Contrasting effects of estradiol and 17 beta-aminoestrogens on blood clotting time in rats and mice.

Eur J Pharmacol

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.

Published: March 2005

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.

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http://dx.doi.org/10.1016/j.ejphar.2005.01.027DOI Listing

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