for small scale preparation is very high.

With an average dose being 3mg/KG.... for me that would cost about $1,000 per dose.

:o