Nefiracetam - CAS 77191-36-7
Catalog number: B0084-076916
Category: Inhibitor
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GABA Receptor
Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions.
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B0084-076916 1 g $398 In stock
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1.Molecular dynamics study-based mechanism of nefiracetam-induced NMDA receptor potentiation.
Omotuyi OI1, Ueda H2. Comput Biol Chem. 2015 Apr;55:14-22. doi: 10.1016/j.compbiolchem.2015.01.004. Epub 2015 Jan 23.
Plastic changes in the brain required for memory formation and long-term learning are dependent on N-methyl-d-aspartic acid (NMDA) receptor signaling. Nefiracetam reportedly boosts NMDA receptor functions as a basis for its nootropic properties. Previous studies suggest that nefiracetam potentiates the NMDA receptor activation, as a more potent co-agonist for glycine binding site than glycine, though the underlying mechanisms remain elusive. Here, using BSP-SLIM method, a novel binding site within the core of spiral β-strands-1-5 of LBD-GLUN1 has been predicted in glycine-bound GLUN1 conformation in addition to the glycine pocket in Apo-GLUN1. Within the core of spiral β-strands-1-5 of LBD-GLUN1 pocket, all-atom molecular dynamics simulation revealed that nefiracetam disrupts Arg523-glycine-Asp732 interaction resulting in open GLUN1 conformation and ultimate diffusion of glycine out of the clamshell cleft. Open GLUN1 conformation coerces other intra-chain domains and proximal inter-chain domains to sample inactivate conformations resulting in closure of the transmembrane gate via a novel gauche trap on threonine 647 (chi-1 dihedral (χ1)=-45° instead of +45°).
2.Apathy following stroke.
Jorge RE1, Starkstein SE, Robinson RG. Can J Psychiatry. 2010 Jun;55(6):350-4.
OBJECTIVE: We will review the available evidence on the frequency, clinical correlates, mechanism, and treatment of apathy following stroke.
3.Chromatographic behaviour predicts the ability of potential nootropics to permeate the blood-brain barrier.
Farsa O1. Sci Pharm. 2013 Mar;81(1):81-91. doi: 10.3797/scipharm.1208-19. Epub 2012 Oct 14.
The log BB parameter is the logarithm of the ratio of a compound's equilibrium concentrations in the brain tissue versus the blood plasma. This parameter is a useful descriptor in assessing the ability of a compound to permeate the blood-brain barrier. The aim of this study was to develop a Hansch-type linear regression QSAR model that correlates the parameter log BB and the retention time of drugs and other organic compounds on a reversed-phase HPLC containing an embedded amide moiety. The retention time was expressed by the capacity factor log k'. The second aim was to estimate the brain's absorption of 2-(azacycloalkyl)acetamidophenoxyacetic acids, which are analogues of piracetam, nefiracetam, and meclofenoxate. Notably, these acids may be novel nootropics. Two simple regression models that relate log BB and log k' were developed from an assay performed using a reversed-phase HPLC that contained an embedded amide moiety. Both the quadratic and linear models yielded statistical parameters comparable to previously published models of log BB dependence on various structural characteristics.
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CAS 77191-36-7 Nefiracetam

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