RESUMO
The syntheses and characterizations of two new 17 beta-aminoestrogens, butolame [17 beta-(4-hydroxy-1-butylamino)-1,3,5(10)-estratrien-3-ol] and pentolame [17 beta-(5-hydroxy-1-pentylamino)-1,3,5(10)-estratrien-3-ol], are presented. Both compounds, when administered in single subcutaneous injections to male mice and rats, produce dose-dependent increases in blood clotting times that may last several days. The estrogenic effects assessed by the vaginal cornification test are of relatively short duration.
Assuntos
Amino Álcoois/síntese química , Anticoagulantes/síntese química , Congêneres do Estradiol/síntese química , Estrenos/síntese química , Amino Álcoois/administração & dosagem , Amino Álcoois/farmacologia , Animais , Anticoagulantes/farmacologia , Coagulação Sanguínea/efeitos dos fármacos , Congêneres do Estradiol/farmacologia , Estrenos/administração & dosagem , Estrenos/farmacologia , Feminino , Cinética , Masculino , Camundongos , Ovariectomia , Ratos , Ratos Wistar , Vagina/efeitos dos fármacos , Vagina/fisiologiaAssuntos
Anisóis/farmacologia , Anticoagulantes/farmacologia , Derivados de Alilbenzenos , Animais , Anisóis/administração & dosagem , Anticoagulantes/administração & dosagem , Coagulação Sanguínea/efeitos dos fármacos , Relação Dose-Resposta a Droga , Injeções Subcutâneas , Masculino , Camundongos , Ratos , Ratos Endogâmicos , Varfarina/farmacologiaRESUMO
The anticoagulant and estrogenic effects of hexolame, N-(3-hydroxy-1,3,5(10)-estratrien-17 beta-yl)-6-hydroxyhexylamine, are described. A single subcutaneous injection of hexolame in adult and infant male mice produced dose-dependent increases in blood clotting time which could be observed even after 2 days. In ovariectomized mice, hexolame produced vaginal cornification (estrogenic response). The data suggested that if used in the treatment of prostatic cancer, hexolame, like prolame, would not induce cardiovascular accidents. It could also be useful in the prevention of thrombosis.
Assuntos
Amino Álcoois/farmacologia , Anticoagulantes , Estrenos/farmacologia , Animais , Animais Recém-Nascidos , Relação Dose-Resposta a Droga , Estrogênios/farmacologia , Feminino , Masculino , Camundongos , Trombose/prevenção & controle , Doenças Vaginais/tratamento farmacológico , Tempo de Coagulação do Sangue TotalRESUMO
The anticoagulant and estrogenic effects of prolame, N-(3-hydroxy-1,3,5(10)-estratrien-17 beta-yl)-3-hydroxypropylamine, are described. A single subcutaneous injection of prolame in male mice, ovariectomized mice, adult and infant male rats, produced dose-dependent increases of blood clotting time, which could be observed with the larger doses even after 4 days. In ovariectomized mice, prolame produced vaginal cornifications of shorter duration than those produced by estradiol-17 beta. The evidence suggests that, in contrast with currently used estrogens, prolame would not generate cardiovascular accidents if used for the treatment of prostatic carcinoma; it could also be exceptionally effective for the prevention of thrombosis.