|NoopeptNootropic and neuroprotective agent|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||157115-85-0||SDF||Download SDF|
|Synonyms||GVS-111;GVS111;GVS 111;SGS-111;SGS 111;SGS111|
|Chemical Name||ethyl 2-(1-(2-phenylacetyl)pyrrolidine-2-carboxamido)acetate|
|Solubility||25℃: DMSO||Storage||Store at -20°C|
Description: IC50 Value: N/A Noopept (GVS-111) is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic. in vitro: Nooglutil exhibits pharmacologically significant competition with a selective agonist of AMPA receptors ([G-3H]Ro 48-8587) for the receptor binding sites (with IC50 = 6.4 +/- 0.2 microM), while the competition of noopept for these receptor binding sites was lower by an order of magnitude (IC50 = 80 +/- 5.6 microM) . GVS-111 significantly increased neuronal survival after H(2)O(2)-treatment displaying a dose-dependent neuroprotective activity from 10 nM to 100 microM, and an IC(50) value of 1.21+/-0.07 microM. GVS-111 inhibited the accumulation of intracellular free radicals and lipid peroxidation damage in neurons treated with H(2)O(2) or FeSO(4), suggesting an antioxidant mechanism of action . in vivo: N-Phenylacetyl-L-prolylglycine ethyl ester (GVS-111) administered intravenously at a dose of 0.5 mg/kg/day, for the first time 1 h after ischaemic lesion and then for 9 post-operative days, with the last administration 15 min before testing, attenuated the deficit . 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 . The most pronounced antiinflammatory effect of dipeptide was observed on the model of adjuvant arthritis in rats, where the drug administered over 25 days in a daily dose of 0.5 mg/kg (i.m.) or 5 mg/kg (p.o.) significantly reduced the chronic immune inflammation (on the 12th day, by 94.0 and 74.1%, respectively) . Toxicity: Noopept administered in this dose range induced no irreversible pathologic changes in the organs and systems studied and exhibited no allergenic, immunotoxic, and mutagen activity . Clinical trial: Discontinued