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Information × Registration Number 0214U005367, 0110U006066 , R & D reports Title Nanoparticles from biodegradable polymers as macromolecular carriers for transportation of potent neuroprotective drugs to central nervous system popup.stage_title Head Vovk Mykhailo Volodymyrovych, Registration Date 18-12-2014 Organization Institute of Organic Chemistry National Academy of Sciences of the Ukraine popup.description2 Molecular design, synthesis and bioactivity testing of new benzothiazole and coumarin derivatives have been conducted. Selective and efficient blockers of receptor-ionophore complex ASIC1a possessing a record half-inhibition value of this ion channel current (IC50=14 nM) have been found. The resulting compounds are proposed as a structural motif for a new generation of highly effective anti-ischemic agents for the treatment of several neurodegenerative diseases of the central nervous system, including ischemic stroke and multiple sclerosis. The advantage of neuroprotective drugs based on ASIC1a antagonists is the possibility of their use for a few hours after the onset of ischemic injury. Using an in vitro model of ischemic stroke it has been shown that the oxygen-glucose deprivation of rat hippocampus slices at prolonged cultivation in the presence of 100 nM ASIC1a blocker reduces the number of dead cells by 51%. On the basis of the developed lead-compounds several salts with palmitic acid have been synthesized, which became the starting substrates for obtaining of solid lipid nanoparticles modified by surfactant polysorbate 80. It has demonstrated that the nanosized solid lipid conjugates can be an effective method for active neuroprotective agents delivery to the central nervous system. Synthesized ASIC1a antagonists have also been used for experimental proof of the essential role of pH-sensitive ion channels in the long-term potentiation, thus supporting the involvement of these receptors in the fundamental process of memory formation and learning. Product Description popup.authors Больбут Андрій Вікторович Васькевич Алла Іржіївна Васькевич Руслан Іванович Вовк Михайло Володимирович Головач Наталія Михайлівна Денисенко Ольга Миколаївна Дехтяр Марина Львівна Зборовський Юрій Леонідович Кемський Сергій Володимирович Мельниченко Ніна Володимирівна Орисик Віктор Васильович Станінець Василь Іванович Сукач Володимир Андрійович Ткачук Віктор Миколайович Чубарук Наталія Григорівна Шоба Вероніка Михайлівна popup.nrat_date 2020-04-02 Close