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Is Noopept water or fat soluble?

noopept

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#31 enemy

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Posted 30 October 2011 - 12:46 AM

That ethyl ester group will hydrolyze in water.

#32 manic_racetam

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Posted 18 November 2011 - 09:59 PM

Hey Devin, if you don't mind helping me out here. Which part of the molecule is actively giving the effect? The two studies I mentioned above seem to have conflicting results. One says noopept is metabolized hepataically and has the first pass effect (meaning for sure that it is metabolized, at least a little). The other one states that it crosses the BBB unchanged. In that study specifically it states the bio-availability through the GI tract. How is it possible that this stuff isn't torn apart by enzymes?

The russian website says that it's a peptide of glycine that is able to cross the BBB. In the frequently asked questions it even says "Why can't I just take glycine?".

Obviously I'm confused on how this stuff works. I see a glycine section in the molecule and can almost see the proline part (a bit lost on that one) but does it have to be metabolized to become active?

A percentage of peptides usually make it through the digestive system. However, since everyone's systems are different and there are many enzymes that break apart peptides into amino acids, this becomes increasingly complicated to find an effective solution for an oral dose. Therefore, other methods of internalizing the medicine are usually thought. For the more complicated peptides, there is nasal spray. For smaller molecules, there is the transdermal patch. For either, you can use sublingual (under the tongue) administration.

Just because the percentage that is absorbed by the GI tract crosses the BBB unchanged does not mean that it had 100% absorption. It does not need 100% absorption to "work" because it is such a strong medicine, and a very unique one at that. Also, it may be broken down in the liver into metabolites, this would not affect the "unchanged" adverb because the noopept that did cross the BBB was unchanged. However, this may be of interest to you... noopept is a pro-drug, so it's metabolites are the active drug.

The part that is actively giving the effect is most likely the "racetam" part, but it may work on glycine receptors using the tail end as well. It works as an anti-oxidant, a blood thinner, a complicated calcium and potassium channel modulator, and a cholinergic uptake enhancer like Piracetam.


Hey Devin, did you have a study that showed Noopept to be choline uptake enhancer? (I'm unable to locate one) And do you think that warrants choline supplementation?

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#33 medievil

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Posted 18 November 2011 - 10:04 PM

Piracetam is one but this doesnt mean you need a choline source with it, with choline there's also no way to see what a racetam actually does, and without choline (but fish oil) several had a lot of succes with piracetam, including me. You wont find a study on noopept as i dont think there is one, anyway in rodents piracetam works, and it works without choline, so if your a rodent no need for choline, and as a human not either, its just another nootropic that can synergize with piracetam, and its exactly the same as stacking 2 differend nootropics.

Srry for posting here, but i figured it would be better to continue in this thread instead of spoiling the other one.

#34 manic_racetam

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Posted 18 November 2011 - 11:03 PM

Good call :)

The choline thing is just a imminst myth, there's no evidence at all that any racetam needs a choline source.


I agree with you in regard to most racetams: Ani, oxi, pi... I think the widespread suggestions of choline supplementation are overstated. And I think choline is over-used in general on this forum esp Alpha-GPC and the other forms that cross the BBB directly.

I guess there's no evidence that any racetams need a choline source but specific racetams do have a direct effect on cholinergic systems in the brain.

This abstract shows that pramiracetam "...accelerat[es] hippocampal acetylcholine turnover..."

Also this abstract showing nefiracetam increases uptake and release of transmitters in the cholinergic systems. And I noticed that when I increased my choline bitartrate dosage when I was using nefiracetam it did tend to relieve the headache-like tension in my head related to doses over 900mgs in a day.

Not pretending to know if the body wouldn't be able to naturally compensate for that extra use of choline in general but I can see where people got the idea to supplement it. I guess the empty-head type effects I got on the extended mega-doses of Noopept without any choline supplement could have been from something besides a lack of choline (perhaps over-inhibition of the calcium channels in my hippocampus or something). Admittedly that was just a partially educated guess on my part.

#35 medievil

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Posted 18 November 2011 - 11:06 PM

Nefiracetam is definatly pro cholinergic, as is methylene blue, id be curious how methylene blue would alevate the headaches, if it can do that atleast.

Yes piracetam enhances choline uptake, but it also modulates serotonin and dopamine depending on the dose, this doesnt mean however that youd need a dopaminergic or a srri once on a certain dose.

The reason i replied to the choline suggestion is that people here say that in one breath with piracetam, like they HAVE to be used togheter wich just isnt true, also it could induce bad side effects like depression for those that are sensitive.

Edited by medievil, 18 November 2011 - 11:59 PM.

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#36 manic_racetam

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Posted 19 November 2011 - 01:09 AM

Yes, I agree completely that too much choline is the number one instigator of negative emotional effects with noots. And over-prescribed by the general imminst community with racetams. That's actually the reason I didn't include any choline in my stack while mega-dosing the Noopept; in an attempt to dispel that myth. But it basically backfired on me as far as I can tell. If the strength is really 1,000 times the potency of piracetam then I was dosing an equivalent of 200-300 grams of piracetam per day, which likely caused a few imbalances to say the least.

#37 thedevinroy

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Posted 19 November 2011 - 01:52 AM

Too much choline can cause overmethylation, which is a bitch. Generic folic acid is a pretty good methyl sponge if you know what I mean (always take with the generic B12, too, which will also help). EDIT: Generic as in, not the active form (active forms would be 5-MTHF and Methylcobalamin, respectively).

The study you wanted: http://www.ncbi.nlm....pubmed/11548439

"...increased amplitude of the neural response to acetylcholine (Ach) microappications in 75% of the isolated neurons..."

"... Ach response in a part of neurons was attenuated or even blocked by scopolamine..."

There you have it. It's either a positive allosteric modulator, it increases AChR densities, or it re-sensitizes. Since there are no allosteric binding sites that I'm aware of, I would guess that it would be the other two. There are other posibilities, I suppose, such as direct agonism with low binding affinity, but I doubt it.

Edited by devinthayer, 19 November 2011 - 01:59 AM.

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#38 Austin Diablo

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Posted 01 January 2012 - 02:48 PM

I am dying to try this! Have used Piracetam in conjunction with Centrophenoxine with really good results. If you use Centrophenoxine you definitely don't need any choline because it does for your brain what the choline is supposed to - potentiates acetylcholine release & easily crosses the blood/brain barrier at much lower dosages than the amount of choline you would need for the same effect. It also has anti-aging benefits & supposedly can aid in reversing cellular damage from aging in the brain. I've gotten my nootropics thus far from cerebral health & noopept is next! Also really want to try Sulbutiamine for added pep in my step - I hear cyclists & other athletes use it to focus & push through the "extra mile" in training. Supposedly it's effects last throughout the day, which would be great.

Edited by Austin Diablo, 01 January 2012 - 02:51 PM.


#39 manic_racetam

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Posted 01 January 2012 - 04:20 PM

I am dying to try this! Have used Piracetam in conjunction with Centrophenoxine with really good results. If you use Centrophenoxine you definitely don't need any choline because it does for your brain what the choline is supposed to - potentiates acetylcholine release & easily crosses the blood/brain barrier at much lower dosages than the amount of choline you would need for the same effect. It also has anti-aging benefits & supposedly can aid in reversing cellular damage from aging in the brain. I've gotten my nootropics thus far from cerebral health & noopept is next! Also really want to try Sulbutiamine for added pep in my step - I hear cyclists & other athletes use it to focus & push through the "extra mile" in training. Supposedly it's effects last throughout the day, which would be great.


Hi! Noopept is pretty cool stuff. I have only one suggestion for when you try it though. I'd strongly suggest staying at the 30mg per day oral dose maximum as suggested in the Russian literature. It really seems that all the cognitive benefits are apparent at that daily dosage and it makes side effects non-existent (for me at least).

Also, do you mind providing the links to the use in athletics? I'd really appreciate it :) Feel free to ask any questions too. We've got plenty of people around here with tons of experience with this stuff these days.

#40 Austin Diablo

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Posted 01 January 2012 - 04:40 PM

http://www.weighttra...ts/sulbutiamine http://medsavailable...of-sulbutiamine http://www.lightspeedlabs.com/formula/ http://supplements.r...amine-p226.aspx All of these make mention of the energy & endurance enhancing effects of Sulbutiamine...And thanks for the advice - I was planning on starting with 20mg of Noopept under the tongue then chased by a gram of Centrophenoxine & some fish or krill oil. ;)

#41 Austin Diablo

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Posted 01 January 2012 - 04:44 PM

Just posted 4 or 5 links referencing the energy/endurance aspects of Sulbutiamine but it didn't post for some reason. Just Google "Sulbutiamine and athletic performance"...

#42 Austin Diablo

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Posted 01 January 2012 - 04:58 PM

Thanks, btw, for the dosage advice...I was planning on trying 20 mg under the tongue to start, chased by a gram of Centrophenoxine & some krill or fish oil. :-D

#43 Austin Diablo

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Posted 01 January 2012 - 05:02 PM

Thanks, btw, for the dosage advice...I was planning on starting with just 20 mg of Noopept under my tongue, then chasing it with a gram of Centrophenoxine & some krill or fish oil. I would put a smiley here, but twice now I've hit the post button after putting a smiley & BAM!!! No post!

#44 manic_racetam

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Posted 01 January 2012 - 05:38 PM

Thanks, btw, for the dosage advice...I was planning on starting with just 20 mg of Noopept under my tongue, then chasing it with a gram of Centrophenoxine & some krill or fish oil. I would put a smiley here, but twice now I've hit the post button after putting a smiley & BAM!!! No post!


Oh yeah, you can't post links or pictures (or emoticons apparently, LOL) until you reach 10 posts or something like that. It's to cut down on spam. Those posts have been sent to the admin approval queue and will be deleted or approved when they get to them.

I'm pretty sure normal forum use kicks in after 10 posts but don't quote me on that.

And might I suggest to try swallowing it after a meal or a snack instead of under the tongue? For the first couple of weeks it increases in intensity everyday you take it and sometimes sublingual administration can make it too intense around day 10, which gives some people uncomfortable side effects.

Eating a snack or meal uses up the enzymes that break down Noopept. Then taking Noopept after that allows for pretty thorough absorption through the GI tract. You can gauge the effects more accurately as the effects increase over the first week this way. And you can definitely feel it starting from the first day anyway.

This method is the best IMHO to reduce any risk of side effects and get a better handle on this cool little molecule. Oh yeah, plus you don't have to keep the unpleasant substance under your tongue waiting for it to absorb.

#45 Austin Diablo

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Posted 01 January 2012 - 05:52 PM

Thanks - good to know! I know Piracetam & Centrophenoxine taste pretty awful dissolved in water so I imagine a similar thing melting under the tongue for several minutes would suck pretty hard!

#46 manic_racetam

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Posted 01 January 2012 - 06:09 PM

Thanks - good to know! I know Piracetam & Centrophenoxine taste pretty awful dissolved in water so I imagine a similar thing melting under the tongue for several minutes would suck pretty hard!


Ha! If you think those taste nasty then you're in for a real surprise ;)

#47 Austin Diablo

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Posted 01 January 2012 - 06:21 PM

Oh gawd...Let me guess...It tastes like acid reflux, hamster vomit & whino poop?!

#48 Baten

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Posted 01 January 2012 - 07:08 PM

Oh gawd...Let me guess...It tastes like acid reflux, hamster vomit & whino poop?!


It's just a tad nastier than centrophenoxine actually. It's nothing as long as it sticks nicely under your tongue.
Once some bits of the saliva+noop solution slips into your mouth, though, you're in for a nasty surprise. Have some water at hand to gulp down :P

#49 manic_racetam

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Posted 02 January 2012 - 03:57 PM

Oh gawd...Let me guess...It tastes like acid reflux, hamster vomit & whino poop?!


hmmm... not really sure what most of those taste like but from my experience it's more like extremely concentrated dried mushroom extract and gasoline actually... but honestly bearable, unlike pramiracetam which really just tastes like poison and intuitively makes you want to spit it out and rinse your tongue for at least 15 minutes.
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#50 Baten

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Posted 03 January 2012 - 02:42 PM

Oh gawd...Let me guess...It tastes like acid reflux, hamster vomit & whino poop?!


hmmm... not really sure what most of those taste like but from my experience it's more like extremely concentrated dried mushroom extract and gasoline actually... but honestly bearable, unlike pramiracetam which really just tastes like poison and intuitively makes you want to spit it out and rinse your tongue for at least 15 minutes.


I honestly doubt that anyone would ever forget the taste of pramiracetam. Nightmare material.
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#51 Austin Diablo

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Posted 07 January 2012 - 11:40 PM

Oh gawd...Let me guess...It tastes like acid reflux, hamster vomit & whino poop?!


It's just a tad nastier than centrophenoxine actually. It's nothing as long as it sticks nicely under your tongue.
Once some bits of the saliva+noop solution slips into your mouth, though, you're in for a nasty surprise. Have some water at hand to gulp down :P


Hate to say it but Centrophenoxine actually reminds my of meth in taste for some reason...Not totally, but one aspect is very similar. Not a meth head, but back in my partying days I did it a couple times.

#52 xzyn

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Posted 26 January 2012 - 09:53 AM

I always dissolve my noopept in an 10% ethanol - water based solution. I keep it in the fridge to make sure it doesn't get spoiled somehow. I am no chemist but this method seems to work fine. I make a 1g/100ml solution which makes precise dosing simple ( take a syringe, pull 1ml in, put it in your mouth and wait a few mins before swallowing. )


gotta agree with the thing about pramiracetam lol .. truly a nightmare
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#53 americancanadian3360

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Posted 04 December 2013 - 04:39 PM

hey guys, so i went to my higher up at the chemistry department and found out within a millisecond that noopept is definetely soluble, on top of which "Dr. X" told me it would most likely suspend in acetic acid without any alteration to the compound, im going to get a couple clean vials and start immersing them together and start injections by friday, i am hoping to see a stronger bioavailability when injected subQ and also looking to avoid that awful "horse dick" taste as described by my close friend who first brought up the beautiful compound with me while vacationing Europe this summer!

#54 Wanderer2

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Posted 14 January 2014 - 05:02 AM

hey guys, so i went to my higher up at the chemistry department and found out within a millisecond that noopept is definetely soluble, on top of which "Dr. X" told me it would most likely suspend in acetic acid without any alteration to the compound, im going to get a couple clean vials and start immersing them together and start injections by friday, i am hoping to see a stronger bioavailability when injected subQ and also looking to avoid that awful "horse dick" taste as described by my close friend who first brought up the beautiful compound with me while vacationing Europe this summer!



So how did it work out?

Edited by Wanderer2, 14 January 2014 - 05:02 AM.


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#55 synchromesh

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Posted 30 July 2014 - 07:52 PM

Hello all,

 

I received my Noopept powder from intellimeds.co.uk today; while I wait for my milligram scales to arrive I've measured 0.10g of Noopept (using my centigram scales) into 10ml of water (on which most of the powder floated) and 40ml of single-malt whisky (into which everything dissolved nicely). So that should keep me going for a week or two. I'm going to start with 10mg once or twice per day after a meal for five days and have the weekends off.

 

I also have Modafinil, ALCAR, Citicoline and Pramiracetam capsules to work with. I'm starting with the ALCAR and some Alpha GPC I have kicking around, and once that's gone I'll start the Citicoline.

 







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