About: Synthesis and activity evaluation of NMDA receptor antagonists     Goto   Sponge   NotDistinct   Permalink

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  • N-Methyl-D-aspartate (NMDA) receptors play a critical positive role in synaptogenesis and synaptic plasticity, although they can also mediate excitotoxicity. Disproportions in the processes can lead to symptoms characteristic of severe diseases of nervous system such as Alzheimer's, Parkinson's, and Huntington's diseases which pose a grave and growing problem in general and for aging population in particular. Endogenous neurosteroid ligands selectively affect the NMDA receptors. We intend to synthesize and evaluate activity of some fluorinated and fluorescent analogues and derivatives with an anionic chain. Such compounds should be useful in the research of NMDA receptors and diagnosis or treatment neuro-degenerative diseases. (en)
  • Receptor pro kyselinu N-Methyl-D-asparagovou (NMDA) je klíčovým faktorem při synaptogenezi a plasticitě synapsí. Zároveň je mediátorem excitotoxicity. Disproporce uvedených procesů může vést k příznakům charakteristickým pro Alzheimrovu, Parkinsonovu a Huntingtonovu chorobu, které jsou vážným a narůstajícím problémem pro všechny, ale zejména pro stárnoucí populaci. Endogenní neurosteroidy selektivně působí na NMDA receptory. Syntetizujeme a ověříme aktivitu serie fluorovaných a fluorescenčních anologů a derivátů s anionickým řetězcem. Tyto sloučeniny jsou potřebné pro výzkum NMDA receptoru a případně i pro diagnostiku a medikaci neurodegenerativních chorob. (cs)
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  • Syntéza a ověření aktivity antagonistů NMDA receptoru (cs)
  • Synthesis and activity evaluation of NMDA receptor antagonists (en)
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  • steroids; NMDA receptor; fluorodeivatives fluorescence (en)
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