Calcium antagonistic effect of 17 alpha-estradiol derivatives: in vitro examinations.
The calcium antagonistic effect of 17 alpha-estradiol derivatives was investigated in vitro in human aortic smooth muscle cells. The substances tested were 17 alpha-estradiol, 17 alpha-ethinylestradiol, the scavestrogens J811 and J861, and 17 beta-estradiol. Examinations were carried out by measuring 45Ca influx into the cells. All compounds showed a significant inhibition of calcium influx at the concentration of 10(-6) M. The strongest effect could be registered for the scavestrogens. Since these substances are virtually devoid of estrogenic activity, they may offer advantages over 17 beta-estradiol in the therapy and prevention of cardiovascular disease.
Seeger
H
H
Department of Obstetrics and Gynecology, University of Tuebingen, Germany.
Mueck
A O
AO
Oettel
M
M
Schwarz
S
S
Lippert
T H
TH
D000975:Antioxidants / Q000494:pharmacology; D001011:Aorta; D002118:Calcium / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D002132:Calcium Radioisotopes / Q000378:metabolism; D004958:Estradiol / Q000494:pharmacology*; D004997:Ethinyl Estradiol / Q000494:pharmacology; D016166:Free Radical Scavengers / Q000494:pharmacology; D006801:Humans; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism*
D000975:Antioxidants; D002132:Calcium Radioisotopes; D016166:Free Radical Scavengers; C115406:J811 scavestrogen; C115405:J861 scavestrogen; D004997:Ethinyl Estradiol; D004958:Estradiol; D002118:Calcium