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Information × Registration Number 0215U003390, 0110U005971 , R & D reports Title Calixarens as high affinity and selectivity supramolecular effectors of ATP-dependent smooth muscle proteins. popup.stage_title Head Kosterin Sergiy Oleksijovych, Registration Date 28-01-2015 Organization A.V.Palladin Institute of Biochemistry of National Academy of Sciences popup.description2 Plasma membrane Ca2+,Mg2+-ATPase is an important element of general myometrium tonus control mechanism, which also makes a contribution to muscle tension relaxation after its contraction. Expiriments were done on the myometrial cell plasma membrane suspension, which was treated with 0.1% digitonin solution. The authors have investigated the inhibitory action of calix[4]arene C-90 (5,11,17,23-tetra(trifluor)methyl(phenylsulphonylimino)-methylamino-25,26,27,28-tetra propoxi-calix[4]arene) on the Ca2+,Mg2+-ATPase activity (the magnitude of І0.5 was 20.2 ± 0.5 mkM). The inhibitory action of calix[4]arene C-90 on the activity of Ca2+, Mg2+-ATPase is explained as cooperative action of four trifluormethyl(phenylsulfonylimino)methylamino groups that are spatially oriented on the calix[4]-arene base rather than with the action of tetraphenol macrocycle or separate pharmacophore sulphonilamidin groups. Considering established kinetic pattern of calix[4]arene C-90 inhibitory action on the plasma membrane Ca2+,Mg2+-TPaseactivity, stationary kinetical model of basal calcium concentration control in unexcited uterus myocytes was developed. It is assumed that obtained results may be promising for creation of new generation ("supramolecular") pharmacological agent - uterus basal tonus stimulator - on the base of calix[4]arene C-90. Product Description popup.authors Бабіч Лідія Григорівна Бевза Олександр Васильович Векліч Тетяна Олександрівна Данилович Ганна Вікторівна Данилович Юрій Володимирович Лабинцева Раїса Дмитрівна Шкрабак Олександр Анатолійович Шликов Сергій Георгійович popup.nrat_date 2020-04-02 Close