Gonadotrophin Inhibiting and Anti-Fecundity Effects of Chloramiphene.

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Abstract
Chloramiphene (l-[p-[beta]-diethylaminoethoxy) phenyl]-l,2-diphenyl-2-chloroethylene) is a pituitary gonadotrophin inhibitor. In immature litter-mate female parabiotic rats (1 castrate: 1 intact) 01 mg/kg/day inhibited ovarian weight gain by 50%. Larger doses (0.3 to 10.0 mg/kg/day) yielded greater inhibition with a plateau of response of approximately 80% (3 to 5 parabiotic pairs per dose level). It was equally active by the oral and subcutaneous routes. Doses of 0.1 mg/kg/day and greater interrupted the estrous cycles of young, mature female rats (4 to 7 per group). Subcutaneous treatment at 0.3 mg/kg/day during cohabitation breeding produced a loss in fecundity which was reversible after cessation of treatment. Pituitaries of rats treated with chloramiphene at 1 mg/kg/day x 20 days had approximately the same weight and gonadotrophin content as control rats. Chloramiphene at 3 mg/kg/day did not inhibit exogenously administered gonadotrophin.

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