265 replies to this topic

[NootropicEU]

TLR sells it as a research chemical, however it can be bought in Russian pharmacies as well. They call it "Pill for your memory". 10 mg x 50 tabs cost only 300 RUB which is about 6 GBP. I am wondering if anyone has ever tried it...

Originally Posted by Riemann Zeta
Noopept (GVS-111) - First Trial - This One's Special

This is my first trial of an experimental pre-clinical cognitive enhancing compound known as Noopept (GVS-111). The compound could loosely be called a piracetam derivative, but in reality it is a pyrrolidine-containing dipeptide. The standardized long-form chemical name of noopept is: N-phenylacetyl-L-prolyl-glycine ethyl ester...just rolls off the tongue, right? Despite the fact that it is a peptide, it is said to be bioavailable and gets to the brain after sublingual, oral and (probably) intranasal administration. Anyway, like the more well known phenylpiracetam, this compound is a Russian-designed nootropic indicated as a neuroprotectant and general cognition expander. There is an older Russian paper (Ostrovskaya et al, 2002) claiming that it is 200-50000 times as potent as good old piracetam in animal models of drain bamage . As it turns out, it's good shit. While phenylpiracetam didn't live up to its promised (i.e. extraordinarily hyped) potency compared to the rest of the 'racetam series, but this one might.

My first dose was a modest 5mg, taken sublingually. Not too much was noticed, effect-wise. Anything that was noticed was likely placebo, a result of the overall excitement of trying a brand new experimental chemical. The second dose the next day was 10mg, again taken sublingually. This time the effects were more apparent: a general increase in alertness/awareness without any kind of amphetaminergic stimulation. Over the next few days, the dose was increased to 10-15mg BID. The effects of this compound seem cumulative, increasing over a few days of dosing (like most of the other piracetam derivatives). During the 4th or 5th day in, I definitely notice an increase in fluidity while writing--it seems more effortless--and my attention is increased. I normally take dextroamphetamine daily for ADD and noopept syncs very nicely with the amphetamine. Pramiracetam was another racetam compound that I found to sync well with amphetamine, but it seemed to greatly increased jaw muscle tension (which I normally don't get unless I'm on a psychedelic). Noopept, on the other hand, feels extremely smooth and crystal clean in concert with (d)-amphetamine. In addition, noopept seems to exert a nice light anxiolytic effect--not a sedating anxiolytic effect, but a feeling that you can handle multitasking without getting overwhelmed.

In short, noopept is highly recommended--it is probably the best piractam-like compound that I have tried (a list that includes piracetam, aniracetam, oxiracetam, pramiracetam and phenylpiracetam). If I had to stand up and pull a number out of my ass, I would say that it is at least a 1000 times the potency of piracetam, but with more enjoyable and profound effects.

Attached Files

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Edited by anony4mous, 07 April 2009 - 11:41 AM.

[NootropicEU]

Noopept stimulates the expression of NGF and BDNF in rat hippocampus.

Ostrovskaya RU, Gudasheva TA, Zaplina AP, Vahitova JV, Salimgareeva MH, Jamidanov RS, Seredenin SB.
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow. rita@nicemail.ru

We studied the effect of original dipeptide preparation Noopept (N-phenylacetyl-L-prolylglycine ethyl ester, GVS-111) with nootropic and neuroprotective properties on the expression of mRNA for neurotropic factors NGF and BDNF in rat hippocampus. Expression of NGF and BDNF mRNA in the cerebral cortex and hippocampus was studied by Northern blot analysis. Taking into account the fact that pharmacological activity of Noopept is realized after both acute and chronic treatment, we studied the effect of single and long-term treatment (28 days) with this drug. Expression of the studied neurotropic factors in the cerebral cortex was below the control after single administration of Noopept, while chronic administration caused a slight increase in BDNF expression. In the hippocampus, expression of mRNA for both neurotrophins increased after acute administration of Noopept. Chronic treatment with Noopept was not followed by the development of tolerance, but even potentiated the neurotrophic effect. These changes probably play a role in neuronal restoration. We showed that the nootropic drug increases expression of neurotrophic factors in the hippocampus. Our results are consistent with the hypothesis that neurotrophin synthesis in the hippocampus determines cognitive function, particularly in consolidation and delayed memory retrieval. Published data show that neurotrophic factor deficiency in the hippocampus is observed not only in advanced Alzheimer's disease, but also at the stage of mild cognitive impairment (pre-disease state). In light of this our findings suggest that Noopept holds much promise to prevent the development of Alzheimer's disease in patients with mild cognitive impairment. Moreover, therapeutic effectiveness of Noopept should be evaluated at the initial stage of Alzheimer's disease.

PMID: 19240853 [PubMed - indexed for MEDLINE]

[jackinbox]

Team Life Reseach says they have it:

http://teamliferesea...6b5983a78774e12

Who want to report by on it?

[yowza]

Team Life Reseach says they have it:

http://teamliferesea...6b5983a78774e12

Who want to report by on it?

I'd be interested in hearing from anybody who orders this and tries it out. I'm planning to order some at some point.

Here's a great scale that I found that can be used to measure out powdered amounts if anyone chooses to order.

This scale measures down to .001g (or 1 mg). I've just ordered 1 and will report back on it's accuracy if anyone's interested.
http://okpocketscale...products_id=463

[jackinbox]

Team Life Reseach says they have it:

http://teamliferesea...6b5983a78774e12

Who want to report by on it?

I'd be interested in hearing from anybody who orders this and tries it out. I'm planning to order some at some point.

Here's a great scale that I found that can be used to measure out powdered amounts if anyone chooses to order.

This scale measures down to .001g (or 1 mg). I've just ordered 1 and will report back on it's accuracy if anyone's interested.
http://okpocketscale...products_id=463

You can have it cheaper on ebay:
http://cgi.ebay.ca/0...2|39:1|240:1318

[jackinbox]

Here is a 2001 article from CNN that mention Nooprept (GVS-111):
http://money.cnn.com...13327/index.htm

They also mention another mysterious substance with the codename 006 supposed to "make circles around piracetam".

[wild2side]

Here is a 2001 article from CNN that mention Nooprept (GVS-111):
http://money.cnn.com...13327/index.htm

They also mention another mysterious substance with the codename 006 supposed to "make circles around piracetam".

I still would not trust taking this drug without more independent research on its effects and toxicology. I used to live in Russia and all of my family still does and believe me, things aren't as regulated as they are in EU and NA. In particular, bribes can get a whole lot of things done and fast. You need a university degree? Np, just pay off the dean and you have it. Need a prescription for some narcotics, again no prob - just bribe a doctor and he will write you any prescription you want. This type of deal making works in all facets of Russian life.

So the fact that this drug is marketed in Russia says nothing in terms of passing any stringent safety control.

[NootropicEU]

Here is a 2001 article from CNN that mention Nooprept (GVS-111):
http://money.cnn.com...13327/index.htm

They also mention another mysterious substance with the codename 006 supposed to "make circles around piracetam".

I still would not trust taking this drug without more independent research on its effects and toxicology. I used to live in Russia and all of my family still does and believe me, things aren't as regulated as they are in EU and NA. In particular, bribes can get a whole lot of things done and fast. You need a university degree? Np, just pay off the dean and you have it. Need a prescription for some narcotics, again no prob - just bribe a doctor and he will write you any prescription you want. This type of deal making works in all facets of Russian life.

So the fact that this drug is marketed in Russia says nothing in terms of passing any stringent safety control.

I agree with you, however there is enough research done on Noopept. Check pubmed.

Edited by anony4mous, 08 April 2009 - 04:29 PM.

[blazewind]

I am surprised that more people are not trying this and reporting. It has very favorable studies on pubmed.

1.5 years ago I bought noopept from TLR and then imported it from Russia through someone I contacted on the internet (I offered him double the cost so $20/500mg and bought 5 boxes, also exporting medicine in Russia is illegal)

From the literature I decided the optimal dosage was 50mg/day, importing from Russia was a hassle, and I ran out of money.

It did not give me some crazy photographic memory effect I was looking for at the time when I was also taking 10 other nootropics, so I decided it was not worth it to continue at the moment.

I got a synthesis quote from China, $1700/1kg, I intend to get it synthesized when I get a full time job.

Also I recently came across this: http://www.bluelight...ad.php?t=417159

Maybe Sublingual is more effective?

[yowza]

I am surprised that more people are not trying this and reporting. It has very favorable studies on pubmed.

1.5 years ago I bought noopept from TLR and then imported it from Russia through someone I contacted on the internet (I offered him double the cost so $20/500mg and bought 5 boxes, also exporting medicine in Russia is illegal)

From the literature I decided the optimal dosage was 50mg/day, importing from Russia was a hassle, and I ran out of money.

It did not give me some crazy photographic memory effect I was looking for at the time when I was also taking 10 other nootropics, so I decided it was not worth it to continue at the moment.

I got a synthesis quote from China, $1700/1kg, I intend to get it synthesized when I get a full time job.

Also I recently came across this: http://www.bluelight...ad.php?t=417159

Maybe Sublingual is more effective?

I'm thinking nasal administration could possibly be pretty effective if this was developed.

Here's other names that Noopept also goes by if someone wants to put in a search:
IUPAC/Chemical Name (this you can type into chemical search databases like e-molecule or chemindustry.com): N-phenyl-acetyl-L-prolyl-glycine ethyl ester

Code Names for Noopept: SGS-111/GVS-111/DVD111

It appears that years ago Saegis Pharmaceutical (used to be Davids Pharma back when it started up in 1999) was able to license Noopept from the Russian Academy of Sciences years ago for clinical trials and used a code name (seen above) for Noopept here in the states. For some odd reason the company quit development on the product and it went in limbo (see link below for SGS-111/codename for Noopept).
http://74.125.95.132.../content/pdf/cd- 547164.pdf+sgs-111%2Bpipeline&cd=1&hl=en&ct=clnk&gl=us

http://money.cnn.com...13327/index.htm (2001 overview of who was involved with the development of cognative enhancers such as Noopept)

Back in 2004, it looks like Saegis decided to outlicense it for whatever reason and there hasn't been much info. since. Unfortunately, Saegis website is down (they may have changed their name again over the past few years) so it's hard to see whatever became of this.

There's a supplier overseas that can ship over here but they'd probably want to do it in bulk.

[Guacamolium]

Though I'm quite sure this wouldn't be as popular as nasal or sublingual administration; due to its chemical make-up I think it would fare very well administered subcutaneously. I guess making a nasal preparation from scratch would be about as easy now that I think about it....

*thinks of Flonase and shudders*

[IronFanatic]

Does Pharmacy1010 sell Noopept?

[NootropicEU]

Does Pharmacy1010 sell Noopept?

No.

[yowza]

The only way to get Noopept at the moment (besides TLR) is thru another chemical supply company (who probably sell miniscule amounts for high $) or Bulk order. Here's an e-mail, I've recieved from a supplier for the bulk order of Noopept:

thank you for your inquired
For the GVS-111 the price for 225 gram is USD 1500 , 450 grams is USD 2000, 1kg is USD 3000
deliver time is 4 weeks, and you need prepay .
If you have any comment, pls let me know, I will try to help you

From various studies, it seems no more than 50 mg of Noopept would be used per day. $1500/6=$250 per person (still alot of $ unfortunately), which would mean 225/6=37.5grams (37,500mg) per person for $250. 37,500/50 (mg per day)=750 days if someone were to take all the way up to 50 mg per day (which may not be recommended).

At 365 days in a year, this amount could last someone about 2 years (and that's only if they took it in higher amounts every day, which obviously I wouldn't do) based on the math for a bulk order of 6 people.

Edited by yowza, 15 April 2009 - 04:31 AM.

[skinniest200]

I have tried it and didn't notice any effects from doses ranging from under 1mg up to 100mg. I'm also the person that started that thread at bluelight and reposted Riemann Zeta's trip report. I ordered mine from TLR, their customer service is excellent. I seem to be a non-responder to most nootropics, so your results could very likely be different. I have the synthesis procedure for noopept and it doesn't look too hard or require special equipment, if anybody is interested. I've got like 250mg left in solution, so I'm looking for people I know that would like to try a dose. There's more info in a thread where I speculate that noopept is probably a pro-drug of something else, I'll try to find it.

[skinniest200]

Here's the thread I was talking about - http://www.imminst.o...o...ic=27545

[blazewind]

pharmacy1010 has added noopept for $16 (russian price is $10)


I think Noopept may be similar to vasopressin.
Vasopressin gets metabolized, and only a fragment of it deals with memories processes in the brain.
The main metabolite of noopept, cycloproglycine, is found naturally in the brain.
Since it is very similar to piracetam, and 1000X more potent than piracetam, this may be what piracetam's method of action is working on.

------------------------------------------------------------------------------------------------------
[Design of the novel dipeptide neuropsychotropic drug preparations]
[Article in Russian]

Gudasheva TA, Skoldinov AP.

Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.

The paper considers a new strategy in the field of neuropsychotropic dipeptide drug design, the main points being as follows: (i) determination of the structural elements of dipeptides, such as fragments of amino acid side radicals and peptide bonds, in nonpeptide drugs; (ii) design of peptide analogs topologically close to the drug; (iii) synthesis and activity testing of these analogs; (iv) determination of the corresponding endogenous neuropeptide among the known neuropeptides or identification of the new neuropeptides in the brain of experimental animals. Using this approach, new pyroglutamyl- and prolyl-containing dipeptides were obtained based on the structure of the well-known classical nootropic drug piracetam. The new drugs exhibit nootropic activity in doses 100-10,000 times lower than those of piracetam. The structure of most active pyroglutamyl dipeptide pGlu-Asn-NH2 coincides with that of the N-end fragment of the endogenous memory peptide AVP(4-9). Noopept (N-phenylacetylprolylglycine ethyl ester), patented in Russia and USA as a new nootropic drug, is currently under stage 2 of successful clinical trials. The main metabolite of noopept, cyclo-Pro-Gly, is identical to the endogenous dipeptide designed in this work and is most close analog of piracetam with respect to pharmacological activity. The universal character of the proposed strategy is demonstrated by the design of active dipeptide analogs of an atypical neuroleptic drug sulpiride. As a result, a potential dipeptide neuroleptic dilept was obtained, which has been patented in Russia and now passes broad preclinical trials.

----------------------------------------------------------------------------------------------------------------------------------------

pdf of actual study: http://www.scribd.co...ents-Disruption


No. 302, a newly synthesized [pGlu4,Cyt 6]AVP(4-9) analogue, prevents
the disruption of avoidance behavior

Kenji Hirate a,,, Masuharu Hirano a, Yoshiharu Nakajima b, Akio Hiyama a, Osamu Maeda a,
Wataru Asakura ~
a Research Laboratories, Nippon Chemiphar Co. Ltd., Misato, Saitama 341, Japan
b Pharmaceuticals Research Laboratories, Fujirebio Inc., Hachioji, Tokyo 192, Japan
Received 8 July 1995; revised 5 February 1996; accepted 6 February 1996
Abstract
We investigated the effects of [pGIu4,Cyt6]AVP(4-9) fragments and its analogues on cycloheximide (CHX)-induced learning
impairment in rats using the step-through-type passive avoidance test in rats. CHX (2.8 mg/kg, s.c.) significantly shortened the
step-through latency in the retention trial, pGlu-Asn-Cys(Cys)-Pro-Arg-Gly-NH2 ([pGlu4,Cyt6]AVP(4--9); 10 ng/kg, s.c.), a
major metabolite of arginine vasopressin, improved the CHX-induced learning impairment. Asn-Cys-Pro-Arg-OH
(I-Cys 6] AVP(5-8); 1 ng/kg) corrected avoidance learning in the CHX-treated group, whereas neither Cys(Cys)-Pro-Arg-OH nor
pGlu-Asn-Cys(Cys)-Pro-OH had any effect (1, 10 and 100 ng/kg, s.c.), pGlu-Asn-Ser-Pro-Arg-Gly-NH2 (No. 302), a newly
synthesized [pGlu4,Cyt6]AVP(4-9) analogue, significantly prolonged the latency shortened by CHX at doses of 0.1, 1 and
10 ng/kg (s.c.). Asn-Ser-Pro-Arg-OH also improved the learning disruption induced by CHX, although the effective dose was
100 times higher than that of No. 302. The half-life of No. 302 in rat blood was about 5.5, 22 and 25 times longer than that of
l- pGlu4,Cyt 6] AVP (4-9), [Cys 6] AVP (5-8) and Asn-Ser-Pro-Arg-OH, respectively. These results suggest that [Cys 6] AVP (5-8)
is the minimal effective amino acid sequence in [pGIu4,Cyt6]AVP(4-9), and show that No. 302 is a potent, pharmacologically
active peptide with high stability in the blood.


--------------------------------------------------------------------------------------------------------------------

pdf of actual study: http://www.scribd.co...loprolylglycine



Identification of a novel endogenous memory facilitating cyclic dipeptide
cyclo-prolylglycine in rat brain

T.A. Gudashevaa,*, S.S. Boykoa, V.Kh. Akparovb , R.U. Ostrovskayaa, S.P. Skoldinova,
G.G. Rozantseva, T.A. Voroninaa, V.P. Zherdeva, S.B. Seredenina
'Institute of Pharmacology, Russian Academy of Medical Science, Baltijskaya, 8, Moscow, 125315, Russian Federation
bState Institute of Genetics and Selection of Industrial Microorganisms, I-st Dorojny proezd, 1, Moscow, 113545 Russian Federation
Received 10 June 1996
Abstract Using high-performance liquid chromatography, gaschromatography
and chromato-mass spectrometry methods a
novel endogenous cyclic dipeptide cyclo-prolylglycine was
identified in rat brain. Its content according to gas chromatography
is 2.8 ± 0.3 nmoUg wet brain. Synthetic cyclo-prolylglycine
has demonstrated anti amnesic activity in the passive
avoidance test in rats at a dose of 0.1 mg/kg i.p. Cyclic dipeptide
cyclo-prolylglycine seems to be a memory facilitating substance
and its presence in rat brain suggests the existence of a new
mechanism of memory regulation.
Key words: Cyclo-prolylglycine; Endogenous cyclic
dipeptide; Memory facilitating substance
1. Introduction
In spite of the fact that many neuropeptides influence training
and memory, only some of them, it is presumed, directly
control these processes [1,2]. The best known is the major
arginine-vasopressin metabolite, [pGly4,Cyt5]AVP(4-9), which
facilitates the consolidation stage of memory formation [3,4],
At the same time there are exogenous medicines, so-called
nootropics, with piracetam as the main representative, which
selectively facilitate processes of training and memory [5,6]. In
1985 we [7] put forward the hypothesis that the classical nootropic
piracetam acts as a peptidomimetic. On the basis of this
hypothesis active dipeptide analogues of piracetam were received
that possessed proline or pyroglutamic acid as their Nterminal
pyrrolidine-containing amino acid. Among the designed
pyroglutamyl-containing dipeptides pyroglutamylasparagine
amide turned out to be the most active [8]. It displayed
nootropic activity in the passive avoidance test in rats
at a dose of 0.01 mg/kg i.p. This effect depended on the
stereochemistry of both amino acid residues [9]. The structure
of pyroglutamylasparagine amide coincides with an N-terminal
fragment of a major vasopressin metabolite,
[pGlu4,Cytfi]AVP(4-9), responsible for the central effects of
the latter [3]. These facts allowed us to assume that piracetam
*Corresponding author. Fax: (7) (95) 1511261.
E-mail: Uusolari@solaris.msk.ru (Internet)
Abbreviations: AA, antiamnesic activity; amu, atomic mass unit;
AVP, arginine vasopressin; FAB, fast atom bombarding mass
spectrometry; GC, gas chromatography; GC-MS, gas chromatography-
mass spectrometry; HPLC, high-performance liquid chromatography;
MES, maximal electroconvulsive shock; MOPS, 3-
morpholinopropanesulfonic acid; PDAH, pyrrolidino-[1,2-a)-2,6-diazacyc1oheptanedione-
I,5; RIC, relative ion current; SIM, selected ion
monitoring; UV, ultraviolet
displays activity due to interaction with one vasopressin receptor
subtype. We have found out, however, that unlike
piracetam, which facilitates the initial processing of memory
engram as well as consolidation, the dipeptide pGlu-Asn-NH2
improved only the phase of information input and retrieval,
but did not influence consolidation [10]. On the other hand,
proline-containing dipeptide analogues of piracetam facilitated
consolidation [11]. The cyclic dipeptide cyclo-(Pro-Gly)
turned out to be the most active of them [12). This cyclic
dipeptide can be assumed to be one of the endogenous ligands
of hypothetic 'nootropic receptors', which selectively regulates
the processes of training and memory. This work is devoted to
the identification of endogenous cyclo-(Pro-Gly) in rat brain.
---------------------------------------------------------------------

Edited by blazewind, 19 April 2009 - 11:24 PM.

[yowza]

pharmacy1010 has added noopept for $16 (russian price is $10)


I think Noopept may be similar to vasopressin.
Vasopressin gets metabolized, and only a fragment of it deals with memories processes in the brain.
The main metabolite of noopept, cycloproglycine, is found naturally in the brain.
Since it is very similar to piracetam, and 1000X more potent than piracetam, this may be what piracetam's method of action is working on.

------------------------------------------------------------------------------------------------------
[Design of the novel dipeptide neuropsychotropic drug preparations]
[Article in Russian]

Gudasheva TA, Skoldinov AP.

Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.

The paper considers a new strategy in the field of neuropsychotropic dipeptide drug design, the main points being as follows: (i) determination of the structural elements of dipeptides, such as fragments of amino acid side radicals and peptide bonds, in nonpeptide drugs; (ii) design of peptide analogs topologically close to the drug; (iii) synthesis and activity testing of these analogs; (iv) determination of the corresponding endogenous neuropeptide among the known neuropeptides or identification of the new neuropeptides in the brain of experimental animals. Using this approach, new pyroglutamyl- and prolyl-containing dipeptides were obtained based on the structure of the well-known classical nootropic drug piracetam. The new drugs exhibit nootropic activity in doses 100-10,000 times lower than those of piracetam. The structure of most active pyroglutamyl dipeptide pGlu-Asn-NH2 coincides with that of the N-end fragment of the endogenous memory peptide AVP(4-9). Noopept (N-phenylacetylprolylglycine ethyl ester), patented in Russia and USA as a new nootropic drug, is currently under stage 2 of successful clinical trials. The main metabolite of noopept, cyclo-Pro-Gly, is identical to the endogenous dipeptide designed in this work and is most close analog of piracetam with respect to pharmacological activity. The universal character of the proposed strategy is demonstrated by the design of active dipeptide analogs of an atypical neuroleptic drug sulpiride. As a result, a potential dipeptide neuroleptic dilept was obtained, which has been patented in Russia and now passes broad preclinical trials.

----------------------------------------------------------------------------------------------------------------------------------------

pdf of actual study: http://www.scribd.co...ents-Disruption


No. 302, a newly synthesized [pGlu4,Cyt 6]AVP(4-9) analogue, prevents
the disruption of avoidance behavior

Kenji Hirate a,,, Masuharu Hirano a, Yoshiharu Nakajima b, Akio Hiyama a, Osamu Maeda a,
Wataru Asakura ~
a Research Laboratories, Nippon Chemiphar Co. Ltd., Misato, Saitama 341, Japan
b Pharmaceuticals Research Laboratories, Fujirebio Inc., Hachioji, Tokyo 192, Japan
Received 8 July 1995; revised 5 February 1996; accepted 6 February 1996
Abstract
We investigated the effects of [pGIu4,Cyt6]AVP(4-9) fragments and its analogues on cycloheximide (CHX)-induced learning
impairment in rats using the step-through-type passive avoidance test in rats. CHX (2.8 mg/kg, s.c.) significantly shortened the
step-through latency in the retention trial, pGlu-Asn-Cys(Cys)-Pro-Arg-Gly-NH2 ([pGlu4,Cyt6]AVP(4--9); 10 ng/kg, s.c.), a
major metabolite of arginine vasopressin, improved the CHX-induced learning impairment. Asn-Cys-Pro-Arg-OH
(I-Cys 6] AVP(5-8); 1 ng/kg) corrected avoidance learning in the CHX-treated group, whereas neither Cys(Cys)-Pro-Arg-OH nor
pGlu-Asn-Cys(Cys)-Pro-OH had any effect (1, 10 and 100 ng/kg, s.c.), pGlu-Asn-Ser-Pro-Arg-Gly-NH2 (No. 302), a newly
synthesized [pGlu4,Cyt6]AVP(4-9) analogue, significantly prolonged the latency shortened by CHX at doses of 0.1, 1 and
10 ng/kg (s.c.). Asn-Ser-Pro-Arg-OH also improved the learning disruption induced by CHX, although the effective dose was
100 times higher than that of No. 302. The half-life of No. 302 in rat blood was about 5.5, 22 and 25 times longer than that of
l- pGlu4,Cyt 6] AVP (4-9), [Cys 6] AVP (5-8) and Asn-Ser-Pro-Arg-OH, respectively. These results suggest that [Cys 6] AVP (5-8)
is the minimal effective amino acid sequence in [pGIu4,Cyt6]AVP(4-9), and show that No. 302 is a potent, pharmacologically
active peptide with high stability in the blood.


--------------------------------------------------------------------------------------------------------------------

pdf of actual study: http://www.scribd.co...loprolylglycine



Identification of a novel endogenous memory facilitating cyclic dipeptide
cyclo-prolylglycine in rat brain

T.A. Gudashevaa,*, S.S. Boykoa, V.Kh. Akparovb , R.U. Ostrovskayaa, S.P. Skoldinova,
G.G. Rozantseva, T.A. Voroninaa, V.P. Zherdeva, S.B. Seredenina
'Institute of Pharmacology, Russian Academy of Medical Science, Baltijskaya, 8, Moscow, 125315, Russian Federation
bState Institute of Genetics and Selection of Industrial Microorganisms, I-st Dorojny proezd, 1, Moscow, 113545 Russian Federation
Received 10 June 1996
Abstract Using high-performance liquid chromatography, gaschromatography
and chromato-mass spectrometry methods a
novel endogenous cyclic dipeptide cyclo-prolylglycine was
identified in rat brain. Its content according to gas chromatography
is 2.8 ± 0.3 nmoUg wet brain. Synthetic cyclo-prolylglycine
has demonstrated anti amnesic activity in the passive
avoidance test in rats at a dose of 0.1 mg/kg i.p. Cyclic dipeptide
cyclo-prolylglycine seems to be a memory facilitating substance
and its presence in rat brain suggests the existence of a new
mechanism of memory regulation.
Key words: Cyclo-prolylglycine; Endogenous cyclic
dipeptide; Memory facilitating substance
1. Introduction
In spite of the fact that many neuropeptides influence training
and memory, only some of them, it is presumed, directly
control these processes [1,2]. The best known is the major
arginine-vasopressin metabolite, [pGly4,Cyt5]AVP(4-9), which
facilitates the consolidation stage of memory formation [3,4],
At the same time there are exogenous medicines, so-called
nootropics, with piracetam as the main representative, which
selectively facilitate processes of training and memory [5,6]. In
1985 we [7] put forward the hypothesis that the classical nootropic
piracetam acts as a peptidomimetic. On the basis of this
hypothesis active dipeptide analogues of piracetam were received
that possessed proline or pyroglutamic acid as their Nterminal
pyrrolidine-containing amino acid. Among the designed
pyroglutamyl-containing dipeptides pyroglutamylasparagine
amide turned out to be the most active [8]. It displayed
nootropic activity in the passive avoidance test in rats
at a dose of 0.01 mg/kg i.p. This effect depended on the
stereochemistry of both amino acid residues [9]. The structure
of pyroglutamylasparagine amide coincides with an N-terminal
fragment of a major vasopressin metabolite,
[pGlu4,Cytfi]AVP(4-9), responsible for the central effects of
the latter [3]. These facts allowed us to assume that piracetam
*Corresponding author. Fax: (7) (95) 1511261.
E-mail: Uusolari@solaris.msk.ru (Internet)
Abbreviations: AA, antiamnesic activity; amu, atomic mass unit;
AVP, arginine vasopressin; FAB, fast atom bombarding mass
spectrometry; GC, gas chromatography; GC-MS, gas chromatography-
mass spectrometry; HPLC, high-performance liquid chromatography;
MES, maximal electroconvulsive shock; MOPS, 3-
morpholinopropanesulfonic acid; PDAH, pyrrolidino-[1,2-a)-2,6-diazacyc1oheptanedione-
I,5; RIC, relative ion current; SIM, selected ion
monitoring; UV, ultraviolet
displays activity due to interaction with one vasopressin receptor
subtype. We have found out, however, that unlike
piracetam, which facilitates the initial processing of memory
engram as well as consolidation, the dipeptide pGlu-Asn-NH2
improved only the phase of information input and retrieval,
but did not influence consolidation [10]. On the other hand,
proline-containing dipeptide analogues of piracetam facilitated
consolidation [11]. The cyclic dipeptide cyclo-(Pro-Gly)
turned out to be the most active of them [12). This cyclic
dipeptide can be assumed to be one of the endogenous ligands
of hypothetic 'nootropic receptors', which selectively regulates
the processes of training and memory. This work is devoted to
the identification of endogenous cyclo-(Pro-Gly) in rat brain.
---------------------------------------------------------------------

Very informative response. Thanks alot. I'm still re-reading it and taking things in. I bought Desmopressin from antiaging-systems.com a while back. The effects are very substle but it does help out. One interesting book that really provides a lot of perspective on peptide/steroid drugs is in the book "Cognative Enhancing Drugs" by Birkhauser (a book that I purchased a year ago that's more concerned with covering categorical classes of potential nootropics as opposed to specific nootropics):
There's a specific chapter (pg.115) that can be found at the following link that kind of sums up the effects of Desmopressin (and other peptide analogues): http://books.google....khauser#PPP1,M1. I could scan a few pages from the peptide chapter if anyone's interested in learning about peptide compounds being used as nootropics (I'd just put it up under my profile page or whatever).

All it took to get the Noopept up on the pharmacy1010 site, was me requesting this to be put on there. All I did was click on the option where you talk to a customer service rep. online and requested it. I was very surprised to see that they provided this for a reasonable price! If there's any other Russian nootropics that aren't on the site, it may be possible to request them (assuming they're from Russia of course).

Edited by yowza, 20 April 2009 - 01:43 AM.

[NootropicEU]

It's my first day on Noopept. To be honest I do not feel anything yet. I guess it will take couple of days for me to start feeling the effect. Otherwise I will increase the dose.

I am aware of several members who have ordered Noopept recently. Could you share you experience? Am I the only one who does not feel any effects?

Edited by anony4mous, 07 May 2009 - 11:43 AM.

[jackinbox]

It's my first day on Noopept. To be honest I do not feel anything yet. I guess it will take couple of days for me to start feeling the effect. Otherwise I will increase the dose.

I am aware of several members who have ordered Noopept recently. Could you share you experience? Am I the only one who does not feel any effects?

How much did you take? I'm on my second day at 10mg.

[jackinbox]

does anyone know the half-life of Noopept? I feel slightly more motivated and less depressed this morning (took 10mg noopept) even if I didn't take my Wellbutrin. Can't say for sure if it's related to noopept or not.

[jackinbox]

I took 30 mg over the course of the evening yesterday. I didn't feel anything but I didn't engage in any social activity so if it's like piracetam, it's normal to not notice anything. It was slightly harder to get an erection but not as worse as it is when I take theanine. I have to be stimulated for a longer period of time before my willy begin to respond. After he wakes up, everything is fine.

[chilp]

It was slightly harder to get an erection but not as worse as it is when I take theanine. I have to be stimulated for a longer period of time before my willy begin to respond. After he wakes up, everything is fine.

What ? I didn't know theanine had an effect on erection...any links to this ?

[jackinbox]

It was slightly harder to get an erection but not as worse as it is when I take theanine. I have to be stimulated for a longer period of time before my willy begin to respond. After he wakes up, everything is fine.

What ? I didn't know theanine had an effect on erection...any links to this ?

I didn't find any reference to it. It just make it a little harder to start the motor but once it's started everything is ok (no problem maintaining the erection). It might have something to to with the relaxation effect.

[jackinbox]

Could someone translate this?

[yowza]

Uggghh...

Dude, I don't mean to seem rude but could you maybe look thru the posts? There's some good info. on dosages and other stuff that's already been posted.

If you search the internet (using yandex; a russian search engine) you'll find a Russian site with the instructions. Google translate it and you're good to go.

[jackinbox]

Thanks. I didn't know about yandex and couldn't find the blinding obvious official Noopept website (http://www.noopept.ru). I should have figured that out! Here is what I got from the website (automatically translated):

On medication

Noopept ® helps to restore memory and cognitive functions, disturbed as a result - the brain injury, ischemia, hypoxia, the effects of alcohol and other toxic substances.

Noopept ® is nootropnym drug peptide structure. Noopepta uniqueness lies in the fact that in the body, it forms an active metabolite, with identical endogenous dipeptidu nootropnoy activity that fiziologichno and safe for humans. Noopept possesses neuroprotective properties - protects brain cells from exposure to damaging factors.

Therapeutic effect Noopepta evident with 5-7 days of treatment, in the form of protivotrevozhnogo and tonic effects. At 7-14 days of therapy, there vegetonormalizuyuschee effect, normalization of sleep. From 14-20 days of therapy revealed a positive effect on cognitive function of the drug, the parameters of attention and memory.

For its effectiveness Noopept ® PIRACETAM exceeds that found in clinical studies, patients with vascular cognitive disorders and posttraumatic genesis.
According to clinical studies, the risk of side effects while taking Noopepta almost twice lower than at admission piratsetama, suggesting the safety of the drug.

® Noopept not cumulative in the body, does not cause drug dependence. With the lifting of the drug is not the abolition of the syndrome.

Noopept ® does not have an injury to internal organs, does not lead to changes in haematological and biochemical parameters, no immunotoksicheskim, teratogenic effects, showed no mutagenic properties.

Noopept ® released in pharmacies without a prescription.

nstructions for use

Registration Number: LS-001577 dated 12.05.2006

Commercial product name: Noopept ®

Rational Chemical name: ethyl ether N-fenilatsetil-L-¬ prolilglitsina.

Drug form: tablets.

Composition
Each tablet contains:
Active substance: noopept ® - 10 mg.
Excipients: microcrystalline cellulose, lactose (milk sugar), potato starch, povidon, magnesium stearate.

Description
Tablets are white, with beveled ploskotsilindricheskie.
Pharmacotherapy group: nootropnoe tool. ID ATH: [N 06 BX].

Pharmacological Effects
Noopept ® is nootropnym drug with nootropnym and neuroprotective properties. Improves learning ability, memory, working on all phases of processing: the primary information processing, consolidation, retrieval. Prevents the development of amnesia caused by electroshock, a blockade of central cholinergic structures glyutamatergicheskih receptor systems ironic phase of sleep deprivation.
Neuroprotective (protective) effect Noopepta ® appears to improve the stability of brain tissue to the damaging effects (trauma, hypoxia, Electro, toxic) and alleviating the degree of damage to brain neurons. The drug reduces the amount of focus on tromboticheskoy models of stroke and prevents the loss of neurons in tissue culture cortex and cerebellum, expose neurotoxic concentrations glyutamata, free radical oxygen.
Noopept ® has antioxidant effects, antagonistic effects on the effects of excess calcium, improves the rheological properties of blood, with antiagregatsionnymi, fibrinolytic, antikoagulyantnymi properties.
Nootropny effect of the drug associated with the formation of tsikloprolilglitsina, similar to the structure of endogenous cyclic dipeptidu having antiamnesticheskoy activity, as well as to the availability holinopozitivnogo action.
Noopept ® transkallozalnogo increases the amplitude of the response, making associations between the cerebral hemispheres at the level of cortical structures.
Noopept ® helps to restore memory and other cognitive functions, disturbed by the damaging effects - brain injury, local and global ischemia, prenatal damage (alcohol, hypoxia).
Therapeutic effect of the drug in patients with organic disorders of central nervous system manifests itself, beginning with 5-7 days of treatment. Initially implemented in the spectrum of activity Noopepta ® anxiolytic and easy stimulatory effects, manifested in the reduction or disappearance of anxiety, increased irritability, affective lability, sleep disturbance. After 14-20 days of treatment revealed the positive impact of the drug on cognitive function, the parameters of attention and memory.
Noopept ® has vegetonormalizuyuschim effect helps to reduce headaches, orthostatic violations tachycardia.
® Noopept not cumulative in the body, does not cause drug dependence. With the lifting of the drug is not the abolition of the syndrome.
Noopept ® does not have an injury to internal organs, does not lead to changes in haematological and biochemical parameters, no immunotoksicheskim, teratogenic effects, showed no mutagenic properties.

Pharmacokinetics
Noopept ®, absorbing into the gastrointestinal tract, in the unaltered system enters the bloodstream, cross the barrier gematoentsefalichesky determined in the brain in high concentrations than in blood. Time to achieve maximum concentration in an average of 15 minutes. The half of the blood plasma - 0.38 h. The drug partially preserved unchanged, partly metabolized to form phenylacetic acid and fenilatsetilprolina tsikloprolilglitsina. It has a high relative bioavailability (99.7%).

Indications for use
Memory, attention and other cognitive functions, and emotionally labile disorder, including those in patients with advanced age, with
• consequences of craniocerebral trauma
• postkommotsionnom syndrome,
• cerebral vascular insufficiency (encephalopathy of different genesis)
• asthenic disorders,
• other states to reduce the signs of intellectual productivity

Contraindications
Pregnancy, lactation period. Age 18 years. Individual intolerance drug. Expressed violations liver and kidneys.

Dosing and Administration
Noopept ® is used inside, after the meal. Treatment begins with application of the drug at a dose of 20 mg, 10 mg distributed in two steps during the day (morning and afternoon). With the lack of effective therapies, and with good portability Noopepta ® drug dose increase to 30 mg (see «Cautions»), distributed to 10 mg for three reception during the day. Do not take the drug later than 18 hours. Running a course of treatment is 1.5 - 3 months. Repeat treatment if necessary, can be carried out after 1 month.

Adverse effects
Possible allergic reactions. In patients with arterial hypertension, mostly severe, against the backdrop of taking the medication may be a rise of blood pressure.

Overdosage
Specific manifestations of overdose has not been determined.

Interaction with other drugs
Unknown Noopepta ® interaction with alcohol, hypnotic and hypotensive drugs means and psihostimuliruyuschego action.

Cautions
If necessary, increase the dose (30 mg / day), with long-term use, and while the use of other drugs, the appearance of adverse reactions or deterioration of the state should call a doctor.

Composition
According to 25 tablets in contour yacheykovoy pack of PVC film and aluminum foil printed varnished.
At 30 or 50 tablets in the banks of polymer with controlled opening.
Bank One or 2 contour yacheykovye packaging along with instructions for use in the stack of cardboard.

Storage conditions
List B. In dry, protected from light, at a temperature no higher than 25 0С.
Keep out of the reach of children.

Shelf life
2 years. Do not use a later date on the package.

Terms of leave from pharmacies
Without prescription.

Manufacturer:
CJSC «Masterklon», Moscow, tel. (495) 781-10-86
produced CJSC «Pharmaceutical Firm« Lecca », Russia.
601125, Vladimir Region., Petushinsky rn, pos. Volginsky,
tel. / fax (49243) 71-5-52.

Claims consumer guide to the JSC «Pharmaceutical Firm« Lecca »: 601125, Vladimir Region., Petushinsky rn, pos. Volginsky, tel. / fax (49243) 71-5-52.

FAQ

Can I take Noopept together other psychotropic drugs?
Noopept no drug interactions and is compatible with other drugs of central action.



The chemical name of active ingredient is glycine. What are the differences of the drug product Noopept glycine, than it better?
Noopept has a peptide structure - composed of amino acids and, together with glycine in Noopepta includes amino acid proline, together they constitute the human body connect tsikloprolilglitsin who has expressed an impact on memory function. Also Noopept unlike glycine has vegetonormalizuyuschim effect (helps to reduce headaches, orthostatic violations tachycardia) and was adopted orally, while the glycine in the intestine to digest and is not absorbed.



Can Noopept to raise arterial blood pressure?
When you receive Noopepta patients with arterial hypertension, mostly III degree, and with inadequate reception facilities may experience hypotensive and rising blood pressure.



Can Noopept cause headaches?
Noopept has vegetonormalizuyuschim action that leads to a reduction in headache arising from autonomic dysfunction.



At what cognitive functions operate Noopept?
Application Noopepta improves cognitive functions such as memory, speech, Gnosis (perception and information processing), Praxis (use of motor skills).



How often can I repeat a course of treatment Noopeptom?
Duration Noopepta receive depends on the nature of the disease, is usually recommended course 1,5-3 months, which can be repeated after one month break.



Can Noopept taken concurrently with alcohol if necessary?
The use of alcohol does not affect the metabolism and effects Noopepta in the body, however, the neuroprotective properties Noopepta increase the stability of brain tissue to the damaging effect of toxic substances, including alcohol.



Can Noopept applied to vegeto-vascular dystonia?
Noopept has vegetonormalizuyuschim effect helps to reduce headaches, orthostatic violations tachycardia and can be used with memory impairment in patients with vegetovascular vascular dystonia.



What is the neuroprotective effect Noopepta?
Neuroprotective (protective) effect Noopepta appears to increase the stability of brain tissue to the damaging effects (trauma, hypoxia, Electro, toxicity, etc.) and reducing the damage to neurons of the brain.



Can I use Noopept children to improve learning?
Noopept registered for use in people older than 18 years, given the low level of toxicity is scheduled to conduct several studies, which would enable to register Noopept children.



Is the use of the drug in pregnancy or in lactation period?
In the experimental data set lack Noopepta teratogenic, mutagenic and immunotoksicheskih properties. However Noopept not studied in women during pregnancy and lactation period, so it does not appear to apply in these cases.



Can I use Noopept human health, to improve the intellectual activity?
Noopept registered for OTC and leave freely allowed in pharmacies, so can be used and healthy people to enhance cognitive function (especially memory), with loads and in critical situations, for example, during sessions, exams, tests, after the holidays to improve efficiency.



Can I apply Noopept, after a mixed stroke, and if you have epileptic attacks?
Noopept is indicated for the treatment of cerebral vascular insufficiency, including the patients after the forward stroke. Data on the adverse impact on the course of epilepsy Noopepta lacking and the existing clinical experience of its good tolerance and efficacy in these patients.



You can get used to Noopeptu, if it take long?
The study found that Noopept does not cause drug dependence (it can not be used) and the syndrome cancel (you can stop taking at any time).



Can Noopept if I have meteopatiya?
You can use Noopept to improve memory, reduce anxiety, improve sleep and normalize the body's resilience to external factors that can reduce the manifestations meteopatii and better portability meteorological changes your body.

[skinniest200]

For anybody that has just got their Noopept, did you guys get it from pharmacy1010 ? If so could you tell me what day you guys placed your orders and when it arrived, I ordered some about 2 weeks ago and am wondering when to expect it. I tried the stuff from TLR without much luck, but I'm a non-responder or have high tolerances to a lot of stuff, so I'm not sure if it was the product or just me. I'll probably be trying a higher and longer dosage plan this time, maybe around 50mg/day, and trying to use up the TLR stuff I have as a pre-loading, in hopes of eventually getting some effect out of the stuff.

[Ben]

Any news from you noopept takers? Have you guys noticed anything different?

[jackinbox]

For anybody that has just got their Noopept, did you guys get it from pharmacy1010 ? If so could you tell me what day you guys placed your orders and when it arrived, I ordered some about 2 weeks ago and am wondering when to expect it. I tried the stuff from TLR without much luck, but I'm a non-responder or have high tolerances to a lot of stuff, so I'm not sure if it was the product or just me. I'll probably be trying a higher and longer dosage plan this time, maybe around 50mg/day, and trying to use up the TLR stuff I have as a pre-loading, in hopes of eventually getting some effect out of the stuff.

It took less than 3 weeks to receive it from pharmacy1010. I ordered Semax 1% but the sent the 0.1% solution but the noopept is what I ordered.

Edited by jackinbox, 10 May 2009 - 04:40 PM.