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产品价格:电议      采购度:1606      原产地:美洲
发布时间:2021/7/24 5:24:30 所属地区:上海 上海市
简要描述:
Omberacetam (GVS-111) 是可作为膳食补充剂的多肽。
标签:GVS-111
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CAS No. : 157115-85-0
MCE 站:Omberacetam
产品活性:Omberacetam (GVS-111) 是可作为膳食补充剂的多肽。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:iGluR
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) [1]. 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 [2].
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 [3]. 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 [4]. 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) [5].
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更新时间:2024/1/2 10:14:41
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