Calcium antagonistic effect of 17 alpha-estradiol derivatives: in vitro examinations

The calcium antagonistic effect of 17 alpha-estradiol derivatives was inves tigated in vitro in human aortic smooth muscle cells. The substances tested were 17 alpha-estradiol, 17 alpha-ethinylestardiol, the scavestrogens J811 and J861, and 17 beta-estradiol. Examinations were carried out by measurin g Ca-45 influx into the cells. All compounds showed a significant inhibitio n of calcium influx at the concentration of 10(-6) M. The strongest effect could be registered for the scavestrogens. Since these substances are virtu ally devoid of estrogenic actitivity, they may offer advantages over 17 bet a-estradiol in the therapy and prevention of cardiovascular disease.