Noopept (GVS-111) is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.IC50 Value:Target: 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 mikroM), while the competition of noopept for these receptor binding sites was lower by an order of magnitude (IC50 = 80 +/- 5.6 mikroM) . GVS-111 significantly increased neuronal survival after H(2)O(2)-treatment displaying a dose-dependent neuroprotective activity from 10 nM to 100 mikroM, and an IC(50) value of 1.21+/-0.07 mikroM. GVS-111 inhibited the accumulation of intracellular free radicals and lipid peroxidation damage in neurons treated with H(2)O(2) or FeSO(4), wat 'n antioksidant meganisme van werking .in vivo voorstel: N-Fenielasetiel-L-prolylglisien etielester (GVS-111) intraveneus toegedien teen 'n dosis van 0.5 mg/kg/dag, vir die eerste keer 1 h na isgemiese letsel en dan vir 9 na-operatiewe dae, met die laaste administrasie 15 min voor toetsing, die tekort verminder het. GVS-111 self is nie in rotbrein gevind nie 1 h na 5 mg/kg i.p. administrasie tot die limiet van opsporing (LOD) onder hoë werkverrigting vloeistofchromatografie (HPLC) voorwaardes. Die mees uitgesproke anti-inflammatoriese effek van dipeptied is waargeneem op die model van adjuvante artritis by rotte, waar die middel toegedien word 25 dae in 'n daaglikse dosis van 0.5 mg/kg (i.m.) of 5 mg/kg (na.) die chroniese immuunontsteking aansienlik verminder (op die 12de dag, deur 94.0 en 74.1%, onderskeidelik) .Toksisiteit: 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
