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Using enzymatic assay and kinetic analysis, we demonstrated that 100 μM calix[4]arene c-956 (5,11,17,23-tetra(trifluoro)methyl-(phenylsulfonylimino) methylamino-25,27-dioctyloxy-26,28-dipropoxycalix[4]arene) had the most significant inhibitory effect on the plasma membrane Са2+,Mg2+-АТРase activity compared to effects of other calix[4]arenes, and had no effect on specific activities of other membrane AtPases . Using confocal microscopy and fluorescent probe fluo-4, we observed an increase of the intracellular level of ca2+ after application of calix[4]arene c-956 to immobilized myocytes. Analysis of the effect of calix[4]arene c-956 on the hydrodynamic diameter of myocytes demonstrated that application of calix[4]arene c-956 solution decreased this parameter by 45.5 ± 9.4% compared to control value that was similar to the action of uterotonic drug oxytocin.

Calix[4]arene С-956 selectively inhibits plasma membrane Са(2+),M(2+)-АТРase in myometrial cells