Half elimination time was 22.05±14.37 min
That would be the half-life of noopept, but I'm not sure the actual drug half-life corresponds to the duration of effects in this case. It looks more like noopept is a pro-drug for cyclo-L-prolylglycine.
This cyclic dipeptide, possessing pronounced antiamnestic activity, was determined in blood plasma of rats up to 5-6 hours after noopept administration. It possible to suppose that not only the parent molecule of noopept, but its metabolite also contribute to clinical effects of this systemically active dipeptide.
Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):245-52.
The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine.
Gudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, Rozantsev GG, Skoldinov AP, Zherdev VP, Seredenin SB.
Institute of Pharmacology, Russian Academy of Medical Science, Moscow, Russia.
The metabolism of a new piracetam analogue, the dipeptide cognitive enhancer N-phenylacetyl-L-prolylglycine ethyl ester (GVS-111) was studied in vivo. GVS-111 itself was not found in rat brain 1 h after 5 mg/kg i.p. administration up to limit of detection (LOD) under high performance liquid chromatography (HPLC) conditions. Three substances corresponding to the three possible GVS-111 metabolites, namely phenylacetic acid, prolylglycine and cyclo-prolylglycine, were found in experimental rat brain samples as well as in controls using HPLC, gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) methods. Only cyclo-prolylglycine concentration increased (2.5-fold) 1 h after GVS-111 administration. Cyclo-prolylglycine formation from GVS-111 in the presence of plasma and brain enzymes was shown in vitro. These data could be considered as evidence that GVS-111 is prodrug which converts in the body to cyclo-prolylglycine, and which is identical to the endogenous cyclopeptide that produces the nootropic activity.
PMID: 9358206 [PubMed - indexed for MEDLINE]
GVS-111 is another name for noopept. From these studies, and the fact that a drug that works for less than an hour would be rather useless and not worth persuing into clinical trials, I'm thinking the half-life of cyclo-L-prolylglycine would be closer to matching the actual duration of effects.
theraputic dosage range was effective at doses as low as .01mg/kg (and that was for patients with AD too!)
Would you have a link to that study? I think I've seen .1mg/kg listed in some studies, but they weren't even on humans.
I thought that thinking of new ways to increase its length of efficacy wouldn't be a bad idea (you can get up to about 80% absorption even with commercially available trandermal delivery systems).
You wouldn't actually be getting longer duration per amount used unless the ceiling for effects was reached well below the standard 5-10mg and the extra was being wasted. Even then it would probably be cheaper and easier to just make some more noopept than to mess with the transdermal route.
From
http://translate.goo...l=e...l=en&sa=GSintez PBS-111 is not only easy because of the lack of chiral center in the glycine and low proline residue danger of racemization, but also inexpensive because low cost of starting compounds - proline, glycine, and phenylacetic acid, especially the last two.
So who know's how to cook? Let's mix us up a batch
!
I have some noopept on order from TLR so we'll figure out the actual duration of action in a few days. I've only seen one experience report on the stuff and they said 10-15mg twice a day was effective, and I'm assuming they mean for all day effects. I'll post a link or copy if anybody's interested.
