The Memory Enhancer “Noopept”

Hello,

If you are looking for something which will improve your memory as well as increase your cognitive perception, there is a little known dipeptide known as “Noopept” which is derived from the nootropic (smart drug) known as “Piracetam”. Piracetam is derived from the amino acid “GABA” and is structurally similar to an important cerebrospinal fluid amino acid known as “pyroglutamate”: http://optimalhealth.cia.com.au/pyroglutamate.html. I have used it and found it to seem to bring back a feeling of natural youthful brain function much more so than for instance the synthetic form of the hormone Vasopressin known as “Desmopressin”, although Desmopressin has a significant degree of efficacy itself.

Below I’ve copied for you some information which I have gleaned from the “Immortality Institute’s” website.

1) Scientific Study Results:

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.

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[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.

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pdf of actual study: http://www.scribd.com/doc/14430524/Prevents-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.

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pdf of actual study: http://www.scribd.com/doc/14430637/cycloprolylglycine

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.

2) Usage and Instructions (translated from Russian):

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.

2) Instructions 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.

3) 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.

 

 

 

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