Agonistic and Antagonistic Effects of Clomiphene Citrate and Its Isomers

摘要: The agonistic and antagonistic properties of clomiphene citrate (CL) its isomers were examined in the rat uterus. Immature rats (21 days old) injected with various doses estradiol benzoate (EB), CL, zuclomiphene (ZUC, cia isomer), enclomiphene (ENC, trans uterine weight or epithelial cell height was measured. EB treatment produced a typical doseresponse curve for steep slope, while curves resulting from ZUC, ENC attenuated very shallow slope. These differences shapes dose-response render determination relative potency estimates inaccurate misleading. In contrast, hypertrophy similarforallfour compounds. more potent than any form clomiphene;however,the maximum extent cellular not as great. half maximal dose each compound EB, 0.35 ± 0.04 Mg; ENC, 25.0 2.0 35.0 3.1 65.0 7.1 ug. ability these drugs to antagonize action by injecting plus measuring 72 h later. All three forms drug EB-induced gain over same ranges which they themselves. No effects observed on stimulation hypertrophy. data show that CL are fully capable stimulating uterus, thus, valid can be obtained this response. This is true when used because differential taken into account. addition, used; however, no antagonism estrogen-stimulated Therefore, broad generalizations concerning estrogenicity antiestrogenicity compounds warranted made only specific endpoints evaluated.