Kinetic regularities of calixarene C-90 action on the myometrial plasma membrane Ca(2+),Mg(2+)-ATPase activity and on the Ca(2+) concentration in unexcited сells of the myometrium

摘要

Plasma membrane Casup2+/sup,Mgsup2+/sup-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 Casup2+/sup,Mgsup2+/sup-ATPase activity (the magnitude of ? sub0.5/sub was 20.2 ± 0.5 mkM). The inhibitory action of calix[4]arene C-90 on the activity of Casup2+/sup,Mgsup2+/sup-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 Casup2+/sup,Mgsup2+/sup-ATPase activity, 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.