Contrasting effects of estradiol and 17 beta-aminoestrogens on blood clotting time in rats and mice.
Estrogens have been associated with thromboembolic events. Our group has described the anticoagulant effect of 17 beta-aminoestrogens in rodents, potentially new alternative estrogenic agents without thrombogenic risk. This work compares the contrasting effects of estradiol and the 17 beta-aminoestrogens (prolame, butolame, and pentolame) on blood clotting time. Ovariectomized CD1 mice received a single injection of 17beta-aminoestrogens, estradiol (20 to 80 mg/kg), or vehicle. Estradiol decreased blood clotting time from -10% to -25% (48 h; P<0.01) and 17 beta-aminoestrogens increased it, differing in latency (approximately 12 h; +48%, P<0.01) and duration (approximately 72 h +58%, P<0.01). In male Wistar rats, similar effects (pentolame +45%; estradiol -31%; P<0.01) were observed 48 h after five consecutive daily injections of 1000 microg/animal/day. The maximum procoagulant effect of estradiol was obtained after 72 h with 10 microg/animal/day (-45%; P<0.01). 17 Beta-aminoestrogens always produced opposite effects to those of estradiol on blood coagulation.
Lemini
Cristina
C
Departamento de Farmacología, Facultad de Medicina, Edificio D, 1er Piso, Universidad Nacional Autónoma de México, Ciudad Universitaria, México, D.F., C.P. 04510, Apdo. Postal 70-297, Mexico. clemini@servidor.unam.mx
Franco
Yanira
Y
Avila
Ma Estela
ME
Jaimez
Ruth
R
D000605:Amino Alcohols / Q000494:pharmacology; D000818:Animals; D001777:Blood Coagulation / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000008:administration & dosage / Q000494:pharmacology*; D045166:Estradiol Congeners / Q000008:administration & dosage / Q000494:pharmacology*; D004963:Estrenes / Q000008:administration & dosage / Q000494:pharmacology; D005260:Female; D008297:Male; D051379:Mice; D010052:Ovariectomy; D051381:Rats; D017208:Rats, Wistar
D000605:Amino Alcohols; D045166:Estradiol Congeners; D004963:Estrenes; C083219:butolame; C083220:pentolame; D004958:Estradiol; C047867:prolame